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Funds affecting neuromuscular transmission
The groupThe stimulation of somatic nerves in the muscles skeletnuu by means of acetylcholine. He is presinapticescoy membrane and binds n-holinoretseptorami; Activation initiates recent set of developments leads to a reduction in muscle. Increased uterine activity can be obtained acetylcholine agonists and preparations causing accumulation mediator in the synaptic junctions - antiholinesteraznami means (see Holinomimeticalkie means).
Contrary to the muscle (see N-holinolitiki (ganglioblokatora)). The group miorelaksantov bring medicines, treatments skeletnuu musculature. To miorelaxation possible blockade of the structures in the central nervous system, braking nervous conductivity, oppression metabolism poperechno-polostah muscles, or a combination of mechanisms.
Substances in the miorelaksantov flaccid action divided into antidepoliarizatora (pahikurare) depoliarizatora (leptokurare), and "mixed". "
Curare and kurarepodobne drugs used in medicine to relax skeletal muscles, mainly in surgery. These drugs linked to ekranirutm influence on n-holinoretseptora postsinapticescoy membranes poperechno-polostah muscles.
Curare is a mixture sguschennah extracts from the South American plant species Strychnos (S. toxifera, etc.) and Chondodendron (Ch. Tomentosum, Ch. Platyphyllum, etc.); It has long been used by Aboriginal as a poison for arrows (a obezdwijivanie or animal death as a result of asphyxia due to the reductions in the respiratory muscles). Even in the last century found that caused by curare obezdwijivanie depends on the transfer of the institution from motor nerves in the muscle (Claude Bernard, EV Pelican).
In 1935 the "tubular" curare and Chondodendron tomentosum have the active ingredient, d-tubokurarin.
It turns out that similar properties have kurarepodobne synthetic compounds, some alkaloids and their derivatives.
Antidepoliarizute nedepoliarizute or muscle relaxants (pahikurare) paralyse neuromuscular transmission, reducing sensitivity n-holinoretseptorov synaptic area for acetylcholine, excluding depolarization tip plates and initiate muscle fibres. These include d-tubokurarin, diplatzin, arduan, atrakurium etc. Connections of the group are true kurarepodobnami substances. Their antagonists, antiholinesteraznae substances : cholinesterase inhibition leads to the accumulation of acetylcholine synapses, which at elevated concentrations of displaced kurarepodobne substance with n-holinoretseptorov and restores neuromuscular conductivity.
Depoliarizatora (leptokurare) rasslablaut muscles, causing, on the other hand, resistance depoliarizatia tip plates making it (like excess quantities acetylcholine) immune to the new momentum, and ultimately the violation of the institution with nerve on the muscle. Regarding the group relatively quickly gidrolizuyutza holinesterzoy and with a one-time offer short-term impact; Saying antiholinesteraznae to reinforce them. The representative of this group is ditilin.
The muscle may have mixed effect - and antidepoliarizutee depoliarizutee.
Several drugs relaxes somatic musculature of central mechanisms. Miorelaksaciu can cause anxiolitiki (see anxiety). In recent years, found compounds (midokalm, baclofen, dantrolen, tizanidin, etc.) miorelaksantny effects associated with the specific impact on the formation retikuljarnuu brain spinale mono-and polisinapticalkie though. They eliminated the highest arbitrary tone muscles without material breach motor functions. They are used in spastic conditions, neck disease, rheumatism and other diseases involving spazmom skeletal muscles (see Противоэпилептически е means). The mechanism of action of these drugs is important Gamkergicakih modulation of the brain.