ADRENOLYTIC MEANS (Latin adrenalis — epinephral and Greek lytikos — weakening) — the connections weakening or preventing effects of adrenomimetichesky means and irritation of sympathetic nerves.
Adrenolytic Means break interaction of an adrenergic mediator (or substance, close to it) with autonomous and motor nerve terminations — adrenoceptors. They are called also adrenoblockers.
On sensitivity to adrenomimetichesky amines (see. Adrenomimetichesky means ) distinguish alpha and beta adrenoceptors [Alkvist (R. River of Ahlquist), 1948]. According to it Adrenolytic Means also divide into α-adrenolytic drugs and β-adrenolytic drugs.......... Most strongly α-adrenoceptors are excited by noradrenaline, and β-receptors — — Isadrinum (see. Adrenoreaktivnaya system ), therefore suppression of effects of these amines is the most specific test for detection of activity of Ampere-second. Treat α-adrenolytic drugs: yohimbine; derivatives of petroldioxane (piperoksan, dibozan); derivatives of imidazoline — a petrollean, Tolazolinum, phentolamine (see); the dihydrogenated derivatives of an ergot — dihydroergotamine (see), dihydroergotoxin (see); derivatives of a β-galoidoalkilamin — dibenamin, simpatolitin, phenoxybenzamine. All β-adrenolytic drugs — — dikhlorizoproteronol, Pronetalolum, propranolol (see), sotalol, INPEA, butoksamin — are the derivatives of tertiary nitrogen containing a phenolic ring and the N-isopro-saw group connected to a ring an oxyethyl or propanol chain. Action of Ampere-second. it is strictly specific. α-adrenolytic drugs block α-adrenoceptors, carrying out excitement of unstriated muscles of vessels, hl. obr. skin, mucous membranes, abdominal organs, a spleen, sphincters went. - kish. a path and a bladder, the muscle expanding a pupil, etc. Derivatives of a β-galoidoalkilamin which cause irreversible, non-competitive blockade of adrenoreaktivny systems have strong α-adrenolytic effect. Other α-adrenolytic drugs affect an adrenoceptor reversibly, competitively with adrenomimetiky; their effect lasts several hours. The most characteristic of α-adrenolytic drugs is influence on vessels. As all vasoconstrictive sympathetic (adrenergic) impulsation is transmitted through α-adrenoceptors, disturbance of this transfer leads to vasodilatation, increase in a peripheral blood-groove and falling of arterial pressure, especially if it was raised. α-adrenolytic drugs very easily suppress vasoconstrictive effects of adrenaline; for suppression of effects of noradrenaline and irritation of sympathetic nerves high doses are required considerably. α-adrenolytic drugs have no specific effect on heart, but eliminate the arrhythmias arising at administration of adrenomimetichesky amines, especially during an anesthesia chloroform, cyclopropane, Ftorotanum. It is connected by hl. obr. with elimination of pressor effect of adrenomimetichesky amines. α-adrenolytic drugs cause a ptosis, a miosis and an enophthalmos, reduce a tone of sphincters and piloerektor, suppress salivary secretion and some other the effects caused by excitement of α-adrenoceptors..........
