© Cambridge University Press 2011. Generic Name: meperidine, pithidine, pethanol.Trade Name: Demerol™.Class of Drug: opioid analgesic (Schedule II).Manufacturers: Abbott Laboratories, Hospital Products Division, Abbott Park, IL 60064; Sanofi-Aventis U.S. LLC, 55 Corporate Drive, Bridgewater, NJ 08807.Chemical Structure: see Figure 17.1.Chemical Name: ethyl 1-methyl-4-phenylpiperidine-4-carboxylate; C15H21NO2.Description:Meperidine is a synthetic phenylpiperidine-based opioid analgesic, with structural similarities to fentanyl and sufentanil. It was first synthesized in 1939 as an anticholinergic agent and subsequently on routine screening its analgesic effect was demonstrated. Meperidine’s analgesic activity is primarily mediated by binding and activating mu opioid receptors and secondarily via activation of alpha 2 adrenergic and delta opioid receptors. In clinically relevant concentrations, meperidine is a potent agonist at the α2B adrenoceptor.Major and minor sites of action: Sodium channel blocker Meperidine reversibly blocks voltage-gated Na+ currents with a half-maximum inhibiting concentration (IC50) of 112 µM. Clinically, meperidine shows a dose-dependent blockade of both the sensory and motor fibers of the ulnar nerve after infiltration. Two percent meperidine blocks both sensory and motor activity at the hypothenar muscle. Intrathecal doses of meperidine 50 mg can provide short-duration spinal anesthesia.
- The Essence of Analgesia and Analgesics
Start / End Page
International Standard Book Number 13 (ISBN-13)
Digital Object Identifier (DOI)