Instructions for use DEXAMETHASON solution

The hormonal agent shows antiallergic, anti-inflammatory and immunosuppressive activity. Injections are prescribed for antitoxic, desensitizing, antishock therapy. Due to the active components, the susceptibility of adrenergic receptors to endogenous catecholamines increases.

Compound

Composition of Dexamethasone in ampoules: dexamethasone sodium phosphate (4 mg/ml), glycerin, propylene glycol, disodium edetate, phosphate buffer solution (7.5 pH), methyl and propyl parahydroxybenzoate, water for injection.
Dexamethasone tablets contain 0.5 mg of the active substance dexamethasone sodium phosphate , as well as lactose in the form of monohydrate, MCC, colloidal anhydrous silicon dioxide, magnesium stearate, croscarmellose sodium.

Dexamethasone eye drops: dexamethasone sodium phosphate (1 mg/ml), boric acid, benzalkonium chloride (preservative), sodium tetraborate, Trilon B, water d/i.

Dexamethasone

Glucocorticosteroid (GCS) is a methylated derivative of fluoroprednisolone, inhibits the release of interleukin-1 and interleukin-2, interferon gamma from lymphocytes and macrophages. It has anti-inflammatory, antiallergic, desensitizing, antishock, antitoxic 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 the number of red blood cells (stimulates the production of erythropoietins).

Interacts with specific cytoplasmic receptors, forms a complex that penetrates the cell nucleus, stimulates the synthesis of mRNA, which induces the formation of proteins, incl. lipocortin, which mediate cellular effects. Lipocortin inhibits phospholipase A2, suppresses the release of arachidonic acid and suppresses the synthesis of endoperoxides, Pg, leukotrienes, which contribute to inflammation, allergies, etc.

Protein metabolism:

reduces the amount of protein in plasma (due to globulins) with an increase in the albumin/globulin ratio, increases the synthesis of albumins in the liver and kidneys; enhances protein catabolism in muscle tissue.

Lipid metabolism:

increases the synthesis of higher fatty acids and triglycerides (TG), redistributes fat (accumulation of fat mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

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 of glucose 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 metabolism:

retains Na+ and water in the body, stimulates the excretion of K+ (MCS activity), reduces the absorption of Ca2+ from the gastrointestinal tract, “washes out” 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 reducing the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes and organelle membranes (especially lysosomal ones).

The antiallergic 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, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, changing the body's immune response.

In chronic obstructive pulmonary disease (COPD), the action is based mainly on inhibition of inflammatory processes, inhibition of development or prevention of swelling of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, 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 small and medium-caliber bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.

Antishock and antitoxic effects are 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 the permeability of the vascular wall, membrane protective properties, and 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 corticosteroids. Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

The peculiarity of the action is significant inhibition of pituitary function and the almost complete absence of MCS activity. Doses of 1-1.5 mg/day inhibit the adrenal cortex; biological T1/2 - 32-72 hours (duration of inhibition of the hypothalamus-pituitary-adrenal cortex system).

In terms of the strength of glucocorticosteroid 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.

Pharmacodynamics and pharmacokinetics

Dexamethasone is a synthetic corticosteroid (adrenal cortex hormone). Wikipedia and the Vidal reference book indicate that the substance, when interacting with cytoplasmic receptors, forms complexes that penetrate the cell nucleus and stimulate the synthesis of m-RNA.

m-RNA, in turn, induces the biosynthesis of proteins (including enzymes that regulate vital processes in cells), which inhibit phospholipase A2, the release of arachidonic acid, the biosynthesis of endoperoxides, LT and PG, which are mediators of allergies, inflammation, pain, etc. .

Inhibits the activity of proteases, collagenase, hyaluronidase, as well as the release of inflammatory mediators from eosinophils, promotes:

• normalization of the function of the intercellular matrix of bone and cartilage tissue;
• decreased capillary permeability;
• stabilization of membranes (including lysosomal) cells;
• inhibition of the release of cytokines from macrophages and lymphocytes (gamma interferon and IL);
• involution of lymphoid tissue;
• acceleration of protein catabolism;
• decreased glucose utilization;
• increased gluconeogenesis in the liver;
• decreased absorption and increased excretion of Ca;
• Na and water retention;
• delayed ACTH secretion.

After oral administration, the substance is almost completely absorbed. The bioavailability of the drug in tablet form is up to 80%. Cmax and the maximum effect of use are observed after one to two hours. The effect after taking a single dose lasts for 2.75 days.

Binding to plasma proteins (mainly albumin ) is approximately 77%.

The substance is fat-soluble, therefore it is able to penetrate both inside the cell and into the intracellular space. The action manifests itself in the central nervous system ( pituitary gland , hypothalamus ), which is due to the ability of dexamethasone to bind to cell membrane receptors.

