The rate and Extent of absorption of oral Meptazinol 200 mg on healthy volunteer

Authors

• Ahmed adel Alaa- Eldin, Mohamed Ibrahim and Mohamed Fahmy Department of Pharmacology & Toxicology, College of Pharmaceutical Sciences and Drug Manufacturing , Misr University for Science and Technology (MUST), 6 October City, Giza Egypt

Abstract

Meptazinol is a centrally acting analgesic belonging to the hexahydro-azepine series, which has demonstrated mixed agonist and antagonist activity at opioid receptors.Receptor binding studies have shown that although meptazinol displays only a low affinity for µ and k opioid receptor sites, it has a some what higher affinity for the subpopulation of µ sites. These binding sites also displays a high affinity for the endogenous opioid peptides, and are thought to be responsible for, among other things, analgesia, but not for the mediation of respiratory depression. A component of its analgesic action is also attributable, in mice at least, to an effect on central cholinergic transmission. In this respect it differs from all conventional analgesic drugs which have been examined (1).Based on this information this drug requires no blocking of opioid receptor during the bioequivalence study. But to achieve the highest degree of safety, close monitoring will be performed to detect the occurrence of any side effect, As well as Anarchole 50mg tablets (Naltrexone, the opioid blocker) will be available at the emergency drugs store to treat any opioid side effect.