Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Histamine release from the basophil leucocytes of patients with apparently non-immune, anaphylactiod reactions to neuromuscular blockers ( NMB ) has been studied in vitro. Substantial release was obtained in the majority of patients with clinical reactions, with little or no release in normal subjects. The chemical specificity and selectivity varied in individual patients: each individual reacting to one agent or a particular combination of NMB drugs. The test was of considerable diagnostic and predictive value. We studied some of the characteristics of the histamine release process and the effect of certain modulators. The findings strongly suggest a non-cytotoxic secretory process requiring the presence of two quaternary ammonium groups as suggested by the rarity of release with tubocurarine; inhibition of succinyldicholine (suxamethonium)-induced histamine release by serum cholinesterase treatment, acetylcholine and tubocurarine; and the bell-shaped dose-response curve, particularly with suxamethonium. Histamine release by all NMB was completely inhibited in calcium-free medium, and markedly potentiated by deuterium oxide, a microtubule stabilizer. Both tachyphylaxis (by prior exposure to the specific agent in absence of calcium), and cross-tachyphylaxis with anti-IgE were elicited.
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PMID:Characteristics of basophil histamine release by neuromuscular blocking drugs in patients with anaphylactoid reactions. 620 65

Sugammadex is the first selective relaxant binding agent which was originally designed to reverse the steroidal NMB drug rocuronium. The results of recent studies demonstrate that sugammadex is effective for reversal of rocuronium and vecuronium-induced neuromuscular block without apparent side-effects. This is in contrast to the currently available cholinesterase inhibitors used to reverse neuromuscular block and which are even ineffective against profound neuromuscular block and have a number of undesirable side-effects. Sugammadex-rocuronium complexes are highly hydrophilic and it has been demonstrated that sugammadex is excreted in a rapid and dose-dependent manner in urine, resulting in a complete elimination from the body. The ability of sugammadex to reverse rocuronium and vecuronium-induced neuromuscular block may have major implications for routine anesthetic practice. Once sugammadex becomes commercially available, anesthesiologists will be capable of maintaining the desired depth of neuromuscular block at any time, thereby assuring optimal surgical conditions. The mechanism by which sugammadex encapsulates rocuronium and vecuronium appears to be superior to currently used neuromuscular block reversal strategies in terms of speed, efficacy and side effects. In this article, clinical studies of sugammadex are discussed.
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PMID:Neuromuscular transmission: new concepts and agents. 1927 37