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Pharm Ch 37
Cancer - Genome Synthesis
| Question | Answer |
|---|---|
| MOA of 5-Fluorouracil (5-FU) | Inhibitor of Thymidylate Synthase ("thymineless" cell death) |
| Converted to FdUMP Tx: breast, GI, BCC, combo w/ folinic acid (leucovorin), DOC for colorectal cancer | 5-Fluorouracil (5-FU) |
| MOA of 6-Mercaptopurine (6-MP), Azathioprine (AZA) | Inhibitors of Purine Metabolism |
| inosine analogue, converted by HGPRT to T-IMP, Tx: ALL, coadmin w/ allopurinol allows dose reduction by 2/3 and prevents "tumor lysis syndrome" | 6-Mercaptopurine (6-MP) |
| MOA of Hydroxyurea | Inhibits Ribonucleotide Reductase (inhibits DNA synthesis) |
| increases HbF, Tx: adult sickle cell, head & neck cancer, PCV, ET ADR: long-term use may cause cancer | Hydroxyurea |
| MOA of Thioguanine, Cytarabine (araC) | Purine & Pyrimidine Analogues that are incorporated into DNA |
| Guanine analogue, Tx: AML, ADR: bone marrow suppression, GI injury | Thioguanine |
| Cytidine analgoue, Synergism w/ cyclophosphamide, Tx: AML (combo w/ anthracycline) | Cytarabine (araC) |
| bis-alkylation (crosslinks DNA), nonreactive prodrug, activation by liver P450 causes acrolein bladder cancer (Tx: mesna) | Cyclophosphamide |
| prodrug of 6-MP, DOC for immunosuppression | Azathioprine (AZA) |
| Nitrosourea, requires bioactivation, Tx: brain tumors | Carmustine (BCNU) |
| MOA of Cyclophosphamide, Carmustine, Mitomycin, Dacarbazine, Procarbazine, Altretamine | Alkylating Agents (directly modify DNA structure) |
| Alkylating antibiotic that targets hypoxic cells (center of solid tumor) | Mitomycin |
| Tx: Hodgkin's, melanoma, sarcoma | Dacarbazine |
| PO, Tx: Hodgkin's, Metabolite is MAOI | Procarbazine |
| Tx: refractory ovarian cancer | Altretamine |
| crosslinks guanine, Tx: testicular, ovarian & bladder cancers (GU) ADR: nephrotoxic (tx: amifostine), N/V, neurotoxicity | Cisplatin |
| Cisplatin analogue, Tx: lung cancer | Carboplatin |
| binds DNA, chelates iron, reacts to oxygen, Tx: testicular, Hodgkin's ADR: pulmonary fibrosis (monitor PFT) | Bleomycin |
| MOA of Irinotecan, Doxorubicin, Etoposide | Topoisomerase (TI) Inhibitors |
| Camptothecin: TI-1, metabolite SN-38, Tx: advanced colon cancer ADR: GI toxicity (massive diarrhea) | Irinotecan |
| Anthracycline: TI-2, ADR: heart failure (tx: dexrazoxane) | Doxorubicin |
| Epipodophyllotoxin: TI-2, Tx: testicular (combo w/ cisplatin & bleomycin), lung cancer, leukemia | Etoposide |
| MOA of Vinblastine, Vincristine | Vinca Alkaloids: inhibit microtubule polymerization |
| MOA of Paclitaxel, Docetaxel | Taxanes: inhibit microtubule depolymerization |
| Tx: lymphomas, testicular (combo w/ cisplatin, bleomycin), ADR: myelosuppression | Vinblastine |
| Tx: ALL, Hodgkin's, NHL, ADR: peripheral neuropathy | Vincristine |
| Tx: ovarian, breast, NSCLC; ADR: hypersensitivity (Tx: dexamethasone), myalgia, myelosuppression, lung, peripheral neuropathy "stock & glove" | Paclitaxel |
| Tx: breast cancer, NSCLC, ADR: hypersensitivity (Tx: dexamethasone), fluid retention, myelosuppression | Docetaxel |