Oncology Rx Flashcards
Methotrexate (MTX)
1) CA: leukemia, lymphoma, choriocarcinoma, sarcoma; non-CA: abortion, ectopic preg, rheumatoid arthritis, psoriasis 2) folate analog: inhibits DHFR –> decr dTMP –> decr DNA + protein syn 3) myelosuppression (reverse w/ leucovorin); macrovesicular fatty liver change; mucositis; teratogenic 4) S-phase specific
5-fluorouracil (5-FU)
1) colon CA, basal cell carcinoma (topical) 2) pyrimidine analog bioactivated to 5F-dUMP (covalently complexes folate) –> complex inhibits thymidylate synthase –> decr dTMP –> decr DNA + protein syn 3) myelosuppression (not reversible w/ leucovorin); OD rescue w/ thymidine; photosensitivity 4) S-phase specific
Cytarabine (arabinofuranosyl cytidine)
1) leukemia, lymphoma 2) pyrimidine analog –> inhibit DNA polymerase 3) leukopenia, thrombocytopenia, megaloblastic anemia 4) S-phase specific
Azathioprine
1) leukemias 2) purine (thiol) analog –> decr de novo purine syn 3) BM, GI, liver; metabolized by xanthine oxidase so incr toxicity w/ allopurinol 4) S-phase specific; activated by HGPRT
6-mercaptopurine (6-MP)
1) leukemias 2) purine (thiol) analog –> decr de novo purine syn 3) BM, GI, liver; metabolized by xanthine oxidase so incr toxicity w/ allopurinol 4) S-phase specific; activated by HGPRT
6-thioguanine (6-TG)
1) leukemias 2) purine (thiol) analog –> decr de novo purine syn 3) BM, GI, liver; metabolized by xanthine oxidase so incr toxicity w/ allopurinol 4) S-phase specific; activated by HGPRT
Dactinomycin (actinomycin D)
1) Wilm’s tumor, Ewin’s sarcoma, rhabdomyosarcoma; peds tumors 2) intercalates in DNA 3) myelosuppression 4) N/A
Doxorubicin (Adriamycin)
1) solid tumors, leukemias, lymphomas 2) makes ROS; non-covalently intercalate in DNA –> breaks DNA –> decr replication 3) cardiotoxicity* (dilated cardiomyopathy; use dexrazoxane, Fe chelator, to prevent), myelosuppression, alopecia; toxic to tissues following extravasation 4) N/A
Daunorubicin
1) solid tumors, leukemias, lymphomas 2) makes ROS; non-covalently intercalate in DNA –> breaks DNA –> decr replication 3) cardiotoxicity* (dilated cardiomyopathy; use dexrazoxane, Fe chelator, to prevent), myelosuppression, alopecia; toxic to tissues following extravasation 4) N/A
Bleomycin
1) testicular CA, Hodgkin’s lymphoma 2) ROS formation –> causes breaks in DNA strands 3) pulm fibrosis*, skin changes; minimal myelosuppression 4) N/A
Cyclophosphamide
1) solid tumors, leukemia, lymphoma, some brain CAs 2) alkylating agent: covalently X-link DNA at guanine N-7 3) myelosuppression; hemorrhagic cystitis (partly prevent w/ mesna, thiol grp of mesna binds toxic metabolite) 4) need liver bioactivation
Ifosfamide
1) solid tumors, leukemia, lymphoma, some brain CAs 2) alkylating agent: covalently X-link DNA at guanine N-7 3) myelosuppression; hemorrhagic cystitis (partly prevent w/ mesna, thiol grp of mesna binds toxic metabolite) 4) need liver bioactivation
Carmustine
1) brain tumors (incl glioblastoma multiforme) 2) alkylating agent: nitrosourea 3) CNS toxicity: dizziness, ataxia 4) needs bioactivation; X’s BBB –> CNS
Lomustine
1) brain tumors (incl glioblastoma multiforme) 2) alkylating agent: nitrosourea 3) CNS toxicity: dizziness, ataxia 4) needs bioactivation; X’s BBB –> CNS
Semustine
1) brain tumors (incl glioblastoma multiforme) 2) alkylating agent: nitrosourea 3) CNS toxicity: dizziness, ataxia 4) needs bioactivation; X’s BBB –> CNS
Streptozocin
