Dexamethasone, pills 0.5 mg, 10 pcs.

Composition

For 1 tablet:Active ingredient:Dexamethasone 0.50 mg, Excipients:lactose monohydrate, pregelatinized starch, colloidal silicon dioxide, magnesium stearate.

Pharmacological action

Pharmacotherapeutic group: Glucocorticosteroid ATX code: H02AB02 Pharmacological Propertiespharmacodynamicadexamethasone is a synthetic glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone, inhibits the release of interleukin-1 and interleukin-2, interferon gamma from lymphocytes and macrophages. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, antitoxic and immunosuppressive effects. It suppresses the release of adrenocorticotropic hormone (ACTH) and beta-lipotropin by the pituitary gland, but does not reduce the content of circulating beta-endorphin. It inhibits the secretion of thyroid-stimulating hormone (TSH) and follicle-stimulating hormone (FSH). Increases the excitability of the central nervous system (CNS), reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (stimulates the production of erythropoietins). It interacts with specific cytoplasmic receptors, forms a complex that penetrates the cell nucleus, and stimulates the synthesis of matrix ribonucleic acid (mRNA), which induces the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid, and suppresses the synthesis of endoperoxides, prostaglandins (Pg), and leukotrienes, which contribute to the processes of inflammation, allergies, and others. Effect on protein metabolism: reduces the amount of protein in plasma (due to globulins) with an increase in the albumin / globulin ratio, increases the synthesis of albumins in the liver and kidneys, increases protein catabolism in muscle tissue. Effect on lipid metabolism: increases the synthesis of higher fatty acids and triglycerides( TG), redistributes fat (accumulation of fat mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia. Effect on carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT), increases the activity of glucose-6-phosphatase, leading to increased glucose intake from the liver to the blood, increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, leading to activation of gluconeogenesis. Effect on water and electrolyte metabolism: detains sodium (Na+) ions and water in the body, stimulates the excretion of potassium (K+) ions (mineralocorticosteroid (MCS) activity), reduces the absorption of calcium (Ca2+) ions from the gastrointestinal tract, “washes” Ca2+ from the bones, increases the excretion of Ca2+ by the kidneys. The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils, induction of lipocortin formation and a decrease in the number of mast cells producing hyaluronic acid, with a decrease in capillary permeability, stabilization of cell membranes and organelle membranes (especially lysosomal). The anti-allergic effect develops as a result of suppressing the synthesis and secretion of allergy mediators, inhibiting the release of histamine and other biologically active substances from sensitized mast cells and basophils, reducing the number of circulating basophils, suppressing the development of lymphoid and connective tissue, reducing the number of T – and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, and changing the body’s immune response. In chronic obstructive pulmonary disease (COPD), the action is mainly based on inhibiting inflammatory processes, inhibiting the development or prevention of mucosal edema, inhibiting eosinophilic infiltration of the submucosal layer of the bronchial epithelium, depositing circulating immune complexes in the bronchial mucosa, as well as inhibiting erosion and desquamation of the mucous membrane. Increases the sensitivity of small and medium-sized bronchial beta-adrenergic receptors to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of bronchial secretions by inhibiting or reducing its production. Anti-shock and antitoxic effects are associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and restoration of sensitivity of adrenoreceptors to them, as well as vasoconstriction), a decrease in vascular wall permeability, membrane – protective properties, and activation of liver enzymes involved in the metabolism of endo-and xenobiotics. The immunosuppressive effect is caused by inhibition of the release of cytokines (interleukin-1, interleukin-2, interferon gamma) from lymphocytes and macrophages. Inhibits the synthesis and secretion of ACTH, and secondarily-the synthesis of endogenous corticosteroids. It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation. The peculiarity of the action is a significant inhibition of pituitary function and almost complete absence of MCS activity. Doses of 1-1.5 mg / day inhibit the adrenal cortex, the biological half-life (T1 / 2) is 32-72 hours (the duration of suppression of the hypothalamic-pituitary-adrenal cortex system). According to the strength of glucocorticosteroid activity,0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone( or prednisone),15 mg of hydrocortisone, or 17.5 mg of cortisone. Pharmacokineticsabsorption After oral administration is rapidly and completely absorbed, the maximum concentration of dexamethasone in blood plasma is 1-2 hours. Distribution In blood plasma binds (60-70%) to a specific carrier protein-transcortin. It easily passes through histohematic barriers (including the blood-brain and placental barriers). Metabolismmetabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. Excretion is eliminated by the kidneys (a small amount of dexamethasone passes into breast milk). The elimination half-life is 3-5 hours.

