GCS for oral administration
Active substance
Release form, composition and packaging
10 pieces. - contour cell packaging (1) - cardboard packs.
10 pieces. - dark glass bottles (1) - cardboard packs.
pharmachologic effect
Glucocorticosteroid (GCS) - a methylated derivative of fluoroprednisolone, inhibits the release of interleukin-1 and interleukin-2, gamma from lymphocytes and macrophages. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, anti-toxic and immunosuppressive effects.
Suppresses the release of adrenocorticotropic hormone (ACTH) and beta-lipotropin by the pituitary gland, but does not reduce the content of circulating beta-endorphin. 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 erythrocytes (stimulates the production of erythropoietins).
Interacts with specific cytoplasmic receptors, forms a complex that penetrates into the cell nucleus, stimulates the synthesis of mRNA, which induces the formation of proteins, incl. lipocortin, which mediate cellular effects. Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the synthesis of endoperoxides, Pg, leukotrienes, which promote inflammation, allergies, etc.
Protein metabolism: reduces the amount of protein in (due to globulins) with an increase in the albumin / globulin ratio, increases the synthesis of albumin in the liver and kidneys; enhances protein catabolism in muscle tissue.
Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides (TG), redistributes fat (fat accumulation mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract (GIT); increases the activity of glucose-6-phosphatase, leading to an increase in the flow from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, leading to the activation of gluconeogenesis.
Water-electrolyte exchange: detains Na + and water in the body, stimulates the excretion of K + (MCS activity), reduces the absorption of Ca2 + from the gastrointestinal tract, "flushes" 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; inducing the formation of lipocortin and decreasing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and membranes of organelles (especially lysosomal).
The effect 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, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells , decrease in the sensitivity of effector cells to allergy mediators, inhibition of antibody production, changes in the body's immune response.
In chronic obstructive pulmonary disease (COPD), the action is mainly based on inhibition of inflammatory processes, inhibition of the development or prevention of edema of the mucous membranes, inhibition of eosinophilic infiltration of the submucous layer of the bronchial epithelium, deposition of circulating immune complexes in the mucous membrane of the bronchi, as well as inhibition of erosion and desquamation ... Increases the sensitivity of beta-adrenergic receptors of the bronchi of small and medium caliber to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.
The anti-shock and antitoxic effect is associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in vascular wall permeability, membrane-protective properties, activation of liver enzymes involved in the metabolism of endo- and xenobiotics.
The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin1, interleukin2; interferon gamma) from lymphocytes and macrophages.
Suppresses the synthesis and secretion of ACTH, and secondarily - the synthesis of endogenous GCS. It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
A feature of the action is a significant inhibition of the function of the pituitary gland and an almost complete absence of ISS activity. Doses of 1-1.5 mg / day inhibit the adrenal cortex; biological T 1/2 - 32-72 hours (duration of inhibition of the hypothalamus-pituitary-adrenal cortex).
In terms of the strength of glucocorticosteroid activity, 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or), 15 mg of hydrocortisone, or 17.5 mg of cortisone.
Pharmacokinetics
Dexamethasone is rapidly and almost completely absorbed after oral administration. The bioavailability of dexamethasone tablets is approximately 80%. C max in blood plasma and the maximum effect after oral administration is achieved in 1-2 hours; after taking a single dose, the effect persists for about 2.75 days.
In blood plasma, approximately 77% of dexamethasone binds to proteins, mainly to. A small amount of dexamethasone binds to non-albumin proteins. Dexamethasone is a fat-soluble substance that can penetrate into extra- and intracellular spaces. In the central nervous system (hypothalamus, pituitary gland), its effects are due to binding to membrane receptors. In peripheral tissues, it binds to cytoplasmic receptors. Its disintegration occurs at the place of its action, i.e. in a cage. It is metabolized mainly in the liver to the formation of inactive metabolites. It is excreted by the kidneys.
Indications
replacement therapy of primary and secondary (pituitary) adrenal insufficiency, congenital adrenal hyperplasia, subacute thyroiditis and severe forms of postradiation 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 (as part of combination therapy): systemic lupus erythematosus (treatment of polyserositis and lesions of internal organs), Sjogren's syndrome (treatment of lesions of the lungs, kidneys and brain), systemic sclerosis (treatment of myositis, pericarditis and alveolitis), polymyositis, dermatomyositis, systemic vasculitis, amyloidosis (replacement therapy for adrenal insufficiency ), scleroderma.
Skin diseases: pemphigoid, bullous dermatitis, dermatitis herpetiformis, exfoliative dermatitis, exudative erythema (severe forms), erythema nodosum, seborrheic dermatitis (severe forms), psoriasis (severe forms), lichen, fungoid mycoses, Quincke's edema, bronchial asthma, atrial dermatitis , serum sickness, allergic rhinitis, drug disease (hypersensitivity to drugs), 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.
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), in combination with cytostatics), , anemia after myelofibrosis with myeloid metaplasia or lymphoplasmacytoid immunocytoma, systemic histiocytosis (systemic process).
Kidney disease: primary and secondary glomerulonephritis (Goodpasture's syndrome), kidney damage in systemic connective tissue diseases (systemic lupus erythematosus, Sjögren's syndrome), systemic vasculitis (usually in combination with cyclophosphamide), glomerulonephritis in polyarteritis nodosa, Churg-Strauss syndrome, Wegener purpureis granulomatosis Genocha, mixed cryoglobulinemia, kidney damage in Takayasu's arteritis, interstitial nephritis, immunosuppressive therapy after kidney transplantation, induction of diuresis or reduction of proteinemia in idiopathic nephrotic syndrome (without uremia) and 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: tuberculous meningitis with subarachnoid blockade (in combination with adequate anti-tuberculosis therapy), trichinosis with neurological or myocardial manifestations.
Contraindications
For short-term use for "vital" indications, the only contraindication is hypersensitivity to the active substance or auxiliary components of the drug.
A drug Dexamethasone contraindicated in patients with galactosemia, lactase deficiency and glucose-galactose malabsorption syndrome, due to the fact that the drug contains lactose.
Diseases of the gastrointestinal tract: peptic ulcer and 12 duodenal ulcer, 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, incl. recent myocardial infarction (in patients with acute and subacute myocardial infarction, it is possible to spread the focus of necrosis, slow down the formation of scar tissue and, as a result, rupture of the heart muscle), decompensated chronic heart failure, arterial hypertension, hyperlipidemia.
Endocrine diseases: diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease.
Severe chronic renal and / or hepatic failure, nephrourolithiasis; hypoalbuminemia and conditions that predispose to its occurrence; systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV stage), poliomyelitis (except for the form of bulbar encephalitis), open-angle and closed-angle glaucoma, lactation period.
Dosage
Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, the tolerance of the drug and the patient's response to the therapy.
Regular supportive dose - from 0.5 mg to 3 mg / day.
