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20 Cards in this Set
- Front
- Back
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Mechlorethamine
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Class - Alkylating agent
+ Nitrogen mustard + IV administration only - subcutaneous causes slough, necrosis - often arterial supply to tumor + fast half-life (several minutes; reacts rapidly) + Adverse effects - Acute -> nausea, vomiting - Delayed -> decreased blood counts, moderate with most doses; minimum levels 10-12 days after treatment, recovery 3-6 weeks - vesicant (blistering agent), caustic (cause corrosion) to skin and mucous membranes Primary use - Hodgkin's disease, part of "MOPP" |
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Cyclophosphamide
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Class - Alkylating agent
+ Oral or Intravenous administration + Activated by host metabolism (primarily in liver) + Adverse effects - Acute-- Nausea and vomiting - Delayed-- bone marrow depression (moderate, dose-related), Alopecia, Sterile hemorrhagic cystitis (irritation and damage to the lining of the bladder; can cause pain, and blood in the urine) Toxic metabolites: Acrolein & Phosphoramide mustard Metabolized by p450s and converted to active metabolites + Acrolein gets excreted in urine - Major cause of cystitis + Protect pt by diluting and flushing it out as fast as you can + Mesna - sulfur containing drug - Thiol that reacts with acrolein |
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Cis-Platin
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Class - Alkylating agents
Bifunctional "platinating agent"-- Cross-links DNA Blocks DNA synthesis (blocks DNA opening) Administer intravenous, cleared in urine Relatively non-toxic to bone marrow Acute adverse effects Severe nausea and vomiting (use HT3 antagonists) Renal Toxicity is dose-limiting; ensure adequate hydration Carboplatin– less nausea and renal, more myelosuppression Oxaliplatin– less renal, but neurotoxic **Side note: A lot of drugs that exhibit renal toxicity are also toxic to the inner ear Oto-toxicity Can be hearing loss; vestibular fx loss |
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Methotrexate
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Class - Antimetabolites (folate analog)
Administered orally, IV, intrathecally Excreted in urine May give high dose, followed by "rescue" with folinic acid (Citrovorin, leucovorin) Efficacy of high dose-- rescue debated Anti-folate effects (bone marrow, GI) Chronic use can produce hepatotoxicity Resistance-- decreased drug accumulation, amplified DHFR, altered DHFR **Side note: Folic acid is the cofactor used anytime we have the donation of single C units Important in things like synthesis of thymidine |
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6-Mercaptopurine, 6-thioguanine
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Class- antimetabolites (Purine analogs)
Oral administration sulfur containing analogs Well-tolerated; bone marrow depression only at high doses Blocks DNA and RNA synthesis—6-MP inhibits AMP and GMP synthesis, 6-TG incorporated into RNA and DNA altering function Resistance from decrease in hprt activity, or increase in alkaline phosphatase |
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5-Fluorouracil (5-FU), Cytarabine, Gemcitabine
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Class - Antimetabolites (Pyrimidine analogs)
Far more toxic than purines: Bone marrow, GI 5-FU inhibits thymidylate synthase (“Thymineless death”), enhanced by folinic acid Cytarabine is cytosine analogue, chain terminator Gemcitabine is cytosine analogue, inhibits polymerase and chain terminator |
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Vinblastine, Vincristine
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Class - Plant Alkaloids (Vinca Alkaloids)
Isolated from Vinca rosea (Periwinkle) Inhibits/reverses tubulin polymerization, disrupts mitotic spindles (microtubules) Causes Metaphase Arrest IV administration Biliary excretion Vinblastine Nausea and vomiting, alopecia, bone marrow depression Vincristine Structurally similar and mechanistically identical to vinblastine Less toxic to bone marrow, no nausea and vomiting Use limited to short duration due to peripheral neuropathy |
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Paclitaxel (Taxol), Docetaxel (Taxotere)
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Class - Plant Alkaloids (Taxanes)
Affects microtubules, but by stabilization Blocks progress through mitosis Intravenous (in Cremophor) Promising results in many solid tumors Acute hypersensitivity, nausea Delayed bone marrow suppression, some neuropathy |
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Etoposide (VP-16)
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Class - Plant Alkaloids (Podophyllotoxins)
