Pharmacology (Full Deck) Flashcards

1
Q

What is the frequency of emesis for an agent with a minimal emetic potential?

A

The frequency of emesis for an agent with this emetic potential is:
- <10%

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2
Q

What is the frequency of emesis for an agent with a low emetic potential?

A

The frequency of emesis for an agent with this emetic potential is:
- 10-30%

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3
Q

What is the frequency of emesis for an agent with a moderate emetic potential?

A

The frequency of emesis for an agent with this emetic potential is:
- 30-90%

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4
Q

What is the frequency of emesis for an agent with a high emetic potential?

A

The frequency of emesis for an agent with this emetic potential is:
- >90%

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5
Q

What drugs are in the anthracycline class?

A

Drugs in this class are:
- Daunorubicin
- Daunorubicin Liposomal
- Daunorubicin and Cytarabine Liposomal
- Doxorubicin
- Doxorubicin Liposomal
- Idarubicin
- Epirubicin
- Valrubicin

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6
Q

What is the brand name of Daunorubicin?

A

The brand name of this generic drug is:
- Daunomycin

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7
Q

What is the brand name of Daunorubicin Liposomal?

A

The brand name of this generic drug is:
- DaunoXome

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8
Q

What is the brand name of Daunorubicin and Cytarabine Liposomal?

A

The brand name of this generic drug is:
- Vyxeos

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9
Q

What is the brand name of Doxorubicin?

A

The brand name of this generic drug is:
- Adriamycin

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10
Q

What is the brand name of Doxorubicin Liposomal?

A

The brand name of this generic drug is:
- Doxil

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11
Q

What is the brand name of Idarubicin?

A

The brand name of this generic drug is:
- Idamycin

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12
Q

What is the brand name of Epirubicin?

A

The brand name of this generic drug is:
- Ellence

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13
Q

What is the brand name of Valrubicin?

A

The brand name of this generic drug is:
- Valstar

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14
Q

What is the generic of name of Daunomycin?

A

The generic name of this brand name drug is:
- Daunorubicin

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15
Q

What is the generic of name of DaunoXome?

A

The generic name of this brand name drug is:
- Daunorubicin Liposomal

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16
Q

What is the generic of name of Vyxeos?

A

The generic name of this brand name drug is:
- Daunorubicin and Cytarabine Liposomal

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17
Q

What is the generic of name of Adriamycin?

A

The generic name of this brand name drug is:
- Doxorubicin

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18
Q

What is the generic of name of Doxil?

A

The generic name of this brand name drug is:
- Doxorubicin Liposomal

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19
Q

What is the generic of name of Idamycin?

A

The generic name of this brand name drug is:
- Idarubicin

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20
Q

What is the generic of name of Ellence?

A

The generic name of this brand name drug is:
- Epirubicin

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21
Q

What is the generic of name of Valstar?

A

The generic name of this brand name drug is:
- Valrubicin

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22
Q

What is the class and MOA of Daunorubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

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23
Q

What is the class and MOA of Doxorubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

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24
Q

What is the class and MOA of Idarubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

