Dexamethasone solution. Dexamethasone is a hormonal synthetic drug from the group of glucocorticoids

Dexamethasone is a synthetic glucocorticosteroid. It is available in several dosage forms: solution for intravenous and intramuscular administration, eye drops, tablets. Its glucocorticoid activity is 25 times greater than that of hydrocortisone, and 7 times greater than that of prednisolone. Inhibits the activity of white blood cells and resident mononuclear phagocytes. Prevents the migration of the former to the inflammatory focus. Stabilizes lysosome membranes, thereby reducing the level of proteases in the inflammatory focus. It neutralizes the effect of histamine on the walls of capillaries, thereby reducing their permeability. Inhibits the proliferative activity of fibroblasts and suppresses collagen synthesis. Reduces the intensity of formation of inflammatory mediators - prostaglandins and leukotrienes. Inhibits the release of cyclooxygenase-2. Promotes the migration of leukocytes from the blood to the lymph. When interacting directly with blood vessels, it exhibits a vasoconstrictor effect. Effect on protein metabolism: reduces the content of globulins in serum, stimulates the formation of albumin in the kidneys and liver, activates catabolic processes in skeletal muscles. Effect on fat metabolism: promotes the formation of fatty acids, redistributes adipose tissue from the extremities to the abdomen, face, shoulder girdle, increases the level of lipids in the blood. Effect on carbohydrate metabolism: promotes the absorption of carbohydrates from the gastrointestinal tract, increases blood glucose levels. In submaximal doses, it makes brain tissue more excitable and increases the risk of seizures. When used systemically, it exhibits anti-inflammatory, antiallergic effects, suppresses immunity and excessive cell proliferation. Local forms of the drug exhibit anti-inflammatory, antiallergic effects, reduce the intensity of exudate entering the inflammation site (due to the vasoconstrictor effect).

Metabolized by microsomal liver enzymes. Half-life is 2-3 hours. Eliminated by the kidneys.

Bacterial, viral and fungal infections require constant medical monitoring of the patient taking Dexamethasone. Severe forms of infectious diseases allow the drug to be taken only in combination with specific therapy. Diseases and conditions in which the drug should also be taken with caution are: immunodeficiency diseases, BCG vaccination, diseases of the gastrointestinal tract (gastric and duodenal ulcers, inflammation of the esophageal mucosa, inflammation of the diverticulum, etc.), cardiovascular pathology, endocrine diseases. Before starting drug therapy with Dexamethasone, it is necessary to monitor blood counts, glucose and electrolytes in the blood. If you abruptly stop taking the drug (especially if it was taken in submaximal doses), rebound syndrome often develops, the manifestations of which are nausea, loss of appetite, musculoskeletal pain, and chronic fatigue. While taking the drug, it is necessary to monitor blood pressure, water-salt balance, and also be observed by an ophthalmologist.

When combined with certain medications, Dexamethasone can cause a number of unwanted side effects. Thus, taking it together with azathioprine or antipsychotic drugs can provoke cataracts, and with anticholinergics - glaucoma. In combination with oral contraceptives, testosterone preparations, female sex hormones, anabolic steroids, Dexamethasone can cause acne and increased male pattern hair growth. In combination with non-steroidal anti-inflammatory drugs, taking the drug increases the risk of erosive and ulcerative lesions of the gastrointestinal tract.

Pharmacology

GKS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. It disrupts the ability of macrophages to phagocytose, as well as to form interleukin-1. Helps stabilize lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A 2, 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; suppresses the formation of antibodies.

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

When directly applied to blood 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 levels activates the release of insulin.

Dexamethasone inhibits the uptake of glucose into fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which leads to fat accumulation.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, 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.

When used systemically, the therapeutic activity of dexamethasone is due to its anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

When applied externally and locally, the therapeutic activity of dexamethasone is due to its anti-inflammatory, antiallergic and antiexudative (due to the vasoconstrictor effect) effect.

Its anti-inflammatory activity is 30 times higher than hydrocortisone, but does not have mineralocorticoid activity.

Pharmacokinetics

Plasma protein binding - 60-70%. Penetrates histohematic barriers. A small amount is 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 eye tissue or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone significantly increases.

Release form

1 ml - dark glass ampoules (5) - contour cell packaging (5) - cardboard packs.
250 ml - ampoules (50) - blister packaging (5) - cardboard boxes - transport boxes (in bulk)

Dosage

Individual. Orally for severe diseases 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. Take small doses 1 time/day in the morning.

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

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

Interaction

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

When used simultaneously with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs is reduced.

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

When used simultaneously with diuretics, increased excretion of potassium is possible; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases.

When used simultaneously with oral anticoagulants, the anticoagulant effect may be weakened.

When used simultaneously with cardiac glycosides, the tolerability of cardiac glycosides may deteriorate due to potassium deficiency.

