British Journal of Anaesthesia, 1980, Vol. 52, No. suppl_1 11S-19S
© 1980 The Board of Management and Trustees of the British Journal of Anaesthesia
research-article |
Pharmacology of Org NC 45 Compared with Other Nondepolarizing Neuromuscular Blocking Drugs
Department of Physiology and Pharmacology, University of Strathclyde Glasgow G1 1XW
Departments of Clinical Pharmacology and Anesthesiology, State University of Groningen Groningen, The Netherlands
Institute of Anesthesiology, Catholic University of Nijmegen Nijmegen, The Netherlands
Department of Anesthesiology, Montefiore Hospital and Medical Center and Albert Einstein College of Medicine Bronx, N.Y. 10467, U.S.A.
From results of pharmacological tests on the neuromuscular and autonomic blocking actions of a series of pancuronium analogues, Org NC 45, the C16 monoquateruary analogue of pancuronium, was selected for detailed study. Org NC 45 has a non-depolarizing mechanism of action, is more rapid in onset and shorter in duration of action than pancuronium. It shows less cumulation than pancuronium or tubocurarine, and is easily antagonized by anticholinesterases and aminopyridines. Org NC 45 exhibits a low propensity to release histamine. Its ability to inhibit cholinesterases is not likely to be important at neuromuscular blocking doses. Org NC 45 possesses negligible ganglion-blocking activity and there is a wide margin between neuromuscular and vagal blocking doses. Thus cardiovascular side-effects are unlikely to occur with the use of Org NC 45. It will hydrolyse mainly to its 3-dash;hydroxy analogue which, like Org NC 45, possesses a wide margin between neuromuscular and vagal blocking doses. Org NC 45 has a high selectivity for the neuromuscular junction and represents a potentially useful addition to the armamentarium of clinically useful muscle relaxants.
* Present address: Department of Anesthesiology, Center for the Health Sciences, University of California at Los Angeles, Los Angeles, Ca 90024, U.S.A.