Zotepine

Initially, 25 mg bid, increased gradually. Max: 75 mg bid.

Initially, 25 mg bid, increased gradually. Max: 75 mg bid.

Zotepine May be taken with or without food.

Severe CNS depression. Personal or family history of epilepsy. Acute gout, history of nephrolithiasis. Patients with preexisting QT prolongation. Treatment of behaviour problems in elderly with dementia. Lactation.

Hepatic and renal impairment, elderly. Angina pectoris due to coronary artery disease, CV diseases e.g. severe hypertension, history of gout or hyperuricaemia, benign prostatic hyperplasia, urinary retention, angle-closure glaucoma, paralytic ileus, Parkinson's disease, tumours of the adrenal medulla e.g. phaeochromocytoma or neuroblastoma. May impair ability to drive or operate machinery. Avoid abrupt withdrawal. Monitor ECG in patients at risk of developing arrhythmias before starting treatment. Correct any electrolytes imbalance before treatment commencement and continue ECG and electrolytes monitoring during treatment, especially at each dose increase. Wkly monitoring of liver function for at least the 1st 3 mth of therapy in hepatic impairment. Pregnancy.

Headache, asthenia, hypotension, tachycardia, elevated LFT, increased prolactin levels, wt gain, constipation, agitation, anxiety, dizziness, insomnia, somnolence, sweating, blurring of vision. Extrapyramidal symptoms and tardive dyskinesia with prolonged treatment. GI disturbances, blood dyscrasias, photosensitisation.
Potentially Fatal: Neuroleptic malignant syndrome.

Increased risk of arrhythmias with drugs that prolong QT interval or cause hypokalaemia. Increased zotepine concentration with fluoxetine, diazepam. Increased CNS depresssion with alcohol, CNS depressants. Additive antimuscarinic effects with antimuscarinics. Additive hypotensive effects with antihypertensives and some anaesthetic drugs.
Potentially Fatal: Increased risk of seizures with high dose of antipsychotic drugs.

Description:
Mechanism of Action: Zotepine is an atypical antipsychotic that is an antagonist at central dopamine (D₁ and D₂) receptors. It also binds to serotonin, adrenergic (α₁), and histamine (H₁) receptors, and inhibits noradrenaline reuptake.
Pharmacokinetics:
Absorption: Well absorbed from GI tract. Peak plasma concentrations: 2-3 hr.
Distribution: Protein-binding of zotepine and norzotepine: 97%. Distributed into breast milk.
Metabolism: Extensive first-pass metabolism to equipotent metabolite norzotepine and inactive metabolites. Mainly metabolised by CYP1A2 and CYP3A4.
Excretion: Excreted mainly in urine and faeces as inactive metabolites. Elimination half-life: 14 hr.

Antipsychotics

N05AX11 - zotepine ; Belongs to the class of other antipsychotics.