ANABOLIC STEROIDS — group of the steroid connections exerting the stimulating impact on synthesis of protein in an organism.
Ampere-second. are derivatives androgens (see) also possess in comparison with male sex hormone considerably the reduced androgenic and increased anabolic activity.
Ampere-second. are derivatives of three index compounds: 5α-дигидротестостерона, testosterone, 19-nortestosteron. It turned out that anabolic activity increases, and androgenic — decreases in the absence of methyl group in situation C19, and also in process of increase in unsaturation in a ring of Ampere-second. More considerable action on protein metabolism characterizes the connections having ketonic group in situation C3 and methyl in situation C7. Anabolic activity increases at the steroids etherified in situation 17, to a large extent, than at 17-alkylated. From 17 connections etherified into a state steroids with a bigger chain length of the radio radical fell more actively. They have the bigger duration of action, less expressed collateral influences are transferred by patients easier.
These patterns find reflection in chemical formulas of the most common Ampere-second in clinical practice. — methandrostenolone (see), Nandrolonum-fenplpropionata (see. Phenobolinum ), Nandrolonum-dekanoata (see. Retabolil ), etilnortestosterona and stanozolona.
Nature of pharmacological action
Influence of Ampere-second. on protein metabolism at the person it is shown in a delay of nitrogen, reduction of concentration of urea in urine, increase in content of crude protein of serum.
For assessment of anabolic action of steroid connections in an experiment and clinic as a test object use a research of dynamics of body weight, weight of separate skeletal muscles, nitrogenous balance, inclusion of marked amino acids in muscles.
The relation of anabolic and androgenic activity (a so-called anabolic index) at Ampere-second. always exceeds unit, and at the most active connections 10 — 15 equals.
According to various researches, androgenic action of Ampere-second. in comparison with Testosteroni propionas taken for 100% makes from 2 to 150% while anabolic activity of some of them reaches 400 — 500%. This change of activity of Ampere-second. it is directly connected with their chemical structure. Increase in a dose of Ampere-second. only to a certain level is followed by increase of anabolic effect. The doses exceeding this level (various for different drugs), do not cause additional digestion of nitrogen. In addition to direct anabolic effect, Ampere-second. cause also anticatabolic action in relation to drugs of a glucocorticoid row.
Strengthening synthesis of protein in the main substance of a bone tissue, Ampere-second. cause a delay of calcium, phosphorus, sulfur.
At the same time strengthening of an alkaline phosphatase is observed that demonstrates strengthening of activity of osteoblasts.
Ampere-second. in therapeutic doses, stimulating growth of bones in length, significantly do not accelerate a differentiation and ossification of a skeleton.
In therapeutic doses they do not cause considerable virilescence of women, stimulate development of a uterus, have accurate progesterono-like effect. On the other hand, at men with the phenomena of a hypogonadism of Ampere-second. promote moderate stimulation of sexual development and increase sexual feeling. Perhaps, it is about various reaction to Ampere-second. depending on a sex.
Ampere-second. have moderately expressed anti-gonadotropic activity concerning preferential luteinizing hormone. By clinical definition of excretion of gonadotrophins it is established that the dose of a steroid causing a delay of nitrogen is insufficient for antpgonadotropny effect. For receiving the last it shall be increased by 3 — 4 times.
Ampere-second. at reduced endogenous somatotropic activity are capable to increase the level of a growth hormone in blood serum of the patient.
Direct action on adrenocorticotropic function of a hypophysis and bark of adrenal glands of Ampere-second. in therapeutic doses do not render.
Ampere-second. reduce absorption of a radioiodine a thyroid gland a little, reduce concentration of the iodine connected with protein, render natural timolitichesky effect. Disturbances of carbohydrate metabolism are not caused. There are data on stimulation by anabolic steroids of β-cells of a pancreas, about their ability to reduce disintegration of a glycogen of a liver by impact on the fermental systems regulating this process, about braking of a neoglycogenesis from protein. Natural zhiromobilizuyushchy action of Ampere-second. (more expressed at use of high-speed drugs) it is shown in strengthening of free fatty acids and ketone bodies of blood. At reception of Ampere-second. elderly people noted decrease in cholesterol and lipoproteids. Ampere-second. increase weight and improve function of kidneys.
The mechanism of effect of anabolic steroids is still insufficiently studied. Their anabolic effect is not mediated by hyperfunction of gonads, adrenal glands and a thyroid gland. Participation of the insulyarny device of a pancreas and somatotropic hormone of a hypophysis in their anabolic action is possible. There are instructions on stimulation under the influence of Ampere-second. speeds of synthesis of RNA.
