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ClozapineAka: Clozaril
- Class
- Neuroleptic
- Dibenzodiazepine Antipsychotic
- Indications
- Not first line
- Agranulocytosis has high mortality
- Higher risk of Diabetes Mellitus
- Refractory Schizophrenia
- Suicidal behavior in Schizophrenia
- Psychosis in the elderly (not FDA approved)
- Bipolar Disorder (not FDA approved)
- Dosing
- Adults
- Initial: 12.5 mg PO qd or bid
- Titrate slowly upwards in increments of 25-50 mg/day
- Target dosing: 300-450 mg/day
- Maximum dose: 900 mg/day
- Elderly
- Initial: 6.5 PO qd
- Titrate slowly upwards in increments of 25 mg/day
- Maximum dose: 450 mg/day
- Cost
- Even generic costs >$250 per month
- Adverse Effects
- Anticholinergic Symptoms
- Agranulocytosis
- Hypotension (alpha-Adrenergic Receptor blockade)
- Tachycardia
- Hyperthermia
- Hyperglycemia including development of Diabetes
- Seizures
- Sialorrhea
- Weight gain
- Sedation
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| Definition (MSH) | A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent. |
| Definition (CSP) | tricyclic dibenzodiazepine, classified as an atypical antipsychotic agent; binds several types of central nervous system receptors, and displays a unique pharmacological profile; it is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype, and also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity; agranulocytosis is a major adverse effect associated with administration of this agent. |
| Definition (NCI) | A synthetic dibenzo-diazepine derivative, atypical antipsychotic Clozapine blocks several neurotransmitter receptors in the brain (dopamine type 4, serotonin type 2, norepinephrine, acetylcholine, and histamine receptors). Unlike traditional antipsychotic agents, it weakly blocks dopamine type 2 receptors. It relieves schizophrenic symptoms (hallucinations, delusions, dementia). (NCI04) |
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Clozapine, CLOZAPINE PREPARATION |
| Spanish | clozapina |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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