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25
What is the class and MOA of Epirubicin?
This drug in the following class: - Anthracycline This drug's MOA is as follows: - Inhibits DNA and RNA synthesis via: - Intercalation (direct binding to DNA) - Inhibition of topoisomerase II (a repair enzyme) - Steric obstruction
26
What is the class and MOA of Valrubicin?
This drug in the following class: - Anthracycline This drug's MOA is as follows: - Inhibits DNA and RNA synthesis via: - Intercalation (direct binding to DNA) - Inhibition of topoisomerase II (a repair enzyme) - Steric obstruction
27
What is the emetic potential of Daunorubicin?
The emetic potential of this drug is: - Moderate
28
What is the emetic potential of Daunorubicin Liposomal?
The emetic potential of this drug is: - Low
29
What is the emetic potential of Daunorubicin and Cytarabine Liposomal?
The emetic potential of this drug is: - Moderate
30
What is the emetic potential of Doxorubicin?
The emetic potential of this drug is: - Moderate if <60 mg/m2 - High if >60 mg/m2
31
What is the emetic potential of Doxorubicin Liposomal?
The emetic potential of this drug is: - Low
32
What is the emetic potential of Idarubicin?
The emetic potential of this drug is: - Moderate
33
What is the emetic potential of Epirubicin?
The emetic potential of this drug is: - Moderate (pediatrics and adults) - High when used in combination with cyclophosphamide (adults)
34
What is the emetic potential of Valrubicin?
The emetic potential of this drug is: - Minimal
35
Describe the emetic potential of the Anthracycline class.
The emetic potential of this drug class is: - Mainly moderate (Daunorubicin, Doxorubicin (<60 mg/m2), Doxorubicin and Cytarabine, Idarubicin, Epirubicin) - High for Doxorucibin >60 mg/m2, and Epirubcin when used in combination with Cyclophosphamide (adults) - All the others are low (Daunorubicin Liposomal, Doxorubicin Liposomal) or minimal (Valrubicin)
36
What drugs in the Anthracycline class have a high emetic potential?
Drugs in the class with a high emetic potential are: - Doxorucibin >60 mg/m2 - Epirubcin when used in combination with Cyclophosphamide (adults)
37
What drugs in the Anthracycline class have a moderate emetic potential?
Drugs in the class with a moderate emetic potential are: - Daunorubicin - Doxorubicin (<60 mg/m2) - Doxorubicin and Cytarabine - Idarubicin - Epirubicin
38
What drugs in the Anthracycline class have a low emetic potential?
Drugs in the class with a low emetic potential are: - Daunorubicin Liposomal - Doxorubicin Liposomal
39
What drugs in the Anthracycline class have a minimal emetic potential?
Drugs in the class with a minimal emetic potential are: - Valrubicin
40
What are the main indications of Daunorubicin?
The main indications of this drug are: - ALL - AML - Kaposi sarcoma (Daunorubicin Liposomal)
41
What are the main indications of Daunorubicin Liposomal?
The main indications of this drug are: - Kaposi sarcoma
42
What are the main indications of Daunorubicin and Cytarabine Liposomal?
The main indications of this drug are: - AML
43
What are the main indications of Doxorubicin?
The main indications of this drug are: - AML - Bladder Cancer - Breast Cancer - Hodkin Lymphoma - Non-Hodkin Lymphoma - Osteosarcoma - Soft Tissue Sarcomas
44
What are the main indications of Doxorubicin Liposomal?
The main indications of this drug are: - Breast Cancer - Kasposi Sarcoma - Ovarian Cancer
45
What are the main indications of Idarubicin?
The main indications of this drug are: - AML
46
What are the main indications of Epirubicin?
The main indications of this drug are: - Breast Cancer - Bladder Cancer - Soft Tissue Sarcomas
47
What are the main indications of Valrubicin?
The main indications of this drug are: - Bladder Cancer
48
What are the main/common indications of the Anthracycline class?
The main/common indications of this drug class are: - Doxorubicin is the workhourse - AML - Bladder Cancer - Breast Cancer - Hodkin Lymphoma - Osteosarcoma - Soft Tissue Sarcomas
49
What are the notable/common monitoring parameters for the Anthracycline class?
The notable/common monitoring parameters for this drug class are: - Echocardiogram to assess left ventricular ejection fraction (LVEF) prior to start of therapy, repeat if S/Sx of HF - History and cardiac exam prior to every cycle
50
What drug(s) require cardiac surveillance and monitoring for heart failure?
Drug(s) requiring this monitoring are: - Anthracyclines
51
Describe the extravasation risk and management strategies for the Anthracycline class.
The extravasation risk and mangement strategies for this drug class are as follows: - All Anthracyclines are vesicants except for Valrubicin (intra-vesical) and liposomal products. - For intravenous administration only through a free flowing central IV line: not for intramuscular or subcutaneous administration. - If extravasation occurs, stop infusion, aspirate, give antidote (dexrazoxane [Totect] 1000 mg/m2 via remote IV site over 1-2 hours x 2 days or dimethyl sulfate [DMSO]), apply dry cold compresses.
52
What are the notable/common ADRs of the Anthracycline class?
The notable/common ADRs of this drug class are: - Cardiac toxicity (through reactive oxygen species, apoptosis, DNA damage (via topoisomerase II inhibition), and inhibition of protein synthesis - Body fluid discoloration (urine, tears, sweat, and saliva)
53
What are the risk factors for developing cardiac toxicity with an Anthracycline?
Risk factors for developing this ADR with this drug class are: - High cumulative exposure (most consistent risk factor) - Older age (>65 years) - Very young age (<4 years) - Female gender - Pre-existing cardiovascular disorders and comorbidities: - Hypertension - Smoking - Hyperlipidemia - Obesity - Diabetes
54
What is the recommended maximum lifetime dose of Anthracyclines?
The recommended maximum lifetime dose of this class is: - 450-550 mg/m2 Doxorubicin equivalents
55
Describe the strategy and rationale for management of cardiac toxicity caused by Anthracyclines.
The strategy and rationale for management of this condition caused by this drug class are: - Limit lifetime exposure (<450-550 mg/m2 Doxorubicin equivalents) - Perform baseline testing (echocardiogram) - Dexrazoxane (Zinecard) can be used for prevention.
56
Describe the use of dexrazoxane in the management of cardiac toxicity associated with Anthracyclines.
The use of this drug in the management of cardiac toxicity associated with this class is as follows: - Given IV in a 10:1 ratio of dexrazoxane:doxorubicin. - Doxorubicin must be administered within 30 minutes of the completion of the dexrazoxane infusion. - Its FDA labeled indication is in women with metastatic breast cancer with a cumulative doxorubicin dose exceeding 300 mg/m2. - May also be used off label and in some pediatric protocols. - It is not recommended for use with initial doxorubicin therapy. - Dexrazoxane is marketed under two different brand names (Totect and Zinecard), however they are not interchangeable. - Totect is indicated for Anthracycline extravasations. - Generic dexrazoxane and Zinecard are indicated for reducing doxorubicin-induced cardiomyopathy.
57
Describe the strategy and rationale for management of urine discoloration caused by Anthracyclines.
The strategy and rationale for management of this condition caused by this drug class are: - This discoloration is harmless and will resolve 1-2 days after the anthracycline dose - Patients should be counselled that urine discoloration from an anthracycline should be painless. If the discoloration (especially if red) is accompanied by symptoms such as urgency, frequency, or discomfort, they should be evaluated by their healthcare provider as these could be signs of blood in the urine.
58
Describe the metabolism of the Anthracycline class.
The metabolism of this drug is as follows: - All drugs in this class are hepatically metabolized and generally require dose adjustments in patients with hepatic dysfunction
59
What agent was given the nickname "the red devil" and why?
This nickname was given to this drug due to its bright red color, vesicant properties, and side-effect profile.
60
What is the nickname given to Doxorubicin and why?
This drug was the nickname "the red devil" due to its bright red color, vesicant properties, and side-effect profile.
61
What drugs are in the anti-tumor antibody class?
Drugs in this class are: - Bleomycin
62
What is the brand name of Bleomycin?
The brand name of this generic drug is: - Blenoxane
63
What is the generic of name of Blenoxane?
The generic name of this brand name drug is: - Bleomycin
64
What are the main indications for use of Bleomycin?
The main indications of this drug are: - Hodgin Lymphoma - Testicular Cancer - Ovarian Germ Cell Cancer
65
What is the class and MOA of Bleomycin?
This drug in the following class: - Anti-tumor antibody This drug's MOA is as follows: - Inhibits synthesis of DNA by binding to DNA leading to single- and double-strand breaks.
66
What are the notable monitoring parameters for Bleomycin?
The notable monitoring parameters for this drug are: - Pulmonary function tests before, during and after chemotherapy
67
What drug(s) notably require monitoring for pulmonary function tests?
Drug(s) requiring this monitoring are: - Bleomycin
68
What is the emetic potential of Bleomycin?
The emetic potential of this drug is: - Minimal
69
Describe the extravasation risk and management strategies for Bleomycin.
The extravasation risk and mangement strategies for this drug are as follows: - None; N/A
70
Describe the administration of Bleomycin.
The administration of this drug is described as follows: - Can be given IM, SubQ, and intrapleural - Due to the possibility of an anaphylactoid reaction, the manufacturer recommends administering test dose of 2 units or less before the first 2 doses. If no acute reaction occurs, then the regular dosage schedule may be followed. Monitor carefully, particularly following the first 2 doses.
71
Describe the metabolism of Bleomycin.
The metabolism of this drug is as follows: - Metabolized by enzymatic inactivation by bleomycin hydrolase which is widely distributed in normal tissues (except for the skin and lungs) - Cleared/excreted in urine
72
What are the notable ADRs of Bleomycin?
The notable ADRs of this drug are: - Pulmonary toxicity (Bleomycin hydrolase is not found in the lungs). - Interstitial pneumonitis is the most common form of bleomycin pulmonary toxicity but it can also progress to pulmonary fibrosis which is irreversible and potentially fatal. - A severe idiosyncratic reaction consisting of HTN, mental confusion, fever, chills, and wheezing has been reported in approximately 1% of lymphoma patients treated with Bleomycin
73
What drug(s) is notable for causing pulmonary toxicity?
The drugs notable for cause this condition are: - Bleomycin
74
Describe the strategy and rationale for management of pulmonary toxicity caused by Bleomycin.
The strategy and rationale for management of this condition caused by this drug are: - Routinely follow pulmonary function tests, including DLCO (diffusing capacity of the lung for carbon monoxide) during therapy and discontinue if there are significant changes in pulmonary function, including a decrease in DLCO of 40-60%.
75
What are the risk factors for developing pulmonary toxicity with Bleomycin?
Risk factors for developing this ADR with this drug/class are: - Age >70 years - Cumulative lifetime dose of >400 units - Use of GCSF
76
What is the threshold lifetime dose of Bleomycin?
The threshold lifetime dose of this drug is: - 400 units - Beyond this, the risk of pulmonary toxicity increases
77
Describe the half-life of Bleomycin.
The half-life of the this drug is described as follows: - ~2 hours but increases exponentially as CrCl decreases
78
What are the clinical pearls of Bleomycin?
The clinical pearls of this drug are as follows: - Guidelines do not recommend the routine use of GCSF during bleomycin therapy when used for the treatment of lymphoma especially since ABVD (Doxorubicin + Bleomycin + Vinblastine + Dacarbazine) can be safely given at full dose intensity without GCSF use. - No increased risk of pulmonary toxicity with GCSF + Bleomycin for the treatment of testicular cancer, thus use of GCSF is acceptable (although still not recommended as primary prophylaxis). - In patients on ABVD for Hodgkin lymphoma, bleomycin can be dropped if there is a positive response (Deauville 1 or 2) on interim PET scan after 2 cycles. In this situation, continuing with just AVD for the remaining cycles is safer (from a pulmonary toxicity standpoint) but no less effective. - Due to the possibility of an anaphylactoid reaction, the manufacturer recommends administering a test dose before the first 2 doses
79
What drugs are in the Folate Antagonist class?
Drugs in this class are: - Methotrexate - Pemetrexed
80
What are the main cancer-related indications for use of Methotrexate?
The main cancer-related indications of this drug are: - ALL - Non-Hodgkin Lymphoma - GVHD - Bladder Cancer - Head and Neck Cancer - Osteosarcoma - Soft Tissue Sarcoma
81
What are the main indications for use of Pemetrexed?
The main indications of this drug are: - Bladder Cancer - Mesothelioma - NSCLC
82
What is the class and MOA of Methotrexate?
This drug in the following class: - Folate antagonist This drug's MOA is as follows: - Inhibits dihydrofolate reductase thus inhibiting the formation of reduced folates. - Inhibits thymidylate synthetase thus inhibiting synthesis of purines and thymidylic acid. - All this leads to inhibition of DNA synthesis, repair, and cellular replication
83
What is the class and MOA of Pemetrexed?
This drug in the following class: - Folate antagonist This drug's MOA is as follows: - Inhibits dihydrofolate reductase thus inhibiting the formation of reduced folates. - Inhibits thymidylate synthetase thus inhibiting synthesis of purines and thymidylic acid. - All this leads to inhibition of DNA synthesis, repair, and cellular replication
84
What are the notable monitoring parameters for Methotrexate?
The notable monitoring parameters for this drug are: - Methotrexate levels with high dose (>500 mg/m2) - monitor daily until cleared - Urine pH with high dose
85
What drug(s) notably require monitoring for urine pH?
Drug(s) notably requiring this monitoring are: - Methotrexate
86
What drug(s) notably require monitoring for drug levels daily until cleared?
Drug(s) notably requiring this monitoring are: - Methotrexate
87
Describe the administration of Methotrexate.
The administration of this drug is described as follows: - Most methotrexate protocols will require the urine pH to be >7 before starting methotrexate. - Alkalization protocols vary per institution but often include IV fluids, sodium bicarbonate (either IV or oral) and/or acetazolamide.
88
What is the emetic potential of Methotrexate?
The emetic potential of this drug is: - Minimal with low lose (<50 mg/m2) - Low with low-moderate doses (50-250 mg/m2) - High with moderate-high doses (>250 mg/m2)
89
What is the emetic potential of Pemetrexed?
The emetic potential of this drug is: - Low
90
Describe the extravasation risk and management strategies for Methotrexate.
The extravasation risk and management strategies for this drug are as follows: - None; N/A
91
Describe the extravasation risk and management strategies for Pemetrexed.
The extravasation risk and management strategies for this drug are as follows: - None; N/A
92
Describe the metabolism of Methotrexate.
The metabolism of this drug is as follows: - Minimal metabolism; excreted primarily (90%) in the urine as unchanged drug - Urine clearance is pH dependant and improved when the urine is alkalized - High dose methotrexate may "third space" or accumulate in fluid collections leading to prolonged methotrexate clearance and increased toxicity. Patients with ascites. pericardial effusions. pleural effusions or other fluid collections should not receive high dose methotrexate until those have been drained.
93
Describe the metabolism of Pemetrexed.
The metabolism of this drug is as follows: - Minimal metabolism; excreted primarily (90%) in the urine as unchanged drug
94
What are the notable ADRs of Methotrexate?
The notable ADRs of this drug are: - Methotrexate toxicity - Renal dysfunction - Bone marrow suppression - Mucositis
95
What are the notable ADRs of Pemetrexed?
The notable ADRs of this drug are: - Main one is that serious and occasionally fatal dermatologic toxicity may occur - Others are myelosuppression, renal dysfunction, and GI toxicities (especially with concomitant Ibuprofen use)
96
Describe the strategy and rationale for management of Methotrexate toxicity.
The strategy and rationale for management of this condition caused by this drug are: - Ensure urine is adequate alkalized before starting methotrexate - Administer leucovorin rescue with doses greater than >500 mg/m2 - Glucarpidase can be administered as an antidote.
97
How does Glucarpidase work as a antidote with Methotrexate?
This drug works as follows when used as a Methotrexate antidote: - Glucarpidase is an enzyme that hydrolyzes the methotrexate into inactive metabolites rapidly reducing the methotrexate concentration.
98
How is Glucarpidase given when used as a Methotrexate antidote?
This drug is given as follows when use as a Methotrexate rescue: - The typical dose is 50 units/kg and it should ideally be given within 48-60 hours of methotrexate infusion (beyond this point, life threating toxicities may not be preventable).
99
Describe the strategy and rationale for management of dermatologic toxicity with Pemetrexed.
The strategy and rationale for management of this condition caused by this drug are: - Pretreat with dexamethasone 4 mg orally twice daily for 3 days to reduce the incidence and severity of cutaneous reactions.
100
What are the clinical pearls of Methotrexate?
The clinical pearls of this drug are as follows: - Most methotrexate protocols will require the urine pH to be >7 before starting methotrexate - Doses >500 mg/m2 require leucovorin "rescue" and inpatient monitoring of levels to ensure appropriate methotrexate clearance - High dose methotrexate may "third space" or accumulate in fluid collections leading to prolonged methotrexate clearance and increased toxicity. Patients with ascites. pericardial effusions. pleural effusions or other fluid collections should not receive high dose methotrexate until those have been drained. - Methotrexate has many drug interactions which can cause delayed clearance. Medications that must be stopped prior to high dose methotrexate include: - Bactrim, PPIs, Penicillins, Salicylates, Probenecid, NSAIDs, Tetracyclines, and Ciprofloxacin. - Many of these agents can be stopped 1-2 days prior to high dose methotrexate and can be resumed after adequate clearance. - Intrathecal methotrexate or low oral doses of methotrexate do not have the same drug interaction concerns. - When checking doses on oral methotrexate, only oncologic indications will have daily dosing options. If a prescription for lupus, psoriasis, arthritis, etc. is written for daily (instead of weekly) it's likely an error!
101
What drugs must be stopped prior to high dose methotrexate?
Medications that must be stopped prior to administration of this drug include: - Bactrim - PPIs - Penicillins - Salicylates - Probenecid - NSAIDs - Tetracyclines - Ciprofloxacin
102
How does Leucovorin work as a "rescue" with Methotrexate?
This drug works as follows when used as a Methotrexate rescue: - It is folinic acid (an active form of folate) that does not need to be processed by dihydrofolate reductase. It is given to rescue healthy cells from the toxicity of methotrexate and replenish the supply of folate metabolites depleted by methotrexate.
103
How is Leucovorin given when used as a Methotrexate rescue?
This drug is given as follows when use as a Methotrexate rescue: - Usually started 12-24 hours post high dose methotrexate and given until serum methotrexate levels are below a certain threshold (often 0.05 mM). - Dosing varies per protocol but oral absorption is saturable at doses >25 mg, so doses >25 mg are often given IV. - Typical dosing frequency is orally every 6 hours, although dose and frequency may be increased if a patient is experiencing methotrexate toxicity.
104
What are the clinical pearls of Pemetrexed?
The clinical pearls of this drug are as follows: - Patients receiving pemetrexed require vitamin supplementation with folic acid and B12. - Give folic acid 400 to 1,000 mcg daily starting 7 days before initial pemetrexed dose and continue daily during treatment and for 21 days after last pemetrexed dose. - Give Vitamin B12 1,000 mcg IM starting 7 days prior to treatment initiation and then every 3 cycles. - To prevent dermatologic toxicity, pretreat with dexamethasone - Patients with a CrCl 45 to 79 mL/min must avoid ibuprofen for 2 days before, the day of, and for 2 days following a dose of pemetrexed. Monitor more frequently for myelosuppression, renal dysfunction, and GI toxicities if concomitant Ibuprofen administration cannot be avoided.
105
What drugs are in the Hypomethylator class?
Drugs in this class are: - Azacitidine - Decitabine
106
What is the brand name of Azacitidine?
The brand name of this generic drug is: - Vidaza (IV, SubQ) - Onureg (Oral)
107
What is the brand name of Decitabine?
The brand name of this generic drug is: - Dacogen
108
What is the generic of name of Vidaza?
The generic name of this brand name drug is: - Azacitidine
109
What is the generic of name of Onureg?
The generic name of this brand name drug is: - Azacitidine
110
What is the generic of name of Dacogen?
The generic name of this brand name drug is: - Decitabine
111
What are the main indications for use of Azacitidine?
The main indications of this drug are: - AML - MDS
112
What are the main indications for use of Decitabine?
The main indications of this drug are: - AML - MDS
113
What are the main/common indications of the Hypomethylator class?
The main/common indications of this drug class are: - AML - MDS
114
What is the class and MOA of Azacitidine?
This drug in the following class: - Hypomethylator This drug's MOA is as follows: - Methylation (via methyltransferase) of tumor suppressor genes can contribute to the growth and survival of the cancer. Hypomethylating agents prevent DNA methylation by inhibiting methyltransferase, thus allowing for tumor suppressor gene expression which thus inhibits cancer growth.
115
What is the class and MOA of Decitabine?
This drug in the following class: - Hypomethylator This drug's MOA is as follows: - Methylation (via methyltransferase) of tumor suppressor genes can contribute to the growth and survival of the cancer. Hypomethylating agents prevent DNA methylation by inhibiting methyltransferase, thus allowing for tumor suppressor gene expression which thus inhibits cancer growth.
116
What is the emetic potential of Azacitidine?
The emetic potential of this drug is: - Moderate
117
Describe the emetic potential of Decitabine.
The emetic potential of this drug is: - Minimal
118
What drugs in the Hypomethylator class have a high emetic potential?
Drugs in the class with a high emetic potential are: - None, N/A
119
What drugs in the Hypomethylator class have a moderate emetic potential?
Drugs in the class with a moderate emetic potential are: - Azacitidine
120
What drugs in the Hypomethylator class have a low emetic potential?
Drugs in the class with a low emetic potential are: - None, N/A
121
What drugs in the Hypomethylator class have a minimal emetic potential?
Drugs in the class with a minimal emetic potential are: - Decitabine
122
Describe the extravasation risk and management strategies for Azacitidine.
The extravasation risk and management strategies for this drug are as follows: - None, N/A
123
Describe the extravasation risk and management strategies for Decitabine.
The extravasation risk and management strategies for this drug are as follows: - None, N/A
124
Describe the extravasation risk and management strategies for the Hypomethylator class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
125
Describe the distribution of the Hypomethylator class.
The distribution of this class is described as follows: - Hypomethylating agents do not cross the blood brain barrier and will have limited utility in treating patients with central nervous system disease.
126
Describe the administration of Azacitidine.
The administration of this drug is described as follows: - Vidaza is given IV or SubQ - Onureg is given orally
127
What are the notable/common ADRs of the Hypomethylator class?
The notable/common ADRs of this drug class are: - Bone marrow suppression
128
Describe the strategy and rationale for management of bone marrow suppression caused by hypomethylators.
The strategy and rationale for management of this condition caused by this drug are: - This is the major side effect of the hypomethylators, however it can be difficult to determine if it is from the chemotherapy or the patient's disease. - In many cases, we will treat through it for the first few cycles of therapy (due to the long time to response of hypomethylators) but patients with this after 3-4 months of therapy may need a bone marrow biopsy to rule out relapsed disease.
129
What are the clinical pearls of the Hypomethylator class?
The clinical pearls of this drug class are as follows: - When used as single agent therapy. hypomethylators have a median response time of 3-4 months. - These agents are typically well tolerated and are a good choice of therapy for older/frail patients who may not be able to tolerate intensive chemotherapy. - Recent data has shown that patients have improved response rates when combining hypomethylators with venetoclax (an oral BCL2 inhibitor). - This combination also increases toxicity but is preferentially used in patients who can tolerate it.
