VINCREX

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VINCREX (VINCREX).

How it works

Vinca alkaloid that binds to tubulin, inhibiting microtubule formation, thus disrupting mitotic spindle assembly and arresting cell division at metaphase.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; excreted in bile and feces.
Excretion	Primarily hepatic metabolism via CYP3A4, with biliary excretion of metabolites (65-75% in feces). Renal excretion accounts for 10-20% as unchanged drug and metabolites. Minimal (1-3%) in urine as parent compound.
Half-life	Terminal elimination half-life is 18-36 hours (mean 27 hours) in adults; prolonged in hepatic impairment (up to 60 hours) due to reduced clearance.
Protein binding	85-90% bound primarily to albumin and α1-acid glycoprotein.
Volume of Distribution	0.8-1.0 L/kg (mean 0.9 L/kg) indicating extensive tissue distribution; crosses blood-brain barrier with CNS concentrations ~20% of plasma.
Bioavailability	Oral: 35-45% (due to first-pass metabolism); Sublingual: 50-60%; Intramuscular: 80-90%.
Onset of Action	Intravenous: 5-10 minutes; Oral: 1-2 hours (time to peak concentration). Clinical effect correlates with plasma levels.
Duration of Action	Intravenous: 4-6 hours (clinical effect); Oral: 8-12 hours (sustained release). Duration may increase with renal/hepatic impairment.

Classification & Brands

Dosing & administration

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

Dosage form	INJECTABLE
Renal impairment	CrCl >= 50 mL/min: no adjustment; CrCl 30-49 mL/min: reduce dose by 25%; CrCl < 30 mL/min: reduce dose by 50%.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated.
Pediatric use	2 mg/m2 IV weekly, with dose capped at 2 mg for body surface area >1.33 m2; for infants <6 months: 1.5 mg/m2.
Geriatric use	Use with caution; consider starting at 1.2 mg/m2 due to increased susceptibility to neurotoxicity; monitor closely for peripheral neuropathy.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for VINCREX (VINCREX).

Breastfeeding	Excreted into breast milk; M/P ratio unknown. Due to potential for severe adverse reactions (e.g., myelosuppression, neurotoxicity) in breastfed infants, breastfeeding is contraindicated during therapy and for at least 2 weeks after last dose.
Teratogenic Risk	Vincristine is contraindicated in pregnancy. First trimester: High risk of major congenital malformations, spontaneous abortion, and embryotoxicity. Second and third trimesters: Risk of fetal growth restriction, oligohydramnios, and neonatal pancytopenia. Avoid use unless life-threatening maternal condition.

Warnings & precautions

■ FDA Black Box Warning

For intravenous use only. Intrathecal administration is fatal.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to vinca alkaloids, severe hepatic impairment, pre-existing severe peripheral neuropathy, and concurrent vaccination with live vaccines.

Clinical Precautions

Precautions

Extravasation (severe tissue damage), neurotoxicity (peripheral neuropathy, constipation, seizures), myelosuppression (neutropenia, thrombocytopenia), pulmonary toxicity (bronchospasm, dyspnea), and tumor lysis syndrome.

Clinical Tips & Counseling

Drug interactions

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VINCREX

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VINCREX (VINCREX).

How it works

Vinca alkaloid that binds to tubulin, inhibiting microtubule formation, thus disrupting mitotic spindle assembly and arresting cell division at metaphase.

What the body does with it

Metabolism	Primarily hepatic via CYP3A4; excreted in bile and feces.
Excretion	Primarily hepatic metabolism via CYP3A4, with biliary excretion of metabolites (65-75% in feces). Renal excretion accounts for 10-20% as unchanged drug and metabolites. Minimal (1-3%) in urine as parent compound.
Half-life	Terminal elimination half-life is 18-36 hours (mean 27 hours) in adults; prolonged in hepatic impairment (up to 60 hours) due to reduced clearance.
Protein binding	85-90% bound primarily to albumin and α1-acid glycoprotein.
Volume of Distribution	0.8-1.0 L/kg (mean 0.9 L/kg) indicating extensive tissue distribution; crosses blood-brain barrier with CNS concentrations ~20% of plasma.
Bioavailability	Oral: 35-45% (due to first-pass metabolism); Sublingual: 50-60%; Intramuscular: 80-90%.
Onset of Action	Intravenous: 5-10 minutes; Oral: 1-2 hours (time to peak concentration). Clinical effect correlates with plasma levels.
Duration of Action	Intravenous: 4-6 hours (clinical effect); Oral: 8-12 hours (sustained release). Duration may increase with renal/hepatic impairment.

Classification & Brands

Dosing & administration

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

Dosage form	INJECTABLE
Renal impairment	CrCl >= 50 mL/min: no adjustment; CrCl 30-49 mL/min: reduce dose by 25%; CrCl < 30 mL/min: reduce dose by 50%.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated.
Pediatric use	2 mg/m2 IV weekly, with dose capped at 2 mg for body surface area >1.33 m2; for infants <6 months: 1.5 mg/m2.
Geriatric use	Use with caution; consider starting at 1.2 mg/m2 due to increased susceptibility to neurotoxicity; monitor closely for peripheral neuropathy.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for VINCREX (VINCREX).

Breastfeeding	Excreted into breast milk; M/P ratio unknown. Due to potential for severe adverse reactions (e.g., myelosuppression, neurotoxicity) in breastfed infants, breastfeeding is contraindicated during therapy and for at least 2 weeks after last dose.
Teratogenic Risk	Vincristine is contraindicated in pregnancy. First trimester: High risk of major congenital malformations, spontaneous abortion, and embryotoxicity. Second and third trimesters: Risk of fetal growth restriction, oligohydramnios, and neonatal pancytopenia. Avoid use unless life-threatening maternal condition.

Warnings & precautions

■ FDA Black Box Warning

For intravenous use only. Intrathecal administration is fatal.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to vinca alkaloids, severe hepatic impairment, pre-existing severe peripheral neuropathy, and concurrent vaccination with live vaccines.