When used simultaneously with aminoglutethimide, the effects of dexamethasone may be reduced or inhibited; with carbamazepine - the effect of dexamethasone may be reduced; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - a decrease in the concentration of imatinib in the blood plasma is possible due to the induction of its metabolism and increased excretion from the body.

When used simultaneously with itraconazole, the effects of dexamethasone are enhanced; with methotrexate - increased hepatotoxicity is possible; with praziquantel - a decrease in the concentration of praziquantel in the blood is possible.

When used simultaneously with rifampicin, phenytoin, and barbiturates, the effects of dexamethasone may be weakened due to increased excretion from the body.

Side effects

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

Metabolism: increased excretion of calcium ions, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating, hypernatremia, hypokalemia.

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

From 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 ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups; rarely - increased activity of liver transaminases and alkaline phosphatase.

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 musculoskeletal system: slower growth and ossification processes in children (premature closure of epiphyseal growth plates), 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, skin thinning, hyper- or hypopigmentation, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis.

Allergic reactions: generalized (including skin rash, skin itching, anaphylactic shock) and when applied topically.

Effects associated with immunosuppressive effects: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants 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 long-term use or application to large areas of skin, systemic side effects characteristic of GCS may develop.

Indications

For oral administration: Addison-Biermer disease; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; UC; 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 use of GCS).

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

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

Contraindications

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 a history), as well as general infectious disease, severe periarticular osteoporosis, absence of signs of inflammation in the joint ("dry" joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformation (sharp narrowing of the joint space, ankylosis), joint instability as a result of arthritis, aseptic necrosis of the forming epiphyseal joint of bones.

For external use: bacterial, viral, fungal skin diseases, skin tuberculosis, skin manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (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 diseases of the eyes, tuberculosis of the eyes, disruption of the integrity of the ocular epithelium, acute form of purulent eye infection in the absence of specific therapy, diseases of the cornea combined with epithelial defects, trachoma, glaucoma.

It should be used with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency conditions (including AIDS or HIV infection).

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

Should be used with caution for diseases of the cardiovascular system, incl. after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, the necrotic focus 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 mellitus ( including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and/or liver failure, 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 closed-angle glaucoma.

If intra-articular administration is necessary, it should be used with caution in patients with a general severe condition, ineffectiveness (or short duration) of the action of 2 previous administrations (taking into account the individual properties of the GCS used).

Before and during GCS therapy, it is necessary to monitor a general blood count, glycemic levels and plasma electrolyte levels.

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

Relative adrenal insufficiency caused by dexamethasone may persist for several months after its discontinuation. Taking this into account, in stressful situations that arise 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 kept in mind. During treatment, it is necessary to monitor intraocular pressure and the condition of the cornea.

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

During the treatment period, monitoring of blood pressure, water and electrolyte balance, peripheral blood picture and glycemic level, as well as observation by an ophthalmologist is required.

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

Dexamethasone is a hormonal drug that has an immunosuppressive effect, fights inflammation, and has a positive effect on the central nervous system. The substances in the composition have anti-allergic and anti-shock properties, and are also capable of removing toxins, so it is actively prescribed to patients with inflammatory processes in the eyeball or with cerebral edema.

Once in the cytoplasm, it interacts with its receptors, resulting in the formation of a complex that, penetrating into the cell nucleus, enhances the synthesis of messenger RNA. Available in the form of tablets and injection solutions. It belongs to the category of vital means and is available with a prescription.

Important! During the course of treatment with Dexamethasone, it is necessary to refrain from driving and other activities that require the fastest and most accurate response to dangerous factors.

Use of the drug

Why is Dexamethasone prescribed? A doctor may prescribe it in cases where the patient has problems with the functioning of certain organ systems, as well as in the presence of a number of diseases:

• endocrine problems
• connective tissue pathologies
• skin diseases
• eye diseases
• problems in the functioning of the gastrointestinal tract
• blood diseases
• renal pathologies
• tumors
• other diseases

Thus, indications for use may include problems associated with adrenal insufficiency, swelling of the brain, the presence of tumors or traumatic brain injuries. The drug is aimed at alleviating conditions caused by malignant tumors and conditions: leukemia, childhood leukemia and others.

Dexamethasone is effective in exacerbation of chronic diseases (bronchitis, asthma), as well as in severe allergic reactions and during infectious diseases (in combination with antibiotics). Prescribed for recovery from a state of shock (anaphylactic shock, burn, toxic, surgical shock). It is also often used in ophthalmology in the treatment of conjunctivitis, scleritis and to eliminate the consequences of eye injuries.

Taking Dexamethasone during pregnancy

Pregnancy can be a contraindication for taking many medications, and Dexamethasone is no exception. Its use in the early stages is indicated only when the possible risk to the life and growth of the embryo is greater than the possible side effect of the drug. Taking medication in the last stages of pregnancy can have a significant impact on the development of the adrenal glands: the child may experience atrophy of their cortex, so after childbirth there may be a need for replacement therapy. If you need to take the drug during lactation, you will have to stop breastfeeding.