In peripheral tissues it binds and acts through cytoplasmic receptors. Dexamethasone breaks down in the cell (at the site of its action). Metabolization occurs primarily in the liver and, partly, in the kidneys and other tissues. The main route of elimination is through the kidneys.

Dexamethasone

Dexamethasone is a synthetic hormone of the adrenal cortex with glucocorticosteroid action (GCS). It has anti-inflammatory and immunosuppressive effects, and also affects energy metabolism, glucose homeostasis and (via negative feedback) the secretion of hypothalamic activating factor and pituitary adrenocorticotropic hormone.

GCS are fat-soluble substances and therefore easily penetrate into target cells through cell membranes. The binding of a hormone to a receptor causes conformational changes in the receptor and increases its affinity for DNA. The hormone-receptor complex enters the cell nucleus and binds to the regulatory region of the DNA molecule, also known as the glucocorticoid response element (GRE).

The activated receptor binds to GREs or specific genes and regulates messenger RNA (mRNA) transcription. The newly formed mRNA is transported to ribosomes, which then participate in the formation of new proteins. Depending on the type of target cells and cellular processes, the formation of new proteins can be either enhanced (for example, the synthesis of tyrosine transaminase in liver cells) or suppressed (for example, the synthesis of IL-2 in lymphocytes). Since receptors for GCS are found in all tissues, their action is realized in most cells of the body.

Effect on energy metabolism and glucose homeostasis:

Dexamethasone, along with insulin, glucagon and catecholamines, regulates the accumulation and expenditure of energy. In the liver, it stimulates the formation of glucose from pyruvate and amino acids and the formation of glycogen. In peripheral tissues, particularly in muscles, it reduces glucose consumption and mobilizes amino acids (from proteins), which are a substrate for gluconeogenesis in the liver. Direct effects on fat metabolism include central redistribution of adipose tissue and increased lipolysis in response to catecholamines.

Through receptors in the proximal tubules of the kidneys, dexamethasone stimulates renal blood flow and glomerular filtration, inhibits the formation and secretion of vasopressin and improves the ability of the kidneys to excrete acids.

Increases the sensitivity of blood vessels to pressor agents.

In high doses, dexamethasone suppresses the formation of collagen types I and III by fibroblasts and the formation of glycosaminoglycans; by inhibiting the formation of extracellular collagen and matrix, they slow down wound healing. Long-term use of high doses causes progressive bone tissue resorption as an indirect effect, and directly reduces its formation (stimulates the secretion of parathyroid hormone and suppresses the secretion of calcitonin). In addition, it leads to a negative calcium balance, reduces calcium absorption in the intestines and increases its excretion by the kidneys. This usually results in secondary hyperparathyroidism and phosphaturia.

Action on the hypothalamus and pituitary gland:

Dexamethasone has a 30 times more pronounced effect than endogenous cortisol. Therefore, it is a more potent inhibitor of the secretion of corticotropin-releasing factor (CRF) and adrenocorticotropic hormone (ACTH). In pharmacological doses, it inhibits the hypothalamic-pituitary-adrenal system and promotes the development of secondary adrenal insufficiency.

Adrenal insufficiency can develop as early as 5-7 days of dexamethasone administration in daily doses equivalent to 20-30 mg of prednisone or after 30 days of low-dose therapy. After discontinuation of a short course of therapy (up to 5 days) with high doses, the function of the adrenal cortex can be restored within one week; after a long course, normalization occurs later; this process usually takes up to 1 year. Some patients may develop irreversible atrophy of the adrenal cortex.

Anti-inflammatory and immunosuppressive effects

glucocorticosteroids is associated with their molecular and biochemical effects. The molecular anti-inflammatory effect is the result of the interaction of glucocorticosteroids with glucocorticoid receptors and changes in the expression of a number of genes that regulate the formation of many information molecules, proteins and enzymes involved in the process of inflammation. This leads to a decrease or prevention of the tissue response to inflammation: inhibition of the accumulation of macrophages and leukocytes, suppression of phagocytosis and release of lysosomal enzymes, synthesis of inflammatory mediators, blocking of the macrophage inhibitory factor.

Dexamethasone reduces the expansion and permeability of capillaries, reduces the adhesion of leukocytes to the endothelium, and inhibits the synthesis of Pg, leukotrienes, and thromboxanes.

Dexamethasone reduces the formation of leukotrienes by reducing the release of arachidonic acid from cellular phospholipids, which results from inhibition of phospholipase A2 activity. The effect on phospholipase is mediated by an increase in the concentration of lipocortin (macrocortin), which is an inhibitor of phospholipase A2. The suppressive effect of dexamethasone on the synthesis of prostaglandins and thromboxane is the result of a decrease in the synthesis of specific mDNA encoding the formation of cyclooxygenase.

