Comparative Pharmacology
Head-to-head clinical analysis: SEROQUEL XR versus ZIPRASIDONE MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: SEROQUEL XR versus ZIPRASIDONE MESYLATE.
SEROQUEL XR vs ZIPRASIDONE MESYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Ziprasidone mesylate is an atypical antipsychotic with high affinity for serotonin 5-HT2A and dopamine D2 receptors. It also antagonizes 5-HT1D, 5-HT2C, and alpha1-adrenergic receptors, and inhibits serotonin and norepinephrine reuptake.
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.
20 mg intramuscularly (IM) as needed, not to exceed 40 mg/day; oral: 20 mg twice daily with food, titrated up to 80 mg twice daily. Maximum: 160 mg/day oral.
None Documented
None Documented
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.
Terminal elimination half-life is approximately 2.2 hours (range 1.4–3.6 h) for the mesylate salt; clinical context: requires twice-daily dosing.
Primarily hepatic; 70-73% excreted in urine as metabolites (mostly inactive), 20-24% in feces. Less than 1% excreted unchanged in urine.
Approximately 20% renal, 80% fecal/biliary. Unchanged drug accounts for <1% of renal excretion.
Category C
Category A/B
Atypical Antipsychotic
Atypical Antipsychotic