Декадрон®

General characteristics. Structure:

Active ingredient: 4 mg of dexamethasone of phosphate in 1 ml of solution.

Pharmacological properties:

Pharmacodynamics. GKS - metilirovanny derivative a ftorprednizolona, slows down release interleykina1 and interleykina2, interferon scale from lymphocytes and macrophages. Renders the antiinflammatory, antiallergic, desensibilizing, antishock, anti-toxic and immunodepressive effect. Suppresses release by a hypophysis of AKTG and beta липотропина, but does not reduce the level of the circulating beta endorphine. Oppresses secretion of TTG and FSG. Increases excitability of TsNS, reduces quantity of lymphocytes and eosinophils, increases - erythrocytes (stimulates production of erythropoetins).

Interacts with specific cytoplasmatic receptors and forms the complex getting into a kernel of a cell and stimulates synthesis of MRNK; the last induces formation of proteins, including the lipokortin mediating cellular effects. Lipokortin oppresses A2 phospholipase, suppresses release of arachidonic acid and suppresses synthesis of endoperoxides, Pg, the leukotrienes promoting processes of an inflammation, an allergy, etc. Protein metabolism: reduces amount of protein in plasma (at the expense of globulins) with increase in coefficient albumine/globulin, increases synthesis of albumine in a liver and kidneys; strengthens a protein catabolism in muscular tissue. Lipidic exchange: increases synthesis of higher fatty acids and TG, redistributes fat (accumulation of fat is preferential in the field of a shoulder girdle, the person, a stomach), leads to development of a hypercholesterolemia.

Carbohydrate metabolism: increases absorption of carbohydrates from a GIT; increases activity of the glyukozo-6-phosphatase leading to increase in intake of glucose from a liver in blood; increases activity of a fosfoenolpiruvatkarboksilaza and synthesis of the aminotransferases leading to activation of a gluconeogenesis. Water and electrolytic exchange: Na + and water in an organism detains, stimulates removal of K+ (the ISS activity), reduces absorption of Ca2 + from a GIT, "washes away" Ca2 + from bones, increases removal of Ca2 + kidneys.

The antiinflammatory effect is connected with release oppression by eosinophils of mediators of an inflammation; induction of formation of a lipokortin and reduction of quantity of the mast cells producing hyaluronic acid; with reduction of permeability of capillaries; stabilization of cellular membranes and membranes of organellas (especially lizosomalny). The antiallergic effect develops as a result of suppression of synthesis and secretion of mediators of an allergy, braking of release from sensitized mast cells and basophiles of a histamine, etc. biologically active agents, reduction of number of the circulating basophiles, suppression of development of adenoid and connecting tissue, decrease in quantity of T-and B-lymphocytes, mast cells, decrease in sensitivity of effector cells to mediators of an allergy, oppression of antibodyformation, change of an immune response of an organism.

At HOBL action is based mainly on braking of inflammatory processes, oppression of development or the prevention of hypostasis of mucous membranes, braking of eosinophilic infiltration of a submucosal layer of an epithelium of bronchial tubes, adjournment in a mucous membrane of bronchial tubes of the circulating cell-bound immune complexes, and also braking of an erozirovaniye and desquamation of a mucous membrane. Increases sensitivity of beta adrenoceptors of bronchial tubes of small and average caliber to endogenous catecholamines and exogenous sympathomimetics, reduces viscosity of slime due to oppression or reduction of its products. Antishock and anti-toxic action is connected with increase in the ABP (due to increase in concentration of the circulating catecholamines and recovery of sensitivity to them of adrenoceptors, and also vasoconstriction), decrease in permeability of a vascular wall, membranoprotektorny properties, activation of the enzymes of a liver participating in metabolism endo-and xenobiotics. The immunodepressive effect is caused by braking of release of cytokines (interleykina1, interleykina2; interferon scale) from lymphocytes and macrophages.

Suppresses synthesis and secretion of AKTG and for the second time - synthesis of endogenous GKS. Slows down connective tissue reactions during inflammatory process and reduces a possibility of formation of cicatricial fabric. Feature of action - considerable inhibition of function of a hypophysis and almost total absence of the ISS of activity. Doses of 1-1.5 mg/days oppress bark of adrenal glands; biological T1/2 - 32-72 h (duration of oppression of system a hypothalamus-hypophysis-bast layer of adrenal glands). On GKS force of activity of 0.5 mg of dexamethasone there correspond about 3.5 mg of Prednisonum (or Prednisolonum), 15 mg of a hydrocortisone or 17.5 mg of a cortisone.

Indications to use:

The inflammatory and allergic diseases, nausea and vomiting caused by chemotherapeutic means, shock and wet brain (injections).

Route of administration and doses:

Inside, in individually selected doses which size is defined by a type of a disease, degree of its activity and character of the answer of the patient. An average daily dose - 0.75-9 mg. In hard cases also the high doses divided into 3-4 receptions can be applied. The maximum daily dose - usually 15 mg.

