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Chemotherapy III Flashcards

1
Q

Class of Doxorubicin

A

Anthracycline Antitumor antibiotic

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2
Q

Cycle specificity of Doxorubicin

A

CCNS

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3
Q

Macromolecular target of Doxorubicin

A

DNA

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4
Q

MOA of Doxorubicin

A

Intercalation between base pairs of DNA leading to strand breaks due to inhibition of topoisomerase II

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5
Q

Topoisomerase II inhibiting drugs that are intercalators

A

Daunomycin
Doxorubicin
Mitoxanthrone
Dactinomycin

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6
Q

Topoisomerase II inhibiting drugs that are non-intercalators

A

Etoposide

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7
Q

Tomoisomerase I inhibiting drugs

A

Topotecan

Irinotecan

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8
Q

Role of topoisomerase I

A

Single strand DNA breaks, relaxation of the strand and re-anneal the strands
Inhibiting agents arrest in the replication fork

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9
Q

Role of topoisomerase II

A

Double strand breaks in the DNA, relaxation and re-anneal the strands of DNA
Inhibiting agents inhibit chromosome replication

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10
Q

Metabolism of Doxorubicin

A

Liver

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11
Q

Excretion of Doxorubicin

A

Excreted as a thiol adduct into the bile

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12
Q

Define multidrug resistance

A

Intercalting and non-intercalating topoisomerase II inhibitors and the tubulin inhibitors (vinca alkaloids) are all cross resistant due to the P-glycoprotein membrane bound efflux pump
Exports big bulky hydrophobic groups

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13
Q

How is the glycoprotein downregulated (reverse resistance)

A

Giving drug as continuous infusion

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14
Q

What drugs may block the efflux pump and reverse resistance

A

Quinine
Verapamil
Cyclosporine

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15
Q

SEs of Doxorubicin

A

Nausea and vomiting
Hair loss
Stomatitis
Myelosuppression (dose limiting toxicity)
Cardiac toxicity- congestive cardiomyopathy (cumulative and schedule dependent )
Vesicant

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16
Q

Dose limiting SE of Doxorubicin

A

Myelosuppression

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17
Q

What tests must be done before administration of Doxorubicin

A 
Determine EF (ECHO or MUGA scan)
Bilirubin level
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18
Q

Dose reduction for Doxorubicin

A

Presence of jaundice

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19
Q

How can cardiac toxicity of Doxorubicin be avoided

A

-Lifetime dose lower than 400mg/M^2
-Longer length of infusion (96 hours) of the dose of the drug
-Pretreatment with an iron chelator may be helpful- dexrazoxane
Prevent cumulative toxicity and schedule dependent toxicity

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20
Q

How can we describe the cardiac toxicity of doxorubicin

A

Cumulative toxicity

Schedule dependent toxicity

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21
Q

Which drug is red?

A

Doxorubicin (good for screening patients for prior treatment)

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22
Q

Schedule dependence of Doxorubicin

A

Schedule dependent cardiac toxicity

Schedule independent cytotoxicity

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23
Q

Presumed mechanism of Doxorubicin cardiac toxicity

A

Free radical damage due to high plasma concentrations
Due to complexes of iron with Doxorubicin

DIFFERENT THAN MOA OF CYTOTOXICITY

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24
Q

Cardiopreotective agent for patients taking Doxorubicin

A

Dexazoxane (iron chelator)

