VINCASAR PFS

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VINCASAR PFS (VINCASAR PFS).

How it works

Vincristine is a vinca alkaloid that binds to tubulin, inhibiting microtubule formation and disrupting mitotic spindle assembly, thereby arresting cell division in metaphase.

What the body does with it

Metabolism	Primarily hepatic metabolism via CYP3A4, with biliary excretion; minor renal elimination.
Excretion	Primarily hepatobiliary excretion; approximately 80% of the dose is eliminated in feces, with less than 20% excreted unchanged in urine. Renal clearance is minor.
Half-life	Terminal elimination half-life ranges from 24 to 35 hours in adults, with a mean of approximately 25 hours. The half-life may be prolonged in patients with hepatic impairment.
Protein binding	About 75% bound to plasma proteins, primarily albumin and beta-globulins.
Volume of Distribution	Volume of distribution is large, approximately 8 L/kg (range 4–15 L/kg), indicating extensive tissue binding and distribution into peripheral compartments.
Bioavailability	Not administered orally; intravenous administration yields 100% bioavailability.
Onset of Action	Following IV administration, clinical effects (e.g., reduction in white blood cell count in leukemia) are typically observed within 7 to 10 days, with maximum effect around 10–14 days.
Duration of Action	Duration of myelosuppressive effect is typically 1 to 3 weeks, but can vary depending on the specific chemotherapeutic regimen and patient factors. Neurotoxicity may persist for weeks to months after discontinuation.

Classification & Brands

Dosing & administration

1.4 mg/m2 intravenously once weekly, typically not exceeding 2 mg.

Dosage form	INJECTABLE
Renal impairment	No dosage adjustment necessary for GFR ≥10 mL/min; for GFR <10 mL/min, reduce dose by 50%.
Liver impairment	Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: avoid use or reduce dose by 75%.
Pediatric use	1.5-2 mg/m2 intravenously once weekly, with maximum single dose of 2 mg.
Geriatric use	Consider starting at 1 mg/m2 intravenously once weekly 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

Comprehensive clinical and safety monograph for VINCASAR PFS (VINCASAR PFS).

Breastfeeding	Excreted into breast milk; M/P ratio not established. Potential for severe neonatal toxicity (myelosuppression, neurotoxicity). Contraindicated during breastfeeding. Advise to discontinue nursing or drug.
Teratogenic Risk	Vincasar PFS is embryotoxic and teratogenic. First trimester exposure carries high risk of spontaneous abortion and major congenital malformations, including skeletal, CNS, and cardiac defects. Second and third trimester exposure is associated with fetal growth restriction, oligohydramnios, and potential neurodevelopmental impairment. Contraindicated in pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Vincristine is for intravenous use only. Fatal if given intrathecally. Extravasation can cause severe local tissue injury.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to vincristine or other vinca alkaloids; intrathecal administration; demyelinating conditions (e.g., Charcot-Marie-Tooth disease).

Clinical Precautions

Precautions

Neurotoxicity (peripheral neuropathy, autonomic neuropathy, cranial nerve palsies), constipation/ileus, myelosuppression, extravasation, hepatic impairment, pulmonary toxicity, SIADH, ocular toxicity.

Clinical Tips & Counseling

Drug interactions

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VINCASAR PFS

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VINCASAR PFS (VINCASAR PFS).

How it works

Vincristine is a vinca alkaloid that binds to tubulin, inhibiting microtubule formation and disrupting mitotic spindle assembly, thereby arresting cell division in metaphase.

What the body does with it

Metabolism	Primarily hepatic metabolism via CYP3A4, with biliary excretion; minor renal elimination.
Excretion	Primarily hepatobiliary excretion; approximately 80% of the dose is eliminated in feces, with less than 20% excreted unchanged in urine. Renal clearance is minor.
Half-life	Terminal elimination half-life ranges from 24 to 35 hours in adults, with a mean of approximately 25 hours. The half-life may be prolonged in patients with hepatic impairment.
Protein binding	About 75% bound to plasma proteins, primarily albumin and beta-globulins.
Volume of Distribution	Volume of distribution is large, approximately 8 L/kg (range 4–15 L/kg), indicating extensive tissue binding and distribution into peripheral compartments.
Bioavailability	Not administered orally; intravenous administration yields 100% bioavailability.
Onset of Action	Following IV administration, clinical effects (e.g., reduction in white blood cell count in leukemia) are typically observed within 7 to 10 days, with maximum effect around 10–14 days.
Duration of Action	Duration of myelosuppressive effect is typically 1 to 3 weeks, but can vary depending on the specific chemotherapeutic regimen and patient factors. Neurotoxicity may persist for weeks to months after discontinuation.

Classification & Brands

Dosing & administration

1.4 mg/m2 intravenously once weekly, typically not exceeding 2 mg.

Dosage form	INJECTABLE
Renal impairment	No dosage adjustment necessary for GFR ≥10 mL/min; for GFR <10 mL/min, reduce dose by 50%.
Liver impairment	Child-Pugh Class A: no adjustment; Class B: reduce dose by 50%; Class C: avoid use or reduce dose by 75%.
Pediatric use	1.5-2 mg/m2 intravenously once weekly, with maximum single dose of 2 mg.
Geriatric use	Consider starting at 1 mg/m2 intravenously once weekly 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

Comprehensive clinical and safety monograph for VINCASAR PFS (VINCASAR PFS).

Breastfeeding	Excreted into breast milk; M/P ratio not established. Potential for severe neonatal toxicity (myelosuppression, neurotoxicity). Contraindicated during breastfeeding. Advise to discontinue nursing or drug.
Teratogenic Risk	Vincasar PFS is embryotoxic and teratogenic. First trimester exposure carries high risk of spontaneous abortion and major congenital malformations, including skeletal, CNS, and cardiac defects. Second and third trimester exposure is associated with fetal growth restriction, oligohydramnios, and potential neurodevelopmental impairment. Contraindicated in pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Vincristine is for intravenous use only. Fatal if given intrathecally. Extravasation can cause severe local tissue injury.

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to vincristine or other vinca alkaloids; intrathecal administration; demyelinating conditions (e.g., Charcot-Marie-Tooth disease).