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56 Cards in this Set
- Front
- Back
S-phase-specific antimetabolite. Folic acid analog that inhibits dihydrofolate
reductase, resulting in ↓ dTMP and therefore ↓ DNA and protein synthesis. |
Methotrexate (MTX)
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Leukemias, lymphomas, choriocarcinoma, sarcomas. Abortion, ectopic pregnancy,
rheumatoid arthritis, psoriasis. |
Methotrexate (MTX)
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Myelosuppression, which is reversible with leucovorin (folinic acid) “rescue.”
Macrovesicular fatty change in liver. |
Methotrexate (MTX)
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S-phase-specific antimetabolite. Pyrimidine analog bioactivated to 5F-dUMP, which
covalently complexes folic acid. This complex inhibits thymidylate synthase, resulting in ↓ dTMP |
5-fluorouracil (5-FU)
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Colon cancer and other solid tumors, basal cell carcinoma (topical). Synergy with
MTX. |
5-fluorouracil (5-FU)
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Myelosuppression, which is NOT reversible with leucovorin; photosensitivity.
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5-fluorouracil (5-FU)
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Blocks de novo purine synthesis. Activated by HGPRTase.
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6-mercaptopurine (6-MP)
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Leukemias, lymphomas (not CLL or Hodgkin’s).
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6-mercaptopurine (6-MP)
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Bone marrow, GI, liver. Metabolized by xanthine oxidase; thus ↑ toxicity with allopurinol.
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6-mercaptopurine (6-MP)
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Inhibits DNA polymerase.
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Cytarabine (ara-C)
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AML.
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Cytarabine (ara-C)
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Leukopenia, thrombocytopenia, megaloblastic anemia.
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Cytarabine (ara-C)
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Alkylating agents; covalently x-link (interstrand) DNA at guanine N-7. Require
bioactivation by liver. |
Cyclophosphamide, ifosfamide
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Non-Hodgkin’s lymphoma, breast and ovarian carcinomas. Also immunosuppressants.
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Cyclophosphamide, ifosfamide
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Myelosuppression; hemorrhagic cystitis, which can be partially prevented with mesna.
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Cyclophosphamide, ifosfamide
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Names of Nitrosoureas
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Carmustine, lomustine, semustine, streptozocin.
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Alkylate DNA. Require bioactivation. Cross blood-brain barrier → CNS.
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Nitrosoureas
Carmustine, lomustine, semustine, streptozocin. |
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Brain tumors (including glioblastoma multiforme).
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Nitrosoureas
Carmustine, lomustine, semustine, streptozocin. |
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CNS toxicity (dizziness, ataxia).
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Nitrosoureas
Carmustine, lomustine, semustine, streptozocin. |
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Act like alkylating agents.
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Cisplatin, carboplatin
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Testicular, bladder, ovary, and lung carcinomas.
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Cisplatin, carboplatin
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Nephrotoxicity and acoustic nerve damage.
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Cisplatin, carboplatin
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Alkylates DNA.
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Busulfan
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CML.
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Busulfan
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Pulmonary fibrosis, hyperpigmentation.
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Busulfan
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Generate free radicals and noncovalently intercalate in DNA (creating breaks in DNA
strand to ↓ replication). |
Doxorubicin (Adriamycin), daunorubicin
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Part of the ABVD combination regimen for Hodgkin’s and for myelomas, sarcomas, and
solid tumors (breast, ovary, lung). |
Doxorubicin (Adriamycin), daunorubicin
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Cardiotoxicity; also myelosuppression and marked alopecia. Toxic extravasation.
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Doxorubicin (Adriamycin), daunorubicin
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Intercalates in DNA.
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Dactinomycin (actinomycin D)
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Wilms’ tumor, Ewing’s sarcoma, rhabdomyosarcoma.
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Dactinomycin (actinomycin D)
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Myelosuppression.
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Dactinomycin (actinomycin D)
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Induces formation of free radicals, which cause breaks in DNA strands.
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Bleomycin
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Testicular cancer, lymphomas (part of the ABVD regimen for Hodgkin’s).
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Bleomycin
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Pulmonary fibrosis, skin changes, but minimal myelosuppression.
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Bleomycin
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G2-phase-specific agent that inhibits topoisomerase II and ↑ DNA degradation.
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Etoposide (VP-16)
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Small cell carcinoma of the lung and prostate, testicular carcinoma.
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Etoposide (VP-16)
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Myelosuppression, GI irritation, alopecia.
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Etoposide (VP-16)
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May trigger apoptosis. May even work on nondividing cells.
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Prednisone
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Most commonly used glucocorticoid in cancer chemotherapy. Used in CLL, Hodgkin’s lymphomas (part of the MOPP regimen). Also an immunosuppressant used in autoimmune diseases.
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Prednisone
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Cushing-like symptoms; immunosuppression, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis.
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Prednisone
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Estrogen receptor mixed agonist/antagonists (“SERMs”) that block the binding of estrogen to estrogen receptor–positive cells.
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Tamoxifen, raloxifene
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Breast cancer. Also useful to prevent osteoporosis.
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Tamoxifen, raloxifene
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_______ may ↑ the risk of endometrial carcinoma via partial agonist effects; “hot flashes.”
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Tamoxifen, raloxifene
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Monoclonal antibody against HER-2 (erb-B2). Helps kill breast cancer cells that overexpress HER-2, possibly through antibody-dependent cytotoxicity.
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Trastuzumab (Herceptin)
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Metastatic breast cancer.
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Trastuzumab (Herceptin)
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Cardiotoxicity.
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Trastuzumab (Herceptin)
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Myoclonal antibody against the Philadelphia chromosome brc-abl tyrosine kinase.
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Imatinib (Gleevec)
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CML, GI stromal tumors.
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Imatinib (Gleevec)
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Fluid retention.
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Imatinib (Gleevec)
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M-phase-specific alkaloids that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form.
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Vincristine, vinblastine
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Part of the MOPP regimen for lymphoma, Wilms’ tumor,
choriocarcinoma. |
(Oncovin [vincristine] is part of MOPP), vinblastine
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neurotoxicity (areflexia, peripheral neuritis), paralytic ileus.
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Vincristine
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Bone marrow suppression
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VinBLASTine BLASTs Bone marrow (suppression).
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M-phase-specific agents that bind to tubulin and hyperstabilize polymerized microtubules so that mitotic spindle cannot break down (anaphase cannot occur).
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Paclitaxel, other taxols
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Ovarian and breast carcinomas.
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Paclitaxel, other taxols
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Myelosuppression and hypersensitivity.
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Paclitaxel, other taxols
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