antineoplastics Flashcards
Methotrexate
folic acid analog, competitively inhibits dihydrofolate reductase -> dec. thymidine synthesis. Tx: CA, abortion, RA, psoriasis, IBD, vasculitis. Tx: myelosuppresion (reversible w/folate), hepatotox, mucositis, pulm fibrosis.
5-FU
pyrimidine analog: inhibits thymidylate synthase -> dec. thymidine synthesis. Tx: colon pancreatic, basal cell CA (topical). tox: myelosuppression (irreversible)
6-MP
dec. de novo purine synthesis
hydroxyurea
inhibits ribonucleotide reductase -> dec. DNA synthesis. Tx: melanoma, CML, HbSS. tox: severe myelosupp, GI upset
alkylating agents
cross-links DNA
cisplatin, carboplatin
cross-links DNA. Tx: testicular, bladder, ovary, lung CA. tox: nephrotox (prevent w/amifostine (free rad scavenger) and chloride diuresis), ototox
bleomycin
induces free radical damage -> DNA strand breakage. Tx: testicular CA, Hodgkins. tox: pulm. fibrosis, inc. skin pigment, mucositis. minimal myelosupp.
dactinomycin
DNA intercalator. Tx: wilms, ewing, rhabdomyosarcoma = CHILDHOOD tumors. tox: myelosupp.
doxorubicin
DNA intercalator + generates free radicals -> DNA breaks. Tx: solid tumors, leukemia, lymphoma. tox: cardiotoxic (dilated. prevent w/Fe chelator dexrazoxane), myelosupp. alopecia. toxic if extravasates.
etoposide, teniposide
inhibits topoisomerase II (makes DNA strand breaks to edit DNA) - like fluoroquinolones. Tx: solid tumors (testicular, small cell lung), leukemias, lymphomas. tox: myelosupp, GI upset, alopecia.
irinotecan, topotecan
inhibits topoisomerase I and prevents DNA unwinding + replication. Tx: colon Ca (irino), ovarian and small cell lung (topo). tox: severe myelosupp, diarrhea.
vinca alkaloids (vincristine, vinblastine)
inhibit microtubule formation (M phase arrest). Tx: solid tumors, leukemias, Hodgkins (blastine), nonH lymphoma (cristine). tox: cristine: neurotox. blastine: blasts bone marrow (myelosupp).
paclitaxel, other taxols
inhibits microtubule disassembly (stuck in M phase, no anaphase). Tx: ovarian and breast CA. tox: myelosupp, alopecia, hypersensitivity.
azathioprene
= purine (thiol) analog. metabolized into 6-MP. dec. de novo purine synthesis. metabolized by xanthine oxidase
cladribine
purine analog. many MoAs: inhibits DNA polymerase, -> DNA strand breaks, etc. Tx: hairy cell leukemia. tox: myelosuppression, nephrotox, neurotox.