CORTEXONE (Desoxycorticosteronum; synonym: DOCK, Cortexonum; joint venture. B) — hormonal drug of bark of adrenal glands, mineralokortikosteroid.
White fine-crystalline powder, we will not dissolve in water. It is alcohol-soluble, acetone and other organic solvents. It is allocated in 1937 from adrenal glands of cattle.
Values of the radical of R in a molecule D. are various (R1, R2 and R3):
Is formed in adrenal glands of cholesterol through pregnenolon — key substance in biosynthesis of all corticosteroids (see). — an intermediate product in biosynthesis Aldosteronum (see) and corticosterone (see). It detains release of sodium with urine approximately by 50 times more actively, than a hydrocortisone, and by 100 times more, than a cortisone. Considerably surpasses in activity a hydrocortisone and a cortisone in tests for extension of life of adrenalectomized animals.
Unlike a hydrocortisone and other glucocorticosteroids, D. rather poorly influences carbohydrate metabolism and a gluconeogenesis. Therefore at D.'s introduction the content of glucose in blood at the starving adrenalectomized animals is not normalized. At a hypocorticoidism release of sodium and water with urine increases. Owing to dehydration of an organism blood pressure goes down and activity of cardiovascular system is broken. Along with increase in release of sodium and water in an organism potassium is late: contents it in blood and in fabrics increases.
Disturbances of a water salt metabolism can be eliminated with introduction to D.'s organism or Aldosteronum. At normally functioning adrenal glands D.'s introduction causes a delay of sodium and water in an organism, at the same time release of potassium with urine increases and the ABP raises. At introduction of high doses of D. the hypopotassemia develops, can lead edges to disturbance of cordial activity (change on an ECG), to increase in blood pressure, weakness, joint pains etc.
The mechanism of participation of D. in metabolism of sodium, potassium and water is not found out completely: apparently, protein synthesis, participating in ion-exchange processes is stimulated. Similar processes of movement of sodium and potassium happen under the influence of D. not only in kidneys, but also in other epithelial fabrics — in salivary and sweat glands, in a mucous membrane of intestines. Sodium from a mucous membrane passes in serous, potassium — on the contrary, from serous into a mucous membrane. On biol, and to mineralokortikosteroidny properties and on the mechanism of action of D. it is similar to Aldosteronum (see), but influences filtration rate in tubules and more less, than Aldosteronum, promotes accumulation in an organism of intercellular liquid. In spite of the fact that D. at a wedge, tests for patients with an addisonovy disease was 25 — 30 times weaker than Aldosteronum, it is the most widely used mineralokortikoidny drug.
Synthetic methods of receiving D. are more available, than methods of receiving Aldosteronum. In to lay down. to practice apply acetic and pivalic ethers D. and partly its ether with enanthic to - that (drug Corticon-Depo). Ethers D. are steadier in an organism, than D., and have more long term of action.
These drugs have an identical therapeutic focus and are applied not only at replacement therapy of hypofunction of bark of an adrenal gland (an addisonov a disease, a hypocorticoidism), but also to treatment of hypotensive states, a pituitary cachexia, intoxications after burns, frostbites, radiations and after infectious diseases, stomach ulcers and a duodenum, an adynamia, the general muscular weakness, etc.
Cortexone acetate II (Desoxycorticosteroni acetas, DOKSA; synonym: Arcort, Cortate, Cortenil; Cortexon, Cortiron, Decorton, Descorterone, Desoxycortoni acetas, Doca, Percorten, etc.; joint venture. B) — white crystal powder, inodorous. Let's not dissolve in water, it is difficult alcohol-soluble, it is easy in ether and in fatty oils. Forms of release: ampoules on 1 ml of 0,5% of solution in oil (0,005 g in 1 ml); sterile tablets for implantation on 0,05 and 0,1 g (in the soldered ampoules) and tablets under language on 0,0025 and 0,005 g (2,5 and 5 mg). Store in banks from orange glass with a ground stopper in the place protected from light. Cortexone acetate is applied depending on disease severity in the form of injections daily or 2 — 3 times a week or in the form of tablets under language once a day or every other day.
Cortexone trimetilatsetat III (Desoxycorticosteroni trimethylacetas; synonym: Desoxycorticosteronum trimethylaceticum, Percorten M; joint venture. B) — white fine-crystalline powder, we will practically not dissolve in water. It is alcohol-soluble also in the majority of organic solvents. Form of release: ampoules on 1 ml containing 25 mg of drug in the form of fine-crystalline suspension. Store in the place protected from light. Cortexone trimetilatsetat at a single intramuscular injection shows to lay down. action during 2 — 3 weeks
Use of drugs of cortexone at some diseases
At an addisonovy disease is entered depending on disease severity from 5 mg by 3 times a week to 10 mg in day of cortexone of acetate before reduction of symptoms of a disease and then on 5 mg of 1 — 2 time a week or 1 time of 25 mg of cortexone of a trimetilatsetat; if during 2 — 3 weeks there is no arterial hypertension and puffiness, the dose is repeated or, depending on a condition of the patient, it is increased or reduced. At an addisonovy disease it is reasonable to enter at the same time glucocorticoids and to give sodium chloride (4 — 10 g a day) in wafers or in the form of water solution from 10 g of sodium chloride, 5 g of sodium citrate with fruit juice.
At acute insufficiency of bark of adrenal glands and at addisonichesky crisis 4 times a day enter 5 — 10 mg of cortexone of acetate.
At hypotensive states because of the lowered function of bark of adrenal glands apply 5 mg of cortexone of acetate every other day or in 2 — 3 days (12 — 15 injections) in combination with anabolic hormones.
Contraindications: an idiopathic hypertensia, cardiovascular insufficiency with hypostases, atherosclerosis, stenocardia, nephrite, a nephrosis, cirrhosis, infectious diseases, a leukopenia, thrombocytopenia.
Bibliography: Biochemistry of hormones and hormonal regulation, under the editorship of N. A. Yudayev, M., 1976, bibliogr.; Klegg P. and Klegg And. Hormones, cells, an organism, the Role of hormones at mammals, the lane with English, M., 1971, bibliogr.; Corticosteroid regulation of a water-salt homeostasis, under the editorship of M. G. Kolpakov, Novosibirsk, 1967; X e f t of m and E. Biokhimiya's N of steroids, the lane with English, M., 1972, bibliogr.; E with to and I. A N. Fundamentals of physiology of closed glands, M., 1975, bibliogr.
V. I. Maximov.