Brands, Medical Use, Clinical Data
Drug Category
- Antineoplastic Agents, Phytogenic
Dosage Forms
- Liquid
- Powder for solution
- Solution
Brands / Synonyms
Indole Alkaloid; Nincaluicolflastine; Rozevin; Velban; Velbe; Vinblastin; Vinblastina [Dcit]; Vinblastine; Vinblastine Sulfate; Vinblastinum [Inn-Latin]; Vincaleucoblastin; Vincaleucoblastine; Vincaleukoblastine; Vincoblastine
Indications
For treatment of breast cancer, testicular cancer, lymphomas, neuroblastoma, Hodgkin's and non-Hodgkin's lymphomas, mycosis fungoides, histiocytosis, and Kaposi's sarcoma.
Pharmacology
Vinblastine is a vinca alkaloid antineoplastic agent. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units: vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vinblastine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.
Mechanism of Action
The antitumor activity of vinblastine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Vinblastine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.
Absorption
Not Available
Toxicity
Oral, mouse: LD50 = 423 mg/kg; Oral, rat: LD50 = 305 mg/kg.
Biotrnasformation / Drug Metabolism
Hepatic. Metabolism of vinblastine has been shown to be mediated by hepatic cytochrome P450 3A isoenzymes.
Contraindications
Vinblastine sulfate is contraindicated in patients who have significant granulocytopenia unless this is a result of the disease being treated. It should not be used in the presence of bacterial infection. Such infections must be brought under control prior to the initiation of therapy with vinblastine sulfate.
Drug Interactions
Vinblastine sulfate should not be diluted with solvents that raise or lower the pH of the resulting solution from
between 3.5 and 5. Solutions should be made with normal saline (with or without preservative) and should not be
combined in the same container with any other chemical. Unused portions of the remaining solutions that do not
contain preservatives should be discarded immediately.
The simultaneous oral or intravenous administration of phenytoin and antineoplastic chemotherapy combinations that
included vinblastine sulfate has been reported to have reduced blood levels of the anticonvulsant and to have
increased seizure activity. Dosage adjustment should be based on serial blood level monitoring. The contribution of
vinblastine sulfate to this interaction is not certain. The interaction may result from either reduced absorption of
phenytoin or an increase in the rate of its metabolism and elimination.
Caution should be exercised in patients concurrently taking drugs known to inhibit drug metabolism by hepatic
cytochrome P450 isoenzymes in the CYP 3A subfamily, or in patients with hepatic dysfunction. Concurrent
administration of vinblastine sulfate with an inhibitor of this metabolic pathway (such as erythromycin, doxorubicin,
or etoposide) may cause an earlier onset and/or an increased severity of side effects.
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