Comparative Pharmacology
Head-to-head clinical analysis: LOXITANE IM versus SERENTIL.
Head-to-head clinical analysis: LOXITANE IM versus SERENTIL.
LOXITANE IM vs SERENTIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
LOXITANE IM (loxapine) is a dibenzoxazepine antipsychotic. Its mechanism of action is not fully established but is thought to be mediated via antagonism of central dopamine D2 and serotonin 5-HT2A receptors. It has high affinity for D2, D3, D4, and 5-HT2A receptors and low affinity for D1 receptors. It also has moderate affinity for histamine H1 and alpha1-adrenergic 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.
Adults: 12.5-50 mg IM every 4-6 hours as needed, not to exceed 150 mg/day.
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: 8-12 hours. Clinically, steady-state reached in 2-3 days; dosing interval based on q6-12h.
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.
Primarily renal: 70% as metabolites; biliary/fecal: 30% as metabolites and unchanged drug.
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