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Handbook of clinical drug data - part 3

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Dược động học. Thuốc được nhanh chóng và hấp thu tốt sau khi uống, hệ thần kinh trung ương cấp được bằng những người trong huyết thanh sau khi 0,5-1,5 giờ. Procarbazine là 70% thu hồi trong nước tiểu, chủ yếu như là một chất chuyển hóa axit, với | Aklylating Agents 219 Adult Dosage. PO 50-200 mg m2 day for 10-25 days repeated in 3-4 weeks. Calculate the dosage based on IBW and reduce dosage for a BUN 40 mg dL Crs 2 mg dL or serum bilirubin 3 mg dL. Dosage Forms. Cap 50 mg. Pharmacokinetics. The drug is rapidly and well absorbed after oral administration CNS levels are equal to those in serum after 0.5-1.5 hr. Procarbazine is 70 recovered in the urine primarily as an acid metabolite with 5 excreted unchanged. Adverse Reactions. Frequent CNS side effects include dizziness headache ataxia nightmares depression and hallucinations in up to 30 of patients . Paresthesias also can occur occasionally. Mild to moderate nausea and vomiting occur in 60-90 of patients but tolerance usually develops rapidly. Dose- and duration-dependent sterility mutagenicity and teratogenicity are reported. The drug predisposes patients to secondary acute nonlymphocytic leukemias. The dose-limiting toxicity is myelosuppression with a pancytopenic nadir at 2-3 weeks. Occasional side effects include a flu-like syndrome allergic pneumonitis and rash. Procarbazine is contraindicated in patients with severe hypersensitivity to the drug or pre-existing bone marrow aplasia. Periodic evaluations of neurologic status and monthly CBCs may be useful. Drug Interactions. Avoid concurrent use with MAO inhibitors alcohol heterocyclic antidepressants sympathomimetics or tyramine-containing foods. Microsomal enzyme-inducing drugs might augment procarbazine cytotoxicity. Procarbazine potentiates barbiturates narcotics and other hepatically metabolized drugs. STREPTOZOCIN Zanosar Pharmacology. Streptozocin is a glucose-containing nitrosourea. it has some selective cytotoxic activity in insulinomas and malignant carcinoid and is active to a lesser extent in other adenocarcinomas of the Gi tract. The drug inhibits DNA synthesis via inhibition of pyrimidine biosynthesis and blockade of key enzymatic reactions in gluconeogenesis pathways. it is cell-cycle .