Indications

From the endocrine system: replacement therapy for primary and secondary (pituitary) adrenal insufficiency, congenital adrenal hyperplasia, subacute thyroiditis and severe forms of post-radiation thyroiditis. Rheumatic diseases: rheumatoid arthritis (including juvenile chronic arthritis) and extra-articular lesions in rheumatoid arthritis (lungs, heart, eyes, cutaneous vasculitis).

Systemic connective tissue diseases, vasculitis and amyloidosis(in combination therapy): systemic lupus erythematosus (treatment of polyserositis and internal organ damage), Sjogren’s syndrome (treatment of lung, kidney and brain damage), systemic sclerosis (treatment of myositis, pericarditis and alveolitis), polymyositis, dermatomyositis, systemic vasculitis, amyloidosis (replacement therapy for adrenal insufficiency), scleroderma.

Skin diseases: pemphigoid, bullous dermatitis, herpetiform dermatitis, exfoliative dermatitis, exudative erythema (severe forms), erythema nodosum, seborrheic dermatitis (severe forms), psoriasis (severe forms), lichen, fungal mycoses, Quincke’s edema, bronchial asthma, contact dermatitis, atopic dermatitis, serum sickness, allergic rhinitis, drug-induced illness (hypersensitivity to medications), urticaria after blood transfusion, systemic immune diseases (sarcoidosis, temporal arteritis).

Eye diseases: proliferative changes in the orbit (endocrine ophthalmopathy, pseudotumors), sympathetic ophthalmia, immunosuppressive therapy in corneal transplantation.

Diseases of the gastrointestinal tract: ulcerative colitis (severe exacerbations), Crohn’s disease (severe exacerbations), chronic autoimmune hepatitis, rejection reaction after liver transplantation.

Blood diseases: congenital or acquired acute pure aplastic anemia, autoimmune hemolytic anemia, secondary thrombocytopenia in adults, erythroblastopenia, acute lymphoblastic leukemia (induction therapy), myelodysplastic syndrome, angioimmunoblastic malignant T-cell lymphoma (in combination with cytostatics), plastocytoma (in combination with cytostatics), anemia after myelofibrosis with myeloid fibrosis metaplasia or lymphoplasmacytoid immunocytoma, systemic histiocytosis (systemic process).

Kidney diseases: primary and secondary glomerulonephritis (Goodpasture syndrome), kidney damage in systemic connective tissue diseases (systemic lupus erythematosus, Sjogren’s syndrome), systemic vasculitis (usually in combination with cyclophosphamide), glomerulonephritis in polyarteritis nodosa, Charg-Strauss syndrome, Wegener’s granulomatosis of Schonlein-Henoch purpura, mixed cryoglobulinemia, kidney damage in arteritis Takayasu, interstitial nephritis, immunosuppressive therapy after kidney transplantation, induction of diuresis or reduction of proteinemia in idiopathic nephrotic syndrome (without uremia) and in kidney damage associated with systemic lupus erythematosus.

Malignant diseases: palliative therapy of leukemia and lymphoma in adults, acute leukemia in children, hypercalcemia in malignant neoplasms.

Other indications: tuberculosis meningitis with subarachnoid block (in combination with adequate antitubercular therapy), trichinosis with neurological or myocardial manifestations.

Contraindications

For short-term use for “vital” indications, the only contraindication is hypersensitivity to the Active ingredient or auxiliary components of the drug.

The drug is contraindicated in patients with galactosemia, lactase deficiency and glucose-galactose malabsorption syndrome, due to the fact that the drug contains lactose.

With caution.Parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transmitted, including recent contact with the patient) – herpes simplex, herpes zoster (viremic phase), chickenpox, measles; amoebiasis, strongyloidosis (established or suspected); systemic mycosis; active and latent tuberculosis, pre – and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after vaccination BCG, immunodeficiency conditions (including AIDS or HIV infection).

Diseases of the gastrointestinal tract:peptic ulcer of the stomach and duodenum 12, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.

Diseases of the cardiovascular system, including recent myocardial infarction (in patients with acute and subacute myocardial infarction, necrosis may spread, scar tissue formation may slow down and, as a result, rupture of the heart muscle), decompensated chronic heart failure, arterial hypertension, hyperlipidemia.

Endocrine diseases:diabetes mellitus (including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko-Cushing’s disease.

Severe chronic renal and / or hepatic insufficiency, nephrourolithiasis; hypoalbuminemia and conditions predisposing to its occurrence; systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (grade III-IV), polio (except for the form of bulbar encephalitis), open-angle and closed-angle glaucoma, lactation.

Side effects

From the immune system: infrequently – hypersensitivity reactions, decreased immune response, and increased susceptibility to infections.

From the endocrine system: often – transient adrenal insufficiency, growth retardation in children and adolescents, adrenal insufficiency and atrophy (reduced stress response), Itsenko-Cushing syndrome, menstrual cycle disorders, hirsuitism, transition from latent diabetes mellitus to clinically manifest, increased need for insulin or oral hypoglycemic medications in patients with diabetes, sodium and water retention, increased potassium loss; very rarely – hypokalemic alkalosis, negative nitrogen balance due to protein catabolism.

Metabolic and nutritional disorders: often – reduced tolerance to carbohydrates, increased appetite and weight gain, obesity; infrequently-hypertriglyceridemia.

Nervous system disorders: often-mental disorders; infrequently-edema of the papillae of the optic nerve and increased intracranial pressure (pseudotumor 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).

From the side of the senses: infrequently – posterior subcapsular cataract, increased intraocular pressure, tendency to develop secondary bacterial, fungal or viral infections of the eye, trophic changes in the cornea, exophthalmos.

From the cardiovascular system: infrequently-arterial hypertension, hypertensive encephalopathy; very rarely-polyfocal ventricular extrasystoles, transient bradycardia, heart failure, myocardial rupture after a recent acute infarction.

From the side of the skin: often-erythema, thinning and fragility of the skin, delayed wound healing, striae, petechiae and ecchymosis, increased sweating, steroid acne, suppression of the skin reaction during allergic tests; very rarely-angineurotic edema, allergic dermatitis, urticaria.

From the musculoskeletal system: often-muscle atrophy, osteoporosis, muscle weakness, steroid myopathy (muscle weakness due to catabolism of muscle tissue); infrequently-aseptic bone necrosis; very rarely-vertebral compression fractures, tendon tears (especially with the combined use of certain quinolones), damage to articular cartilage and bone necrosis (associated with frequent intra-articular injections).

From the hematopoietic system: rarely-thromboembolic complications, decreased monocyte and/or lymphocyte count, leukocytosis, eosinophilia (as with other glucocorticosteroids), thrombocytopenia and non-thrombocytopenic purpura.

Allergic reactions: rarely – skin rash, pruritus, angioedema, bronchospasm, anaphylactic shock.

From the genitourinary system: rarely-impotence.

Interaction

Concomitant use of dexamethasone and nonsteroidal anti-inflammatory drugs (NSAIDs) increases the risk of developing and forming gastrointestinal ulcers.

The effect of dexamethasone decreases with the simultaneous use of inducers of the SURZA 4 isoenzyme (for example, phenytoin, phenobarbitone, carbamazepine, primidone, rifabutin, rifampicin) or drugs that increase the metabolic clearance of glucocorticoids (ephedrine and aminoglutetimide); in such cases, the dose of dexamethasone should be increased.

