Antitussive properties of butorphanol.
Butorphanol (levo-N-cyclobutylmethyl-3, 14-dihydroxy morphinan), a potent analgetic agent of the narcotic antagonist type with a low abuse potential in laboratory animals, was evaluated for antitussive activity in unanesthetized guinea-pigs and dogs. Subcutaneously, it was over 100 times more active than codeine, dextromethorphan and dl-pentazocine and about 20 times more active than morphine in the guinea-pig, while in the dog it was 100, 10 and 4 times more active than codeine, dl-pentazocine and morphine, respectively. Orally, butorphanol was 15-20 times more active than either codeine or dextromethrophan in both species. Naloxone reversed the antitussive effects of butorphanol, codeine, morphine and dl-pentazocine while those of dextromethorphan were not antagonized. The antitussive effect of butorphanol and morphine lasted about 4 hr and both compounds were longer acting than codeine. Butorphanol was also shown to be as effective against cough of pathological origin as against experimentally induced cough in the dog.
D000818:Animals; D000996:Antitussive Agents; D001991:Bronchitis / Q000188:drug therapy; D003371:Cough / Q000188:drug therapy / Q000503:physiopathology; D003503:Cyclobutanes / Q000009:adverse effects / Q000627:therapeutic use; D004285:Dogs; D004558:Electric Stimulation; D006168:Guinea Pigs; D008297:Male; D009019:Morphinans / Q000009:adverse effects / Q000627:therapeutic use*; D009270:Naloxone / Q000627:therapeutic use; D013997:Time Factors; D014136:Tracheitis / Q000188:drug therapy
D000996:Antitussive Agents; D003503:Cyclobutanes; D009019:Morphinans; D009270:Naloxone