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62 Cards in this Set
- Front
- Back
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What is the mechanism of methotrexate (MTX)?
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S-phase specific: folic acid analog that inhibits dihydrofolate reductase, decreasing dTMP and therefore DNA and protein synthesis
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What is the clinical use of methotrexate?
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Leukemias, lymphomas, choriocarcinoma, sarcoma, abortion, ectopic pregancy, rheumatoid arthritis, psoriasis
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What is the toxicity of methotrexate?
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Myelosuppression, macrovesicular fatty change in liver, mucositis
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How do you reverse the myelosuppression that can occur with methotrexate?
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Leucovorin
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What is the mechanism of 5-fluorouracil (5-FU)?
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S-phase specific: pyrimidine analog bioactivated to 5F-dUMP --> covalently complexes folic acid --> inhibits thymidylate synthase --> decreases dTMP and therefore DNA and protein synthesis
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What is the clinical use of 5-fluorouracil?
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Colon cancer and other solid tumors, basal cell carcinomas (topical); works synergistically with MTX
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What is the toxicity of 5-fluorouracil?
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Myelosuppression, photosensitivity
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How can you somewhat reverse the toxicity of 5-fluorouracil?
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Thymidine
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What is the mechanism of 6-mercaptopurine (6-MP)?
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Blocks de novo purine synthesis, activated by hypoxanthine-guanin phosphoribosyltransferase
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What is the clinical use of 6-mercaptopurine?
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Leukemias, lymphomas (not CLL or Hodkin's)
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What is the toxicity of 6-mercaptopurine?
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Bone marrow, GI, liver; toxicity increases with allopurinol because metabolized by xanthine oxidase
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What is the mechanism of cyclophosphamide and ifosfamide?
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Alkylating agents: covalently x-link DNA at guanine N-7; needs to be bioactivated by liver
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What is the clinical use of cyclophosphamide and ifosfamide?
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Non-Hodgkin's lymphoma, breast and ovarian carcinomas, immunosuppresants
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What is the toxicity of cyclophosphamide or ifosfamide?
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Myelosuppression, hemorrhagic cystitis
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How to you prevent hemorrhagic cystitis from the use of cyclophosphamide or ifosfamide?
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Mensa
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What are carmustine, lomustine, semustine, and streptozocin?
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Nitrosoureas
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What is the mechanism of nitrosoureas?
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Alkylate DNA; require bioactivation
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What is the clinical use of nitrosoureas?
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Brain tumors (including glioblastoma multiforme); can cross blood brain barrier
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What is the toxicity of nitrosoureas?
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Dizziness and ataxia from CNS toxicity
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What is the mechanism of cisplastin and carboplatin?
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Similar to alkylating agents
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What is the clinical use of cisplastin and carboplatin?
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Testicular, bladder, ovary and lung carcinomas
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What is the toxicity of cisplastin and carboplatin?
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Nephrotoxicity and acoustic nerve damage
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What is the mechanism of busulfan?
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Alkylates DNA
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What is the clinical use of busulfan?
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CML
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What is the toxicity of busulfan?
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Pulmonary fibrosis, hyperpigmentation
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What is the mechanism of doxorubicin (adriamycin) and daunorubicin?
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Generates free radicals and noncovalently intercalate in DNA --> creating breaks in DNA strand to decrease replication
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What is the clinical use of doxorubicin (adriamycin) and daunorubicin?
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Part of the ABVD combination regimen for Hodgkin's and for myelomas, sarcomas, and solid tumors (breast, ovary, lung)
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What is the toxicity of doxorubicin (adriamycin) and daunorubicin?
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Cardiotoxicity, myelosuppression and marked alopecia, toxic extravasation
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What is ABVD and what is it used for?
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Adriamycin (doxorubicin), Bleomycin, Viznblastine, Dacarbazine; Hodgkin's lymphoma
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What is the mechanism of dactinomycin (actinomycin D)
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Intercalates DNA
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What is the clinical use dactinomycin (actinomycin D)?
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Wilm's tumor, Ewing's sarvcoma, rhabdomyosarcoma
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What is the toxicity of dactinomycin (actinomycin D)?
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Myelosuppression
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What is the mechanism of bleomycin?
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Induces formation of free radicals, which causes breaks in DNA strands
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What is the clinical use of bleomycin?
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Testicular cancer, lymphomas (part of ABVD for Hodgkin's)
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What is the toxicity of bleomycin?
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Pulmonary fibrosis, skin changes, but minimal myelosuppression
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What is the mechanism of hydroxyurea?
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Inhibits ribonucleotide reductase --> deccreases DNA synthesis; S-phase specific
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What is the clinical use of hydroxyurea?
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Melanoma, CML, sickle cell disease
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What is the toxicity of hydroxyurea?
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Bone marrow suppression, GI upset
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What is the mechanism of etoposide (VP-16)?
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G2-phase-specific agent that inhibits topoisomerase II and increases DNA degradation
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What is the clinical use of etoposide (VP-16)?
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Small cell carcinoma of the lung and prostate, testicular carcinoma
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What is the toxicity of etoposide (VP-16)?
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Myelosuppression, GI irritation, alopecia
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What is the mechanism of prednisone?
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May trigger apoptosis, may work on nondividng cells
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What is the clinical use of prednisone?
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CLL, Hodgkin's lymphomas (part of MOPP regimen), immunosuppresion
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What is the toxicity of prednisone?
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Cushing-like syndromes, immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis
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What is the mechanism of tamoxifen and raloxifene?
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Acts as estrogen-receptor antagonists in breast and agonists in bone
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What is the clinical use of tamoxifen and raloxifene?
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Breast cancer, osteoporosis prevention
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What is the toxicity of tamoxifen?
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Increase risk of endometrial carcinoma via partial agonists effect; hot flashes
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Why doesn't raloxifine increase the risk of endometrial carcinoma?
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It is an endometrial antagonist
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What is the mechanism of trastuzumab (herceptin)?
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Monoclonal antibody against HER-2 (erb-B2) --> helps kill breast cancer cells that overexpress HER-2
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What is the clinical use of trastuzumab (herceptin)?
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Metastatic breast cancer
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What is the toxicity of trastuzumab (herceptin)?
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Cardiotoxicity
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What is the mechanism of imatinib (gleevec)?
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Philadelphia chromosome bcr-acl tyrosine kinase inhibitor
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What is the clinical use of imatinib (gleevec)?
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CML, GI stromal tumors
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What is the toxicity of imatinib (gleevec)?
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Fluid retention
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What is the mechanism of vincristine, vinblastine?
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M-phase-specific alkaloids that bind to tubulin and block polymerization of microtubules --> mitotic spindle cannot form
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What is the clinical use of vincristine, vinblastine?
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Part of the MOPP regimen for lymphoma, Wilm's tumor, choriocarcinoma
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What is the toxicity of vincristine?
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Neurotoxicity (areflexia, peripheral neuritis), paralytic ileus
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What is the toxicity of vinnlastine?
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Bone marrow suppression
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What is the mechanism of paclitaxel, other taxols?
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M-phase specific agents that bind to tubulin and hyperstabilize polymerized microtubules so that mitotic spindle cannot break down and anaphase cannot occur
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What is the clinical use of paclitaxel, other taxols?
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Ovarian and breast carcinomas
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What is the toxicity of paclitaxel, other taxols?
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Myelosuppression and hypersensitivity
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What is MOPP and what is it used for?
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Mustaren, Oncovin (Vincristine), Procarbazine, Prednisone; Hodgkin's disease
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