Indications to use
Ampere-second. are widely applied in clinical practice. Ability of these drugs to strengthen synthetic processes in protein metabolism allows to use them for the purpose of stimulation of weight and improvement of the general state at the diseases proceeding with the phenomena of exhaustion in the preoperative and postoperative periods, at radiation therapy, at acute and hron. infections, in a stage of reconvalescence after a serious illness, at interstitial and pituitary insufficiency, a toxic craw. Absence at use of moderate doses of Ampere-second. virilescences of female patients and increase in sexual desire of male patients, lack of noticeable progressing of a differentiation and ossification of a skeleton allows to apply Ampere-second successfully. for the purpose of stimulation of growth and physical development of premature children and patients with hypoplastic forms of low-tallness.
Use of Ampere-second. it was very favorable also at a pituitary and cerebral and pituitary nanism.
Ampere-second. render positive effect in case of a myocardial infarction, accelerating reparative processes in heart. At their inclusion in a complex of remedies positive dynamics of an ECG, smaller, than before their use, number of aneurisms, ruptures of a myocardium etc. is noted.
Ampere-second. at rheumatism improve a condition of a myocardium, raise indicators of nonspecific immunity. Improvement of function of kidneys and decrease in content of residual nitrogen in blood under the influence of Ampere-second. does them by useful symptomatic cure for a renal failure, and also at a nephrotic hypoproteinemia. Ampere-second. improve a trophicity of a vascular wall, increase permeability of capillaries that is used in therapy of diabetic angiopatiya: nephropathy and retinopathy. Under their influence increase in glomerular filtering of kidneys and in some cases improvement of a condition of an eyeground is noted: a rassasyvaniye of exudates with preservation, and sometimes and with increase in visual acuity.
Anticatabolic properties of Ampere-second. cause efficiency of their use at an endogenous giperglyukokortitsizm (Itsenko's disease — Cushing, steroid diabetes) and long therapy by corticosteroids.
Ability of Ampere-second. to strengthen synthesis of protein in a bone matrix and to detain calcium, phosphorus, sulfur and other minerals allows to apply with success them at various forms of osteoporosis, it is long not beginning to live changes, imperfect bone formation. For achievement of effect at treatment of Ampere-second. patients shall receive adequate amounts of proteins, fats, carbohydrates, vitamins and mineral substances with food.
Activity of Ampere-second is explained by anti-gonadotropic action. at a breast cancer and a climacteric angioneurosis at women, progesteronopodobny action — effect at functional metrorrhagias and a mastopathy.
Some Ampere-second., hl. obr. ethylated l metilirovanny in situation 17, active at peroral introduction, can at certain patients (more often at suffering hron. diseases of a liver) to have a passing hepatotoxic action, a cut it is shown in the form of increase in a liver, emergence of the dispeptic phenomena, sometimes jaundices. At the same time the delay of elimination of a bromsulfalein, increase in transaminases is observed, at a puncture biopsy of a liver the phenomena of cholestasias, formation of bilious blood clots in hepatic channels are noted. These phenomena pass independently in 40 — 50 days after cancellation of drugs, and at treatment by cholagogue means — in earlier terms.
At prolonged use of high doses of Ampere-second. at women by-effects can come to light: greasiness of skin, acne vulgaris, coarsening of a voice, a hirsutism, increase in a clitoris, it is extremely rare — disturbance of a menstrual cycle. These phenomena are not resistant and usually gradually pass at drug withdrawal.
In isolated cases of Ampere-second. can cause the phenomena of a medicamentous allergy.
Contraindications: prostate cancer, acute diseases of a liver; relative contraindications — pregnancy and the period of a lactation, acidosis at a diabetes mellitus.
Bibliography: Anabolic steroids in medicine, under the editorship of E. V. Vasyukova and G. P. Shultsev, M., 1969; Akhr A. A. and Titov Yu. A. Anabolic steroids, Zhurn. Vsesoyuz. chemical islands of Mendeleyev, t. 10, No. 6, page 684, 1965; N. A Mark. Anabolic steroids, Probl. endokrinol. and gormonoter., t. 11, No. 2, page 106, 1965, bibliogr.; Boris A., Stevenson R. N of a. Trmal T. A comparison of the androgenic and myotrophic activities of some anabolic steroids in the castrated rat, J. Steroid Biochem; v. 1, p. 349, 1970; Kochakian C. D. Die anabole und androgene Aktivitat von Androgenen, Klin. Wschr., S. 881, 1961; Krüskemper H. L. Anabole Steroide, Stuttgart, 1965, Bibliogr.
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