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Antineoplastic (chemo). Alkylating agent class. Mechanism: 3 membered ring attaches to DNA, esp guanine. DNA is crosslinked, strand breaks, apoptosis. |
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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. |
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Antineoplastic (chemo). Nitrogen gas/ Alkylating agent. Also makes acrolein, so give with Mesna. Use: testis cancer and sarcoma. |
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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. |
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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. |
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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. |
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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. |
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Antineoplastic (chemo). Antimetabolite. Can be given alone or with Leucovorin. Pro-drug. Inhibits Thymidylate Synthase (which makes dTMP). Tox: mucisitis, severe, dose dependent. |
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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. |
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Antineoplastic (chemo). Vinca Alkaloid. Binds tubulin of the mitotic spindle, causing metaphase arrest. NOT myleosupressive, but IS neurotoxic. |
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Antineoplastic (chemo). Vinca Alkaloid. Binds tubulin of the mitotic spindle, causing metaphase arrest. IS myleosupressive, but NOT neurotoxic. |
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=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. |
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=taxotere. see Paclitaxel. |
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= 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. |
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Antineoplastic (chemo). Antibiotic. nicks DNA and inhibits DNA ligase. Generates ROS. Tox: mild mylosupression, Pulmonary** fibrosis dose dependent (terrible). Use: Hodgkins, testicuar. |
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Antineoplastic (chemo). Antibiotic. Prodrug, no Topo1 inhibition. Use: colon cancer. Tox: delayed diarrhea*, mild myelosupression. |
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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. |
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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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