ISSN:
1432-1041
Schlagwort(e):
neuromuscular blockade
;
fazadinium
;
pharmacokinetics
;
pharmacodynamics
;
predictive model
;
receptor occupation
Quelle:
Springer Online Journal Archives 1860-2000
Thema:
Chemie und Pharmazie
,
Medizin
Notizen:
Summary 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 simulations performed, the pharmacodynamic parameters determined: KB-apparent value of equilibrium constant of fazadinium — receptors exchange (mean ± SEM) 0.404+0.045 µmol/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 in simulating dose/effect relationships of non-depolarizing neuromuscular blocking agents are discussed and illustrated.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1007/BF00610063
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