1) brain tumors (incl glioblastoma multiforme) 2) alkylating agent: nitrosourea 3) CNS toxicity: dizziness, ataxia 4) needs bioactivation; X’s BBB –> CNS
Busulfan
1) CML; also to ablate BM before BMT 2) alkylating agent 3) pulm fibrosis*; hyperpigmentation 4) N/A
Vincristine
1) solid tumors, leukemias, lymphomas 2) microtubule inhibitor: alkaloid that binds to tubulin in M phase + blocks polymerization so mitotic spindle can’t form 3) neurotoxicity: areflexia, periph neuritis; paralytic ileus 4) N/A
Vinblastine
1) solid tumors, leukemias, lymphomas 2) microtubule inhibitor: alkaloid that binds to tubulin in M phase + blocks polymerization so mitotic spindle can’t form 3) BM suppression (VinBLASTine BLASTS Bone Marrow) 4) N/A
Paclitaxel
1) ovarian + breast carcinomas 2) microtubule inhibitor: hyperstabilizes polymerized microtubules in M phase so mitotic spindle can’t break down (blocks anaphase) 3) myelosuppression, hypersensitivity 4) N/A
Cisplatin
1) testicular, bladder, ovary, lung carcinomas 2) X-links DNA 3) nephrotoxicity (prevent w/ amifostine, ROS scavenger), acoustic nerve damage, chloride diuresis 4) N/A
Carboplatin
1) testicular, bladder, ovary, lung carcinomas 2) X-links DNA 3) nephrotoxicity (prevent w/ amifostine, ROS scavenger), acoustic nerve damage, chloride diuresis 4) N/A
Etoposide
1) solid tumors, leukemias, lymphomas 2) topo II inhibitor –> incr DNA degradation 3) myelosuppression, GI irritation, alopecia 4) N/A
Teniposide
1) solid tumors, leukemias, lymphomas 2) topo II inhibitor –> incr DNA degradation 3) myelosuppression, GI irritation, alopecia 4) N/A
Hydroxyurea
1) melanoma, CML, sickle cell dz (incr HbF) 2) inhibits ribonucleotide reductase –> decr DNA syn (S-phase specific) 3) BM suppression, upset GI 4) N/A
Prednisone
1) CA chemotx: CLL, non-Hodgkin’s lymphomas; immunosuppressant (autoimmune dz) 2) glucocorticoid; may trigger apoptosis; may work on non-dividing cells 3) Cushing-like sx’s; immunosuppression, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis 4) N/A
Prednisolone
1) CA chemotx: CLL, non-Hodgkin’s lymphomas; immunosuppressant (autoimmune dz) 2) glucocorticoid; may trigger apoptosis; may work on non-dividing cells 3) Cushing-like sx’s; immunosuppression, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis 4) N/A
Tamoxifen
1) breast CA tx + prophylaxis; prevent osteoporosis 2) SERM: R antagonist in breast + agonist in bone; block estrogen binding to ER+ cells 3) partial agonist in endometrium –> incr endometrial CA risk; “hot falshes” 4) compare toxicity to raloxifene
Raloxifene
1) breast CA tx + prophylaxis; prevent osteoporosis 2) SERM: R antagonist in breast + agonist in bone; block estrogen binding to ER+ cells 3) no incr in endometrial carcinoma b/c it’s an endometrial antagonist 4) compare toxicity to tamoxifen
Trastuzumab (Herceptin)
1) HER-2 (+) breast CA 2) monoclonal ab against HER-2 (c-erbB2), a tyrosine kinase –> kill breast CA cells taht overexpress HER-2 (ab-dependent cytotoxicity) 3) cardiotoxicity 4) N/A
Imatinib (Gleevec)
1) CML, GI stromal tumors 2) Ph chr bcr-abl tyroxine kinase inhibitor 3) fluid retention 4) N/A
Rituximab
1) non-Hodgkin’s lymphoma, rheumatoid arthritis (w/ MTX) 2) monoclonal ab against CD20 (found on most B-cell neoplasms) 3) N/A 4) N/A
Vemurafenib
1) metastatic melanoma 2) small molec inhibitor of B-Raf kinases that have V600E mute 3) N/A 4) N/A
Bevacizumab
1) solid tumors 2) monoclonal ab against VEGF –> inhibits angiogenesis 3) N/A 4) N/A
