antineoplastic Flashcards
cyclophosphamide
o Transferring alkyl group to cellular constituent (can be mon of bifunctional)
o Interstrnd DNA cross links
o Oxidized by CYP 450
o Alopecia
o Myelosuppression
o Hemorrhagic cystitis- acrolein metabolite irritates bladder lining (give water)
o Acute/delayed N/V
cisplatin
o platinum analog Non-specific o DNA cross link o Hydration rqd to convert to active species o N/V is HUGE o Renal toxicity o Myelosuppression o Hepatotoxicity o Anaphylaxis
antimetabolites
antifolates
fluopyrimidine
purine antagonist
antifoliate (methotrexate)
o Irreversible binding to DHFR- dec reduced folates incorporated into purine bases
o Mucositis
o Diarrhea
o Myelosuppression
o CAUTION in renally eliminated drugs
Fluopyrimidine (5-fluorouracil)
o False pyrimidine
o Inhibits thymidylate synthase- rate limiting step
o Myelosuppression
o Mucositis with continued infusion, diarrhea
o Skin- hand and foot syndrome
♣ Grade 1- numbness, discomfort in hands and feet
♣ Grade 2- painful erythema and swelling of hands/feet
♣ Grade 3- moist desquamation, ulceration, blistering, severe pain
o neurotoxicity
Purine antagonist (6-MP)
o Pediatrics, immunosuppressant
o inhibit Inosinic acid to adenine and guanine to inhibit DNA syn.
o Myelosuppression
o Pulmonary fibrosis
o Pancreatitis
o DI- allopurinol-reduce 6-MP dose by 50-75%
natural products
paclitaxel
docetaxel
paclitaxel
o Yew tree
o Microtubule assembly results in inhibition of mitosis, cell division
o ACUTE
♣ N/V, arrhythmias, hypersensitivity
o DELAYED
♣ Myelosuppression, peripheral neuropathy
docetaxel
o Semisynthetic from European yew tree
o ACUTE
♣ Hypersensitivity (pre medicate with steroid)
o DELAYED
♣ Neurotoxicity, fluid retention, myelosuppression
Antitumor Ab (anthracyclines/doxorubicin)-
bind with DNA to produce irreversible complexes that inhibit cell division
Vinca alkaloids (vincristine)
stop cell division by binding to tubulin (mitotic spindle)
Hormones (tamoxifen, anastrazole)
both hormone agonists and antagonists used in breast and prostrate cancer
Podophyllotoxins (etoposide)
inhibits topiosmerase 2
Camptothecins (topotecan)
inhibits topoisomerase 1
Tyrosine kinase inhibitor (imatinib)
interrupt intracellular signaling pathway