Perphenazine (Trilafon)

Class

First-generation (typical) antipsychotic; piperazine phenothiazine derivative

Mechanism

Dopamine D₂ receptor antagonist with moderate anticholinergic and antihistaminic properties; also has antiemetic effects via dopamine blockade in the chemoreceptor trigger zone

FDA-Approved Use

Schizophrenia, severe nausea and vomiting

Off-Label Use

Augmentation in treatment-resistant depression (especially in tricyclic antidepressant [TCA] combinations), acute agitation, and behavioral dysregulation in neuropsychiatric conditions

Formulation

Oral tablet, oral solution, short-acting intramuscular (IM) injection

Titration

Typically initiated at 4–8 mg p.o. twice daily, titrated gradually based on response and tolerability

Dose Range

8–64 mg/day, divided BID to QID

Kinetics

Hepatic metabolism via CYP2D6 with variable half-life (~8–12 hours); steady state reached in several days

Common AEs

Extrapyramidal symptoms (EPS), sedation, dry mouth, constipation, blurred vision, and weight gain

Serious/Rare AEs

Tardive dyskinesia, neuroleptic malignant syndrome (NMS), QTc prolongation, cholestatic jaundice, and seizure threshold lowering

Monitoring

Monitor for EPS (e.g., AIMS every 6–12 months), weight and metabolic parameters periodically, and ECG if cardiac risk factors or polypharmacy. Consider prolactin or liver enzymes if symptomatic.

Black Box Warning

Increased mortality in elderly patients with dementia-related psychosis

Considerations

Use caution in older adults and individuals with cognitive impairment, Parkinson’s disease (PD), or traumatic brain injury (TBI) due to heightened risk of rigidity, sedation, and falls. Perphenazine is not typically used first-line for psychosis in dementia due to increased sensitivity to EPS and anticholinergic burden. Lower doses and close monitoring may be considered if used in medically complex patients.