Pharmacokinetics and pharmacodynamics of the muscle relaxant drug Org NC-45 and each of its hydroxy metabolites in dogs.
The pharmacodynamics and pharmacokinetics of Org NC-45 and each of its metabolites were studied in anaesthetized dogs. Only Org NC-45 and C3-deacetylated NC-45 produced neuromuscular blockade at the doses studied. The plasma half-lives varied from 3 to 15 min, and are about one third 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 1/2 h infustion was of the same order as the extracellular fluid volume. It seems that no significant entero-hepatic recirculation occurs. Thus, long term continuous infusions of Org NC-45 may be safe.
D000818:Animals; D001711:Biotransformation; D004285:Dogs; D006900:Hydroxylation; D007700:Kinetics; D009119:Muscle Contraction / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000378:metabolism* / Q000494:pharmacology; D010197:Pancuronium / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D014673:Vecuronium Bromide
D009466:Neuromuscular Blocking Agents; D014673:Vecuronium Bromide; D010197:Pancuronium