Vinblastine Sulfate (Vinblastine) - Uses & Pharmacology

Vinblastine Sulfate

Generic: Vinblastine

Medicinal Chemistry

Molecular Weight 909.1

Molecular Formula C46H58N4O9.H2SO4

IUPAC Name

Dimethyl (2beta,3beta,4beta,5alpha,12beta,19alpha)-15-[(5S,7S,9S)-5-ethyl-5-hydroxy-9-(methoxycarbonyl)-1,4,5,6,7,8,9,10-octahydro-2H-3,7-methanoazacycloundecino[5,4-b]indol-9-yl]-3-hydroxy-16-methoxy-1-methyl-6,7-didehydroaspidospermidine-3,4-dicarboxylate sulfate

Pharmacognosy

Biological Source

Catharanthus roseus (Madagascar Periwinkle)

Active Constituents

Vinblastine, Vincristine

Pharmacology & Synthesis

Mechanism of Action

Binds specifically to tubulin, inhibiting assembly of microtubules and arresting cells in the metaphase of mitosis.

Pharmacokinetics (ADME)

A: Poor oral absorption; strictly administered IV.
D: Highly protein bound, extensive tissue binding.
M: Hepatic via CYP3A4 to active deacetylvinblastine.
E: Biliary and fecal.

Pharmacodynamics

Cytotoxic to rapidly dividing cells; primarily affects leukocyte production and is used in lymphomas (Hodgkin's).

Synthesis Pathway

Dimeric alkaloid formed naturally by the coupling of vindoline and catharanthine.

Safety, Warnings & Interactions

Adverse Effects

Bone marrow suppression (dose-limiting), alopecia, severe tissue necrosis if extravasated.

Contraindications

Active bacterial infection, severe baseline bone marrow suppression.

Drug Interactions

CYP3A4 inhibitors (erythromycin) increase toxicity; mitomycin (pulmonary toxicity).

Pharmaceutics & Compendia

Dosage Forms Injection (as Vinblastine Sulfate)

Official Compendia IP, BP, USP