Help on Tele2, tariffs, questions

Pharmacodynamics: 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 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, in particular in muscles, it reduces glucose consumption and mobilizes amino acids (from proteins), which are the substrate of gluconeogenesis in the liver. Direct effects on fat metabolism are manifested by central redistribution of adipose tissue, and increased lipolysis in response to the effects of 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; due to inhibition of the formation of extracellular collagen and matrix, they slow down wound healing. Long-term, high doses cause progressive resorption of bone tissue, as an indirect effect, and directly reduce its formation (stimulates the secretion of parathyroid hormone and suppresses the secretion of calcitonin). In addition, it leads to a negative calcium balance - it reduces the absorption of calcium in the intestines and increases its excretion by the kidneys. This usually results in secondary hyperparathyroidism and phosphaturia. Effect 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 years of age. the day of administration of dexamethasone 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. The anti-inflammatory and immunosuppressive effects of glucocorticosteroids are also 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) and 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 the primary immune response. 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. Pharmacokinetics: the maximum concentration of dexamethasone is achieved in the blood plasma within 5 minutes after intravenous administration (IV) and 1 hour after intramuscular administration (IM). When administered locally into joints or soft tissues (into lesions), absorption occurs more slowly than with intramuscular administration. When administered intravenously, the effect develops quickly; when administered intramuscularly, the clinical effect develops after 8 hours. The effect is long-lasting: from 17 to 28 days after IM application and from 3 days to 3 weeks after topical application. The transition of dexamethasone phosphate to dexamethasone in blood plasma and synovial fluid occurs quickly. In blood plasma, approximately 77% of dexamethasone is bound to proteins, mainly albumin. Only a small amount of dexamethasone binds to non-albumin proteins. Penetrates into extra- and intracellular spaces. In the central nervous system (hypothalamus, pituitary gland), its effects are due to binding to membrane receptors. In peripheral tissues it binds to cytoplasmic receptors. The decay occurs at the site of its action, i.e. in the cell. Metabolized primarily in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites, as well as in the kidneys and other tissues. It is excreted primarily by the kidneys. Half-life (T1/2) -190 min.

Other dosage forms: eye ointment, tablets.

Dexamethasone ampoules are produced by several manufacturers; in addition, there are synonyms:

• Decadron;
• Dexaven;
• Dexazone;
• Dexamed;
• Dexafar;
• Dexon.

Price

Average price online* 197 rub. (pack of 25 ampoules)

Where can I buy:

Instructions for use

Dexamethasone is a drug that is used as an anti-inflammatory agent and also relieves attacks of allergies and itchy skin. The medicine belongs to the group of glucocorticoids, therefore it is used only as prescribed by the attending physician.

Description and properties

Dexamethasone is a broad-spectrum hormonal agent. The drug has the following properties:

• effectively relieves inflammation;
• eliminates allergic reactions;
• has an anti-shock effect;
• normalizes water balance;
• participates in glycogen synthesis;
• maintains glucose homeostasis;
• helps to establish the exchange of sodium and potassium;
• exhibits immunosuppressive activity;
• relieves itching (on the skin and mucous membranes).

The main component of the drug is dexamethasone, which has a powerful effect on the epicenter of the lesion, allowing you to quickly cope with even high-intensity inflammatory processes.

"Dexamethasone" for injection is available in the form of a solution in ampoules of 1 and 2 ml (25 ampoules per package).

The therapeutic effect occurs:

• with intravenous administration - instantly (within 5-15 minutes);
• when administered intramuscularly – after 8 hours.

The drug has a long-term effect, which reaches from 3 to 4 weeks (when injected into the muscle) and from 3 days to 3 weeks when used topically (injecting the substance into the affected area).

Indications

Dexamethasone in the form of injections is usually used for severe inflammatory processes, as well as allergic reactions to external irritants (usually in emergency cases).

