Pharmacokinetics and Pharmacodynamics of Aminosteroidal Neuromuscular Blocking Agents and Their Metabolites

  • Naosuke Sugai
  • Choku Yajima


With the refinement of analytical methods for aminostero idal neuromuscular blocking agents using gas chromatography and mass spectroscopy(1), it is becoming increasingly important to analyze the parent compound as well as their metabolites in evaluating the pharmacokinetics and pharmacodynamics of these agents. Much evidence is coming out demonstrat ing, for example, that 3-OH vecuronium is playing an important role in the neuromuscular blocking action of vecuronium when it is given for a long time or to patients with compromised organs(2,3).


Neuromuscular Blockade Bolus Administration Neuromuscular Blocking Agent Prolonged Neuromuscular Blockade Pharmacokinetic Simulation 


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  1. 1).
    Furuta T, Canfell PC, Castagnoli KP, Sharma ML, Miller RD: Quantification of pancuronium, 3-desacetylpancuronium, vecuronium, 3-desacetylvecuronium,pipecuronium and 3-desacetylpipecuronium in biological fluids by capillary gas chromatography using nitrogensensitive detection. J Chromatogr 427:41–53, 1988PubMedCrossRefGoogle Scholar
  2. 2).
    Segredo V, Matthay MA, Sharma ML, Gruenke LD, Caldwell JE, Miller RD: Prolongedneuromuscular blockade after long term administration of vecuronium in two critically ill patients. Anesthesiology 72: 566–570, 1990PubMedCrossRefGoogle Scholar
  3. 3).
    Sugai N: Paralys is after long-term administration of neuromuscular blocking agents. Masui 41: 2–10, 1991Google Scholar
  4. 4).
    Sheiner LB, Stanski DR, Vozeh S, Miller RD, Ham J: Simultaneous modeling of pharmacokinetics and pharmacodynamics: application to d-tubocurarine. Clin Pharmacol Ther 3: 358–371, 1979Google Scholar
  5. 5).
    Yajima C, Sugai N, Hanaoka K, Numata K: A pharmacodynamic analysis of the onset of neuromuscular blockade by nondepolarizing muscle relaxants.-The pharmacodynamics of a large dose of vecuronium. Masui 39: 2–7, 1990PubMedGoogle Scholar
  6. 6).
    Ohta Y, Kinjo M, Ono K, Morita K, Kosaka F: Paradoxical antagonism of neuromuscular block by vecuronium metabolite. Anesthesiology 63:A357, 1985CrossRefGoogle Scholar
  7. 7).
    Segredo V, Shin Y, Sharma ML, Gruenke LD, Caldwell JE, Khuenl-Brady KS, Agoston S, Miller RD: Pharmacokinetics,neuromuscular effects and biodisposition of 3-desacetylvecuronium (Org 7268) in cats. Anesthesiology 74: 1052–1059, 1991PubMedCrossRefGoogle Scholar

Copyright information

© Springer Japan 1995

Authors and Affiliations

  • Naosuke Sugai
    • 1
  • Choku Yajima
    • 1
  1. 1.Department of AnesthesiologyUniversity of TokyoBunkyo-ku, Tokyo, 113Japan

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