β-adrenolytic drugs block β-adrenoceptors, the carrying-out sympathetic innervations of heart (excitement) and braking of unstriated muscles of bronchial tubes, a stomach, some vessels, a ciliary muscle, cross-striped muscles, and also regulation of a glycogenolysis and lipolysis. Some researchers [Lands (A. M. Lands), etc., 1967; R. F. Furchgott, 1970] divide β-adrenoceptors into two types: β1 (rendering hrono-and inotropic influence on heart and on a lipolysis) and β2 (the expanding vessels and bronchial tubes). The nature of influence of all β-adrenolytic drugs on an adrenoceptor — competitive, reversible; their effect can be suppressed big concentration of an adrenomimetik. Influence of β-adrenolytic drugs on heart and on the processes of exchange happening in it is the most considerable; they slow down a rhythm, extend a systole, reduce intensity of cordial reductions, a coronary blood stream and consumption by heart of oxygen, suppress automatism atrioventricular and ectopic nodes. β-adrenolytic drugs eliminate influence on heart of adrenomimetik and irritation of sympathetic nerves, suppress the arrhythmias caused by toxic doses of cardiac glycosides, adrenomimetika, especially during an anesthesia chloroform, cyclopropane and Ftorotanum, electric cardiac activation, and also arising during heart operations. The antiarrhytmic effect of β-adrenolytic drugs is caused not only their specific adrenoceptor blocking, but also hinidinopodobny action. β-adrenolytic drugs cause a spasm of bronchial tubes and eliminate bronchodilatory effect of adrenomimetik, suppress a glycogenolysis and a lipolysis by elimination of the activating influence of katekhinamin on system of adenyl cyclase. In a result in fabrics the level of a glycogen, and in blood — glucose, milk to - you and free fatty acids decreases. Derivatives of a metoksamin have especially expressed effect on processes of exchange without significant effect on adrenoceptors of other bodies (butoksamin).
At assessment of effects of Ampere-second. it is necessary to consider specific sensitivity α-and β-adrenoceptors ((((((((((receptors of a liver, a uterus, etc.). Expressiveness of action of Ampere-second. depends on an initial tone of a sympathetic nervous system: the it is higher, the effect is more considerable. On education and allocation of an adrenergic mediator of Ampere-second. do not influence; the maintenance of a mediator in the blood flowing from body can even be increased at the expense of the slowed-down inactivation of a mediator, and it is possible, and reduction of its return absorption by adrenergic nerve terminations.
α-adrenolytic drugs apply at the diseases connected with disturbances of peripheric circulation: at an endarteritis, a Raynaud's disease, a Crocq's disease, trophic ulcers; β-adrenolytic drugs — — at arrhythmias (a Bouveret's disease, premature ventricular contraction), a hypertension, a thyrotoxicosis. At a pheochromocytoma α-adrenolytic drugs apply together with β-adrenolytic drugs..........
At use of Ampere-second. by-effects are possible: hypotonia, bradycardia, heart failure, heart block, dispnoe, stridor.
Adrenolytic Means are contraindicated at the expressed heart failure, bronchial asthma, tendency to a bronchospasm, a fresh myocardial infarction, disturbance of atrioventricular conductivity.
Bibliography: Zabirov I. Sh. and Haunina R. A. Pharmakologiya of the means blocking adrenergic mediation, Frunze, 1964, bibliogr.; Haunina R. A. β-adrenoblockers, Pharm. and toksikol., t. 33, No. 1, page 112, 1970, bibliogr.; Fitzgerald J. D. Perspectives in adrenergic beta-receptor blockade, Clin. Pharmacol. Ther., v. 10, p. 292, 1969, bibliogr.; Furchgott R. F. Pharmacological characteristics of adrenergic receptors, Fed. Proc., v. 29, p. 1352, 1970; Lands A. M. a. o. Differentiation of receptor systems activated by sympalhomimetic amines, Nature (Lond.), y. 214, p. 597, 1967; New adrenergic blocking drugs, their pharmacological, biochemical and clinical actions, Ann. N. Y. Acad. Sci., v. 139, art. 3, 1967; Nickerson M. and. Hollenberg N. K. Blockade of α-adrenergic receptors, in book: Physiol. Pharmacol., ed. by W. S. Root a. F. G. Hofmann, v. 4, p. 243, N. Y. — L., 1967, bibliogr.; Pharmacological basis of therapeutics, ed. by L. S. Goodman a. L. A. Gilman, p. 549, N. Y., 1970; Symposium on beta adrenergic receptor biockade, Amer. J. Cardiol., v. 18, No. 3, 1966, bihliogr.; Symposium on propranoJol (inderal) first adrenergic beta receptor blocking agent in practice, Cardiologia (Basel), v. 49, suppl. 2, 1966.
P. A. Haunina.