Comparative Pharmacology
Head-to-head clinical analysis: LOXAPINE SUCCINATE versus ORAP.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LOXAPINE SUCCINATE versus ORAP.
LOXAPINE SUCCINATE vs ORAP
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Loxapine is a dibenzoxazepine antipsychotic that exerts its effects primarily through antagonism of dopamine D2 and serotonin 5-HT2A receptors. It also has moderate affinity for histamine H1, alpha-1 adrenergic, and muscarinic acetylcholine receptors.
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.
Initial: 10 mg twice daily orally; increase to 25-50 mg twice daily over 7-10 days; maximum 250 mg/day. IM: 12.5-50 mg every 4-6 hours.
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."
Terminal elimination half-life: 12–19 hours (mean 16 hours) after oral administration; steady-state reached within 3–5 days.
Terminal elimination half-life is 20–40 hours (mean 27 hours). Steady-state achieved in 4–7 days.
Renal (approximately 60% as metabolites, <1% unchanged) and fecal (approximately 40% as metabolites).
Primarily hepatic metabolism; approximately 40% excreted in urine as metabolites, 15% in feces as unchanged drug and metabolites.
Category C
Category C
Antipsychotic
Antipsychotic