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22 Cards in this Set
- Front
- Back
methotrexate
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inhibits formation of thymine. folate analog that inhibits dihydrofolate reductase. S-phase specific antimetabolite.
toxicity: myelosuppression (reversible with leucovorin a.k.a. folinic acid), macrovesicular fatty change in liver |
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5-fluoruracil (5-FU)
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inhibits formation of thymine. pyrimidine analog bioactivated to 5F-dUMP which covalently complexes folic acid (CH2-THF). complex inhibits thymidilate synthase.
toxicity: myelosuppression (NOT reversible by leucovorin), photosensitivity. can rescue with thymidine |
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6-mercaptopurine (6-MP)
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blocks de novo purine synthesis. activated by HGPRTase.
Toxicity: BM toxicity, GI tox, liver tox. toxicity enhanced by allopurinol since both are metabolized by xanthine oxidase |
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cytarabine (ara-C)
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inhibits DNA polymerase.
toxicity: leukopenia, thrombocytopenia, megaloblastic anemia |
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cyclophosphamide
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alkylating agent. covalently x-link DNA strands at guanine N-7. bioactivated in liver
toxicity: myelosuppression, hemorrhagic cystitis (prevented partially by mesna which binds toxic metabolites through its sulfhydryl groups) |
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carmustine
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nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS. CNS toxicity (dizziness, ataxia)
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lomustine
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nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS. CNS toxicity (dizziness, ataxia)
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semustine
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nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS
toxicity: CNS (dizziness, ataxia) |
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streptozocin
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nitrosoureas. alkylate DNA. require bioactivation. cross BBB -> CNS. CNS toxicity (dizziness, ataxia)
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cisplatin, carabplatin
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alkylating agent.
toxicity: nephrotoxicity and acoustic nerve damage. |
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busulfan
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alkylating agent
toxicity: pulmonary fibrosis, hyperpigmentation |
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doxorubicin
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make free radicals and noncovalently intercalate in DNA. make breaks in strand to decrease replication.
toxicity: cardiotoxicity (dialated cardiomyopathy), myelosuppression, marked alopecia |
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dactinomycin
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intercalates in DNA inhibiting txn. myelosuppression
toxicity: myelosuppression |
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bleomycin
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induces free radicals which cause breaks in DNA strands.
toxicity: pulmonary fibrosis, skin changes, NOT much myelosuppression |
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hydroxyurea
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inhibits ribonucleotide reductase -> decreased DNA synthesis (s-phase specific)
bone marrow suppression, GI upset |
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etoposide (VP-16)
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inhibits topoisomerase II increasing DNA degredation
toxicity: myelosuppression, GI irritation, alopecia |
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prednisone
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may trigger apoptosis. even on nondividing cells
toxicity: cushings, hyperglycemia, immunosuppression, cataracts, acne, osteoporosis, peptic ulcers, hyperglycemia, psychosis |
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tamoxifen, raloxifene
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receptor antagonists in breast, agonists in bone. block binding of estrogen to estrogen receptor-positive cells
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trastuzumab
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monoclonal Ab against HER2. Kills breast cancer cells that over express HER 2 through ADCC
toxicity: cardiotoxicity |
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imantinib
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(gleevec). Abl tyrosine kinase inhibitor. inhibits Bcr-Abl tyrosine kinase in CML
Toxicity: fluid retention |
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vincristine, vinblastin
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alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form
toxicity: vincristine = neurotoxicity, paralytic ileus vinblastin = bone marrow suppression |
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paclitaxel
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bind tubulin and hyperstabilize polymerized microtubules so that mitotic spindle cannot break down (no anaphase)
toxicity: myelosuppression and hypersensitivity |