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EXAM2:Pharm L14+15
Chemo drugs
18
Medical
Graduate
05/26/2009

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Cards

Term
Nitrogen Mustards
Definition
Antineoplastic (chemo). Alkylating agent class. Mechanism: 3 membered ring attaches to DNA, esp guanine. DNA is crosslinked, strand breaks, apoptosis.
Term
Cyclophosphamide
Definition
Antineoplastic (chemo). Nitrogen gas/ alkylating agent: most widely used. Pro-drug, activated by P450s. Makes 2 toxic metabolites. Phosophoramide mustard is the active agent, Acrolein is toxic to the bladder, so give with Mesna to avoid toxicity. Used in Hodgkins.
Term
Ifosfamide
Definition
Antineoplastic (chemo). Nitrogen gas/ Alkylating agent. Also makes acrolein, so give with Mesna. Use: testis cancer and sarcoma.
Term
Cisplatin
Definition
Antineoplastic (chemo). Platinum-based Alkylating agent. Mech: covalently binds and platinates DNA bases, disrupts DNA function, DNA crosslinked at guanines. Tox: renal insufficiency with Mg wasting, hypoK, nausea and vometing, peripheral neuropathy, auditory impairment, some myelosupression (not a ton). Give with Mg suppliment and monitor electrolytes. Use with caution with other nephrotoxic drugs, dont give if creatinine clearance is low, maintain diuresis. Curative for testicular cancer, good for ovarian.
Term
Carboplatin
Definition
Antineoplastic (chemo). Platinum based Alkylating agent. Platinates DNA like cisplatin. Not cross resistant with cisplatin. Tox: myelosupression*** esp WBCs and platlets, Nausea and vometing, much less nephrotoxic then cisplatin, give to patients with decreased renal fxn. Dose in proportion to creatinine clearence.
Term
Methotrexate
Definition
Antineoplastic (chemo). Antimetabolite. A folic acid analog. Inhibits dihydrofolate reductase, leading to depletion of folates, cell cant make DNA. Renal excretion, maintain diuresis. Use Leucovorin to reverse toxicities. Tox: Myelosupression, Mucositis, Renal tubular obstruction, Pneumonitis. Caution: reduce dose with creatinine clearance. monitor plasma concentrations.
Term
Leucovorin
Definition
Antineoplastic (chemo); not really a cytotoxic drug. reduced folate molecule. Give wtih Methotrexate to reverse toxicity. Protects normal cells only, not tumor cells, provides a source of folate for resynthesis of DNA. Give with 5-FU to create a ternary complex of FU+ L + TS which is more active than just FU. Survival up from 20 percent to 40 percent.
Term
5-Fluorouracil
Definition
Antineoplastic (chemo). Antimetabolite. Can be given alone or with Leucovorin. Pro-drug. Inhibits Thymidylate Synthase (which makes dTMP). Tox: mucisitis, severe, dose dependent.
Term
Gemcitibine
Definition
Antineoplastic (chemo). Antimetabolite. Useful in solid tumors only. Fool cells into thinking they have 2x strand breaks. Is a DNA poly inhibitor, ribonucleotide reductase inhibitor, incoorporated into DNA, leading to strand termination. Pancreating cancer (1st drug!), bladder, lung. Tox: mild myelosupression, flu-like. Radiosensitizer.
Term
Vincristine
Definition
Antineoplastic (chemo). Vinca Alkaloid. Binds tubulin of the mitotic spindle, causing metaphase arrest. NOT myleosupressive, but IS neurotoxic.
Term
Vinblastine
Definition
Antineoplastic (chemo). Vinca Alkaloid. Binds tubulin of the mitotic spindle, causing metaphase arrest. IS myleosupressive, but NOT neurotoxic.
Term
Paclitaxel
Definition
=taxol. Antineoplastic (chemo). Taxane. Binds to tubulin at diff site from vinca alkyloids. increases microtubule number: binds alpha of tubulin, promotes polymierization and blocks depolymerization ("stuck"). binds to BCL2, letting BIM go to mitochondria and cause apoptosis. Tox: myleosupressive, peropheral neuropathy, allergies from sugars. Use: ovarian, prostate, breast, lung.
Term
Docetaxel
Definition
=taxotere. see Paclitaxel.
Term
Doxorubicin
Definition
= Adriamycin. Antineoplastic (chemo). Antibiotic. Intercalcation = false mechanism. Fe cycling and ROS = mech of cardiac toxicity bc heart lacks catalase. Newest mech = stabalizes complex btw Topo2 and DNA, cell senses 2x strand breaks. Cap dose to prevent cardiac tox. Other tox: myelosupression, mucositis, hair loss, skin necrosis if extavasated, radiation sensitizer.
Term
Bleomycin
Definition
Antineoplastic (chemo). Antibiotic. nicks DNA and inhibits DNA ligase. Generates ROS. Tox: mild mylosupression, Pulmonary** fibrosis dose dependent (terrible). Use: Hodgkins, testicuar.
Term
Irinotecan
Definition
Antineoplastic (chemo). Antibiotic. Prodrug, no Topo1 inhibition. Use: colon cancer. Tox: delayed diarrhea*, mild myelosupression.
Term
Tamoxifen
Definition
Antineoplastic (chemo). Effects hormones. Only ER+ patients respond. Estrogen receptor inhibitor. Tox: bone pain, hyperCa, menopause, more endrometrial cancer, thrombosis. Use: adjuvunct in breast cancer.
Term
Leuprolide
Definition
Antineoplastics (chemo). Gonadotrophin-releasing hormone analogues and LHRH analogs. "flare": short term agonists of gonadotrophins, avoid with antiandrogens. long term antagonists of testosterone (levels fall as if had a castration). Use: prostate cancer. Tos: menopause in men, loss of libido, impotence.
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