Pharmacological study of a new competitive neuromuscular blocking steroid, pipecurium bromide.
2 beta, 16 beta-Bis-(4'-dimethyl-1'-piperazino)-3 alpha, 17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), a newly synthetized bisquaternary steroid, produces competitive neuromuscular blockade in chicks, rats, cats, rabbits and dogs. The onset of paralysis is rapid. Pipecurium bromide is 2-4 times as potent as pancuronium bromide. The duration of action is about twice as long as that of pancuronium bromide in equiactive doses. Neostigmine rapidly and completely antagonises the neuromuscular blockade caused by pipecurium bromide. Even one hundred times higher dose than the effective blocking dose (2-6 microgram/kg) does not influence the cardiovascular system. Higher doses (1-2 mg/kg) cause transient decrease in blood pressure, in 10-20 mg/kg doses pipecurium bromide has ganglion blocking effect. In 1 mg/kg dose pipecurium bromide does not release histamine. Many times higher doses than the effective dose administered for 20 days, do not cause any toxic damage to respirated beagle dogs. According to examinations in rats, the placentary transfer of pipecurium bromide is lower than 0.1%. According to preliminary clinical examinations pipecurium bromide is free from side effects, and elicits as well controllable muscle relaxation.
D000200:Action Potentials / Q000187:drug effects; D015113:Androstane-3,17-diol / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000633:toxicity; D000732:Androstanols / Q000494:pharmacology*; D000758:Anesthesia; D000818:Animals; D002415:Cats; D004285:Dogs; D004347:Drug Interactions; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D006636:Histamine Release / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000494:pharmacology* / Q000633:toxicity; D009474:Neurons / Q000187:drug effects; D010197:Pancuronium / Q000494:pharmacology; D017300:Pipecuronium; D010879:Piperazines / Q000494:pharmacology* / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D009435:Synaptic Transmission / Q000187:drug effects
D000732:Androstanols; D009466:Neuromuscular Blocking Agents; D010879:Piperazines; D017300:Pipecuronium; D015113:Androstane-3,17-diol; D010197:Pancuronium