Minimally effective the daily dose is 0.5-1 mg.
Maximum daily the 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 a 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, it is necessary to take antacids. The duration of the 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 injections of corticotropin are prescribed).
- at bronchial asthma, rheumatoid arthritis, ulcerative colitis - 1.5-3 mg / day;
- at systemic lupus erythematosus - 2-4.5 mg / day;
- at 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; Day 2 - by mouth, 4 mg 3 times a day; 3, 4 days - by mouth, 4 mg 2 times a day; 5, 6 days - 4 mg / day, inside; Day 7 - drug withdrawal.
Dosing in children
Children (depending on age) are prescribed 2.5-10 mg / m 2 body surface area / day, dividing the daily dose into 3-4 doses.
Diagnostic tests for hyperfunction of the adrenal cortex
Short 1mg Dexamethasone Test: 1 mg dexamethasone orally at 11.00; blood sampling for determination of serum cortisol at 8.00 the next day.
Special 2-day test with 2 mg dexamethasone: 2 mg dexamethasone by mouth every 6 hours for 2 days; 24-hour urine is collected to determine the concentration of 17-hydroxycorticosteroids.
Side effects
Classification of the incidence of side effects (WHO): very often\u003e 1/10, often from\u003e 1/100 to< 1/10, нечасто от > 1/1000 to< 1/100, редко от >1/10000 to< 1/1000, очень редко от < 1/10000, включая отдельные сообщения.
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 (decreased response to stress), Itsenko-Cushing syndrome, menstrual irregularities, hirsutism, transition of latent diabetes mellitus to clinically manifest, increased need for insulin or oral hypoglycemic drugs in patients with diabetes mellitus, sodium and water retention, increased potassium loss; very rarely - hypokalemic alkalosis, negative nitrogen balance due to protein catabolism.
Metabolic and nutritional disorders: often - decreased carbohydrate tolerance, increased appetite and weight gain, obesity; infrequently - hypertriglyceridemia.
From the nervous system: 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, stomach or duodenal ulcers; very rarely - esophagitis, perforation of ulcers 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 senses: infrequently - posterior subcapsular cataract, increased intraocular pressure, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.
On the part of 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, excessive sweating, steroid acne, suppression of skin reactions during allergological tests; very rarely - angioedema, allergic dermatitis, urticaria.
From the side of the musculoskeletal system: often - muscle atrophy, osteoporosis, muscle weakness, steroid myopathy (muscle weakness due to muscle tissue catabolism); infrequently - aseptic bone necrosis; very rarely - compression fractures of the vertebrae, tendon ruptures (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, a decrease in the number of monocytes and / or lymphocytes, leukocytosis, eosinophilia (as in other glucocorticosteroids), thrombocytopenia and non-thrombocytopenic purpura.
Allergic reactions: rarely - skin rash, itching, angioedema, bronchospasm, anaphylactic shock.
From the genitourinary system: rarely - impotence.
Signs and symptoms of glucocorticosteroid withdrawal syndrome
If a patient who has been taking glucocorticosteroids for a long time, quickly reduce the dose of the drug, signs of adrenal insufficiency, arterial hypotension, and death may develop.
In some cases, withdrawal symptoms may be similar to symptoms and signs of exacerbation or recurrence of the disease for which the patient is being treated. With the development of severe adverse events, drug treatment Dexamethasone should be terminated.
Overdose
A single use of a large number of tablets does not lead to clinically significant intoxication.
Symptoms: possibly increased dose-related side effects. In this case, the dose of the drug should be reduced.
Treatment: supportive and symptomatic.
There is no specific antidote.
Hemodialysis is ineffective.
Drug interactions
The simultaneous use of dexamethasone and non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of developing and forming ulcers of the gastrointestinal tract.
The effect of dexamethasone is reduced with the simultaneous use of inducers of the CYP3A4 isoenzyme (for example, phenytoin, phenobarbitone, carbamazepine, primidone, rifabutin, rifampicin) or drugs that increase the metabolic clearance of glucocorticoids (ephedrine and aminoglutethimide); in such cases, it is necessary to increase the dose of dexamethasone.
Interaction between dexamethasone and the above drugs can distort the results of dexamethasone suppression tests. If tests with dexamethasone are to be performed during therapy with one of the listed drugs, this interaction should be considered when interpreting the test results.
The simultaneous use of dexamethasone and inhibitors of the isoenzyme CYP3A4 (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 CYP3A4 (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, reduce the dose of these drugs).
Dexamethasone can change the effect of coumarin anticoagulants, therefore, 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 the simultaneous use of oral contraceptives, T 1/2 of glucocorticosteroids may increase, with a corresponding increase in their biological effects and an increase in the frequency of adverse side effects.
The simultaneous use of ritodrin and dexamethasone during labor is contraindicated, since this can lead to the death of the mother due to pulmonary edema. The combined use of dexamethasone and thalidomide can cause toxic epidermal necrolysis.
Potential, therapeutically beneficial interactions:the simultaneous use of dexamethasone and metoclopramide, diphenhydramine, prochlorperazine, or 5-HT 3 receptor antagonists (serotonin or 5-hydroxytryptamine receptors type 3), such as ondansetron or granisetron, is effective in the prevention of nausea and vomiting caused by chemotherapy, cyclophosphoidomine, cyclophthalmicide ).
special instructions
In patients requiring long-term dexamethasone therapy, after stopping therapy, a "withdrawal" syndrome (also without clear signs of adrenal insufficiency) may develop: fever, nasal discharge, conjunctival hyperemia, headache, dizziness, drowsiness and irritability, muscle and joint pain , vomiting, weight loss, weakness, convulsions. Therefore, dexamethasone should be discontinued by gradual dose reduction. Rapid withdrawal of the drug can be fatal.
In patients receiving long-term therapy with dexamethasone and exposed to stress after its withdrawal, it is necessary to resume the use of dexamethasone, due to the fact that induced adrenal insufficiency can persist for several months after drug withdrawal.
Dexamethasone therapy can mask signs of existing or new infections and signs of bowel perforation in patients with ulcerative colitis. Dexamethasone can aggravate the course of systemic fungal infections, latent amoebiasis, or pulmonary tuberculosis.
For patients with acute pulmonary tuberculosis, dexamethasone can be prescribed (together with anti-tuberculosis drugs) only in the case of a fulminant or severe disseminated process. Patients with inactive pulmonary tuberculosis receiving therapy with dexamethasone, or patients with positive tuberculin tests, should simultaneously receive anti-tuberculosis chemoprophylaxis.
Patients with osteoporosis, arterial hypertension, heart failure, tuberculosis, glaucoma, hepatic or renal failure, diabetes mellitus, active peptic ulcers, fresh intestinal anastomoses, ulcerative colitis and epilepsy need special attention and careful medical supervision. Carefully the drug is prescribed in the first weeks after acute myocardial infarction, to patients with thromboembolism, myasthenia gravis, glaucoma, hypothyroidism, psychosis or psychoneuroses, as well as to patients over 65 years of age.