Mode of application

Dexamethasone is used according to an individually drawn up plan. Taken orally (tablets), by injection, conjunctivally.

• Tablets for adults. Taken after or during meals, from 2-3 to 10-15 mg per day (depending on the doctor’s instructions).

• Tablets for children. 3-4 times a day, depending on the child’s body weight.

• Injections for adults. For emergency care – from 4 to 20 mg, up to 4 times a day. For shock, a loading dose of 20 mg is used, then 3 mg per 1 kg of weight during the day.

• Injections for children. Calculated depending on body weight.

• For ophthalmological diseases - up to 2 drops hourly, after that - every 5-6 hours (if the condition is acute). In other cases - up to 2 drops 3 times a day. The course is usually a couple of weeks.

Contraindications

If the body has diseases of the gastrointestinal tract (ulcers, gastritis, colitis, diverculitis), as well as the cardiovascular system (heart failure and especially myocardial infarction), taking Dexamethasone is fraught with rupture of the heart muscle. Disturbances in the functioning of the endocrine system (diabetes, hypothyroidism and others) and pathologies of the kidneys and liver are also contraindications. And, as mentioned above, pregnancy and lactation period.

Side effects and overdose

In case of an overdose, the threat to the body is not so large-scale, but it is there. Blood pressure rises, swelling appears, and consciousness may change. That is why the drug must be prescribed by a doctor and taken according to an individual plan.

It interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus and stimulates the synthesis of mRNA: the latter induces the formation of proteins, including lipocortin, that mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, PGs, leukotrienes, which promote inflammation, allergies, etc. It prevents the release of inflammatory mediators from eosinophils and mast cells. Inhibits the activity of hyaluronidase, collagenase and proteases, normalizes the functions of the intercellular matrix of cartilage tissue and bone tissue. Reduces capillary permeability, stabilizes cell membranes, incl. lysosomal, inhibits the release of cytokines (interleukins and gamma-interferron) from lymphocytes and macrophages, causes involution of lymphoid tissue. Restores the sensitivity of adrenergic receptors to catecholamines. Accelerates protein catabolism, reduces glucose utilization by peripheral tissues and increases gluconeogenesis in the liver. Reduces absorption and increases excretion of calcium; inhibits sodium (and water) ACTH secretion.

Pharmacokinetics

When administered intravenously, it binds to a specific carrier protein – transcortin – by 70-80%; when high doses of the drug are administered, protein binding is reduced to 60-70% due to saturation of transcortin. Easily passes through histohematic barriers, including blood-brain and placental. Cmax is achieved within 1-2 hours. Biotransformed in the liver, mainly by conjugation with glucuronic and sulfuric acids, to inactive metabolites. The half-life from the blood T1/2 is 3-5 hours, the biological half-life is 36-54 hours. When administered parenterally, it is metabolized faster and, accordingly, the pharmacological effects are less durable. It is excreted mainly in the urine (a small part by the lactating glands) in the form of 17-ketosteroids, glucuroids, and sulfates. About 15% of Dexamethasone is excreted unchanged in the urine. When applied to the skin, absorption is determined by many factors (integrity of the skin, presence of an occlusive dressing, dosage form, etc.) and varies greatly.

Indications for use

Diseases requiring the administration of a fast-acting glucocorticosteroid, as well as cases where oral administration of the drug is impossible.

Addison's disease, congenital adrenal hyperplasia, adrenal insufficiency (usually in combination with mineralocorticoids), adrenogenital syndrome, non-suppurative thyroiditis, hypothyroidism, tumor hypercalcemia, shock (anaphylactic, post-traumatic, postoperative, cardiogenic, blood transfusion, etc.), rheumatoid arthritis in the acute phase, acute rheumatic carditis, collagenosis (rheumatic diseases - as an additional therapy for short-term treatment of exacerbation of the disease, disseminated lupus erythematosus, etc.), joint diseases (post-traumatic osteoarthritis, acute gouty arthritis, psoriatic arthritis, synoveitis in osteoarthritis, acute nonspecific tenosynovitis, bursitis, epicondylitis , ankylosing spondylitis, etc.), bronchial asthma, status asthmaticus, anaphylactoid reactions, incl. caused by drugs; cerebral edema (due to tumors, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis); nonspecific ulcerative colitis, sarcoidosis, berylliosis, disseminated tuberculosis (only in combination with anti-tuberculosis drugs), Loeffler's disease and other severe respiratory diseases; anemia (autoimmune, hemolytic, congenital, hypoplastic, idiopathic, erythroblastopenia), idiopathic thrombocytopenic purpura (in adults), secondary thrombocytopenia, lymphoma (Hodgkin and non-Hodgkin), leukemia, lymphocytic leukemia (acute, chronic), serum sickness, allergic reactions during blood transfusion , acute infectious laryngeal edema (adrenaline is the drug of first choice), trichinosis with damage to the nervous system or involvement of the myocardium, nephrotic syndrome, severe inflammatory processes after eye injuries and operations, skin diseases: pemphigus, Stevens-Johnson syndrome, exfoliative dermatitis, bullous dermatitis herpetiformis , severe seborrheic dermatitis, severe psoriasis, atopic dermatitis.