130
What drugs are in the Platinum Analogue class?
Drugs in this class are: - Carboplatin - Cisplatin - Oxaliplatin
131
What is the brand name of Carboplatin?
The brand name of this generic drug is: - Paraplatin
132
What is the brand name of Cisplatin?
The brand name of this generic drug is: - Platinol
133
What is the brand name of Oxaliplatin?
The brand name of this generic drug is: - Eloxatin
134
What is the generic of name of Paraplatin?
The generic name of this brand name drug is: - Carboplatin
135
What is the generic of name of Platinol?
The generic name of this brand name drug is: - Cisplatin
136
What is the generic of name of Eloxatin?
The generic name of this brand name drug is: - Oxaliplatin
137
What are the main indications for use of Carboplatin?
The main indications of this drug are: - Anal Cancer - Bladder Cancer - Breast Cancer - Esophageal Cancer - Gastric Cancer - Head and Neck Cancer - Hodgkin Lymphoma - Non-Hodgkin Lymphoma - NSCLC - SCLC - Gynecologic Cancer - Testicular Cancer
138
What are the main indications for use of Cisplatin?
The main indications of this drug are: - Anal Cancer - Bladder Cancer - Breast Cancer - Esophageal Cancer - Gastric Cancer - Head and Neck Cancer - Hodgkin Lymphoma - Non-Hodgkin Lymphoma - NSCLC - SCLC - Gynecologic Cancer - Testicular Cancer
139
What are the main indications for use of Oxaliplatin?
The main indications of this drug are: - Esophageal Cancer - Gastric Cancer - Non-Hodgkin Lymphoma - Testicular Cancer - Biliary Adencocarcinoma - Colorectal Cancer - Pancreatic Cancer
140
What is the class and MOA of Carboplatin?
This drug in the following class: - Platinum Analogues This drug's MOA is as follows: - Alkylating agents which covalently binds to DNA and interfere with the function of DNA by producing interstrand DNA cross-links. - They preferentially bind to the N-7 position of guanine.
141
What is the class and MOA of Cisplatin?
This drug in the following class: - Platinum Analogues This drug's MOA is as follows: - Alkylating agents which covalently binds to DNA and interfere with the function of DNA by producing interstrand DNA cross-links. - They preferentially bind to the N-7 position of guanine.
142
What is the class and MOA of Oxaliplatin?
This drug in the following class: - Platinum Analogues This drug's MOA is as follows: - Alkylating agents which covalently binds to DNA and interfere with the function of DNA by producing interstrand DNA cross-links. - They preferentially bind to the N-7 position of guanine.
143
What are the notable monitoring parameters for the Platinum Analogues?
The notable monitoring parameters for this drug class are: - S/Sx of nephrotoxicity - renal panel - S/Sx of ototoxicity - consider audiometric and vestibular testing, particularly in all pediatric patients receiving cisplatin (pediatric patients should receive audiometric testing at baseline, prior to each dose, and for several years after discontinuing therapy). - S/Sx of neuropathy - neurologic evaluation prior to each dose and periodically thereafter
144
What is the emetic potential of Carboplatin?
The emetic potential of this drug is: - High if AUC >4 - Moderate if AUC <4
145
What is the emetic potential of Cisplatin?
The emetic potential of this drug is: - High (commonly regarded as the most emetogenic of all chemotherapies)
146
What is the emetic potential of Oxaliplatin?
The emetic potential of this drug is: - Moderate
147
Describe the emetic potential of the Platinum Analogues.
The emetic potential of this drug class is: - Moderate (Oxaliplatin, Carboplatin AUC <4) to High (Carboplatin AUC >4, Cisplatin)
148
What drugs in the Platinum Analogue class have a high emetic potential?
Drugs in the class with a high emetic potential are: - Cisplatin (commonly regarded as the most emetogenic of all chemotherapies) - Carboplatin if AUC >4
149
What drugs in the Platinum Analogue class have a moderate emetic potential?
Drugs in the class with a moderate emetic potential are: - Carboplatin if AUC <4 - Oxaliplatin
150
What drugs in the Platinum Analogue class have a low emetic potential?
Drugs in the class with a low emetic potential are: - None, N/A
151
What drugs in the Platinum Analogue class have a minimal emetic potential?
Drugs in the class with a minimal emetic potential are: - None, N/A
152
Describe the extravasation risk and management strategies for Oxaliplatin.
The extravasation risk and management strategies for this drug are as follows: - Irritant with vesicant- like properties - If extravasation occurs, stop infusion and aspirate. Data conflicts regarding use of warm or cold compresses - Cold compresses may reduce cellulary injury but could potentially precipitate or exacerbate peripheral neuropathy - Warm compresses may increase local drug removal but may increase cellular uptake and injury
153
Describe the extravasation risk and management strategies for the Platinum Analogue class.
The extravasation risk and management strategies for this drug class are as follows: - Carboplatin may be an irritant - Cisplatin is a vesicant at higher concentrations - Oxaliplatin is irritant with vesicant like properties
154
Describe the metabolism of the Platinum Analogues.
The metabolism of this drug is as follows: - Clearance is renal - The mean AUC of unbound platinum increases as renal function decreases - 40% increase with mild (CrCl 50 to 80 ml /minute) renal impairment - 95% increase with moderate (CrCl 30 to 49 ml /minute) renal impairment - 342% increase with severe (CrCl <30 ml /minute) renal impairment
155
What are the notable ADRs of Carboplatin?
The notable ADRs of this drug are: - Chronic Peripheral Neuropathy - Nephrotoxicity - Hypersensitivity Reactions
156
What are the notable ADRs of Cisplatin?
The notable ADRs of this drug are: - Ototoxicity - Chronic Peripheral Neuropathapy - Nephrotoxicity - Hypersensitivity Reactions
157
What are the notable ADRs of Oxaliplatin?
The notable ADRs of this drug are: - Chronic Peripheral Neuropathapy - Acute Peripheral Neuropathy (unique to oxaliplatin vs other platinums) - Nephrotoxicity - Hypersensitivity Reactions
158
What are the notable/common ADRs of the Platinum Analogue class?
The notable/common ADRs of this drug class are: - Chronic Peripheral Neuropathy (acute is unique to oxaliplatin) - Nephrotoxicity - Ototoxicity (cisplatin) - Hypersensitivity Reactions (especially carboplatin and oxaliplatin)
159
What drug(s) of the Platinum Analogue class is notable for causing electrolyte wasting?
The drugs in this class notable for cause this condition are: - All can but it is especially notable for Cisplatin
160
What drug(s) of the Platinum Analogue class is notable for causing ototoxicity?
The drugs in this class notable for cause this condition are: - Cisplatin (especially in children and even moreso in pediatrics)
161
What drug(s) of the Platinum Analogue class is notable for causing acute peripheral neuropathy?
The drugs in this class notable for cause this condition are: - Oxaliplatin
162
What drug(s) of the Platinum Analogue class is notable for causing hypersensitivity reactions?
The drugs in this class notable for cause this condition are: - All can but it is especially notable for Carboplatin and Oxaliplatin
163
Describe the strategy and rationale for management of Peripheral Neuropathy caused by Platinum Analogues.
The strategy and rationale for management of this condition caused by this drug class are: - This can be broken down into two types: acute and chronic - Chronic mimics traditional peripheral neuropathy with numbness/tingling in the fingers and toes. - This can occur >14 days after the dose. - Can be persistent and interfere with daily activities like writing or walking. - Symptoms may improve in some patients upon discontinuing treatment. - Acute is unique to oxaliplatin and presents as cold-induced neuropathy. - Often occurs within hours of the oxaliplatin infusion and resolves within 7 days. - Symptoms may include transient paresthesia, dysesthesia, and hypoesthesia (in the hands, feet, perioral area, or throat), jaw spasm, abnormal tongue sensation, or a feeling of chest pressure. - Patients should be counseled to avoid ice chips, exposure to cold temperatures, and cold food/beverages during or within hours after oxaliplatin infusion.
164
Describe the strategy and rationale for management of nephrotoxicity caused by Platinum Analogues.
The strategy and rationale for management of this condition caused by this drug class are: - All of the platinum agents have the potential to cause nephrotoxicity. - Patients should receive aggressive pre and post platinum hydration with normal saline, ideally targeting urine output of 100 ml/hour prior to the chemotherapy infusion. - Patients also should receive potassium and magnesium replacement as these agents (especially cisplatin) can cause electrolyte wasting.
165
Describe the strategy and rationale for management of ototoxicity caused by Platinum Analogues.
The strategy and rationale for management of this condition caused by this drug class are: - Cisplatin may cause cumulative and severe ototoxicity. - Manifested by tinnitus, high-frequency (4,000 to 8,000 Hz) hearing loss, and/or decreased ability to hear normal conversational tones. - May occur during or after treatment and may be unilateral or bilateral. - More common in children and even moreso in pediatrics (40%-60%). - Consider audiometric and vestibular testing, particularly in all pediatric patients receiving cisplatin.
166
Describe the strategy and rationale for management of hypersensitivity reactions caused by Platinum Analogues.
The strategy and rationale for management of this condition caused by this drug class are: - Platinum agents are the second most common source of hypersensitivity reactions among chemotherapy agents (following asparaginase products). - Especially common with Carboplatin and Oxaliplatin - For Carboplatin: - The incidence of carboplatin hypersensitivity reactions is between 1-44%. - Most common after 6 -8 doses - Patients with mild-moderate reactions can be desensitized and may continue to receive infusions - For Oxaliplatin: - The incidence of acute reactions is between 12-25% with up to 30% of those being severe infusion reactions. - Reactions may occur within minutes of drug administration and with any cycle - Similar to carboplatin, the risk of hypersensitivity reaction is higher with multiple cycles of therapy. - Patients with mild reactions may be re-challenged.
167
What are the clinical pearls of Carboplatin?
The clinical pearls of this drug are as follows: - Dosing is based off target AUC (usually 2-6)
168
Describe the use of the Calvert formula.
This use of this formula is as follows: - Used to calculate Carboplatin dose using target AUC - Total dose (mg) = Target AUC x (GFR + 25) - If estimating instead of measuring GFR (as with Cockroft Gault), protocols typically cap GFR at a maximum of 125 ml/minute to avoid potential toxicity (although this does vary per indication)
169
What are the clinical pearls of the Platinum Analogue class?
The clinical pearls of this drug class are as follows: - They are the second most common source of hypersensitivity reactions among chemotherapy agents (following asparaginase products).
170
What drugs are in the Purine Antagonist class?
Drugs in this class are: - 6-Mercatopurine (6-MP) - Fludarabine - Cladribine - Clofarabine - Nelarabine - Pentostatin - Thioguanine
171
What is the brand name of 6Mercatopurine (6MP)?
The brand name of this generic drug is: - Purixan
172
What is the brand name of Fludarabine?
The brand name of this generic drug is: - Fludara
173
What is the brand name of Cladribine?
The brand name of this generic drug is: - Mavenclad - Leustatin
174
What is the brand name of Clofarabine?
The brand name of this generic drug is: - Clolar - Clofarex
175
What is the brand name of Nelarabine?
The brand name of this generic drug is: - Arranon
176
What is the brand name of Pentostatin?
The brand name of this generic drug is: - Nipent
177
What is the brand name of Thioguanine?
The brand name of this generic drug is: - Nipent
178
What is the generic of name of Purixan?
The generic name of this brand name drug is: - 6Mercatopurine
179
What is the generic of name of Fludara?
The generic name of this brand name drug is: - Fludarabine
180
What is the generic of name of Mavenclad?
The generic name of this brand name drug is: - Cladribine
181
What is the generic of name of Clolar?
The generic name of this brand name drug is: - Clofarabine
182
What is the generic of name of Arranon?
The generic name of this brand name drug is: - Nelarabine
183
What is the generic of name of Nipent?
The generic name of this brand name drug is: - Pentostatin
184
What is the generic of name of Nipent?
The generic name of this brand name drug is: - Thioguanine
185
What are the main indications for use of 6Mercatopurine?
The main indications of this drug are: - ALL
186
What are the main indications for use of Fludarabine?
The main indications of this drug are: - CLL - AML - HSCT - Non-Hodkin Lymphoma
187
What are the main/common indications of the Purine Antagonist class?
The main/common indications of this drug class are: - Leukemias with Fludarabine - Non-Hodgkin Lymphoma with 6MP
188
What is the class and MOA of 6Mercaptopurine?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
189
What is the class and MOA of Fludarabine?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
190
What is the class and MOA of Cladribine?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
191
What is the class and MOA of Clofarabine?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
192
What is the class and MOA of Nelarabine?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
193
What is the class and MOA of Pentostatin?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
194
What is the class and MOA of Thioguanine?
This drug in the following class: - Purine Antagonist This drug's MOA is as follows: - Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite. - The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis. - They are specific for the S phase of the cell cycle.
195
What is the emetic potential of 6Mercatopurine?
The emetic potential of this drug is: - Minimal to Low
196
What is the emetic potential of Fludarabine?
The emetic potential of this drug is: - Minimal
197
Describe the emetic potential of the Purine Antagonist class.
The emetic potential of this drug class is: - Minimal to Low except for Clofarabine (Moderate)
198
What drugs in the Purine Antagonist class have a high emetic potential?
Drugs in the class with a high emetic potential are: - None, N/A
199
What drugs in the Purine Antagonist class have a moderate emetic potential?
Drugs in the class with a moderate emetic potential are: - Clofarabine
200
What drugs in the Purine Antagonist class have a low emetic potential?
Drugs in the class with a low emetic potential are: - All are Minimal to Low except for: - Fludarabine and Cladribine (Minimal) - Clofarabine (Moderate)
201
What drugs in the Purine Antagonist class have a minimal emetic potential?
Drugs in the class with a minimal emetic potential are: - Fludarabine - Cladribine - All the rest are "Minimal to Low" except for Clofarabine (Moderate)
202
Describe the extravasation risk and management strategies for the Purine Antagonist class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
203
Describe the metabolism of 6Mercaptopurine.
The metabolism of this drug is as follows: - Total body clearance of the principal metabolite correlates with creatinine clearance
204
Describe the metabolism of Fludarabine.
The metabolism of this drug is as follows: - Renal impairment may result in slower elimination of parent drug and metabolite, and a greater cumulative effect
205
What are the clinical pearls of 6Mercaptopurine?
The clinical pearls of this drug are as follows: - Doses for ALL are typically titrated to maintain an ANC between 500-1500 cells/mcL. Methods of dose titration will vary per protocol but typically involve adjusting doses every 4-8 weeks. - In patients intolerant to this drug (abnormally low CBC unresponsive to dose reduction, severe bone marrow toxicities, or repeated myelosuppressive episodes), consider genotyping of NUDT15 and TPMT. - NUDT15 and TPMT genotyping or phenotyping may assist in identifying patients at risk for developing toxicity and those who may needs empiric dose reductions due to decreased metabolism of 6-MP.
206
What drugs are in the Pyrimidine Antagonist class?
Drugs in this class are: - Gemcitabine - 5Fluorouracil (5FU) - Capecitabine - Cytarabine - Floxuridine
207
What is the brand name of Gemcitabine?
The brand name of this generic drug is: - Infugem - Gemzar
208
What is the brand name of 5Fluorouracil?
The brand name of this generic drug is: - Adrucil
209
What is the brand name of Capecitabine?
The brand name of this generic drug is: - Xeloda
210
What is the brand name of Cytarabine?
The brand name of this generic drug is: - AraC - Cytosar
211
What is the brand name of Floxuridine?
The brand name of this generic drug is: - Fluorouridine deoxyribose
212
What is the generic of name of Infugem?
The generic name of this brand name drug is: - Gemcitabine
213
What is the generic of name of Gemzar?
The generic name of this brand name drug is: - Gemcitabine
214
What is the generic of name of Adrucil?
The generic name of this brand name drug is: - 5Fluorouracil
215
What is the generic of name of Xeloda?
The generic name of this brand name drug is: - Capecitabine
216
What is the generic of name of AraC?
The generic name of this brand name drug is: - Cytarabine
217
What is the generic of name of Cytosar?
The generic name of this brand name drug is: - Cytarabine
218
What is the generic of name of Fluorouridine deoxyribose?
The generic name of this brand name drug is: - Floxuridine
219
What are the main indications for use of Gemcitabine?
The main indications of this drug are: - Breast Cancer - Head and Neck Cancers - Pancreatic Cancer - Bladder Cancer - Hodgkin Lymphoma - Non-Hodgkin Lymphoma - Small Cell Lung Cancer - Non-Small Cell Lung Cancer
220
What are the main indications for use of 5Fluorouracil?
The main indications of this drug are: - Anal Cancer - Breast Cancer - Colorectal Cancer - Esophageal Cancer - Gastric Cancer - Head and Neck Cancers - Pancreatic Cancer
221
What are the main indications for use of Capecitabine?
The main indications of this drug are: - Anal Cancer - Breast Cancer - Colorectal Cancer - Esophageal Cancer - Gastric Cancer - Head and Neck Cancers - Pancreatic Cancer
222
What is the class and MOA of Gemcitabine?
This drug in the following class: - Pyrimidine Antagonist This drug's MOA is as follows: - It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine. - The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death.
223
What is the class and MOA of 5Fluorouracil?
This drug in the following class: - Pyrimidine Antagonist This drug's MOA is as follows: - It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine. - The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death. - After activation, F-UMP (an active metabolite) is incorporated into RNA to replace uracil and inhibit cell growth - The active metabolite F-dUMP inhibits thymidylate synthetase
224
What is the class and MOA of Capecitabine?
This drug in the following class: - Pyrimidine Antagonist This drug's MOA is as follows: - Capecitabine is a prodrug of fluorouracil. - It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine. - The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death. - After activation of Fluorouracil, F-UMP (an active metabolite) is incorporated into RNA to replace uracil and inhibit cell growth - The active metabolite F-dUMP inhibits thymidylate synthetase
225
What is the class and MOA of Cytarabine?
This drug in the following class: - Pyrimidine Antagonist This drug's MOA is as follows: - Cytarabine is a pyrimidine analog and is incorporated into DNA; however, the primary action is inhibition of DNA polymerase resulting in decreased DNA synthesis and repair.
226
What is the class and MOA of Floxuridine?
This drug in the following class: - Pyrimidine Antagonist This drug's MOA is as follows: - It is catabolized to fluorouracil after intra-arterial administration, resulting in activity similar to fluorouracil - It inhibits thymidylate synthetase - It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine. - The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death.
227
What are the notable monitoring parameters for 5Fluorouracil?
The notable monitoring parameters for this drug are: - Monitor INR closely if patients are receiving concomitant warfarin therapy due to a drug-drug interaction.
228
What are the notable monitoring parameters for Capecitabine?
The notable monitoring parameters for this drug are: - Monitor INR closely if patients are receiving concomitant warfarin therapy due to a drug-drug interaction.
229
What are the notable/common monitoring parameters for the Pyrimidine Antagonist class?
The notable/common monitoring parameters for this drug class are: - Monitor INR closely if patients are receiving concomitant warfarin therapy and 5Fluorouracil or Capecitabine due to a drug-drug interaction.
230
What drug(s) notably require monitoring of INR if on concomitant warfarin therapy?
Drug(s) notably requiring this monitoring are: - 5Fluorouracil - Capecitabine
231
What is the emetic potential of 5Fluorouracil?
The emetic potential of this drug is: - Low
232
What is the emetic potential of Capecitabine?
The emetic potential of this drug is: - Low
233
What is the emetic potential of Gemcitabine?
The emetic potential of this drug is: - Low
234
What is the emetic potential of Cytarabine?
The emetic potential of this drug is: - Adults: - Moderate if >1,000 mg/m2 - Low if ≤1,000 mg/m2 - Pediatrics: - High if ≥3,000 mg/m2/day: High (>90%). - Moderate for 75 mg/m2/dose.
235
Describe the emetic potential of the Pyrimidine Antagonist class.
The emetic potential of this drug class is: - Low (except for Cytarabine*)
236
Describe the extravasation risk and management strategies for the Pyrimidine Antagonist class.
The extravasation risk and management strategies for this drug class are as follows: - Fluorouracil may be an irritant. avoid extravasation.
237
Describe the administration of 5Fluorouracil.
The administration of this drug is described as follows: - 5-FU is given as a 46-hour continuous infusion with some chemotherapy regimens. - In these cases, leucovorin is often given to enhance the mechanism of 5-FU by adding additional inhibition of thymidylate synthase. This leads to increased cancer cell death but can also cause increased toxicities.
238
Describe the administration of Capecitabine.
The administration of this drug is described as follows: - It is given orally often in divided doses, 12 hours apart, for 2 weeks on and 1 week off. - It should be taken with food. - Oral administration is similar to continuous infusion 5-FU in terms of toxicity.
239
Describe the administration of Floxuridine.
The administration of this drug is described as follows: - Administered as a continuous hepatic intra-arterial infusion using an infusion pump.
240
Describe the metabolism of 5Fluorouracil.
The metabolism of this drug is as follows: - HEPATICALLY metabolized to form active metabolites. 5-fluoroxyuridine monophosphate (F-UMP) and 5-5-fluoro- 2'-deoxyuridine-5'-0 -monophosphate (F-dUMP)
241
Describe the metabolism of Capecitabine.
The metabolism of this drug is as follows: - Enzymatically metabolized to fluorouracil.
242
Describe the metabolism of Gemcitabine.
The metabolism of this drug is as follows: - Metabolized intracellularly by nucleoside kinases to the active diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleoside metabolites
243
Describe the metabolism of Cytarabine.
The metabolism of this drug is as follows: - Primarily hepatic - Metabolized by deoxycytidine kinase to aracytidine triphosphate (active) - ~90% of dose is metabolized to inactive uracil arabinoside (ARA-U); intrathecal administration results in little conversion to ARA-U due to the low levels of deaminase in the cerebral spinal fluid.
244
What are the notable ADRs of 5Fluorouracil?
The notable ADRs of this drug are: - Hand-foot syndrome, also called palmar-plantar erythrodysesthesia. Patients can experience redness, swelling, and pain on the palms of the hands and/or the soles of the feet. - A bolus dose of 5-FU is associated with myelosuppression while the continuous infusion 5-FU/capecitabine is more likely to cause diarrhea and hand/foot syndrome.
245
What are the notable ADRs of Capecitabine?
The notable ADRs of this drug are: - Hand-foot syndrome, also called palmar-plantar erythrodysesthesia. Patients can experience redness, swelling, and pain on the palms of the hands and/or the soles of the feet.
246
What are the notable ADRs of Cytarabine?
The notable ADRs of this drug are: - Cytarabine syndrome which is almost flu-like and is characterized by fever, myalgia, bone pain, chest pain (occasionally), maculopapular rash, conjunctivitis, and malaise. - Occurs in up to 1/3rd of patients receiving Cytarabine for AML (most of whom have had prior exposure to the drug) - It generally occurs 6 to 12 hours following administration.
247
What are the notable/common ADRs of the Pyrimidine Antagonist class?
