The Comparative Potency and Pharmacokinetics of Pancuronium and Its Metabolites in Anesthetized Man

Miller, Ronald D.; Ágoston, S.; Booij, L.H.D.J.; Kersten, U.; Crul, J. F.; Ham, Jay

doi:10.1097/00132586-197912000-00005

Cited by 13 publications

(19 citation statements)

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“…The pharmacokinetic properties of these 3 metabolites in patients are similar to those of pancuronium (Miller et al 1978). …”

Section: Renal and Hepatic Failurementioning

confidence: 74%

“…Approximately 20% of the injected dose appeared as the 3-deacetyl (3-0H) metabolite in the urine and bile Somogyi et al 1977b) and less than 5% was identified as 17-deacetyl (17-0H) or 3,17-deacetyl (3,17-0H) pancuronium in the urine (Buzello 1975;Somogyi et al 1977b). The 3-OH metabolite shows neuromuscular blocking activity with a potency of about 50% of that of the parent compound (Miller et al 1978). The 17-0H and 3, 17-0H derivatives are less active, having potencies of <2% of that of pan cur onium in humans.…”

Section: Renal and Hepatic Failurementioning

confidence: 99%

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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 pharmacokinetic properties of these 3 metabolites in patients are similar to those of pancuronium (Miller et al 1978). …”

Section: Renal and Hepatic Failurementioning

confidence: 74%

Section: Renal and Hepatic Failurementioning

confidence: 99%

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

Ágoston

Vandenbrom

Wierda

1992

Clinical Pharmacokinetics

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“…In contrast to the 3‐OH derivatives of other steroid type muscle relaxants, which are less potent than their 3‐acetoxy analogs (12–14), SZ1677 is two times more potent than its 3‐acetoxy analog SZ1676 in mice, rats, and guinea pigs (Table 1). SZ1823 (17‐OH derivative of SZ1677, see Fig.…”

Section: Discussionmentioning

confidence: 99%

A new short‐acting non‐depolarizing muscle relaxant (SZ1677) without cardiovascular side‐effects

Vizi

Tuba

Mahó

et al. 2003

Acta Anaesthesiol Scand

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“…7). This contrasts with pancuronium, in which the main metabolite (3-hydroxypancuronium), representing approximately 25% of an injected dose, is 50% as potent as the parent drug (36). Biliary excretion of vecuronium in animals and humans accounts for 30-50% of the injected dose (37)(38)(39)(40).…”

Section: Metabolism and Excretionmentioning

confidence: 98%

Comparison of the Pharmacology of Vecuronium and Atracurium with That of Other Currently Available Muscle Relaxants

Hilgenberg¹

1983

Anesthesia & Analgesia

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The search for new muscle relaxants is an attempt to improve on the undesirable pharmacologic properties of currently available nondepolarizing muscle relaxants. Ideally, new muscle relaxants would exhibit fewer cardiovascular hemodynamic side effects, have fewer cumulative effects, possess rapid onset of and shorter durations of action, and be less dependent on hepatic and/or renal function for metabolism and excretion. Furthermore, drug metabolites should be pharmacologically inactive. Two new nondepolarizing muscle relaxants, vecuronium (Norcuron) and atracurium (BW 33A), are examples of drugs approaching these ideal muscle-relaxant characteristics. Currently, these drugs are used clinically in Europe and are undergoing clinical trials in this country.

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The Comparative Potency and Pharmacokinetics of Pancuronium and Its Metabolites in Anesthetized Man

Cited by 13 publications

References 0 publications

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

A new short‐acting non‐depolarizing muscle relaxant (SZ1677) without cardiovascular side‐effects

Comparison of the Pharmacology of Vecuronium and Atracurium with That of Other Currently Available Muscle Relaxants

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