During dexamethasone therapy, diabetes mellitus decompensation or the transition of latent diabetes to clinically manifest diabetes is possible.
With long-term treatment, it is necessary to control the level of potassium in the blood serum.
Vaccination with live vaccines is contraindicated during dexamethasone therapy.
Immunization with killed viral or bacterial vaccines does not give the expected increase in the titer of specific antibodies and therefore does not have the necessary protective effect. Dexamethasone is usually not given 8 weeks before vaccination and for 2 weeks after vaccination.
Patients taking high doses of dexamethasone for a long time should avoid contact with patients with measles; in case of accidental contact, prophylactic treatment with immunoglobulin is recommended.
Care must be taken when treating patients who have recently undergone surgery or bone fracture, as dexamethasone can slow the healing of wounds and fractures.
The effect of glucocorticosteroids is enhanced in patients with liver cirrhosis or hypothyroidism.
Dexamethasone is used in children and adolescents only under strict indications. During treatment, strict control of the growth and development of the child or adolescent is required.
Special information about some components of the drug
Dexamethasone contains lactose, and therefore, its use in patients with galactosemia, lactase deficiency and glucose-galactose malabsorption syndrome is contraindicated.
Influence on the ability to drive vehicles and other complex mechanisms
Dexamethasone has no effect on the ability to drive vehicles and work with technical devices that require concentration of attention and speed of psychomotor reactions.
Pregnancy and lactation
During pregnancy (especially in the first trimester), the drug Dexamethasone can be used only when the expected therapeutic effect outweighs the potential risk to the fetus. With prolonged therapy with dexamethasone during pregnancy, the possibility of impaired fetal growth is not excluded. If the drug is used Dexamethasone in the last trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.
If a woman received glucocorticosteroids during pregnancy, additional use of glucocorticosteroids is recommended during childbirth. If labor is delayed or a caesarean section is planned, it is recommended to inject 100 mg of hydrocortisone intravenously every 8 hours during the peripartum period.
Terms of dispensing from pharmacies
The drug is available by prescription.
Storage conditions and periods
Store the drug at a temperature not exceeding 25 ° C, in its original packaging. Keep out of the reach of children.
The shelf life is 5 years. Do not use the drug after the expiration date.
Dexamethasone
International non-proprietary name
Dexamethasone
Dosage form
0.5 mg tablets
Composition
One tablet contains
active substance - dexamethasone 0.5 mg,
inauxiliary substances: lactose monohydrate, corn starch, povidone, magnesium stearate, talc, colloidal anhydrous silicon dioxide
Description
Round tablets of white or almost white color with a flat surface, scored on one side and a bevel.
Pharmacotherapeutic group
Corticosteroids for systemic use. Glucocorticosteroids. Dexamethasone
ATX code H02AB02
Pharmacological properties
Pharmacokinetics
Dexamethasone is rapidly and almost completely absorbed when taken orally. The bioavailability of dexamethasone is 80%. After oral administration, Cmax in blood plasma was noted after 1-2 hours; after a single dose, the effect lasts about 66 hours.
In blood plasma, about 77% of dexamethasone binds to plasma proteins, and most of it is converted to albumin. Only a minimal amount of dexamethasone binds to non-albumin proteins. Dexamethasone is a fat-soluble compound. The drug is initially metabolized in the liver. Small amounts of dexamethasone are metabolized in the kidneys and other organs. The predominant excretion occurs through urine. The half-life (T1 \\ 2) is about 190 minutes.
Pharmacodynamics
Dexamethasone is a synthetic adrenal cortex hormone (corticosteroid) with glucocorticoid action. The drug has a pronounced anti-inflammatory, anti-allergic and desensitizing effect, has immunosuppressive activity.
To date, enough information has been accumulated on the mechanism of action of glucocorticoids to understand how they act at the cellular level. There are two well-defined receptor systems found in the cytoplasm of cells. Through glucocorticoid receptors, corticosteroids exert anti-inflammatory and immunosuppressive effects and regulate glucose homeostasis; through mineralocorticoid receptors, they regulate the metabolism of sodium and potassium, as well as water and electrolyte balance.
Indications for use
replacement therapy of primary and secondary (pituitary) adrenal insufficiency
congenital adrenal hyperplasia
subacute thyroiditis and severe forms of postradiation thyroiditis
rheumatic fever
acute rheumatic heart disease
pemphigus, psoriasis, dermatitis (contact dermatitis affecting a large surface of the skin, atopic, exfoliative, bullous herpetiformis, seborrheic, etc.), eczema
toxidermia, toxic epidermal necrolysis (Lyell's syndrome)
malignant exudative erythema (Stevens-Johnson syndrome)
allergic reactions to drugs and food
serum sickness, drug exanthema
urticaria, angioedema
allergic rhinitis, hay fever
diseases that threaten vision loss (acute central
chorioretinitis, inflammation of the optic nerve)
allergic conditions (conjunctivitis, uveitis, scleritis, keratitis, iritis)
systemic immune diseases (sarcoidosis, temporal arteritis)
proliferative changes in the orbit (endocrine ophthalmopathy, pseudotumors), sympathetic ophthalmia
immunosuppressive therapy for corneal transplantation
ulcerative colitis, Crohn's disease, local enteritis
sarcoidosis (symptomatic)
acute toxic bronchiolitis, chronic bronchitis, bronchial asthma (exacerbations)
agranulocytosis, panmyelopathy, anemia (including autoimmune hemolytic, congenital hypoplastic, erythroblastopenia)
idiopathic thrombocytopenic purpura
secondary thrombocytopenia in adults, lymphoma (Hodgkin's, non-Hodgkin's)
leukemia, lymphocytic leukemia (acute, chronic)
kidney disease of autoimmune origin (including acute glomerulonephritis)
nephrotic syndrome
palliative care for leukemia and lymphoma in adults
acute leukemia in children
hypercalcemia in malignant neoplasms
cerebral edema due to primary tumors or brain metastases due to craniotomy or head trauma
Method of administration and dosage
With long-term oral administration of high doses of dexamethasone, the drug is recommended to be taken with meals, and in the intervals between meals, it is necessary to take antacids. It is recommended to use it during the day taking into account the daily fluctuations in the endogenous secretion of glucocorticoids in the interval from 6 to 8 am.
Adults
The recommended starting dose for adults is 0.5 mg to 9 mg per day. The maximum daily dose is 10-15 mg. The daily dose can be divided into 2 - 4 doses. The usual maintenance dose is 0.5 mg to 3 mg per day.
