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Cancer Drugs
N/A
41
Pharmacology
Graduate
11/23/2009

Additional Pharmacology Flashcards

 


 

Cards

Term
Drug Interactions with Cancer Drugs
Definition
Warfarin (blood thinner) & Hydrochlorothiazide (diuretic)
Term
Tissues with high growth fraction
Definition
Bone marrow, GI tract, hair follicles, buccal mucosa, & sperm forming cells
Term
Common adverse effects
Definition
Severe vomiting, nausea, stomatitis & alopecia
Term
Most common dose-limiting toxicity
Definition
Myelosuppression: can manifest as leukopenia, thrombocytopenia & anemia
Term
Alkylating Agents: Mechanism of Action
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
Term
Cyclophosphamide
Definition
Alkylating agent; may cause hemorrhagic cystitis due to accumulation of acrolein; Cystitis can be reduced or prevented via Mesna
Term
Cisplatin
Definition
Alkylating agent; may cause nephrotoxicity &/or ototoxicity
Term
Antimetabolites
Definition
Structural analogs to compounds necessary for cell proliferation
Term
Folic acid analogs
Definition
ie. Methotrexate; bind to active site of dihydrofolate reductase & interfere with de novo synthesis of thymidylate, purine nucleotides & serine & methionine
Term
Methotrexate
Definition
Antimetabolite; folic acid analog; can also affect healthy cells, which are saved via Leucovorin (sparing GI & bone marrow toxicity from high dose)
Term
5-fluorouracil
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
Term
Vinca Alkaloids
Definition
Vinblastine & vincristine; natural antimitotic drug; bind to beta-tubulin & inhibit microtubule assembly (M phase); hair loss & local cellulitis if extravasated
Term
Taxanes
Definition
Paclitaxel & docetaxel; natural antimitotic drug; bind to beta-tubulin & promote microtubule formation & stabilization; can cause myelosuppression & peripheral sensory neuropathy
Term
Camptothecin analogs
Definition
Topotecan & irinotecan; inhibit activity of topoisomerase I (results in DNA damage & blockade of DNA replication & transcription); can cause myelodepression, NVD
Term
Antitumor Antibiotics
Definition
Bind to DNA through intercalation bw specific bases & block the synth of DNA, RNA or both
Term
Anthracyclines
Definition
Doxorubicin; antitumor antibiotic; prod free radcals which can cause cardiotoxicity
Term
Dactinomycin
Definition
Antitumor antibiotic; binds tightly to dsDNA & intercalates bw adjacent GC pairs; can cause anorexia, NV
Term
Bleomycin
Definition
Antitumor antibiotic; leads to ss & ds breaks in DNA; causes minimal myelosuppression; can cause pulmonary toxicity
Term
Mitomycin
Definition
Antitumor antibiotic; prodrug; cross-links DNA strands
Term
Epipodophyllotoxins
Definition
Etoposide & teniposide; inhibit topoisomerase II; leads to DNA damage through strand breakage
Term
Enzymes
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
Term
Hydroxyurea
Definition
Inhibibits ribonucleoside diphosphate reductase & blocks the conversion of ribonucleotides to deoxyribonucleotides; Adverse effects: myelosuppression, HA, lethargy, maculopapular skin rash
Term
Retinoids
Definition
Binds to 1+ nuclear receptors & induces clonal proliferation &/or granulocyte differentiation; may cause vitamin A toxicity
Term
Arsenic Trioxide
Definition
Induces apoptosis by causing the release of cytochrome C with caspase activation
Term
Imatinib
Definition
Protein tyrosine kinase inhibitor; specificity for PDGFR, ABL & KIT; inhibits BCR-ABL from philadelphia chromosomal translocation (chronic myelogenous leukemia)
Term
Erlotinib & Gefitinib
Definition
Tx of non-small cell lung cancer
Term
Thalidomide
Definition
Tx of multiple myeloma
Term
Estramustine
Definition
Destabilizes microtubules & inhibits mitosis; tx prostate cancer; causes myelosuppression & estrogen side effects
Term
Trastuzumab
Definition
Monoclonal antibody; binds to HER2/neu receptor & inhibits IC signaling events & neoplastic cell proliferation; can cause cardiotoxicity
Term
Glucocorticoids
Definition
Prednisone; suppress mitosis in lymphocytes
Term
Progestins
Definition
2nd line therapy for neoplasms; stimulate appetite & restore sense of well-being in cachectic patients
Term
Antiestrogens & Antiandrogens
Definition
Therapy for prostate & mammary gland cancers
Term
Selective estrogen-receptor modulators (SERMs)
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
Term
Selective estrogen-receptor downregulators (SERDs)
Definition
Fulvestrant; bind to ERs & inhibit dimerization while increasing protein degradation; on pre- & post-menopausal women
Term
Aromatase Inhibitors (AIs)
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)
Term
Antiandrogen Therapy (ADT)
Definition
Carcinoma of the prostate is uniquely dependent upon hormonal stimulation with androgens
Term
Gonadotropin-releasing hormone (GnRH)agonist
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)
Term
Gonadotropin-releasing hormone (GnRH) antagonist
Definition
Abarelix; rapidly reduce serum testosterone levels without the transient initial increase observed after GnRH agonists
Term
Androgen Receptor (AR) Blockers
Definition
Completely inhibit the natural ligands of the AR
Term
Complete Androgen Blockade (CAB) Chemo
Definition
Flutamide; Combined admin of AR blockers & GnRH agonists; often used in prostate cancer to block androgens from adrenals
Term
Cancer Vaccines
Definition
Hep B & HPV
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