[Pharmacokinetics and pharmacodynamics of vecuronium in children]. / Pharmacocinétique et pharmacodynamique du vécuronium chez l'enfant.

Pharmacodynamics of vecuronium have been studied in children 1 to 10 years old. Doses from 0.015 to 0.1 mg/kg were given and the effects measured mechanically and by electromyography. For 0.1 mg/kg the pharmacokinetics were established. A smaller distribution volume and higher plasma clearance in children as compared to adults have been found, while the dose-effect ratio is the same. The action of vecuronium is shorter in children than in adults.

Potentiation of pancuronium induced neuromuscular blockade by calcium channel blockers in vitro.

The calcium channel blockers verapamil, methoxyverapamil, diltiazem, and nisoldipine have been tested for interactions with the nondepolarizing muscle relaxant pancuronium bromide by using the indirectly stimulated in vitro preparation of the rat hemidiaphragm. Dose response curves of each calcium channel blocker, pancuronium bromide, and combinations of both were determined. Each of the four calcium channel blocking drugs showed agonistic interaction in potentiating pancuronium induced neuromuscular blockade.

[Interaction of the calcium antagonists nifedipine and nisoldipine with the nondepolarizing muscle relaxant vecuronium bromide in an vivo rat preparation]. / Zur Wechselwirkung der Ca-Antagonisten Nifedipin und Nisoldipin mit dem nichtdepolarisierenden Muskelrelaxans Vecuroniumbromid im "in vivo" Rattenpräparat.

The interaction of two orally administered Ca-channel blockers, the dihydropyridines nisoldipine and nifedipine, with the non-depolarizing muscle relaxant, vecuronium bromide, was tested in the indirectly stimulated tibialis anterior muscle of anesthetized and ventilated Sprague-Dawley rats. In both the nisoldipine and the nifedipine group, depression of twitch tension and duration of vecuronium-induced neuromuscular blockade was potentiated when compared with a control group. The possible clinical relevance of these findings is discussed.

Lipid solubility of pancuronium and vecuronium determined by n-octanol/water partitioning.

We have measured the n-octanol/water distribution coefficients at 37 degrees C of two steroidal myoneural blockers (pancuronium and vecuronium) and of their 3-hydroxy metabolites over a pH range from 1.5 to 11. Pancuronium was found not to be lipid soluble. The mean distribution coefficient of 3-hydroxy vecuronium at pH = 7.4 was 0 and that of vecuronium 0.12 (SD 0.1). Distribution coefficients of the parent drug showed a slightly greater lipid solubility than the metabolite (11.37 (2.91) and 9.53 (3.44), respectively (mean t0.05 x SE)). Because of its lipid solubility, vecuronium may penetrate into lipid structures.

Porcine model for studying the passage of non-depolarizing neuromuscular blockers through the blood-brain barrier.

A method has been developed for blood-brain barrier disruption to provide reproducible access to the cerebrospinal fluid of the cerebello-medullary cistern. The technique was used successfully to investigate transfer of pancuronium to the cerebral CSF compartment in pigs. After osmotic disruption of the blood-brain barrier, pancuronium concentrations increased significantly in the cerebrospinal fluid.