Comparative Pharmacology
Head-to-head clinical analysis: LOXAPINE SUCCINATE versus SERENTIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LOXAPINE SUCCINATE versus SERENTIL.
LOXAPINE SUCCINATE vs SERENTIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Loxapine is a dibenzoxazepine antipsychotic that exerts its effects primarily through antagonism of dopamine D2 and serotonin 5-HT2A receptors. It also has moderate affinity for histamine H1, alpha-1 adrenergic, and muscarinic acetylcholine receptors.
SERENTIL (mesoridazine) is a phenothiazine antipsychotic that blocks postsynaptic dopamine D2 receptors in the mesolimbic system, and also exhibits alpha-adrenergic blocking, anticholinergic, and antihistaminic effects. It has high affinity for D2, 5-HT2A, and alpha-1 receptors.
Initial: 10 mg twice daily orally; increase to 25-50 mg twice daily over 7-10 days; maximum 250 mg/day. IM: 12.5-50 mg every 4-6 hours.
Oral: 50–100 mg 3 times daily; maximum 400 mg/day. IM: 25 mg every 4–6 hours.
None Documented
None Documented
Terminal elimination half-life: 12–19 hours (mean 16 hours) after oral administration; steady-state reached within 3–5 days.
Terminal elimination half-life is approximately 24-30 hours in adults. Does not correlate well with duration of antipsychotic effect due to active metabolite formation.
Renal (approximately 60% as metabolites, <1% unchanged) and fecal (approximately 40% as metabolites).
Primarily renal (70-80% as conjugated and unconjugated metabolites) and fecal (15-20%). Biliary excretion contributes to enterohepatic circulation.
Category C
Category C
Antipsychotic
Antipsychotic