Dexamethasone prevents or inhibits cellular immune reactions (delayed hypersensitivity reactions), reduces the number of T-lymphocytes (T-helper type I), monocytes and eosinophils, the binding of immunoglobulins to their receptors, inhibits the synthesis of interleukins: reduces T-lymphocytic blastogenesis and reduces primary immune answer. Activates humoral immunity by stimulating T-helper type II - enhances the production of antibodies. A significant effect is a decrease in the formation of tumor necrosis factor (TNF) and IL-1.

Indications for use

Why is Dexamethasone prescribed in injections and tablets?

Diseases amenable to systemic treatment are indicated for the use of Dexamethasone (if necessary, the drug can be used as an addition to the main therapy). The solution is administered intravenously and intramuscularly in cases where oral administration or local treatment is ineffective or impossible.

The drug Dexamethasone (injections and tablets) is indicated for rheumatic and allergic diseases, cerebral edema , shock of various origins, certain kidney diseases, autoimmune disorders, respiratory tract diseases, blood diseases, acute severe dermatoses, IBD, during HRT (for example, in case of insufficiency adenohypophysis/adrenal glands).

Why is Dexamethasone eye drops prescribed?

In ophthalmological practice, the use of the drug is advisable for allergic and non-purulent conjunctivitis, iridocyclitis , iritis , keratitis , keratoconjunctivitis without damaging the integrity of the corneal epithelium, blepharoconjunctivitis , scleritis , blepharitis , episcleritis , sympathetic ophthalmia , as well as for relieving inflammation after surgery or eye injury.

What is instillation of the drug into the ear indicated for?

The drug is instilled into the canal of the external ear for inflammatory and allergic diseases of the ear.

Dexamethasone for coronavirus COVID-19

Based on the results of clinical trials (not yet published), it can be assumed that Dexamethasone is most effective in treating severe cases of coronavirus. ventilators decreased by a third compared to the control group. Mortality decreased by 20% in patients receiving oxygen therapy without mechanical ventilation. No effect was observed in the treatment of mild forms of coronavirus.

Contraindications

The only contraindication for systemic use in a short course for health reasons is hypersensitivity to the components of the drug.

Contraindications to the use of Dexamethasone (IV, IM, per os):

• infectious and parasitic diseases of a bacterial or viral nature;
• systemic mycoses ;
• immunodeficiency states;
• the period before and after preventive vaccination (especially before and after antiviral vaccinations);
• myasthenia gravis , systemic osteoporosis ;
• gastrointestinal diseases ( ulcer , colitis , diverticulitis , newly created intestinal anostomosis, etc.);
• CVD diseases;
• diabetes;
• psychosis;
• acute liver and kidney failure .

Intra-articular administration is prohibited when:

• joint instability;
• pathological bleeding;
• previous arthroplasty;
• transarticular fractures;
• the presence of infected lesions of joints, intervertebral spaces,
• periarticular soft tissues;
• severe periarticular osteoporosis .

Contraindications to the use of eye drops:

• tuberculous, fungal, viral eye lesions;
• trachoma;
• glaucoma;
• epithelial damage to the cornea.

Instillations into the ear canal are contraindicated if the integrity of the eardrum is compromised.

What does Dexamethasone help with, indications and contraindications

The drug is a synthetic corticosteroid, an analogue of the hormone of the adrenal cortex. The component composition of the medication helps:

• normalize the functioning of extracellular structures of cartilage and bone tissues;
• reduce the level of capillary permeability;
• stabilize membranes;
• slow down the processes of cytokine release from lymphocytes and macrophages;
• accelerate protein catabolism;
• slow down glucose utilization and calcium absorption;
• retain water and sodium ions in tissues.

The processing of components occurs in the liver, partially in the kidneys and other organs. Metabolic products are excreted through the genitourinary system.

The drug is used against pathologies amenable to systemic therapy, as an addition to the main course of treatment. Intravenous and intramuscular injections are given when tablets or local medications are ineffective.

Dexamethasone is prescribed to patients:

• with allergies and rheumatic diseases;
• swelling of brain tissue;
• shock states of various origins;
• individual kidney lesions;
• autoimmune disorders;
• diseases of the respiratory tract, blood;
• acute severe dermatoses.

The drug is prescribed for hormone replacement therapy and the fight against inflammatory bowel pathologies. Dexamethasone is contraindicated:

• with hypersensitivity to the component composition;
• infectious, parasitic diseases of bacterial and viral origin;
• systemic mycoses, osteoporosis, immunodeficiency;
• myasthenia gravis, ulcers, colitis and other gastrointestinal diseases;
• lesions of the cardiovascular department;
• diabetes mellitus, psychosis, acute renal or liver failure.

