Comparative Pharmacology
Head-to-head clinical analysis: ADASUVE versus PERMITIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ADASUVE versus PERMITIL.
ADASUVE vs PERMITIL
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.
Antagonist at dopamine D2 receptors, also blocks alpha-1 adrenergic, histaminergic, and muscarinic receptors.
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.
2.5-10 mg orally every 8-12 hours; maximum 40 mg/day. For severe psychosis: initial 10 mg IM, then 5-10 mg IM every 6-8 hours; maximum 30 mg/day IM.
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: 20-30 hours; clinically, steady-state achieved in 5-7 days; prolonged in elderly and hepatic impairment
Primarily renal (30-40% as unchanged drug and metabolites; ~50% as loxapine metabolites), with minor biliary/fecal elimination (<10%).
Renal: <1% unchanged; Hepatic: extensively metabolized, metabolites excreted in urine (50-60%) and feces (30-40%)
Category C
Category C
Antipsychotic
Antipsychotic