Structure-pharmacokinetics relationship of series of aminosteroidal neuromuscular blocking agents in the cat

JH Proost*, JMKH Wierda, MC Houwertjes, J Roggeveld, DKF Meijer

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

9 Citations (Scopus)

Abstract

To obtain more insight in the relationship between physicochemical properties of neuromuscular blocking agents (NMBAs) and their pharmacokinetic characteristics, a series of 12 aminosteroidal NMBAs, supplemented with data on five related NMBAs from the literature, was investigated in anaesthetized cats. After i.v. bolus injection, plasma concentration decreased very rapidly, showing a biphasic pattern, with half-lives ranging from 0.4 to 1.4 min, and from 3 to 10 min, respectively. Clearance was in the range from 24 to 58 ml . min(-1) . kg(-1). Compounds containing an acetyl-ester group at position 3 were partly metabolized to the 3-OH derivative. The urinary excretion of the parent drug and metabolites amounted to

Original languageEnglish
Pages (from-to)861-869
Number of pages9
JournalJournal of Pharmacology and Experimental Therapeutics
Volume292
Issue number3
Publication statusPublished - Mar-2000

Keywords

  • ORGANIC CATIONS
  • VECURONIUM BROMIDE
  • DRUGS
  • DISPOSITION
  • GLYCOPROTEIN
  • ROCURONIUM
  • TRANSPORT
  • BINDING
  • TIME
  • ACID

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