The medicine is not injected into the joints if they are unstable, spontaneous bleeding of the apparatus, fractures or infectious lesions. The ban includes periarticular osteoporosis, the postoperative period - after arthroplasty.

Side effects of Dexamethasone

The incidence and severity of side effects of Dexamethasone depend on the dosage of the drug, duration of use of the drug, and the possibility of use taking into account the circadian rhythm.

Systemic side effects of Dexamethasone:

• from the sensory organs and the nervous system: delirium, euphoria, depressive/manic episode, disorientation, hallucinations, increased ICP with congestive optic disc syndrome (benign intracranial hypertension , the development of which is a consequence of a rapid reduction in the dosage of the drug and is accompanied by blurred vision and headaches), vertigo , sleep disturbances, headache, dizziness, loss of vision (when the solution is administered in the area of ​​the nasal concha, head, neck, scalp), cataract with localization of clouding in the back of the lens, glaucoma , eye hypertension with the possibility of damage to the optic nerve, development of secondary viral/fungal infection of the eye, steroid exophthalmos ;
• from the cardiovascular system: arterial hypertension , myocardial dystrophy , ECG changes characteristic of hypokalemia, hypercoagulation , thrombosis , if predisposed - the development of CHF, with parenteral use - rushes of blood to the head;
• from the digestive system: nausea, hiccups, vomiting, pancreatitis , erosive and ulcerative lesions of the digestive canal, increased/decreased appetite, erosive esophagitis;
• metabolic disorders: peripheral edema due to water and Na+ retention, nitrogen deficiency, hypocalcemia , hypokalemia , weight gain;
• endocrine disorders: hyper- or hypocorticism syndrome, manifestation of latent diabetes mellitus , steroid diabetes, growth retardation in children, irregular menstrual bleeding, hirsutism ;
• from the locomotor system: joint or muscle pain, back pain, steroid myopathy, tendon rupture, osteoporosis , muscle weakness, decreased muscle mass; with intra-articular administration of the solution, the intensity of pain in the joint may increase;
• from the skin: stretch marks , ecchymosis and petechiae, steroid acne, thinning of the skin, increased sweating, poor wound healing;
• hypersensitivity reactions: urticaria , skin rashes, difficulty breathing, stridor, facial swelling, anaphylactic shock .

Also possible: decreased immune system function, activation of infectious diseases, withdrawal syndrome (general weakness, lethargy, nausea, anorexia, abdominal pain).

Local reactions when injecting the solution: numbness, burning, paresthesia, pain, infection at the injection site, scarring at the injection site, hypo- or hyperpigmentation. When administered intramuscularly, the process of atrophy of the subcutaneous tissue and skin may begin.

Reactions to the use of ophthalmic forms: long-term (more than 3 weeks in a row) use of eye drops may be accompanied by an increase in intraocular pressure, the formation of glaucoma with damage to the optic nerve fibers, posterior subcapsular cataracts , visual impairment (for example, loss of its fields), thinning/perforation cornea, spread of infection (bacterial or herpetic).

In case of hypersensitivity to benzalkonium chloride or dexamethasone blepharitis and conjunctivitis are possible .

Local reactions are manifested by burning and itching of the skin, irritation, and dermatitis.

Instructions for use of Dexamethasone (Method and dosage)

Dexamethasone injections, instructions for use

Methods of administration of Dexamethasone: intravenous, intramuscular, local.

The daily dose is equivalent to 1/3-01/2 of the oral dose and ranges from 0.5 to 24 mg. It should be given for 2 injections. Treatment is carried out in the minimum effective dose and for the shortest possible course. The drug is discontinued gradually. For long-term use, the highest dose is 0.5 mg/day.

Injections are prescribed for emergency conditions, as well as in cases where oral administration is not possible. In emergency conditions, higher doses of the drug (4-20 mg) are allowed, and the dose is repeated until the required therapeutic effect is achieved. The daily dose in rare cases exceeds 80 mg.

Once the required results are achieved, treatment is continued at a dose of 2-4 mg, gradually reducing it until the drug is completely discontinued.

To maintain a long-term effect, injections are indicated at intervals of 3-4 hours. It is also possible to administer Dexamethasone intravenously by long-term drip infusion.

After completion of the acute phase of the disease, the patient is transferred to taking the drug orally.

No more than 2 ml of the product can be injected into the muscle at the same place.

