Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2018 Publisher: Hospira UK Limited, Horizon, Honey Lane, Hurley, Maidenhead, SL6 6RJ, UK
Pharmacotherapeutic group: Antineoplastic agent – vinca alkaloid
ATC Code: L01 A02
Vincristine is an antineoplastic drug with broad-spectrum anti-tumor activity in man. The drug may act by mitotic inhibition, causing an arrest of cell division in metaphase. The drug is relatively marrow-sparing and is thus suitable for use in combination with other cancer chemotherapeutic agents.
Vincristine is poorly absorbed orally. The clearance of the drug after rapid intravenous injection follows a triphasic decay pattern: a very rapid steep descent (alpha phase); a narrow-middle region (beta-phase) and a much longer terminal region (gamma phase). The terminal phase half-life of the drug varies from 15-155 hours.
Dosing with the drug more frequently than once weekly is therefore probably unnecessary.
Vincristine is primarily excreted by the biliary route.
Patients with impaired hepatic or biliary function, as evidenced by a raised serum alkaline phosphatase, have been shown to have a significantly prolonged vincristine elimination half-life.
Both in vivo and in vitro laboratory tests have failed to demonstrate conclusively that this product is mutagenic. No evidence of carcinogenicity was found following intraperitoneal administration in rats and mice, although this study was limited.
In several animal species, vincristine can include teratogenic effects, as well as embryo lethality, with doses that are non-toxic to the pregnant animal.
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