MajorFirst-generation antipsychotics. Butyrophenone derivatives×Antituberculous antibiotic
Updated · Methodology
Mechanism
Rifampicin strongly induces CYP3A4 – the main haloperidol metabolic route. Haloperidol plasma levels fall by 70%; antipsychotic effect weakens.
Symptoms
Return of positive symptoms: hallucinations, delusions, agitation. In schizophrenia: risk of acute relapse.
Management
During anti-TB therapy, increase haloperidol 2- to 3-fold with clinical monitoring. Alternative antipsychotics without CYP3A4 dependence: olanzapine or aripiprazole.
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Sources
- FDA: Rifampin capsule (Ani Pharmaceuticals, Inc.) – Prescribing Information (2010)– ; DailyMed setid b389b1a3-672f-47e3-916c-4a9c044b211b
- AEMPS: Ficha técnica: Haloperidol Esteve 2 mg/ml solución oral (nº registro 58355), secciones 4.4 y 4.5 (2020)– AEMPS, CIMA, nº registro 58355, revisión 07/2020, secciones 4.4 y 4.5
- AEMPS: Ficha técnica: Rifampicina (nº registro 49034), sección 4.5 (2026)– AEMPS, CIMA, nº registro 49034, revisión 08/2026, sección 4.5