British journal of anaesthesia
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Comparative Study
Comparison of the cardiovascular actions of ORG NC 45 with those produced by other non-depolarizing neuromuscular blocking agents in experimental animals.
The cardiovascular actions of 1- [(2 beta,3 alpha, 16 beta,17 beta)-3,17-bis(acetyloxy)-2-(1-piperidinyl)-androstan-16-yl]-1-methyl-piperidinium bromide (Org NC 45) are reviewed and compared with those of other non-depolarizing neuromuscular blocking drugs. Results obtained in anaesthetized cats and dogs have demonstrated that, in contrast to other neuromuscular blocking drugs, Org NC 45, even in doses 20 times greater than those required for neuromuscular block, has no effects on heart rate, arterial pressure, autonomic ganglia, adrenoceptors or baroreceptors activity. Studies in pithed rats and on guineapig atria have further shown that Org NC 45 has little effect on cardiac muscarinic receptors or on noradrenaline re-uptake mechanisms. These results suggest that Org NC 45 possesses significant advantages over presently used non-depolarizing neuromuscular blocking drugs, since its clinical use should not be associated with cardiovascular side-effects.
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Comparative Study
Pharmacology of ORG NC 45 compared with other non-depolarizing neuromuscular blocking drugs.
From results of pharmacological tests on the neuromuscular and autonomic blocking actions of a series of pancuronium analogues, Org NC 45, the C16 monoquaternary 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. ⋯ Thus cardiovascular side-effects are unlikely to occur with the use of Org NC 45. It will hydrolyse mainly to its 3-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.