Comparative Pharmacology
Head-to-head clinical analysis: ARIPIPRAZOLE versus SEROQUEL XR.
Head-to-head clinical analysis: ARIPIPRAZOLE versus SEROQUEL XR.
ARIPIPRAZOLE vs SEROQUEL XR
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.
SEROQUEL XR (quetiapine fumarate) is an atypical antipsychotic that acts as an antagonist at multiple neurotransmitter receptors: serotonin 5-HT1A and 5-HT2A, dopamine D1 and D2, histamine H1, and adrenergic α1 and α2 receptors. It also has partial agonist activity at 5-HT1A receptors. The therapeutic efficacy in schizophrenia and bipolar disorder is primarily attributed to dopamine D2 and serotonin 5-HT2A antagonism.
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: 300 mg orally once daily; may increase by 300 mg/day every 2-3 days. Target dose: 400-800 mg/day for schizophrenia; 300-600 mg/day for bipolar depression; 400-800 mg/day for acute mania. Maximum: 800 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: approximately 7 hours (range 6-9 hours) for the extended-release formulation. Clinical context: once-daily dosing achieves steady-state within 2 days.
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.
Primarily hepatic; 70-73% excreted in urine as metabolites (mostly inactive), 20-24% in feces. Less than 1% excreted unchanged in urine.
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic