clozapine

Clozapine is an atypical (second-generation) antipsychotic medication primarily used to treat schizophrenia in patients who have not responded adequately to at least two other antipsychotics. It is also approved for reducing the risk of recurrent suicidal behavior in people with schizophrenia or schizoaffective disorder. Clozapine acts on multiple neurotransmitter receptors in the brain, including dopamine and serotonin receptors; it is a dopamine D2 receptor antagonist and a serotonin 5-HT2A receptor antagonist. Additionally, it has activity at muscarinic acetylcholine receptors (antagonist at M1/M2/M3/M5 and agonist at M4), adrenergic alpha-adrenergic receptors, histamine H1 receptor antagonism, among others. Its precise mechanism of action remains incompletely understood but involves modulation of several neurotransmitter systems implicated in psychosis. Clozapine was first synthesized in 1958 and introduced clinically in 1972 as the first atypical antipsychotic drug. It is included on the World Health Organization's List of Essential Medicines due to its unique efficacy for treatment-resistant schizophrenia[1][7]. The drug requires regular blood monitoring because of its risk for agranulocytosis (a potentially life-threatening drop in white blood cells). Other serious risks include seizures, myocarditis/cardiomyopathy, severe constipation/gastrointestinal hypomotility (which can be fatal), metabolic syndrome/weight gain/hyperglycemia, hypersalivation due to M4 agonism[1][3][7].

Brand names

ClozarilClopineZaponexApo-clozapineGen-clozapine

Other names

氯氮平