The Neuromuscular Blocking Effects and Pharmacokinetics of ORG 9426 and ORG 9616 in the Cat

Khuenl-Brady, Karin S.; Castagnoli, Kay; Canfell, P. Claver; Caldwell, James E.; Ágoston, S.; Miller, Ronald D.

doi:10.1097/00000542-199004000-00016

Cited by 80 publications

(39 citation statements)

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“…This is not surprising, inasmuch as both drugs are closely related chemically and eliminated primarily via the liver. Forty percent of vecuronium is eliminated in the liver in 24 h, whereas a preliminary study in cats has shown that rocuronium is eliminated unchanged, primarily via the bile (50% in 2 h) (9).…”

Section: Discussionmentioning

confidence: 98%

Pharmacokinetics and Pharmacodynamics of Rocuronium (Org 9426) in Elderly Surgical Patients

Matteo

Ornstein

Schwartz

et al. 1993

Anesthesia & Analgesia

113

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The effects of age on the pharmacokinetic and pharmacodynamic responses to rocuronium (Org 9426) were studied in 20 elderly (> 70 yr) and 20 younger control patients (< 60 yr) during N2O/O2, fentanyl anesthesia. The onset times were the same for both the elderly and younger control group, but the duration of action of rocuronium was significantly prolonged in the elderly patients. Elderly patients, when compared with the younger, also exhibited a significant decrease in plasma clearance (3.67 +/- 1.0 vs 5.03 +/- 1.5 mL.kg-1.min-1, mean +/- SD) and volume of distribution (399 +/- 122 vs 553 +/- 279 mL/kg, mean +/- SD). During the recovery phase of paralysis, no significant difference was seen in the log plasma concentration versus twitch tension response relationship between 20% and 80% paralysis in young and elderly patients receiving rocuronium. The differences in action of rocuronium between the elderly and younger groups can be fully explained by the observed differences in the distribution and elimination of rocuronium between the two groups. The decreased total body water and decreased liver mass which normally accompany aging are likely explanations for the pharmacokinetic changes found in the elderly in this study. We conclude that the action of rocuronium is prolonged in patients aged more than 70 yr because of decreased elimination of the drug.

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Section: Discussionmentioning

confidence: 98%

Pharmacokinetics and Pharmacodynamics of Rocuronium (Org 9426) in Elderly Surgical Patients

Matteo

Ornstein

Schwartz

et al. 1993

Anesthesia & Analgesia

113

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“…In cats a mean percentage of 8.7% of an injected dose of rocuronium is excreted into the urine in 6 h [15]. Rocuronium is not dependent on renal blood flow for its major route of excretion, but is taken up by the liver and excreted into the bile in high concentrations [9].…”

Section: Discussionmentioning

confidence: 99%

Reversal of rocuronium-induced neuromuscular block by sugammadex is independent of renal perfusion in anesthetized cats

et al. 2011

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“…Metabolites were absent or below the detection limit (5 ~g/L). There are no human data on biliary excretion; however, in cats (Khuenl-Brady et al 1990) 50% of the administered dose of rocuronium was recovered from the bile and only <9% from the urine within 6h after injection, indicating that CL is mainly determined by hepatobiliary excretion in this species. It is conceivable, therefore, that the hepatic clearance (CLH) of rocuronium in humans could be at least as important as that of vecuronium.…”

Section: Rocuroniummentioning

confidence: 92%

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

Ágoston

Vandenbrom

Wierda

1992

Clinical Pharmacokinetics

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Neuromuscular blocking agents provide muscle relaxation for a great variety of surgical procedures with light planes of general anaesthesia. Besides having a significant impact in the development of anaesthesia and surgery, these agents continue to play an important role as pharmacological tools in the elucidation of the physiological and pharmacological regulation of neuromuscular transmission and the morphofunctional organisation of the neuromuscular junction. In the daily practice of anaesthesia, muscle relaxants are considered to be safe drugs with predictable, straightforward pharmacological actions. However, the use of relaxants constitutes a deliberate encroachment on respiration, one of the most important physiological mechanisms. The pharmacokinetic behaviour of this class of agents is little influenced by age or anaesthetic agents; however, hepatic or renal disease may profoundly alter their excretion pattern, resulting in prolonged duration of neuromuscular blockade. Biotransformation plays an important role in the total elimination of recently introduced compounds. Consequently, knowledge of the disposition pharmacokinetics, excretion and biotransformation of this class of drugs is indispensable for their rational choice for various surgical procedures. In this review, the known pharmacokinetics of standard compounds (introduced before 1980) are briefly summarised and new information generated by the development of vecuronium, rocuronium, pipecuronium (steroidal agents) and atracurium, mivacurium, doxacurium (benzylisoquinolinium esters) is discussed in more detail.

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The Neuromuscular Blocking Effects and Pharmacokinetics of ORG 9426 and ORG 9616 in the Cat

Cited by 80 publications

References 0 publications

Pharmacokinetics and Pharmacodynamics of Rocuronium (Org 9426) in Elderly Surgical Patients

Pharmacokinetics and Pharmacodynamics of Rocuronium (Org 9426) in Elderly Surgical Patients

Reversal of rocuronium-induced neuromuscular block by sugammadex is independent of renal perfusion in anesthetized cats

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

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