PAPAVERINE (Papaverinum; synonym: Cerespan, Pavabid, Vasospan etc.) — an antispasmodic; alkaloid of opium of an isoquinolinic row. Receive from opium (see) or by chemical synthesis. In medical practice it is applied in the form of a hydrochloride (Papaverini hydrochloridum; GFH, joint venture. Б). 6,7-Dimetoksi-1-(3,4-dimetoksibenzit) - isoquinoline a hydrochloride; With 20 H 21 O 4 N • HCl:
White crystal powder of slightly bitterish taste. Let's slowly dissolve in water (1:40), we will dissolve in 95% alcohol a little. pH of water solutions 3,0 — 4,5. Pier. weight 375,86.
The item has myotropic spasmolytic effect on smooth muscles (relaxes smooth muscles of intestines, biliary and urinary tract, bronchial tubes, a uterus and other smooth muscle bodies, especially at spasms). The item relaxes also smooth muscles of blood vessels (coronary, pulmonary arteries, vessels of a brain, extremities and arterioles of many vascular zones). At the same time peripheric resistance decreases. The spasmolytic effect of P. is caused by its direct impact on smooth muscle cells. The mechanism of spasmolytic action of P. is not quite clear. On modern representations, P. inhibits activity of phosphodiesterase in smooth muscle cells that leads to increase in concentration of cyclic AMF and the relaxation of smooth muscles connected with its accumulation.
On action on a cardiac muscle of P. (in high doses) it is similar to quinidine. It lowers excitability of a myocardium, oppresses endocardiac conductivity and increases the refractory period.
of page P. is well soaked up from went. - kish. path. Can collect in a liver and fatty tissue. Collapses microsomal enzymes of a liver. Apprx. 60% of the entered P. it is allocated with urine during 48 hours in the form of the conjugated phenolic metabolites, in small amounts — in not changed look.
As an antispasmodic of the Item. apply at spasms of smooth muscles of internals (ureters, bile-excreting channels, stomach, intestines, bronchial tubes). P.'s ability to relax muscles of vessels is the cornerstone of use it at a hypertension, stenocardia, an endarteritis. The good effect gives P.'s use at nek-ry forms of disturbances of cerebral circulation since it increases a blood stream in vessels of a brain, significantly without changing oxygen consumption.
Adult appoint inside in tablets on 0,04 g 3 — 4 times a day, subcutaneously on 1 — 2 ml of 2% of solution 2 — 4 times a day, intravenously (very slowly) on 1 — 2 ml of 2% r-ra2 — 4 times a day, rektalno in the form of the candles containing 0,02 g of P.
the Highest doses for adults: inside one-time 0,2 g, daily 0,6 g; under skin, intramusculary and in a vein of one-time 0,1 g, daily 0,3 g.
To P. children appoint depending on age in doses: from 6 months to 1 year of 0,005 — 0,01 g; 2 years 0,01 — 0,02 g; 3 — 4 years 0,015 — 0,03 g; 5 — 6 years 0,02 — 0,04 g; 7 — 9 years 0,03 — 0,06 g; 10 — 14 years 0,05 — 0,1 g.
Side reactions and complications at P.'s use happen seldom and are shown by nausea, anorexia, diarrhea or a lock, an indisposition, drowsiness, dizziness, a headache, perspiration, skin rashes. Cases of hypersensitivity of a liver to P. with development of jaundice, eosinophilia, changes of function are described. In such cases drug is cancelled. After intravenous administration of P. the general discomfort, rush of blood to the person, short wind, tachycardia, small falling of the ABP, oppression of c can appear. N of page.
It is necessary to observe big care at intravenous administration of P. because of danger of emergence of the atrioventricular block, ventricular ekstrasistoliya and fibrillation of ventricles. At P.'s glaucoma can cause increase in intraocular pressure.
The item reduces effect of action of a levodopa. At P.'s appointment along with morphine it is necessary to consider that the last is antagonist P. on influence on smooth muscles.
Intravenous administration of P. is contraindicated at the full atrioventricular block, rectal — at inflammatory processes in lower parts of a large intestine.
Form of release: tablets on 0,02 g and 0,04 g; ampoules on 2 ml of 2% of solution; candles on 0,02 g of P. is also a part of the combined tablets «Paphyllinum», «Khellatrinum», «Khelliverinum», «Nicoverinum», etc. Keep in the place protected from light.
Bibliography: Mashkovsky M. D. Pharmaceuticals, p.1, page 383, M., 1977; In e 1 p an i r e F. M, R about s s e 1 1 M. T. and. In about g an e r t M. G. Metabolism of papaverine, Xenobiotica, v. 8, p. 297, 1978; The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, p. 735, L., 1975; W h i p p 1 e G. H. Papaverine as an antiarrhytmic agent, Angiolo-gy, v. 28, p. 737, 1977.
S. I. Zolotukhin.