Onset–potency relationship of nondepolarizing muscle relaxants: a reexamination using simulations

Bhatt, S. B.; Amann, Anton; Nigrovic, V.

doi:10.1139/y07-072

Cited by 6 publications

(5 citation statements)

References 30 publications

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“…NMBDs should bind to 70–90% or more of nAChRs to block neuromuscular function at the neuromuscular junction. If the drug potency is low, administering a large dose can lead to binding to nAChRs among a large number of molecules, which then also leads to a rapid onset of action [ 14 ].…”

Section: Factors That Affect Onset Timementioning

confidence: 99%

Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

Kim

Sung

Yang

2017

Korean J Anesthesiol

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Neuromuscular blockade plays an important role in the safe management of patient airways, surgical field improvement, and respiratory care. Rapid-sequence induction of anesthesia is indispensable to emergency surgery and obstetric anesthesia, and its purpose is to obtain a stable airway, adequate depth of anesthesia, and appropriate respiration within a short period of time without causing irritation or damage to the patient. There has been a continued search for new neuromuscular blocking drugs (NMBDs) with a rapid onset of action. Factors that affect the onset time include the potency of the NMBDs, the rate of NMBDs reaching the effect site, the onset time by dose control, metabolism and elimination of NMBDs, buffered diffusion to the effect site, nicotinic acetylcholine receptor subunit affinity, drugs that affect acetylcholine (ACh) production and release at the neuromuscular junction, drugs that inhibit plasma cholinesterase, presynaptic receptors responsible for ACh release at the neuromuscular junction, anesthetics or drugs that affect muscle contractility, site and methods for monitoring neuromuscular function, individual variability, and coexisting disease. NMBDs with rapid onset without major adverse events are expected in the next few years, and the development of lower potency NMBDs will continue. Anesthesiologists should be aware of the use of NMBDs in the management of anesthesia. The choice of NMBD and determination of the appropriate dosage to modulate neuromuscular blockade characteristics such as onset time and duration of neuromuscular blockade should be considered along with factors that affect the effects of the NMBDs. In this review, we discuss the factors that affect the onset time of NMBDs.

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Section: Factors That Affect Onset Timementioning

confidence: 99%

Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

Kim

Sung

Yang

2017

Korean J Anesthesiol

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“…When given in large doses, they bind to a large number of nicotinic acetyl-choline receptors, resulting in rapid onset of action. [ 8 – 10 ] Priming technique is believed to enhance this onset of action of NMBDs; However, it has its own disadvantages like, lung aspiration, respiratory weakness and visual disturbances. [ 11 ] So, we avoided using the priming technique.…”

Section: Discussionmentioning

confidence: 99%

Comparison of different doses of atracurium for quality of muscle relaxation during modified rapid sequence induction in emergency laparotomy: A prospective randomised double blind study

Holkunde¹,

Masur²,

Patil³

et al. 2022

Indian Journal of Anaesthesia

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Background and Aims: In emergency and non-fasting patients posted for laparotomy under general anaesthesia, rapid sequence induction (RSI) is preferred, and it is routinely done by using succinylcholine or rocuronium. Using higher doses of atracurium [i.e. 3-4 times the 95% effective dose (ED95)] can provide acceptable intubating conditions in a short time. The primary objective of our study was to compare two different higher doses of atracurium to achieve good intubating conditions for RSI without using a priming dose. The secondary objective was to compare the duration of muscle relaxation using neuromuscular monitoring and haemodynamic responses during and after intubation. Methods: Sixty patients were enroled and randomly assigned into two groups:-, group A1 (atracurium: 0.75 mg/kg) and group A2 (atracurium: 1 mg/kg). After premedication, anaesthesia was induced with propofol 2-2.5 mg/kg and atracurium injections, followed by intubation within a minute by trained anaesthesiologists. Meanwhile, intubating conditions, neuromuscular monitoring using train-of-four (TOF) measurements and post-tetanic-count and haemodynamics were recorded. Data were analysed statistically by using the Chi-square test and Student’s t-test. Results: Excellent intubation conditions (without coughing or bucking) were attained in 56.7% of cases in group A2 and in 13.3% in group A1 ( P < 0.001). Duration of muscle relaxation, measured by time until TOF is two, was more prolonged in group A2 (79.2 ± 9.2 min) than in group A1 (60.13 ± 8.7 min, P < 0.001). Conclusion: Acceptable intubating conditions can be achieved in a minute with the use of a high dose of atracurium (1 mg/kg) during RSI. Hence, atracurium can be used as an alternative drug for RSI.

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“…The physiological saline used to dilute RB may have attenuated the affinity of RB to nicotinic acetylcholine receptors, and the change in free molecules due to dilution may have delayed the onset of muscle relaxation. In addition, as the onset time of NMBD and its titer are inversely correlated [9], it is necessary to increase the dose to accelerate the onset time of NMBD if the titer is low [11]. If the RB titer was decreased by dilution with 0.9% saline, the dose of diluted RB should be increased in order to accelerate the onset time of action.…”

Section: Discussionmentioning

confidence: 99%

The effect of various dilute administration of rocuronium bromide on both vascular pain and pharmacologic onset: a randomized controlled trial

et al. 2019

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Background Rocuronium bromide (RB) is known to cause vascular pain. Although there have been a few reports that diluted administration causes less vascular pain, there have been no studies investigating diluted administration and the onset time of muscle relaxation. Therefore, we examined the influence of diluted administration of RB on the onset time of muscle relaxation and vascular pain. Methods 39 patients were randomly assigned to three groups: RB stock solution 10 mg/ml (Group 1), two-fold dilution 5 mg/ml (Group 2), or three-fold dilution 3.3 mg/ml (Group 3). After the largest vein of the forearm was secured, anesthesia was induced by propofol and 0.6 mg/kg of RB was administered. The evaluation method devised by Shevchenko et al. was used to evaluate the degree of vascular pain. The time from RB administration until the maximum blocking of T1 by TOF stimulation was measured. Results There was no significant difference in escape behaviors of vascular pain among the three groups, and the onset time of muscle relaxation was significantly slower in Group 3 than in Group 1 ( p = 0.033). Conclusion Our results suggested that it is unnecessary to dilute RB before administration if a large vein in the forearm is used. Trial registration UMINCTR Registration number UMIN000026737 . Registered 29 Mar 2017.

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Onset–potency relationship of nondepolarizing muscle relaxants: a reexamination using simulations

Cited by 6 publications

References 30 publications

Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents

Comparison of different doses of atracurium for quality of muscle relaxation during modified rapid sequence induction in emergency laparotomy: A prospective randomised double blind study

The effect of various dilute administration of rocuronium bromide on both vascular pain and pharmacologic onset: a randomized controlled trial

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