The treatment regimen depends on the indications:

• for shock - 2-6 mg/kg IV bolus, repeated injections - every 2-6 hours or as a long-term infusion using a dose of 3 mg/kg/day. The drug is prescribed as an addition to the main antishock therapy. The administration of these doses is permissible only for conditions that threaten the patient’s life, and, as a rule, this period lasts up to 72 hours.
• For cerebral edema (CBE), treatment begins with a dose of 10 mg (iv), then - until symptoms stop (within 12-24 hours) - 4 mg is administered every 6 hours. After 2-4 days, the dose is reduced and Dexamethasone administration is stopped within 5-7 days.
• For cancer, maintenance therapy may be required - 2 mg IV or IM 2 or 3 times a day.
• In case of acute AMG, the patient requires short-term intensive therapy. The loading dose of the drug for an adult is 50 mg, for a child weighing up to 35 kg - 20 mg (injected into a vein). After this, the dose is gradually reduced while increasing the intervals between drug administrations.
• For allergies (in particular, with exacerbation of chronic diseases of an allergic nature and with acute self-limiting reactions), parenteral administration is combined with oral administration of the drug. Allergy injections are given only on the first day, injecting the patient with 4 to 8 mg of Dexamethasone into a vein. On days 2-3, take 1 mg of the drug orally 2 times, on days 4-5 - 2 times 0.5 mg, on days 6-7 - 0.5 mg (once). On day 8, the effectiveness of treatment is assessed.

When status asthmaticus requires immediate intravenous administration of the drug, the combination Dexamethasone + Eufillin . The first medicine reduces the release of mediators ( heparin , histamine , serotonin ) from the cell, protects tissues from destructive processes, prevents the formation of arachidonic acid metabolites, and Eufillin reduces the resistance of blood vessels, relieves bronchospasm , inhibits platelet aggregation and dilates coronary vessels.

Instructions for Dexamethasone in ampoules for topical use

When applying the solution topically, 2 to 4 mg is injected into large joints, and 0.8 to 1 mg into small joints. Treatment of soft tissue infiltrates involves the use of 2-6 mg of the drug. 1-2 mg of the drug should be injected into the nerve ganglia, 2 to 3 mg into the joint capsules, and 0.4 to 1 mg into the synovial vagina. The dose is administered once. The course lasts from 3-5 to 14-20 days.

For children, the drug is administered in minimally effective doses.

Use of Dexamethasone in ampoules for inhalation

Inhaled use of Dexamethasone is indicated for acute inflammatory diseases of the respiratory tract (for example, bronchitis or laryngitis , as well as bronchial obstruction ).

Inhalations with Dexamethasone for children should be done 3 times a day, mixing 0.5 ml of the drug with 2-3 ml of saline solution. As a rule, treatment is continued for 3 to 7 days.

You can dilute the drug in saline in a ratio of 1:6, and then use 3-4 ml of the prepared solution for inhalation.

Dexamethasone tablets, instructions for use

The dose for oral administration is selected individually depending on the type of disease, the activity of its course and the nature of the patient’s response to the prescribed treatment.

The average daily dose ranges from 0.75 to 9 mg. For severe diseases, the dose can be increased, and it is divided into several doses. The highest dose is 15 mg/day.

The optimal dosage for children is selected depending on age, and usually ranges from 2.5 to 10 mg/m2/day. It must be divided into 3 or 4 doses.

The duration of the course is determined by the nature of the pathological process and the patient’s body’s response to treatment. In some cases, Dexamethasone is continued for several months.

Liddle's test

The test with Dexamethasone is carried out in the form of small and large tests.

A small test involves prescribing the patient 0.5 mg of Dexamethasone 4 times a day at regular intervals (6 hours). Urine to determine free cortisol should be collected from 8:00 to 8:00 on the second day before the drug is prescribed and at the same time intervals after taking the required dose.

2 mg of Dexamethasone taken over the course of 24 hours suppresses the production of corticosteroids in almost every healthy person. The cortisol content 6 hours after taking the last 0.5 mg of the drug does not exceed 135-138 nmol/l. A decrease in the daily excretion of free cortisol below 55 nmol, and 17‑OX below 3 mg/day. eliminates hyperfunction of the adrenal cortex.

In hypercortisolism syndrome, no changes in drug secretion are observed.

A large test involves prescribing 2 mg once every 6 hours for 48 hours. Hypercortisolism syndrome diagnosed by reducing free cortisol and 17-OCS levels by 50 (or more) percent.

In patients with ACTH-ectopic syndrome and adrenal tumors, drug excretion rates do not change. In some cases, with ACTH-ectopic syndrome, they do not change even when taking 32 mg of Dexamethasone per day.

Dexamethasone eye drops, instructions for use

Eye drops are intended for topical use. In case of severe inflammation, in the first day or two of treatment, 1-2 drops are instilled into the conjunctival sac. every 2 hours. Further, the intervals between instillations are extended to 4-6 hours.

To prevent the development of inflammation in the first 24 hours after injury or surgery, the patient is instilled 4 times a day. 1-2 drops, then treatment is continued at the same dose, but with a smaller frequency of applications (usually the procedure is repeated 3 times a day). The course lasts 14 days.

