PMID: 6134623Jan 1, 1983

Analytical model of some pharmacokinetic and pharmacodynamic properties of fazadinium in man

European Journal of Clinical Pharmacology
A A d'HollanderJ M Desmonts

Abstract

The neuromuscular blocking characteristics and plasma concentration decay of fazadinium bromide, a short acting, non-depolarizing muscular relaxant, were simultaneously observed under standardised conditions in 6 healthy, anaesthetized, adult patients. The results were analyzed by a new pharmacodynamic model, which takes into account certain relationships describing the binding of non-depolarizing neuromuscular blocking agents and the postsynaptic receptor occupation ratio. According to the simultaneous performed, the pharmacodynamic parameters determined: KB-apparent value of equilibrium constant of fazadinium--receptors exchange (mean +/- SEM) 0.404 + 0.045 mumol/l, and the value of postsynaptic occupation ratio for 50% paralysis of 0.89 +/- 0.004 were in agreement with values reported in the literature for mammalian neuromuscular junctions in vitro. The apparent validity of the pharmacodynamic model and its value is simulating dose/effect relationships of non-depolarizing neuromuscular blocking agents are discussed and illustrated.

References

Jan 1, 1978·Acta Anaesthesiologica Scandinavica·F Camu, A d'Hollander
Aug 1, 1978·British Journal of Anaesthesia·P DuvaldestinJ M Desmonts
Sep 1, 1979·The Journal of Physiology·D L Armstrong, H A Lester
Mar 1, 1978·British Journal of Anaesthesia·C A ShanksE J Triggs
Nov 1, 1978·British Journal of Anaesthesia·C J HullM J Watson
Mar 1, 1979·Clinical Pharmacology and Therapeutics·L B SheinerJ Ham
Dec 1, 1975·The American Journal of Physiology·D R Waud, B E Waud
Mar 1, 1971·Masui. The Japanese journal of anesthesiology·K Fukushima, K Miyashita
Jul 1, 1967·The Journal of Physiology·W D Paton, D R Waud
Jun 1, 1971·Anesthesiology·R L Katz
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Dec 1, 1980·British Journal of Anaesthesia·C J HullA Sibbald
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Feb 1, 1980·European Journal of Clinical Pharmacology·M I RamzanC A Shanks

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