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Chemotherapy Drugs Flashcards

1
Q

Melphalan

A

Nitrogen mustard derivative bifunctional alkylating agent Alkylates DNA resulting in breaks and cross-linking

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2
Q

Chlorambucil

A

Nitrogen mustard derivative bifunctional alkylating agent Alkylates DNA resulting in breaks and cross-linking

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3
Q

Cyclophosphamide

A

Nitrogen mustard derivative bifunctional alkylating agent Alkylates DNA resulting in cross-linking at guanine N-7 Must be activated by the liver Side effects: cystitis, myocardial necrosis, myelosuppression

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4
Q

Carmustine

A

Nitrosurea alkylating agent Alkylates DNA resulting in breaks and cross-linking Can penetrate CNS Can be used as implantable wafer

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5
Q

Lomustine

A

Nitrosurea alkylating agent Alkylates DNA resulting in breaks and cross-linking Can penetrate CNS

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6
Q

Cisplatin

A

Platinum alkylating agent Cross-links DNA Side effects: nephrotoxicity, ototoxicity

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7
Q

Oxaliplatin

A

Platinum alkylating agent Cross-links DNA Side effects: neurotoxicity Treats colorectal cancer

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8
Q

Carboplatin

A

Platinum alkylating agent Cross-links DNA

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9
Q

Procarbazine

A

Nonspecific alkylating agent Treats non-Hodgkin lymphoma Side effects: MAOI (eat less tyramine)

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10
Q

Vincristine

A

Binds to tubulin, prevents polymerization into microtubules, arrests cells in M-phase Side effects: neurotoxicity

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11
Q

Vinblastine

A

Binds to tubulin, prevents polymerization into microtubules, arrests cells in M-phase Side effects: neurotoxicity, mucositis, myelosuppression

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12
Q

Paclitaxel

A

Promotes polymerization and stability of microtubules and inhibits disassembly Side effects: neutropenia, mucositis

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13
Q

Docetaxel

A

Promotes polymerization and stability of microtubules and inhibits disassembly Affect G2/M-phase Side effects: neutropenia, mucositis

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14
Q

Ixabepilone

A

Binds β-tubulin and promotes polymerization and stability of microtubules and inhibits disassembly Affect G2/M-phase Side effects: neutropenia, cardiotoxicity, peripheral neuropathy

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15
Q

Etoposide

A

Inhibits topoisomerase II Affects G2/S-phase Side effects: myelosuppression

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16
Q

Teniposide

A

Inhibits topoisomerase II Affects G2/S-phase Side effects: myelosuppression

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17
Q

Irinotecan

A

Inhibits topoisomerase I Affects S-phase Side effects: neutropenia, diarrhea

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18
Q

Topotecan

A

Inhibits topoisomerase I Affects S-phase Side effects: neutropenia, diarrhea

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19
Q

Daunorubicin

A

Anthracycline antibiotic: 1) intercalates in DNA inhibiting DNA and RNA polymerase 2) induces free radical formation which breaks DNA 3) inhibits DNA topoisomerase II Side effects: cardiotoxicity (free radical damage) Dexrazoxane may reduce cardiac damage

20
Q

Doxorubicin

A

Anthracycline antibiotic: 1) intercalates in DNA inhibiting DNA and RNA polymerase 2) induces free radical formation which breaks DNA 3) inhibits DNA topoisomerase II Side effects: cardiotoxicity (free radical damage) Dexrazoxane may reduce cardiac damage

21
Q

Dexrazoxane

A

Iron chelator inhibits free radical formation and reduces cardiac damage associated with daunorubicin and doxorubicin (anthracycline antibiotics) Affects G2-phase

22
Q

Bleomycin

A

Forms DNA-bleomycin-Fe complex that is oxidized –> free radicals break DNA Affects G2-phase Side effects: pulmonary fibrosis, hyperpigmentation of hands

