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Anticholinergic agents that block predominantly peripheral cholinergic systems

Anticholinergic, or holinoliticheskimi means called substances that weaken, prevent or stop the interaction of acetylcholine with cholinergic receptors. Blocking the cholinergic receptors, they act in the opposite way to acetylcholine. The term "anticholinergic agents" is widely used in the literature. However, given that the destruction (lysis) of acetylcholine these substances do not cause, it is more correct to talk about "anticholinergic" or "holinoblokiruyuschih" funds.
Synthetically, substances have been obtained that can inhibit the synthesis of acetylcholine and disrupt the cholinergic transmission in the synapses of the nervous system. The most active of these substances is hemicholinium (HC-3). These compounds do not yet have practical applications. Some oppression of the formation of acetylcholine causes novocaine.
In accordance with the division of cholinergic receptors into m- and n-cholinergic receptors, cholinolytic substances are also subdivided into substances with predominant m- or n-cholinolytic action. Such a division corresponds to a rather high selectivity of the action of the substances of each of these groups. It should, however, be taken into account that to some extent, m-cholinolytic substances lower the reactivity of nicotine-sensitive, and n-cholinolytic substances - the reactivity of muscarinic-sensitive receptors.
Substances with a pronounced cholinolytic activity include atropine and related alkaloids (scopolamine, platyphylline, etc.), as well as a number of semisynthetic and synthetic compounds. Depending on the chemical structure and physico-chemical characteristics, these compounds differ not only in their predominant effect on m- and n-cholinergic receptors, but also on the ability to penetrate the blood-brain barrier, the barrier and other biological membranes, the duration of action and other properties. This together determines the indications for their differentiated use as medicines.
It should be borne in mind that quaternary ammonium compounds (metacin, atriovent, triventol, etc.) penetrate badly through the blood-brain barrier and are used as substances of peripheral cholinolytic action. At the same time, a number of anticholinergics easily penetrate the blood-brain barrier and actively bind to the central cholinergic receptors (amisyl, spasmolytin, etc.), which served as the basis for combining them into the group of "central cholinolytics", although to some extent they also exert peripheral cholinolytic act.
Blocking effect on m-holinoretseptory (with the simultaneous blocking of n-holinoretseptorov) have atropine and related alkaloids, as well as a number of synthetic cholinolytic drugs (spasmolitin, aprofen, etc.). Metacin more selectively blocks m-holinoretseptory.
In recent years, in connection with the identification of subtypes of m-cholinergic receptors (MM, etc.), pharmacological substances selectively acting on these receptor subtypes began to be sought, such newly created drugs include pirentsepin (gastrotsepin), selectively blocking M, Cholinergic receptors, and the search for drugs that selectively act on other subtypes of m-holinoretseptorov.
N-holinoliticheskie substances in accordance with the characteristics of peripheral n-holinoretseptorov are divided into two groups. Substances predominantly acting in the field of ganglionic synapses, in connection with the features of action and therapeutic use, are isolated into a special group of "ganglion-blocking substances". Substances that act primarily in the field of somatic neuromuscular synapses are isolated into the group of "curare-like substances"
Cholinolytic substances can predominantly influence central m and n-cholinergic receptors: a) substances with m-cholinolytic activity (scopolamine, amisil), acting mainly on the cholinergic receptors of the synapses of the ascending reticular formation and some other subcortical formations of the brain; B) substances with n-cholinolytic activity (spasmolitin, gangleron, etc.), acting mainly in the area of ​​synapses of the cortex and hippocampus; C) substances of mixed type of action, affecting m- and n-cholinoreactive systems (aprophen, etc.), which have a blocking effect in the area of ​​synapses of the cortex and subcortical formations of the brain.
A number of substances that have predominantly central and cholinolytic or mixed effects and have found application in the treatment of parkinsonism and other extrapyramidal system diseases have been singled out as a separate group (see Remedies for the Treatment of Parkinsonism). Some central anticholinergics have been used as tranquilizers (see Amizil).
Holinolytic properties are possessed not only by substances of the listed groups but also to some extent by some antihistamines (diphenhydramine, diprasine, etc.), local anesthetics and other means.

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Subgroup Means acting on peripheral cholinergic processes include drugs: