- Usage: Clinical, Hospital
- Dose: 50mg/5ml
- Molecular weight: 1079.12
- Concentration: 30-40 mu M
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Vinorelbine Tartrate Injection is for intravenous administration. Each vial contains vinorelbine tartrate equivalent to 10 mg (1-mL vial) or 50 mg (5-mL vial) vinorelbine in Water for Injection, USP. No preservatives or other additives are present. The aqueous solution is sterile and nonpyrogenic. Vinorelbine tartrate is a semi-synthetic vinca alkaloid with antitumor activity. The chemical name is 3’,4’-didehydro-4’-deoxy-C’-norvincaleukoblastine [R-(R*,R*)-2,3-dihydroxybutanedioate (1:2)(salt)]. Vinorelbine tartrate has the following structure.
Vinorelbine tartrate is a white to yellow or light brown amorphous powder with the molecular formula C45H54N4O8·2C4H6O6 and molecular weight of 1079.12. The aqueous solubility is >1,000 mg/mL in distilled water.The pH of Vinorelbine Injection is approximately 3.5. Clinical Pharmacology :
Vinorelbine is a vinca alkaloid that interferes with microtubule assembly. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units, vindoline and catharanthine. Unlike other vinca alkaloids, the catharanthine unit is the site of structural modification for vinorelbine. The antitumor activity of vinorelbine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Like other vinca alkaloids, vinorelbine may also interfere with: 1) amino acid, cyclic AMP, and glutathione metabolism, 2) calmodulin- dependent Ca++-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis. In intact tectal plates from mouse embryos, vinorelbine, vincristine, and vinblastine inhibited mitotic microtubule formation at the same concentration (2 µM), inducing a blockade of cells at metaphase. Vincristine produced depolymerization of axonal microtubules at 5 µM, but vinblastine and vinorelbine did not have this effect until concentrations of 30 µM and 40 µM, respectively. These data suggest relative selectivity of vinorelbine for mitotic microtubules. Indications And Usage :
Vinorelbine is indicated as a single agent or in combination with for the first-line treatment of ambulatory patients with unresectable, advanced nonsmall cell lung cancer (NSCLC). In patients with Stage IV NSCLC, Vinorelbine is indicated as a single agent or in combination with. In Stage III NSCLC, Vinorelbine is indicated in combination with. Contraindications :
Administration of Vinorelbine is contraindicated in patients with pretreatment granulocyte counts <1,000 cells/mm3 Warning :
Vinorelbine should not be used in pregnancy,lactation and in pediatrics..