GANGLIOBLOKIRUYUSHCHY MEANS (synonym: ganglioblokator, ganliolitik, gangliolytic means, ganglioplegic means) — the medicinal substances oppressing interneural transfer of excitement in vegetative gangliya. Of page block N-holinoretseptivnye of structure sympathetic and parasympathetic ganglions, a carotid ball and marrow of adrenal glands.
G.'s studying by the village began since 1889 when J. Langley in experiences on an upper cervical ganglion showed that nicotine blocks momentum transfer with pre-on postganglionic fibers. In applied medicine nicotine did not find application because of high toxicity. Tetraethylammonium was the first G. the page applied in clinic, then other, more effective G. of page appeared.
On a chemical structure distinguish the following groups G.
of page I. Quaternary ammonium compounds:
1) monoonium — tetraethylammonium, Quateronum (see);
III. Secondary amino: mekamin, Nanophynum (see), isoprene.
Treats group of monoonium compounds arfonad, at to-rogo function of the cationic center carries out positively charged sulfur atom.
On the mechanism of action the pages listed to G. belong to not depolarizing substances. Ganglioblokiruyushchy action is shown by decrease in the ABP, increase in intensity of a blood-groove in peripheral vessels (e.g., in the lower extremities), oppression of gastric secretion, braking of motility went. - kish. path, oppression of some interoceptive reflexes etc. Expressiveness ganglioblokiruyushchy) effect is in direct dependence on an initial tone of the relevant centers. So, e.g., at destruction of vasomotor centers in G.'s experiment of page do not cause falling of the ABP and, on the contrary, at a high tone of a sympathetic innervation this effect is especially well-marked.
Of page, applied in clinic, shall block selectively vegetative a ganglion, without breaking function of other parts of the nervous system; shall not possess muskarino-, atropino-and kurarepodobny activity, and also influence release of a histamine; their action shall proceed without phase of excitement. Along with high performance and the determined duration of action of G. of page shall keep activity at enteral and parenteral administration, to be whenever possible low-toxic, to possess a broad spectrum of activity, not to cause serious side effects.
Two groups G. of page are of the greatest interest: the first — the substances intended for prolonged use (at an idiopathic hypertensia, a peptic ulcer, an obliterating endarteritis, etc.); the second — quickly acting, intended for the managed hypotension.
Substances of the first group shall have high activity at different ways of introduction, the big duration of action, a hypotoxicity and not to cause serious side effects. It is desirable that accustoming to G. of page developed whenever possible slowly or did not arise at all. Partially bi-quarternary ammonium salts meet these requirements (petrolhexonium, Pentaminum, Dicolinum, etc.). They have rather high activity and the expressed selectivity of action, but duration of the effect caused by them is small (2 — 6 hours). In went. - kish. a path they are soaked up badly and not completely therefore it is reasonable to enter them parenterally. Secondary and basic nitriles are most acceptable for prolonged use (Pyrilenum, Temechinum, dimekamin, mekamin). They are well soaked up in went. - kish. a path, have high activity and considerable duration of action (8 — 12 hours and more), but, unlike quaternary ammonium salts, get through a blood-brain barrier that can be the reason of their negative influence on functions of c. N of page (there can be mental disturbances, a tremor, etc.).
Treat the second group G. of page gigroniya and arfonad; the ganglioblokiruyushchy effect caused by them is observed within 10 — 20 min. Arfonad promotes release of a histamine and has direct myotropic effect on a vascular wall that leads to decrease in a tone of vessels and falling of the ABP. Gigrony has bigger selectivity of ganglioblokiruyushchy action and by 5 — 6 times is less toxic, than arfonad. For the managed hypotension of gigroniya and arfonad it is reasonable to enter into a vein kapelno or fractionally. After the termination of administration of these substances ABP quickly reaches initial level.
Of page is applied at various diseases connected with disturbance of nervous control when reduction of receipt to bodies of nervous impulses can give desirable therapeutic effect, including at spasms of peripheral vessels (obliterating endarteritis), at an early stage of an idiopathic hypertensia (in the absence of organic changes in cardiovascular system), at hypertensive crises, kauzalgiya, a peptic ulcer of a stomach, some forms of bronchial asthma, etc. In surgery of a gangliolitika use for the managed hypotension at heart, lungs operations and vessels. Decrease in the ABP and reduction of bleeding from vessels of a surgery field facilitate carrying out such operations as thyroidectomies, a mastectomy, etc. Besides, G. the village at operative measures to a certain extent warns a possibility of negative reflex influences on heart, vessels and other internals. In neurosurgery the hypotensive effect of G. of page is used for treatment and the prevention of wet brain.
The side effects observed at G.'s use by the village are connected by hl. obr. with oppression vegetative gangliyev and sometimes with disturbance of neuromuscular transmission. The faint, an orthostatic collapse can result from excessive hypotension. For the prevention of development of a collapse it is recommended that before introduction of a ganglioblokator and within 2 — 2,5 hours after its introduction patients were in a prone position. Quite often at G.'s use by the village oppression of motility is observed went. - kish. a path, the possibility of paralytic Ilheus is not excluded. Besides, there can be a mydriasis, disturbance of accommodation, a dysarthtia, a dysphagy, a delay of an urination. Such phenomena as the general weakness, dizziness, increase of pulse, dryness in a mouth, expansion of pupils, an injection of vessels of scleras, take place usually independently.
At G.'s overdose by the village for elimination of the phenomena of poisoning inhalation of oxygen, artificial ventilation of the lungs, introduction of analeptics, and also the prozerin who is the antagonist G. of page is recommended. For increase in the ABP it is necessary to use adrenomimetichesky means (adrenaline, noradrenaline, ephedrine, a phenylephine hydrochloride). The substances exciting m-holinoretseptory (e.g., Carbacholinum), are recommended at disturbance of accommodation, expansion of pupils, and also for stimulation of motility went. - kish. path.
Are contraindicated to of page at hypotension, the expressed atherosclerosis, insufficiency of coronary circulation, at glaucoma, damages of kidneys and a liver, organic lesions of a myocardium, degenerative changes in c. N of page.
Bibliography: Denisenko of P. P. Gangliolitiki, L., 1959; New kurarepodobny and Ganglioblokiruyushchy means, under the editorship of D. A. Harkevich, M., 1970; X and r-kevich D. A. Ganglionic means, M., 1962.
D. A. Harkevich.