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Clozapine

Class
  • Tricylic dibenzodiazepine atypical antipsychotic
Indications
Administration/Absorption
  • Oral
Dosage

Distribution
  • 97% protein bound
Mechanism
  • Selective monoaminergic antagonist with high affinity for:
    • serotonin Type 2 (5HT2)
    • dopamine Type 2 (D2)
  • Clozapine acts as an antagonist at other receptors, but with lower potency, explaining side effects
    • Antagonism of histamine H1 receptors may explain somnolence
    • Antagonism of adrenergic a1 receptors may explain orthostatic hypotension
  • Antipsychotic action is likely mediated through a combination of antogistic effects at:
    • D2 receptors in the mesolimbic pathway
      • Relieves positive symptoms
    • 5-HT2A receptors in the frontal cortex
      • Alleviates negative symptoms.
Excretion
  • Half-life 8 hours (range 4-12 hours)
  • Approximately 50% of the administered dose is excreted in the urine and 30% in the feces
Side effects
Interactions
  • Fluvoxamine inhibits the metabolism of clozapine leading to significantly increased blood levels of clozapine
  • Alcohol
  • Caffeine
Contraindications
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