A Study of the Anticholenesterase and Anticurare Effects of Some Cholinesterase Inhibitors

Barrow, M.E.H.; Johnson, Jaime

doi:10.1093/bja/38.6.420

Cited by 20 publications

(6 citation statements)

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“…Testing the enzyme activity in vivo after the injection of reversible inhibitors raises the problem of using undiluted serum. This source of error was pointed out previously by Strauss and Goldstein (1943) and was re-emphasized by Barrow and Johnson (1966). The test-paper method used by Dalai and colleagues (1972) makes use of undiluted serum, but gave very poor results in our hands.…”

Section: Discussionmentioning

confidence: 64%

The Inhibition of Cholinesterases by Pancuronium

Stovner¹,

Oftedal²,

Holmboe³

1975

British Journal of Anaesthesia

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Pancuronium causes a powerful and highly selective inhibition of human serum cholinesterase in vitro. The inhibition was studied in serum from 14 individuals of both sexes (5-60 years of age) with normal reactions to suxamethonium. Pancuronium, in a concentration of 2.3 x 10(-7) M, caused a 50% inhibition of the enzymatic hydrolysis of acetylcholine, when this substrate was present in a concentration of 10 x 10(-3) M. The same I50 value was also found for a commercial preparation of human serum cholinesterase. The inhibition was reversible and competitive in type. Pancuronium inhibition of the acetylcholinesterase in human red blood cells and from the electric eel was more than one thousand times weaker. Thus pancuronium is one of the most selective inhibitors of serum cholinesterase described so far. The in vivo activity of the serum cholinesterase in four patients receiving pancuronium 0.1 mg/kg decreased, during the first 3 min, by 60-80%, from the pre-induction value. After this a slow recovery occurred with 40% depression remaining at 45 min after the injection. The tachycardia produced by pancuronium may be related to this selective inhibition of serum cholinesterase. It is suggested that relaxants which selectively inhibit serum cholinesterase also selectively block the cardiac muscarinic receptors.

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Section: Discussionmentioning

confidence: 64%

The Inhibition of Cholinesterases by Pancuronium

Stovner¹,

Oftedal²,

Holmboe³

1975

British Journal of Anaesthesia

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“…AChE is concentrated in the synaptic cleft of the NMJ and rapidly hydrolyses ACh (4000 ACh molecules second À1 ) (Soreq & Shlomo 2001), thus limiting the half-life of the neurotransmitter Reversal of neuromuscular block RS Jones et al (Barrow & Johnson 1996). Recovery of NMB depends on the ACh concentration relative to that of the relaxant drug in order to overcome the competitive neuromuscular block (Fig.…”

Section: Neuromuscular Transmission and Reversal Of Nmbmentioning

confidence: 99%

Reversal of neuromuscular block in companion animals

Jones

Auer

Mosing

2015

Veterinary Anaesthesia and Analgesia

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“…As a result, acetylcholine and neuromuscular blockers compete each other in postsynaptic field and restore neuromuscular blockade [1]. Sugammadex is the first member, which has circular modified gamma cyclodextrin including 8 glucose molecules that returning effects of neuromuscular block agents [2].…”

Section: Introductionmentioning

confidence: 99%

Effect of sugammadex and neostigmine on tracheal muscle: In vitro study

Erel¹

2018

Ann Clin Anal Med

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Aim: There are limited numbers of in vitro organ studies both neostigmine and, sugammadex. Up to date, we can reach no study in the literature comparing advantages and disadvantages of two agents in vitro. The study, we aimed to compare and demonstrate in vitro effects of neostigmine and sugammadex in rat trachea with basal and supramaximal tonus. Material and Method: A total of 24 adult male rats were divided into four groups: Group 1; Basal tonus+sugammadex, Group 2; Supramaximal contraction+sugammadex, Group 3; Basal tonus + neostigmine, Group 4; Supramaximal contraction+neostigmine.After anesthesia, trachea of each rats were removed and suspended in Krebs solution. After the vitality of the tissues was shown with acetylcholine and atropine, sugammadex was applied to group 1 and neostigmine to group 3 all in basal tonus. In other two groups, after supramaximal tonus with acetylcholine, sugammadex was applied to group 2, neostigmine to group 4. The contraction responses of each group were compared. Results: There was no significant change in comparison of the sugammadex groups (p>0.05). On the other hand, neostigmine increased tracheal tonus both in the basal tonus group (mean 25-40% ± 3.54), (p <0.05) and supramaximal tonus group (mean 15% ± 2.8) and were statistically significant (p <0.05). Discussion: In our study, neostigmine increased tracheal tone in both basal and supramaximal contractions. Neostigmine use, which may increase the risk of tracheal contractility, can be risky for surgical procedures. Therefore sugammadex may be preferred as there is no effect on tracheal tissue.

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A Study of the Anticholenesterase and Anticurare Effects of Some Cholinesterase Inhibitors

Cited by 20 publications

References 0 publications

The Inhibition of Cholinesterases by Pancuronium

The Inhibition of Cholinesterases by Pancuronium

Reversal of neuromuscular block in companion animals

Effect of sugammadex and neostigmine on tracheal muscle: In vitro study

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