PYRILENUM (Pirilenum; synonym: Pempidini Tosylas, Pempidine Tosylate; GFH, joint venture. B) — ganglioblokiruyushchy means. 1, 2, 2, 6, 6 — Penta-methyl-piperidine para-toluene sulphonate; With 10 H 21 N-C 7 H 8 O 3 S:
Almost inodorous crystal powder, white or white with creamy shade. Let's easily dissolve in water and alcohol, we will difficult dissolve in acetone, it is almost insoluble on air. It is not hygroscopic; pier. weight (weight) 327,49; t ° pl 156 — 160 °. Abroad similar drug in the form of tartrate is produced under the names Pempidintartrat, Rivon, Synapleg, Tenormal, etc.
P. oppresses transfer of nervous impulses, is preferential in sympathetic and parasympathetic vegetative ganglions. Blocks also N-holinoretseptory in c. N of page. By stabilization of a postsynaptic membrane in cholinergic synapses of P. prevents influence of acetylcholine which is released from presynaptic nerves on holinoretseptor. Thanks to blockade sympathetic gangliyev P. causes vasodilatation, lowers peripheric resistance and raises a regional blood stream, lowers the ABP. At the same time P. expands venous vessels, promoting deposition in them of blood, lowers venous return and cordial emission. Oppression of parasympathetic ganglions is followed by increase of a cordial rhythm, a mydriasis, paralysis of accommodation, decrease in secretion, a tone and motility went. - kish. path, relaxation of smooth muscles of other internals, decrease in secretion of sweat glands. Expressiveness of the listed effects considerably varies depending on specific features of an organism and stage of a disease. Existence in P.'s structure of a tertiary nitrogen atom causes easy absorbability it from went. - kish. path. Duration of ganglioblokiruyushchy effect of P. apprx. the 8th hour. Drug gets through hematoencephalic and placental barriers, does not kumulirut.
The main indications to P.'s use spasms of peripheral vessels, a hypertension, hypertensive encephalopathy and a retinopathy, toxicosis of pregnancy, a peptic ulcer of a stomach and duodenum, spastic enteritis, a spastic colitis, hepatic, renal, intestinal gripes serve.
Item. appoint inside the adult on 0,0025 — 0,005 g usually 2 — 3 times a day. Course of treatment of 2 — 6 weeks; repeated courses are conducted through 2 — 3 yaed.
The highest doses for adults inside: one-time 0,01 g, daily 0,03 g.
At P.'s use there are locks and a meteorism, to-rye pass at co-administration of the corresponding diet and purgatives. The wedge, a picture of acute poisoning of P. does not differ from that at use of other ganglioblokiruyushchy means and is characterized by falling of the ABP, tachycardia, a mydriasis, a xeroderma and mucous membranes. Treatment comes down to purpose of antikholinesterazny means (Galantaminum, a prozerin), and also Carbacholinum. For increase in the ABP appoint noradrenaline and other adrenomimetik. Adrenomimetiki and m-holino-mimetiki at P.'s poisonings should appoint with care because «pharmacological denervation» of P. and other ganglioblokator is followed by sensitization adreno-and m-holinoretseptorov to agonists.
Item. it is contraindicated at organic lesions of c. N of page and a myocardium, severe forms of atherosclerosis, in acute stages of thromboses, at glaucoma, diseases of a liver and kidneys, an atony of a stomach, intestines and a bladder, a hypertrophy of a prostate.
Form of release: tablets on 0,005 g. Keep in well corked container.
See also Ganglioblokiruyushchy means .
Bibliography: See bibliogr, to St. Ganglioblokiruyuishche of means .