Comparative Pharmacology
Head-to-head clinical analysis: ARIPIPRAZOLE versus SAPHRIS.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ARIPIPRAZOLE versus SAPHRIS.
ARIPIPRAZOLE vs SAPHRIS
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.
Asenapine is an atypical antipsychotic with high affinity for serotonin 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors; dopamine D2, D3, and D4 receptors; and alpha2-adrenergic receptors. It also has moderate affinity for histamine H1 and alpha1-adrenergic receptors, and low affinity for muscarinic M1 receptors.
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.
5 mg sublingually twice daily, may increase to 10 mg twice daily based on tolerability and efficacy.
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 30-40 hours, supporting once-daily dosing.
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.
After oral administration, approximately 50% of the dose is excreted in urine (mostly as metabolites, <1% unchanged) and 40% in feces (mostly as metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic