More info
Active ingredients
Dexamethasone
Release form
Pills
Composition
1 tablet contains: Active ingredient: dexamethasone 500 mcg.
Pharmacological effect
GKS. Suppresses the function of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of inflammation. Violates the ability of macrophages to phagocytosis, as well as the formation of interleukin-1. It contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of inflammation. Reduces capillary permeability due to histamine release. Suppresses the activity of fibroblasts and the formation of collagen. Inhibits the activity of phospholipase A2, which leads to the suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins. Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed to the lymphoid tissue; inhibits the formation of antibodies. Dexamethasone inhibits the release of ACTH pituitary and β-lipotropin, but does not reduce the level of circulating β-endorphin. It inhibits the secretion of TSH and FSH. When directly applied to the vessels, it has a vasoconstrictor effect. Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, increases the activity of gluconeogenesis enzymes. In the liver, dexamethasone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose activates insulin secretion. Dexamethasone inhibits glucose uptake by fat cells, which leads to the activation of lipolysis. However, due to an increase in insulin secretion, lipogenesis is stimulated, which leads to fat accumulation. It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term therapy of corticosteroids. As a result of the catabolic action, growth suppression in children is possible. At high doses, dexamethasone may increase the excitability of brain tissue and help lower the threshold of convulsive readiness.Stimulates excessive production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers. With systemic use, therapeutic activity of dexamethasone is due to anti-inflammatory, antiallergic, immunosuppressive and anti-proliferative effect. ) action. By anti-inflammatory ak exceeds hydrocortisone by 30 times, does not possess mineralocorticoid activity.
Pharmacokinetics
Plasma protein binding is 60-70%. Penetrates histohematogenous barriers. In a small amount excreted in breast milk. Metabolized in the liver. T1 / 2 is 2-3 hours. It is excreted by the kidneys. When applied locally in ophthalmology, it is absorbed through the cornea with the intact epithelium into the moisture of the anterior chamber of the eye. When inflammation of the eye tissue or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone increases significantly.
Indications
Symptomatic therapy of painful and inflammatory processes of various origins, including: rheumatoid arthritis and periarthritis, ankylosing spondylitis (Bechterew's disease), psoriatic arthritis, reactive arthritis (Reiter’s syndrome), osteoarthrosis of various localization, tendinitis, bursitis, myalgia, neuralgia, radiculitis; musculoskeletal system (including sports), bruised muscles and ligaments, sprains, ligaments and tendons of the muscles.
Contraindications
For short-term use for "vital" indications, the only Contraindications is hypersensitivity to the active substance or auxiliary components of the drug. Dexamethasone is contraindicated in patients with galactosemia, lactase deficiency and glucose-galactose malabsorption syndrome, due to the fact that lactose is included in the preparation.
Use during pregnancy and lactation
During pregnancy (especially in the first trimester), as well as during lactation, dexamethasone is used taking into account the expected therapeutic effect and the negative effect on the fetus. With prolonged therapy during pregnancy does not exclude the possibility of fetal growth disorders.In the case of use at the end of pregnancy there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.
Dosage and administration
Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, the tolerability of the drug and the patient's response to therapy. The recommended starting dose for adults is between 0.5 mg and 9 mg / day. The usual maintenance dose is from 0.5 mg to 3 mg / day. The minimum effective daily dose is 0.5-1 mg. The maximum daily dose is 10-15 mg. The daily dose can be divided into 2 - 4 doses. After reaching the therapeutic effect, the dose is gradually reduced (usually by 0.5 mg every 3 days until the maintenance dose is reached). With long-term use of high doses inside, the drug is recommended to be taken with food, and in the intervals between meals, antacids should be taken. The duration of dexamethasone use depends on the nature of the pathological process and the effectiveness of treatment and ranges from several days to several months or more. The treatment is stopped gradually (at the end, several injections of corticotropin are prescribed). With bronchial asthma, rheumatoid arthritis, ulcerative colitis -1.5-3 mg / day; - in systemic lupus erythematosus - 2-4.5 mg / day; - in hematologic diseases - 7.5-10 mg. For the treatment of acute allergic diseases, it is advisable to combine parenteral and oral administration: 1 day - 4-8 mg parenterally; 2 day - inside, 4 mg 3 times a day; 3, 4 days - by mouth, 4 mg 2 times a day; 5, 6 day - 4 mg / day, inside; Day 7 - drug discontinuation. Dosing in children. Children (depending on age) are prescribed 2.5-10 mg / m2 of body surface area / day, dividing the daily dose into 3-4 doses. Diagnostic tests for hyperfunction of the adrenal cortex. Short 1-mg dexamethasone test: 1 mg of dexamethasone orally at 11 am; blood sampling to determine serum cortisol at 8.00 the next day. Special 2-day test with 2 mg of dexamethasone: 2 mg of dexamethasone orally every 6 hours for 2 days; daily urine is collected to determine the concentration of 17-hydroxycorticosteroids.
