PHARMACOLOGY OF ETHYL-1 (4-AMINOPHENETHYL)-4??? PHENYLISONIPECOTATE, ANILERIDINE, A NEW POTENT SYNTHETIC ANALGESIC

Abstract

Ethyl-1-(4-aminophenethyl)-4-phenylisonipecotate dihydrochloride, anileridine dihydrochloride, is a potent analgesic with high oral activity and relatively mild side reactions. In animals the compound approaches the analgesic potency of morphine and is ten to twelve times more potent than meperidine. In dogs it is equally effective when given orally or subcutaneously. It has a prompt onset of action (twenty to thirty minutes), and a long duration of analgesia (five to six hours). Unlike meperidine, anileridine is a good antitussive agent against experimental cough in animals. In addition, it has mild anticholinergic and antihistaminic properties which are similar to those or meperidine. Anileridine does not produce vomiting or signs of nausea; on the contrary, it successfully antagonizes the emetic effects of apomorphine and morphine in dogs. The side reactions of the drug, such as general depression and sedation, depression of respiration and lowering of blood pressure, are considerably milder than those produced by morphine and somewhat milder than those of meperidine. Unlike morphine and similar to meperidine, the compound does not produce constipation in animals. Studies of the toxicological properties of anileridine show that it is well tolerated by mice, rats, rabbits, cats and dogs either in single doses or on repeated administration.