DEXAMETHASONE (Dexamethasonum; synonym: Decadron, Deltafluoren, Dexadrol, Dexacorten, Dexameson, Dexaschereson, Dexason, Hexadecadrol, Millicorten, Graderon etc.) — synthetic drug of glucocorticoid hormones. On a chemical structure represents 9 - alpha fluorine - 1b - alpha Methylprednisolonum:
— white or almost white crystal powder. It is steady on air. It is badly alcohol-soluble, methanol and dioxane. Let's well dissolve in chloroform and ether. Pier. weight (weight) 392,47.
Administration of fluorine in situation 9 an alpha and methyl group in situation 16 an alpha in a molecule of Prednisolonum increased its antiinflammatory, antirheumatic and antiasthmatic activity by 5 — 10 times. At the same time its side effects decreased. Is less, than others corticosteroids (see), influences exchange of electrolytes and for a delay of water and sodium chloride in an organism; it does not stimulate a gluconeogenesis and exerts weaker impact on mentality. On therapeutic activity of 0,5 mg of D. there correspond to influence of 3,5 mg of Prednisolonum, 15 mg of a hydrocortisone or 17,5 mg of a cortisone. Is well transferred by patients.
apply orally for treatment of kollagenoz — hron, a pseudorheumatism, rheumatism, the disseminated lupus erythematosus, a sclerodermitis; polyarthritis; at allergic states — bronchial asthma, status asthmaticus, vasculomotor rhinitis, hypostasis of upper respiratory tracts, posttransfusion reactions, Stephens's syndrome — Johnson; at diseases of blood — hemolitic anemia, hypoplastic anemia, an agranulocytosis, an idiopathic thrombopenia, acute and hron, leukemia, a granulomatosis, a lymphogranulomatosis; at diseases of skin — eczemas, a dermatosis, a lupus, an itch, urtikariya; for treatment of eye diseases — an iritis, a uveitis, a retinitis, an iridocyclitis, etc. It is applied also at insufficiency of adrenal glands, an adrenogenital syndrome, hepatitis, a sarcoidosis, idiopathic to a spr, ultserozny colitis, a subacute thyroiditis.
D.'s dose is established depending on character and disease severity. At oral administration the daily dose is divided into 3 — 4 parts, and the patient accepts drug in time or after food. Initial daily doses for adult 2 — 3 mg; after achievement a wedge, improvements they gradually decrease to 0,5 — 1 mg — the smallest maintenance doses. At some diseases apply higher dosages.
Intravenously enter 4 — 20 mg of drug, in especially hard cases the dose increases. The drug is administered slowly. After achievement of improvement of D. continue to apply orally. D.'s doses for children till 1 year — 1/10, up to 2 years — 1/5, up to 3 years — 1/4, from 5 to 10 years — 1/33 doses of adults. After 15 years apply the dosages recommended to adults. At acute adrenal insufficiency, terminal states of D. enter intravenously and intramusculary 1 — 5 ml a day.
The termination of treatment of D. as well as other corticosteroids, is carried out gradually.
Prolonged use of high doses of D. or hypersensitivity to kortikoida can cause disturbance of exchange of proteins, increase in a sugar content in blood, osteoporosis, excitement, sleeplessness, sometimes disturbance of a menstrual cycle. Catabolic action of D. can be reduced by simultaneous use of anabolic drugs.
Absolute contraindication for D.'s use — herpes simplex. Drug is contraindicated at severe forms of an idiopathic hypertensia, a hypercorticoidism, pregnancy, an acute endocarditis, psychoses, neuritis, osteoporosis, a peptic ulcer of a stomach and duodenum, after recently undergone operations, and also at active tuberculosis, severe forms of a diabetes mellitus.
Forms of release: tablets on 0,5 and 1 mg, ampoules on 1 ml containing 0,004 g of a soluble form D. (dexamethasone-21-phosphate in the form of sodium salt). Store with precaution (list B).
See also Glucocorticoid hormones .
Bibliography: Mashkovsky M. D. Pharmaceuticals, p.1, page 579, M., 1977.
V. I. Maximov.