Topoisomerase II inhibitor, double strand breaks, DNA degradation Arrests cells in S-G2 stage Oral and Intravenous Nausea and vomiting, alopecia, bone marrow suppression |
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Irinotecan
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Class - Camptothecins
Pro-drug; converted to active SN-38 by esterase SN-38 inhibits Topoisomerase I SN-38 also responsible for adverse effects Acute adverse effects are nausea, vomiting, diarrhea Delayed effects are bone marrow suppression, nausea, dose-limiting diarrhea Glucuronidation by UGT1A1 inactivates SN-38 |
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Doxorubicin, Daunorubicin
(Idarubicin, Epirubicin) |
Class - Anti-tumor antibiotics (Anthracyclines)
Intercalate into DNA Block Topoisomerase II, inhibit DNA and RNA synthesis, cause strand breaks Generate free radicals Intravenous, metabolized in liver Bone marrow suppression, gastrointestinal distress, severe alopecia Signature adverse effect is Cardiotoxicity Function of cumulative dose May be exacerbated by radiation, other drugs Arrhythmias, cardiomyopathy, CHF Free radical mechanism Minimize by administering Dexrazoxane |
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Bleomycin
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Class - Anti-tumor antibiotics
Mixture of glycopeptides Binds DNA, generates radicals Causes strand breaks Active in G2 (CCS) Hypersensitivity, cutaneous reactions Pulmonary toxicity, fibrosis |
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Hydrocortisone, Prednisone
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Class - Hormone and Hormone Modulators (Adrenocorticosteroids)
Suppress proliferation of immune cells (leukocytes, lymphocytes) Administered orally Used in therapy for leukemias, lymphomas Delayed adverse effects include fluid retention, immunosuppression, diabetes |
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Anastrazole, Letrozole
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Class - Hormone and Hormone Modulators (Aromatase Inhibitors)
Blocks conversion of androgens to estrogens Specific for estrogen production Anastrazole, Letrozole Azole, similar to anti-fungal drugs Treatment for ER+ primary and metastatic breast cancer Adverse Effects of Aromatase Inhibitors Acute– Mild nausea, headache Delayed– Fatigue, hot flushes |
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Tamoxifen
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Class - Hormone and Hormone Modulators [Selective Estrogen Receptor Antagonists (SERMs)]
Competing ligands for ER More effective in post-menopausal women Tamoxifen ER antagonist in breast ER agonist in endometrium Chemopreventive use against breast cancer Treatment for ER+ primary and metastatic breast cancer Administered orally, Activation by CYP2D6 may be key Adverse effects include nausea, hot flushes, vaginal bleeding |
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Flutamide
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Class - Hormone and Hormone Modulators (Androgen Receptor Antagonists)
Non-steroidal ligands for AR Diminish androgen effects Flutamide Oral administration Used with radiation for prostate cancer Adverse effects mild, include nausea, hot flushes, transient hepatic effects |
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Interferon-α
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Class - Biologicals
Polypeptide cytokine (~19.5 KD) produced by white blood cells Parenteral administration Alters gene expression, antiviral and immunomodulatory Used against hematologic malignancies, metastatic melanoma, renal cell carcinoma Causes fever and chills, can cause anorexia, weakness |
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Trastuzumab (Herceptin)
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Class - Biologicals
Monoclonal antibody against HER2neu/ErbB-2 oncogene product (Epidermal growth factor receptor) Receptor is amplified in ~25% of breast cancers, poor prognosis Intravenous administration Infusion reactions, hypersensitivity, cardiomyopathy Effective against HER2neu+ primary and metastatic breast tumors when pharmaocokinetics allow |
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STI-571 (Imatinib, Gleevec)
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Class - Signal Transduction Inhibitors
Inhibits Bcr-Abl and other tyr kinases Blocks growth factor signaling in chronic myelogenous leukemia (CML) Also blocks kit kinase in gastrointestinal stromal tumors (GIST) Myelosuppressive Edema and fluid retention, hepatotoxicity |
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Gefitinib (Iressa, ZD183)
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Class - Signal Transduction Inhibitors
Inhibits EGF-R tyrosine kinase Orally administered For non-small cell lung cancer May cause fever, dyspnea |
