Comparative Pharmacology
Head-to-head clinical analysis: ADASUVE versus INAPSINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ADASUVE versus INAPSINE.
ADASUVE vs INAPSINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Loxapine (the active ingredient in ADASUVE) is a dibenzoxazepine antipsychotic agent that acts primarily as a dopamine D2 receptor antagonist. It also exhibits affinity for serotonin 5-HT2A, 5-HT2C, and histamine H1 receptors, and to a lesser extent, alpha-adrenergic and muscarinic receptors. The exact mechanism of its antipsychotic effect is thought to involve dopamine and serotonin receptor blockade.
Butyrophenone antipsychotic; antagonizes dopamine D2 receptors in the CNS, also exhibits alpha-adrenergic blocking activity.
Inhalation: 10 mg as a single dose via oral inhalation up to a maximum of 2 doses within a 24-hour period, each dose separated by at least 2 hours. For agitation associated with schizophrenia or bipolar I disorder.
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.
None Documented
None Documented
Mean terminal half-life of loxapine is 6-8 hours; active metabolite 7-hydroxyloxapine (amoxapine) has half-life of ~30 hours. Clinically, steady state achieved within 3-5 days.
Terminal elimination half-life is 10-22 hours (mean 14.5 hours) in adults; may be prolonged in elderly or patients with hepatic impairment.
Primarily renal (30-40% as unchanged drug and metabolites; ~50% as loxapine metabolites), with minor biliary/fecal elimination (<10%).
Primarily renal (50-70% as unchanged drug and metabolites); biliary/fecal excretion accounts for approximately 20-30%.
Category C
Category C
Antipsychotic
Antipsychotic