23
Q

Methotrexate

A

Competitively inhibits dihydrofolate reductase: 1) prevents formation of dTMP 2) decreases synthesis of purine ring structure Affects S-phase Side effects: myelosuppression, mucositis, hepatotoxicity (high dose), abortifacient Can use leucovorin (folinic acid) to reverse side effects

24
Q

5-fluorouracil

A

Pyrimidine analogue converted to 5-FdUMP which inhibits thymidylate synthase; 5-FdUTP incorporated into RNA resulting in defective transcripts Side effects: myelosuppression, photosensitivity Leucovorin potentiates effects

25
Capecitabine
5-FU prodrug whose final set of activation is catalyzed by thymidine phosphorylase, and enzyme elevated in tumor cells
26
Cytarabine
Cytidine analogue converted to Ara CTP which inhibits DNA polymerase and causes DNA chain termination when incorporated Causes pancytopenia
27
Gemcitabine
Cytidine analogue inhibits DNA polymerase and ribonucleotide reductase
28
Azacitidine
Pyrimidine nucleoside analog gets incorporated into RNA and inhibits processing and function Treats myelodysplastic syndrome
29
6-mercaptopurine
Purine analogue: 1) inhibits de novo purine synthesis 2) competitively inhibits biosynthetic reactions 3) incorporated into DNA and RNA Side effects: myelosuppression, hepatotoxicity
30
6-thioguanine
Purine analogue: 1) inhibits de novo purine synthesis 2) competitively inhibits biosynthetic reactions 3) incorporated into DNA and RNA Side effects: myelosuppression, hepatotoxicity
31
Asparaginase
Catalyzes conversion of asparagine to aspartate to inhibit protein synthesis (asparagine levels are low in tumor cells) Side effects: reduced protein synthesis (clotting factors, insulin, albumin), hypersensitivity reactions, hepatotoxicity
32
Imatinib mesylate
Competitively blocks ATP-binding side of c-abl tyrosine kinase Inhibits c-kit and PDGF-associated tyrosine kinases Treats CML and Ph+ ALL Side effects: myelosuppression and CHF
33
Erlotinib
Inhibits EGF receptor-associated tyrosine kinase Side effects: CHF
34
Gefitinib
Inhibits EGF receptor-associated tyrosine kinase Side effects: CHF
35
Vemurafenib
Inhibits B-raf serine-threonine kinase with V600E mutation Treats melanoma
36
Cetuximab
Antibody against EGF receptor
37
Trastuzumab (Herceptin)
Inhibitor of HER2 tyrosine kinase receptor (extracellular domain)
38
Bevacizumab
Antibody against VEGF --\> inhibits angiogenesis
39
Rituximab
Anti-CD20 antibody that promotes complement-mediated lysis of malignant B cells May cause reactivation of HBV
40
Ipilimumab
Antibody against CTLA-4 that blocks inhibitory activity Treats malignant melanoma
41
Pembrolizumab
Bind to PD-1 receptor on T cells
42
Gamtuzumab ozogamicin
Antibody against CD33 (myeloid surface antigen)
43
Bortezomib
Proteasome inhibitor Treats multiple myeloma and mantle cell lymphoma
44
all-trans-retinoic acid
Treats promyelocytic leukemia by causing blasts to mature
45
Heparin
Anticoagulant Activates antithrombin --\> inactivates thrombin and factor Xa Monitor with PTT Can reverse with protamine sulfate Can cause heparin-induce thrombocytopenia --\> IgG develops against heparin bound to platelet factor 4 --\> activates platelets --\> thrombosis and thrombocytopenia
46
Warfarin (Coumadin)
Anticoagulant Inactivates vitamin K epoxide reductase --\> reduced gamm-carboxylation of factors II, VII, IX, X, proteins C and S Monitor with PT/INR Contraindicated in pregnancy (crosses placenta) May cause tissue necrosis

Pharmacology (8 decks)

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