Brands, Medical Use, Clinical Data
Brands / Synonyms
22-Oxovincaleukoblastine; Indole alkaloid; LCR; Leurocristine; Marqibo; Onco TCS; Oncovin; Oncovin (1:1 sulfate salt); VCR; VIN; Vincaleukoblastine, 22-oxo-; Vincasar (1:1 sulfate salt); Vincasar PFS; Vincrex; Vincrex (1:1 sulfate salt); Vincristina [DCIT]; Vincristine; Vincristine Sulfate; Vincristine Sulfate PFS; Vincristinum [INN-Latin]; Vincrstine; Vincrystine; Vinkristin; Z-D-Val-Lys(Z)-OH
For treatment of acute leukaemia, malignant lymphoma, Hodgkin's disease, acute erythraemia, acute panmyelosis
Vincristine is a vinca alkaloid antineoplastic agent used as a treatment for various cancers including breast cancer, Hodgkin's disease, Kaposi's sarcoma, and testicular cancer. 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. Vincristine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death. Vincristine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.
Mechanism of Action
The antitumor activity of Vincristine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Like other vinca alkaloids, Vincristine may also interfere with: 1) amino acid, cyclic AMP, and glutathione metabolism, 2) calmodulin-dependent Ca2+-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis.
IVN-RAT LD50 1300 mg/kg; IPR-MUS LD50 5.2 mg/kg
Biotrnasformation / Drug Metabolism
Patients with the demyelinating form of Charcot-Marie-Tooth syndrome would not be given vincristine sulfate injection.
The simultaneous oral or intravenous administration of phenytoin and antineoplastic chemotherapy combinations that included vincristine sulfate has been reported to reduce blood levels of the anticonvulsant and to increase seizure activity. Dosage adjustment should be based on serial blood level monitoring. The contribution of vincristine sulfate to this interaction is not certain. The interaction may result from reduced absorption of phenytoin and an increase in the rate of its metabolism and elimination.