Contraindications

Hypersensitivity, systemic mycoses, amoebic infections, infectious lesions of joints and periarticular soft tissues, active forms of tuberculosis, the period before and after preventive vaccinations (especially antiviral ones), glaucoma, acute purulent eye infection (retrobulbar administration).

Pregnancy and lactation

Use during pregnancy is allowed if the expected effect of therapy outweighs the potential risk to the fetus. Breastfeeding should be stopped during treatment. Infants born to mothers who received significant doses of corticosteroids during pregnancy should be closely monitored for signs of adrenal hypofunction.

Directions for use and doses

Intended for intravenous, intramuscular, intraarticular, periarticular and retrobulbar administration. The dosage regimen is individual and depends on the indications, the patient’s condition and his response to therapy.

To prepare a solution for intravenous drip infusion, you should use an isotonic sodium chloride solution or a 5% dextrose solution. Administration of high doses of dexamethasone can be continued only until the patient's condition has stabilized, which usually does not exceed 48 to 72 hours. For adults in acute and emergency conditions, it is administered intravenously slowly, in a stream or drip, or intramuscularly at a dose of 4-20 mg 3-4 times a day. The maximum single dose is 80 mg. Maintenance dose – 0.2-9 mg per day. The course of treatment is 3-4 days, then switch to oral administration of Dexamethasone. Children - IM at a dose of 0.02776-0.16665 mg/kg every 12-24 hours. For local treatment, the following doses may be recommended:

Large joints (eg knee joint): 2 to 4 mg;

Small joints (eg, interphalangeal, temporal joint): from 0.8 to 1 mg;

Joint capsules: from 2 to 3 mg;

Tendons: from 0.4 to 1 mg;

Soft tissue: 2 to 6 mg;

Nerve ganglia: 1 to 2 mg.

The drug is re-prescribed at intervals from 3 days to 3 weeks as needed; The maximum dose for adults is 80 mg per day. For shock, adults - 20 mg intravenously once, then 3 mg/kg over 24 hours as a continuous infusion or intravenously 2-6 mg/kg once, or iv 40 mg every 2- 6 hours. For cerebral edema (adults) – 10 mg IV, then 4 mg every 6 hours IM until symptoms disappear; the dose is reduced after 2-4 days and gradually - over 5-7 days - treatment is stopped. For adrenal insufficiency (children), IM 0.0233 mg/kg (0.67/mg/m2) per day in 3 injections every third day, or daily 0.00776-0.01165 mg/kg ( 0.233-0.335 mg/m2) per day.

In case of an acute allergic reaction or exacerbation of a chronic allergic disease, dexamethasone should be prescribed according to the following schedule, taking into account a combination of parenteral and oral administration: dexamethasone injection solution 4 mg/ml: 1 day, 1 or 2 ml (4 or 8 mg) intramuscularly; dexamethasone tablets 0.75 mg: second and third days, 4 tablets in 2 divided doses per day, 4th day, 2 tablets in 2 divided doses, 5th and 6th days, 1 tablet every day, 7th day - without treatment, 8th day - observation.

Side effect

Sodium and fluid retention, loss of potassium and calcium, edema, hypokalemic alkalosis, erosive and ulcerative lesions of the gastrointestinal tract (with exacerbation of peptic ulcer up to perforation, bleeding), hemorrhagic pancreatitis, gastrointestinal atony, increased appetite, nausea and vomiting, weight gain, hiccups , hepatomegaly, abdominal bloating, ulcerative esophagitis, muscle weakness, myopathy, loss of muscle mass, osteoporosis, pathological fractures of long tubular bones, vertebral compression fractures, aseptic necrosis of the femoral and humeral head, tendon ruptures, arrhythmia, bradycardia, increased blood pressure, congestive heart disease failure, myocardial infarction and dystrophy, myocardial rupture in recent myocardial infarction, Itsenko-Cushing syndrome, HCM in low birth weight infants, hyperglycemia, hyperlipoproteinemia, negative nitrogen balance, dysmenorrhea, growth retardation in children, hirsutism, decreased immunity, suppression of regenerative and reparative processes, dizziness, headaches, mood disorders, psychosis, increased intracranial pressure with papilledema, vertigo, neuropathy, convulsions, polymorphonuclear leukocytosis, thinning and vulnerability of the skin, impaired wound healing, petechiae, ecchymosis, acne, stretch marks, erythema and changes in skin pigmentation, degeneration of the skin or subcutaneous tissues, sterile abscess, burning at the injection site (after intra-articular injection), false negative results during skin allergy tests, burning or tingling (especially in the perineum), angioedema, arthropathy resembling Charcot arthropathy, increased sweating, increased intraocular pressure, exophthalmos, glaucoma, cataracts, exophthalmos, rare cases of blindness, retinopathy of prematurity, secondary fungal or viral eye infections; thrombosis and thromboembolism, withdrawal symptoms after long-term therapy (with rapid withdrawal of corticosteroids): fever, myalgia, arthralgia, malaise. This can occur in patients even without signs of adrenal insufficiency; depression, secondary adrenal insufficiency, menstrual irregularities, development of Cushingoid conditions, growth suppression in children, decreased tolerance to carbohydrates, latent diabetes mellitus, the need to increase the dose of insulin and oral hypoglycemic agents in patients with diabetes, hirsutism; rarely - allergic reactions (rash, itching), urticaria, Quincke's edema.