The notable/common ADRs of this drug class are: - Hand/Foot Syndrome (especially 5Fluorouracil and Capecitabine)
248
What drug(s) of the Pyrimidine Antagonist class is notable for causing Hand/Foot Syndrome?
The drugs in this class notable for cause this condition are: - 5Fluorouracil and Capecitabine (and to a lesser degree Cytarabine)
249
Describe the strategy and rationale for management of intolerability to 5Fluorouracil.
The strategy and rationale for management of this condition caused by this drug are: - Leucovorin is often given to enhance the mechanisam of 5-FU by adding additional inhibition of thymidylate synthase. This leads to increased cancer cell death but can also cause increased toxicities. - In patients who are poorly tolerating their 5-FU/leucovorin containing regimens. you may consider omitting the leucovorin (instead of decreasing the 5-FU dose)
250
Describe the strategy and rationale for management of Hand/Foot Syndrome caused by 5Fluorouracil/Capecitabine.
The strategy and rationale for management of this condition caused by this drug are: - It is thought to be caused by damage to the deep capillaries, leading to COX inflammatory-type reactions or related to enzymes involved in 5-FU metabolism - It can be prevented by avoiding friction causing activities (lifting weights, running), avoiding hot water or other sources of heat, and using lotions or creams to keep skin moist. - It is treated by holding chemotherapy, and applying topical or oral anti-inflammatory agents and analgesics.
251
Describe the strategy and rationale for management of Cytarabine Syndrome.
The strategy and rationale for management of this condition caused by this drug are: - While the etiology is unclear, it is probably related to cytokine release rather than immune-mediated - Acetaminophen before and after dose may reduce the frequency of the cytarabine syndrome. - Glucocorticoids may also be beneficial for both treatment and prevention of the cytarabine syndrome. - Retreatment after Cytarabine syndrome can usually be safely accomplished with increased premedication, even in patients with multiple reactions
252
What are the clinical pearls of Capecitabine?
The clinical pearls of this drug are as follows: - Oral capecitabine has many drug interactions to be aware of including: - PPIs (which can decrease efficacy) - Warfarin (increased INR)
253
What drugs are in the Taxanes class?
Drugs in this class are: - Docetaxel - Cabazitaxel - Paclitaxel - NabPaclitaxel
254
What is the brand name of Docetaxel?
The brand name of this generic drug is: - Taxotere
255
What is the brand name of Cabazitaxel?
The brand name of this generic drug is: - Jevtana
256
What is the brand name of Paclitaxel?
The brand name of this generic drug is: - Taxol
257
What is the brand name of NabPaclitaxel?
The brand name of this generic drug is: - Abraxane
258
What is the generic of name of Taxotere?
The generic name of this brand name drug is: - Docetaxel
259
What is the generic of name of Jevtana?
The generic name of this brand name drug is: - Cabazitaxel
260
What is the generic of name of Taxol?
The generic name of this brand name drug is: - Paclitaxel
261
What is the generic of name of Abraxane?
The generic name of this brand name drug is: - NabPaclitaxel
262
What are the main indications for use of Docetaxel?
The main indications of this drug are: - Breast Cancer - Esophageal Cancer - Gastric Cancer - Head and Neck Cancer - Non-Small Cell Lung Cancer - Ovarian Cancer - Prostate Cancer - Small Cell Lung Cancer
263
What are the main indications for use of Paclitaxel?
The main indications of this drug are: - Breast Cancer - Esophageal Cancer - Gastric Cancer - Head and Neck Cancer - Non-Small Cell Lung Cancer - Ovarian Cancer - Small Cell Lung Cancer - Anal Cancer - Bladder Cancer - Cervical Cancer - Endometrial Cancer - Kaposi Sarcoma
264
What are the main indications for use of NabPaclitaxel?
The main indications of this drug are: - Breast Cancer - Non-Small Cell Lung Cancer - Ovarian Cancer - Bladder Cancer - Cervical Cancer - Biliary Cancer - Pancreatic Cancer
265
What is the class and MOA of Docetaxel?
This drug in the following class: - Taxanes This drug's MOA is as follows: - Taxanes inhibit the mitotic spindle. - They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process. - These drugs are cell-cycle specific in the M-phase.
266
What is the class and MOA of Cabazitaxel?
This drug in the following class: - Taxanes This drug's MOA is as follows: - Taxanes inhibit the mitotic spindle. - They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process. - These drugs are cell-cycle specific in the M-phase - Unlike other taxanes, this drug has a poor affinity for multidrug resistance (MDR) proteins, therefore conferring activity in resistant tumors.
267
What is the class and MOA of Paclitaxel?
This drug in the following class: - Taxanes This drug's MOA is as follows: - Taxanes inhibit the mitotic spindle. - They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process. - These drugs are cell-cycle specific in the M-phase.
268
What is the class and MOA of NabPaclitaxel?
This drug in the following class: - Taxanes This drug's MOA is as follows: - Taxanes inhibit the mitotic spindle. - They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process. - These drugs are cell-cycle specific in the M-phase.
269
Describe the emetic potential of the Taxanes class.
The emetic potential of this drug class is: - Low (all agents)
270
Describe the extravasation risk and management strategies for Paclitaxel.
The extravasation risk and management strategies for this drug are as follows: - Irritant with vesicant-like properties - Consider the use of hyaluronidase - Administer 1 to 6 ml (150 units/ml) into existing IV line: usual dose is 1 ml for each 1 ml of extravasated drug.
271
Describe the extravasation risk and management strategies for Docetaxel.
The extravasation risk and management strategies for this drug are as follows: - Irritant with vesicant-like properties
272
Describe the extravasation risk and management strategies for the Taxanes class.
The extravasation risk and management strategies for this drug class are as follows: - Paclitaxel and Docetaxel are irritants with vesicant-like properties - NabPaclitaxel may be an irritant
273
Describe the administration of Docetaxel.
The administration of this drug is described as follows: - Use Low-sorb tubing BUT NO IN-LINE FILTER
274
Describe the administration of Cabazitaxel.
The administration of this drug is described as follows: - Use Low-sorb tubing with an in-line filter
275
Describe the administration of Paclitaxel.
The administration of this drug is described as follows: - Use Low-sorb tubing with an in-line filter
276
Describe the general techniques for administration of the Taxanes class.
The general techniques for administration of this drug class is described as follows: - Paclitaxel and Cabazitaxel require low-sorb tubing and in-line filter - Docetaxel requires low-sorb tubing BUT NO IN-LINE FILTER
277
Describe the metabolism of Docetaxel.
The metabolism of this drug is as follows: - Primarily hepatic metabolism by CYP3A4 (CYP2C8 minor). - Dose adjustments are recommended in patients with hepatic impairment.
278
Describe the metabolism of Cabazitaxel.
The metabolism of this drug is as follows: - Primarily hepatic metabolism by CYP3A4/3A5 (CYP2C8 minor). - Dose adjustments are recommended in patients with hepatic impairment.
279
Describe the metabolism of Paclitaxel.
The metabolism of this drug is as follows: - Primarily hepatic metabolism by CYP2C8 (CYP3A4 minor). - Dose adjustments are recommended in patients with hepatic impairment.
280
Describe the metabolism of NabPaclitaxel.
The metabolism of this drug is as follows: - Primarily hepatic metabolism by CYP2C8 (CYP3A4 minor). - Dose adjustments are recommended in patients with hepatic impairment.
281
What are the notable ADRs of Paclitaxel?
The notable ADRs of this drug are: - Infusion reactions
282
What are the notable ADRs of Docetaxel?
The notable ADRs of this drug are: - Peripheral edema (black box warning)
283
Describe the strategy and rationale for management of infusion reactions caused by Paclitaxel.
The strategy and rationale for management of this condition caused by this drug are: - This drug has poor water solubility and is thus formulated with a polyethoxylated castor oil (Cremophor). - This viscous solution is likely to cause hypersensitivity reactions, but these reactions are due to the Cremophor (not the drug itself). - In order to prevent these reactions, patients should be premedicated with antihistamines and corticosteroids. Typically, patients receive dexamethasone 10-20 mg oral 12 and 6 hours prior to the infusion, plus diphenhydramine 50 mg IV and ranitidine 50 mg IV 30 minutes prior to the infusion.
284
Describe the strategy and rationale for management of peripheral edema caused by Docetaxel.
The strategy and rationale for management of this condition caused by this drug are: - Characterized by pleural effusions (requiring immediate drainage), ascites with pronounced abdominal distention, peripheral edema, dyspnea at rest, cardiac tamponade, and/or generalized edema. - Premedication with corticosteroids for 3 days, beginning the day before drug administration, is recommended to prevent pulmonary/peripheral edema. - Patients typically receive dexamethasone 8mg oral twice daily 1 day prior to drug and continuing for 2 days after.
285
What are the clinical pearls of NabPaclitaxel?
The clinical pearls of this drug are as follows: - Not interchangeable with other paclitaxel formulations and cannot be substituted for conventional paclitaxel.
286
What is the history of the Taxanes class?
The history of this drug class is as follows: - Discovered in 1971 by NCI researchers during a plant screening program when a crude extract with anti-tumor activity was isolated from the bark of the Pacific Yew, Taxus brevifolia. - But the amount of paclitaxel in yew bark was small and extracting it was complicated and expensive and the collection of Pacific Yew bark also became restricted for environmental reasons. - This led to production of semi-synthetic form of paclitaxel derived from the needles of the Himalayan yew tree, Taxus bacatta.
287
What drug(s) of the Taxanes class is notable for causing Peripheral Edema?
The drugs in this class notable for cause this condition are: - Docetaxel
288
What drug(s) of the Taxanes class is notable for causing Infusion Reactions?
The drugs in this class notable for cause this condition are: - Paclitaxel (due to Cremophor)
289
What drugs are in the Topoisomerase Inhibitors class?
Drugs in this class are: - lrinotecan - Topotecan - Etoposide - Teniposide - Mitoxantrone
290
What is the brand name of lrinotecan?
The brand name of this generic drug is: - Camptosar
291
What is the brand name of Topotecan?
The brand name of this generic drug is: - Hycamtin
292
What is the brand name of Etoposide?
The brand name of this generic drug is: - Toposar, Vepesid, VP16
293
What is the brand name of Teniposide?
The brand name of this generic drug is: - VM26
294
What is the brand name of Mitoxantrone?
The brand name of this generic drug is: - Novantrone
295
What is the generic of name of Camptosar?
The generic name of this brand name drug is: - lrinotecan
296
What is the generic of name of Hycamtin?
The generic name of this brand name drug is: - Topotecan
297
What is the generic of name of Toposar?
The generic name of this brand name drug is: - Etoposide
298
What is the generic of name of Vepesid?
The generic name of this brand name drug is: - Etoposide
299
What is the generic of name of VP16?
The generic name of this brand name drug is: - Etoposide
300
What is the generic of name of VM26?
The generic name of this brand name drug is: - Teniposide
301
What is the generic of name of Novantrone?
The generic name of this brand name drug is: - Mitoxantrone
302
What are the main indications for use of lrinotecan?
The main indications of this drug are: - Non-Small Cell Lung Cancer - Small Cell Lung Cancer - Colorectal Cancer - Esophageal Cancer - Gastric Cancer - Pancreatic Cancer
303
What are the main indications for use of Topotecan?
The main indications of this drug are: - Small Cell Lung Cancer - Cervical Cancer - CNS Malignancy - Ewing Sarcoma - Ovarian Cancer - Rhabdomyosarcoma
304
What are the main indications for use of Etoposide?
The main indications of this drug are: - Breast Cancer - Hematopoietic Stem Cell Transplant - Hemophagocytic Lymphohistiocytosis - Hodgkin Lymphoma - Non-Hodgkin Lymphoma - Non-Small Cell Lung Cancer - Small Cell Lung Cancer - Testicular Cancer
305
What is the class and MOA of lrinotecan?
This drug in the following class: - Topoisomerase I Inhibitors This drug's MOA is as follows: - Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology. - DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase I introduces single stranded nicks into DNA to allow DNA relaxation. - In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.
306
What is the class and MOA of Topotecan?
This drug in the following class: - Topoisomerase I Inhibitors This drug's MOA is as follows: - Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology. - DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase I introduces single stranded nicks into DNA to allow DNA relaxation. - In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.
307
What is the class and MOA of Etoposide?
This drug in the following class: - Topoisomerase II Inhibitors (Podophyllotoxin Derivative) This drug's MOA is as follows: - Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology. - DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase II introduces double stranded nicks into DNA to allow DNA relaxation. - In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.
308
What is the class and MOA of Teniposide?
This drug in the following class: - Topoisomerase II Inhibitors (Podophyllotoxin Derivative) This drug's MOA is as follows: - Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology. - DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase II introduces double stranded nicks into DNA to allow DNA relaxation. - In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.
309
What is the class and MOA of Mitoxantrone?
This drug in the following class: - Topoisomerase II Inhibitors (Anthracenedione) This drug's MOA is as follows: - Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology. - DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase II introduces double stranded nicks into DNA to allow DNA relaxation. - In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.
310
What is the emetic potential of Etoposide?
The emetic potential of this drug is: - Low
311
What is the emetic potential of Topotecan?
The emetic potential of this drug is: - Low
312
What is the emetic potential of Irinotecan?
The emetic potential of this drug is: - Moderate
313
What is the emetic potential of Teniposide?
The emetic potential of this drug is: - Low
314
What is the emetic potential of Mitoxantrone?
The emetic potential of this drug is: - Low
315
Describe the emetic potential of the Topoisomerase Inhibitors class.
The emetic potential of this drug class is: - All low except for topotecan (moderate)
316
Describe the extravasation risk and management strategies for the Topoisomerase Inhibitors class.
The extravasation risk and management strategies for this drug class are as follows: - All irritants except for mitoxantrone (irritant with vesicant like properties)
317
Describe the metabolism of lrinotecan.
The metabolism of this drug is as follows: - In patients with hepatic dysfunction, clearance is decreased and exposure to the active metabolite (SN-38) is increased proportional to the degree of hepatic impairment.
318
Describe the metabolism of Etoposide.
The metabolism of this drug is as follows: - In renal function impairment, total body clearance is reduced, AUC is increased, and Vd is lower.
319
Describe the metabolism of Topotecan.
The metabolism of this drug is as follows: - AUC after oral administration is 30% higher in Asian patients as compared to white patients.
320
What are the notable ADRs of lrinotecan?
The notable ADRs of this drug are: - Diarrhea - Neutropenia if homozygous for the UGT1A1*28 allele
321
What drug(s) of the Topoisomerase Inhibitors class is notable for causing Diarrhea?
The drugs in this class notable for cause this condition are: - Irinotecan
322
Describe the strategy and rationale for management of EARLY onset diarrhea caused by Irinotecan.
The strategy and rationale for management of this condition caused by this drug are: - Early-onset diarrhea occurs during or within 24 hours of infusion. - This is caused by direct inhibition of acetylcholinesterase by the drug and is accompanied with cholinergic symptoms such as cramps, diaphoresis, flushing, salivation, visual disturbances, and lacrimation. - Acute diarrhea is treated with atropine 0.25-1 mg SO or IV. Patients may also be given atropine as secondary prophylaxis after experiencing acute diarrhea in previous chemotherapy cycles.
323
Describe the strategy and rationale for management of LATE onset diarrhea caused by Irinotecan.
The strategy and rationale for management of this condition caused by this drug are: - Late-onset diarrhea is the dose limiting toxicity of this drug and typically occurs >24 hours after drug administration (median time to onset is 6 days). - This is thought to occur due to secretory processes caused by the active metabolite of the drug. - Late onset diarrhea is treated with high dose loperamide and supportive care including fluids if needed. - Patient should be instructed to take loperamide 4 mg at first sign of diarrhea, followed by 2 mg every 2 hours (4 mg every 4 hours at night) until 12 hours following last bowel movement up to 24 mg/day. Exceeding the daily limit of loperamide 16 mg/day is recommended for treatment of irinotecan-associated diarrhea in adults. - Atropine has no role in the treatment of late onset diarrhea.
324
Describe the strategy and rationale for management of neutropenia caused by Irinotecan.
The strategy and rationale for management of this condition caused by this drug are: - A test is available for genotyping of UGT1A1, however, use of the test is not widely accepted as dose reductions are already recommended in patients who have experienced toxicity regardless of genotype.
325
What are the risk factors for developing neutropenia with Irinotecan?
Risk factors for developing this ADR with this drug/class are: - Homozygous for the UGT1A1*28 allele are at increased risk. - Heterozygous carriers may also be at increased neutropenic risk, however, most patients have tolerated normal starting doses
326
What drugs are in the Vinca Alkaloids class?
Drugs in this class are: - Vincristine - Vinorelbine - Vinblastine
327
What is the brand name of Vincristine?
The brand name of this generic drug is: - Oncovin
328
What is the brand name of Vinorelbine?
The brand name of this generic drug is: - Navelbine
329
What is the brand name of Vinblastine?
The brand name of this generic drug is: - Velban
330
What is the generic of name of Oncovin?
The generic name of this brand name drug is: - Vincristine
331
What is the generic of name of Navelbine?
The generic name of this brand name drug is: - Vinorelbine
332
What is the generic of name of Velban?
The generic name of this brand name drug is: - Vinblastine
333
What are the main indications for use of Vincristine?
The main indications of this drug are: - Acute Lymphoblastic Leukemia - Non-Hodgkin Lymphoma - Rhabdomyosarcoma - Central nervous system tumors - Chronic lymphocytic leukemia/small lymphocytic leukemia - Ewing sarcoma - Hodgkin Lymphoma
334
What are the main indications for use of Vinorelbine?
The main indications of this drug are: - Hodgkin Lymphoma - Soft Tissue Sarcoma - Non-small cell Lung cancer - Small-cell Lung cancer - Breast Cancer - Cervical Cancer - Ovarian cancer - Mesothelioma
335
What are the main indications for use of Vinblastine?
The main indications of this drug are: - Hodgkin Lymphoma - Soft Tissue Sarcoma - Testicular cancer - Kaposi Sarcoma - Bladder cancer - Non-small cell Lung cancer
336
What is the class and MOA of Vincristine?
This drug in the following class: - Vinca Alkaloids This drug's MOA is as follows: - Binds to tubulin and inhibits microtubule formation stopping cell growth by disrupting the formation of the mitotic spindle. These drugs specifically target the M and S phases of the cell cycle.
337
What is the class and MOA of Vinorelbine?
This drug in the following class: - Vinca Alkaloids This drug's MOA is as follows: - Binds to tubulin and inhibits microtubule formation stopping cell growth by disrupting the formation of the mitotic spindle. These drugs specifically target the M and S phases of the cell cycle.
338
What is the class and MOA of Vinblastine?
This drug in the following class: - Vinca Alkaloids This drug's MOA is as follows: - Binds to tubulin and inhibits microtubule formation stopping cell growth by disrupting the formation of the mitotic spindle. These drugs specifically target the M and S phases of the cell cycle.
339
What is the emetic potential of Vincristine?
The emetic potential of this drug is: - Minimal
340
What is the emetic potential of Vinorelbine?
The emetic potential of this drug is: - Minimal
341
What is the emetic potential of Vinblastine?
The emetic potential of this drug is: - Minimal
342
Describe the emetic potential of the Vinca Alkaloids class.
The emetic potential of this drug class is: - All are minimal
343
Describe the extravasation risk and management strategies for the Vinca Alkaloids class.
The extravasation risk and management strategies for this drug class are as follows: - All are vesicants - If extravasation occurs, stop infusion immediately and gently aspirate extravasated solution (do not flush the line). - Initiate hyaluronidase antidote and apply warm dry compresses for 20 minutes four times a day for 1-2 days.
344
Describe the general techniques for administration of the Vinca Alkaloids class.
The general techniques for administration of this drug class is described as follows: - These agents are for IV use only and are FATAL if administered intrathecally - The Institute for Safe Mediation Practices (ISMP) recommends dispensing vinca alkaloids in a mini-bag (not a syringe) to prevent inadvertent intrathecal administration. - Vincristine is commonly used in the treatment of adult and pediatric ALL which also includes frequent administration of intrathecal chemotherapy. ISMP has reported 135 fatalities worldwide due to inadvertent intrathecal administration of vincristine. all of which were dispensed in a syringe.
345
Describe the metabolism of the Vinca Alkaloids class.
The metabolism of this drug is as follows: - Extensively hepatic metabolism, mostly via CYP3A4
346
What are the notable ADRs of Vincristine?
The notable ADRs of this drug are: - When used as a single agent, this drug does not typically cause myelosuppression - Neuropathy (peripheral and autonomic [constipation])
347
What are the notable ADRs of Vinorelbine?
The notable ADRs of this drug are: - This drug can typically cause cytopenias - Neuropathy (peripheral and autonomic [constipation])
348
What are the notable ADRs of Vinblastine?
The notable ADRs of this drug are: - This drug can typically cause cytopenias - Neuropathy (peripheral and autonomic [constipation])
349
What are the notable/common ADRs of the Vinca Alkaloids class?
The notable/common ADRs of this drug class are: - When used as a single agent, Vincristine does not typically cause myelosuppression. Vinorelbine and vinblastine however can both cause cytopenias. - Neuropathy (most common dose limiting side effect of this drug class)
350
Describe the strategy and rationale for management of Neuropathy caused by the Vinca Alkaloids.
The strategy and rationale for management of this condition caused by this drug class are: - This is the most common dose limiting side effect of this drug class. - This can not only affect the peripheral nerves (leading to numbness and tingling in the extremities) but it can also affect the autonomic nerves leading to constipation. - Patients should be on an aggressive bowel regimen while receiving drugs in this class and be evaluated for neuropathy at every visit. - The presence of peripheral neuropathy may require a dose reduction or omission of the vinca alkaloid.
351
Describe the strategy and rationale for management of hepatic dysfunction when using Vinca Alkaloids.
The strategy and rationale for management of this condition caused by this drug class are: - All of the vinca alkaloids are hepatically metabolized and require hepatic dose adjustments. - The only exception is based on clinical judgement if the liver dysfunction is known to be due to the disease.
352
Describe the history of the Vinca Alkaloids.
The history of this drug class is as follows: - They are derived from the Madagascar periwinkle plant, Vinca rosea. - This plant was said to be useful in the treatment of diabetes. Attempts to verify the antidiabetic properties of the plants extracts in the 1950's led instead to the discovery and isolation of vinblastine. - Scientists first observed vinblastine's anticancer properties in a lab in 1962 with the observation of regression of lymphocytic leukemia in rats.
353
What drugs are in the Aromatase Inhibitors class?
Drugs in this class are: - Anastrozole - Exemestane - Letrozole
354
What is the brand name of Anastrozole?
The brand name of this generic drug is: - Arimidex
355
What is the brand name of Exemestane?