After achievement of therapeutic effect the dose is gradually reduced (usually by 0.5 mg in 3 days) to supporting - 2-4.5 mg/days. Minimum effective dose - 0.5-1 mg/days. To children (depending on age) appoint 83.3-333.3 mg/kg or 2.5-10 mkg / кв.м / days in 3-4 receptions. Duration of use of dexamethasone depends on the nature of pathological process and efficiency of treatment and makes from several days to several months and more. Treatment is stopped gradually (at the end appoint several injections of corticotropin).

At bronchial asthma, a pseudorheumatism, ulcer colitis - 1.5-3 mg/days; at hard currency - 2-4.5 mg/days; at oncohematological diseases - 7.5-10 mg.

For treatment of acute allergic diseases it is reasonable to combine parenteral and peroral administration: 1 day - 4-8 mg parenterally; 2 day - inside, 4 mg 3 times a day; 3, 4 day - inside, 4 mg 2 times a day; 5, 6 day - 4 mg/days, inside; 7 day - drug withdrawal.

Test with dexamethasone (Liddl's test). It is carried out in the form of small and big tests. At the small test each 6 h within a day give dexamethasone to the patient on 0.5 mg (i.e. in 8 h morning, in 14 h, 20 h and 2 h morning). I wet for definition 17-OKC or free cortisol collect from 8 h morning to 8 h morning 2 days before purpose of dexamethasone and also 2 days in the same temporary intervals after reception of the specified dexamethasone doses. These doses of dexamethasone oppress formation of corticosteroids almost at all almost healthy faces. In 6 h after the last dose of dexamethasone the maintenance of cortisol in plasma is lower than 135-138 nmol/l (less than 4.5-5 mkg / 100 of ml). Decrease in removal 17-OKC is lower than 3 mg/days, and free cortisol lower than 54-55 nmol/days (lower than 19-20 mkg/days) exclude hyperfunction of bark of adrenal glands. At the persons having a disease or an Icenco-Cushing syndrome when carrying out the small test of change of secretion of corticosteroids it is not noted. When carrying out the big test dexamethasone is appointed on 2 mg by each 6 h during 2 days (i.e. 8 mg of dexamethasone a day). Also carry out collecting urine for definition 17-OKC or free cortisol (if necessary define free cortisol in plasma).

At Itsenko-Cushing's disease decrease in removal 17-OKC or free cortisol for 50% and more while at tumors of adrenal glands or AKTG-ektopirovannom (or kortikoliberin-malrelated) a syndrome removal of corticosteroids does not change is noted.

At some patients with AKTG-ektopirovannym a syndrome of decrease in removal of corticosteroids does not come to light even after reception of dexamethasone in a dose of 32 mg/days.

Features of use:

Prior to the beginning of and during GKS of therapy it is necessary to control the general blood test, level of a glycemia and content of electrolytes in plasma.

Appointing dexamethasone at intercurrent infections, septic states and tuberculosis, it is necessary to carry out treatment by bactericidal antibiotics at the same time.

At daily use by 5 months of treatment the atrophy of bark of adrenal glands develops. Can mask some symptoms of infections; during treatment it is useless to carry out immunization.

At sudden cancellation, especially in case of the previous use of high doses, there is a syndrome of "cancellation" of GKS (it is not caused by a hypocorticoidism): loss of appetite, nausea, block, generalized musculoskeletal pains, adynamy. After cancellation within several months relative insufficiency of bark of adrenal glands remains. If during this period there are stressful situations, appoint (according to indications) for the period of GKS, in need of a combination to the ISS. At children during prolonged treatment careful observation of dynamics of growth and development is necessary.

To children who during treatment were in contact with patients with measles or chicken pox preventively appoint specific Ig. In the I trimester, in the period of a lactation appoint only according to "vital" indications, taking into account the expected medical effect and negative influence on a fruit.

At long therapy during pregnancy - a fruit growth disorder. In the III trimester of pregnancy - danger of emergence of an atrophy of bark of adrenal glands at a fruit that can demand performing replacement therapy from the newborn.

During treatment by dexamethasone (especially long) observation of the oculist, control of the ABP and water and electrolytic balance, and also a picture of peripheral blood and level of a glycemia is necessary. For the purpose of reduction of by-effects it is possible to appoint anabolic steroids, antacids, and also to increase receipt of K+ in an organism (a diet, the drugs K+). Food has to be rich K+, proteins, vitamins, with the maintenance of a small amount of fats, carbohydrates and salts.

At children in a growth period of GKS have to be applied only according to absolute indications and under especially careful observation of the attending physician.

Side effects:

Frequency of development and expressiveness of side effects depend on duration of use, size of the used dose and a possibility of observance of a circadian rhythm of appointment.

