Description of the drug dexamethasone. Instructions for use of dexamethasone solution - composition, indications and action. What does Dexamethasone help with?

1 ampoule (1 ml) contains:

active substance: dexamethasone sodium phosphate 4.4 mg (corresponding to 4.0 mg dexamethasone phosphate);

Excipients: methyl parahydroxybenzoate 1.5 mg, propyl parahydroxybenzoate 0.2 mg, sodium disulfite 1.0 mg, disodium edetate 1.0 mg, sodium hydroxide to pH 7.0-8.5, water for injection up to 1.0 ml.

Clear, colorless to light yellow solution.

Dexamethasone is a synthetic hormone of the adrenal cortex, a glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, anti-allergic, desensitizing, antishock, antitoxic and immunosuppressive action.

Interacts with specific cytoplasmic glucocorticosteroid receptors to form a complex that penetrates the cell nucleus and stimulates the synthesis of matrix ribonucleic acid, the latter inducing the formation of proteins, including lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation, allergies, etc.

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; enhances protein catabolism in muscle tissue.

Influence at lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of ​​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, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, which leads to the activation of gluconeogenesis.

Influence at water-electrolyte exchange: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, "washes" calcium from the bones, increases the excretion of calcium by the kidneys.

Anti-inflammatory action associated with inhibition of the release of inflammatory mediators by eosinophils; induction of the formation of lipocortin and a decrease in the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).

Antiallergic action develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils active substances, 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 production, changing the body's immune response.

In chronic obstructive pulmonary disease, the action is mainly based on inhibition of inflammatory processes, inhibition of development or prevention of mucosal edema, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, and inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of bronchial secretions by inhibiting or reducing its production.

Antishock And antitoxic action associated with an increase blood pressure(AD) (by increasing the concentration of circulating catecholamines and restoring the sensitivity of adrenoreceptors to them, as well as vasoconstriction), a decrease in permeability vascular wall, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

Immunosuppressive action due to inhibition of the release of cytokines (interleukin-1 and interleukin-2, gamma-interferon) from lymphocytes and macrophages. Suppresses the synthesis and release of adrenocorticotropic hormone (ACTH) by the pituitary gland and, secondarily, the synthesis of endogenous corticosteroids. It inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone. Suppresses the release of beta-lipotropin, but does not reduce the content of circulating beta-endorphin.

It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Increases the excitability of the central nervous system.

Reduces the number of lymphocytes and eosinophils, increases - erythrocytes (by stimulating the production of erythropoietins).

The peculiarity of the action is a significant inhibition of the function of the pituitary gland and practically complete absence mineralocorticoid activity. Doses of 1-1.5 mg/day inhibit the adrenal cortex; biological half-life (T 1/ 2) - 32-72 hours (duration of inhibition of the hypothalamic-pituitary-adrenal system).

Absorption

The maximum concentration of dexamethasone in plasma is reached within 5 minutes after intravenous administration and 1 hour after intramuscular administration.

Distribution

Communication with plasma proteins (mainly with albumins) - 77%. Penetrates through the blood-brain and placental barriers. Half-life (T 1/ 2) from plasma is 190 min.

Metabolism

Metabolized in the liver. A small amount of dexamethasone is metabolized in the kidneys and other organs.

breeding

Up to 65% of the dose is excreted by the kidneys within 24 hours, a small amount of dexamethasone passes into breast milk.

Replacement therapy for adrenal insufficiency (in combination with sodium chloride and / or mineralocorticosteroids): acute insufficiency bark adrenal glands (Addison's disease, bilateral adrenalectomy); relative adrenal insufficiency that develops after discontinuation of GCS treatment; primary or secondary insufficiency of the adrenal cortex.

Symptomatic and pathogenetic therapy of other diseases requiring the introduction of a fast-acting GCS, as well as in cases where oral administration of the drug is not possible:

- endocrine diseases: congenital hyperplasia of the adrenal cortex, subacute thyroiditis;

Shock (burn, traumatic, surgical, toxic) - with the ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;

Cerebral edema (only after confirmation of symptoms of increased intracranial pressure by the results of magnetic resonance or computed tomography caused by a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury);

Asthmatic status; severe bronchospasm (exacerbation of bronchial asthma);

- heavy allergic reactions, anaphylactic shock;

- rheumatic diseases;

Systemic connective tissue diseases; acute severe dermatoses;

Malignant diseases: palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; hypercalcemia in patients suffering from malignant tumors, when oral treatment is not possible;

Blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;

In ophthalmic practice (subconjunctival, retrobulbar or parabulbar administration): allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injury surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after corneal transplantation;

Local application (in the area of ​​pathological formation): keloids, discoid lupus erythematosus, granuloma annulare;

Poisoning with caustic fluids (the need to reduce inflammation and prevent cicatricial narrowing in case of poisoning with caustic fluids).