Side effects
On the part of the immune system, infrequently: hypersensitivity reactions, a decrease in the immune response and an increase in susceptibility to infections.On the part of the endocrine system, often: transient adrenal insufficiency, growth retardation in children and adolescents, adrenal insufficiency and atrophy (reduction of the stress response), Itsenko-Cushing syndrome, menstrual disorders, hirsituism, the transition of latent diabetes mellitus to clinically manifest, increased insulin or oral hypoglycemic drug requirements in patients with diabetes mellitus, sodium and water retention, increased potassium loss; - very rare: hypokalemic alkalosis, negative nitrogen balance due to protein catabolism. Metabolic and nutritional disorders — often: decrease in carbohydrate tolerance, increased appetite and weight gain, obesity. —Frequently: hypertriglyceridemia. On the part of the nervous system, often: mental disorders. -frequently: swelling of the papillae of the optic nerve and increased intracranial pressure (pseudo-tumor of the brain) after discontinuation of therapy, dizziness, headache, very rarely; convulsions, euphoria, insomnia, irritability, hyperkinesia, depression; - rarely: psychosis. From the digestive system - infrequently: peptic ulcers, acute pancreatitis, nausea, hiccups, gastric or duodenal ulcers, - very rarely: esophagitis, perforation of the ulcer and bleeding of the gastrointestinal tract (hematomesis, melena), pancreatitis, perforation of the gallbladder and intestines (especially in patients with chronic inflammatory diseases of the large intestine). On the part of the sense organs - infrequently: posterior subcapsular cataract, increased intraocular pressure, a tendency to develop secondary bacterial, fungal or viral infections of the eye, trophic changes of the cornea, exophthalmos. From the side of the cardiovascular system - infrequently: arterial hypertension, hypertensive encephalopathy. - very rarely: polyfocal ventricular extrasystoles, transient bradycardia, heart failure, myocardial rupture after a recent acute heart attack. On the part of the skin - often: erythema, thinning and brittleness of the skin, delayed healing of wounds, striae, petechiae and ecchymosis, excessive sweating, steroid acne, suppression of the skin reaction during allergological tests, - very rare: angineurotic edema, allergic dermatitis, urticaria.On the part of the musculoskeletal system, often: muscle atrophy, osteoporosis, muscle weakness, steroid myopathy (muscle weakness due to catabolism of muscle tissue); - infrequently: aseptic necrosis of bones; -very rarely; vertebral compression fractures, tendon tears (especially when some quinolones are used together), damage to the articular cartilage, and bone necrosis (associated with frequent intra-articular injections). On the part of the hematopoietic system - rarely: thromboembolic complications, a decrease in the number of monocytes and / or lymphocytes, leukocytosis, eosinophilia (like other glucocorticosteroids), thrombocytopenia and nonthrombocytopenic purpura. shock. From the genitourinary system, rarely: impotence. Signs and symptoms of withdrawal of glucocorticosteroids If a patient who is taking glucocorticosteroids for a long time, quickly reduce the dose of the drug, may develop signs of adrenal insufficiency, hypotension, and death. In some cases, withdrawal symptoms may be similar to the symptoms and signs of an exacerbation or recurrence of the disease about which the patient is receiving treatment. With the development of severe adverse events, dexamethasone treatment should be discontinued.
