Comparative Pharmacology
Head-to-head clinical analysis: ADASUVE versus MELLARIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ADASUVE versus MELLARIL.
ADASUVE vs MELLARIL
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.
Thioridazine is a phenothiazine antipsychotic that blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors, and also blocks alpha-adrenergic receptors, histamine H1 receptors, and muscarinic M1 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.
Typical adult dose: 10-25 mg orally 3 times daily. Maximum dose: 200 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 21-24 hours; steady-state achieved within 5-7 days
Primarily renal (30-40% as unchanged drug and metabolites; ~50% as loxapine metabolites), with minor biliary/fecal elimination (<10%).
Primarily renal (70-80% as metabolites, <1% unchanged); biliary/fecal (20-30%)
Category C
Category C
Antipsychotic
Antipsychotic