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NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Phenothiazines with piperazine structure
thiopropazate
N05AB05
Forms & Strengths
- Oral tablets: 5 mg
- Oral tablets: 10 mg
Adult Dosing
- Schizophrenia/Psychosis: Initial 5 to 10 mg orally 3 times daily
- Maintenance: Titrated based on clinical response up to 40 mg daily
- Maximum daily dose: 60 mg in divided doses
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 12 years
- Not generally recommended for pediatric use due to high risk of extrapyramidal symptoms
Indications
- Management of manifestations of psychotic disorders, particularly schizophrenia
- Control of severe nausea and vomiting (historical indication)
Mechanism of Action
- Piperazine phenothiazine antipsychotic
- Acts as a dopamine receptor antagonist in the brain (primarily D2 receptors in the mesolimbic pathway)
- Exerts anticholinergic, antihistaminic, and alpha-1 adrenergic blocking properties
Contraindications
- Hypersensitivity to thiopropazate or other phenothiazines
- Central nervous system depression or comatose states
- Severe cardiovascular disease or bone marrow depression
- Concurrent use of large amounts of central nervous system depressants
Adverse Reactions
- High incidence of extrapyramidal symptoms (acute dystonia, akathisia, parkinsonism)
- Tardive dyskinesia with long-term use
- Sedation, drowsiness, and dizziness
- Anticholinergic effects (dry mouth, blurred vision, urinary retention, constipation)
- Orthostatic hypotension and tachycardia
- Rare risk of neuroleptic malignant syndrome
Drug Interactions
- Potentiation of CNS depression with alcohol, opioids, sedatives, and hypnotics
- Enhanced anticholinergic toxicity when combined with drugs possessing anticholinergic properties
- Increased risk of extrapyramidal symptoms with other dopamine antagonists or metoclopramide
- Hypotensive effects enhanced by antihypertensive agents
Curated Content: Needs Vetting Before Put to Clinical Use