As an alternative to drops, Dexamethasone ointment can be used. It is squeezed out into a 1-1.5 cm strip and placed behind the lower eyelid. The frequency of procedures is 2-3 during the day. You can combine the use of ointment and drops (for example, drops during the day and ointment before bed).

To treat otitis media , the drug is injected into the ear canal of the diseased ear 2-3 times a day. 3-4 drops each.

Instructions for use for Dexamethasone injections

The medication is administered intravenously or intramuscularly; it is recommended for emergency conditions. In difficult cases, the dosage is increased from 4 to 20 mg, injections are repeated until the required therapeutic effect is obtained, the daily dose does not exceed 80 mg. After stabilization of the condition, treatment continues at 2-4 mg, with a gradual decrease in volumes until the medication is discontinued.

To create a long-lasting effect, injections are administered every 3-4 hours; the use of droppers with a solution is allowed. The treatment regimen depends on the indications:

• shock states - from 2 to 6 mg per kilogram of body weight, repeated after 2-6 hours, for 3 days;
• swelling of brain tissue - the first dose is 10 mg, later to suppress symptoms - 4 mg every 6 hours, for 1-2 days, on days 2-4 the dosage is reduced, the total time of therapy does not exceed 1 week;
• oncology - maintenance treatment 2 mg 2-3 times a day;
• allergies – 4-8 mg once a day.

The dose of the drug and its changes depend on health indicators and relief of clinical signs of acute phases of pathologies.

special instructions

Application in bodybuilding

Taking Dexamethasone provokes a shift in metabolism towards anabolism, which, when using even a small dose of anabolic steroids, can accelerate the growth of muscle mass and make it more significant.

In addition, by suppressing the secretion of catabolic hormones , the drug helps increase endurance, accelerates the athlete's recovery after training, and suppresses pain and inflammation when ligaments and joints are damaged.

Since Dexamethasone belongs to the group of stress hormones, their use in sports is allowed only for short-term courses.

Dexamethasone in veterinary medicine

In veterinary medicine, the drug is used as an active anti-shock, anti-allergenic and anti-inflammatory agent.

Why is Dexamethasone prescribed to cats and dogs? The drug is used to treat shock conditions, injuries, arthritis, bursitis, allergic diseases, edema, poisoning, ketosis and acute mastitis.

The therapeutic dose for dogs and cats is 0.1-1 ml (depending on the size of the animal and indications).

Dexamethasone analogs

Level 4 ATC code matches:
Prednisolone

Polcortolon

Cortef

Dexazone

Metipred

Cortisone

Flosteron

Depo-Medrol

Medrol

Solu-Medrol

Diprospan

Kenalog

Analogues of solution and tablets:

• Dexazone
• Dexamethasone-Vial
• Dexamed
• Megadexane
• Dexamethasone-Ferrain

Similar preparations for eye drops:

• Dexamethasone-LENS
• Dexapos
• Ozurdex
• Maxidex
• Dexamethasonelong

The drug Maxidez, unlike other analogues, has 2 dosage forms: drops and eye ointment. Dexamethasone ointment can be replaced with Hydrocortisone .

Which is better: Prednisolone or Dexamethasone?

Prednisolone is a synthetic analogue of hydrocortisone , which is considered a standard agent with an average duration of action and is most often used in clinical practice.

Compared to Hydrocortisone, its glucocorticoid activity is 4 times higher, however, in terms of mineralocorticoid activity, Prednisolone is inferior to Hydrocortisone.

Dexamethasone is a long-acting medicine. Unlike its analogue, the drug is fluoridated. The glucocorticoid activity of the drug is 7 times higher than that of prednisolone . However, it does not have a mineralocorticoid effect.

To a greater extent than other drugs, it provokes inhibition of the hypothalamic-pituitary-adrenal axis, causes severe disturbances in calcium, lipid and carbohydrate metabolism, has a psychostimulating effect, and therefore is not recommended for long-term use.

Dexamethasone during pregnancy and when planning pregnancy

Tablets are not used during treatment and breastfeeding.

Drops are not recommended during pregnancy. If used during lactation, breastfeeding should be stopped.

Injections during pregnancy are used only for health reasons (especially in the 1st trimester).

When planning pregnancy, Dexamethasone can be used in situations where the reason for the inability to get pregnant/bear a child is hyperandrogenism . During pregnancy, it is most often prescribed when there is a threat of miscarriage, when the immune system perceives the embryo as a foreign body (the drug helps suppress immune activity).

Reviews of Dexamethasone during pregnancy allow us to conclude that although the drug is in some cases the only chance to get pregnant and maintain a pregnancy, its use is almost always associated with certain inconveniences.