The initial dose of dexamethasone should be used until a therapeutic effect is achieved, then it is gradually reduced (usually by 0.5 mg in 3 days) to a maintenance dose of 2 - 4.5 mg or more / day. If high-dose therapy continues for more than a few days, the dose is gradually reduced over the next few days or over a longer period. The minimum effective dose is 0.5-1 mg / day. Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, the tolerance of the drug and the patient's response to the therapy. The duration of the use of Dexamethasone ranges from 5-7 days to several 2-3 months or more. Treatment is stopped gradually.
Dosing in children over 6 years of age
Side effects
decreased glucose tolerance, "steroid" diabetes mellitus or manifestation of latent diabetes mellitus
itsenko-Cushing's syndrome, weight gain
hiccups, nausea, vomiting, increased or decreased appetite, flatulence, increased activity of "liver" transaminases and alkaline phosphatase, pancreatitis
"steroid" ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract
arrhythmias, bradycardia (up to cardiac arrest), development (in predisposed patients) or increased severity of chronic heart failure, increased blood pressure
hypercoagulability, thrombosis
delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia
increased intracranial pressure, nervousness, anxiety, insomnia, headache, dizziness, convulsions, vertigo
cerebellar pseudotumor
sudden loss of vision (with parenteral administration, the deposition of crystals of the drug in the vessels of the eye is possible), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, trophic changes in the cornea, exophthalmos, the development of secondary bacterial, fungal or viral eye infections
negative nitrogen balance (increased protein breakdown), hyperlipoproteinemia
increased sweating
fluid and sodium retention (peripheral edema), hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue)
growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones)
increased calcium excretion, osteoporosis, pathological bone fractures, aseptic necrosis of the humerus and femur head, tendon rupture
"steroid" myopathy, muscle atrophy
delayed wound healing, tendency to develop pyoderma and candidiasis
petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae
generalized and local allergic reactions
decreased immunity, development or exacerbation of infections
leukocyturia
violation of the secretion of sex hormones (violation of the menstrual cycle, hirsutism, impotence, delayed sexual development in children
withdrawal syndrome
Contraindications
hypersensitivity to the active substance or auxiliary components of the drug
peptic ulcer of the stomach and duodenum
osteoporosis
acute viral, bacterial and systemic fungal infections (when appropriate therapy is not used)
cushing's syndrome
severe arterial hypertension
severe renal failure
obesity III - IV degree
active tuberculosis
acute psychoses
pregnancy and lactation
cirrhosis of the liver or chronic hepatitis
children under 6 years old
Drug interactions
The simultaneous use of Dexamethasone and pain relievers (non-steroidal anti-inflammatory drugs), antihypertensive drugs, antidiabetic drugs, antiepileptic drugs, diuretics, anticoagulants, anti-asthma aerosols or ritodrin can enhance or weaken its effect and / or cause undesirable effects. Therefore, these drugs should not be used at the same time.
During the period of treatment with Dexamethasone, you should refrain from alcoholic beverages.
special instructions
With diabetes mellitus, tuberculosis, bacterial and amoebic dysentery, arterial hypertension, thromboembolism, heart and renal failure, ulcerative colitis, diverticulitis, newly formed intestinal anastomosis, Dexamethasone should be used very carefully and provided that the underlying disease can be adequately treated. If the patient has a history of psychoses, then glucocorticosteroid treatment is carried out only for health reasons.
With a sudden withdrawal of the drug, especially in the case of high doses, there is a withdrawal syndrome of glucocorticosteroids: anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness. After discontinuation of the drug for several months, the relative insufficiency of the adrenal cortex may persist. If during this period stressful situations arise, temporarily prescribe glucocorticoids, and, if necessary, mineralocorticoids.
Before using the drug, it is advisable to examine the patient for the presence of ulcerative pathology of the gastrointestinal tract. Patients with a predisposition to the development of this pathology should be prescribed antacids for prophylactic purposes.
During treatment with the drug, the patient should adhere to a diet rich in potassium, proteins, vitamins, with a reduced content of fats, carbohydrates and sodium.
If the patient has intercurrent infections, a septic condition, treatment with Dexamethasone should be combined with antibiotic therapy.
If treatment with Dexamethasone is carried out for 8 weeks before and 2 weeks after active immunization (vaccination), then the effect of immunization will be reduced or completely neutralized. Patients with severe craniocerebral trauma and ischemic cerebral circulation disorder should be prescribed glucocorticoids with caution. Application in pediatrics
In children over 6 years of age, during long-term treatment, it is necessary to carefully monitor the dynamics of growth and development. In children, during the growth period, glucocorticosteroids should be used only for health reasons and under the close supervision of a physician. To prevent disturbances in growth processes during prolonged treatment with the drug in children aged 6 to 14 years, it is advisable to take a 4-day break in treatment every 3 days.
Children who are in contact with patients with measles, chickenpox during treatment are prescribed specific immunoglobulins.
Features of influence drug on the ability to drive a vehicle or potentially dangerous machinery
Since Dexamethasone can cause dizziness and headache, it is recommended to refrain from driving a car and operating other potentially dangerous machinery.
Overdose
Symptoms: possible aggravation of the side effects described in the corresponding section.
Treatment: the drug should be discontinued and symptomatic therapy should be prescribed. There is no specific antidote.
After the symptoms of overdose disappear, the drug is resumed.
(Dexamethason)
INSTRUCTIONS (information for specialists)
on the medical use of the drug
Registration number P N016061 / 01
Tradename: Dexamethasone
International non-proprietary name: Dexamethasone
Chemical name: 9-fluoro-11 beta, 17,21 -trihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione 21 sodium dihydrogen phosphate
Dosage form: tablets
Composition:
1 tablet contains:
active substance: dexamethasone - 0.0005 g (0.5 mg);
excipients: refined sugar, potato starch, stearic acid.
Description:
White biconvex tablets.
Pharmacotherapeutic group: Glucocorticosteroid.
The codeATX: Н02АВ02.
Pharmacological properties
Pharmacodynamics.
Synthetic glucocorticosteroid (GCS) is a methylated derivative of fluoroprednisolone. It has anti-inflammatory, anti-allergic, desensitizing, immunosuppressive, anti-shock and antitoxic effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are present in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells.) Protein metabolism: reduces the amount of globulins in plasma, increases the synthesis of albumin in the liver and kidneys (with an increase in the albumin / globulin ratio); reduces synthesis and enhances protein catabolism in muscle tissue.
Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (mobilization from the subcutaneous tissue of the extremities and the accumulation of fat mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increasing the flow of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.
Water-electrolyte metabolism: detains Na + and water in the body, stimulates the excretion of K + (mineralocorticoid activity), reduces the absorption of Ca2 + from the gastrointestinal tract, causes "leaching" of calcium from bones and increases its renal excretion, reduces bone mineralization.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; by inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. Acts at all stages of the inflammatory process: inhibits the synthesis of prostaglandins (Pd) at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leicotrienes that promote inflammation, allergies, etc.), cytokines "pro-inflammatory" (pro-inflammatory, etc.) interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.