From endocrine system: decrease in tolerance to glucose, a "steroid" diabetes mellitus or manifestation of a latent diabetes mellitus, oppression of function of adrenal glands, an Icenco-Cushing syndrome (a crescent-shaped face, obesity of pituitary type, a hirsutism, increase in the ABP, a dysmenorrhea, an amenorrhea, a myasthenia, striya), a delay of sexual development at children.

From the alimentary system: nausea, vomiting, pancreatitis, "steroid" stomach ulcer and 12-perstny gut, erosive esophagitis, bleedings and perforation of a GIT, increase or loss of appetite, meteorism, hiccups. In rare instances - increase in activity of "hepatic" transaminases and ShchF.

From CCC: arrhythmias, bradycardia (up to a cardiac standstill); development (at predisposed patients) or strengthening of expressiveness of HSN, ECG change characteristic of a hypopotassemia, increase in the ABP, hypercoagulation, fibrinferments. Patients with an acute and subacute myocardial infarction have a distribution of the center of a necrosis, delay of formation of cicatricial fabric that can lead to a rupture of a cardiac muscle.

From a nervous system: delirium, disorientation, euphoria, hallucinations, maniac-depressive psychosis, depression, paranoia, increase in intracranial pressure, nervousness or concern, sleeplessness, dizziness, вертиго, cerebellum pseudoneoplasm, headache, spasms.

From sense bodys: a back subkapsulyarny cataract, increase in intraocular pressure with possible injury of an optic nerve, tendency to development of consecutive bacterial, fungal or viral infections of eyes, trophic changes of a cornea, an exophthalmos. From a metabolism: the increased removal of Ca2+, a hypocalcemia, increase in body weight, negative nitrogenous balance (the increased disintegration of proteins), the increased sweating. The caused ISS activity - a delay of liquid and Na + (peripheral hypostases), a hypernatremia, a gipokaliyemichesky syndrome (a hypopotassemia, arrhythmia, a mialgiya or a spasm of muscles, unusual weakness and fatigue).

From a musculoskeletal system: delay of growth and processes of ossification at children (premature closing of epiphyseal regions of growth), osteoporosis (it is very rare - pathological fractures of bones, an aseptic necrosis of a head humeral and a femur), a rupture of sinews of muscles, a "steroid" myopathy, decrease in muscle bulk (atrophy).

From integuments and mucous membranes: the slowed-down healing of wounds, petechias, ecchymomas, thinning of skin, an atrophy of skin and hypodermic cellulose, hyper - or hypopigmentation, steroid eels, striya, tendency to development of a pyoderma and candidiases.

Allergic reactions: generalized (skin rash, skin itch, acute anaphylaxis), local allergic reactions. Other: development or an exacerbation of infections (emergence of this side effect is promoted jointly by the applied immunodepressants and vaccination), a leukocyturia, a syndrome of "cancellation". Overdose.

Symptoms: strengthening of the described side effects is possible. In this case the dose of drug should be reduced. Treatment: symptomatic.

Interaction with other medicines:

Change of effects at simultaneous use with acetylsalicylic acid, Phenytoinum, phenobarbital, ephedrine, Rifampinum, indometacin, coumarinic anticoagulants, diuretics is possible.

Contraindications:

For short-term use according to "vital" indications the only contraindication is giperchuvstvitelnost.s care.

Parasitic and infectious diseases of the virus, fungal or bacterial nature (now or recently postponed, including recent contact with the patient) - the herpes simplex surrounding herpes (a viremichesky phase), chicken pox, measles; the amebiasis, a strongyloidosis (established or suspected); system mycosis; active and latent tuberculosis.

Use at serious infectious diseases is admissible only against the background of specific therapy. Pre-and the postvaccinal period (8 weeks to and 2 weeks after vaccination), lymphadenitis after BTsZh inoculation. Immunodeficiency (including AIDS or HIV infection).

Gastrointestinal diseases - a peptic ulcer of a stomach and a 12-perstny gut, an esophagitis, gastritis, an acute or latent round ulcer, recently created intestines anastomosis, nonspecific ulcer colitis with threat of perforation or abscessing, a diverticulitis.

Diseases of CCC, including recently postponed myocardial infarction (at patients with an acute and subacute myocardial infarction distribution of the center of a necrosis, delay of formation of cicatricial fabric and thereof - a rupture of a cardiac muscle is possible), dekompensirovanny HSN, arterial hypertension, lipidemia.

Endocrine diseases - a diabetes mellitus (including disturbance of tolerance to carbohydrates), a thyrotoxicosis, a hypothyroidism, Itsenko-Cushing's disease.

Heavy chronic renal and/or liver failure, нефроуролитиаз. The hypoalbuminemia and states contributing to its emergence.

System osteoporosis, gravis myasthenia, acute psychosis, obesity (the III-IV Art.), poliomyelitis (except for a form of bulbar encephalitis), open and closed-angle glaucoma, the lactation period.

Storage conditions:

List B. To store in the place protected from light. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

In ampoules on 1 ml or 2 ml of solution, in packaging on 10 pieces of ampoules or 1 piece.