Interaction with other drugs
With simultaneous use with antipsychotics, bukarbanom, azathioprine, there is a risk of developing cataracts; with anticholinergic agents - risk of developing glaucoma. When used simultaneously with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs is reduced. When used simultaneously with hormonal contraceptives, androgens, estrogens, anabolic steroids, hirsutism, acne, and chromomas are possible. excretion of potassium; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. If used simultaneously with oral anticoagulants, a decrease in the anticoagulant effect is possible. If used simultaneously with cardiac glycosides, porosity may deterioratecardiac glycosides due to potassium deficiency. When used simultaneously with aminoglutethimide, it is possible to reduce or inhibit the effects of dexamethasone; with carbamazepine - may decrease the action of dexamethasone; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - a decrease in plasma concentration of imatinib is possible due to the induction of its metabolism and an increase in excretion from the body. With simultaneous use of itraconazole, the effects of dexamethasone are enhanced; with methotrexate - may increase hepatotoxicity; with praziquantel - perhaps a decrease in the concentration of praziquantel in the blood. When used simultaneously with rifampicin, phenytoin, barbiturates, the effects of dexamethasone can be weakened due to an increase in its elimination from the body.
special instructions
With caution should be used for parasitic and infectious diseases of viral, fungal or bacterial nature (currently or recently transferred, including recent contact with the patient) - herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amebiasis, strongyloidosis (established or suspect), systemic mycosis; active and latent tuberculosis. Use in severe infectious diseases is permissible only against the background of specific therapy. It should be used with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, and with immunodeficiency states (including AIDS or HIV infection). С caution should be used in diseases of the gastrointestinal tract: gastric ulcer and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, a newly created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscessing, diverticulitis. It should be used with caution in diseases of the cardiovascular system, including after a recent myocardial infarction (patients with acute and subacute myocardial infarction may spread necrosis, slow the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, hypertension, hyperlipidemia), with endocrine diseases - diabetes ( includingviolation of tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, in severe chronic renal and / or liver failure, nephrorolithiasis, in hypoalbuminemia and conditions predisposing to its occurrence, in systemic osteoporosis, myasthenia, in the case of osteoporosis, myasthenia, in the case of osteoporosis, myastheniama, in the case of osteoporosis, myastheniama, in the case of osteoporosis, myastheniama syndrome IV degree), in case of poliomyelitis (with the exception of the form of bulbar encephalitis), open-and-angle-closure glaucoma. If necessary, intra-articular administration should be used with caution in patients with general severe disease. The ineffectiveness (or short duration) of the 2 previous injections (taking into account the individual properties of the used GCS). Before and during the treatment of GCS, it is necessary to monitor the complete blood count, glycemia level and plasma electrolytes. During intercurrent infections, septic conditions and tuberculosis , simultaneous antibiotic therapy is necessary. The relative adrenal insufficiency caused by dexamethasone may persist for several months after its withdrawal. Given this, when stressful situations occur during this period, hormone therapy is resumed with the simultaneous appointment of salts and / or mineralocorticoids. When using dexamethasone in patients with herpes, the cornea should be borne in mind that it can be perforated. During treatment, it is necessary to control intraocular pressure and the state of the cornea. When dexamethasone is abruptly canceled, especially in the case of previous high doses, there is a so-called withdrawal syndrome (not caused by hypocorticism), manifested by anorexia, nausea, inhibition, generalized musculoskeletal pain, general weakness. After dexamethasone is canceled for a few months, relative adrenal insufficiency may persist. If during this period there are stressful situations, they are prescribed (if indicated) for the time of GCS, if necessary in combination with mineralocorticoids. In the period of treatment, control of blood pressure, water and electrolyte balance, pictures of peripheral blood and blood glucose levels, as well as observation of an oculist are required. during prolonged treatment, careful monitoring of the dynamics of growth and development is necessary.Children who were in contact with measles or chicken pox during the treatment period are prescribed specific immunoglobulins prophylactically.