For short-term use for "vital" indications, the only contraindication is hypersensitivity to active ingredient or any other component of the drug;

- systemic mycoses;

- period breastfeeding;

- simultaneous use of live and attenuated vaccines with immunosuppressive doses of the drug.

With caution, the drug should be prescribed for the following diseases / conditions / risk factors:

Vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccinations. Immunodeficiency states (including AIDS or HIV infection).

Gastrointestinal diseases: peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.

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

Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, obesityIII- IV degree.

Severe chronic renal and / or liver failure, nephrourolithiasis.

Hypoalbuminemia and conditions predisposing to its occurrence.

Liver failure.

Systemic osteoporosis, myasthenia gravisgravity, poliomyelitis (with the exception of the form of bulbar encephalitis), epilepsy, "steroid" myopathy.

Acute psychosis, severe affective disorders (including history, especially "steroid" psychosis).

Open and closed angle glaucoma, eye herpes (risk of corneal perforation).

Pregnancy.

Elderly patients - due to the high risk of developing osteoporosis and arterial hypertension.

In children during the period of growth, the drug should be used only for absolute readings and under the close supervision of the attending physician.

Dexamethasone crosses the placenta and can reach high concentrations in the fetus. During pregnancy (especially in the first trimester) or in women planning a pregnancy, the drug is indicated if the expected therapeutic effect of the drug exceeds the risk negative influence on the mother or fetus. GCS should be prescribed during pregnancy only for absolute indications. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. 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.

A small amount of dexamethasone passes into breast milk.

If it is necessary to carry out treatment with the drug during breastfeeding, breastfeeding should be discontinued, as this may lead to a delay in the growth of the child and a decrease in the secretion of his endogenous corticosteroids.

The dosage regimen is individual and depends on the indications, the patient's condition and his response to therapy.

The drug is administered intravenously (in / in) slowly in a stream or drip (in acute and emergency conditions); intramuscularly (in / m); possibly also local (in pathological formation) and subconjunctival, retrobulbar or parabulbar administration.

In order to prepare a solution for intravenous infusion, an isotonic sodium chloride solution or a 5% glucose (dextrose) solution should be used.

The drug is administered intravenously and intramuscularly at a dose of 0.5-24 mg / day in 2 divided doses (equivalent to 1/3-1/2 oral dose) in the shortest possible course at the minimum effective dose, the treatment is canceled gradually. Long-term treatment should be carried out at a dose not exceeding 0.5 mg / day. V / m in the same place is injected no more than 2 ml of the solution.

In shock administered strictly in/in bolus at a dose of 2-6 mg/kg. If necessary, repeated doses are administered every 2 to 6 hours or as a long-term intravenous infusion at a dose of 3 mg/kg/day. Treatment with dexamethasone should be carried out as part of complex therapy shock. Application pharmacological doses permissible only in life-threatening conditions, and, as a rule, this time does not exceed 48 - 72 hours.

With cerebral edema an initial dose of 10 mg is administered intravenously, then 4 mg every 6 hours until relief of symptoms (usually within 12-24 hours). After 2-4 days, the dose is reduced and the use of the drug is gradually stopped over 5-7 days. Patients with malignant neoplasms maintenance treatment may be required - 2 mg intramuscularly or intravenously 2-3 times a day.

At acute edema brain spend short-term intensive care: for adults, the loading dose is 50 mg IV, then on days 1-3, 8 mg is administered every 2 hours, on the 4th day - 4 mg every 2 hours, on days 5-8 - 4 mg every 4 hours, further, the daily dose is reduced by 4 mg / day until it is completely canceled. For children weighing more than 35 kg, the loading dose is 25 mg IV, then on days 1-3, 4 mg is administered every 2 hours, on the 4th day - 4 mg every 4 hours, on days 5-8 - 4 mg every 6 hours, then the daily dose is reduced by 2 mg / day until it is completely canceled. For children weighing less than 35 kg, the loading dose is 20 mg IV, then on days 1-3, 4 mg is administered every 3 hours, on the 4th day - 4 mg every 6 hours, on days 5-8 - 2 mg every 6 hours, then the daily dose is reduced by 1 mg / day until it is completely canceled.

