Comparative Pharmacology
Head-to-head clinical analysis: ARIPIPRAZOLE versus CLOZARIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARIPIPRAZOLE versus CLOZARIL.
ARIPIPRAZOLE vs CLOZARIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Partial agonist at D2 and 5-HT1A receptors; antagonist at 5-HT2A receptors.
Clozapine is an atypical antipsychotic that binds to multiple receptors including dopamine D1-D5 (with greater affinity for D4), serotonin 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, histamine H1, muscarinic M1-M5, and adrenergic α1- and α2-receptors. Its therapeutic efficacy is primarily attributed to antagonism of D2 and 5-HT2A receptors. It also has weak D2 antagonism and rapid dissociation from D2 receptors, which may contribute to lower extrapyramidal side effects.
Oral: 10-15 mg once daily; initial and target dose 10-15 mg; maximum 30 mg/day. IM: 9.75 mg single dose, then 5.25-9.75 mg every 2 hours if needed; maximum 30 mg/day.
Initial 12.5 mg orally once or twice daily, titrate by 25-50 mg/day over 2 weeks to target 300-450 mg/day in divided doses; max 900 mg/day.
None Documented
None Documented
Clinical Note
moderateAripiprazole + Torasemide
"Aripiprazole may increase the hypotensive activities of Torasemide."
Clinical Note
moderateAripiprazole + Etacrynic acid
"Aripiprazole may increase the hypotensive activities of Etacrynic acid."
Clinical Note
moderateAripiprazole + Furosemide
"Aripiprazole may increase the hypotensive activities of Furosemide."
Clinical Note
moderateAripiprazole + Bumetanide
"Aripiprazole may increase the hypotensive activities of Bumetanide."
Aripiprazole has a terminal elimination half-life of approximately 75 hours in extensive CYP2D6 metabolizers and about 146 hours in poor metabolizers. The active metabolite, dehydro-aripiprazole, has a half-life of about 94 hours. This long half-life allows for once-daily dosing and gradual achievement of steady state (14 days in extensive metabolizers).
Terminal elimination half-life is approximately 8–12 hours at steady state; range 6–26 hours, increasing with dose due to saturable metabolism.
Aripiprazole is extensively metabolized primarily by the liver via CYP2D6 and CYP3A4. Approximately 25% of the dose is excreted unchanged in urine, and about 55% in feces. The major metabolite, dehydro-aripiprazole, accounts for about 40% of the AUC and is also excreted in urine and feces.
Approximately 50% excreted renally as metabolites, with less than 1% unchanged; 30% eliminated in feces via biliary excretion.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic