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57 Cards in this Set
- Front
- Back
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Methotrexate Mechanism
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Mechanism: S-phase specific antimetabolites. Folic acid analog that inhibits dihydrofolate reductase resulting in decreased dTMP and decreased DNA synthesis
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Methotrexate Uses
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Leukemias
Lymphomas Choriocarcinoma Sarcomas Abortion Ectopic Pregnancy RA Psoriasis |
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Methotrexate Toxicity
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Myelosupression
Macrovesicular fatty change in the liver Mucositis "Rescue with leucorvin" |
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5 Fluorouracil Mechanism
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S phase specific antimetabolite. Pyrimidine analog which forms 5F-dUMP which covalently complexes folic acid inhibiting thymidylate synthase.
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5-Fluorouracil Uses
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Colon Cancer and other solid tumors, topical use for basal cell carcinoma
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5-Florouracil Toxicity
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Myelosupression- which is not reversible with leucovorin
Photosensitivity Can "rescue" with thymidine |
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6 Mercaptopurine Mechanism
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Blocks de novo purine synthesis. Activated by HGPRTase
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6 Mercaptopurine Uses
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Leukemias, Lymphomas (not CLL or Hodgkins)
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6 Mercaptopurine Toxicity
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Bone Marrow
Liver GI Metabolized by xanthine oxidase, thus increased toxicity with allopurinol |
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Cytarabine Mechanism
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Inhibits DNA Polymerase
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Clinical Use of Cystarbine
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AML
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Cystarabine Toxicity
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Megaloblastic anemia
Leukopenia RThrombocytopenia |
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Cyclophosphamide/ ifosfamide
Mechanism |
Alkylating agent- covalently links DNA at guanine N7. Drug requires bioactivation by the liver
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Cyclophosphamide Clinical use
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Non Hodgkin Lymphoma, Breast and ovarian carcinoma
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Cyclophosphamide Toxicity
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Myelosuppression
Hemorrhagic cystitisCan partial be prevented with mensa |
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Nitrosoureas (Carmustine, lomustine, semustine, streptozocin) Mechanism
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Alkylate DNACan Cross BBB
Requires bioactivation |
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Nitrosoureases Uses
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Brain Tumors
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Nitrosoureas
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CNS toxicity (dizziness, ataxia)
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Cisplatin, Carboplatin Mechanism
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Act like alkylating Agents
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Cisplatin, Carboplatin Clinical Use
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Testicular, Bladder, Ovary and lung carcinoma
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Cisplatin, Carboplatin Toxicity
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Nephrotoxicity and acustic nerve damage
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Busulfan Mechanism
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Alkylates DNA
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Busulfan Use
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CML
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Busulfan Toxicity
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Pulmonary fibrosis, hyperpigmentation
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Doxorubicin, Daunorubicin Mechanism
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Generates free radicles and non covalently intercalates DNA
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Doxorubicin Uses
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Hodgkin's and for myelomsa, sarcomas and solid tumors
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Doxorubicin Toxicity
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Cardiotoxicity
Myelosupression |
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Dactinomycin (Actinomycin D) Mechanism
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Intercalates DNA
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Dactinomycin Uses
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Child tumors:
Wilm's tumor Ewing's sarcoma Rhabdomyosarcoma |
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Dactinomycin Toxicity
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Myelosupression
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Bleomycin Mechanism
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Induces formation of free radicles
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Bleomycin Uses
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Testicular cancer, lymphomas, Hodgkins
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Bleomycin Toxicity
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Pulmonary fibrosis
Skin changes minimal myelosupression |
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Hydroxyurea Mechanism
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Inhibits Ribonucleotide
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Hydroxyurea USes
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Melanoma
CML Sickle Cell |
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Hydroxyurea Toxicity
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Bone marrow supression
Upset GI |
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Etoposide Mechanism
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G2 Specific agent that inhibits topoisomerase II and increases DNA degradation
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Etoposide Uses
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Small cell carcinoma of the lung
Prostate Testicular carcinoma |
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Etoposide Toxicity
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Myelosupression
Gi irritation Alopecia |
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Prenisone Mechanism
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May trigger apoptosis
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Prednisone Uses
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CLL
Hodgkin's lmphomas Autoimmune diseases |
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Prednisone Toxicity
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Cushing like symptoms
Immunosupression Cataracts Acne Osteoporosis HTN peptic ulcers hyperglycemia psycosis |
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Tamoxifen, Raloxifen Mechanism
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Receptor antagonists in breast, agoinists in the bone- blocks the binding of estrogen to estrogen recptor- positive cells
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Tamoxifen, Raloxifen Uses
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Breast Cancer- also useful in preventing osteoporosis
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Tamoxifen, Raloxifen Toxicity
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Increased risk of endometrial carcinoma only with tamxifen
Hot flashes |
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Trastuzumab (herceptin) Mechanism
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Monoclonal antibody against the HER-2
Antibody dependent cytotoxicity |
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Trastuzumab Uses
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Metastatic breast cancer
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Trastuzumab Toxicity
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Cardiotxicity
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Imatinib (Gleevec) Mechanism
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Thyrosin kinase inhibitor for philadelphia chromosome- bcr-abl
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Imatinib Use
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CML
GI Stromal Tumors |
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Imatinib Toxicity
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Fluid retention
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Vincristine/ Vinblastine Mechanism
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M-Phase specicfic alkaloids that bind to tubulin and block the olymerization of microtubeules.
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Vincristine/ Vinblastine Uses
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Lymphoma
Wilm's tumor Choriocarcinoma |
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Vincrisitine/ Vinblastine Toxicity
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Vincristine- neurotoxicity, paralytic ileus
|Vinblastine- bone marrow supression |
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Paclitaxel and other taxols mechanism
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M phase specific agent that binds to tubulin and hyper stabilizes polymerized microtubutles so that mitotic spindle cannot break
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Paclitaxel and other taxol uses
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Ovarian and breast carcinomas
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Paclitaxel and other taxols toxicity
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Myelosupression and hypersensitivity
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