After all, Dexamethasone - what is it? A powerful hormonal drug. Therefore, almost all women who took it noted changes in body weight, hormonal disorders, and a tendency to depression.

Dexamethasone

Use during pregnancy and breastfeeding

During pregnancy (especially in the first trimester), as well as during lactation, dexamethasone is used taking into account the expected therapeutic effect and negative effect on the fetus. With long-term therapy during pregnancy, the possibility of fetal growth disturbances cannot be excluded. If used at the end of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

Use for liver dysfunction

Use with caution in severe chronic liver failure.

Use for renal impairment

Use with caution in severe chronic renal failure.

Use in children

Contraindications for external use: children under 2 years of age, for itching in the anus - up to 12 years.

special instructions

Caution should be used in case of parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently suffered, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles, amoebiasis, strongyloidiasis (established or suspected), systemic mycosis;
active and latent tuberculosis. Use for severe infectious diseases is permissible only against the background of specific therapy. It should be used with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, 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.

Reviews about Dexamethasone

Reviews of Dexamethasone injections and reviews of Dexamethasone tablets allow us to draw the following conclusions: the drug is effective, has a wide range of indications (it is used as a remedy for allergies , for oncology , cerebral edema (including post-radiation), bacterial meningitis , for prevention and treatment vomiting and nausea during chemotherapy , to stimulate the synthesis of surfactant in the alveoli of the lungs in premature infants, when planning pregnancy, etc.), can only be used as prescribed by a doctor, in short courses and only after possible contraindications have been established.

Despite its effectiveness, the drug provokes pronounced adverse reactions, and this is its main disadvantage.

Reviews from doctors about eye drops and dosage forms for systemic use indicate that the danger of hormonal drugs is often exaggerated.

The main thing to consider when prescribing them is the presence/absence of direct contraindications. In addition, dose selection should be based on all available indicators: weight, age, test results for relevant hormones, etc.

The drug can be used in veterinary medicine. Why is Dexamethasone prescribed to animals? In principle, the medicine has the same indications as in humans. It is used for allergies, injuries, shock conditions.

Instructions for use DEXAMETHASON solution

Allergic reactions may occur (although rarely) during parenteral use of corticoids. Appropriate measures should be taken before starting treatment, taking into account this possibility (especially in patients with a history of allergic reactions to any drugs).

Patients undergoing long-term treatment with dexamethasone may experience corticoid withdrawal syndrome. Therefore, the dosage of dexamethasone should be gradually reduced.

If during therapy or when discontinuing a drug the patient is exposed to unexpected stress (trauma, surgery or serious illness), then the dose of dexamethasone should be increased or hydrocortisone or cortisone prescribed. In patients who have experienced severe stress after discontinuation of long-term dexamethasone, dexamethasone should be restarted as induced adrenal insufficiency may persist for several months after discontinuation of treatment.

Treatment with dexamethasone or natural glucocorticoids may mask signs of existing or new infection and signs of interstitial perforation.

Dexamethasone can aggravate the course of systemic fungal infections, latent amebiasis and pulmonary tuberculosis.

In patients with active pulmonary tuberculosis, dexamethasone should be prescribed (in combination with antituberculosis therapy) in cases of fulminant or severe disseminated pulmonary tuberculosis. Patients with inactive tuberculosis who are taking dexamethasone or patients with a positive tuberculin test should receive chemoprophylaxis.

Particular caution and close medical monitoring should be performed in patients with osteoporosis, hypertension, heart failure, tuberculosis, glaucoma, liver failure, renal failure, diabetes, active gastric and duodenal ulcers, recent intestinal anastomosis, ulcerative colitis and epilepsy. Particular attention should be paid to patients in the first weeks after myocardial infarction, as well as patients with thromboembolism, asthenic bulbar palsy, glaucoma, hypothyroidism, psychosis or psychoneurosis, and elderly patients.

During treatment with dexamethasone, an exacerbation of diabetes or a transition from a latent form to the form of clinical manifestations of diabetes may occur.

During long-term treatment, it is necessary to monitor serum potassium levels. Vaccination with live vaccines is contraindicated during treatment with dexamethasone. Immunization with killed viral or bacterial vaccines does not lead to the expected increase in antibodies and does not have the expected protective effect. Dexamethasone is usually not prescribed 8 weeks before and 2 weeks after vaccination. Patients receiving or taking high doses of dexamethasone for a long time should avoid contact with people with measles; In case of accidental contact, prophylactic treatment with immunoglobulin is recommended. Caution is advised in patients recovering from recent surgery and a bone fracture, as dexamethasone may delay the healing of wounds and fractures.

