Comparative Pharmacology
Head-to-head clinical analysis: ADASUVE versus ORAP.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ADASUVE versus ORAP.
ADASUVE vs ORAP
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.
Orap (pimozide) is a diphenylbutylpiperidine antipsychotic that selectively blocks dopamine D2 receptors in the central nervous system, with weak antagonism at alpha1-adrenergic and H1-histamine receptors. Its anti-dyskinetic effect in Tourette syndrome may also involve blockade of calcium channels.
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.
Initial: 2 mg orally twice daily; maintenance: 2-10 mg twice daily. Maximum 20 mg/day.
None Documented
None Documented
Clinical Note
moderateVorapaxar + Tranilast
"Vorapaxar may increase the anticoagulant activities of Tranilast."
Clinical Note
moderateVorapaxar + Resveratrol
"Vorapaxar may increase the anticoagulant activities of Resveratrol."
Clinical Note
moderateVorapaxar + Nimesulide
"Vorapaxar may increase the anticoagulant activities of Nimesulide."
Clinical Note
moderateVorapaxar + Epoprostenol
"Vorapaxar may increase the antiplatelet activities of Epoprostenol."
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 20–40 hours (mean 27 hours). Steady-state achieved in 4–7 days.
Primarily renal (30-40% as unchanged drug and metabolites; ~50% as loxapine metabolites), with minor biliary/fecal elimination (<10%).
Primarily hepatic metabolism; approximately 40% excreted in urine as metabolites, 15% in feces as unchanged drug and metabolites.
Category C
Category C
Antipsychotic
Antipsychotic