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Pharm Ch 37

Cancer - Genome Synthesis

QuestionAnswer
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
Created by: fmuralid
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