RESERPINUM (Reserpinum; synonym: Deserpine, Elserpine, Neoserfin, Rausedyl, Reserpin, Serpasil, Transerpin etc.; GFH, joint venture. A) — sympatholytic; alkaloid of Rauwolfia serpentine (Rauwolfia serpentina Benth.) this. dogbane family (Apocynaceae). Methyl ether 2 an alpha, 11-диметокси-3-(3,4,5-триметоксибензоил-окси) - yokhimban-1-carboxylic to - you; With 33 H 40 N 2 O 9 :
White or yellowish fine-crystalline powder. We will dissolve in water, 95% alcohol and ether very little; let's easily dissolve in chloroform and acetic to - those; pier. weight (weight) 608,7.
The river oppresses function of c. N of page, rendering sedative, and in high doses — antipsychotic action. Causes a condition of emotional calmness, indifference to external irritants. Under the influence of R. delay of a respiration rate, bradycardia, reduction of cordial emission, decrease in the systolic and diastolic ABP is observed.
The central and peripheral effects of R. are caused by its ability to devastate stocks of catecholamines and serotonin in c. N page, sympathetic neurons, chromaffin and enterokhromaffinny cells. The river exerts a direct impact on mechanisms of deposition of monoamines in neurons; this effect is reproduced on the isolated bodies and cuts of nervous tissue. By methods of preparative biochemistry and submicroscopy it is established that R. exhausts stocks of noradrenaline in granules of the terminations of sympathetic nerves. Significantly without breaking the return capture of monoamines, R. suppresses absorption by their synoptic vesicles at the expense of irreversible inhibition of the mechanism of active transport of monoamines through a membrane of vesicles. In this regard the monoamines synthesized in a neuroplasm and returned from a synaptic gap are not deposited in vesicles and collapse in neurons under the influence of MAO. The devastation of reserves of monoamines caused by R. is proportional to functional activity of neurons.
Exhaustion of stocks of a mediator in terminalyakh axons of sympathetic neurons is the cornerstone of inherent R. of sympatholytic action, a cut is shown by reduction of influence of a sympathetic innervation by internals. Almost important result of this action of R. is the hypotensive effect caused, first of all, by reduction of sympathetic influences on heart owing to what bradycardia develops and minute volume decreases. Disturbance of momentum transfer from sympathetic nerves to unstriated muscles of vessels is followed by decrease in the general peripheric resistance. The decrease in a tone of the vasculomotor centers caused by R. is of secondary importance. The lasting hypotensive effect under the influence of R. develops slowly (during 1 — 2 week), but after drug withdrawal long remains.
The river is well soaked up in went. - kish. a path and from places of parenteral administration, easily gets through a blood-brain barrier, it is temporarily deposited in fatty tissue. In the first days after R.'s introduction it is metabolized in a liver and allocated with urine in the form of metabolites (rezerpinovy, siringovy to - you and their methyl ethers). In 24 — 30 hours nemetabolizirovanny part P. within several days remains in fabrics, collecting hl. obr. in places of deposition of amines. Ability of synoptic vesicles to absorb monoamines is recovered only in process of formation of new vesicles.
Apply River it is preferential as an antihypertensive. At an idiopathic hypertensia it is most effective in the I—II stages of a disease. Less often R. use at local circulatory disturbances (Raynaud's disease), and also at the tachycardia and takhisistolichesky arrhythmia arising against the background of a thyrotoxicosis and late toxicoses of pregnancy. Sometimes it is applied as antipsychotic means, by hl. obr. at the mental disorders arising against the background of increase in the ABP.
In early stages of an idiopathic hypertensia of R. appoint inside, more rare subcutaneously, since a dose of 0,0001 — 0,00025 g a day and gradually increasing a daily dose to 0,0003 — 0,001 g. Increase in a daily dose higher than 0,001 g is inexpedient since is not followed by strengthening of hypotensive effect. In 2 weeks after achievement of therapeutic effect the dose is reduced. In the absence of R.'s effect combine with diuretics, antihypertensives of myotropic action. At mental diseases of R. appoint in dozakh0,001 — 0,01 g a day.
The highest doses for adults inside: one-time — 0,002 and, daily — 0,01 g.
In small doses of R. it is usually transferred well, however in some cases skin rashes, a delay of water and increase in the weight (weight) in a body, dispeptic frustration, diarrhea, dizziness, drowsiness can be observed. At prolonged use of R. development of a depression, and also the phenomena of medicinal parkinsonism is possible, to-rye are weakened at use of Cyclodolum.
River. it is contraindicated at depressions, heavy heart failure, the expressed cerebral sclerosis, a nephrosclerosis, a peptic ulcer of a stomach and duodenum.
Forms of release: powder and tablets on 0,0001 and 0,00025 g. In VNR under the name «Rausedyl» P. is issued in ampoules on 1 ml of 0,1 and 0,25% of solution. Powder is kept in well corked banks of orange glass in the cool place protected from light, by tablets — in the cool, protected from light place>
Bibliography: Komissarov I. V. Medicinal regulation of adrenergic processes, page 72, Kiev, 1976; K. S. Pharmakologiya's Rajevski of neuroleptics, page 65, M., 1976; Erina E. V. Treatment of an idiopathic hypertensia, page 66, M., 1973; The pharmacological basis of therapeutics, ed. by A. G. Gilman a. o., N. Y., 1980; Reserpine and breast cancer, Report from the Boston collaborative drug surveillance program, Lancet, v. 2, p. 669, 1974.
I. V. Komissarov.