Oncology Meds Flashcards

Question

What is the MOA of mercaptopurine (6-MP, Purinethol)and thioguanine (6-TG, Tabloid)?

Answer 1

They are structural analogs of guanine that undergo conversion by hypoxanthine guanine-phosphoribosyltransferase and are incorporated into DNA and inhibit purine nucleotide synthesis.

Answer 2

They are triphosphate derivatives that inhibit ribonucleotide reductase and are incorporated into DNA and RNA.

Answer 3

They inhibit adenosine deaminase, interfering with adenosine nucleotide synthesis.

Answer 4

AML ALL CML

Answer 5

``` Myelosuppression (7-10 days) Dry skin Rash Photo sensitivity Hepatoxicity Jaundice Hyperbilirubinemia N/V ```

Answer 6

Dose reduction is required if co-admin with allopurinol

Answer 7

``` Myelosuppression (7-10 days) Increased LFTs Mucositis Rash N/V ```

Answer 8

Hairy cell leukemia CLL AML Follicular lymphoma

Answer 9

``` Myelosuppression (10-14 days), including decreased T cells Diarrhea CNS toxicity (rare) Somnolence Peripheral neuropathies Hearing and visual changes AMS Seizures, pulmonary toxicity, TLS ```

Answer 10

``` Myelosuppression (7-9 days) N/V/D Hypokalemia Hypophosphatemia Cytokine release syndrome Increased hepatic enzymes ```

Answer 11

``` Hairy cell leukemia CLL CML Mantle cell lymphoma Non-Hodgkin’s lymphoma ```

Answer 12

Myelosuppression (5-10 days) Fever (onset by day 6, persisting for about 3 days) Immunosuppressive Severe opportunistic infections

Answer 13

Prophylactic antibiotics and antiviral meds are recommended due to long-lasting T-cell suppression

Answer 14

MTX inhibits DHFR, the enzyme responsible for reducing dihydrofolate to tetrahydrofolate for the production of dTMP from dUMP. This results in the depletion of intracellular pools of reduced folates essential for thymidylate and purine synthesis. The DHFR-mediated effects of antifolates on normal and tumor cells may be neutralized by supplying reduced folates exogenously. The reduced folate used clinically for ‘’rescue’’ is leucovorin (folinic acid), which bypasses the metabolic block induced by DHFR inhibitors.

Answer 15

``` ALL Non-Hodgkin’s lymphoma Sarcomas Breast Head and neck Lung Stomach Esophagus ```

Answer 16

``` Myelosuppression (~10 days) Mucositis Renal dysfunction at high doses N/V CNS toxicity (more severe with IT administration) Hepatoxicty ```

Answer 17

``` CBC LFTs Renal function Urine pH MTX drug levels with high dose ```

Answer 18

3rd spaces (ascites, edema, plural effusion) Can have long T1/2, may require prolonged leucovorin rescue Drugs that are highly protein bound may displace MTX from albumin and increase toxicity (sulfonamides, salicylates, phenytoin, tetracyclines) NSAIDs and PPIs compete for renal excretion of MTX and increase serum drug levels

Answer 19

Peripheral T-cell lymphoma

Answer 20

``` Myelosuppression Mucositis N/V/V Anemia Fatigue Edema ```

Answer 21

Mesothelioma NSCLC Ovarian cancer (not FDA approved)

Answer 22

``` Myelosuppression (8-10 days) Stomatitis Pharyngitis Rash Desquamation ```

Answer 23

Begin oral folic acid supplementation 10 days prior to intimacy dose and continue for 30 days after last dose Vitamin B12 IM injection within 10 weeks prior to initial dose and every 8-10 weeks thereafter

Answer 24

It is a recombinant form of the bacterial enzyme carboxypeptidase-G2. It hydrolyzes the carboxyl-terminal glutamate residue from extra cellular methotrexate into inactive metabolites (DAMPA and glutamate). Allows for rapid reduction of methotrexate concentrations independent of renal function.

Answer 25

Methotrexate toxicity with MTX concentration > 1 mcg/L when leucovorin rescue alone is insufficient. Can be used off-labeled for IT MTX toxicity. Very expensive

Answer 26

They are micro assembly inhibitors. They prevent formulation and induce destabilization of microtubules.

Answer 27

They are microtubule disassembly inhibitors. They work by stabilizing microtubules.

Answer 28

Vinca alkaloids bind to tubulin alpha and beta subunits, inhibiting polymerization into mitotic spindles during metaphase.

