ONCOVIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ONCOVIN (ONCOVIN).

How it works

Vincristine is a vinca alkaloid that binds to tubulin, inhibiting microtubule formation and disrupting mitotic spindle assembly, leading to metaphase arrest and cell death.

What the body does with it

Metabolism	Vincristine is primarily metabolized by the hepatic cytochrome P450 system, specifically CYP3A4 and CYP3A5, to active and inactive metabolites. It is extensively distributed and excreted primarily via bile and feces.
Excretion	Primarily hepatobiliary (fecal) excretion: ~80% as unchanged drug and metabolites via bile into feces. Renal excretion: <10% unchanged in urine. Extensive metabolism in liver via CYP3A4.
Half-life	Terminal elimination half-life: approximately 19-155 hours (mean ~85 hours) in adults. In elderly and hepatic impairment, half-life is prolonged. Highly variable due to extensive tissue binding and prolonged terminal phase.
Protein binding	~75% bound to serum proteins, primarily albumin and also to α1-acid glycoprotein and lipoproteins.
Volume of Distribution	Very large, mean Vd: 8.0-15.0 L/kg (range 6-20 L/kg) indicating extensive tissue binding and distribution into tissues including heart, liver, kidney, and peripheral nerves (highest in thyroid, liver, kidney, and lung).
Bioavailability	Oral bioavailability is negligible (<5%) due to extensive first-pass metabolism and active efflux by P-glycoprotein; therefore, not administered orally. Only approved via IV route.
Onset of Action	IV administration: Onset of clinical effect (e.g., mitotic arrest, symptomatic improvement) typically within 24-48 hours for solid tumors and leukemia.
Duration of Action	Duration of antimitotic effect persists for several days to weeks after a single dose. Neurotoxic effects (e.g., peripheral neuropathy) can be prolonged or irreversible.

Classification & Brands

Dosing & administration

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

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for GFR ≥ 10 mL/min; avoid in GFR < 10 mL/min not on dialysis
Liver impairment	Child-Pugh A: 1.4 mg/m2; Child-Pugh B: 50% dose reduction; Child-Pugh C: avoid
Pediatric use	1.5-2 mg/m2 IV weekly, maximum 2 mg; BSA < 0.5 m2: 0.05 mg/kg weekly
Geriatric use	Monitor neurotoxicity; consider starting at 1 mg IV weekly

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ONCOVIN (ONCOVIN).

Breastfeeding	Excreted into breast milk; M/P ratio unknown. Potential for serious adverse reactions in nursing infants, including myelosuppression and gastrointestinal toxicity. Contraindicated during breastfeeding. Discontinue breastfeeding or discontinue drug.
Teratogenic Risk	Pregnancy Category D. First trimester: high risk of fetal malformations including craniofacial defects, skeletal anomalies, and CNS abnormalities. Second and third trimesters: risk of intrauterine growth restriction, prematurity, myelosuppression, and neonatal pancytopenia. Avoid use in pregnant women unless potential benefit outweighs severe fetal risk.

Warnings & precautions

■ FDA Black Box Warning

ONCOVIN (vincristine) is for intravenous use only. Intrathecal administration is fatal and can cause progressive paralysis, coma, and death. Syringes containing this product must be labeled 'For Intravenous Use Only' and should be prepared and dispensed in a manner that prevents intrathecal administration.

Side Effect Profile

Common Effects	Urinary tract infection
Serious Effects

Absolute Contraindications

["Intrathecal administration (absolute contraindication)","Hypersensitivity to vincristine or any component of the formulation","Active severe infection (relative)","Significant bone marrow suppression (relative)"]

Clinical Precautions

Precautions

["Neurotoxicity: Dose-limiting peripheral neuropathy, including motor, sensory, and autonomic dysfunction; risk increases with cumulative dose.","Extravasation: Causes severe tissue damage if extravasation occurs; administer via running IV infusion with close monitoring.","Neuromuscular toxicity: May cause severe constipation, paralytic ileus, or urinary retention; use prophylactic bowel regimen.","Myelosuppression: May cause leukopenia, thrombocytopenia, and anemia; monitor blood counts regularly.","Patients with pre-existing neuromuscular disease or prior neurotoxic chemotherapy are at higher risk for neurotoxicity.","Hepatic impairment: Dose reduction recommended for significant hepatic dysfunction.","Carcinogenicity: Has been associated with secondary malignancies.","Fertility impairment: May cause irreversible testicular or ovarian failure."]