In acute self-limiting allergic reactions or exacerbation of chronic allergic diseases combined parenteral and oral administration dexamethasone: 1st day - iv 4-8 mg, 2-3 days - inside 1 mg 2 times a day, 4-5 days - inside 0.5 mg 2 times a day, 6-7 days - inside 0 .5 mg once. On the 8th day evaluate the effectiveness of therapy.

For emergencies used in higher doses: the initial dose is 4-20 mg, which is repeated until the desired effect is achieved, the total daily dose rarely exceeds 80 mg. After achieving a therapeutic effect, the drug is administered in doses of 2-4 mg as needed, followed by a gradual withdrawal of the drug. To maintain a long-term effect, the drug is administered every 3-4 hours or as a long-term drip infusion. After stopping acute conditions, the patient is transferred to taking the drug inside.

Doses of the drug for children (in / m):

The dose of the drug during replacement therapy (with adrenal insufficiency) is 0.0233 mg / kg of body weight or 0.67 mg / m 2 of body surface area, divided into 3 doses, every 3rd day or 0.00776-0, 01165 mg/kg body weight or 0.233-0.335 mg/m 2 body surface area daily.

Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenal insufficiency.

The frequency of development and severity of side effects depend on the duration of use and the size of the dose used.

Violations by endocrine system : decreased glucose tolerance, "steroidal" diabetes mellitus or manifestation of latent diabetes mellitus, adrenal suppression, Itsenko-Cushing's syndrome (moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, "steroidal" striae), delayed sexual development in children.

Gastrointestinal disorders : nausea, vomiting, pancreatitis, "steroid" gastric and duodenal ulcer, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups, abdominal pain, discomfort in the epigastric region. In rare cases, an increase in the activity of "liver" transaminases and alkaline phosphatase.

Heart disorders : arrhythmias, bradycardia (up to cardiac arrest), development (in predisposed patients) or aggravation of the severity of CHF, changes in the electrocardiogram characteristic of hypokalemia. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.

Vascular disorders : increased blood pressure, hypercoagulability, thrombosis, with a / in the introduction: "flushing" of blood to the face, vasculitis, increased capillary fragility.

Psychiatric disorders : delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, nervousness or anxiety, insomnia, emotional lability, suicidal tendencies.

Nervous System Disorders : increased intracranial pressure, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.

Violations of the organ of vision : sudden loss of vision parenteral administration in the head, neck, turbinates, scalp, crystals of the drug may be deposited in the vessels of the eye), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral infections eye, trophic changes in the cornea, exophthalmos, chemosis, ptosis, mydriasis, corneal perforation, central serous chorioretinopathy.

Metabolic and nutritional disorders : increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypercholesterolemia, epidural lipomatosis.

Caused by mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

Musculoskeletal and connective tissue disorders : growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), muscle tendon rupture, "steroid" myopathy, decreased muscle mass(atrophy).

Renal disorders and urinary tract : leukocyturia.

Skin and subcutaneous tissue disorders :delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, "steroid" acne, "steroid" striae, a tendency to develop pyoderma and candidiasis.

Violations by immune system : generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.

General disorders and disorders at the injection site : development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), "withdrawal" syndrome.

Local for parenteral administration : burning, numbness, pain, paresthesia and infection at the injection site; rarely - necrosis of surrounding tissues, scarring at the injection site; skin atrophy and subcutaneous tissue with i / m administration (especially dangerous is the introduction into the deltoid muscle).

With / in the introduction: arrhythmias, flushes of blood to the face, convulsions.

Symptoms: increased blood pressure, edema (peripheral), peptic ulcer, hyperglycemia, impaired consciousness.

Treatment: symptomatic, there is no specific antidote.

Dexamethasone is pharmaceutically incompatible with other medicines(LS) (may form insoluble compounds). It is recommended to administer it separately from other drugs (in / in bolus, or through another dropper, as a second solution). When mixing a solution of dexamethasone with heparin, a precipitate forms. increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of developing arrhythmias increases).

Accelerates the excretion of acetylsacililic acid, reduces the content of its metabolites in the blood (with the abolition of dexamethasone, the concentration of salicylates in the blood increases and the risk of side effects increases).

At simultaneous application with live antiviral vaccines and against the background of other types of immunizations increases the risk of virus activation and the development of infections.