The immunosuppressive effect is due to the involution of lymphoid tissue caused by the inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of the migration of B-cells and the interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1,2; gamma-interferon) from lymphocytes and macrophages and decreased antibody production.
The antiallergic effect develops as a result of a decrease in the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells, reducing the sensitivity of effector cells to allergy mediators, inhibition of antibody production, changes in the body's immune response.
In obstructive diseases of the respiratory tract, the action is mainly due to the inhibition of inflammatory processes, the prevention or reduction of the severity of edema of the mucous membranes, a decrease in eosinophilic infiltration of the submucous layer of the bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of the bronchi of small and medium caliber to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation. Suppresses the synthesis and secretion of ACTT and, secondarily, the synthesis of endogenous GCS.
A feature of the action is a significant inhibition of the function of the pituitary gland and an almost complete absence of mineralocorticosteroid activity. Doses of 1-1.5 mg / day inhibit the function of the adrenal cortex; biological half-life - 32-72 hours (duration of inhibition of the hypothalamus-pituitary adrenal gland system).
In terms of glucocorticoid activity, 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisolone), 15 mg of hydrocortisone, or 17.5 mg of cortisone.
Pharmacokinetics
After oral administration, it is rapidly and completely absorbed. The maximum concentration in the blood is reached after 1-2 hours. In the blood it binds (60-70%) with a specific carrier protein - transcortin. Easily passes through the histohematogenous barriers (including through the hemato-encephalic and placental). It is metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. It is excreted in the urine (a small part by the lactating glands). The half-life is 3-5 hours.
Indications for use
- Primary and secondary adrenal insufficiency (usually in combination with mineralocorticoids);
- congenital hyperplasia of the adrenal cortex;
- subacute thyroiditis;
- hypercalcemia in malignant neoplasms;
- bronchial asthma;
- rheumatoid arthritis in the acute phase;
- systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, etc.);
- skin diseases (psoriasis, eczema, dermatitis, pemphigus, acute erytoderma, etc.);
- nonspecific ulcerative colitis;
- diseases of the hematopoietic organs: agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, acute lympho- and myeloid leukemias, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocytic anemia), congenital anemia;
- cerebral edema (usually after prior parenteral administration of a glucocorticosteroid);
- conducting a test in the differential diagnosis of hyperplasia (hyperfunction) and tumors of the adrenal cortex.
Contraindications
The only contraindication for short-term use for health reasons is hypersensitivity to dexamethasone or drug components.
In children, during the period of growth, GCS should be used only for absolute indications and under the particularly close supervision of the attending physician. With caution, the drug should be prescribed for the following diseases and conditions:
Application during pregnancy and breastfeeding
During pregnancy (especially in the first trimester), the drug can be used only for health reasons. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not excluded. If used in the third trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn. If it is necessary to carry out drug treatment during breastfeeding, then breastfeeding should be discontinued.
Method of administration and dosage
The dosage regimen of the drug is individual and depends on the indications, the severity of the disease and the patient's response to therapy. Dexamethasone is administered orally during or after meals, once in the morning (small dose) or in 2-3 doses (large dose). The average daily intake for adults ranges from 2-3 mg to 6 mg. The maximum daily dose is 10-15 mg. After achieving a therapeutic effect, the dose is gradually reduced (usually by 0.5 mg every 3 days) to a maintenance dose of 2-4.5 or more mg / day. The minimum effective dose is 0.5-1 mg / day. Children are prescribed 0.0833-0.3333 mg / kg or 0.0025-0.0001 mg / m2 per day in 3-4 divided doses depending on age.
The duration of the 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.
Side effect
Usually Dexamethasone is well tolerated. It has low mineralocorticoid activity, i.e. its effect on water-electrolyte metabolism is small. As a rule, low and medium doses of Dexamethasone do not cause sodium and water retention in the body, increased potassium excretion. The following side effects have been described:
From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, inhibition of adrenal function, Itsenko-Cushing's syndrome (moon face, pituitary obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, stretch marks), delay ...
From the digestive system: nausea, vomiting, pancreatitis, steroid stomach and duodenal ulcer, erosive esophagitis, bleeding and gastrointestinal perforation, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases - an increase in the activity of "hepatic" transaminases and alkaline phosphatase.
On the part of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.
From the 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 senses: 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 of metabolism: increased calcium excretion, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating.
Due to mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).
From the side of the musculoskeletal system: slowing down the growth 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).
On the part of the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, acne, striae, a tendency to develop pyoderma and candidiasis.
Allergic reactions: skin rash, itching, anaphylactic shock.
Others: the development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccinations), leukocyturia. withdrawal syndrome.
Overdose
An increase in the side effects described above is possible. It is necessary to reduce the dose of Dexamethasone. Treatment is symptomatic.
Interaction with other medicinal products
Simultaneous appointment of Dexamethasone with:
inducers of "hepatic" microsomal enzymes (phenobarbital, rifampicin, phenytoin, theofipline, ephedrine) leads to a decrease in its concentration;
diuretics (especially "thiazide" and carbonic anhydrase inhibitors) and amphotericin B can lead to increased excretion of K + from the body; with sodium-containing drugs - the development of edema and increased blood pressure;
amphotericin B - the risk of developing heart failure increases;
cardiac gpicosides - their tolerance worsens and the likelihood of developing ventricular extrasystole (due to induced hypokalemia) increases;
indirect anticoagulants weakens (less often enhances) their effect (dose adjustment is required);
anticoagulants and thrombolytics - the risk of bleeding from ulcers in the gastrointestinal tract increases;
ethanol and non-steroidal anti-inflammatory drugs (NSAIDs) - the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs in the treatment of arthritis, it is possible to reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect);
paracetamol the risk of developing hepatotoxicity increases (induction of liver enzymes and the formation of a toxic metabolite of paracetamol);
acetylsapicylic acid accelerates its excretion and reduces the concentration in the blood (when dexamethasone is canceled, the level of salicylates in the blood increases and the risk of side effects increases);
insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness decreases.
vitamin D - its effect on the absorption of Ca2 + in the intestine decreases.
growth hormone reduces the effectiveness of the latter, and with praziquantel - its concentration;
M-anticholinergics (including antihistamines and tricyclic antidepressants) and nitrates helps to increase intraocular pressure;
isoniazid and mexelitine increases their pletabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.
Carbonic anhydrase inhibitors and loop diuretics may increase the risk of developing osteoporosis.
Indomethacin, displacing Dexamethasone from its association with albumin, increases the risk of developing its side effects.
ACTH enhances the effect of Dexamethasone.
Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by Dexamethasone.
Cyclosporine and ketoconazole, slowing down the metabolism of Dexamethasone, can in some cases increase its toxicity.