Overdose

Reports of acute toxic poisoning and/or death due to glucocorticoid overdose are extremely rare. With the development of adverse events - treatment symptomatic, aimed at maintaining vital functions; Itsenko-Cushing syndrome - administration of aminoglutemide.

Interaction with other drugs

The therapeutic and toxic effects of Dexamethasone are reduced by barbiturates, phenytoin, rifabutin, carbamazepine, ephedrine and aminoglutethimide, rifampicin (accelerate metabolism); somatotropin; antacids (reduce absorption), enhance - estrogen-containing oral contraceptives. Concomitant use with cyclosporine increases the risk of developing seizures in children. The risk of arrhythmias and hypokalemia is increased by cardiac glycosides and diuretics, the likelihood of edema and arterial hypertension is increased by sodium-containing drugs and nutritional supplements, severe hypokalemia, heart failure and osteoporosis is increased by amphotericin B and carbonic anhydrase inhibitors; the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract - non-steroidal anti-inflammatory drugs. When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of viral activation and the development of infection. Concomitant use with thiazide diuretics, furosemide, ethacrynic acid, carbonic anhydrase inhibitors, amphotericin B can lead to severe hypokalemia, which can enhance the toxic effects of cardiac glycosides and non-depolarizing muscle relaxants. Weakens the hypoglycemic activity of insulin and oral antidiabetic agents; anticoagulant - coumarins; diuretic – diuretic diuretics; immunotropic – vaccination (suppresses antibody formation). Worsens the tolerance of cardiac glycosides (causes potassium deficiency), reduces the concentration of salicylates and praziquantel in the blood. It may increase the concentration of glucose in the blood, which requires dose adjustment of hypoglycemic drugs, sulfonylurea derivatives, and asparaginase. GCS increase the clearance of salicylates, therefore, after discontinuation of Dexamethasone, it is necessary to reduce the dose of salicylates. When used concomitantly with indomethacin, the Dexamethasone suppression test may give false negative results.

Features of application

Restricted for use in: peptic ulcers of the gastrointestinal tract, peptic ulcer of the stomach and duodenum, esophagitis, gastritis, intestinal anastomosis (in the immediate history); congestive heart failure, arterial hypertension, thrombosis, diabetes mellitus, osteoporosis, Itsenko-Cushing's disease, acute renal and/or liver failure, psychosis, convulsive states, myasthenia gravis, open-angle glaucoma, AIDS, pregnancy, breastfeeding. With long-term treatment (more than 3 weeks) in high doses (more than 1 mg of Dexamethasone per day) to prevent secondary adrenal insufficiency, Dexamethasone is discontinued gradually. This condition can last for several months, so if stress occurs (including during general anesthesia, surgery or trauma), an increase in the dose or administration of Dexamethasone is necessary.
Topical use of Dexamethasone may lead to systemic effects. When administered intra-articularly, it is necessary to exclude local infectious processes (septic arthritis). Frequent intra-articular administration can lead to damage to joint tissue and osteonecrosis. Patients are not recommended to overload the joints (despite the reduction in symptoms, inflammatory processes in the joint continue).

Precautionary measures

Caution should be exercised when prescribing against the background of ulcerative colitis, intestinal diverticulitis, and hypoalbuminemia. Prescription in case of intercurrent infections, tuberculosis, septic conditions requires preliminary and then simultaneous antibacterial therapy. GCS may increase susceptibility or mask symptoms of infectious diseases. Chickenpox, measles and other infections can be more severe and even fatal in non-immunized individuals. Immunosuppression often develops with long-term use of GCS, but can also occur with short-term treatment. Against the background of concomitant tuberculosis, it is necessary to carry out adequate antimycobacterial chemotherapy. Concomitant use of dexamethasone in high doses with inactivated viral or bacterial vaccines may not produce the desired result. Immunization against the background of GCS replacement therapy is acceptable. It is necessary to take into account the increased effect in hypothyroidism and cirrhosis of the liver, aggravation of psychotic symptoms and emotional lability at their high initial level, masking of some symptoms of infection, the likelihood of relative adrenal insufficiency persisting for several months (up to 1 year) after discontinuation of Dexamethasone (especially in the case of long-term use ). During a long course, the dynamics of growth and development of children are carefully monitored, an ophthalmological examination is systematically carried out, and the condition of the hypothalamic-pituitary-adrenal system and blood glucose levels are monitored. Stop therapy only gradually. It is recommended to be careful when performing any kind of surgery, the occurrence of infectious diseases, injuries, avoid immunization, and avoid drinking alcohol. In children, in order to avoid overdose, the dose is calculated based on the body surface area. In case of contact with patients with measles, chickenpox and other infections, concomitant preventive therapy is prescribed.

