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cholinesterase inhibitors

Pharmacological agents capable of inactivating cholinesterase lead to an accumulation of acetylcholine, liberated in the cholinergic nerve endings, and enhance its effect on organs and tissues. Caused by cholinesterase inhibitors (anticholinesterase agents) the effects are similar in many respects therefore effects due to nicotinic acetylcholine and substances.
Cholinesterase inhibition can have a different character. Some substances (physostigmine, galantamine, neostigmine methylsulfate, and others.) Cause a temporary, reversible inhibition of enzyme activity. Their effect is relatively short; after termination of its interaction with the enzyme activity is restored again. Other substances (Armin and other phosphorous compounds) form a stable complex with the enzyme (causing its phosphorylation), and if not use special Reaktivatory (see Dipiroksin, Alloksin, Izonitrozin etc...), The enzyme activity is not restored; the normal process of hydrolysis of acetylcholine to start again only when there will be a new cholinesterase biosynthesis. The action of these substances is so persistent, irreversible.
Nowadays different pharmacological agents are known, whose action is connected with the inhibition of various enzymatic systems of the organism (see monoamine oxidase inhibitors;. Carbonic anhydrase inhibitors, angiotensin converting enzyme inhibitors, and others.). Anticholinesterase agents are one of the groups antifermental preparations.
The common ground for use anticholinesterase drugs as medicaments is the activation process of synaptic transmission in the cholinergic nerve endings. Depending on the chemical structure and physico-chemical properties of the different drugs in this group differ.
Tertiary amines (physostigmine galantomin et al.) Penetrate through biological membranes, including the blood-brain barrier and have a pronounced effect on the CNS. Quaternary ammonium derivatives (neostigmine methylsulfate, pyridostigmine, oksazil et al.) It is difficult to penetrate the blood-brain barrier. Varies to some extent and scope of the various anticholinesterase drugs.