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. |
| Molecular Weight | 909.05 |
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 | Contraindicated; risk of teratogenicity and fetal loss due to antimitotic activity. Pregnancy should be excluded before treatment. |
| 2nd trimester | Contraindicated; may cause fetal harm. Use only if maternal benefit outweighs risk; consider termination. |
| 3rd trimester | Contraindicated; may cause neonatal toxicity. Avoid use near term. |
Clinical note
Strong CYP3A4 inhibitors may increase levels Can cause severe myelosuppression and extravasation injury.
| Placental transfer | Crosses placenta; embryotoxic and teratogenic in animal studies. Human data limited but presumed transfer. |
| Breastfeeding | Discontinue breastfeeding during therapy and for at least 2 weeks after last dose. Vinblastine is excreted in breast milk and may cause severe adverse effects in nursing infants. |
■ 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 any componentSevere myelosuppression (ANC < 1500/mm3, platelets < 75,000/mm3)Active infectionPre-existing neurological toxicity (e.g., Charcot-Marie-Tooth)Pregnancy (unless therapeutic abortion)
| 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. |
Loading safety data…
| Lactation Rating |
| L5 - Contraindicated |
| 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. |
| 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. |
| Food/Dietary | Grapefruit and grapefruit juice may increase vinblastine toxicity; avoid consumption. St. John's Wort may reduce efficacy; avoid concurrent use. No other specific food restrictions. |
| Clinical Pearls | Vinblastine is a vesicant; administer via slow IV push into a freely flowing IV line to avoid extravasation. Monitor for myelosuppression (especially neutropenia) and neurotoxicity (peripheral neuropathy, constipation). Dose adjustment required in hepatic impairment (biliary obstruction increases toxicity). Contraindicated in patients with significant bacterial infection or bone marrow suppression not caused by malignancy. |
| Patient Advice | Report any signs of infection (fever, sore throat) or unusual bleeding/bruising immediately. · Avoid live vaccines during and for 6 months after treatment. · Use effective contraception during therapy and for at least 3 months after. · Notify your doctor if you experience constipation, numbness/tingling in hands/feet, or muscle weakness. · This drug can cause hair loss, which is usually reversible after treatment ends. |