The brand name of this generic drug is: - Aromasin
356
What is the brand name of Letrozole?
The brand name of this generic drug is: - Femara
357
What is the generic of name of Arimidex?
The generic name of this brand name drug is: - Anastrozole
358
What is the generic of name of Aromasin?
The generic name of this brand name drug is: - Exemestane
359
What is the generic of name of Femara?
The generic name of this brand name drug is: - Letrozole
360
What are the main/common indications of the Aromatase Inhibitors class?
The main/common indications of this drug class are: - Breast Cancer
361
What is the class and MOA of Anastrozole?
This drug in the following class: - Aromatase Inhibitors This drug's MOA is as follows: - Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen. - This thus reduces estrogen mediated stimulation of breast cancer tissue - This one is a non-steroidal aromatase inhibitor - it decreases estrogen synthesis without compromising adrenal steroid synthesis
362
What is the class and MOA of Exemestane?
This drug in the following class: - Aromatase Inhibitors This drug's MOA is as follows: - Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen. - This thus reduces estrogen mediated stimulation of breast cancer tissue - This one is a steroidal aromatase inhibitor - it has a similar structure to androgen and irreversibly binds to aromatase
363
What is the class and MOA of Letrozole?
This drug in the following class: - Aromatase Inhibitors This drug's MOA is as follows: - Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen. - This thus reduces estrogen mediated stimulation of breast cancer tissue - This one is a non-steroidal aromatase inhibitor - it decreases estrogen synthesis without compromising adrenal steroid synthesis
364
What are the notable/common monitoring parameters for the Aromatase Inhibitors class?
The notable/common monitoring parameters for this drug class are: - Baseline and periodic bone mineral density screening (every 1 to 2 years). - Cholesterol and hepatic function tests at baseline and periodically during therapy.
365
Describe the emetic potential of the Aromatase Inhibitors class.
The emetic potential of this drug class is: - None, N/A
366
Describe the extravasation risk and management strategies for the Aromatase Inhibitors class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A (all are oral)
367
Describe the metabolism of the Aromatase Inhibitors class.
The metabolism of this drug class is as follows: - Extensively hepatic
368
What are the notable/common ADRs of the Aromatase Inhibitors class?
The notable/common ADRs of this drug class are: - Musculoskeletal side effects including carpal tunnel. arthralgias. joint stiffness. and/or bone pain
369
Describe the strategy and rationale for management of Musculoskeletal side effects caused by Aromatase Inhibitors.
The strategy and rationale for management of this condition caused by these drugs are: - This includes carpal tunnel, arthralgias, joint stiffness, and/or bone pain. - In up to 1/3 of patients these symptoms can be severe and may be the cause of treatment discontinuation in 10-20% of patients on Als. - The best strategy for managing these adverse effects includes exercise and nonsteroidal anti-inflammatory drugs.
370
What are the clinical pearls of the Aromatase Inhibitors class?
The clinical pearls of this drug class are as follows: - 70% estradiol reduction after 24 hours; 80% after 2 weeks of therapy - Aromatase inhibitors work in the peripheral fat to decrease estrogen synthesis. - In pre-menopausal women, estrogen is also produced by the ovaries so aromatase inhibitors are NOT effective therapy as monotherapy for pre-menopausal women. Some sort of ovarian suppression must be used in pre-menopausal women receiving Als. - An Al is the preferred adjuvant treatment of post-menopausal women, although tamoxifen is an acceptable alternative for women who are intolerant of Als. - Data shows similar clinical outcomes and tolerability between the AIs. Individuals may tolerate one of these agents better than another. Consider switching to an alternative Al if the initial Al is poorly tolerated and strategies to manage the side effects have been ineffective. - ASCO recommends a maximum duration of 5 years of AI therapy for postmenopausal women. Als may be combined with tamoxifen for a total duration of up to 10 years of endocrine therapy. - Aromatase inhibitors are currently being studied as risk reduction agents in post-menopausal women at a high risk for breast cancer
371
What drugs are in the Estrogen Receptor Antagonists class?
Drugs in this class are: - Tamoxifen - Fulvestrant - Elacestrant - Toremifene
372
What is the brand name of Tamoxifen?
The brand name of this generic drug is: - Soltamox - Nolvadex
373
What is the brand name of Fulvestrant?
The brand name of this generic drug is: - Faslodex
374
What is the brand name of Elacestrant?
The brand name of this generic drug is: - Orserdu
375
What is the brand name of Toremifene?
The brand name of this generic drug is: - Fareston
376
What is the generic of name of Soltamox?
The generic name of this brand name drug is: - Tamoxifen
377
What is the generic of name of Nolvadex?
The generic name of this brand name drug is: - Tamoxifen
378
What is the generic of name of Faslodex?
The generic name of this brand name drug is: - Fulvestrant
379
What is the generic of name of Orserdu?
The generic name of this brand name drug is: - Elacestrant
380
What is the generic of name of Fareston?
The generic name of this brand name drug is: - Toremifene
381
What are the main/common indications of the Estrogen Receptor Antagonists class?
The main/common indications of this drug class are: - Breast Cancer
382
What is the class and MOA of Tamoxifen?
This drug in the following class: - Estrogen Receptor Antagonists This drug's MOA is as follows: - Binds to estrogen receptors on tumors and other tissue targets inhibiting estrogens effects and thus tumor growth
383
What is the class and MOA of Fulvestrant?
This drug in the following class: - Estrogen Receptor Antagonists This drug's MOA is as follows: - Binds to estrogen receptors on tumors and other tissue targets inhibiting estrogens effects and thus tumor growth
384
What is the class and MOA of Elacestrant?
This drug in the following class: - Estrogen Receptor Antagonists - Selective estrogen receptor degrader (SERD) This drug's MOA is as follows: - Elacestrant is an estrogen receptor antagonist and nonsteroidal selective estrogen receptor degrader (SERD), which degrades estrogen receptor alpha in a dose-dependent manner, and inhibits estradiol-dependent estrogen-receptor directed gene transcription and tumor growth.
385
What is the class and MOA of Toremifene?
This drug in the following class: - Estrogen Receptor Antagonists This drug's MOA is as follows: - Binds to estrogen receptors on tumors and other tissue targets inhibiting estrogens effects and thus tumor growth
386
What are the notable/common monitoring parameters for the Estrogen Receptor Antagonists class?
The notable/common monitoring parameters for this drug class are: - Bone mineral density at baseline and periodically during treatment (every 1-2 years) - Gynecologic exam (baseline and annually, continuing after discontinuation of therapy) - Liver function tests periodically during therapy
387
Describe the emetic potential of the Estrogen Receptor Antagonists class.
The emetic potential of this drug class is: - None, N/A
388
Describe the extravasation risk and management strategies for the Estrogen Receptor Antagonists class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A (all are oral)
389
Describe the metabolism of the Estrogen Receptor Antagonists class.
The metabolism of this drug class is as follows: - Primarily hepatic (mainly CYP2D6 for tamoxifen, mainly CYP3A4 for the others)
390
What are the notable ADRs of Tamoxifen?
The notable ADRs of this drug are: - Hot flashes - Thromboembolism - Endometrial malignancies
391
What are the notable/common ADRs of the Estrogen Receptor Antagonists class?
The notable/common ADRs of this drug class are: - See tamoxifen (possible class effect?)
392
What drug(s) of the Estrogen Receptor Antagonists class is notable for causing hot flashes?
The drugs in this class notable for cause this condition are: - Tamoxifen (possible class effect?)
393
What drug(s) of the Estrogen Receptor Antagonists class is notable for causing thromboembolism?
The drugs in this class notable for cause this condition are: - Tamoxifen (possible class effect?)
394
What drug(s) of the Estrogen Receptor Antagonists class is notable for causing endometrial malignancies?
The drugs in this class notable for cause this condition are: - Tamoxifen (possible class effect?)
395
Describe the strategy and rationale for management of hot flashes caused by tamoxifen.
The strategy and rationale for management of this condition caused by this drug are: - Chemotherapy + this drug can cause more frequent and severe hot flashes than natural menopause, which often results in decreased quality of life and may affect medication adherence. - This is thought to be due to a central nervous system antiestrogenic effects causing thermoregulatory dysfunction. - 80% of women prescribed this drug complain of hot flashes, with 30% of those having severe symptoms. - Venlafaxine 75 mg orally daily has been shown to be more effective in managing hot flashes when compared to placebo, clonidine and gabapentin. - Data also supports the use of paroxetine*, fluoxetine*, sertraline, and citalopram to manage hot flashes. - *Drug interaction with CYP2D6
396
Describe the strategy and rationale for management of thromboembolism caused by tamoxifen.
The strategy and rationale for management of this condition caused by this drug are: - There is a significant procoagulant effect when this drug is added to chemotherapy.
397
Describe the strategy and rationale for management of thromboembolism caused by endometrial malignancies.
The strategy and rationale for management of this condition caused by this drug are: - Women taking tamoxifen should be informed about the risks of endometrial proliferation, endometrial hyperplasia, endometrial cancer, and uterine sarcomas. - The risk of developing endometrial cancer from tamoxifen is about 1 in 500. - Any abnormal vaginal bleeding, bloody vaginal discharge, or spotting should be investigated in post-menopausal women. - Premenopausal women treated with tamoxifen have no known increased risk of uterine cancer and require no additional monitoring beyond routine gynecologic care.
398
What are the risk factors for developing hot flashes with by tamoxifen?
Risk factors for developing this ADR with this drug/class are: - Coadministration with chemotherapy? - Premenopausal women - Polymorphisms in drug metabolizing enzymes - Coadministration of drugs that inhibit the activity of CYP2D6 - Specific estrogen receptor genotypes
399
What are the risk factors for developing thromboembolism with by tamoxifen?
Risk factors for developing this ADR with this drug/class are: - Coadministration with chemotherapy? - The relative risks of venous thromboembolism are increased 2-3-fold in older women receiving tamoxifen and this elevated risk continues as long as the patient takes the drug.
400
What are the clinical pearls of Tamoxifen?
The clinical pearls of this drug are as follows: - Oral solution is bioequivalent to tamoxifen tablets - It is the endocrine agent of choice for the adjuvant treatment of premenopausal women with breast cancer and for postmenopausal women who are not candidates for an aromatase inhibitor for whatever reason. - Converted to its active metabolites by CYP2D6 and UGT2B7 - drugs that inhibit CYP2D6 (fluoxetine and paroxetine) may potentially alter the metabolism of tamoxifen. - Unlike the aromatase inhibitors, this drug may help prevent bone loss and lowers total cholesterol
401
What are the clinical pearls of the Estrogen Receptor Antagonists class?
The clinical pearls of this drug class are as follows: - See tamoxifen (possible class effect?)
402
What drugs are in the GNRH Agonists class?
Drugs in this class are: - Triptorelin - Goserelin - Leuprolide - Histrelin
403
What is the brand name of Triptorelin?
The brand name of this generic drug is: - Trelstar Mixject - Triptodur
404
What is the brand name of Goserelin?
The brand name of this generic drug is: - Zoladex
405
What is the brand name of Leuprolide?
The brand name of this generic drug is: - Camcevi - Eligard - Fensolvi - Lupron
406
What is the brand name of Histrelin?
The brand name of this generic drug is: - Vantas
407
What is the generic of name of Trelstar Mixject?
The generic name of this brand name drug is: - Triptorelin
408
What is the generic of name of Triptodur?
The generic name of this brand name drug is: - Triptorelin
409
What is the generic of name of Zoladex?
The generic name of this brand name drug is: - Goserelin
410
What is the generic of name of Camcevi?
The generic name of this brand name drug is: - Leuprolide
411
What is the generic of name of Eligard?
The generic name of this brand name drug is: - Leuprolide
412
What is the generic of name of Fensolvi?
The generic name of this brand name drug is: - Leuprolide
413
What is the generic of name of Lupron?
The generic name of this brand name drug is: - Leuprolide
414
What is the generic of name of Vantas?
The generic name of this brand name drug is: - Histrelin
415
What are the main indications for use of Triptorelin?
The main indications of this drug are: - Prostate Cancer - Endometrial stromal sarcoma
416
What are the main indications for use of Goserelin?
The main indications of this drug are: - Prostate Cancer - Breast Cancer - Prevention of early menopause during chemotherapy
417
What are the main indications for use of Leuprolide?
The main indications of this drug are: - Prostate Cancer - Breast Cancer - Prevention of early menopause during chemotherapy
418
What are the main/common indications of the GNRH Agonists class?
The main/common indications of this drug class are: - Prostate Cancer (primary) - Breast Cancer
419
What is the class and MOA of Triptorelin?
This drug in the following class: - GNRH Agonists This drug's MOA is as follows: - Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.
420
What is the class and MOA of Goserelin?
This drug in the following class: - GNRH Agonists This drug's MOA is as follows: - Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.
421
What is the class and MOA of Leuprolide?
This drug in the following class: - GNRH Agonists This drug's MOA is as follows: - Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.
422
What is the class and MOA of Histrelin?
This drug in the following class: - GNRH Agonists This drug's MOA is as follows: - Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.
423
What are the notable/common monitoring parameters for the GNRH Agonists class?
The notable/common monitoring parameters for this drug class are: - Serum testosterone levels - Prostate-specific antigen to monitor response to therapy
424
Describe the emetic potential of the GNRH Agonists class.
The emetic potential of this drug class is: - None, N/A
425
Describe the extravasation risk and management strategies for the GNRH Agonists class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
426
Describe the administration of Triptorelin.
The administration of this drug is described as follows: - Given IM by a healthcare provider - Canadian product can be given SubQ
427
Describe the administration of Goserelin.
The administration of this drug is described as follows: - This drug is an implant that is administered/implanted SubQ
428
Describe the administration of Leuprolide.
The administration of this drug is described as follows: - Administered SubQ expect for depot formulations (IM)
429
Describe the administration of Histrelin.
The administration of this drug is described as follows: - This drug is an implant that is surgically implanted SubQ
430
What are the notable/common ADRs of the GNRH Agonists class?
The notable/common ADRs of this drug class are: - Long term use can cause ADRs related to decreased testosterone levels including osteoporosis, bone fractures. obesity, insulin resistance, hyperlipidemia, and increased risk of diabetes/cardiovascular events. - Disease flare - Gynecomastia - Hot flashes - Erectile dysfunction - Edema - Injection site reactions
431
Describe the strategy and rationale for management of disease flare caused by GNRH Agonists.
The strategy and rationale for management of this condition caused by this drug are: - This is thought to be caused by initial induction of luteinizing hormone (LH) and follicte stimulating hormone (FSH) by the GNRH agonist. - This can manifest as increased bone pain or increased urinary symptoms. - Antiandrogen therapy should be started before beginning a GNRH agonist and be continued in combination for at least 7 days for patients with metastases to help reduce tumor flare. - This flare reaction usually resolves after 2 weeks and has a similar onset and duration pattern between the depot and regular acting GNRH agonists.
432
Describe the onset of GNRH Agonists.
The onset of drugs in this class is described as follows: - Following a transient increase, testosterone suppression occurs at ~2 to 4 weeks of continued therapy
433
What are the clinical pearls of the GNRH Agonists class?
The clinical pearls of this drug class are as follows: - Also referred to as luteinizing hormone-releasing hormone (LHRH) agonists - GnRH agonists are a reversible method of androgen ablation and are as effective as orchiectomy in treating prostate cancer - In the context of prostate cancer, goal is to induce castrate levels of testosterone. - This can be accomplished by surgical castration (orchiectomy) or medical/chemical castration (GNRH agonists or antagonists). - When using GNRH agonists, the goal serum testosterone level is <50 ng/dl after 1 month of therapy. - Use in combination with antiandrogen to reduce disease flare
434
What drugs are in the Immune Modulators (IMiDs) class?
Drugs in this class are: - Lenalidomide - Pomalidomide - Thalidomide
435
What is the brand name of Lenalidomide?
The brand name of this generic drug is: - Revlimid
436
What is the brand name of Pomalidomide?
The brand name of this generic drug is: - Pomalyst
437
What is the brand name of Thalidomide?
The brand name of this generic drug is: - Thalomid
438
What is the generic of name of Revlimid?
The generic name of this brand name drug is: - Lenalidomide
439
What is the generic of name of Pomalyst?
The generic name of this brand name drug is: - Pomalidomide
440
What is the generic of name of Thalomid?
The generic name of this brand name drug is: - Thalidomide
441
What are the main indications for use of Lenalidomide?
The main indications of this drug are: - Multiple Myeloma - Non-Hodgkin Lymphoma - Myelodysplastic Syndrome - CLL
442
What are the main indications for use of Pomalidomide?
The main indications of this drug are: - Multiple Myeloma - Pomalidomide - Kaposi Sarcoma
443
What are the main indications for use of Thalidomide?
The main indications of this drug are: - Multiple Myeloma
444
What are the main/common indications of the Immune Modulators (IMiDs) class?
The main/common indications of this drug class are: - Multiple Myeloma
445
What is the class and MOA of Lenalidomide?
This drug in the following class: - Immune Modulators (IMiDs) This drug's MOA is as follows: - The mechanism of action is still under investigation but it is believed to exert direct cytotoxic effects on the tumor cells causing apoptosis
446
What is the class and MOA of Pomalidomide?
This drug in the following class: - Immune Modulators (IMiDs) This drug's MOA is as follows: - The mechanism of action is still under investigation but it is believed to exert direct cytotoxic effects on the tumor cells causing apoptosis
447
What is the class and MOA of Thalidomide?
This drug in the following class: - Immune Modulators (IMiDs) This drug's MOA is as follows: - The mechanism of action is still under investigation but it is believed to exert direct cytotoxic effects on the tumor cells causing apoptosis
448
What are the notable/common monitoring parameters for the Immune Modulators (IMiDs) class?
The notable/common monitoring parameters for this drug class are: - Females of reproductive potential should receive a pregnancy test 10 to 14 days and 24 hours prior to initiating therapy, weekly during the first 4 weeks of treatment, then every 2 to 4 weeks through 4 weeks after therapy discontinued.
449
Describe the emetic potential of the Immune Modulators (IMiDs) class.
The emetic potential of this drug class is: - Minimal-Low
450
Describe the extravasation risk and management strategies for the Immune Modulators (IMiDs) class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
451
Describe the metabolism of the Immune Modulators (IMiDs) class.
The metabolism of this drug is as follows: - Excreted primarily as unchanged drug in the urine (70-90%)
452
What are the notable/common ADRs of the Immune Modulators (IMiDs) class?
The notable/common ADRs of this drug class are: - Risk of birth defects (fetal death; limb (seal-like), eye, urinary tract, and heart problems). - Thromboembolism
453
Describe the strategy and rationale for management of birth defects caused by the Immune Modulator (IMiDs) class.
The strategy and rationale for management of this condition caused by drugs in this class are: - Women of childbearing potential need to be on effective contraception for at least 4 weeks prior to starting therapy, during therapy, and for at least 4 weeks after discontinuing therapy. - Pregnancy screening should be done prior to initiating therapy and pregnancy must be excluded by 2 negative pregnancy tests. - During the first month of therapy patients are required to undergo weekly pregnancy tests, then monthly thereafter in women with regular menstrual cycles or every 2 weeks for women with irregular menstrual cycles while on treatment. - If pregnancy does occur, therapy must be discontinued. - Drug is present in semen so male patients are required to use condoms during any sexual contact with females of childbearing potential while on treatment and for up to 28 days after receiving therapy and must not donate sperm.
454
Describe the strategy and rationale for management of thromboembolism caused by the Immune Modulator (IMiDs) class.
The strategy and rationale for management of this condition caused by drugs in this class are: - All patients receiving these drugs need some sort of VTE prophylaxis. - The SAVED score can estimate VTE risk and takes into account: recent surgeries, race, VTE history, age, and dexamethasone dosing to estimate VTE risk while taking these drugs. - Patients at low risk for VTE (per the SAVED score) can receive aspirin 81 mg once daily. - High risk patients should receive full dose warfarin (target INR 2-3), enoxaparin 40 mg daily, Dalteparin 5,000 units daily, or apixaban 2-5 mg every 12 hours. - Patient can also receive full dose anticoagulation if indicated for another medical condition.
455
What are the clinical pearls of the Immune Modulators (IMiDs) class?
The clinical pearls of this drug class are as follows: - All of these drugs have a REMS program with restrictions for prescribing and dispensing due to the risk of fetal toxicity. - If patients are deemed transplant eligible, collect stem cells within first 4 cycles of lenalidomide as this increases the likelihood of a successful collection.
456
Describe the history of Thalidomide Babies.
The history of this is as follows: - This drug was first marketed in 1957 in Europe as an over the counter medication. It was said to help with anxiety, trouble sleeping, and morning sickness. - While it was initially thought to be safe in pregnancy, concerns regarding birth defects arose in 1961 and the medication was removed from the market. - It is estimated that 10,000 embryos were affected by the use of thalidomide during pregnancy - of which 40% died at the time of birth. Those who survived had limb (seal-like), eye, urinary tract, and heart problems. - This led to public support for stronger drug laws in the United States and the creation of the Kefauver-Harris drug amendment.
457
What drugs are in the Anti-PD-1 class?
Drugs in this class are: - Nivolumab - Pembrolizumab - Cemiplimab - Dostarlimab - Retifanlimab - Nivolumab+Relatlimab
458
What drugs are in the Anti-PD-L1 class?
Drugs in this class are: - Atezolizumab - Avelumab - Durvalumab
459
What drugs are in the Anti-CTLA4?
Drugs in this class are: - lpilimumab - Tremelimumab
460
What is the brand name of Nivolumab?
The brand name of this generic drug is: - Opdivo
461
What is the brand name of Pembrolizumab?
The brand name of this generic drug is: - Keytruda
462
What is the brand name of Cemiplimab?
The brand name of this generic drug is: - Libtayo
463
What is the brand name of Dostarlimab?
The brand name of this generic drug is: - Jemperli
464
What is the brand name of Retifanlimab?
The brand name of this generic drug is: - Zynyz
465
What is the brand name of Nivolumab+Relatlimab?
The brand name of this generic drug is: - Opdualag
466
What is the brand name of Atezolizumab?
The brand name of this generic drug is: - Tecentriq
467
What is the brand name of Avelumab?
The brand name of this generic drug is: - Bavencio
468
What is the brand name of Durvalumab?
The brand name of this generic drug is: - Imfinzi
469
What is the brand name of lpilimumab?
The brand name of this generic drug is: - Yervoy
470
What is the brand name of Tremelimumab?
The brand name of this generic drug is: - Imjudo
471
