Trifluoperazine is a high-potency, first-generation (typical) piperazine phenothiazine antipsychotic. It is primarily indicated for the management of schizophrenia and other psychotic disorders, and secondarily for the short-term management of severe anxiety and nausea/vomiting. It acts as a potent dopamine D2 receptor antagonist in the mesolimbic pathway, with significant alpha-1 adrenergic and muscarinic cholinergic blockade contributing to its side effect profile. In India, it is a widely used, cost-effective antipsychotic, though its use is tempered by a higher risk of extrapyramidal symptoms (EPS) compared to many atypical antipsychotics.
Adult: Psychosis: Initial: 2-5 mg twice daily. May increase gradually to 15-20 mg/day in divided doses. Max rarely exceeds 40 mg/day. Anxiety: 1-2 mg twice daily. Max: 6 mg/day; not for long-term use (>12 weeks).
Note: Administer orally with or without food (food may slightly delay absorption). To minimize orthostatic hypotension, advise taking with a full glass of water and avoiding sudden posture changes. The tablet should be swallowed whole, not crushed or chewed. For anxiety, use the lowest effective dose for the shortest duration.
Trifluoperazine exerts its primary antipsychotic effect through potent and relatively selective antagonism of postsynaptic dopamine D2 receptors in the mesolimbic pathway of the brain, reducing positive symptoms of psychosis (e.g., hallucinations, delusions). Its antiemetic effect is due to D2 antagonism in the chemoreceptor trigger zone (CTZ). Its anxiolytic effect is less clear but may involve limbic system modulation.
Pregnancy: Category C (US FDA). Not recommended unless potential benefit justifies risk. Risk of EPS and withdrawal symptoms in the neonate if used in the 3rd trimester. Use only if clearly needed and under psychiatric supervision.
Driving: May impair alertness, coordination, and reaction time. Patients should not drive or operate machinery until their individual response is known, especially during initial therapy and dose adjustments.
| Levodopa, Dopamine Agonists (e.g., Pramipexole) | Mutual antagonism of therapeutic effects | Major |
| Other CNS Depressants (Alcohol, Opioids, Benzodiazepines) | Additive CNS and respiratory depression | Major |
| Anticholinergics (Trihexyphenidyl, Atropine) | Increased anticholinergic side effects (ileus, hyperthermia, confusion) | Moderate |
| Antihypertensives (especially Alpha-blockers) | Potentiated hypotension | Moderate |
| QTc-prolonging drugs (Amiodarone, Sotalol, Ciprofloxacin) | Increased risk of torsades de pointes | Major |
| CYP2D6 Inhibitors (Paroxetine, Fluoxetine, Quinidine) | Increased trifluoperazine levels and toxicity | Moderate |
| Lithium | Increased risk of neurotoxicity (encephalopathy) and EPS | Moderate |
| Metoclopramide, Prochlorperazine | Increased risk of EPS | Moderate |
Same composition (Trifluoperazine (5mg)), different brands: