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Pronunciation

KLOE-za-peen

Classifications

Therapeutic Classification: antipsychotics

Indications

BEERS REMS


Action

  • Binds to dopamine receptors in the CNS.
  • Also has anticholinergic and alpha-adrenergic blocking activity.
  • Produces fewer extrapyramidal reactions and less tardive dyskinesia than standard antipsychotics but carries high risk of hematologic abnormalities.
Therapeutic effects:
  • Diminished schizophrenic behavior.
  • Diminished suicidal behavior.

Pharmacokinetics

Absorption: Well absorbed after oral administration.

Distribution: Rapid and extensive distribution; crosses blood-brain barrier.

Protein Binding: 95%.

Metabolism/Excretion: Mostly metabolized through the liver by the CYP1A2, CYP2D6, and CYP3A4 isoenzymes; (the CYP2D6 enzyme system exhibits genetic polymorphism; 7% of population may be poor metabolizers and may have significantly clozapine concentrations and an risk of adverse effects).

Half-Life: 8–12 hr.

Time/Action Profile

(antipsychotic effect)

ROUTEONSETPEAKDURATION
POunknownwk4–12 hr



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: hypotension, tachycardia, bradycardia, CARDIAC ARREST, DEEP VEIN THROMBOSIS, HF, hypertension, MITRAL VALVE INCOMPETENCE, MYOCARDITIS, QT interval prolongation, syncope, TORSADES DE POINTES, VENTRICULAR ARRHYTHMIAS

Derm: rash, sweating

EENT: visual disturbances

Endo: hyperglycemia

GI: constipation, salivation, abdominal discomfort, dry mouth, GI ISCHEMIA/INFARCTION/NECROSIS, GI OBSTRUCTION, GI PERFORATION, HEPATOTOXICITY, nausea, ulceration, vomiting

GU: nocturnal enuresis

Hemat: AGRANULOCYTOSIS, LEUKOPENIA

Metab: hyperlipidemia, weight gain

Neuro: dizziness, sedation, extrapyramidal reactions, NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES

Resp: PULMONARY EMBOLISM

Misc: fever

Interactions

Drug-drug:

Drug-Natural Products:

Route/Dosage

Availability

(Generic available)

Assessment

Lab Test Considerations:

Toxicity and Overdose:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Clozaril, FazaClo, Versacloz

Code

NDC Code