Answer 29

``` Leukemia Hodgkin’s and non-Hodgkin’s lymphoma Neuroblastoma Rhabdomyosarcoma Ewing’s sarcoma Wilms’ tumor Multiple myeloma Thyroid and brain tumors ```

Answer 30

Peripheral neuropathy Motor sensory, autonomic, and cranial nerves may be affected (paresthesias, ileus, urinary retention, facial palsies) - irreversible SIADH Myelosuppression

Answer 31

Signs of neurotoxicity (tingling in extremities,constipation.CNS toxicity) LFTs

Answer 32

NEVER ADMIN INTRATHECALLY Inject hyaluronidase intradermally and apply moderate heat for extravasation. Doses should be adjusted in pts with elevated bilirubin Prevent ileus by treating constipation aggressively. Vincristine doses capped at 2 mg to minimize neurotoxicity.

Answer 33

``` Hodgkin’s and non-hodgkin’s T-cell lymphoma Testicular Breast Lung Head and neck Bladder Kaposi’s sarcoma Choriocarcinoma ```

Answer 34

``` Myelosuppression (5-10 days) Mucositis Neurotoxicity - less common than Oncovin Myalgias SIADH (rare) ```

Answer 35

NSCLC Breast Ovarian Hodgkin’s disease

Answer 36

``` Myelosuppression (5-10 days) Mucositis Neurotoxicity- less common than Oncovin Myalgias SIADH (rare) ```

Answer 37

Bind temporarily to low-affinity sites on the exterior of the microtuble and later migrate to high-affinity sites within the lumen. Promote assembly of microtubules from tubulin diners and stabilize microtubules by preventing depolymerization. Induce abnormal arrays or ‘’bundles’’ of microtubules throughout the cell cycle and during mitosis.

Answer 38

``` Breast Ovarian NSCLC Cervical Prostate Testicular Others ```

Answer 39

``` Myelosuppression (10-12 days) Infection Hypersensitivity reactions Peripheral neuropathy Myalgias or arthralgias Mucositis Cardiac arrhythmia Alone is ```

Answer 40

Premed with steroids and antihistamines Admin BEFORE platinums Dose reduction in pts with hepatic impairment

Answer 41

Breast NSCLC Pancreatic cancer

Answer 42

``` Myelosuppression (10-12 days) Infection Peripheral neuropathy Myalgias or arthralgias Mucositis Cardiac arrhythmias Slope is ```

Answer 43

This formulation lack Camaphor solvent which is responsible for hypersensitivity reactions NOT interchangeable with paclitaxel

Answer 44

``` Breast NSCLC Stomach Head and neck Prostate ```

Answer 45

``` Myelosuppression (5-9 days) Fluid retention and edema Pleural effusions Ascites Alopecia Rash Peripheral neuropathy Hypersensitivity reactions ```

Answer 46

Premed with dexamethasone x 3 days, beginning day before chemo CI in pts with hepatic impairment

Answer 47

Prostate cancer

Answer 48

``` Myelosuppression (8-12 days) Infection Hypersensitivity reactions N/V/D Asthenia Renal failure ```

Answer 49

Premed with steroids and antihistamines Avoid in pts with hepatic impairment

Answer 50

Binds to the beta-tubulin subunit of the microtubule, stabilizing tubulin polymerization and stabilizing microtubular function. Arrests cell cycle at the G2/M phase and induces apoptosis.

Answer 51

``` Myelosuppression Peripheral neuropathies Hypersensitivity reactions Asthenia Arthralgias Alopecia ```

Answer 52

Premed with steroids and antihistamines Dose reduce in pts with hepatic impairment

Answer 53

Binds to high affinity sites at the ends of existing microtubules. Inhibits formation of mitotic spindles causing mitotic breakage and arresting the cell cycle at the G2/M phase.

Answer 54

``` Myelosuppression (~day 13) Peripheral neuropathies Asthenia Alopecia N/C ```

Answer 55

Dose reduce in pts with hepatic impairment May cause QT prolongation

Answer 56

Estradiol suppresses circulating levels of testosterone. Estramustine binds covalently to microtubule-associated proteins that are part of the structural support for microtubules. Causes separation of these proteins from microtubules, inhibiting microtubule assembly and eventually causing disassembly.

Answer 57

Estrogenic side effects (breast tenderness/enlargement, edema) Increase in LFTs N/D

Answer 58

Topoisomerases are essential enzymes involved in maintaining DNA topological structure during replication and transcription. DNA topoisomerase enzymes relieve torsional strain during DNA unwinding by producing strand breaks. Topoisomerase I produces single strand breaks; topo II produces double strand breaks

Answer 59

Inhibit topo I resulting in the stabilization of the ‘’cleavable complexes’’ causing reversible single-stranded breaks.

