Meptazinol. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy.
Meptazinol is a new opioid-type analgesic with mixed agonist/antagonist properties. It may be given orally, intravenously or intramuscularly. In studies in patients with moderate to severe pain of various aetiologies, usually following surgery or in obstetrics, the characteristics of analgesia with meptazinol were comparable to those seen with equianalgesic doses of pentazocine, pethidine or a combination of dextropropoxyphene and paracetamol. Preoperative use and use as a component of anaesthesia require further investigation before conclusions may be drawn on its effectiveness in these areas. Onset of action, recorded in a few studies, was faster than that with the other analgesics but duration was shorter than that of morphine, buprenorphine and pentazocine. Only a small number of patients with chronic pain have received long term therapy with meptazinol; in such patients there was no need for increased doses as treatment progressed. Respiratory depression has only been observed in patients receiving meptazinol as a premedication or while undergoing anaesthesia. Similarly any haemodynamic changes have been limited to preoperative patients or patients undergoing anaesthesia. Like other agonist/antagonist analgesic drugs, the abuse potential of meptazinol seems relatively low, but only wider clinical use for longer periods can establish this with certainty. The most commonly reported side effects have been gastrointestinal in nature, and although the incidence of central nervous system side effects has been relatively low, drowsiness and dizziness have caused occasional problems. Thus, meptazinol is a relatively potent but safe addition to the analgesics available for treatment of the patient with moderate to severe pain.
D000818:Animals; D001381:Azepines / Q000494:pharmacology*; D002986:Clinical Trials as Topic; D004347:Drug Interactions; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D007408:Intestinal Absorption; D007700:Kinetics; D008621:Meptazinol / Q000008:administration & dosage / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D009292:Narcotic Antagonists; D011229:Preanesthetic Medication; D011957:Receptors, Opioid / Q000187:drug effects; D012119:Respiration / Q000187:drug effects; D019966:Substance-Related Disorders; D014018:Tissue Distribution
D001381:Azepines; D009292:Narcotic Antagonists; D011957:Receptors, Opioid; D008621:Meptazinol