Comparative Pharmacology
Head-to-head clinical analysis: ZIPRASIDONE MESYLATE versus ZYPREXA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ZIPRASIDONE MESYLATE versus ZYPREXA.
ZIPRASIDONE MESYLATE vs ZYPREXA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Olanzapine is an atypical antipsychotic that antagonizes dopamine D2 and serotonin 5-HT2A receptors, with higher affinity for 5-HT2A than D2. It also blocks histamine H1, alpha-1 adrenergic, and muscarinic M1 receptors.
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.
5-10 mg orally once daily; may increase by 5 mg/day at intervals of at least 1 week; maximum 20 mg/day.
None Documented
None Documented
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.
Terminal elimination half-life ~30 hours (range 21–54 h) in adults, allowing once-daily dosing; steady-state reached in ~5–7 days. Half-life prolonged in elderly, females, and hepatic impairment.
Approximately 20% renal, 80% fecal/biliary. Unchanged drug accounts for <1% of renal excretion.
Primarily hepatic metabolism via CYP1A2 and CYP2D6; ~7% excreted unchanged in urine, ~57% in urine as metabolites, ~30% in feces (mostly metabolites).
Category A/B
Category C
Atypical Antipsychotic
Atypical Antipsychotic