Interactions between dexamethasone and the above drugs may distort the results of dexamethasone suppression tests. If dexamethasone tests are to be performed during therapy with one of the listed drugs, this interaction should be taken into account when interpreting the test results.

Concomitant use of dexamethasone and inhibitors of the SURZA 4 isoenzyme (for example, ketoconazole, macrolide antibiotics) may lead to an increase in the concentration of dexamethasone in the blood.

Concomitant use of drugs that are metabolized by SURZA 4 (for example, indinavir, erythromycin) may increase their clearance, which may be accompanied by a decrease in their serum concentrations.

Dexamethasone reduces the effectiveness of hypoglycemic drugs, antihypertensive drugs, praziquantel and natriuretics (it is necessary to increase the dose of these drugs); increases the activity of heparin, albendazole and potassium-sparing diuretics (if necessary, the dose of these drugs is reduced).

Dexamethasone may alter the effect of coumarin anticoagulants, so more frequent monitoring of prothrombin time is recommended during therapy. Antacids reduce the absorption of dexamethasone in the stomach. Smoking does not affect the pharmacokinetics of dexamethasone.

With simultaneous use of oral contraceptives, the T1/2 of glucocorticosteroids may increase, with a corresponding increase in their biological effects and an increase in the frequency of adverse side effects.

Simultaneous use of ritodrin and dexamethasone during labor is contraindicated, since this can lead to the death of the mother due to pulmonary edema. Concomitant use of dexamethasone and thalidomide may cause toxic epidermal necrolysis.

Potential, therapeutically beneficial interactions: concomitant use of dexamethasone and metoclopramide, diphenhydramine, prochlorperazine or 5-HT3 receptor antagonists (serotonin or 5-hydroxytryptamine type 3 receptors), such as ondansetron or granisetron, is effective in preventing nausea and vomiting caused by chemotherapy (cisplatin, cyclophosphamide, methotrexate, fluorouracil).

How to take, course of administration and dosage

Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, tolerability of the drug and the patient’s response to the therapy.

The recommended starting dose for adults is 0.5 mg to 9 mg / day.

The usual maintenance dose is 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 the therapeutic effect is achieved, the dose is gradually reduced (usually by 0.5 mg every 3 days until the maintenance dose is reached).

With prolonged use of high doses inside, the drug is recommended to be taken with meals, and in the intervals between meals, antacids should be taken. The duration of use of dexamethasone depends on the nature of the pathological process and the effectiveness of treatment and ranges from several days to several months or more. Treatment is stopped gradually (at the end, several corticotropin injections are prescribed).

• for bronchial asthma, rheumatoid arthritis, ulcerative colitis-1.5-3 mg / day;
• for systemic lupus erythematosus-2-4.5 mg/day;
• for oncohematological 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 day-inside,4 mg 2 times a day; 5,6 day-4 mg / day, inside; 7 day-drug withdrawal.

Dosage in children

Children (depending on their age) are prescribed 2.5-10 mg / m2 of body surface area/, dividing the daily dose into 3-4 doses.

Diagnostic tests for hyperfunction of the adrenal cortex

Short 1-mg dexamethasone test: 1 mg dexamethasone orally at 11: 00. ; blood sampling for serum cortisol determination at 8: 00 the next day.

Special 2-day test with 2 mg dexamethasone: 2 mg dexamethasone orally every 6 hours for 2 days; daily urine is collected to determine the concentration of 17-hydroxycorticosteroids.

Overdose

A single application of a large number of tablets does not lead to clinically significant intoxication.

Symptoms: possible increase in dose-dependent side effects. In this case, the dose of the drug should be reduced.

Treatment: supportive and symptomatic treatment.

There is no specific antidote.

Hemodialysis is ineffective.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C, in the original packaging

Shelf life

5 years

Active ingredient

Dexamethasone

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Blepharitis, Cancer, Eczema, Inflammatory Eye Diseases, Infectious Diseases, Conjunctivitis, Dermatosis, Rheumatoid Arthritis, Bronchospasm, Allergies, Iridocyclitis

Weight

Weight: 17 gr.