Cancer drugs Flashcards
methotrexate moa
folic acid analog that inhibits DHFR, decreasing DNA and protein synthesis
methotrexate toxicity
myelosuppression, reversible with leucovorin; macro vesicular fatty change in liver; mucositis, teratogenic
5-FU moa
pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid; this inhibits thymidylate synthetase; decreasing DNA and protein synthesis
cytarabine moa
pyrimidien analog that inhibits DNA polymerase
5-FU toxicity
myelosuppression and photosensitivity; tx overdose with uridine;
cytarabine toxicity
leukopenia, thrombocytopenia, megaloblastic anemia,
azathioprine, 6-MP, and 6-TG moa
purine analogs; decrease de novo purine synthesis; activated by HGPRT and metabolized by xanthine oxidase
azathioprine, 6-MP, and 6-TG toxicity
bone marrow suppression, GI, and liver toxicity; increased toxicity with allopurinol
dactinomycin moa
intercalates in DNA
doxorubicin and daunorubicin moa
generation of free radicals, DNA intercalation
doxorubicin and daunorubicin toxicity
dilated cardiomyopathy; dexrazoxane used to prevent cardiotoxicity
belomycin moa
induces free radical formation which causes breaks in DNA strands
bleomycin toxicity
pulmonary fibrosis, skin changes, mucositis
cyclophosphamide and ifosfamide moa
covalently X-link (inter strand) DNA at guanine N-7; require bioactivation by liver
cyclophosphamide and ifosfamide toxicity
hemorrhagic cystitis; partially prevented by meson (binds to toxic metabs)
nitrosoureas (carmustine, lomustine, semustine, streptozocin) moa
cross link DNA
cross the BBB
require bioactivation
nitrosoureas (carmustine, lomustine, semustine, streptozocin)
CNS toxicity - convulsions, dizziness, ataxia
busulfan moa
cross links DNA
busulfan toxicity
severe myelosuppression; pulmonary fibrosis, hyperpigmentation
vinca alkaloids moa
bind beta-tubulin and inhibit polymerization of microtubules (M-phase cycle arrest)
paclitaxel moa
hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down
cisplatin, carboplatin moa
cross link DNA
vinca alkaloids toxicty
peripheral neuritis
cisplatin and carboplatin toxicity
nephrotoxicity and acoustic nerve damage; prevent nephrotoxicity with amifostine (free radical scavenger)
etoposide and teniposide moa
inhibits topoisomerase II and increases DNA degradation (cannot relieve supercoils)
irinotecan, topotecan moa
inhibit toposiomerase I and prevent DNA unwinding and replication
hydroxyurea moa
inhibits ribonucleotide reductase, decreasing DNA synthesis (S-phase specific)
prednisone moa
triggers apoptosis in cancer cells
tamoxifen raloxifene moa
selective estrogen receptor modulators; antagonists in breast and agonists in bone;
tamoxifen toxicity
partial agonist in endometrium which increases the risk of endometrial cancer; hot flashes
trastuzumab moa
mAB to HER-2 (erbB2)
trastuzumab toxicity
cardiotoxicity
imatinib moa
tyrosine kinase inhibitor of BCR-ABL
rituximab moa
mAB to CD20
vermurafenib moa
small molecule inhibitor of forms of the braf kinase with v600E mutation
Bevacizumab moa
mAB against VEGF; inhibits agiogenesis
S-phase specific
etoposide and antimetabolites (MTX, 5-FU, cytarabine, axathioprine, 6-MP, 6-TG)
M-phase specific
vinca alkaloids and taxanes
G2 phase specific
bleomycin and etoposide