In rare cases, anaphylactoid reactions may occur in patients receiving parenteral corticosteroids. Patients should take appropriate precautions prior to administration, especially if the patient has a history of allergy to any drug.

Corticosteroids may aggravate systemic fungal infections and therefore should not be used in the presence of such infections.

Corticosteroids can activate latent amoebiasis. Therefore, it is recommended to exclude latent or active amebiasis before starting corticosteroid therapy.

Moderate to high doses of cortisone or hydrocortisone can cause increased blood pressure, salt and water retention, and increased potassium excretion. In this case, it may be necessary to limit salt and potassium. All corticosteroids increase calcium excretion.

Use corticosteroids with great caution in patients with recent myocardial infarction due to the risk of ventricular wall rupture.

Corticosteroids should be used with caution in patients with eye infection due to herpes simplex due to the risk of corneal perforation.

Aspirin should be used with caution in combination with corticosteroids due to the risk of hypoprothrombinemia.

In some patients, steroids may increase or decrease sperm motility and count.

May be observed:

Loss of muscle mass;

Pathological fractures of long tubular bones;

Compression fractures of the vertebrae;

Aseptic necrosis of the head of the femur and humerus.

Impact on the ability to drive a car and other potentially dangerous mechanisms. During treatment, you should not drive vehicles or engage in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Conditions for dispensing from pharmacies

By doctor's prescription.

Dexamethasone is a drug that comes in several forms: injection (by RLS), powder or eye drops. It has a spectrum of actions, such as anti-inflammatory, anti-allergenic and others - for the treatment of a number of diseases.

Dexamethasone - indications for use

The use of Dexamethasone is recommended for allergies, connective tissue diseases, malignant tumors, serum sickness, Addison-Birmer disease and others. The instructions for use describe the drug Dexamethasone as a remedy with a wide range of purposes. Contraindications, effectiveness and methods of administration (administered intramuscularly, in a dropper, orally) are also indicated for use.

Indications for the use of Dexamethasone are as follows:

• for shock diseases and external damage to the skin (burns, ruptures, open wounds, cuts, acute eczema, etc.);
• during edematous processes (cerebral edema, acute erythroderma, thyroiditis, aplasia and hypoplasia of hematopoiesis, autoimmune hemolytic anemia and others);
• anaphylactic shock, complex allergic reactions, acute eczema, urticaria;
• status asthmaticus;
• cancer (oncology), congenital adrenogenital syndrome;
• for asthma, for bronchitis;
• dermatological problems, otitis media, psoriasis;
• infectious diseases (with a course of antibiotics);
• hypothyroidism;
• nonspecific ulcerative colitis (UC) with pain;
• progressive ophthalmopathy, thrombocytopenia and more.
• agranulocytosis

Dexamethasone - instructions

The instructions for Dexamethasone include a description of the method of use. If we are talking about an injection, then dexamethasone should be used intravenously or intramuscularly, depending on the initial problem. When treating some complicated diseases (for example, tuberculosis), it is necessary to use a parallel course of antibiotics for safety.

How to take Dexamethasone? You should study the instructions. Be sure to consult your doctor. You will find all the conditions for the drug Dexamethasone - the instructions for use describe and indicate the consequences and method of administration. The average course of treatment (oral administration of the drug) lasts no more than five days, after which they switch to maintenance doses.

Dexamethasone eye drops

There is a separate form of release of the drug - Dexamethasone eye drops. They are used for allergies, inflammation, infections and other types of eye diseases (human visual organs). One drop is effective immediately after use. After a few hours, a person notices a positive effect in the form of relief from swelling, inflammation and pain. According to patient reviews, when applied, the drop easily penetrates into the orbit, into the cornea and conjunctiva.

Dexamethasone in ampoules is used in cases where another method of administration (oral) is prohibited by the doctor. The main active ingredient (according to INN) is a phosphated glucocorticoid. It has an effect on the formation of proteins, lipocortin and others. The contents of the ampoule are administered as part of a dropper, or an injection is given intravenously (intramuscular method). This method of use is prohibited if there are infections in areas near the veins. It is possible to install a dropper; in this case, a 5% sodium chloride solution should be prepared (the amount should be prescribed by a doctor).