Drug interactions

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ONCOVIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ONCOVIN (ONCOVIN).

How it works

Vincristine is a vinca alkaloid that binds to tubulin, inhibiting microtubule formation and disrupting mitotic spindle assembly, leading to metaphase arrest and cell death.

What the body does with it

Metabolism	Vincristine is primarily metabolized by the hepatic cytochrome P450 system, specifically CYP3A4 and CYP3A5, to active and inactive metabolites. It is extensively distributed and excreted primarily via bile and feces.
Excretion	Primarily hepatobiliary (fecal) excretion: ~80% as unchanged drug and metabolites via bile into feces. Renal excretion: <10% unchanged in urine. Extensive metabolism in liver via CYP3A4.
Half-life	Terminal elimination half-life: approximately 19-155 hours (mean ~85 hours) in adults. In elderly and hepatic impairment, half-life is prolonged. Highly variable due to extensive tissue binding and prolonged terminal phase.
Protein binding	~75% bound to serum proteins, primarily albumin and also to α1-acid glycoprotein and lipoproteins.
Volume of Distribution	Very large, mean Vd: 8.0-15.0 L/kg (range 6-20 L/kg) indicating extensive tissue binding and distribution into tissues including heart, liver, kidney, and peripheral nerves (highest in thyroid, liver, kidney, and lung).
Bioavailability	Oral bioavailability is negligible (<5%) due to extensive first-pass metabolism and active efflux by P-glycoprotein; therefore, not administered orally. Only approved via IV route.
Onset of Action	IV administration: Onset of clinical effect (e.g., mitotic arrest, symptomatic improvement) typically within 24-48 hours for solid tumors and leukemia.
Duration of Action	Duration of antimitotic effect persists for several days to weeks after a single dose. Neurotoxic effects (e.g., peripheral neuropathy) can be prolonged or irreversible.

Classification & Brands

Dosing & administration

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

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for GFR ≥ 10 mL/min; avoid in GFR < 10 mL/min not on dialysis
Liver impairment	Child-Pugh A: 1.4 mg/m2; Child-Pugh B: 50% dose reduction; Child-Pugh C: avoid
Pediatric use	1.5-2 mg/m2 IV weekly, maximum 2 mg; BSA < 0.5 m2: 0.05 mg/kg weekly
Geriatric use	Monitor neurotoxicity; consider starting at 1 mg IV weekly

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for ONCOVIN (ONCOVIN).

Breastfeeding	Excreted into breast milk; M/P ratio unknown. Potential for serious adverse reactions in nursing infants, including myelosuppression and gastrointestinal toxicity. Contraindicated during breastfeeding. Discontinue breastfeeding or discontinue drug.
Teratogenic Risk	Pregnancy Category D. First trimester: high risk of fetal malformations including craniofacial defects, skeletal anomalies, and CNS abnormalities. Second and third trimesters: risk of intrauterine growth restriction, prematurity, myelosuppression, and neonatal pancytopenia. Avoid use in pregnant women unless potential benefit outweighs severe fetal risk.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Common Effects	Urinary tract infection
Serious Effects

ONCOVIN

How it works

What the body does with it

Classification & Brands

Dosing & administration

Use during pregnancy

Warnings & precautions

Side Effect Profile

Absolute Contraindications

Clinical Precautions

Drug interactions

ONCOVIN

How it works

What the body does with it

Classification & Brands

Dosing & administration

Use during pregnancy

Warnings & precautions

Side Effect Profile

Absolute Contraindications

Clinical Precautions

Drug interactions

Clinical Tips & Counseling