Inhibition of the enzymic degradation of suxamethonium and mivacurium increases the onset time of submaximal neuromuscular block
| العنوان: | Inhibition of the enzymic degradation of suxamethonium and mivacurium increases the onset time of submaximal neuromuscular block |
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| المصدر: | Anesthesiology. 89(3):707-714 |
| بيانات النشر: | LIPPINCOTT WILLIAMS & WILKINS, 1998. |
| سنة النشر: | 1998 |
| مصطلحات موضوعية: | PHARMACOKINETICS, POTENTIATION, onset of action, MUSCLE-RELAXANTS, SUCCINYLCHOLINE, PATIENT, PANCURONIUM, CARBOXYLESTERASES, time course of action, plasma clearance, SPEED, PHARMACOLOGY, neuromuscular blocking agents, ATYPICAL PLASMA CHOLINESTERASE |
| الوصف: | Background: The factors that influence the onset time of submaximal (Methods: Twenty pigs received either suxamethonium or mivacurium Dose finding (70% block) was done for each pig. The enzymic degradation of the muscle relaxant was randomly inhibited by selective inhibition of plasma cholinesterase activity by tetraisopropyl pyrophosphoramide (10 pigs) or was not inhibited (10 pigs). Plasma cholinesterase activities and the mechanomyographic muscle response after peroneal nerve stimulation (0.1 Hz) were measured.Results: Inhibition of plasma cholinesterase activity (by 93% and 89%, respectively) increased the onset time of suxamethonium from a median of 40 s (range, 20-45 s) to 131 s (range, 114-166 s; P = 0.009) and of mivacurium from a median of 52 s (range, 40-59 s) to 105 s (range, 90-125 s; P = 0.009). Inhibition of degradation decreased the effective dose of suxamethonium that resulted in 70% depression of the initial twitch height from 900 mu g/kg (range, 400-1,000 mu g/kg) to 150 mu g/kg (range, 135-150 mu g/kg) and of mivacurium from 100 mu g/kg (range, 80-150 mu g/kg) to 35 mu g/kg (range, 20-50 mu g/kg).Conclusions: Inhibition of the enzymic degradation of suxamethonium and mivacurium increases the onset time of submaximal neuromuscular block Therefore, pharmacokinetics influence the onset time of submaximal neuromuscular block. These results imply that to obtain an ultrashort onset time, muscle relaxants should be developed that not only have a low affinity for the receptor but also rapidly disappear from plasma. |
| اللغة: | English |
| تدمد: | 1528-1175 0003-3022 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=dris___01423::9eb80ff34c40e4f263d76433a4abc633Test https://research.rug.nl/en/publications/42f7d70f-543c-4130-9e6a-8057457906a4Test |
| رقم الانضمام: | edsair.dris...01423..9eb80ff34c40e4f263d76433a4abc633 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15281175 00033022 |
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