Answer 60

Colorectal | Pancreatic

Answer 61

``` N/V/D Myelosuppression Alopecia Fatigue Increased LFTs Pulmonary toxicity Diffused infiltrates Fever Dyspnea ```

Answer 62

Diarrhea: Early (24 h): atropine Late (>24 h): loperamide Use in caution in pts with hepatic impairment or UGT1A deficiency

Answer 63

Ovarian Cervical SCLC

Answer 64

Myelosuppression (8-11 days) Mucositis Reversible elevations in transaminases Less N/D than irinotecan

Answer 65

Dose reduction for renal impairment

Answer 66

They stabilize ‘’cleavable complex” (topo II with the DNA strand cut) allowing DNA complex to break down leaving a double strand break. The strand breaks are capped by remnants of the topoisomerase protein, making them difficult to repair. They arrest cells in the S or early G2 phase. And also bind to tubulin and interfere with microtubule.

Answer 67

``` SCLC Testicular ALL AML Adrenal carcinoma ```

Answer 68

``` Myelosuppression (7-14 days) N/V Alopecia Mucositis Hypotension Infusion-related and hypersensitivity reactions ```

Answer 69

May cause secondary malignancies such as leukemias.

Answer 70

Myelosuppression (7-10 days) Mucositis N/V/D

Answer 71

They induce formation of covalent DNA-topo II complexes, preventing re-ligation of DNA, causing strand breaks. Also intercalated between base pairs in the DNA, causing additional DNA strand breaks. Metabolism of anthracyclines (but not mitoxandrone) forms oxygen free radicals that add to cytotoxicity.

Answer 72

Liposomal encapsulation of the doxorubicin limits cardiotoxicity.

Answer 73

``` Breast Ovarian Uterine Bladder Thyroid Lymphomas Leukemias ```

Answer 74

``` Myelosuppression (10-14 days) Infusion pain Alopecia Mucositis N/V Radiation recall reactions ```

Answer 75

AIDS-related Kaposi’s sarcoma Breast Ovarian

Answer 76

``` Myelosuppression (10-14 days) Hand-foot syndrome Alopecia N/V Mucositis Fatigue ```

Answer 77

``` Myelosuppression (10-14 days) Mucositis N/V Alopecia Severe vesicant ```

Answer 78

ALL AML CML MDS

Answer 79

Breast cancer

Answer 80

Breast Prostate AML NHL

Answer 81

``` Myelosuppression (10-15 days) Mucositis N/V Alopecia Severe vesicant Cardiac toxicity ```

Answer 82

``` Myelosuppression (8-14 days) Mucositis N/V Alopecia Severe vesicant injury Cardiac toxicities ```

Answer 83

``` Myelosuppression (10-14 days) N/V Mucositis Alopecia Less cardiotoxic than the anthracyclines ```

Answer 84

May discolor urine and sweat. Extravasation: apply cold and infuse IV dexrazoxane. ``` Cardio toxicity (acute): not related to cumulative dose; arrhythmias, pericarditis Cardiac toxicity (chronic): cumulative injury to myocardium (total dose > 450-550 mg/m2 doxorubicin equivalents) ```

Answer 85

Prevention of doxorubicin cardiomyopathy. | Treatment of anthracycline extravasation

Answer 86

A potent intracellular chelating agent. Cardiomyopathy: scavenges iron-mediated oxygen free radical generation responsible for anthracycline-induced cardiomyopathy. Extravasation: reversibility inhibits topo II, protecting tissue from anthracycline cytotoxicity

Answer 87

Covalently bind to highly reactive alkyl groups of nucleic acids and some proteins —> cross-linking. Interstrand: between bases on opposite strands Intrastate: between 2 bases in the same strand. Greatest effect is seen in rapidly dividing cells.

