m-Anticholinergics

To m-Anticholinergics are substances that block the muscarinic receptors in the region of the endings of parasympathetic nerve fibers, resulting in dilation of the pupils, paralysis of accommodation, tachycardia, improved AV conduction, decreased tone of bronchi, bladder, weakening of intestinal motility, reduced secretion of glands (bronchial and intestinal). m-Holinoblokiruta activity possess some alkaloids (atropine, scopolamine), a number of semisynthetic and synthetic compounds. Besides alkaloids, used drugs belladonna, Datura, henbane. Extracts and tinctures of belladonna, containing alkaloids (hyoscyamine, scopolamine, etc.), used as an antispasmodic and pain relievers for diseases of the stomach, gallstones, and also by smooth muscle spasm (various types of colic), bradycardia associated with overstimulation of n.vagus. In the form of dry extract of belladonna alkaloids are part of many complex tablets: Besalol, Bellastezin. From the leaves of Datura and henbane receive oil, serve the basis for the manufacture of liniment for external use in neuralgia, myositis, and rheumatoid arthritis. The difference in the chemical structure (presence of the Quaternary or tertiary nitrogen atoms, etc.) determines not only the distinction of receptor effects, but also the penetration through the GEB (a Central effect), duration, and other properties that ultimately leads to the differentiation of indications for use. Natural alkaloids and many m-holinoliticheskie funds related to tertiary amines, well absorbed in the intestine, pass through the conjunctival membrane and other gistogematicalkie barriers and penetrate various tissues and organs after absorption from the site of injection. Quaternary ammonium compounds (metotsiniya iodide, fubrogoniya iodide, etc.) do not pass through GEB and used as a peripheral anticholinergic drugs.

In recent years, selected subtypes of m-cholinergic receptors (M1, m2, m3) and established drugs of selective action (pirenzepine, ipratropium bromide, etc.), which was used at gastrointestinal diseases and bronchial asthma.

In addition to these groups of compounds possess anticholinergic activity, also antihistamines, antipsychotic and antidepressive means, because have similar chemical structure.



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