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Pharmacology > Chemotherapy Drugs > Flashcards

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
Q

Capecitabine

A

5-FU prodrug whose final set of activation is catalyzed by thymidine phosphorylase, and enzyme elevated in tumor cells

26
Q

Cytarabine

A

Cytidine analogue converted to Ara CTP which inhibits DNA polymerase and causes DNA chain termination when incorporated Causes pancytopenia

27
Q

Gemcitabine

A

Cytidine analogue inhibits DNA polymerase and ribonucleotide reductase

28
Q

Azacitidine

A

Pyrimidine nucleoside analog gets incorporated into RNA and inhibits processing and function Treats myelodysplastic syndrome

29
Q

6-mercaptopurine

A

Purine analogue: 1) inhibits de novo purine synthesis 2) competitively inhibits biosynthetic reactions 3) incorporated into DNA and RNA Side effects: myelosuppression, hepatotoxicity

30
Q

6-thioguanine

A

Purine analogue: 1) inhibits de novo purine synthesis 2) competitively inhibits biosynthetic reactions 3) incorporated into DNA and RNA Side effects: myelosuppression, hepatotoxicity

31
Q

Asparaginase

A

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
Q

Imatinib mesylate

A

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
Q

Erlotinib

A

Inhibits EGF receptor-associated tyrosine kinase Side effects: CHF

34
Q

Gefitinib

A

Inhibits EGF receptor-associated tyrosine kinase Side effects: CHF

35
Q

Vemurafenib

A

Inhibits B-raf serine-threonine kinase with V600E mutation Treats melanoma

36
Q

Cetuximab

A

Antibody against EGF receptor

37
Q

Trastuzumab (Herceptin)

A

Inhibitor of HER2 tyrosine kinase receptor (extracellular domain)

38
Q

Bevacizumab

A

Antibody against VEGF –> inhibits angiogenesis

39
Q

Rituximab

A

Anti-CD20 antibody that promotes complement-mediated lysis of malignant B cells May cause reactivation of HBV

40
Q

Ipilimumab

A

Antibody against CTLA-4 that blocks inhibitory activity Treats malignant melanoma

41
Q

Pembrolizumab

A

Bind to PD-1 receptor on T cells

42
Q

Gamtuzumab ozogamicin

A

Antibody against CD33 (myeloid surface antigen)

43
Q

Bortezomib

A

Proteasome inhibitor Treats multiple myeloma and mantle cell lymphoma

44
Q

all-trans-retinoic acid

A

Treats promyelocytic leukemia by causing blasts to mature

45
Q

Heparin

A

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
Q

Warfarin (Coumadin)

A

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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