What is the generic of name of Opdivo?
The generic name of this brand name drug is: - Nivolumab
472
What is the generic of name of Keytruda?
The generic name of this brand name drug is: - Pembrolizumab
473
What is the generic of name of Libtayo?
The generic name of this brand name drug is: - Cemiplimab
474
What is the generic of name of Jemperli?
The generic name of this brand name drug is: - Dostarlimab
475
What is the generic of name of Zynyz?
The generic name of this brand name drug is: - Retifanlimab
476
What is the generic of name of Opdualag?
The generic name of this brand name drug is: - Nivolumab+Relatlimab
477
What is the generic of name of Tecentriq?
The generic name of this brand name drug is: - Atezolizumab
478
What is the generic of name of Bavencio?
The generic name of this brand name drug is: - Avelumab
479
What is the generic of name of Imfinzi?
The generic name of this brand name drug is: - Durvalumab
480
What is the generic of name of Yervoy?
The generic name of this brand name drug is: - lpilimumab
481
What is the generic of name of Imjudo?
The generic name of this brand name drug is: - Tremelimumab
482
What is the class and MOA of Nivolumab?
This drug in the following class: - Immunotherapy - Anti-PD-1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
483
What is the class and MOA of Pembrolizumab?
This drug in the following class: - Immunotherapy - Anti-PD-1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
484
What is the class and MOA of Cemiplimab?
This drug in the following class: - Immunotherapy - Anti-PD-1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
485
What is the class and MOA of Dostarlimab?
This drug in the following class: - Immunotherapy - Anti-PD-1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
486
What is the class and MOA of Retifanlimab?
This drug in the following class: - Immunotherapy - Anti-PD-1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
487
What is the class and MOA of Nivolumab+Relatlimab?
This drug in the following class: - Immunotherapy - Anti-PD-1 + Anti-LAG-3 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
488
What is the class and MOA of Atezolizumab?
This drug in the following class: - Immunotherapy - Anti-PD-L1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
489
What is the class and MOA of Avelumab?
This drug in the following class: - Immunotherapy - Anti-PD-L1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
490
What is the class and MOA of Durvalumab?
This drug in the following class: - Immunotherapy - Anti-PD-L1 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
491
What is the class and MOA of lpilimumab?
This drug in the following class: - Immunotherapy - Anti-CTLA4 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
492
What is the class and MOA of Tremelimumab?
This drug in the following class: - Immunotherapy - Anti-CTLA4 This drug's MOA is as follows: - Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.
493
What are the notable/common monitoring parameters for the Immunotherapy class?
The notable/common monitoring parameters for this drug class are: - TSH/T4 at baseline and every 4-6 weeks - LFTs (AST, ALT, and bilirubin) at baseline and periodically during treatment - Serum creatinine at baseline and periodically during treatment
494
Describe the emetic potential of the Anti-PD-1 class.
The emetic potential of this drug class is: - Minimal
495
Describe the emetic potential of the Anti-PD-L1 class.
The emetic potential of this drug class is: - Minimal
496
Describe the emetic potential of the Anti-CTLA4 class.
The emetic potential of this drug class is: - Minimal
497
Describe the extravasation risk and management strategies for the Anti-PD-1 class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
498
Describe the extravasation risk and management strategies for the Anti-PD-L1 class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
499
Describe the extravasation risk and management strategies for the Anti-CTLA4 class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
500
What are the notable/common ADRs of the Immunotherapy class Immune Checkpoint inhibitors: Anti-PD-1, Anti-PD-L1, Anti-CTLA4)?
The notable/common ADRs of this drug class are: - Immune related adverse events (irAEs) - These irAEs can affect any organ/tissue in the body (skin, GI tract lungs, liver, thyroid, etc.). - The most common irAEs with these agents are rash, pruritus, diarrhea, colitis, elevated liver enzymes/ bilirubin, hepatitis, hypophysitis, and hypothyroidism.
501
Describe the strategy and rationale for management of irAEs caused by Immunotherapy (Immune Checkpoint inhibitors: Anti-PD-1, Anti-PD-L1, Anti-CTLA4).
The strategy and rationale for management of this condition caused by this drug are: - Patients should be educated on the mechanism of action of immunotherapy and when a new side effect occurs, there should be a high suspicion for it being treatment-related. - Though treatment interruption may be needed for some irAEs depending on severity, dose adjustments are not recommended after restarting therapy following toxicity. - Toxicity Management (except hypothyroidism): - Grade 1 toxicity: Continue immunotherapy with close monitoring - Grade 2 toxicity: Hold immunotherapy (may resume when toxicity< grade 1). Prednisone 0.5-1 mg/kg/day or equivalent may be administered - Grade 3 toxicity: Hold immunotherapy (may resume when toxicity< grade 1). Start prednisone 1-2 mg/ kg/ day or methylprednisolone IV 1-2 mg/kg/day with taper over > 4-6 weeks. If no improvement after 48-72 hours, then consider infliximab - Grade 4 toxicity: Permanently discontinue immunotherapy
502
Describe the strategy and rationale for management of hypothyroidism caused by Immunotherapy (Immune Checkpoint inhibitors: Anti-PD-1, Anti-PD-L1, Anti-CTLA4).
The strategy and rationale for management of this condition caused by this drug are: - Thyroid supplementation in symptomatic patients with TSH levels> 10 mIU/L, monitor every 6-8 weeks while titrating
503
Describe the half-life of Immunotherapy (Immune Checkpoint inhibitors: Anti-PD-1, Anti-PD-L1, Anti-CTLA4).
The half-life of the this drug is described as follows: - The typical half-life of these agents ranges from 15-27 days - This leads to a longer time to tumor response compared to traditional cytotoxic chemotherapy
504
What are the clinical pearls of the Immunotherapy class (Immune Checkpoint inhibitors: Anti-PD-1, Anti-PD-L1, Anti-CTLA4)?
The clinical pearls of this drug class are as follows: - Drug interactions - As steroids are known to reduce the immune response (and are used to treat immune related adverse events), they may diminish the therapeutic effect of Immune Checkpoint Inhibitors. - Carefully consider the need for corticosteroids during the initiation of Immune Checkpoint inhibitor therapy. - Generally, doses of a prednisone-equivalent of 10 mg or less per day are permitted. - Combining nivolumab (anti-PD-1) with ipilimumab (anti-CTLA-4) results in enhanced T-cell function that is greater than that of either antibody alone, resulting in improved anti-tumor responses in metastatic melanoma and advanced renal cell carcinoma.
505
What are the clinical pearls of Pembrolizumab?
The clinical pearls of this drug are as follows: - It was one of the first oncology drugs approved for a specific genetic marker (tumors with high microsatellite instability) regardless of cancer type or tissue diagnosis. - This means that any patient whose tumor is MSI high is eligible to receive this drug.
506
What is the brand name of Trastuzumab?
The brand name of this generic drug is: - Herceptin
507
What is the brand name of Cetuximab?
The brand name of this generic drug is: - Erbitux
508
What is the brand name of Panitumumab?
The brand name of this generic drug is: - Vectibix
509
What is the brand name of Pertuzumab?
The brand name of this generic drug is: - Perjeta
510
What is the brand name of Bevacizumab?
The brand name of this generic drug is: - Avastin
511
What is the brand name of Daratumumab?
The brand name of this generic drug is: - Darzalex
512
What is the brand name of Rituximab?
The brand name of this generic drug is: - Rituxan
513
What is the generic of name of Herceptin?
The generic name of this brand name drug is: - Trastuzumab
514
What is the generic of name of Erbitux?
The generic name of this brand name drug is: - Cetuximab
515
What is the generic of name of Vectibix?
The generic name of this brand name drug is: - Panitumumab
516
What is the generic of name of Perjeta?
The generic name of this brand name drug is: - Pertuzumab
517
What is the generic of name of Avastin?
The generic name of this brand name drug is: - Bevacizumab
518
What is the generic of name of Darzalex?
The generic name of this brand name drug is: - Daratumumab
519
What is the generic of name of Rituxan?
The generic name of this brand name drug is: - Rituximab
520
What is the general MOA of the Monoclonal Antibodies class?
The MOA of this drug class is as follows: - Bind to specific targets (immune cells. cell receptors. tumor molecules. etc.) to exert anti-tumor effects, the specific target varies per antibody. - This leads to very specific anti-tumor effects using biologic agents.
521
What are the notable monitoring parameters for Daratumumab?
The notable monitoring parameters for this drug are: - Type and screen prior to starting therapy (this drug can affect the ability to determine a patient's blood type if a transfusion is needed)
522
What are the notable monitoring parameters for Bevacizumab?
The notable monitoring parameters for this drug are: - Blood pressure and urine protein prior to starting therapy and periodically during treatment
523
What are the notable monitoring parameters for Trastuzumab?
The notable monitoring parameters for this drug are: - Assess left ventricular ejection fraction at baseline, every 3 months during therapy, every 4 weeks if therapy is withheld for significant left ventricular cardiac dysfunction, and every 6 months for at least 2 years following completion of therapy
524
What are the notable monitoring parameters for Pertuzumab?
The notable monitoring parameters for this drug are: - Assess left ventricular ejection fraction at baseline, every 3 months during therapy, every 4 weeks if therapy is withheld for significant left ventricular cardiac dysfunction, and every 6 months for at least 2 years following completion of therapy
525
What are the notable/common monitoring parameters for the Monoclonal Antibodies class?
The notable/common monitoring parameters for this drug class are: - Hepatitis B screening prior to starting therapy (patients may need hepatitis B prophylaxis if positive)
526
Describe the overall emetic potential of the Monoclonal Antibodies class.
The emetic potential of this drug class is: - Minimal
527
Describe the overall extravasation risk and management strategies for the Monoclonal Antibodies class.
The extravasation risk and management strategies for this drug class are as follows: - None, N/A
528
Describe the overall metabolism of the Monoclonal Antibodies class.
The metabolism of drugs in this class is as follows: - Generally, agents undergo intracellular lysosomal degradation
529
What are the notable/common ADRs of the Monoclonal Antibodies class?
The notable/common ADRs of this drug class are: - Infusion Reactions
530
Describe the strategy and rationale for management of infusion reactions caused by Monoclonal Antibodies.
The strategy and rationale for management of this condition caused by this drug are: - Infusion reactions occur due to the immunogenicity of these agents, this can lead to the development of anti-monoclonal antibodies, which can cause acute hypersensitivity reactions. - The risk of reaction varies depending on the species whose proteins form the base of the molecule. Even fully humanized antibodies can cause allergic reactions. - Infusion reactions typically occur in the first 1-2 hours of starting an infusion. They can affect any organ system and range from mildly irritating injection-site reactions, fever or itching/rash to potentially life-threatening anaphylaxis. - Mild reactions are common. Many patients will receive premedication with acetaminophen and diphenhydramine prior to their infusion. - In the event of an infusion reaction, always stop the infusion as soon as possible. From there, treatment depends on the severity of the reaction. - After a mild reaction (slight rash or itching), the infusion can often be continued after temporarily stopping it with a slower infusion rate or additional doses of antipyretics or antihistamines. - More severe reactions (like anaphylaxis) can be managed with epinephrine and may require permeant discontinuation of the drug. - Humanized antibodies are produced by merging the DNA that encodes the binding protein of a monoclonal mouse antibody with human antibody producing DNA. This can reduce the risk of hypersensitivity reactions.
531
Describe the half-life of the Monoclonal Antibodies class.
The half-life of the this drug class is described as follows: - These agents typically have a long half-life (many are >15 days) - This often leads to a slower onset of actions (many antibodies can take at least a several weeks before a meaningful effect is achieved)
532
What are the clinical pearls of the Monoclonal Antibodies class?
The clinical pearls of this drug class are as follows: - These agents are very large proteins (molecular weight of ~146,000 Dal and therefore have poor CNS penetration
533
Describe the naming conventions of the Monoclonal Antibodies class.
The naming conventions of this drug class are as follows: - Chimeric monoclonal antibodies contain "-xi-" (ex. Cetuximab) - Humanized monoclonal antibodies contain "-zu-" (ex. Trastuzumab) - Fully human antibodies contain "-u-" (ex. Panitumumab)
534
What is the brand name of Hydroxyurea?
The brand name of this generic drug is: - Hydrea
535
What is the brand name of All-Trans Retinoic Acid (ATRA, Tretinoin)?
The brand name of this generic drug is: - Vesanoid
536
What is the brand name of Arsenic Trioxide (ATO)?
The brand name of this generic drug is: - Trisenox
537
What is the generic of name of Hydrea?
The generic name of this brand name drug is: - Hydroxyurea
538
What is the generic of name of Vesanoid?
The generic name of this brand name drug is: - All-Trans Retinoic Acid (ATRA, Tretinoin)
539
What is the generic of name of Trisenox?
The generic name of this brand name drug is: - Arsenic Trioxide (ATO)
540
What is the MOA of Tretinoin?
This drug's MOA is as follows: - Binds one or more nuclear receptors and decreases proliferation and induces differentiation of APL cells
541
What is the MOA of Arsenic Trioxide?
This drug's MOA is as follows: - Induces apoptosis in APL cells via DNA fragmentation and damages the fusion protein: promyelocytic leukemia (PML)-retinoic acid receptor (RAR) alpha
542
What is the MOA of Hydroxyurea?
This drug's MOA is as follows: - Antimetabolite that selectively inhibits ribonucleoside diphosphate reductase and interferes with DNA repair. - In sickle cell anemia, this drug increases hemoglobin F levels.
543
What are the main indications for use of Hydroxyurea?
The main indications of this drug are: - Cytoreduction in hematologic malignancies - CML - Head and Neck Cancer - Sickle Cell Anemia - Essential Thrombocythemia - Polycythemia Vera
544
What are the main indications for use of Arsenic Trioxide?
The main indications of this drug are: - Acute Promyelocytic Leukemia
545
What are the main indications for use of Tretinoin?
The main indications of this drug are: - Acute Promyelocytic Leukemia
546
What are the notable monitoring parameters for Tretinoin?
The notable monitoring parameters for this drug are: - Confirm t(15:17) translocation or the presence of the PML/RAR-alpha fusion protein (confirming diagnosis of acute promyelocytic leukemia). - Monitor patient multiple times daily during the initiation of therapy for signs of APL differentiation syndrome (monitor volume status, pulmonary status, temperature, respiration). - Coagulation parameters at baseline then at least 2 to 3 times a week during induction and at least weekly during consolidation. - Pregnancy test
547
What are the notable monitoring parameters for Arsenic Trioxide?
The notable monitoring parameters for this drug are: - Confirm t(15:17) translocation or the presence of the PML/RAR-alpha fusion protein (confirming diagnosis of acute promyelocytic leukemia). - Monitor patient multiple times daily during the initiation of therapy for signs of APL differentiation syndrome (monitor volume status, pulmonary status, temperature, respiration). - Coagulation parameters at baseline then at least 2 to 3 times a week during induction and at least weekly during consolidation. - QTc via 12-lead EKG at baseline then weekly or twice weekly
548
What are the notable monitoring parameters for Hydroxyurea?
The notable monitoring parameters for this drug are: - CBC with differential and platelets (once weekly for antineoplastic indications, every 2 weeks initially for sickle cell anemia)
549
What is the emetic potential of Hydroxyurea?
The emetic potential of this drug is: - Minimal to Low
550
What is the emetic potential of Tretinoin?
The emetic potential of this drug is: - Minimal to Low
551
What is the emetic potential of Arsenic Trioxide?
The emetic potential of this drug is: - Low
552
Describe the extravasation risk and management strategies for Hydroxyurea.
The extravasation risk and management strategies for this drug are as follows: - None
553
Describe the extravasation risk and management strategies for Tretinoin.
The extravasation risk and management strategies for this drug are as follows: - None
554
Describe the extravasation risk and management strategies for Arsenic Trioxide.
The extravasation risk and management strategies for this drug are as follows: - None
555
Describe the administration of Hydroxyurea.
The administration of this drug is described as follows: - Hydroxyurea can be used for cytoreduction (urgently bringing down a high white blood cell count) in newly diagnosed hematologic malignancy patients or as maintenance therapy for patients with essential thrombocythemia, sickle cell disease, and chronic myeloid leukemia. - Regardless of indication, doses are typically titrated to specific white blood cell or platelet counts (that vary depending on indication). - When titrating doses for cytoreduction, doses are typically adjusted every few days. - When used for maintenance indications, doses are typically titrated every few weeks.
556
Describe the metabolism of Hydroxyurea.
The metabolism of this drug is as follows: - Exposure is higher in patients with CrCl <60 mL/minute or end-stage renal disease
557
Describe the metabolism of Arsenic Trioxide.
The metabolism of this drug is as follows: - Systemic exposure to metabolites may also be increased in patients with renal impairment
558
What are the notable ADRs of Tretinoin?
The notable ADRs of this drug are: - Differentiation Syndrome (DS) - Pregnancy risk/fetal deformity
559
What are the notable ADRs of Arsenic Trioxide?
The notable ADRs of this drug are: - Differentiation Syndrome (DS) - QTc Prolongation
560
What are the notable ADRs of Hydroxyurea?
The notable ADRs of this drug are: - Myelosuppression - Hair Thinning - Skin/Nail Changes - Birth Defects
561
What drug(s) is notable for causing Differentiation Syndrome (DS)?
The drugs in this class notable for cause this condition are: - Tretinoin - Arsenic Trioxide
562
What APL drug(s) is notable for causing QTc Prolongation?
The drugs in this class notable for cause this condition are: - Arsenic Trioxide
563
What APL drug(s) is notable for causing fetal deformity?
The drugs in this class notable for cause this condition are: - Tretinoin
564
Describe the strategy and rationale for management of Differentiation Syndrome (DS).
The strategy and rationale for management of this condition caused by this drug are: - While acute promyelocytic leukemia (APL) is highly treatable, this is a potentially fatal complication of APL treatment. - It occurs in approximately 25% of patients who are treated for APL and typically presents in the first 7-12 days of treatment. - The pathogenesis of DS is incompletely understood, but in APL, treatment can induce maturation of promyelocytes and promote tissue infiltration which is linked to the production of inflammatory cytokines. - Patients are started on APL induction therapy in the hospital to closely monitor for DS. - Typical clinical findings of DS include dyspnea, fever, peripheral edema, hypotension, weight gain, pleuro-pericardial effusion, acute renal failure, musculoskeletal pain, and hyperbilirubinemia - Treatment of DS includes prompt steroid treatment and holding agents that can cause DS (ATRA and ATO) until signs and symptoms resolve. (Both ATRA and ATO have black boxed warnings for DS). - These agents are typically restarted at a lower dose before slowly titrating back up to full dose.
565
Describe the strategy and rationale for management of QTc Prolongation caused by Arsenic Trioxide.
The strategy and rationale for management of this condition caused by this drug are: - This drug has a black box warning for QTc interval prolongation, complete atrioventricular block, and torsade de pointes, which can be fatal. - Before administering this drug, assess the OTc interval, correct pre-existing electrolyte abnormalities (Potassium >4 and magnesium >2), and consider discontinuing drugs known to prolong OTc interval. - EKGs should be checked at baseline and 1-2 times per week during therapy. - QTc is calculated using the Framingham formula (QTc = QT interval + 154 * (1 - RR interval)) and QTc elevation is considered to be >450-500 msec. - Withhold arsenic trioxide until resolution and resume at reduced dose for QTc prolongation.
566
Describe the strategy and rationale for management of fetal deformity caused by Tretinoin.
The strategy and rationale for management of this condition caused by this drug are: - There is a high risk that a severely deformed infant will result if this drug is administered during pregnancy. - Within 1 week prior to starting tretinoin therapy, collect blood or urine from the patient for a serum or urine pregnancy test with a sensitivity of at least 50 milliunits/mL. - When possible, delay therapy until a negative result from this test is obtained.
567
Describe the history of Hydroxyurea.
The history of this drug is as follows: - Hydroxyurea was the first drug FDA approved for the treatment of sickle cell disease back in 1998. - It was nearly 20 years before another drug was approved for sickle cell disease in 2017! - Since then, there have been 3 new drug approvals and more therapies are being investigated.
568
What drugs are in the Somatostatin Analogs class?
Drugs in this class are: - Octreotide - Lanreotide
569
What is the brand name of Octreotide?
The brand name of this generic drug is: - SandoSTATIN/LAR Depot
570
What is the brand name of Lanreotide?
The brand name of this generic drug is: - Somatuline Depot
571
What is the generic of name of SandoSTATIN?
The generic name of this brand name drug is: - Octreotide
572
What is the generic of name of Somatuline Depot?
The generic name of this brand name drug is: - Lanreotide
573
What are the main/common indications of the Somatostatin Analogs class?
The main/common indications of this drug class are: - Carcinoid Crisis/Syndrome - Neuroendocrine Tumors
574
What is the class and MOA of Octreotide?
This drug in the following class: - Somatostatin Analogs This drug's MOA is as follows: - Mimics natural somatostatin by inhibiting serotonin release and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide - Control symptoms that result from release of peptides and neuroamines from neuroendocrine tumors and help control the disease itself
575
What is the class and MOA of Lanreotide?
This drug in the following class: - Somatostatin Analogs This drug's MOA is as follows: - Mimics natural somatostatin by inhibiting serotonin release and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide - Control symptoms that result from release of peptides and neuroamines from neuroendocrine tumors and help control the disease itself
576
What are the notable/common ADRs of the Somatostatin Analogs class?
The notable/common ADRs of this drug class are: - Bradycardia - Edema - Hyperglycemia
577
Describe the half-life of Octreotide.
The half-life of this drug is described as follows: - Duration of action: - SubQ: 6 to 12 hours - IM (LAR depot suspension): Following a single injection, a steady concentration is achieved within 2 to 3 weeks and maintained for an additional 2 to 3 weeks; steady-state levels are achieved after 3 injections administered at 4-week intervals.
578
What are the clinical pearls of the Somatostatin Analogs class?
The clinical pearls of this drug class are as follows: - Carcinoid syndrome primary occurs in patients with well differentiated metastatic neuroendocrine tumors. - Signs and symptoms include diarrhea and flushing. - Serotonin is thought to be the most important factor in the etiology of carcinoid syndrome diarrhea. - Long acting somatostatin analogs are highly active for the control of flushing/diarrhea as well as long term disease control. - Short acting analogs can be used for immediate effect in patients with uncontrolled carcinoid syndrome. - Short-acting octreotide can also be added to octreotide long-acting release for the treatment of breakthrough symptoms.
579
What drugs are in the BCR-ABL TKIs class?
Drugs in this class are: - Bosutinib - Dasatinib - lmatinib - Nilotinib - Ponatinib - Asciminib