Increases the metabolism of isoniazid, mexiletine (especially in "fast acetylators"), which leads to a decrease in their plasma concentrations.

Increases the risk of developing hepatotoxic effects of paracetamol (induction of liver enzymes and the formation of a toxic metabolite of paracetamol).

Increases (with prolonged therapy) the content of folic acid.

Hypokalemia caused by dexamethasone may increase the severity and duration of muscle blockade in the presence of muscle relaxants.

In high doses, it reduces the effect of somatropin.

Dexamethasone reduces the effect of hypoglycemic drugs; enhances the anticoagulant effect of coumarin derivatives.

Weakens the effect of the vitaminDon calcium absorption in the intestinal lumen. and parathyroid hormone prevent the development of osteopathy caused by dexamethasone.

Reduces the concentration of praziquantel in the blood.

Cyclosporine (inhibits metabolism) and (reduces clearance) increase toxicity.

Thiazide diuretics, carbonic anhydrase inhibitors, other corticosteroids and amphotericin B increase the risk of hypokalemia, sodium-containing drugs - edema and increased blood pressure.

Non-steroidal anti-inflammatory drugs (NSAIDs) and increase the risk of ulceration of the gastrointestinal mucosa and bleeding, in combination with NSAIDs for the treatment of arthritis, it is possible to reduce the dose of GCS due to the summation of the therapeutic effect.

In patients with diabetes mellitus, blood glucose concentrations should be monitored and, if necessary, doses of hypoglycemic drugs should be adjusted.

Dexamethasone may increase susceptibility or mask symptoms of infectious diseases. Chickenpox, measles, and other infections can be more severe and even lead to lethal outcome in non-immunized individuals. Immunosuppression often develops with long-term use of dexamethasone, but can also occur with short-term treatment.

Children who during the period of treatment were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically. Children during long-term treatment the drug requires careful monitoring of the dynamics of growth and development.

When using dexamethasone, there is a risk of developing severe anaphylactic reactions, bradycardia.

Against the background of drug therapy, the risk of activation of strongyloidiasis increases.

The dose of dexamethasone should be temporarily increased in stressful situations during therapy (surgery, trauma). A temporary increase in the dose of the drug in stressful situations is necessary both before and after stress.

During drug therapy, careful monitoring of the condition of patients with chronic heart failure, uncontrolled arterial hypertension, injuries and ulcerative lesions of the cornea, glaucoma is necessary.

May worsen the course of myasthenia gravis.

Taking the drug may mask the symptoms of "irritation of the peritoneum" in patients with perforation of the wall of the stomach or intestines.

Against the background of the use of GCS, a change in the mobility and number of spermatozoa is possible.

During the period of treatment, it is necessary to refrain from driving vehicles and other mechanisms that require increased concentration of attention and speed of psychomotor reactions.

Solution for injections, 4 mg/ml.

1.0 ml of the drug in dark glass ampoules. On 25 ampoules in a cellular cardboard lattice, on 1 lattice together with the application instruction in a cardboard pack.

5 ampoules in a plastic pallet, 5 pallets with instructions for use in a cardboard box. Information update date:   22.04.2017 Illustrated Instructions

GKS. Suppresses the functions of leukocytes and tissue macrophages.
Drug: DEXAMETHASONE
The active substance of the drug: dexamethasone
ATX encoding: H02AB02
KFG: GCS for injections
Registration number: P No. 014442/01-2002
Date of registration: 11.10.02
The owner of the reg. Credit: SHREYA LIFE SCIENCES Pvt.Ltd. (India)

Release form Dexamethasone (solution for injection), drug packaging and composition.

1 amp.

4 mg

1 ml - dark glass ampoules (25) - cardboard boxes.
1 ml - dark glass bottles (25) - cardboard boxes.

Solution for injection is clear, colorless or pale yellow.

1 ml
1 amp.
dexamethasone sodium phosphate (in terms of dexamethasone phosphate)
4 mg
8 mg

Excipients: methylparaben, propylparaben, sodium metabisulfite, disodium edetate, sodium hydroxide, water for injections.

2 ml - dark glass ampoules (25) - cardboard boxes.
2 ml - dark glass bottles (25) - cardboard boxes.

DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information provided is provided only for familiarization with the drug, you should consult a doctor about the possibility of using it.

Pharmacological action Dexamethasone (solution for injection)

GKS. Suppresses the functions 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 to the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to the release of histamine. Suppresses the activity of fibroblasts and the formation of collagen.

