Clinical Overview
Zuclopenthixol is a typical antipsychotic available in multiple formulations including oral tablets, short-acting injection (Acuphase), and long-acting depot injection. It is primarily used in European and other international markets for schizophrenia and other psychotic disorders, with the Acuphase formulation specifically designed for rapid control of acute psychotic episodes.
Primary Clinical Applications
Zuclopenthixol is indicated for schizophrenia and other psychotic disorders. The Acuphase formulation is specifically indicated for initial treatment of acute psychosis and exacerbations of chronic psychosis where rapid control is essential. The depot formulation is used for maintenance therapy in patients with chronic psychotic disorders.
Mechanism and Clinical Profile
Zuclopenthixol blocks dopamine D1 and D2 receptors, providing antipsychotic effects typical of first-generation antipsychotics. It also has some activity at serotonin, histamine, and alpha-adrenergic receptors. The Acuphase formulation uses a special oil vehicle that provides sustained release over 2-3 days for rapid but prolonged action.
Formulation Advantages
The availability of three formulations (oral, short-acting injection, depot) allows for flexible treatment approaches from acute intervention to long-term maintenance. The Acuphase formulation is unique in providing rapid onset with sustained action, bridging the gap between immediate intervention and long-term depot therapy.
Prescribing Information
Dosing & Administration
Oral (Acute Treatment):
- Initial: 20-30 mg daily in divided doses
- Range: 20-60 mg daily
- Maximum: 150 mg daily for severe cases
Oral (Maintenance):
- Range: 10-50 mg daily
- Divide into 2-3 doses
Clopixol Acuphase (Short-acting IM):
- Dose: 50-150 mg IM
- Duration: Effects last 2-3 days
- Maximum: 400 mg per course, 4 injections total
- Repeat: May repeat after 2-3 days if needed
Clopixol Depot (Long-acting IM):
- Initial: 200-400 mg IM every 2-4 weeks
- Maintenance: 200-600 mg every 2-4 weeks
- Maximum: 600 mg every 2 weeks
Administration:
- Oral: Take with food to reduce GI upset
- IM injections: Deep gluteal injection, alternate injection sites
Indications
- Treatment of schizophrenia and other psychotic disorders
- Acuphase: Initial treatment of acute psychosis, exacerbations of chronic psychosis
- Depot: Maintenance treatment of chronic psychotic disorders
Contraindications
- Hypersensitivity to zuclopenthixol or thioxanthenes
- Circulatory collapse, CNS depression, comatose states
- Phaeochromocytoma
- Prolactin-dependent tumors
Warnings & Precautions
- Extrapyramidal symptoms: High incidence with typical antipsychotics
- Tardive dyskinesia: Risk increases with duration of treatment
- Neuroleptic malignant syndrome: Rare but potentially fatal
- QT prolongation: Monitor ECG in patients with cardiac risk factors
- Hyperprolactinemia: Monitor prolactin levels
- Acuphase specific: Limited to short-term use, maximum 4 injections
Drug Interactions
- CNS depressants: Enhanced sedation and respiratory depression
- Anticholinergics: Increased anticholinergic effects
- Antihypertensives: Enhanced hypotensive effects
- QT-prolonging drugs: Additive cardiac effects
- Levodopa: Antagonized by dopamine blockade
Adverse Reactions
Common:
- Extrapyramidal symptoms (dystonia, akathisia, parkinsonism)
- Sedation, dizziness, dry mouth, constipation
- Weight gain, hyperprolactinemia
Serious:
- Tardive dyskinesia, neuroleptic malignant syndrome
- QT prolongation, sudden death (rare)
Injection site (depot):
- Pain, swelling, nodule formation
Special Populations
- Elderly: Start with lower doses, monitor for extrapyramidal symptoms
- Hepatic/Renal Impairment: Use caution, may require dose reduction
- Pregnancy: Category C – use only if benefits outweigh risks
- Depot monitoring: Regular assessment for injection site reactions and s