The Fate of Pancuronium Bromide in Man

Ágoston, S.; Vermeer, G. A.; Kersten, U.; Meijer, Dirk K. F.

doi:10.1111/j.1399-6576.1973.tb00839.x

Cited by 97 publications

(21 citation statements)

References 16 publications

(11 reference statements)

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“…Pharmacokinetic studies with pancuronium in surgical patients have also indicated that this agent shows pronounced muIticompartment behaviour (Agoston et al, 1973;Buzello, 1975;Gibaldi et al, 1971;Mcleod et ai., 1976;Somogyi et al, 1976). Agoston and associates (1973) noted the presence of a terminal elimination phase (t1/2 = 108 to 147 minutes), together with 2 residual phases, when plasma concentration data for pancuronium was plotted against time.…”

Section: Pancuroniummentioning

confidence: 97%

“…The biliary elimination of pancuronium accounts for about 6 % of the dose as intact drug (Agoston et al, 1973;Buzello, 1975). Metabolism, presumably hepatic, has also been shown to occur.…”

Section: Elimination (Excretion and Metabolism)mentioning

confidence: 99%

“…Cohen (1963b), however, found that extraction of dtubocurarine had to be achieved as a preliminary step if this general method was to be used for quantitation of the drug in biological fluids and tissues. Further progress was made by Kersten et al (1973) who used the above rose bengal procedure to develop a method for the determination of pancuronium in plasma, bile and urine. Moreover, this method did not require prior extraction of the relaxant from the fluid sample.…”

mentioning

confidence: 99%

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Clinical Pharmacokinetics of the Non-depolarising Muscle Relaxants

Ramzan

Somogyi

Walker

et al. 1981

Clinical Pharmacokinetics

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Muscle relaxants are of great benefit to the anaesthetist as adjuncts to anaesthesia. These drugs are used to facilitate endotracheal intubation and to reduce muscle tone during surgery, and may also find application in assisting ventilator care in the intensive care situation. The pharmacological effect of the relaxants may be readily assessed by the anaesthetist by means of a variety of techniques to quantify muscular activity in response to electrical stimulation. A number of factors may modify the effects of the muscle relaxants including anaesthetic agents, hypothermia, patient age and disease status and a variety of drugs. The disposition kinetics of the muscle relaxants have been well characterised although information on protein binding and placental transfer is somewhat scanty. A common characteristic of their pharmacokinetics is multicompartmental behaviour. Clearance of the relaxants ranges from total elimination by the kidneys (gallamine) to substantial hepatic clearance (fazadinium), and thus their clearance may be adversely affected by renal or hepatic disease. Dosage regimens have been designed using knowledge of the disposition kinetics of the relaxants to provide for continuous adequate relaxation during prolonged surgical procedures. With the use of sophisticated pharmacokinetic and pharmacodynamic models good relationships have been demonstrated between plasma concentrations of the relaxants throughout the entire range of relaxant response.

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Section: Pancuroniummentioning

confidence: 97%

“…The biliary elimination of pancuronium accounts for about 6 % of the dose as intact drug (Agoston et al, 1973;Buzello, 1975). Metabolism, presumably hepatic, has also been shown to occur.…”

Section: Elimination (Excretion and Metabolism)mentioning

confidence: 99%

mentioning

confidence: 99%

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Clinical Pharmacokinetics of the Non-depolarising Muscle Relaxants

Ramzan

Somogyi

Walker

et al. 1981

Clinical Pharmacokinetics

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“…Vecuronium and pancuronium are both steroidal substances, with vecuronium being the monoquaternary homologue of pancuronium (Savage et al 1980). Both muscle relaxants are taken up by the liver and metabolized to hydroxy-derivatives (Agoston et al 1973;Booij et al 1981). Atracurium, on the other hand, has a different chemical structure which is derived from the benzylisoquinolinium molecule.…”

Section: Discussionmentioning

confidence: 99%

Inhibition of Hepatic Microsomal Drug Metabolism by Atracurium Administration in the Rat

Böhrer

Schmidt

Bach

et al. 1993

Pharmacology & Toxicology

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The muscle relaxant atracurium is known to undergo extrahepatic degradation via Hofmann elimination and ester hydrolysis. The purpose of the present study was to evaluate the effects of atracurium on hepatic P450-dependent enzyme activities. Thirty-two male Sprague-Dawley rats were anaesthetized, mechanically ventilated, and randomly allocated to one of four study groups: group 1 received saline, group 2 atracurium, group 3 vecuronium, and group 4 pancuronium intravenously for a period of 3 hr. Equipotent doses of the muscle relaxants were applied; the doses had been obtained in a pilot study using evoked electromyography. At the end of the study period, the livers were removed and analyzed. All three muscle relaxants may lead to inhibition of hepatic drug metabolism. Atracurium influences hepatic P450, although it is predominantly degraded in extrahepatic tissues. Further studies are needed to evaluate the contribution of the major metabolite laudanosine to this inhibitory action.

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“…I n addition, other factors, such as species differences, are also likely to be involved. Biliary excretion of pancuronium was reported to be unimportant in the rat both in uivo ) and in uitro (MEIJER & WEITERINC 1970), but appreciable in man (AGOSTON et al 1973b).…”

Section: Discussionmentioning

confidence: 99%

The Relationship between Disposition and Duration of Action of a Congeneric Series of Steroidal Neuromuscular Blocking Agents

Ágoston

Crul

Kersten

et al. 1977

Acta Anaesthesiol Scand

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The renal and hepatic elimination and biotransformation, as well as the relation between disposition and duration of action of pancuronium and two of its analogues, dacuronium and ORG.6368, have been investigated in the cat. In pharmacokinetic studies, appreciable amounts of the latter two compounds were found in the urine, bile and liver 8 h after their intravenous administration. Various proportions of the injected dose of the respective drugs were metabolized. In another series of experiments it was shown that the early hepatic uptake (during the first 3 min after the injection) of ORG.6368 was significantly greater than that of dacuronium and pancuronium. The intensity and duration of action of the neuromuscular blocking effect of the three compounds were studied after intravenous and "close" intraarterial injection. On the basis of these pharmacokinetic and neuromuscular studies, it was concluded that the short duration of action of ORG.6368 is due primarily to its early hepatic uptake. The possibility cannot be excluded, however, that differences in the kinetics of the drug action of ORG.6368 and the other two compounds also contributed significantly to the differences seen in the duration of action of these compounds.

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The Fate of Pancuronium Bromide in Man

Cited by 97 publications

References 16 publications

Clinical Pharmacokinetics of the Non-depolarising Muscle Relaxants

Clinical Pharmacokinetics of the Non-depolarising Muscle Relaxants

Inhibition of Hepatic Microsomal Drug Metabolism by Atracurium Administration in the Rat

The Relationship between Disposition and Duration of Action of a Congeneric Series of Steroidal Neuromuscular Blocking Agents

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