Inhibits the activity of phospholipase A2, which leads to 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 into the lymphoid tissue; inhibits the formation of antibodies.

Dexamethasone inhibits the release of pituitary ACTH and β-lipotropin, but does not reduce the level of circulating α-endorphin. Inhibits the secretion of TSH and FSH.

When applied directly 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 protein metabolism products. An increase in blood glucose stimulates the secretion of insulin.

Dexamethasone inhibits the uptake of glucose 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's syndrome are the main factors limiting long-term therapy with corticosteroids. As a result of the catabolic action, growth suppression in children is possible.

In high doses, dexamethasone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.

With systemic use, the therapeutic activity of dexamethasone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

With external and topical application The therapeutic activity of dexamethasone is due to anti-inflammatory, anti-allergic and anti-exudative (due to the vasoconstrictor effect) action.

By anti-inflammatory activity exceeds hydrocortisone by 30 times, does not have mineralocorticoid activity.

Pharmacokinetics of the drug.

Plasma protein binding - 60-70%. Penetrates through histohematic barriers. IN a small amount excreted in breast milk.

Metabolized in the liver.

T1 / 2 is 2-3 hours. Excreted by the kidneys.

When applied topically in ophthalmology, it is absorbed through the cornea with intact epithelium into the moisture of the anterior chamber of the eye. With inflammation of the tissues of the eye or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone significantly increases.

Indications for use:

For oral administration: Addison-Birmer disease; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; NUC; connective tissue diseases; autoimmune hemolytic anemia, thrombocytopenia, aplasia and hypoplasia of hematopoiesis, agranulocytosis, serum sickness; acute erythroderma, pemphigus (common), acute eczema(at the beginning of treatment); malignant tumors(as palliative therapy); congenital adrenogenital syndrome; cerebral edema (usually after preliminary parenteral administration of corticosteroids).

For parenteral administration: shock of various origins; cerebral edema (with a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); asthmatic status; severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction on medications, serum transfusion, pyrogenic reactions); acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; severe infectious diseases (in combination with antibiotics); acute insufficiency of the adrenal cortex; sharp croup; joint diseases (humeroscapular periarthritis, epicondylitis, styloiditis, bursitis, tendovaginitis, compression neuropathy, osteochondrosis, arthritis various etiologies, osteoarthritis).

For use in ophthalmic practice: non-purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharoconjunctivitis, blepharitis, episcleritis, scleritis, inflammation after eye injuries and surgical interventions, sympathetic ophthalmia.

Dosage and method of application of the drug.

Individual. Inside at serious illnesses at the beginning of treatment, up to 10-15 mg / day is prescribed, the maintenance dose can be 2-4.5 mg or more per day. The daily dose is divided into 2-3 doses. In small doses, take 1 time / day in the morning.

For parenteral administration, it is administered intravenously in a slow stream or drip (in acute and emergency conditions); i / m; periarticular and intraarticular administration is also possible. During the day, you can enter from 4 to 20 mg of dexamethasone 3-4 times. The duration of parenteral use is usually 3-4 days, then they switch to maintenance therapy with an oral form. In the acute period various diseases and at the beginning of treatment, dexamethasone is used at higher doses. When the effect is achieved, the dose is reduced at intervals of several days until a maintenance dose is reached or until treatment is stopped.

When used in ophthalmology in acute conditions, 1-2 drops are instilled into the conjunctival sac every 1-2 hours, then, with a decrease in inflammation, every 4-6 hours. The duration of treatment is from 1-2 days to several weeks, depending on the clinical course diseases.

Side effects Dexamethasone (solution for injection):

On the part of the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing's syndrome (moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, myasthenia gravis, striae), delay sexual development in children.

From the side of metabolism: increased excretion of calcium ions, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.

From the side of the central nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.

From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle; with intracranial administration - nosebleeds.

From the digestive system: nausea, vomiting, pancreatitis, steroid stomach ulcer and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups; rarely - increased activity of hepatic transaminases and alkaline phosphatase.

From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.

From the side musculoskeletal system: growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely, pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, steroid myopathy, decreased muscle mass (atrophy).

Dermatological reactions: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, a tendency to develop pyoderma and candidiasis.

Allergic reactions: generalized (skin rash, skin itching, anaphylactic shock) and topical application.

Effects associated with immunosuppressive action: the development or exacerbation of infections (the appearance of this side effect is promoted by jointly used immunosuppressive drugs and vaccination).