580
What is the brand name of Bosutinib?
The brand name of this generic drug is: - Bosulif
581
What is the brand name of Dasatinib?
The brand name of this generic drug is: - Sprycel
582
What is the brand name of lmatinib?
The brand name of this generic drug is: - Gleevec
583
What is the brand name of Nilotinib?
The brand name of this generic drug is: - Tasigna
584
What is the brand name of Ponatinib?
The brand name of this generic drug is: - Iclusig
585
What is the brand name of Asciminib?
The brand name of this generic drug is: - Scemblix
586
What is the generic of name of Bosulif?
The generic name of this brand name drug is: - Bosutinib
587
What is the generic of name of Sprycel?
The generic name of this brand name drug is: - Dasatinib
588
What is the generic of name of Gleevec?
The generic name of this brand name drug is: - lmatinib
589
What is the generic of name of Tasigna?
The generic name of this brand name drug is: - Nilotinib
590
What is the generic of name of Iclusig?
The generic name of this brand name drug is: - Ponatinib
591
What is the generic of name of Scemblix?
The generic name of this brand name drug is: - Asciminib
592
What are the main indications for use of Bosutinib?
The main indications of this drug are: - Chronic Myeloid Leukemia
593
What are the main indications for use of Dasatinib?
The main indications of this drug are: - Chronic Myeloid Leukemia - Acute lymphoblastic Leukemia - Gastrointestinal stromal tumors
594
What are the main indications for use of lmatinib?
The main indications of this drug are: - Chronic Myeloid Leukemia - Acute lymphoblastic Leukemia - Gastrointestinal stromal tumors
595
What are the main indications for use of Nilotinib?
The main indications of this drug are: - Chronic Myeloid Leukemia - Acute lymphoblastic Leukemia - Gastrointestinal stromal tumors
596
What are the main indications for use of Ponatinib?
The main indications of this drug are: - Chronic Myeloid Leukemia - Acute lymphoblastic Leukemia
597
What are the main indications for use of Asciminib?
The main indications of this drug are: - Chronic Myeloid Leukemia
598
What are the main/common indications of the BCR-ABL TKIs class?
The main/common indications of this drug class are: - Chronic Myeloid Leukemia - Acute lymphoblastic Leukemia - Gastrointestinal stromal tumors
599
What is the class and MOA of Bosutinib?
This drug in the following class: - BCR-ABL TKIs This drug's MOA is as follows: - Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
600
What is the class and MOA of Dasatinib?
This drug in the following class: - BCR-ABL TKIs This drug's MOA is as follows: - Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
601
What is the class and MOA of lmatinib?
This drug in the following class: - BCR-ABL TKIs This drug's MOA is as follows: - Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
602
What is the class and MOA of Nilotinib?
This drug in the following class: - BCR-ABL TKIs This drug's MOA is as follows: - Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
603
What is the class and MOA of Ponatinib?
This drug in the following class: - BCR-ABL TKIs This drug's MOA is as follows: - Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
604
What is the class and MOA of Asciminib?
This drug in the following class: - BCR-ABL TKIs This drug's MOA is as follows: - Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia - This drug is a novel first in class STAMP (Specifically Targeting the ASL Myristoyl Pocket) inhibitor. This drug potently inhibits ABL1 kinase activity of the BCR-ABL1 fusion protein via allosteric binding to the ASL myristoyl pocket.
605
What are the notable/common monitoring parameters for the BCR-ABL TKIs class?
The notable/common monitoring parameters for this drug class are: - CBC weekly for first month, biweekly for the second month, then periodically thereafter - Liver function tests (at baseline and monthly) - In patients who discontinue therapy after a sustained molecular response, monitor BCR-ABL transcript levels and CBC with differential monthly for 1 year, then every 6 weeks for the second year, and every 12 weeks thereafter
606
What is the emetic potential of Bosutinib?
The emetic potential of this drug is: - Minimal-Low if <400 mg/day - Moderate-High if >400 mg/day
607
What is the emetic potential of Dasatinib?
The emetic potential of this drug is: - Minimal-Low
608
What is the emetic potential of lmatinib?
The emetic potential of this drug is: - Minimal-Low if <400 mg/day - Moderate-High if >400 mg/day
609
What is the emetic potential of Nilotinib?
The emetic potential of this drug is: - Minimal-Low
610
What is the emetic potential of Ponatinib?
The emetic potential of this drug is: - Minimal-Low
611
What is the emetic potential of Asciminib?
The emetic potential of this drug is: - Minimal-Low
612
Describe the emetic potential of the BCR-ABL TKIs class.
The emetic potential of this drug class is: - Most are Minimal-Low - Bosutinib and Imatinib are Moderate-High if >400 mg/day
613
What drugs in the BCR-ABL TKIs class have a moderate-high emetic potential?
Drugs in the class with a moderate-high emetic potential are: - Bosutinib and Imatinib if >400 mg/day
614
What drugs in the BCR-ABL TKIs class have a minimal-low emetic potential?
Drugs in the class with a low emetic potential are: - All of them except if >400 mg/day for Bosutinib and Imatinib (Moderate-High)
615
Describe the administration of Bosutinib.
The administration of this drug is described as follows: - Once Daily
616
Describe the administration of Dasatinib.
The administration of this drug is described as follows: - Once Daily
617
Describe the administration of lmatinib.
The administration of this drug is described as follows: - Usually Once Daily - select regimens are Twice Daily
618
Describe the administration of Nilotinib.
The administration of this drug is described as follows: - Twice Daily (may influence adherence)
619
Describe the administration of Ponatinib.
The administration of this drug is described as follows: - Once Daily
620
Describe the administration of Asciminib.
The administration of this drug is described as follows: - Usually Once Daily - select regimens are Twice Daily
621
Describe the general techniques for administration of the BCR-ABL TKIs class.
The general techniques for administration of this drug class is described as follows: - All are once daily except for Nilotinib and select regimens of Imatinib and Asciminib (twice daily)
622
What are the notable/common ADRs of the BCR-ABL TKIs class?
The notable/common ADRs of this drug class are: - Edema - Thrombocytopenia - Neutropenia - Bleeding
623
What are the clinical pearls of the BCR-ABL TKIs class?
The clinical pearls of this drug class are as follows: - Food and/or medications may enhance or decrease absorption - Neither dasatinib, nilotinib or bosutinib have shown improved overall survival or progression free survival rates compared to imatinib, so choice of first-line therapy should be individualized. - The following should be considered when choosing an agent: - toxicity profile - patient's age and ability to tolerate therapy - adherence/ease of administration - comorbid conditions - drug interactions - cost - feasibility of treatment discontinuation - In patients with disease progression, the selection of an alternative agent in this class is based on prior therapy, concurrent disease states, and/or mutational testing.
624
Describe considerations for discontinuation of BCR-ABL TKIs.
Considerations for discontinuation of agents in this class are as follows: - The management of CML as a chronic disease requires long-term therapy which can cause both adverse effects and a financial burden. - Discontinuation of TKI may be feasible in selected patients and with careful monitoring. - Discontinuation of TKI therapy may be considered only in patients who met all of the following criteria: - Chronic phase -CML with no history of accelerated phase or blast crisis - Have been on TKI therapy for at least 3 years with no history of resistance - Had stable molecular response for >2 years on at least 4 tests performed at least 3 months apart - Patients who do quality for TKI discontinuation must have monthly molecular monitoring for the first year following discontinuation, then every 6 weeks during the second year, and quarterly thereafter if still in a major molecular response. - If a patient loses their molecular response, they must have prompt resumption of therapy within 4 weeks.
625
Describe considerations for resistance to BCR-ABL TKIs.
Considerations for resistence to agents in this class are as follows: - Point mutations in the ABL kinase domain are the most frequent mechanism of secondary resistance to these drugs. - Among mutations in the ABL domain, the presence of the T315i mutation is the most common and displays resistance to all currently available agents except ponatinib and asciminib. - T315i mutation is also associated with disease progression and poorer survival. - Asciminib binds allosterically to the ABL pocket and is less susceptible to mutations that drive resistance. It has demonstrated activity against wild-type BCR-ABL1 and several mutant forms (including T315i), even showing activity in heavily pretreated patients. - Consider performing BCR-ABL kinase domain mutational analysis in patients who fail to achieve the response milestones, patients with any loss of response, or patients who experience disease progression to accelerated phase-CML or blast crisis-CML.
626
Describe considerations for interactions with BCR-ABL TKIs.
Considerations for interactions with agents in this class are as follows: - Dasatinib, Bosutinib, and Ponatinib require an acidic environment for absorption. - Avoid the use of proton pump inhibitors and separate H2-antagonists by at least two hours.
627
Describe considerations for CNS penetration of BCR-ABL TKIs.
Considerations for CNS penetration of agents in this class are as follows: - Of the available agents, dasatinib crosses blood-brain barrier to the greatest extent.
628
What drugs are in the BRAF Inhibitors class?
Drugs in this class are: - Dabrafenib - Vemurafenib - Encorafenib
629
What is the brand name of Dabrafenib?
The brand name of this generic drug is: - Tafinlar
630
What is the brand name of Vemurafenib?
The brand name of this generic drug is: - Zelboraf
631
What is the brand name of Encorafenib?
The brand name of this generic drug is: - Braftovi
632
What is the generic of name of Tafinlar?
The generic name of this brand name drug is: - Dabrafenib
633
What is the generic of name of Zelboraf?
The generic name of this brand name drug is: - Vemurafenib
634
What is the generic of name of Braftovi?
The generic name of this brand name drug is: - Encorafenib
635
What are the main indications for use of Dabrafenib?
The main indications of this drug are: - Melanoma (with BRAFV6ooE or BRAFV6ooK mutation) - Non-small cell lung cancer (with BRAF V6ooE mutation) - Thyroid cancer (with BRAF V6ooE mutation)
636
What are the main indications for use of Vemurafenib?
The main indications of this drug are: - Melanoma (with BRAFV6ooE or BRAFV6ooK mutation) - Non-small cell lung cancer (with BRAF V6ooE mutation) - Erdheim-Chester disease (with BRAF V6oo mutation)
637
What are the main indications for use of Encorafenib?
The main indications of this drug are: - Melanoma (with BRAFV6ooE or BRAFV6ooK mutation) - Colorectal cancer (with BRAF V6ooE mutation)
638
What is the class and MOA of Dabrafenib?
This drug in the following class: - BRAF Inhibitors This drug's MOA is as follows: - Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.
639
What is the class and MOA of Vemurafenib?
This drug in the following class: - BRAF Inhibitors This drug's MOA is as follows: - Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.
640
What is the class and MOA of Encorafenib?
This drug in the following class: - BRAF Inhibitors This drug's MOA is as follows: - Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.
641
What are the notable monitoring parameters for Vemurafenib?
The notable monitoring parameters for this drug are: - See common parameters for class - EKG at baseline. 15 days after initiation. then monthly for 3 months. then every 3 months thereafter (more frequently if clinically appropriate) and with dosage adjustments.
642
What are the notable/common monitoring parameters for the BRAF Inhibitors class?
The notable/common monitoring parameters for this drug class are: - BRAFV6ooK or V6ooE mutation status prior to treatment - Dermatologic evaluations prior to initiation, every 2 months during therapy, and for up to 6 months following discontinuation to assess for new cutaneous malignancies
643
What is the emetic potential of Dabrafenib?
The emetic potential of this drug is: - Moderate - High
644
What is the emetic potential of Vemurafenib?
The emetic potential of this drug is: - Minimal - Low
645
What is the emetic potential of Encorafenib?
The emetic potential of this drug is: - Moderate - High
646
Describe the emetic potential of the BRAF Inhibitors class.
The emetic potential of this drug class is: - All moderate-high except for Vemurafenib (minimal-low)
647
What drugs in the BRAF Inhibitors class have a moderate-high emetic potential?
Drugs in the class with a moderate-high emetic potential are: - Dabrafenib - Encorafenib
648
What drugs in the BRAF Inhibitors class have a minimal-low emetic potential?
Drugs in the class with a minimal-low emetic potential are: - Vemurafenib
649
Describe the administration of Dabrafenib.
The administration of this drug is described as follows: - Oral: Absorption decreased with a high fat meal (-1,000 calories: 58 to 75 grams of fat)
650
Describe the administration of Vemurafenib.
The administration of this drug is described as follows: - Oral
651
Describe the administration of Encorafenib.
The administration of this drug is described as follows: - Oral
652
Describe the metabolism of Dabrafenib.
The metabolism of this drug is as follows: - Patients with moderate (bilirubin >1,5 to 3 times ULN and any AST) or severe (bilirubin >3 to 10 times ULN and any AST) hepatic impairment may have increased exposure to this drug
653
What are the notable ADRs of Vemurafenib?
The notable ADRs of this drug are: - Secondary skin cancers - QT prolongation
654
What are the notable/common ADRs of the BRAF Inhibitors class?
The notable/common ADRs of this drug class are: - Secondary skin cancers - QT prolongation with Vemurafenib
655
Describe the strategy and rationale for management of secondary skin cancers caused by BRAF inhibitors.
The strategy and rationale for management of this condition caused by this drug class are: - Secondary cutaneous squamous cell cancers and keratoacanthomas are the result of compensatory RAF signaling seen with BRAF inhibition. - The risk of these additional cancers is decreased with the addition of a MEK inhibitor. - These cancers are typically localized and easily treated with surgical excision or topical fluorouracil cream. - Regular skin assessments should be done throughout therapy with BRAF inhibitors.
656
Describe the half-life of Encorafenib.
The half-life of this drug is described as follows: - This drug has a longer dissociation half-life than other BRAF inhibitors, allowing for sustained inhibition of BRAF (and thus tumor growth)
657
What are the clinical pearls of the BRAF Inhibitors class?
The clinical pearls of this drug class are as follows: - Though the BRAF inhibitors were initially evaluated as single agents, combination therapy with a MEK inhibitor (ex: Trametinib) is now the recommended treatment regimen.
658
Describe the therapy selection process for BRAF Inhibitors?
The therapy selection process for this drug class is as follows: - All metastatic tumors should be evaluated for the V6oo mutation. - In V6ooE or V6ooK mutated tumors, the initial selection between BRAF inhibitors and immunotherapy is commonly done based on the aggressive nature of the tumor. - Rapidly growing tumors that are symptomatic are treated with BRAF-directed therapy because it generates a higher rate of response that occurs quicker, while asymptomatic or more indolent tumors may be treated with immunotherapy.
659
Describe resistance among BRAF Inhibitors?
Resistance to this drug class is as follows: - Though the BRAF inhibitors were initially evaluated as single agents, combination therapy with a MEK inhibitor (example: Trametinib) is now the recommended treatment regimen. - This is due to the development of resistance to the single agent BRAF inhibitors after 6-7 months - Combination therapy with both BRAF and MEK inhibitors may suppress the downstream resistance mechanism
660
Describe the symptoms of melanoma.
Symptoms of this condition are: - ABCDE: asymmetry, border, color, diameter, and evolving - A: Asymmetry - melanomas are often asymmetrical - B: Border - melanomas often have an irregular border - C: Color - melanomas often have more than one color or shade in the mole - D: Diameter: melanomas are often larger than 6mm, or the size of a pencil eraser - E: Evolving: melanomas tend to change over time while benign moles do not
661
What drugs are in the EGFR Inhibitors class?
Drugs in this class are (not all inclusive): - Gefitinib - Erlotinib - Osimertinib - Afatinib
662
What is the brand name of Gefitinib?
The brand name of this generic drug is: - Iressa
663
What is the brand name of Erlotinib?
The brand name of this generic drug is: - Tarceva
664
What is the brand name of Osimertinib?
The brand name of this generic drug is: - Tagrisso
665
What is the brand name of Afatinib?
The brand name of this generic drug is: - Gilotrif
666
What is the generic of name of Iressa?
The generic name of this brand name drug is: - Gefitinib
667
What is the generic of name of Tarceva?
The generic name of this brand name drug is: - Erlotinib
668
What is the generic of name of Tagrisso?
The generic name of this brand name drug is: - Osimertinib
669
What is the generic of name of Gilotrif?
The generic name of this brand name drug is: - Afatinib
670
What are the main indications for use of Gefitinib?
The main indications of this drug are: - Non-Small Cell Lung Cancer with EGFR mutation
671
What are the main indications for use of Erlotinib?
The main indications of this drug are: - Non-Small Cell Lung Cancer with EGFR mutation - Pancreatic Cancer with EGFR mutation
672
What are the main indications for use of Osimertinib?
The main indications of this drug are: - Non-Small Cell Lung Cancer with EGFR mutation, T790M EGFR-mutation positive, or brain/leptomeningeal metastases
673
What are the main indications for use of Afatinib?
The main indications of this drug are: - Non-Small Cell Lung Cancer with EGFR mutation
674
What are the main/common indications of the EGFR Inhibitors class?
The main/common indications of this drug class are: - Certain cancers (such as Non-Small Cell Lung Cancer) with EGFR mutation
675
What is the class and MOA of Gefitinib?
This drug in the following class: - EGFR Inhibitors This drug's MOA is as follows: - EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.
676
What is the class and MOA of Erlotinib?
This drug in the following class: - EGFR Inhibitors This drug's MOA is as follows: - EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.
677
What is the class and MOA of Osimertinib?
This drug in the following class: - EGFR Inhibitors This drug's MOA is as follows: - EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.
678
What is the class and MOA of Afatinib?
This drug in the following class: - EGFR Inhibitors This drug's MOA is as follows: - EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.
679
What are the notable/common monitoring parameters for the EGFR Inhibitors class?
The notable/common monitoring parameters for this drug class are: - Confirm EGFR mutation positive before beginning therapy
680
Describe the emetic potential of the EGFR Inhibitors class.
The emetic potential of this drug class is: - Minimal-Low
681
Describe the administration of Gefitinib.
The administration of this drug is described as follows: - Oral
682
Describe the administration of Erlotinib.
The administration of this drug is described as follows: - Oral - Absorption is ~60% on an empty stomach, increases to ~100% with food
683
Describe the administration of Osimertinib.
The administration of this drug is described as follows: - Oral
684
Describe the administration of Afatinib.
The administration of this drug is described as follows: - Oral - Absorption is decreased with high-fat meals
685
Describe the metabolism of EGFR Inhibitors.
The metabolism of this drug class is as follows: - Primarily hepatic with the exception of Afatinib (minimal enzymatic metabolism)
686
What are the notable/common ADRs of the EGFR Inhibitors class?
The notable/common ADRs of this drug class are: - Acneiform Rash - N/V/D - Skin/nail changes - Dry mouth - Decreased appetite - Hepatic dysfunction - Disease flare (after discontinuation)
687
Describe the strategy and rationale for management of Acneiform Rash caused by EGFR Inhibitors.
The strategy and rationale for management of this condition caused by this drug are: - This is a common side effect of this class. - EGFR is expressed in many different tissues, including epithelial tissue, skin, hair follicles, and the gastrointestinal tract. - During treatment with EGFR inhibitors cutaneous adverse events occur in 65-90% of patients. This rash usually develops in the first 1-2 weeks, peaks at 3-4 weeks of therapy, and its intensity decreases after 2 weeks but can often persist over some months. - Management: - Mild Rash: patients may not require any form of intervention. Consider topical hydrocortisone cream or clindamycin gel. - Moderate Rash: hydrocortisone cream or clindamycin gel plus doxycycline 100 mg oral twice daily or minocycline 100 mg oral twice daily. - Studies have found that the development of a rash seems to be associated with an increased likelihood of tumor response and/or survival in NSCLC.
688
What are the clinical pearls of the EGFR Inhibitors class?
The clinical pearls of this drug class are as follows: - For patients with asymptomatic progression on a TKI, continuation of EGFR-TKI therapy can be considered - For patients who have not received osimertinib, recommend testing for the T790M mutation at time of progression. - If positive, osimertinib therapy is indicated. - For patients with symptomatic progression on a TKI, options include: - Continuing with an EGFR inhibitor - Switching to osimertinib if T790M mutation positive - Switching to systemic chemotherapy - EGFR mutations are present in 10-15% of non-small cell lung cancers and typically occur more commonly in women, Asian ethnicities, and never-smokers. - K-RAS and EGFR mutations are mutually exclusive. Meaning that if a patient has a K-RAS mutation, they will not respond to EGFR inhibitors.
689
Describe resistance among EGFR Inhibitors?
Resistance to this drug class is as follows: - The T790M mutation is the most common EGFR resistance mechanism (seen in 50-60% of patients) and can be present at diagnosis or develop during treatment. - This mutation increases affinity of kinase to ATP and decreases affinity to erlotinib and gefitinib. - Patients with the T790M mutation should be switched to osimertinib as is a third-generation EGFR-TKI that is selective for both EGFR-TKI-sensitizing and T790M resistance mutations.
690
What drugs are in the VEGF Inhibitors class?
Drugs in this class are: - Axitinib - Cabozantinib - Lenvatinib - Vandetanib - Pazopanib - Regorafenib - Sorafenib - Sunitinib
691
What is the brand name of Axitinib?
The brand name of this generic drug is: - Inlyta
692
What is the brand name of Cabozantinib?
The brand name of this generic drug is: - Cabometyx - Cometriq
693
What is the brand name of Lenvatinib?
The brand name of this generic drug is: - Lenvima
694
What is the brand name of Vandetanib?
The brand name of this generic drug is: - Caprelsa
695
What is the brand name of Pazopanib?
The brand name of this generic drug is: - Votrient
696
What is the brand name of Regorafenib?
The brand name of this generic drug is: - Stivarga
697
What is the brand name of Sorafenib?
The brand name of this generic drug is: - NexAVAR
698
What is the brand name of Sunitinib?
The brand name of this generic drug is: - Sutent
699
What is the generic of name of Inlyta?
The generic name of this brand name drug is: - Axitinib
700
What is the generic of name of Cabometyx?
The generic name of this brand name drug is: - Cabozantinib
701
What is the generic of name of Cometriq?
The generic name of this brand name drug is: - Cabozantinib
702
What is the generic of name of Lenvima?
The generic name of this brand name drug is: - Lenvatinib
703
What is the generic of name of Caprelsa?
The generic name of this brand name drug is: - Vandetanib
704
What is the generic of name of Votrient?
The generic name of this brand name drug is: - Pazopanib
705
What is the generic of name of Stivarga?
The generic name of this brand name drug is: - Regorafenib
706
What is the generic of name of NexAVAR?
The generic name of this brand name drug is: - Sorafenib
707
What is the generic of name of Sutent?
The generic name of this brand name drug is: - Sunitinib
708
What are the main/common indications of the VEGF Inhibitors class?
The main/common indications of this drug class are: - Endometrial cancer - Hepatocellular carcinoma - Renal cell carcinoma - Thyroid cancer
709
What is the class and MOA of Axitinib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
710
What is the class and MOA of Cabozantinib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
