Clozapine
- OralClozapineClopine, Clozaril5-HT2A and D4 receptor blocker, with weak D2 receptor antagonism
Used for treatment-resistant schizophrenia
Causes myocarditis / myopathy, agranulocytosis
Mechanism of Action
- Seems to cause transient antagonism of D2 receptors, as well as serotonin 5-HT2A antagonism.
Pharmacology
- Less extrapyramidal adverse effects and less hyperprolactinaemia than first generation antipsychotics.
Clinical Use
- Indications
- Psychosis - schizophrenia, and related disorders
- Acute mania
- Maintenance therapy for bipolar I disorder (low-dose)
- Adverse Effects
- Drowsiness
- Postural hypotension
- Prolonged QTc
- Dyslipidaemia
- Weight gain
- Anticholinergic - dry mouth, blurred vision, constipation, urinary retention, delirium
- Extrapyramidal - dystonia, akathisia, parkinsonism, tardive dyskinesia
- Hyperprolactinaemia - gynaecomastia, galactorrhoea, infertility, sexual dysfunction