VESPRIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VESPRIN (VESPRIN).
Trifluoperazine is a typical antipsychotic that blocks postsynaptic D2 dopamine receptors in the mesolimbic pathway. It also has alpha-adrenergic blocking and anticholinergic effects.
| 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. |
| Molecular Weight | 352.36 |
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 |
| 1st trimester | Avoid. Vesprin (triflupromazine) is an antipsychotic of the phenothiazine class. First trimester exposure may be associated with increased risk of congenital malformations, though data are limited. Use only if benefit outweighs risk. |
| 2nd trimester | Avoid. Second trimester use may cause maternal hypotension and affect placental perfusion. Neonatal effects include extrapyramidal symptoms and withdrawal. Use only if clearly needed. |
| 3rd trimester | Avoid. Third trimester use has been associated with neonatal extrapyramidal symptoms, agitation, hypertonia, hypotonia, and withdrawal. Use near term may prolong labor due to oxytocic effects. |
Clinical note
Comprehensive clinical and safety monograph for VESPRIN (VESPRIN).
| Placental transfer | Phenothiazines, including triflupromazine, cross the placenta. Transfer is expected to be moderate based on molecular weight and lipophilicity. Animal studies show fetal distribution, but human data are limited. |
| Breastfeeding |
■ 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.
| Serious Effects |
Comatose states from CNS depressantsKnown hypersensitivity to phenothiazinesSevere bone marrow depressionPheochromocytomaSubcortical brain damage
| Precautions | Increased risk of cerebrovascular events in elderly dementia patients; neuroleptic malignant syndrome; tardive dyskinesia; QT prolongation; seizures; anticholinergic effects; orthostatic hypotension. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase drug levels. Limit caffeine intake. Take with food or milk if gastrointestinal upset occurs. Avoid high-tyramine foods (aged cheeses, cured meats) if taking MAOIs concurrently. |
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| Triflupromazine is excreted into breast milk in low concentrations. Monitor infant for drowsiness, irritability, and developmental milestones. Use with caution; consider alternative agents with better safety profile (e.g., lower potency antipsychotics). |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| Fetal Monitoring | Monitor maternal blood pressure, liver function, CBC, EKG. Assess fetal growth and wellbeing via ultrasound. Monitor neonate for extrapyramidal symptoms, jaundice, and sedation. |
| Fertility Effects | May cause hyperprolactinemia leading to menstrual irregularities, galactorrhea, and temporary infertility. Effects on female fertility via prolactin elevation. Male fertility may be affected due to sexual dysfunction. |
| Clinical Pearls | VESPRIN (triflupromazine) is a phenothiazine antipsychotic with potent antiemetic properties. Start at low doses and titrate slowly to avoid orthostatic hypotension. Monitor for extrapyramidal symptoms (EPS), especially in elderly. Use with caution in patients with QT prolongation or electrolyte imbalances. Avoid concurrent use with other CNS depressants. |
| Patient Advice | Avoid alcohol and driving until you know how this medication affects you. · Rise slowly from sitting or lying positions to prevent dizziness. · Report any involuntary muscle movements or rigidity immediately. · Maintain adequate hydration and avoid excessive sun exposure due to photosensitivity. · Do not stop abruptly; taper under medical supervision. |