ATSETILHOLIN (Acetylcholinum).

     Acetylcholine to biogenic amines, substances formed in the body. For use as a medicinal substance and pharmacological isslelovany that are synthetic compounds through in the form of chloride or salt.

     Acetylcholine is monoammonievym quarternary compounds. This is a superficial chemical substance that the body with the specific enzyme cholinesterase (acetylcholinesterase) easily destroyed with the formation of acetic acid and choline.

     Obrazuschiysya in the body (endogenous) acetylcholine plays an important role in the life : he has been involved in the transfer of neural excitation in the central nervous system, vegetative nodes, after parasimpaticheskih and motor nerves.

     Acetylcholine is a chemical transmitter (mediator) nervous excitation; End of nerve fibers, for which he served as mediator called holinergicheskimi and receptors interacting with him, called holinoretseptorami. Holinoretseptor (on the rationale for emennoy p p p ubezhnoy those glossary, "holinotsepto p") is a complex protein macromolecule (nukleoproteidom) localized on the outside postsinapticheskoy membranes. It holinoretseptor postganglionarnyh holinergicheskih nerves (heart, smooth muscle, glands) known as m-holinoretseptory (muskarinochuvstvitelnye), and located in ganglionarnyh synapses and somatic nervnomyshechnyh synapses as n-holinoretseptory (nikotinochuvstvitelnnye) (Anichkov SV). Such divisions connected with the reaction from interaction with these biochemical acetylcholine system : muskarinopodobnyh in the first case and nikotinopodobnyh-second (see Antiholinergicheskie funds); M - and n-holinoretseptory are also in different divisions of CNS.

     Current data muskarinochuvstvitelnye receptors are divided into normal, and M2- M3- receptors, which are differently distributed in the body and varied on the physiological significance (see Atropine, Pirentsepin).

     Acetylcholine has not strictly distinguishing between holinoretseptorov variety. In some degree it is at m and n-holinoretseptory and sub m holinoretseptorov.

     Peripheral muskarinopodobnoe of acetylcholine in a slowing down of heartbeat, increased peripheral blood vessels and lower blood pressure, strengthen the peristalsis of stomach and intestines, reducing bronchial muscles, uterus, pancreas and bladder, enhancing digestive secretions, bronchitis, and the port sleznyh glands, narrowing the pupil ( excessive). Miotichesky effects associated with the increased reduction in the circular muscle iris, which innerviruetsya postganglionarnymi holinergicheskimi glazodvigatelnogo nerve fibers (n. oculomotorius). At the same time, reducing the ciliated muscle relaxation tsinnovoy links ciliated belt comes causes accommodation.

     Narrowing missed due to the action of acetylcholine, usually accompanied by a reduction in inner pressure. This effect is partly due to the fact that maybe narrowing and flattening iris growing shlemmov channel (venous sin sklery) and fontanovy space (prosgranstva raduzhno- corneal angle), which provides the best drain fluid from domestic media eye. It remains possible, however, that lowering the inner pressure involved, and other mechanisms. With the ability to reduce inner pressure of the substance, acting like acetylcholine (holinomimetiki, anticholinesterase drugs) are widely used to treat glaucoma [Note that the introduction of these drugs in the bag konyuktivalny they imbibed in the blood and providing rezorbtivnoe act could cause characteristic for these drugs side effects. It should also be noted that long (in years) of mioticheskih substances can sometimes lead to the development of resistant (irreversible) mioza, education back petehy and other complications, as long as the application miotikov anticholinesterase drugs may contribute to the development of cataracts.

     Peripheral nikotinopodobnoe deysvie acetylcholine due to his involvement in the transfer of nerve impulses to preganglionarnyh fibers at postganglionarnye in vegetative nodes, as well as with the motor nerves in the poperechnopolosatuyu musculature. In small doses, it is a physiological transmitter nervous excitement in high doses can cause lasting depolarization of synapses and block the transfer of excitation.

     Acetylcholine also has an important role as mediator CNS. He is involved in the transfer of impulses across the brain, with the help of small and big-brake synaptic transmission. Changes in the exchange of acetylcholine can lead to brain dysfunction. Some tsentralnodeystvuyuschie antagonists acetylcholine (see Amizil) are psychotropic drugs (see also Atropine). Overdosing acetylcholine antagonists may cause disruptions higher nervous activity (to gallyutsinogenny effects, etc.).

     For use in medical practice and for pilot studies published atsetilholin- chloride (Acetylcholini chloridum).

     Synonyms : Acetylchlolinum chloratum, Acecoline, citocholine, Miochol and others.

     Clear crystals or a white crystalline mass. Rasplyvaetsya in air. The easily soluble in water and alcohol.

     As drug atsetilholin- chloride is widely used. When ingestion acetylcholine ineffective, as it quickly hydrolyses. When parenteral provides a fast, sharp, but short effect. Like other quaternary compounds, acetylcholine poorly crosses the blood-brain barrier and have no significant impact on the central nervous system.

     Sometimes used as acetylcholine sosudorasshiryayuschim funds in perifercheskih vascular spasm (endarteriit, peremezhayuschayasya limp, nutritional disorder in the tree, etc.), with retinal artery spasm. In rare cases impose acetylcholine in atony bowel and bladder.

     Acetylcholine is also sometimes used to facilitate X-ray diagnosis ahalazii oesophagus.

     The agent appointed under the skin and intramuscular injection dose (for adults) 0.05, or 0.1 g. injections if necessary repeat 2 to 3 times a day. When injections, be sure not to move the needle in vein.

     Intravenous introduction is not allowed because of the possibility of a sharp decrease in blood pressure and heart stoppage.

     Higher doses under the skin and intramuscularly to adults : single 0.1 g daily 0.3 g.

     Acetylcholine is contraindicated in bronchial asthma, strokes, atherosclerosis, organic heart disease, epilepsy.

     When using acetylcholine should keep in mind that it is narrowing venechnyh vascular heart.

     In overdose may occur sharp fall in blood pressure with aetiology and violations of heart rhythm, then profuzny, coma, increased peristalsis of the bowel and other phenomena. In these cases should be immediately put in veins under the skin or 1 ml of 0.1% solution of atropine (if needed again) or another holinolitichesky product (see Metatsin).

     Product : The capacity of 5 ml ampoules containing 0.1 and 0.2 g dry matter. Diluted dissolve immediately before use. Reveal the vials and syringes give it the required number (2 to 5 ml), sterile water for injection.

     When boiling and extended storage solutions decompose.

     Storage : List B. In potted ampoules.

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