Pharmacokinetics and Pharmacodynamics of Bw B1090u in Healthy Surgical Patients Receiving N2o/O2isoflurane Anesthesia

deBros, F.; Basta, S. J.; Ali, Hassan H.; Margin, W.; Welch, R. M.; Beecher, Henry K.

doi:10.1097/00000542-198709001-00609

Cited by 9 publications

(3 citation statements)

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“…The pharmacokinetics of atracurium (Vandenbrom et al 1990;Ward & Weatherley 1986), vecuronium (Bencini et al 1986a), pipecuronium (Caldwell et al 1989), doxacurium (Dresner et al 1990) and rocuronium (Wierda et al 1991 a) have been reported. There is limited information on the pharmacokinetics of mivacurium (De Bros et al 1987). …”

Section: Standard Nondepolarising Neuromuscular Blocking Agentsmentioning

confidence: 99%

“…The maximum rate of in vitro mivacurium hydrolysis is approximately 90% that of succinylcholine. Human pharmacokinetics of mivacurium have been reported only in an abstract (De Bros et al 1987) in 5 healthy patients. The data indicate a V d of 200 ml/kg and CL of 54.4 ml/kg/min, resulting in a t' 12!3 of 17 min, which is approximately 8 times that of atracurium.…”

Section: Mivacuriummentioning

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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Section: Standard Nondepolarising Neuromuscular Blocking Agentsmentioning

confidence: 99%

Section: Mivacuriummentioning

confidence: 99%

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

Ágoston

Vandenbrom

Wierda

1992

Clinical Pharmacokinetics

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“…Mivacurium has a plasma clearance about 10 times greater and a shorter elimination half-life (TiB) than atracurium [3]. This is believed to be due to a rapid breakdown by plasma cholinesterase [2] and explains previous reports of a markedly increased duration of action of mivacurium from prolonged TiB in patients with abnormal cholinesterase activities [5, 61.…”

Section: Discussionmentioning

confidence: 99%

Discrepancy of recovery times related to potency between atracurium and mivacurium simultaneously administered in isolated forearms

Kim

Hwang

et al. 1995

Anaesthesia

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SummaryRecovery from potent non-depolarising muscle relaxants is slower than from the less potent agents. However, recovery from mivacurium, which is more potent than atracurium, is faster than from atracuriurn following systemic administration. In an attempt to conjrm this discrepancy we compared recovery times following simultaneous administration of equipotent doses of atracurium and mivacurium into the isolated forearms of human volunteers (n = 10). This method enabled us to study the interaction of muscle relaxants with receptors at the neuromuscular junction separated from the effects of plasma drug concentration. In these experiments, the recovery times from maximum block to 50% recovery of control twitch height were significantly longer with rnivacurium than with atracurium (mean 25.2(SD 4.7) versus 22.6(3.1) min, p < 0.01). We found that the evidence that mivacurium has a slower recovery than the less potent atracurium may be true using the bilateral isolated forearm technique and that the discrepancy might be due to a difference in the pharmacokinetic variables of the two drugs. Key wordsNeuromuscular relaxants; atracurium, mivacurium. Pharmacokinetics; recovery.Previous studies have shown that speed of recovery from neuromuscular blockade is fast with low potency nondepolarising muscle relaxants and slow with those with a high potency [ 11. However, following systemic bolus administration of equipotent doses the recovery time of mivacurium is faster than that of atracurium in spite of being three times more potent [2]. This discrepancy has been attributed to the difference in their metabolism. Mivacurium undergoes rapid hydrolysis by plasma cholinesterase whereas atracurium is metabolised at a slower rate by the Hofmann reaction and ester hydrolysis [2, 31. The comparison of recovery times is influenced by their different plasma concentration. This study was carried out in the isolated forearm in order to ascertain what correlation exists between the recovery time and potency of the two drugs following simultaneously administered equipotent doses. The isolated forearm technique allows separation of the effect at the neuromuscular junction from changes secondary to the plasma concentration of drug [4]. MethodsApproval from the ethics committee of Soon Chun Hyang University Hospital was obtained for this study. We investigated the spontaneous recovery of a mivacurium-and atracurium-induced neuromuscular block following simultaneous administration in the isolated forearm of ten volunteers. All subjects were conscious healthy adults who were not receiving any medication which might have influenced neuromuscular transmission. A vein on the dorsum of each hand was cannulated and forearm pneumatic tourniquets were placed on each forearm. The 3M surface electrodes (Red Dot, Ag/AgCl) were applied over the ulnar nerve at the wrists and supramaximal transcutaneous stimulation from a Grass S88 two-channel nerve stimulator using a 0.2 ms square wave pattern at 0.2 Hz were applied.The twitch response of the thumb a...

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Anesthesia for Patients Undergoing Renal Transplantation

Sear¹,

Dyar²

2008

Kidney Transplantation

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Pharmacokinetics and Pharmacodynamics of Bw B1090u in Healthy Surgical Patients Receiving N2o/O2isoflurane Anesthesia

Cited by 9 publications

References 0 publications

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

Clinical Pharmacokinetics of Neuromuscular Blocking Drugs

Discrepancy of recovery times related to potency between atracurium and mivacurium simultaneously administered in isolated forearms

Anesthesia for Patients Undergoing Renal Transplantation

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