Comparative Pharmacology
Head-to-head clinical analysis: ADASUVE versus LOXITANE IM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ADASUVE versus LOXITANE IM.
ADASUVE vs LOXITANE IM
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.
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.
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.
Adults: 12.5-50 mg IM every 4-6 hours as needed, not to exceed 150 mg/day.
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: 8-12 hours. Clinically, steady-state reached in 2-3 days; dosing interval based on q6-12h.
Primarily renal (30-40% as unchanged drug and metabolites; ~50% as loxapine metabolites), with minor biliary/fecal elimination (<10%).
Primarily renal: 70% as metabolites; biliary/fecal: 30% as metabolites and unchanged drug.
Category C
Category C
Antipsychotic
Antipsychotic