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25
Contraindications of Doxorubicin
Prior mediastinal irradiation and long standing uncontrolled HTN (increased risk of cardiotoxicity)
26
Uses of Doxorubicin
Breast cancer Leukemia Sarcoma Hodgkin's and non Hodgkin's lymphomas
27
Compounds in the anthracycline antibiotic class
``` Doxorubicin Daunomycin Idarubicin Epirubicin Mitoxantrone ```
28
Differences between Daunomycin and Doxorubicin
Less cardiac toxic | Less effective against solid tumors
29
Use of Daunomycin
Treatment of some leukemias | NOT solid tumrs
30
Use of Idarubicin and epirubicin
Exclusively leukemia
31
SEs of all anthracycline antibiotics
Dose limiting myelosuppression
32
Class of Irinotecan
Camptothecin Topoisomerase I inhibitor Plant alkaloid
33
Macromolecular target of Irinotecan
DNA
34
Cycle specificity of Irinotecan
CCNS
35
Bioactivation of Irinotecan
Prodrug | Converted by carboxylesterase to 7-ethyl-10-hydroxycamptothecin (SN-38)
36
MOA of Irinotecan
Topoisomerase I inhibition leading to single strand breaks in the DNA
37
Metabolism of Irinotecan
Hepatic metabolism
38
Dose reduction of Irinotecan
Jaundice
39
Metbolism of Irinotecan
UGTIAI is responsible for clearance by glucuronidation of drug and bilirubin
40
Gilbert's Syndrome and Irinotecan use
Gilbert's syndrome: genetic polymorphism (7/7 genotype) in the UGT1A1 promoter (UGT1A1*28) results in enzyme underexpression and decreased bilirubin and irinotecan metabolism Decreased glucoronidation No guidelines of what to do however
41
SEs of Irinotecan
``` Nausea Vomiting Myelosupression (dose limiting) Stomatitis Hair loss Early cholinergic diarrhea Late secretory diarrhea (7-10 days later) Death ```
42
Treatment of cholinergic diarrhea from Irinotecan
Atropine (pre-medicate)
43
Treatment of secretory diarrhea from Irinotecan
Imodium
44
Uses of Irinotecan
GI tract malignancies (Colon cancer)
45
Use of Topotecan
Ovarian cancer patients who have become resistant to carboplatin and paclitaxel
46
Class of Bleomycin
Antitumor antibiotic
47
Cycle specificity of Bleomycin
CCS (G2-M phase)
48
Macromolecular target of Bleomycin
DNA
49
MOA of Bleomycin
Binds to DNA, free radical production leading to single and double strand DNA breaks
50
Active species of Bleomycin
Bleomycin- iron form
51
Excretion of Bleomycin
50% in urine
52
Inactivation of Bleomycin
Liver and kidneys rapidly inactivate the drug via bleomycin hydrolase Lung and skin have low levels of bleomycin hydrolase= toxicities
53
SEs of Bleomycin
Pulmonary toxicity is dose limiting - cumulative toxicity (dec. in pulmonary diffusion capacity) Hyperpigmented skin- hyperkeratosis of the palms Stomatitis and hair loss NOT myelosuppressive Anaphylactoid reactions (following first dose in lymphoma) Fever and chills are common
54
Dose limiting toxicity of Bleomycin
Pulmonary toxicity
55
Dosing of Bleomycin
30 units per dose X ~13 doses | No more than 400 units total dose
56
Testing before use of Bleomycin
Test dose to monitor for severe reactions | Test pulmonary function
57
Monitoring of Bleomycin
Diffusion capacity of carbon monoxide- PFTs
58
Routes of administration of Bleomycin
IV, IM, subcutaneous, intracavitary (pleural space for palliation of a pleural effusion)
59
Caution of O2 administration in patients treated with Bleomycin
If given high inspired oxygen concentrations, these is a risk of pulmonary damage and death (ARDS) Give lowest FiO2 to maintain O2 saturation >90%
60
Dose reduction of Bleomycin
Renal insufficiency
61
Uses of Bleomycin
``` Testicular cancer (30 units IV weekly for 12 weeks) Hodgkin's disease ```
62
What is the BEP regimen for testicular cancer
Bleomycin, etoposide, cisplatin
63
Drug class of Prednisone
Steroid
64
Macromolecular target of Prednisone
Steroid receptor
65
SEs of Prednisone
``` Euphoria Weight gain Increased appetitite Mania Hypertension Sodium and fluid retention Aggrevation of diabetes Hypokalemia Alteration of the sleep-wake cycle Peptic ulceration of the stomach Spontaneous colon performation Cataracts Osteoporosis Cushingoid appearance Suppression of the pituitary adrenal axis ```
66
Use of Prednisone
100 mg/ day or more Hodgkin's disease and non-Hodgkin's lymphoma Multiple myeloma Some leukemias
67
Use of dexamethasone
Reduce cerebral edema in patients with brain metastases | Potentiates effect of 5HT3 receptor antagonists (ondansetron)- used to control emesis and nausea
68
Class of Tamoxifen
SERM
69
Macromolecular target of Tamoxifen
Estrogen receptor
70
Bioactivation of Tamoxifen
Prodrug and is metabolized in the liver to 4-hydroxytamoxifen
71
MOA of Tamoxifen
Ant of breast cancer ER | Agonist of endometrial and bone ER
72
Metabolism of Tamoxifen
Metabolized by the liver
73
SEs of Tamoxifen
``` Weight gain Hot flashes Endometrial cancer Thrombosis *Dec. bone loss ```
74
Use of Tamoxifen
``` Breast cancer (20 mg daily) Chemoprevention of breast cancer (5 years) - can develop ER - breast CA ```
75
Use of Raloxifene
Breast cancer chemoprevention
76
Class of Anastrozole
Selective Aromatase inhibitor
77
Effect of Anastrozole
Reduce estradiol 70% after 24 hours | 80% reducton after 2 weeks
78
Metabolism of Anastrozole
Liver
79
SEs of Anastrozole
``` Hot flashes Mood disturbance Arthritis Arthralgias Bone pain Bone loss Osteoporosis ```
80
Route of administration of Anastrozole
Oral
81
Use of Anastrozole
Hormone receptor + breast cancer
82
Aromatase inhibitors
Anastrozole, Letrozole, Exemestane
83
MOA of Flutamide
Inhibits the uptake and binding of the testosterone to specific receptors in hormonally sensitive prostate cancer cells
84
SEs of Flutamide
Well-tolerated Diarrhea (20% of patients) Elevated LFTs
85
Use of Flutamide
Androgen deprivation treatment therapy of metastatic prostate cancer
86
Testosterone receptor antagonists
Flutamide, Bicalutamide, Nilutamide
87
Benefit of Bicalutamide and Nilutamide
Less diarrhea
88
Class of Leuprolide acetate
GnRH receptor agonist
89
MOA of Leuprolide acetate
Binds to the pituitary GnRH receptors and initially produces an increase in LH and FSH leading to an increase in T and thus initially can stimulate tumor growth By interrupting the normal pulsatile stimulation of the GnRH receptors, leuprolide down regulates the secretion of LH and FSH, leading to a reduction in T levels
90
SES of Leuprolide
Tumor flare reaction (pretreat with flutamide or bicalutamide) Hot flashes Androgen deprivation therapy (ADT): weakness, decreased libido, loss of muscle mass, ED, change in body fat distribution, gynecomastia
91
Coadministration of Leuprolide with:
Flutamide or bicalutamide for 2-4 weeks before institutation of leuprolide acetate treatment (depot injections)
92
Route of administration of Leuprolide
IM | Depot injections
93
GnRH receptor agonists
Leuprolide | Goserelin (agonist of LHRH)

Chemotherapy Viruses (5 decks)

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