The simultaneous administration of androgens and steroid anabolic drugs with Dexamethasone contributes to the development of peripheral edema and hirsutism, the appearance of acne.
Estrogens and oral estrogen-containing contraceptives reduce the clearance of Dexamethasone, which may be accompanied by an increase in the severity of its action.
Mitotan and other inhibitors of adrenal cortex function may necessitate an increase in the dose of Dexamethasone.
When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of virus activation and the development of infections.
Antipsychotics (neuroleptics) and azathioprine increase the risk of developing cataracts when dexamethasone is prescribed.
The simultaneous administration of antacids reduces the absorption of Dexamethasone.
With simultaneous use with antithyroid drugs, it decreases, and with thyroid hormones, the clearance of Dexamethasone increases.
Special instructions.Before starting treatment, the patient should be examined to identify possible contraindications. Clinical examination should include examination of the cardiovascular system, X-ray examination of the lungs, examination of the stomach and duodenum, urinary system, organs of vision; control of blood count, glucose and electrolytes in blood plasma. During treatment with Dexamethasone (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure and the state of water and electrolyte balance. as well as pictures of peripheral blood and blood glucose levels.
In order to reduce side effects, antacids can be prescribed, as well as to increase the intake of K + into the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with limited content of fats, carbohydrates and table salt.
The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug can exacerbate existing emotional instability or psychotic disturbances. If a history of psychoses is indicated, Dexamethasone in high doses is prescribed under the strict supervision of a physician.
In stressful situations during supportive treatment (for example, surgery, trauma or infectious diseases), the dose of the drug should be adjusted due to the increased need for glucocorticosteroids.
With daily use for 5 months. treatment develops atrophy of the adrenal cortex. The patient should be closely monitored for a year after the end of long-term therapy with Dexamethasone in connection with the possible development of relative adrenal insufficiency. If during this period stressful situations arise, they are prescribed (according to indications) for the time of GCS, if necessary in combination with mineralocorticoids.
With a sudden cancellation, especially in the case of the previous use of high doses, it is possible to develop a withdrawal syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness), as well as exacerbation of the disease, for which Dexamethasone was prescribed.
During treatment with Dexamethasone, vaccination should not be carried out due to a decrease in its effectiveness (immune response).
Prescribing Dexamethasone for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with antibiotics with bactericidal action.
Dexamethasone can mask some of the symptoms of infections.
In children, during long-term treatment with Dexamethasone, 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 prophylactically prescribed specific immunoglobulins. In patients with diabetes mellitus, blood glucose should be monitored and therapy should be corrected if necessary. X-ray control of the osteoarticular system is shown (images of the spine, hand).
In patients with latent infectious diseases of the kidneys and urinary tract, Dexamethasone can cause leukocyturia, which may be of diagnostic value.
Dexamethasone increases the content of 11- and 17-hydroxyketocorticosteroid metabolites.
Release form
0.5 mg tablets. 50 tablets in polypropylene cases. The pencil case, together with the instructions for use, is placed in a cardboard box.
Shelf life
3 years. Do not use after the expiration date printed on the package.
Storage conditions
Slisok B. In a dry, protected by light and inaccessible to children at a temperature of 15 to 25 ° C.
Terms of dispensing from pharmacies
On prescription.
LLC "Experimental plant" GNTSLS ", Ukraine
Consumer claims should be sent to the manufacturer.
Dexamethasone is a hormonal drug that is considered in modern medicine as one of the vital pharmaceuticals belonging to the group of synthetic glucocorticosteroids. Dexamethasone is able to penetrate into the tissues of all organs and systems, including the brain and nervous system, and affect the entire body. In severe conditions - shock, acute systemic allergies, severe inflammation, pathological immune reactions, the medicine can save lives.
For the treatment of various types of diseases, Dexamethasone is produced in 4 dosage forms, the therapeutic basis of which is sodium phosphate of dexamethasone.
This substance is a synthetic analogue of the natural steroid hormone that the adrenal glands produce in the body.
Basic forms:
- Tablets of 0.5 mg (0.5 mg of active ingredient) in a pack of 10 units.
- Injection solution (0.4%) in 1 ml ampoules, containing 4 mg of active ingredient (5 or 25 units per package). It is used for injection into muscle, vein (jet or drip), into the joint, into the soft tissues surrounding it, into the fiber of the eyeball.
- Dexamethasone eye drops (ear) 10 ml with an active substance concentration of 0.1% (1 mg in 1 ml).
- Eye ointment - 2.5 g tube.
All forms of medication as auxiliary components contain substances that are necessary to stabilize, shape and transport dexamethasone to the painful focus, as well as preservatives and additives that facilitate the absorption of the drug.
Each therapeutic form has its own purposefulness in use, certain indications and contraindications, so you should not engage in treatment on your own - only a specialist is able to develop the necessary therapy regimen, calculate the doses and frequency of use.
The drug is a prescription drug, where the name of the drug in Latin is dexamethasoni.
Pharmacological properties and pharmacokinetics
Healing properties
The mechanism of the drug's therapeutic action is based on its ability to create a high concentration of the component in the blood and inflammation foci, penetrate into all tissues and exert an effect at the cellular level.
This allows the active substance to work in the brain and nerve tissues, relieve cerebral and lung edema in case of hemorrhage, poisoning, injuries, tumors, taking the patient out of a life-threatening state of shock, inhibiting the course of cancer processes, and eliminating the manifestations of acute allergies.
Glucocorticosteroid activates a series of processes that lead to a decrease in the permeability of the vascular walls, strengthening the protection of cell membranes and blocking inflammation at any stage of development.
By suppressing an acute reaction of the immune system to allergens, the drug stops the development of an allergic reaction, including anaphylactic shock, reduces the degree of edema of the mucous membranes of the respiratory organs, bronchi, restoring air intake in case of laryngeal edema or asthmatic attack.
At the same time, the drug inhibits the production of histamine, stopping the pathological manifestations of allergies.
Slows down the formation of cicatricial changes in the tissues of various organs.
Absorption and excretion from the body
The corticosteroid is actively and almost completely absorbed not only after injection, but also after internal administration. The bioavailability or amount of the medicinal substance reaching the focus of exposure is 77 - 79%, due to which the therapeutic effect of the drug is maximum.
In the blood, 65 - 70% of dexamethasone binds to the transport protein transcortin, which provides a high concentration of the drug in the blood. With the blood flow, the protein delivers dexamethasone throughout the body, penetrating into the intracellular spaces of tissues.
The greatest amount of active substance in the blood, providing the maximum therapeutic effect, is observed within 40 to 90 minutes, depending on the method of application.
The active substance is processed by liver enzymes to inactive intermediates. It is excreted from the body along with urine and is excreted in small quantities (about 10%) by the intestines. A small amount of dexamethasone penetrates into human milk, which should be taken into account when prescribing the drug to a nursing mother.