Answer 88

``` Lymphoma (Hodgkin’s and NHL) Breast SCLC Leukemias Multiple myeloma BMT ```

Answer 89

``` Hemorrhagic cystitis NV Myelosuppression (10-14 days) Alopecia SIADH (doses >2 g/m2) Secondary malignancies (bladder, acute leukemia) Infertility, sterility ```

Answer 90

``` Testicular Soft-tissue sarcomas Lung Breast Ovarian Bladder Lymphomas ```

Answer 91

``` Hemorrhagic cystitis Nephrotoxicity Myelosuppression (10-14 days) CNS effects (somnolence, confusion,disorientation, cerebellar symptoms that are dose-related N/V -acute and delayed ```

Answer 92

Advise pts to drink lots of fluids (>3 liters/day). Administer with mesna (all ifosfamide, high-dose cyclophosphamide). Dose reduce for renal impairment>

Answer 93

Prophylaxis of hemorrhagic cystitis induced by ifosfamide or high dose cyclophosphamide. Administered IV or PO prior to or along with chemo.

Answer 94

Acrolein: toxic metabolite of cyclophosphamide and ifosfamide. Acrolein binds to sulhydryl groups in the bladder wall causing hematuria, urinary frequency and dysuria. Mesna contains a free sulfhydryl group which binds acrolein excreted in the urine before it can bind to the bladder wall.

Answer 95

Lymphomas (Hodgkin’s and NHL) Cutaneous T-cell lymphoma Breast Lung

Answer 96

``` Myelosuppression (14-21 days) Infection Dermatologic reactions including SJS TLS Infusion reactions ```

Answer 97

``` Myelosuppression (~14 days) N/V/D Alopecia Mucositis Taste changes ```

Answer 98

Treat extravasation with sodium thiosulfate

Answer 99

``` Multiple myeloma BMT Neuroblastoma Breast Ovarian ```

Answer 100

CLL Lymphomas (Hodgkin’s and NHL) Ovarian Breast

Answer 101

``` Myelosuppression (8-10 days) N/V/D Mucositis Alopecia Arrhythmia Nephrotoxicity ```

Answer 102

``` Myelosuppression (~14 days) Increased LFTs Skin rash Menstrual irregularities Pulmonary toxicity Risk of secondary malignancies Infertility and sterility Teratogenic ```

Answer 103

Take on an empty stomach

Answer 104

These alkylate DNA through chloroethyl moeity. Lipophilic —> able to cross BBB

Answer 105

``` Brain tumors Multiple myeloma Lymphomas (Hodgkin’s and NHL) Melanoma Lung Colorectal ```

Answer 106

``` Hodgkin’s Intracranial tumors Breast Colorectal lung Multiple myeloma NHL ```

Answer 107

``` Myelosuppression (4-5 days) Severe N/V Cumulative nephrotoxicity Pulmonary fibrosis Facial flushing during infusion ```

Answer 108

Take on an empty stomach with fluids

Answer 109

CML AML BMT

Answer 110

``` Myelosuppression (14-21 days) Skin hyperpigmentation Pulmonary fibrosis Gynecomastia Adrenal insufficiency High dispose toxicities: seizures,hepatic venoocclusive disease, severe N/V ```

Answer 111

Seizure prophylaxis with high doses PK monitoring is required with IV busulfan

Answer 112

Undergo demethylation to active intermediate monoethyl triazenoimidazolecarboxamide. Decomposes to methylcarbonium ion, a nucleophile which alkylates DNA at the O6 and N7 positions of purines. Temozolamide is almost 100% orally absorbed can can cross the BBB. Dacarbazine does not cross the BBB.

Answer 113

Brain tumors

Answer 114

``` Melanoma Hodgkin’s Soft-tissue sarcomas Neuroblastoma Fibrosarcomas Rhabdomyosarcoma Thyroid cancer ```

Answer 115

``` Myelosuppression (7-10 days) Severe N/V Increased liver enzymes Flu-like syndrome Flushing Photosensitivity ```

Answer 116

Requires prophylaxis for PJP

Answer 117

Release ethylenimines radicals that behave like nitrogen mustards

Answer 118

``` Leukemias Hodgkin’s Breast Ovarian Bladder BMT ```

Answer 119

``` Myelosuppression (7-10 days) N/V Mucositis Pruritus Dermatitis ```

Answer 120

May be excreted in sweat, be especially conscientious of skin care in high-dose regimens.

Answer 121

Platinum salts undergo Aquarian once inside the cell. The platinum atom binds covalently to the N7 position to form inter and intra strand crosslinks. Platinum-DNA adductor cause replication arrest, transcription inhibition, cell-cycle arrest, DNA repair and apoptosis.

Answer 122

``` Testicular Ovarian Bladder Head and neck Lung Breast Cervical Gastric Colorectal ```

Answer 123

``` Ovarian Breast Lung Head and neck CNS or germ cell tumors Osteogenic sarcomas ```

Answer 124

Colorectal GI Breast

Answer 125