Dexamethasone tablets

This product is affordable: its cost according to pharmacy catalogs is less than an analogue of ampoules or eye drops (data may vary in different pharmacy kiosks and chains). The dosage of the main component in this form of release of the drug is 0.5 mg per tablet. This medicinal supplement has a positive effect on the intestinal tract, improves lipid and protein metabolism (according to reviews from doctors and patients). Additionally, Dexamethasone tablets have an anti-inflammatory effect. The medicine should be stored in a cool place.

Dexamethasone - side effects

Overdose and incorrect dose calculation can cause side effects. Side effects of Dexamethasone are as follows:

• nausea, vomiting, stomach or duodenal ulcers;
• hormonal imbalance (impaired hormone secretion, failure of the adrenal glands, formation of diabetes mellitus, increased blood pressure);
• gastrointestinal bleeding, convulsions, headaches, allergies, rheumatoid arthritis, pemphigus (in rare cases);
• cataracts, vision problems, impaired vision quality, retinal detachment;
• paranoia, depression, nervousness and others;
• increased sweating, calcium secretion, pain in the neck and back;
• tendon rupture with light load, weight loss, accelerated weight loss, thinness;
• slow healing of external and internal wounds, formation of steroid acne, nitrogen imbalance, skin clearing, pallor;
• sleep disturbance, lack of appetite, constant fatigue.

Dexamethasone - contraindications

There is a list of contraindications for the use of this type of medication:

• if you have tuberculosis, you do not undergo a course of antibiotic treatment;
• hypersensitivity to constituent elements;
• cannot be used by children under six years of age;
• for diseases of fungus, herpes, smallpox;
• recent heart disease (heart attack, operations related to the cardiovascular system).

Additionally, Dexamethasone is contraindicated for renal failure and osteoporosis. Reviews from doctors claim that it can be used during pregnancy if the benefit significantly exceeds the permissible harm (for example, there is a risk of death of the fetus (child) or mother).

Inflammatory processes in modern medicine are treated with the help of hormonal drugs, which are analogues of the hormone of the adrenal cortex. Such medications include Dexamethasone injections, which allows them to be used to treat joint diseases and relieve allergic reactions.

Properties of the drug and its use

The substance Dexamethasone is a synthetic analogue of the secretion of the adrenal cortex, which is normally produced in humans, and has the following effects on the body:

1. It reacts with the receptor protein, which allows the substance to penetrate directly into the nuclei of membrane cells.
2. Activates a number of metabolic processes by inhibiting the enzyme phospholipase.
3. Blocks mediators of inflammatory processes in the immune system.
4. Inhibits the production of enzymes that affect protein breakdown, thereby improving the metabolism of bone and cartilage tissue.
5. Reduces the production of leukocytes.
6. Reduces vascular permeability, thereby preventing the spread of inflammatory processes.

As a result of the listed properties, the substance Dexamethasone has a powerful antiallergic, anti-inflammatory, anti-shock, and immunosuppressive effect.

Important! A distinctive positive property of the drug is that when administered intravenously, it has an almost instantaneous effect (when administered intramuscularly, after 8 hours).

Dexamethasone in ampoules is used for the systemic treatment of pathologies, in cases where local therapy and internal medication have not produced any results, or their use is impossible.

Dexamethasone injections can be purchased for 35-60 rubles, or replaced with analogues, including Oftan Dexamethasone, Maxidex, Metazon, Dexasone

Most often, Dexamethasone injections are used to relieve allergic reactions, as well as to treat joint diseases. The description of the drug indicates the following conditions and diseases for which Dexamethasone is used:

• Development of acute adrenal insufficiency;
• Rheumatic pathologies;
• Intestinal diseases of unknown nature;
• Shock conditions;
• Acute forms of thrombocytopenia, hemolytic, severe types of diseases of an infectious nature;
• Skin pathologies: psoriasis, dermatitis;
• , humeroscapular periarthritis, osteoarthritis, ;
• Acute laryngotracheitis in children;
• Absentminded ;
• Swelling of the brain due to traumatic brain injuries, tumors, hemorrhages, radiation injuries, neurosurgical interventions,.

Note! Dexamethasone injections have a powerful anti-inflammatory and antiallergic effect, which is 35 times more effective than the use of cortisone.

Dexamethasone injections are used in the development of acute and emergency conditions, when human life depends on the effectiveness and speed of action of the drug. The drug is usually used for a short course, taking into account vital indications.

How to use Dexamethasone injections

The instructions for Dexamethasone indicate that injections can be used starting from the first year of life, not only intramuscularly, but also intravenously. Determination of the dose depends on the form and severity of the disease, the presence and manifestations of side effects, and the age of the patient.

Dexamethasone injections intramuscularly for adults

For adults, Dexamethasone can be administered in amounts from 4 mg to 20 mg, while the maximum daily dose should not exceed 80 ml, i.e. The drug is administered three to four times a day. In the event of acute, dangerous situations, the daily dosage can be increased with the consent and under the supervision of a physician.

In the form of injections, Dexamethasone is usually used for no more than 3-4 days, and if it is necessary to continue therapy, they switch to taking the drug in tablet form.

