VINCRISTINE SULFATE PFS

Clinical safety rating: avoid

Contraindicated (not allowed)

How it works

Vincristine is a vinca alkaloid that binds to tubulin, inhibiting microtubule formation and disrupting mitotic spindle assembly, causing metaphase arrest in dividing cells.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; excreted in bile and feces; renal excretion is minor.
Excretion	Primarily hepatobiliary excretion (70-80%); renal excretion accounts for 10-20% (mostly metabolites); <1% excreted unchanged in urine.
Half-life	Terminal half-life is 19-155 hours (mean ~85 hours) in adults; prolonged in hepatic impairment or elderly.
Protein binding	75-90% bound, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Vd: 4-10 L/kg (large, indicating extensive tissue binding and distribution).
Bioavailability	Oral bioavailability is <10% (not administered orally); administered IV only.
Onset of Action	IV: Onset within 4-7 days for hematologic effects; peak effect at 7-10 days.
Duration of Action	Duration of action: Approximately 7-10 days; neurotoxicity may persist for weeks to months after cessation.

Classification & Brands

Dosing & administration

1.4 mg/m2 IV push weekly, maximum single dose 2 mg.

Dosage form	INJECTABLE
Renal impairment	No adjustment required for GFR >10 mL/min; for GFR ≤10 mL/min, consider 50% dose reduction.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: reduce dose by 75%.
Pediatric use	1.5-2 mg/m2 IV weekly, maximum 2 mg; for infants ≤10 kg: 0.05 mg/kg IV weekly.
Geriatric use	Start at lower end of dosing range (e.g., 1 mg/m2) due to increased risk of neurotoxicity; monitor closely.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Strong CYP3A4 inhibitors may increase levels Can cause severe peripheral neuropathy and extravasation injury.

Breastfeeding	Excretion into human milk is unknown; however, due to its high molecular weight and low lipophilicity, transfer is likely minimal. No M/P ratio available. Because of potential severe adverse effects (e.g., immunosuppression, neurotoxicity) in the nursing infant, breastfeeding is not recommended during therapy and for at least 1 month after last dose.
Teratogenic Risk	Vincristine is embryotoxic and fetotoxic in animals. First trimester exposure carries a high risk of spontaneous abortion and major congenital malformations (e.g., skeletal, cardiac, CNS). Second and third trimester use may cause fetal growth restriction, oligohydramnios, and neonatal myelosuppression. Use is contraindicated in pregnancy unless no alternative.

Warnings & precautions

■ FDA Black Box Warning

For intravenous use only; fatal if given intrathecally. Must be administered under the supervision of a physician experienced in cancer chemotherapy.

Side Effect Profile

Common Effects	lymphomas
Serious Effects

Absolute Contraindications

Hypersensitivity to vincristine or other vinca alkaloids; intrathecal administration; patients with demyelinating conditions (e.g., Charcot-Marie-Tooth disease) due to increased neurotoxicity risk.

Clinical Precautions

Precautions

Neurotoxicity (peripheral neuropathy, areflexia, autonomic dysfunction); myelosuppression; constipation and ileus; extravasation risk; monitor hepatic function; dose adjustments in hepatic impairment.

Clinical Tips & Counseling

Drug interactions

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