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Antineoplastic Agents ANTIBETABOLITES Drug Methotrexate (MTX)

Mechanism Folic acid analog that inhibits dihydrofolate reductase to decrease dTMP and decrease DNA and Protein synthesis

Clinical Use Leukemia, lymphoma, choriocarcinoma

Toxicity
l. Myelosuppression, which is reversible with leucovorin (folinic acid) "rescue." 2. Macrovesicular fatty change in liver. 3. Mucositis. 4. Teratogenic. l. Myelosuppression, which is not reversible with leucovorin. Overdose: "rescue" with thymidine. 2. Photosensitivity Bone marrow, GI, liver. Metabolized by xanthine oxidase; thus I toxicity with allopurinol. Bone marrow depression, liver. Can be given with allopurinol. Leukopenia, thrombocytopenia, megaloblastic anemia.

5-fluorouracil (5-FU)

Pyrimidine analog bioactivated to 5FdUMP, which covalently complexes folic acid.

Colon cancer and other solid tumors, basal cell carcinoma, synery with MTX

6-mercaptopurine (6-MP)

Purine analog to decrease purine synthesis

Leukemias, lymphomas (not CLL or Hodgkins)

6-thioguanine (6-TG)

Same as 6-MP

Acute Lymphoid leukemia

Cytarabine (ara-C)

Pyrimidine antagonist to decrease DNA polymerase

AML, ALL, high grade non hodgkins lymphoma

ANTIBIOTICS Drug Dactinomycin (Actinomycin D) Doxorubicin (Adriamycin); daunorubicin Bleomycin Etoposide (VP-16); teniposide

Mechanism Intercalates in DNA Generate free radicals. Noncvalently intercalate in DNA to breaks in DNA to decrease replication Induces free radical formation, which causes breaks in DNA strands Inhibits topoisomerase II increase DNA degradation

Clinical Use Wilms tumor, Ewings sarcoma, rhabdomyosarcoma Hodgkins lymphomas; also for myelomas, sarcomas, and solid tumors Testicular cancer, Hodgins lymphoma Small cell carcinoma of the lung and prostate, testicular carcinoma

Toxicity
Myelosuppression. Cardiotoxicity, myelosuppression, and alopecia. Toxic to tissues with extravasation. Pulmonary fibrosis, skin changes. Minimal myelosuppression. Myelosuppression, Gl irritation, alopecia.

ALKYLATING AGENTS Drug Cyclophosphamide; ifosfamide

Mechanism Covalently X link DNA at guanine N-7. Require bioactivation by liver

Clinical Use Non hodgkins lymphoma, breast and ovarian carcinomas. Also immunosuppressant

Toxicity
Myelosuppression; hemorrhagic cystitis, partially prevented with mesna (thiol group of mesna binds toxic metabolite). CNS toxicity (dizziness, ataxia). Pulmonary fibrosis, hyperpigmentation.

Nitrosureas (carmustine, lomustine, semustine, streptozocin) Busulfan

Require bioactivation. Cross blood brain barrier to CNS Alkylates DNA

Brain tumors (including glioblastoma multiforme) CML. Also used to ablate patients bone marrow before bone marrow transplantation

MICROTUBULE INHIBITORS Drug Vincristine; vinblastine

Mechanism Alkaloids that bind to tubulin in Mphase and block polymerization of microtubules so that mitotic spindle cannot form. Microtubules are the vines of your cells. Hyperstabilize polymerized microtubules in M-phase so that mitotic spindle cannot break down. It is Taxing to stay polymerized.

Clinical Use Hodgkins lymphoma, Wilms tumor choriocarcinoma

Toxicity Vincristine- neurotoxicity (areflexia, peripheral block polymerization choriocarcinoma. neuritis), paralytic ileus. VinBLASTine BLASTs Bone marrow Myelosuppression and hypersensitivity.

Paclitaxel

Ovarian and breast carcinomas

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