When the expected effect occurs, the dosage of the drug begins to be gradually reduced to a maintenance dose, and discontinuation of the drug is prescribed by the attending physician.

Important! For intravenous and intramuscular use, rapid administration of Dexamethasone in a large dose should not be allowed, because this can lead to heart complications.

For cerebral edema, the dosage of the drug in the initial stage of treatment should be no more than 16 mg. After this, 5 mg of the drug is administered intramuscularly or intravenously every 6 hours until a positive effect occurs.

Dexamethasone injections intramuscularly for children

Dexamethasone is administered to children intramuscularly. The dosage is determined according to the child’s weight - 0.2-0.4 mg per day per kilogram of weight. When treating children, treatment with the drug should not be prolonged, and the dosage should be kept to a minimum depending on the nature and severity of the disease.

Dexamethasone injections during pregnancy

Dexamethasone should be used with extreme caution during pregnancy, because active forms of the drug are able to penetrate through any barriers. The medicine can have a negative effect on the fetus and cause complications both in the fetus and in the subsequently born child. Therefore, the doctor decides whether the drug can be used during pregnancy, because this is advisable only when there is a threat to the mother’s life.

Treatment of joint diseases

When therapy for joint diseases using non-steroidal drugs does not bring the expected effect, doctors are forced to use Dexamethasone injections.

The use of Dexamethasone in the treatment of joint diseases is permissible in the following conditions:

• Scleroderma with articular lesions;
• Still's disease;
• Joint syndrome with.

Note! To eliminate inflammatory processes in the joints of the arms and legs, Dexamethasone injections can in some cases be injected directly into the joint capsule. However, long-term use inside joints is unacceptable, because may cause tendon rupture.

The medicine can be administered to the joint area no more than once per course. The drug can be re-administered in this way only after 3-4 months, i.e. per year, the use of intra-articular Dexamethasone should not exceed three to four times. Exceeding this norm can cause destruction of cartilage tissue.

The intra-articular dosage can vary from 0.4 to 4 mg depending on the patient's age, weight, size of the shoulder or knee joint and the severity of the pathology.

Treatment of allergic diseases

If allergies are accompanied by severe inflammatory processes, then conventional medications will not be able to relieve this condition. In these cases, Dexamethasone is used, which is a derivative of prednisolone, which reduces the manifestation of allergic symptoms.

When to use Dexamethasone injections:

• , eczema and other skin allergic manifestations;
• Inflammatory allergic reactions on the nasal mucosa;
• Angioneurotic and.

A description of the use of Dexamethasone injections indicates that for allergies it is advisable to use injections in conjunction with oral medications. Typically, injections are given only on the first day of therapy - 4-8 mg intravenously. Next, tablets are prescribed for 7-8 days.

Side effects and contraindications

If there are serious complications and the risk of developing severe conditions, the main contraindication to the use of Dexamethasone is the presence of individual intolerance of the patient to the components of the drug.

For chronic pathologies and the use of the drug as prophylaxis, the following contraindications for use are taken into account:

Development of immunodeficiency (acquired and congenital);

• Severe form;
• Joint fractures;
• Infectious diseases of viral, fungal and bacterial nature in the active phase;
• Internal bleeding;
• Mental disorders.

The advisability of using Dexamethasone in the presence of contraindications should be taken into account in each individual case separately. In some cases, the use of the drug for any contraindication may lead to the development of side effects.

The use of Dexamethasone during pregnancy is allowed if the expected effect of therapy outweighs the potential risk to the fetus. Breastfeeding should be stopped during treatment. Infants born to mothers who received significant doses of corticosteroids during pregnancy should be closely monitored for signs of adrenal hypofunction.

Dexamethasone has a certain effect on the body, which can cause side effects:

1. It has a depressing effect on the immune system, which increases the risk of tumors and the development of severe infectious diseases;
2. Prevents healthy bone formation because inhibits absorption;
3. Redistributes deposits of fat cells, which causes fat tissue to be deposited on the torso;
4. Retains sodium ions and water in the kidneys, which interferes with the removal of adrenocorticotropic hormone from the body.

Such properties of Dexamethasone can cause negative side reactions:

• Arterial hypertension;
• Decrease in the level of monocytes and lymphocytes;
• Insomnia, mental disorders, hallucinations, depression;
• , nausea, vomiting, internal bleeding, hiccups, muscle weakness, damage to articular cartilage, tendon rupture;
• , increased intraocular fluid, cataracts, exacerbations of infectious processes in the eyes.

At the injection site, pain and local symptoms may occur - scarring, atrophy of the skin.

Note! You can reduce the negative impact of the drug by reducing the dosage, but in some cases only stopping the drug helps. In any case, if you feel unwell, you should immediately inform your doctor.

Negative consequences can occur if the course of therapy is abruptly completed without medical consent. In such cases, the development of arterial hypertension, adrenal insufficiency, and sometimes death was observed.