What is the drug prescribed for?
The action of the drug is used in many diseases of internal organs, systemic, autoimmune pathologies, in diseases of the joints, eyes, skin and in many other areas of medicine.
The list of pathological conditions that require injections or Dexamethasone tablets include:
- life-threatening shock conditions of all forms, including painful shock, toxic, cardiogenic, allergic, postoperative, blood transfusion (after blood transfusions);
- edema of brain tissue (with hemorrhage, meningitis, tumor, encephalitis, trauma, surgery);
- an attack of bronchial asthma or long-term status asthma;
- lung pathologies: beryllium disease, tuberculosis, alveolitis, pneumonia, Leffler's syndrome (resistant to other medicines);
- allergic reactions: urticaria, Quincke's edema, hay fever, allergy to drugs and foods, serum sickness;
- endocrine disorders - adrenal insufficiency, thyroid disease, thyrotoxic crisis, thyroiditis, adrenogenital syndrome;
- autoimmune diseases - rheumatic heart disease, multiple sclerosis, systemic lupus erythematosus, pemphigus, scleroderma, systemic vasculitis;
- pain with inflammation of the reproductive organs, including prostatitis; various types of myositis;
- intractable skin diseases - eczema, dermatitis of various types, psoriasis, toxidermia, Lyell and Stevens-Johnson syndromes, discoid lupus erythematosus, keloid scars (topical application);
- eye lesions of an allergic and inflammatory nature: scleritis, corneal ulcer, various types of conjunctivitis (except for purulent), uveitis, keratitis, blepharitis, inflammation of the optic nerve, ophthalmopathy against the background of diabetes mellitus;
- swelling of the larynx and glottis with acute croup;
- inflammation of the joints of various courses: arthritis of various forms, osteoarthritis, polyarthritis, ankylosing spondylitis, bursitis, tendosynovitis and others;
- hematopoietic disorders: Addison's disease, lymphoma, agranulocytosis, anemia of various origins, thrombocytopenia;
- critical conditions with lesions of the gastrointestinal system: enteritis, including granulomatous, hepatitis and hepatic coma, ulcerative colitis;
- allergic-toxic reaction with massive helminthic aggression;
- lesions of the esophagus and stomach in case of alkali, acid poisoning to suppress inflammation and prevent cicatricial narrowing;
- acute renal pathologies - glomerulonephritis, nephrotic syndrome;
- malignant processes in the lungs, leukemia, lymphocytic leukemia, myeloma;
- nausea and vomiting while taking cytostatics.
Instructions for the use of Dexamethasone
The treatment regimen with Dexamethasone and the dosage regimen is established only by the attending physician in order to obtain the maximum therapeutic effect with a minimum risk of unwanted side reactions.
Tablets
Usually prescribed in the chronic course of pathology or after the removal of an acute condition.
The dose is determined for each patient separately, taking into account the nature and severity of the disease, the planned duration of the course, age, drug tolerance and patient response.
The usual minimum effective dose for adults per day is 0.5 to 9 mg. A small dose is taken at a time, a large dose is divided into 3 - 4 doses. The largest amount of dexamethasone per day should not exceed 10-15 mg.
The average maintenance dose per day is 0.5 - 3 mg.
With long-term use of the drug in a large dose, the drug intake is combined with food. In this case, between meals, it is advisable to use agents that reduce gastric acidity (antacids).
After improving the patient's condition, the dose should be gradually reduced - every 3 days by 0.5 mg to a maintenance dose.
The duration of the course of application ranges from 3 to 5 days to several months.
It is unacceptable to abruptly stop treatment with Dexamethasone, so as not to cause withdrawal syndrome,
which is expressed in an exacerbation of the underlying disease and painful manifestations of withdrawal symptoms (weakness, weight loss, vomiting, diarrhea, falling blood sugar and pressure, muscle pain, fever).
Dosing for children
Young patients are prescribed in accordance with body weight or body area, age and severity of the pathological process.
The approximate children's dose per day is 0.0833 - 0.333 mg per 1 kilogram of the child's body weight. Thus, according to the calculation, a child weighing 25 kg can receive a maximum of 0.333 x 25 \u003d 8.36 mg of the drug per day, divided into 3-4 doses. The minimum dose that will give a therapeutic effect for a small patient with such a weight is 0.0833 x 25 \u003d 2.08 mg.
More precisely, the child's dose is calculated by the surface area of \u200b\u200bthe child's body at the rate of 0.0025 - 0.0001 mg per 1 square meter per day in 3 - 4 doses, depending on age.
Injections
Dexamethasone injections for systemic diseases are given inside the muscles, or injected intravenously, which is preferable in life-threatening situations when there is a high risk to the patient's life. The solution enters the bloodstream immediately, providing a quick therapeutic effect.
For urgent short-term or one-time use of the drug, only intolerance to any of the substances in Dexamethasone is considered a contraindication. In critical situations, the side effects of the medication are neglected.
Adults in acute and urgent conditions can be administered 3-4 times a day, 4-20 mg each. In the acute phase of the pathology, as well as at the beginning of therapy, higher doses of corticosteroid are used. The highest dose is 80 mg, but in critical cases it is higher.
Children's doses for intramuscular administration are calculated by the weight of the child at the rate of 0.02776 - 0.16665 mg per kilogram of body weight after 12 - 24 hours.
The duration of injection with a gradual decrease in the dose usually does not exceed 3 to 4 days, after which the patient is transferred to taking tablets in a maintenance dose.
Eye and ear drops
In acute inflammation, patients over 12 years of age are dripped 4 - 5 times a day ophthalmic solution for the lower eyelid, 1 - 2 drops, for 48 hours. When the degree of inflammation decreases, the treatment is continued for another 4-6 days, reducing the frequency of instillation to 3 times a day.
In chronic processes, the agent is used twice a day for no longer than 20 - 40 days.
For allergic eye damage, similar doses are used up to 5 times a day for 48 hours, then the frequency of instillation is gradually reduced to 2 times a day and treatment is canceled for 7 to 12 days.
For patients 6 - 12 years old, to eliminate inflammation and allergic phenomena, 1 drop is administered per eyelid up to 4 times a day for no longer than 10 days.
The solution is used from day 8 after surgery to eliminate cataracts, retinal detachment, strabismus up to 4 times a day for 2 to 4 weeks.
In case of ear inflammation (otitis media) of a non-viral nature, 3-4 drops (children 1 - 2) are instilled into the sore ear in a warm form three times a day.
Lenses are removed before instilling the product. You can put them on only after 15 minutes.
Dexamethasone eye ointment
It is used for the same indications as ophthalmic drops in patients from 6 years old. A strip of ointment 10-15 mm long is carefully placed behind the lower eyelid 3 times a day. The maximum duration of treatment is no more than 20 days.
