VINBLASTINE SULFATE
Clinical safety rating: avoid
Contraindicated (not allowed)
Vinca alkaloid that inhibits microtubule formation by binding to tubulin, thereby disrupting mitotic spindle assembly and preventing cell division during metaphase.
| Metabolism | Hepatic metabolism primarily via CYP3A4; also metabolized to active metabolite 4-O-deacetylvinblastine. Excreted mainly in bile (feces) with minimal renal excretion. |
| Excretion | Primarily hepatobiliary. Approximately 95% of the dose is excreted in feces via bile, with less than 5% excreted unchanged in urine. Renal excretion is a minor pathway. |
| Half-life | Terminal elimination half-life is approximately 25 hours (range 20-30 hours). This prolonged half-life supports a weekly dosing schedule. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily tubulin and other tissue proteins, as well as albumin. |
| Volume of Distribution | Volume of distribution is extensive, approximately 27-75 L/kg (mean about 30 L/kg), indicating extensive tissue binding and distribution. |
| Bioavailability | Not orally bioavailable (<<5%). Administered only intravenously. |
| Onset of Action | IV: Antitumor effect typically observed within 1-2 weeks, but maximal response may take 4-6 weeks. |
| Duration of Action | Myelosuppression (leukopenia) nadir occurs at 5-10 days post-dose, with recovery in 7-21 days. Neurologic effects may persist for weeks to months. |
Adult: 3.7-18.5 mg/m2 IV weekly, typically 6-8 mg/m2; dose titrated based on leukocyte count.
| Dosage form | Injectable |
| Renal impairment | No specific dose adjustment recommended; consider alternative if CrCl <10 mL/min or hemodialysis. |
| Liver impairment | Child-Pugh A: 50% dose reduction. Child-Pugh B: 75% dose reduction. Child-Pugh C: avoid use. |
| Pediatric use | Weight-based: 2.5-7.5 mg/m2 IV weekly; adjust based on CBC and clinical response. |
| Geriatric use | No specific dose adjustment; monitor for increased neurotoxicity and myelosuppression due to age-related decline in clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Strong CYP3A4 inhibitors may increase levels Can cause severe myelosuppression and extravasation injury.
| Breastfeeding | Contraindicated during breastfeeding. Vinblastine is excreted into human milk; M/P ratio not determined. Potential for severe adverse effects in nursing infant, including immunosuppression and growth impairment. |
| Teratogenic Risk | Pregnancy Category D. Vinblastine is embryotoxic and teratogenic in animal studies. First trimester: high risk of spontaneous abortion and major malformations (neural tube defects, skeletal anomalies). Second and third trimesters: increased risk of growth restriction, preterm birth, and fetal myelosuppression. |
■ FDA Black Box Warning
Vinblastine sulfate should be administered only under the supervision of a physician experienced in cancer chemotherapy. Extravasation during intravenous administration may cause severe local tissue damage, including necrosis. Intrathecal administration is contraindicated and can be fatal.
| Common Effects | other cancers |
| Serious Effects |
Hypersensitivity to vinblastine or other vinca alkaloids; severe leukopenia (white blood cell count < 2000/µL) or thrombocytopenia; severe hepatic impairment; intrathecal administration
| Precautions | Bone marrow suppression (especially leukopenia); dose-dependent and reversible. Monitor complete blood counts. Hepatotoxicity; reduce dose in hepatic impairment. Avoid extravasation; administer through a running IV line. Use with caution in patients with infection or severe debilitation. May cause neurotoxicity (peripheral neuropathy). Discontinue if severe stomatitis or bone marrow depression occurs. |
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| Fetal Monitoring |
| Complete blood count with differential prior to each dose and during nadir (days 7-10). Liver function tests (bilirubin, transaminases). Renal function (serum creatinine). Fetal ultrasound for growth and anatomy if exposure occurs. Monitor for signs of infection, bleeding, and neuropathy. |
| Fertility Effects | May cause gonadal suppression and irreversible azoospermia or amenorrhea. Risk of premature ovarian failure in females and testicular atrophy in males. Fertility preservation counseling recommended before treatment. |