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Drug Interactions with Cancer Drugs |
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Definition
Warfarin (blood thinner) & Hydrochlorothiazide (diuretic) |
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Tissues with high growth fraction |
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Definition
Bone marrow, GI tract, hair follicles, buccal mucosa, & sperm forming cells |
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Severe vomiting, nausea, stomatitis & alopecia |
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Most common dose-limiting toxicity |
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Definition
Myelosuppression: can manifest as leukopenia, thrombocytopenia & anemia |
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Alkylating Agents: Mechanism of Action |
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Definition
Form covalent linkages with DNA: alkylation of DNA leads to intra- & inter-strand cross-linking, which prevents the tumor from unwinding DNA for mRNA production or DNA replication |
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Alkylating agent; may cause hemorrhagic cystitis due to accumulation of acrolein; Cystitis can be reduced or prevented via Mesna |
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Alkylating agent; may cause nephrotoxicity &/or ototoxicity |
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Structural analogs to compounds necessary for cell proliferation |
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ie. Methotrexate; bind to active site of dihydrofolate reductase & interfere with de novo synthesis of thymidylate, purine nucleotides & serine & methionine |
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Definition
Antimetabolite; folic acid analog; can also affect healthy cells, which are saved via Leucovorin (sparing GI & bone marrow toxicity from high dose) |
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Definition
Antimetabolite; active compound FdUMP covalently binds thymidylate synthetase & blocks de novo synthesis of thymidylate (interfering with DNA synthesis & function, RNA processing, & mRNA translation); most widely used in CRC |
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Definition
Vinblastine & vincristine; natural antimitotic drug; bind to beta-tubulin & inhibit microtubule assembly (M phase); hair loss & local cellulitis if extravasated |
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Paclitaxel & docetaxel; natural antimitotic drug; bind to beta-tubulin & promote microtubule formation & stabilization; can cause myelosuppression & peripheral sensory neuropathy |
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Definition
Topotecan & irinotecan; inhibit activity of topoisomerase I (results in DNA damage & blockade of DNA replication & transcription); can cause myelodepression, NVD |
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Definition
Bind to DNA through intercalation bw specific bases & block the synth of DNA, RNA or both |
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Doxorubicin; antitumor antibiotic; prod free radcals which can cause cardiotoxicity |
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Antitumor antibiotic; binds tightly to dsDNA & intercalates bw adjacent GC pairs; can cause anorexia, NV |
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Definition
Antitumor antibiotic; leads to ss & ds breaks in DNA; causes minimal myelosuppression; can cause pulmonary toxicity |
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Antitumor antibiotic; prodrug; cross-links DNA strands |
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Etoposide & teniposide; inhibit topoisomerase II; leads to DNA damage through strand breakage |
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Definition
Asparaginase; hydrolyzes circulating L-aspargine into aspartic acid & ammonia (inhibiting protein synth); effective against ALL bc req exogenous source; main adverse effect is acute hypersensitivity reaction |
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Definition
Inhibibits ribonucleoside diphosphate reductase & blocks the conversion of ribonucleotides to deoxyribonucleotides; Adverse effects: myelosuppression, HA, lethargy, maculopapular skin rash |
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Definition
Binds to 1+ nuclear receptors & induces clonal proliferation &/or granulocyte differentiation; may cause vitamin A toxicity |
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Induces apoptosis by causing the release of cytochrome C with caspase activation |
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Definition
Protein tyrosine kinase inhibitor; specificity for PDGFR, ABL & KIT; inhibits BCR-ABL from philadelphia chromosomal translocation (chronic myelogenous leukemia) |
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Definition
Tx of non-small cell lung cancer |
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Destabilizes microtubules & inhibits mitosis; tx prostate cancer; causes myelosuppression & estrogen side effects |
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Monoclonal antibody; binds to HER2/neu receptor & inhibits IC signaling events & neoplastic cell proliferation; can cause cardiotoxicity |
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Prednisone; suppress mitosis in lymphocytes |
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Definition
2nd line therapy for neoplasms; stimulate appetite & restore sense of well-being in cachectic patients |
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Antiestrogens & Antiandrogens |
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Definition
Therapy for prostate & mammary gland cancers |
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Term
Selective estrogen-receptor modulators (SERMs) |
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Definition
Tamoxifen, Competitive inhibitors of estradiol binding to the ER & can prod estrogenic or anti-estrogenic effects depending on specific organ; Used on pre- & post-menopausal women |
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Term
Selective estrogen-receptor downregulators (SERDs) |
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Definition
Fulvestrant; bind to ERs & inhibit dimerization while increasing protein degradation; on pre- & post-menopausal women |
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Term
Aromatase Inhibitors (AIs) |
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Definition
Anastrazole, Letrozole & Exemestane; Inhibit aromatase, which is responsible for conversion of androstenedione & testosterone to the estrogens estrone & estradiol; only postmenopausal women (Post: conversion in periphery, Pre: ovary) |
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Antiandrogen Therapy (ADT) |
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Definition
Carcinoma of the prostate is uniquely dependent upon hormonal stimulation with androgens |
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Gonadotropin-releasing hormone (GnRH)agonist |
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Definition
Leuprolide; Suppression of androgens from pituitary; reduction of testicular prod of testosterone to levels seen with surgical castration (initially surges due to surge in LH & FSH) |
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Gonadotropin-releasing hormone (GnRH) antagonist |
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Definition
Abarelix; rapidly reduce serum testosterone levels without the transient initial increase observed after GnRH agonists |
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Androgen Receptor (AR) Blockers |
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Definition
Completely inhibit the natural ligands of the AR |
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Complete Androgen Blockade (CAB) Chemo |
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Definition
Flutamide; Combined admin of AR blockers & GnRH agonists; often used in prostate cancer to block androgens from adrenals |
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