``` Severe N/V Nephrotoxicity K and Mg wasting Neurotoxicity Mild myelosuppression (14-23 days) ```

Answer 126

Myelosuppression-thrombocytopenia (~21 days) N/V -acute and delayed Risk of hypersensitivity reactions at higher cumulative doses

Answer 127

Peripheral neuropathy Pharyngolaryngeal dysesthesias N/V Anaphylaxis risk

Answer 128

Administer with pre and post hydration

Answer 129

Dose per AUC not mg/m2

Answer 130

Causes cold-induced neuropathy

Answer 131

Dose (mg) = Target AUC x (CrCl + 25) Typical target AUC ranges from 2-7 Learn how to do this: IBW, ABW, or TBW?

Answer 132

Intercalates at GC-rich portions of DNA. Generates oxygen free radicals which produce single and double stranded DNA breaks. Specific for G2 phase of cell cycle.

Answer 133

Alkylates DNA creating interstrand crosslinks and to a lesser extent also inhibits RNA and protein synthesis.

Answer 134

``` Testicular Lymphomas (HL and NHL) Squamous cell cancers Melanoma Sarcoma ```

Answer 135

``` Stomach Pancreatic Anal Bladder Breast Cervical Colorectal Head and neck NSCLC ```

Answer 136

Pulmonary fibrosis Anaphylaxis and hypersensitivity reactions Fever and flu-like symptoms Mucositis

Answer 137

``` Myelosuppression (4-6 days) Mucositis N/V Vesicant Pulmonary fibrosis Hemolytic anemia Uremic syndrome ```

Answer 138

Pulmonary toxicity associated with cumulative dose >400 units and preexisting pulmonary disease and with concomitant use of G-CSF use.

Answer 139

Apply ice or cold packs to site for extravasation

Answer 140

Inhibits ribonucleotide reductase, preventing production of DNA nucleotides from RNA. Cells accumulate in the S phase. May be classified as an antimetabolite.

Answer 141

``` Myelosuppression (~10 days) Rash Skin hyperpigmentation TLS Secondary leukemias ```

Answer 142

Used primarily to reduce WBC prior to standard chemotherapy.

Answer 143

The precise mechanism of action of arsenic in acute promyelocytic leukemia (APL) remains to be clearly defined. Selective apoptosis of APL cells mediated by activation of cysteine-proteases (caspases) Induces damage and degradation of the fusion protein PML/RAR-alpha. Upgrade the expression of NADPH-oxidase, leading to increase in production of reactive oxygen species. Disrupts mitochondria transmembrane potential.

Answer 144

Acute promyelocytic leukemia (APL)

Answer 145

QT prolongation Differentiation syndrome (pulmonary infiltrates, respiratory distress, fever, and hypotension) Electrolyte abnormalities (hypo or hyperkalemia, hypomagnesemia) Hyperglycemia Rash, lightheaded ness, fatigue Musculoskeletal pain

Answer 146

Differentiation syndrome must be treated promptly with corticosteroids Do not give if QTc > 500 msec Replace electrolytes before therapy

Answer 147

Direct cell differentiation by binding to retinoid and retinoic acids receptors. In APL, prompt leukemic cells to differentiate and cause apoptosis.

Answer 148

Kaposi’s sarcoma

Answer 149

Cutaneous T-cell lymphoma

Answer 150

``` Headache Differentiation syndrome ‘’ATRA syndrome’’: consisting of pulmonary symptoms, fever, hypotension, and pleural effusions Dry skin and mucous membranes Mucositis Elevation in transaminases and bilirubin ```

Answer 151

Rash | Itching

Answer 152

``` Increase TG and cholesterol Peripheral edema Insomnia Headache Fever Hypothyroidism Leukopenia Anemia ```

Answer 153

Differentiation syndrome must be treated promptly with corticosteroids Teratogenic

Answer 154

Exact MOA is unknown. Decreases protein production, including oncoproteins Bcr-Abl and Mcl-1

Answer 155

MOA is unknown. Binds and alkylates DNA at the N2 position of guanine. Interferes directly with transcription. Generates DNA double-stranded breaks.

Answer 156

``` Myelosuppression - thrombocytopenia (14-21 days) Increased risk of hemorrhage Anemia, neutropenia, lymphopenia N/D Fatigue Asthenia Injection site reaction Pyrexia, infection, hyperglycemia ```

Answer 157

``` Myelosuppression (~14 days) Increased liver enzymes Anemia N/V/C Electrolyte disturbances Fatigue Muscle and joint pain ```