Local reactions: with parenteral administration - tissue necrosis.

For external use: rarely - itching, hyperemia, burning, dryness, folliculitis, acne, hypopigmentation, perioral dermatitis, allergic dermatitis, skin maceration, secondary infection, skin atrophy, stretch marks, prickly heat. With prolonged use or application to large areas of the skin, systemic side effects characteristic of GCS may develop.

Contraindications to the drug:

For short-term use for health reasons - hypersensitivity to dexamethasone.

For intra-articular injection and injection directly into the lesion: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including history), as well as common infectious disease, severe periarticular osteoporosis, no signs of inflammation in the joint (“dry” joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of the joint joint of the epiphyses of bones.

For external use: bacterial, viral, fungal skin diseases, tuberculosis of the skin, skin manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), childhood(up to 2 years, with itching in the anus - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.

For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculous eye damage, violation of the integrity of the eye epithelium, acute purulent eye infection in the absence of specific therapy, corneal diseases, combined with epithelial defects, trachoma, glaucoma.

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, the possibility of fetal growth disorders is not excluded. 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.

Special instructions for use Dexamethasone (solution for injection).

Use with caution for 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency states (including AIDS or HIV infection).

Use with caution in diseases of the gastrointestinal tract: peptic ulcer stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.

Use with caution in diseases of the cardiovascular system, incl. after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, the focus of necrosis may spread, slowing down the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, arterial hypertension, hyperlipidemia), with endocrine diseases — diabetes(including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and / or hepatic insufficiency, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV degree), with poliomyelitis (with the exception of the form of bulbar encephalitis), open- and angle-closure glaucoma.

If intra-articular administration is necessary, use with caution in patients with general serious condition, inefficiency (or short duration) of the action of 2 previous injections (taking into account the individual properties of the used GCS).

Before starting and during GCS therapy, it is necessary to control the complete blood count, glycemia and plasma electrolytes.

With intercurrent infections, septic conditions and tuberculosis, simultaneous antibiotic therapy is necessary.

Dexamethasone-induced relative adrenal insufficiency may persist for several months after its withdrawal. Given this, in stressful situations that occur during this period, hormonal therapy is resumed with the simultaneous administration of salts and / or mineralocorticoids.

When using dexamethasone in patients with corneal herpes, the possibility of corneal perforation should be borne in mind. During treatment, it is necessary to control intraocular pressure and the condition of the cornea.

With the sudden cancellation of dexamethasone, especially in the case of previous use in high doses, the so-called withdrawal syndrome occurs (not due to hypocorticism), manifested by anorexia, nausea, lethargy, generalized musculoskeletal pain, and general weakness. After the abolition of dexamethasone, relative insufficiency of the adrenal cortex may persist for several months. If stressful situations arise during this period, they are prescribed (according to indications) for the time of GCS, if necessary, in combination with mineralocorticoids.

During the period of treatment, control of blood pressure, water and electrolyte balance, peripheral blood patterns and glycemic levels, as well as observation by an oculist is required.

In children during long-term treatment, careful monitoring of the dynamics of growth and development is necessary. Children who during the period of treatment were in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.

Interaction of Dexamethasone (solution for injection) with other drugs.

When used simultaneously with antipsychotics, bucarban, azathioprine there is a risk of developing cataracts; with agents that have an anticholinergic effect - the risk of developing glaucoma.

With simultaneous use with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs decreases.

When used simultaneously with hormonal contraceptives, androgens, estrogens, anabolic steroids are possible hirsutism, acne.

With simultaneous use with diuretics, it is possible to increase the excretion of potassium; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

With simultaneous use with oral anticoagulants, the anticoagulant effect may be weakened.

With simultaneous use with cardiac glycosides, the tolerability of cardiac glycosides may worsen due to potassium deficiency.

With simultaneous use with aminoglutethimide, a decrease or inhibition of the effects of dexamethasone is possible; with carbamazepine - a decrease in the effect of dexamethasone is possible; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - a decrease in the concentration of imatinib in blood plasma is possible due to the induction of its metabolism and increased excretion from the body.

With simultaneous use with itraconazole, the effects of dexamethasone are enhanced; with methotrexate - possibly increased hepatotoxicity; with praziquantel - a decrease in the concentration of praziquantel in the blood is possible.

With simultaneous use with rifampicin, phenytoin, barbiturates, it is possible to weaken the effects of dexamethasone due to an increase in its excretion from the body.