Drug intelligence / Profile preview

meperidine + promethazine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intramuscular, Intravenous, Oral
01

Overview

Meperidine + promethazine is a fixed-dose combination drug product, most notably marketed under the brand name **Mepergan**. It consists of meperidine hydrochloride, a synthetic phenylpiperidine-derivative opioid agonist, and promethazine hydrochloride, a phenothiazine derivative with potent antihistaminic and sedative properties. Meperidine provides analgesia primarily through its action as an agonist at the mu-opioid receptor. Promethazine acts as a competitive H1 receptor antagonist and also exhibits anticholinergic and antiemetic effects, which help to potentiate the sedative effects of the opioid and mitigate opioid-induced nausea. The combination was historically indicated for the management of moderate to severe pain and as a preanesthetic medication to provide both analgesia and sedation. While the parenteral injection form received FDA approval, it is no longer actively marketed in the United States, and the oral capsule formulation was withdrawn after being found to lack substantial evidence of effectiveness.

Brand names
MeperganMepergan Fortis
Other names
meperidine hydrochloride + promethazine hydrochloride
02

Targets

mAChR (Muscarinic acetylcholine receptors)HRH1 (Histamine H1 Receptor)MOR (Mu opioid receptor)DRD2 (Dopamine D2 Receptor)

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