The effect of glucocorticoids is potentiated in patients with liver cirrhosis or hypothyroidism. Intra-articular administration of corticoids can cause local and systemic effects. Frequent use may cause damage to articular cartilage and bone necrosis.

Before intra-articular injection, synovial fluid should be evacuated from the joint and examined (for possible infection). Injecting corticosteroids into infected joints should be avoided. If septic inflammation of the joint develops after the injection, then appropriate antibacterial treatment must be started.

Patients should be informed that it is necessary to avoid putting stress on the joints into which the injection was performed until the inflammatory process has completely resolved.

Injections into unstable joints are not recommended. Corticosteroids may interfere with allergy skin test results. Dexamethasone is used in children and adolescents only under strict indications. During treatment with dexamethasone, the growth and development of children and adolescents should be carefully monitored.

Special information about some of the ingredients of the drug.

This drug contains less than 1 mmol (23 mg) sodium per dose, which is a negligible amount.

Pregnancy and lactation.

Dexamethasone should be prescribed to pregnant women only in selected urgent cases when the expected benefit to the mother justifies the risk to the fetus.

Particular care should be taken in case of preeclampsia. According to general recommendations for glucocorticoid treatment during pregnancy, the lowest effective dose to control the underlying disease should be used.

Glucocorticoids are excreted in small quantities in breast milk. Therefore, breastfeeding is not recommended for mothers taking dexamethasone, especially when using high physiological doses (about 1 mg). This can lead to fetal growth retardation and decreased secretion of endogenous corticosteroids.

Impact on the ability to drive a car or use other machinery.

Dexamethasone does not affect the ability to drive a car or operate machinery.

Dexamethasone price, where to buy

In Russian pharmacies, the price for Dexamethasone eye drops starts from 80-150 rubles. The injections are sold for 120-170 rubles. for package No. 5, the price of tablets is from 40 rubles. Eye ointment with dexamethasone can be bought from 150 rubles.

In Ukraine, the price of Dexamethasone in 4 mg ampoules is from 15 UAH. Eye drops can be bought from 20 UAH. The price of Dexamethasone in tablets is from 30 UAH.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

ZdravCity

• Dexamethasone tablets 0.5 mg 10 pcs. JSC KRKA, d.d., Novo Mesto
  36 rub. order
• Dexamethasone eye drops 0.1% bottle 10ml NOT DEFINED

  84 rub. order

• Dexamethasone eye drops 0.1% 10mlS.C.Rompharm Company SrL

  123 RUR order

• Dexamethasone eye drops 0.1% vial. 5ml RUP Belmedpreparaty

  76 RUR order

• Dexamethasone hl. drops 0.1% tube dropper 10ml RenewalАО Update PFK

  130 rub. order

Pharmacy Dialogue

• Dexamethasone (amp. 4 mg/1 ml 1 ml No. 5)KPKA

  59 RUR order

• Dexamethasone tablets 0.5 mg No. 56Update PFC JSC

  48 RUR order

• Dexamethasone (amp. 4 mg/1 ml 1 ml No. 25) Ellara LLC

  140 rub. order

• Dexamethasone 0.1% eye drops 10ml dropper bottleUpdate PFC JSC

  129 RUR order

• Dexamethasone (0.5 mg tablet No. 10)KPKA

  41 rub. order

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Pharmacy24

• Dexamethasone phosphate 0.4% 1 ml No. 10 solution PAT "Farmak", Ukraine
  20 UAH. order
• Dexamethasone 0.5 mg No. 10 tablets KPKA, d.d., Novo Mesto, Slovenia

  35 UAH order

• Dexamethasone 4 mg/ml 1 ml N5 solution AT Lekhim-Kharkiv, Ukraine

  10 UAH.order

• Dexamethasone Darnitsa 4 mg/ml 10 ampoules of 1 ml injection solution PrAT" Pharmaceutical company "Darnitsa", Ukraine

  28 UAH order

• Dexamethasone-Biopharma 0.1% 10 ml eye drops TOV"FZ "Biopharma", Ukraine

  19 UAH order

PaniPharmacy

• DEXAMETHASONE liquid Dexamethasone suspension. eye. 0.1% 5ml Poland, Warsaw Federal Law

  58 UAH order

• Dexamethasone-Darnitsa solution d/in. 4 mg/ml amp. 1 ml No. 10

  28 UAH order

• Dexamethasone ampoule Dexamethasone solution d/in. 0.4% amp. 1ml No. 5 Ukraine, Darnitsa ChAO

  12 UAH order

• Dexamethasone liquid Dexamethasone h/c 0.1% 10ml Ukraine, Darnitsa ChAO

  15 UAH order

• DEXAMETHASONE ampoule Dexamethasone solution d/in. 4mg amp. 1ml No. 25 Slovenia, KRKA dd Novo Mesto

  337 UAH. order

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