711
What is the class and MOA of Lenvatinib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
712
What is the class and MOA of Vandetanib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
713
What is the class and MOA of Pazopanib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
714
What is the class and MOA of Regorafenib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
715
What is the class and MOA of Sorafenib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
716
What is the class and MOA of Sunitinib?
This drug in the following class: - VEGF Inhibitors This drug's MOA is as follows: - Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels
717
What are the notable/common monitoring parameters for the VEGF Inhibitors class?
The notable/common monitoring parameters for this drug class are: - Blood pressure after 1 week, then every 2 weeks for 2 months, and at least monthly thereafter - Check urine for proteinuria at baseline and periodically during treatment (frequency depends on institutional standards, likely every 1-2 cycles) - TSH at baseline, then monthly for 4 months, then every 2 to 3 months - Baseline echocardiogram (sunitinib, pazopanib)
718
Describe the emetic potential of the VEGF Inhibitors class.
The emetic potential of this drug class is: - Minimal-Low for all except cabozantinib and high dose Lenvatinib (>12 mg/day - Moderate-High)
719
What is the emetic potential of Axitinib?
The emetic potential of this drug is: - Minimal-Low
720
What is the emetic potential of Cabozantinib?
The emetic potential of this drug is: - Moderate-High
721
What is the emetic potential of Lenvatinib?
The emetic potential of this drug is: - Minimal-Low if low dose <12 mg/day - Moderate-High if high dose >12 mg/day
722
What is the emetic potential of Vandetanib?
The emetic potential of this drug is: - Minimal-Low
723
What is the emetic potential of Pazopanib?
The emetic potential of this drug is: - Minimal-Low
724
What is the emetic potential of Regorafenib?
The emetic potential of this drug is: - Minimal-Low
725
What is the emetic potential of Sorafenib?
The emetic potential of this drug is: - Minimal-Low
726
What is the emetic potential of Sunitinib?
The emetic potential of this drug is: - Minimal-Low
727
What drugs in the VEGF Inhibitors class have a moderate-high emetic potential?
Drugs in the class with a high emetic potential are: - Cabozantinib - High dose Lenvatinib (>12 mg/day)
728
What drugs in the VEGF Inhibitors class have a minimal-low emetic potential?
Drugs in the class with a moderate emetic potential are: - All except for Cabozantinib and high dose Lenvatinib (>12 mg/day) - Axitinib - Lenvatinib (low dose <12 mg/day) - Vandetanib - Pazopanib - Regorafenib - Sorafenib - Sunitinib
729
Describe the metabolism of the VEGF Inhibitors class.
The metabolism of this drug class is as follows: - Hepatic (primarily metabolized by CYP3A4)
730
What are the notable ADRs of Sunitinib?
The notable ADRs of this drug are: - This drug can cause yellowing of the skin and hair - Think "shine like the sun" to help you remember
731
What are the notable/common ADRs of the VEGF Inhibitors class?
The notable/common ADRs of this drug class are: - Hypertension - Proteinuria - Bleeding/Thrombotic Events - Impaired Wound Healing - Hepatotoxicity
732
Describe the strategy and rationale for management of hypertension caused by VEGF Inhibitors.
The strategy and rationale for management of this condition caused by this drug class are: - VEGF plays a role in nitric oxide production and vasodilation. When the VEGF-signaling pathway is inhibited, hypertension may occur secondary to the decrease in nitric oxide production. - Hypertension associated with drug class should be managed similarly to hypertension in the general population (JNC guidelines). - A common BP goal is <140/90 mmHg. - Patients should have their BP monitored (and well controlled) prior to starting therapy and then checked at least every 2 to 3 weeks for the duration of treatment.
733
Describe the strategy and rationale for management of proteinuria caused by VEGF Inhibitors.
The strategy and rationale for management of this condition caused by this drug class are: - Proteinuria is a common adverse side effect of any anti-angiogenic agent. - VEGF is critical to the maintenance of normal renal function - Under-expression of VEGF can disrupt normal glomerular function leading to proteinuria. - Patients should have their urine checked for protein on a regular basis during VEGF inhibitor therapy. Frequency may vary per institutional protocol but it is often checked every 1-2 cycles of chemotherapy. - The presence of protein typically requires interruption of anti-VEGF therapy. - In the majority of cases, proteinuria resolves or significantly improves with removal of VEGF inhibitors.
734
Describe the strategy and rationale for management of bleeding/thrombotic events caused by VEGF Inhibitors.
The strategy and rationale for management of this condition caused by this drug class are: - These agents are associated with bleeding events sich as: - Epistaxis - Hemoptysis - Hematemesis - Gastrointestinal bleeding (including GI perforation which is infrequent but potentially life-threatening) - These agents are associated with arterial thromboembolic events such as: - Stroke/transient ischemic attack - Myocardial infarction - This predisposition to thrombosis and bleeding after inhibition ofVEGF signaling reflects the multitude of actions VEGF has on vascular walls and the coagulation system.
735
Describe the strategy and rationale for management of impaired wound healing caused by VEGF Inhibitors.
The strategy and rationale for management of this condition caused by this drug class are: - VEGF receptor inhibitors are associated with impaired wound healing due to decreased angiogenesis. - Therapy should typically be held for at least 1 month prior to surgery and only resumed when adequate wound healing has occurred.
736
Describe the strategy and rationale for management of hepatotoxicity caused by VEGF Inhibitors.
The strategy and rationale for management of this condition caused by this drug class are: - The VEGF inhibitors undergo hepatic metabolism and many of them can cause hepatotoxicity. In fact, many of the TKls have a black boxed warning for hepatotoxicity - Depending on the level of AST/ALT elevations, you may need to hold or reduce the dose of the VEGF inhibitor.
737
What are the risk factors for developing hypertension with VEGF Inhibitors?
Risk factors for developing this ADR with this drug/class are: - Pre-existing hypertension - Obesity - Older age
738
What are the risk factors for developing thrombotic events with VEGF Inhibitors?
Risk factors for developing this ADR with this drug/class are: - Age greater than 65 years - Pre-existing history of thromboembolic events
739
What are the clinical pearls of Cabozantinib?
The clinical pearls of this drug are as follows: - Cabozantinib is used to treat multiple disease states. However, the tablets and capsules are NOT interchangeable. - The tablets are used for renal cell carcinoma and the capsules are used for thyroid cancer.
740
What drugs are in the Anti-Androgens class?
Drugs in this class are: - Flutamide - Abiraterone acetate - Apalutamide - Bicalutamide - Enzalutamide - Nilutamide - Darolutamide
741
What is the brand name of Flutamide?
The brand name of this generic drug is: - Eulexin
742
What is the brand name of Abiraterone acetate?
The brand name of this generic drug is: - Yonsa - Zytiga
743
What is the brand name of Apalutamide?
The brand name of this generic drug is: - Erleada
744
What is the brand name of Bicalutamide?
The brand name of this generic drug is: - Casodex
745
What is the brand name of Enzalutamide?
The brand name of this generic drug is: - Xtandi
746
What is the brand name of Nilutamide?
The brand name of this generic drug is: - Nilandron
747
What is the brand name of Darolutamide?
The brand name of this generic drug is: - Nubeqa
748
What is the generic of name of Eulexin?
The generic name of this brand name drug is: - Flutamide
749
What is the generic of name of Yonsa?
The generic name of this brand name drug is: - Abiraterone acetate
750
What is the generic of name of Zytiga?
The generic name of this brand name drug is: - Abiraterone acetate
751
What is the generic of name of Erleada?
The generic name of this brand name drug is: - Apalutamide
752
What is the generic of name of Casodex?
The generic name of this brand name drug is: - Bicalutamide
753
What is the generic of name of Xtandi?
The generic name of this brand name drug is: - Enzalutamide
754
What is the generic of name of Nilandron?
The generic name of this brand name drug is: - Nilutamide
755
What is the generic of name of Nubeqa?
The generic name of this brand name drug is: - Darolutamide
756
What are the main/common indications of the Anti-Androgens class?
The main/common indications of this drug class are: - Prostate cancer
757
What is the class and MOA of Flutamide?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues
758
What is the class and MOA of Abiraterone acetate?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone
759
What is the class and MOA of Apalutamide?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Nonsteroidal androgen receptor antagonist
760
What is the class and MOA of Bicalutamide?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone
761
What is the class and MOA of Enzalutamide?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Pure androgen receptor signaling inhibitor
762
What is the class and MOA of Nilutamide?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues
763
What is the class and MOA of Darolutamide?
This drug in the following class: - Anti-Androgens This drug's MOA is as follows: - Competitive androgen receptor inhibitor, also inhibits androgen receptor translocation and androgen receptor-mediated transcription
764
What are the notable/common monitoring parameters for the Anti-Androgens class?
The notable/common monitoring parameters for this drug class are: - Serum transaminases at baseline, monthly for 4 months. and periodically thereafter: monitor liver function tests at the first sign or symptom of liver dysfunction - Prostate specific antigen (PSA) to monitor response to therapy
765
Describe the emetic potential of the Anti-Androgens class.
The emetic potential of this drug class is: - N/A (minimal)
766
Describe the metabolism of the Anti-Androgen class.
The metabolism of this drug class is as follows: - Extensively hepatic
767
What are the notable/common ADRs of the Anti-Androgens class?
The notable/common ADRs of this drug class are: - Headache - Peripheral edema - Hot flashes - Gynecomastia - Secondary infections
768
What are the clinical pearls of Flutamide?
The clinical pearls of this drug are as follows: - See common pearls for class - Used in combination with a GNRH agonist - Response rate = 50-87%
769
What are the clinical pearls of Abiraterone acetate?
The clinical pearls of this drug are as follows: - See common pearls for class - Approved for metastatic, castration-resistant prostate cancer in combination with a steroid BID. - Co-administration with the recommended dose of steroid compensates for drug-induced reductions in serum cortisol and blocks the compensatory increase in adrenocorticotropic hormone seen with this drug
770
What are the clinical pearls of Bicalutamide?
The clinical pearls of this drug are as follows: - See common pearls for class - Used in combination with a GNRH agonist - Response rate = 54-70%
771
What are the clinical pearls of Enzalutamide?
The clinical pearls of this drug are as follows: - See common pearls for class - Requires dose adjustments for strong CYP2C8 inhibitors and CYP3A4 inducers
772
What are the clinical pearls of Nilutamide?
The clinical pearls of this drug are as follows: - See common pearls for class - Used in combination with orchiectomy - Response rate = 40%
773
What are the clinical pearls of the Anti-Androgens class?
The clinical pearls of this drug class are as follows: - Monotherapy is less effective than GNRH agonist therapy and is not currently recommended to be used alone (unless patient had orchiectomy) - Therefore, used in combination with androgen ablation therapy - Overall efficacy is similar, but bicalutamide is generally preferred due to better toxicity profile
774
Describe the dosing schedule and administration for the anti-androgen class.
Dosing schedule and administration for drug class: - All are given PO - All are given once daily except: - Flutamide (TID) - Abiraterone acetate (BID) - Darolutamide (BID)
775
Describe the dosing schedule and administration for flutamide.
Dosing schedule and administration for this drug: - PO TID
776
Describe the dosing schedule and administration for abiraterone acetate.
Dosing schedule and administration for this drug: - PO BID
777
Describe the dosing schedule and administration for apalutamide.
Dosing schedule and administration for this drug: - PO once daily
778
Describe the dosing schedule and administration for bicalutamide.
Dosing schedule and administration for this drug: - PO once daily
779
Describe the dosing schedule and administration for enzalutamide.
Dosing schedule and administration for this drug: - PO once daily
780
Describe the dosing schedule and administration for nilutamide.
Dosing schedule and administration for this drug: - PO once daily
781
Describe the dosing schedule and administration for darolutamide.
Dosing schedule and administration for this drug: - PO BID
782
What drugs are in the Alkylating Agents class?
Drugs in this class are: - Cyclophosphamide - lfosfamide - Busulfan - Melphalan - Bendamustine
783
What is the brand name of Cyclophosphamide?
The brand name of this generic drug is: - Cytoxan
784
What is the brand name of lfosfamide?
The brand name of this generic drug is: - Ifex
785
What is the brand name of Busulfan?
The brand name of this generic drug is: - Busulfex - Myleran
786
What is the brand name of Melphalan?
The brand name of this generic drug is: - Alkeran - Evomela
787
What is the brand name of Bendamustine?
The brand name of this generic drug is: - Belrapzo - Bendeka - Treanda - Vivimusta
788
What is the generic of name of Cytoxan?
The generic name of this brand name drug is: - Cyclophosphamide
789
What is the generic of name of Ifex?
The generic name of this brand name drug is: - lfosfamide
790
What is the generic of name of Busulfex?
The generic name of this brand name drug is: - Busulfan
791
What is the generic of name of Myleran?
The generic name of this brand name drug is: - Busulfan
792
What is the generic of name of Alkeran?
The generic name of this brand name drug is: - Melphalan
793
What is the generic of name of Evomela?
The generic name of this brand name drug is: - Melphalan
794
What is the generic of name of Belrapzo?
The generic name of this brand name drug is: - Bendamustine
795
What is the generic of name of Bendeka?
The generic name of this brand name drug is: - Bendamustine
796
What is the generic of name of Treanda?
The generic name of this brand name drug is: - Bendamustine
797
What is the generic of name of Vivimusta?
The generic name of this brand name drug is: - Bendamustine
798
What are the main indications for use of Cyclophosphamide?
The main indications of this drug are: - Non-Hodgkin lymphoma - Hodgkin lymphoma - Hematopoietic stem cell transplant - Acute lymphoblastic leukemia - Breast cancer - Ewing sarcoma - Graft-vs-host disease prophylaxis - Multiple myeloma - Osteosarcoma - Rhabdomyosarcoma - Small cell lung cancer
799
What are the main indications for use of lfosfamide?
The main indications of this drug are: - Non-Hodgkin lymphoma - Hodgkin lymphoma - Ewing sarcoma - Osteosarcoma - Testicular cancer - Bladder cancer - Cervical cancer - Ovarian cancer - Soft tissue sarcoma
800
What are the main indications for use of Busulfan?
The main indications of this drug are: - Hematopoietic stem cell transplant - Polycythemia vera - Essential thrombocythemia
801
What are the main indications for use of Melphalan?
The main indications of this drug are: - Hematopoietic stem cell transplant - Multiple myeloma
802
What are the main indications for use of Bendamustine?
The main indications of this drug are: - Chronic lymphocytic leukemia - Non-Hodgkin lymphoma - Hodgkin lymphoma
803
What is the class and MOA of Cyclophosphamide?
This drug in the following class: - Alkylating Agents This drug's MOA is as follows: - Alkylates and cross-links DNA preventing DNA synthesis and cell division
804
What is the class and MOA of lfosfamide?
This drug in the following class: - Alkylating Agents This drug's MOA is as follows: - Alkylates and cross-links DNA preventing DNA synthesis and cell division
805
What is the class and MOA of Busulfan?
This drug in the following class: - Alkylating Agents This drug's MOA is as follows: - Alkylates and cross-links DNA preventing DNA synthesis and cell division
806
What is the class and MOA of Melphalan?
This drug in the following class: - Alkylating Agents This drug's MOA is as follows: - Alkylates and cross-links DNA preventing DNA synthesis and cell division
807
What is the class and MOA of Bendamustine?
This drug in the following class: - Alkylating Agents This drug's MOA is as follows: - Alkylates and cross-links DNA preventing DNA synthesis and cell division
808
What are the notable monitoring parameters for Cyclophosphamide?
The notable monitoring parameters for this drug are: - Monitor for blood in urine (either through patient report or urine dipstick depending on protocol)
809
What are the notable monitoring parameters for lfosfamide?
The notable monitoring parameters for this drug are: - Monitor for blood in urine (either through patient report or urine dipstick depending on protocol)
810
What are the notable monitoring parameters for Busulfan?
The notable monitoring parameters for this drug are: - Monitor hepatic function for signs of veno-occlusive disease - Monitor pharmacokinetics when giving high dose for stem cell transplant
811
What is the emetic potential of Cyclophosphamide?
The emetic potential of this drug is: - High if >1500 mg/m2 - Moderate if <1500 mg/m2
812
What is the emetic potential of lfosfamide?
The emetic potential of this drug is: - High if >2 g/m2 - Moderate if <2 g/m2
813
What is the emetic potential of Busulfan?
The emetic potential of this drug is: - Moderate
814
What is the emetic potential of Melphalan?
The emetic potential of this drug is: - High if >140 mg/m2 - Moderate if <140 mg/m2
815
What is the emetic potential of Bendamustine?
The emetic potential of this drug is: - Moderate
816
Describe the emetic potential of the Alkylating Agents class.
The emetic potential of this drug class is: - All are either moderate or high
817
What drugs in the Alkylating Agents class have a high emetic potential?
Drugs in the class with a high emetic potential are: - Cyclophosphamide >1500 mg/m2 - Ifosfamide >2 g/m2 - Melphalan >140 mg/m2
818
What drugs in the Alkylating Agents class have a moderate emetic potential?
Drugs in the class with a moderate emetic potential are: - Cyclophosphamide <1500 mg/m2 - Ifosfamide <2 g/m2 - Melphalan <140 mg/m2 - Busulfan - Bendamustine
819
What drugs in the Alkylating Agents class have a low emetic potential?
Drugs in the class with a low emetic potential are: - None (all are moderate or higher)
820
What drugs in the Alkylating Agents class have a minimal emetic potential?
Drugs in the class with a minimal emetic potential are: - None (all are moderate or higher)
821
Describe the extravasation risk and management strategies for Benamustine.
The extravasation risk and management strategies for this drug are as follows: - Carries risk as it is an irritant with vesicant like properties. - If extravasation occurs: - Stop infusion - Aspirate extravasated solution - Elevate extremity - Apply cold compress for 20 minutes 4 times daily - Consider sodium thiosulfate (2 mL SQ for each mg of drug suspected to have extravasated)
822
Describe the extravasation risk and management strategies for the Alkylating Agents class.
The extravasation risk and management strategies for this drug class are as follows: - Bendamustine carries extravasation risk as it is an irritant with vesicant like properties.
823
Describe the metabolism of the Alkylating Agents class.
The metabolism of this drug class is as follows: - All agents are hepatically metabolized - lfosfamide/cyclophosphamide are converted into active metabolites and acrolein
824
What is acrolein?
This metabolite is what cyclophosphamide and ifosfamide are converted into. It is toxic and causes bladder irritation and hemorrhagic cystitis.
825
Which alkylating agent(s) is most notable for causing mucositis (most common and most severe)?
Of the agents in this drug class, this ADR is most notable with melphalan.
826
What are the notable ADRs of melphalan?
The notable ADRs of this drug are: - Mucositis ranging from mouth sores to irritation of the GI tract leading to severe diarrhea.
827
What are the notable ADRs of Ifosfamide?
The notable ADRs of this drug are: - Hemorrhagic cystitis (irritation and bleeding of the bladder) due to accumulation of the toxic metabolite acrolein in the bladder. - Rare cases of neurotoxicity (<15%) with symptoms developing hours to days after the dose (typical onset is 48-72 hours)
828
What are the notable ADRs of cyclophosphamide?
The notable ADRs of this drug are: - Hemorrhagic cystitis (irritation and bleeding of the bladder) due to accumulation of the toxic metabolite acrolein in the bladder.
829
What are the notable ADRs of busulfan?
The notable ADRs of this drug are: - Veno-occlusive disease (VOD)/Sinusoidal Obstructive Syndrome (SOS) (when used in high doses for bone marrow transplantation)
830
Which alkylating agent(s) is most notable for causing veno-occlusive disease?
Of the agents in this drug class, this ADR is most notable with busulfan (high dose as is used in stem cell transplant).
831
Which alkylating agent(s) is most notable for causing hemorrhagic cystitis?
Of the agents in this drug class, this ADR is most notable with cyclophosphamide and ifosfamide.
832
What are the notable/common ADRs of the Alkylating Agents class?
The notable/common ADRs of this drug class are: - Mucositis - Hemorrhagic cystitis - Neurotoxicity - Hepatic veno-occlusive disease/sinusoidal obstructive syndrome
833
Describe the strategy and rationale for management of mucositis caused by melphalan.
The strategy and rationale for management of this condition caused by this drug are: - Oral mucositis can be prevented with cryotherapy. Due to short half-life, patients can chew on ice chips during and shortly after infusion causing vasoconstriction in the mouth and preventing chemotherapy from reaching the mucous membranes. - GI mucositis is managed with anti-motility agents after ruling out infectious causes of diarrhea
834
Describe the strategy and rationale for management of hemorrhagic cystitis caused by alkylating agents (cyclophosphamide and ifosfamide).
The strategy and rationale for management of this condition caused by this drug are: - Mesna is used as a chemoprotectant. - Hemorrhagic cystitis is caused by accumulation of the toxic metabolite acrolein in the bladder. - Mesna is oxidized to dimesna which in turn is reduced back to mesna in the kidneys supplying a free thiol group which binds and inactivates acrolein. - Mesna is always given with ifosfamide and if often given with high dose cyclophosphamide. - Mesna dose if typically 20% of the total daily ifosfamide/cyclophosphamide dose and is given for 3 doses - Vigorous hydration is also used as both prevention and treatment of hemorrhagic cystitis. - Additional treatments include bladder irrigation, hyperbaric oxygen, prostaglandin E2, and cystectomy for refractory cases.
835
Describe the strategy and rationale for management of neurotoxicity caused by ifosfamide.
The strategy and rationale for management of this condition caused by this drug are: - Patients should monitor for S/Sx with a daily signature log. - Symptoms generally resolve within 3 days of treatment discontinuation and can be managed with supportive care or methylene blue.
836
Describe the strategy and rationale for management of veno-occlusive disease (VOD) caused by busulfan.
The strategy and rationale for management of this condition caused by this drug are: - Also called sinusoidal obstructive syndrome (SOS) - Most commonly seen with high dose regimens use for stem cell conditioning - Risk increases with higher areas under the curve - Thus, pharmacokinetics measurements are often monitored, and doses are adjusted to target a specific AUC - Patient should be monitored for hepatic dysfunction, unexplained weight gain, edema, abdominal pain, and jaundice - Treatment options range from supportive care to defibrotide
837
Describe the half-life of drugs in the alkylating agents class.
The half-life of drugs in this class is described as follows: - All are relatively short, ranging from 40 minutes with Bendamustine to 15 hours with ifosfamide - This becomes especially important when managing adverse effects of melphalan with cryotherapy
838
Describe the history of alkylating agents.
The history of this drug class is as follows: - These drugs were the first anti-cancer drugs and remain a cornerstone of anti-cancer therapy. - The utility was discovered during World War I when researchers at Yale noticed that soldiers affected by mustard gas had low WBCs. They speculated that if mustard gas could destroy healthy WBCs, that it could destroy cancerous WBCs - this led to the use of alkylating agent as chemotherapy.