VESPRIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VESPRIN (VESPRIN).

How it works

Trifluoperazine is a typical antipsychotic that blocks postsynaptic D2 dopamine receptors in the mesolimbic pathway. It also has alpha-adrenergic blocking and anticholinergic effects.

What the body does with it

Metabolism	Hepatic metabolism via CYP450 enzymes; primarily CYP1A2 and CYP3A4.
Excretion	Primarily hepatic metabolism with metabolites excreted in urine and feces. Approximately 20-30% of a single dose is excreted unchanged in urine, with the remainder as metabolites in urine (30-40%) and feces (20-30%).
Half-life	Terminal elimination half-life ranges from 1 to 2.5 hours, with a mean of approximately 1.5 hours. Due to its short half-life, multiple daily dosing is required to maintain therapeutic levels, and the drug is rapidly cleared after discontinuation.
Protein binding	Approximately 90-95% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is approximately 3.0-5.0 L/kg, indicating extensive tissue distribution and high lipophilicity. This large Vd results in low plasma concentrations relative to tissue levels.
Bioavailability	Oral bioavailability is approximately 10-20% due to extensive first-pass metabolism. Intramuscular bioavailability is nearly 100% because it bypasses hepatic first-pass effect.
Onset of Action	Intramuscular: 10-15 minutes. Oral: 30-60 minutes. Intravenous: 5-10 minutes.
Duration of Action	Intramuscular: 2-4 hours. Oral: 3-4 hours. Intravenous: 1-2 hours. Clinical duration may be shorter due to rapid metabolism and redistribution. Duration is dose-dependent.

Classification & Brands

Dosing & administration

10-50 mg intramuscularly every 4-6 hours as needed; oral: 25-50 mg every 4-6 hours

Dosage form	INJECTABLE
Renal impairment	No specific adjustment criteria established; use caution in severe renal impairment (CrCl <30 mL/min) due to potential accumulation
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use or use with extreme caution
Pediatric use	Not recommended for use in pediatric patients due to lack of safety and efficacy data
Geriatric use	Initiate at lower doses (e.g., 5-10 mg IM or 10-25 mg oral) with careful titration; monitor for hypotension, sedation, and anticholinergic effects

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for VESPRIN (VESPRIN).

Breastfeeding	Present in breast milk; M/P ratio unknown. Potential for sedation, extrapyramidal effects in infant. Use caution; monitor infant for adverse effects. Consider alternative agents.
Teratogenic Risk	VESPRIN (triflupromazine) is a phenothiazine antipsychotic. First trimester: Limited data; animal studies show embryotoxicity at high doses; no evidence of major malformations in humans. Second and third trimesters: Risk of extrapyramidal symptoms and withdrawal in neonates if used near term. Not recommended unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. VESPRIN is not approved for the treatment of dementia-related psychosis.

Side Effect Profile

Serious Effects

Absolute Contraindications

Comatose states; CNS depression; bone marrow suppression; known hypersensitivity to phenothiazines; narrow-angle glaucoma; concurrent use with large doses of other CNS depressants.

Clinical Precautions

Precautions

Increased risk of cerebrovascular events in elderly dementia patients; neuroleptic malignant syndrome; tardive dyskinesia; QT prolongation; seizures; anticholinergic effects; orthostatic hypotension.

Clinical Tips & Counseling

Drug interactions

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VESPRIN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for VESPRIN (VESPRIN).

How it works

Trifluoperazine is a typical antipsychotic that blocks postsynaptic D2 dopamine receptors in the mesolimbic pathway. It also has alpha-adrenergic blocking and anticholinergic effects.

What the body does with it

Metabolism	Hepatic metabolism via CYP450 enzymes; primarily CYP1A2 and CYP3A4.
Excretion	Primarily hepatic metabolism with metabolites excreted in urine and feces. Approximately 20-30% of a single dose is excreted unchanged in urine, with the remainder as metabolites in urine (30-40%) and feces (20-30%).
Half-life	Terminal elimination half-life ranges from 1 to 2.5 hours, with a mean of approximately 1.5 hours. Due to its short half-life, multiple daily dosing is required to maintain therapeutic levels, and the drug is rapidly cleared after discontinuation.
Protein binding	Approximately 90-95% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is approximately 3.0-5.0 L/kg, indicating extensive tissue distribution and high lipophilicity. This large Vd results in low plasma concentrations relative to tissue levels.
Bioavailability	Oral bioavailability is approximately 10-20% due to extensive first-pass metabolism. Intramuscular bioavailability is nearly 100% because it bypasses hepatic first-pass effect.
Onset of Action	Intramuscular: 10-15 minutes. Oral: 30-60 minutes. Intravenous: 5-10 minutes.
Duration of Action	Intramuscular: 2-4 hours. Oral: 3-4 hours. Intravenous: 1-2 hours. Clinical duration may be shorter due to rapid metabolism and redistribution. Duration is dose-dependent.

Classification & Brands

Dosing & administration

10-50 mg intramuscularly every 4-6 hours as needed; oral: 25-50 mg every 4-6 hours

Dosage form	INJECTABLE
Renal impairment	No specific adjustment criteria established; use caution in severe renal impairment (CrCl <30 mL/min) due to potential accumulation
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use or use with extreme caution
Pediatric use	Not recommended for use in pediatric patients due to lack of safety and efficacy data
Geriatric use	Initiate at lower doses (e.g., 5-10 mg IM or 10-25 mg oral) with careful titration; monitor for hypotension, sedation, and anticholinergic effects

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for VESPRIN (VESPRIN).

Breastfeeding	Present in breast milk; M/P ratio unknown. Potential for sedation, extrapyramidal effects in infant. Use caution; monitor infant for adverse effects. Consider alternative agents.
Teratogenic Risk	VESPRIN (triflupromazine) is a phenothiazine antipsychotic. First trimester: Limited data; animal studies show embryotoxicity at high doses; no evidence of major malformations in humans. Second and third trimesters: Risk of extrapyramidal symptoms and withdrawal in neonates if used near term. Not recommended unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. VESPRIN is not approved for the treatment of dementia-related psychosis.

Side Effect Profile

Serious Effects

Absolute Contraindications

Comatose states; CNS depression; bone marrow suppression; known hypersensitivity to phenothiazines; narrow-angle glaucoma; concurrent use with large doses of other CNS depressants.

Clinical Precautions

Precautions

Increased risk of cerebrovascular events in elderly dementia patients; neuroleptic malignant syndrome; tardive dyskinesia; QT prolongation; seizures; anticholinergic effects; orthostatic hypotension.

Clinical Tips & Counseling

Drug interactions

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