PHARMACOKINETICS AND PHARMACODYNAMICS OF THE MUSCLE-RELAXANT DRUG ORG NC-45 AND EACH OF ITS HYDROXY METABOLITES IN DOGS

  • 1 January 1981
    • journal article
    • research article
    • Vol. 30  (7) , 329-333
Abstract
The pharmacodynamics and pharmacokinetics of Org NC-45 (2.beta.,16.beta.-dipiperidine-5.alpha.-androstane-3.alpha.,17.beta.-diol diacetate monomethobromide) and each of its metabolites were studied in anesthetized dogs. Only Org NC-45 and C3-deacetylated NC-45 produced neuromuscular blockade at the doses studied. The plasma half-lives varied from 3-15 min and are about 1/3 of that of the structurally-related compound pancuronium. Renal excretion was of the order 5-20% and the biliary excretion 7-20% 6 h after administration of each of the 4 compounds. The apparent volume of distribution after a 1.5 h infusion was of the same order as the extracellular fluid volume. It seems that no significant entero-hepatic recirculation occurs. Long term continuous infusions of Org NC-45 may be safe.

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