Comparative Pharmacology
Head-to-head clinical analysis: INAPSINE versus LOXITANE IM.
Head-to-head clinical analysis: INAPSINE versus LOXITANE IM.
INAPSINE vs LOXITANE IM
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Butyrophenone antipsychotic; antagonizes dopamine D2 receptors in the CNS, also exhibits alpha-adrenergic blocking activity.
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.
IM: 2.5-10 mg every 3-4 hours as needed; IV: 2.5-10 mg slow IV push (over 2-3 minutes), repeat every 30-60 minutes as needed; maximum total dose 20 mg.
Adults: 12.5-50 mg IM every 4-6 hours as needed, not to exceed 150 mg/day.
None Documented
None Documented
Terminal elimination half-life is 10-22 hours (mean 14.5 hours) in adults; may be prolonged in elderly or patients with hepatic impairment.
Terminal elimination half-life: 8-12 hours. Clinically, steady-state reached in 2-3 days; dosing interval based on q6-12h.
Primarily renal (50-70% as unchanged drug and metabolites); biliary/fecal excretion accounts for approximately 20-30%.
Primarily renal: 70% as metabolites; biliary/fecal: 30% as metabolites and unchanged drug.
Category C
Category C
Antipsychotic
Antipsychotic