Use during pregnancy and lactation
In a study on small mammals, it was revealed that Dexamethasone, like many other hormonal agents, crosses the placenta into the embryonic tissue and can lead to early death of the embryo and fetal malformations. The class of action of the drug on the fetus is C (according to FDA).
Therefore, Dexamethasone is used during pregnancy only if there is a threat to the mother's life.
If a pregnant woman received Dexamethasone, after childbirth, it is necessary to monitor the baby's health - since the child may be diagnosed with adrenal dysfunction, which requires immediate intensive treatment.
Since the drug passes into human milk, breastfeeding mothers need to switch to artificial feeding or refuse the drug.
With long-term use of ointment or drops, the drug is partially absorbed into the blood. Therefore, these dosage forms are allowed to be used by expectant mothers only after 12 weeks of gestation, in very short courses of up to 3 days and in minimal doses.
During lactation, treatment with ointment and drops for no longer than 7-10 days is permissible.
Can I drink alcohol while taking the drug
Dexamethasone treatment is incompatible with alcohol consumption, otherwise the consequences of concurrent use will be very serious.
There is a high probability of such severe manifestations as:
- indomitable diarrhea;
- partial loss of vision;
- abdominal pain, vomiting;
- acute pain at the injection site;
- redness of the skin on the chest, hives, acne on the face;
- ulceration of the mucous membrane of the digestive organs;
- internal bleeding.
If the patient has a serious alcohol dependence and is unable to refuse alcohol during therapy, other drugs are required.
Drug interactions with other drugs
The combination of Dexamethasone and non-hormonal anti-inflammatory pharmaceuticals (Aspirin, Paracetamol) increases the likelihood of formation or deepening of ulcers of the digestive organs.
The effect of the corticosteroid is reduced when used in parallel:
- antacids, which reduce the absorption of the medicinal substance in the stomach;
- somatotropin;
- drugs from the series of inducers of the CYP3A4 isoenzyme (for example, phenobarbital, phenobarbital, rifabutin, rifampicin, carbamazepine);
- aminoglutethimide and ephedrine.
With parallel use, Dexamethasone is capable of:
- reduce the therapeutic effects of insulin, hypoglycemic drugs, drugs for high blood pressure, Praziquantel and diuretic-natriuretics;
- enhance the effect of Heparin, Albendazole.
- increase the excretion of potassium when combined with diuretics; influence the action of coumarin-based anticoagulants;
Antifungal agents based on ketoconazole, contraceptive pills, macrolide antibiotics can lengthen the time of dexamethasone excretion in the urine and increase the frequency and degree of adverse reactions.
The combination of a medication with Thalidomide can provoke the development of Lyell's syndrome, with anticholinergics - glaucoma, with antipsychotics and Azathioprine - cataracts; with cardiac glycosides - arrhythmias.
The combination with anabolic steroids, androgens, contraceptives, estrogens can cause increased hair growth of the face, breasts, edema, and the development of acne.
The use of antiviral vaccines in parallel with Dexamethasone therapy increases viral aggressiveness against a background of decreased immunity.
Contraindications, side effects and overdose
Contraindications
If Dexamethasone is urgently required to save life, all contraindications (except for drug intolerance), and possible adverse reactions are ignored.
For any severe infections, injections and tablets of Dexamethasone can be prescribed only with simultaneous specific treatment of these diseases.
Contraindications for intra-articular injections:
- tendency to bleeding;
- intra-articular bone fracture;
- infection, osteoporosis, instability, deformity in the joint area, bone destruction, ankylosis;
- surgery (arthroplasty);
- articular bone necrosis;
- low efficiency after 2 previous injections.
Contraindications for local forms (ointment, drops):
- eye damage with a tubercle bacillus, fungus, viruses, including herpes;
- glaucoma;
- acute suppuration of the structures of the eye (if antibiotic treatment is not carried out);
- trauma and ulcer of the cornea, the period after removal of a foreign object;
- hole in the eardrum.
Important! Dexamethasone ointment and drops can reduce the severity of manifestations in the development of bacterial and fungal infections of the ears and eyes.
Therefore, after clarifying the diagnosis and detecting infection, the drug should be used with appropriate antimicrobial treatment.
Side effects
The hormonal agent has a profound effect on all body systems. The task of the attending physician is to minimize the risk, frequency and severity of adverse reactions with a high therapeutic effect of the drug.
Undesirable manifestations depend on the duration of the course, dosages, age and condition of the patient.
Basic side effects:
- allergic rashes, pruritus, urticaria, facial edema, respiratory distress, bronchospasm, anaphylactic shock;
- anxiety, disorientation, depressive, paranoid or euphoric states;
- double vision, visual disturbances, pain in the head due to an increase in intracranial pressure, characteristic of a rapid dose reduction;
- insomnia, dizziness;
- persistent increase in blood pressure;
- weakening of the myocardium, arrhythmias;
- potassium deficiency and heart problems associated with hypokalemia;
- decreased adrenal function, development of diabetes mellitus, Itsenko-Cushing's syndrome, excessive hair growth, disorder of the monthly cycle, developmental delay in children;
- a sharp increase in blood viscosity and thrombus formation;
- nausea, bouts of vomiting, ulceration of the digestive organs, gastritis, pancreatitis, colitis;
- frequent infections against the background of suppression of immunity;
- osteoporosis, abnormal fractures, joint and muscle pain, femoral head necrosis, tendon rupture;
- acne, sweating, dry skin, slow healing of damage;
- swelling of the limbs, weight gain;
- a sharp deterioration in vision (with injections in the face, neck and head);
- increased pain when injected into the joint;
- burning, itching of the mucous membrane and skin (ointment and drops), with treatment longer than 20 days, allergies, glaucoma and cataracts may develop, and decreased visual function.
Transport drivers and workers who require increased concentration should be careful when treating with Dexamethasone, as concentration is impaired when it is taken.
Overdose
Excessive doses of a corticosteroid or long-term treatment can lead to overdose, which manifests itself in an increase in unwanted side reactions.
The drug is immediately canceled and the symptoms of an overdose are eliminated with the help of drugs that can relieve certain manifestations.
Long-term therapy requires constant monitoring of the development of children, periodic examination of the organs of vision, control of intraocular, intracranial pressure, sugar and blood clotting, functions of the adrenal glands and the hypothalamic-pituitary system.
Dexamethasone analogs
Synonyms - drugs with the same active ingredient as Dexamethasone, and a similar therapeutic effect: Dexamethasone-Vial, Dexamethasone-Ferein, eye drops - Dexamethasonlong, Maxidex, Oftan Dexamethasone, Ozurdex.
Analogues with a similar action, but a different composition:
- drops with Dexamethasone and other active ingredients: Sofradex, Dexon;
- Prednisolone is a corticosteroid medication with a similar but weaker therapeutic effect.