Indications for the use of Dexamethasone injections are:

• brain tumors accompanied by the formation of edema;
• swelling of the brain resulting from traumatic brain injury or surgery;
• bronchial asthma (in the acute stage);
• acute bronchitis;
• dysfunction (acute failure) of the adrenal cortex;
• state of shock (including anaphylactic shock);
• therapy for lymphoma and leukemia in patients over 18 years of age;
• leukemia (acute) in pediatric patients;
• hypercalcemia due to cancer (if oral use is impossible);
• the need for diagnostic examination of the adrenal cortex;
• conjunctivitis and other eye diseases (if there is a risk of vision loss or significant deterioration);
• fibrous compacted folliculitis;
• granuloma annulare;
• sarcoidosis;
• severe allergy attacks (extreme);
• joint damage accompanied by inflammation of a non-infectious nature.

Directions for use and doses

Dexamethasone is a prescription hormonal drug; the injectable form must be prescribed and administered by a specialist. Self-medication is fraught with consequences.

“Dexamethasone” can be diluted with saline or glucose before use, but it is strictly forbidden to mix the drug with other medications (in the same syringe or dropper bottle).

The initial dosage for adult patients is 0.5-0.9 mg (administered intravenously or intramuscularly), after which the dosage regimen can be adjusted if necessary.

For allergic diseases, the drug is administered intramuscularly in the first injection of 4-8 mg. Further treatment is preferably carried out with tablets.

Intravenous administration through a syringe is performed when emergency assistance is needed. Even in this case, the administration of the drug should last several minutes.

It is preferable to administer intravenously by infusion (dropper). For infusion, isotonic sodium chloride solution or 5% dextrose solution is used.

For the treatment of shock - iv 20 mg for the first injection, then 3 mg/kg over 24 hours in the form of iv infusion or iv bolus - from 2 to 6 mg/kg as a single injection or 40 mg as a single dose injections given every 2-6 hours; possible intravenous administration of 1 mg/kg once. Shock therapy should be discontinued as soon as the patient's condition has stabilized, the usual duration being no more than 2-3 days.

For oncology:

For nausea and vomiting during chemotherapy, 8-20 mg is prescribed intravenously 5-15 minutes before the chemotherapy session.

Dosage of the drug for other routes of administration:

Important!

The drug is administered into the joint area only once, subsequent administration is allowed after 3-4 months. The total number of injections per year (in one joint) should not exceed 3-4 times, otherwise there is a risk of damage to cartilage tissue.

Dosage of the drug when used in children (intramuscular route only)

Contraindications

Dexamethasone injections are used in short courses, however, there are certain restrictions for its use, for example:

• osteoporosis;
• fungal and viral lesions of the organs of vision, purulent eye infections, trachoma, glaucoma, corneal pathologies (for use in ophthalmology);
• infectious diseases without treatment (viral, fungal and bacterial);
• lactation;
• Cushing's syndrome;
• idiopathic thrombocytopenic purpura (for injection into the muscle);
• intolerance to the components of the drug.

Dexamethasone should be used with caution in persons with the following diagnoses:

• cirrhosis of the liver;
• hepatitis;
• renal dysfunction;
• psychosis.

Use during pregnancy and breastfeeding

Use during pregnancy is possible only for health reasons. The drug crosses the placenta, FDA category of action on the fetus is C (animal studies revealed a negative effect on the fetus, there were no adequate studies in pregnant women).

Unfortunately, sometimes a situation arises that threatens the patient’s life; in this case, there are no alternatives. All glucocorticoids are classified as category C.

Side effects

When administering Dexamethasone injections, the following undesirable consequences were diagnosed:

• redness of the skin in the face and neck;
• convulsions;
• heart rhythm disturbances;
• nervous excitability;
• feeling of anxiety;
• violation of orientation in space;
• euphoria, hallucinations;
• cataract;
• glaucoma;
• increased intraocular pressure;
• local reactions (with local administration);
• burning and numbness at the injection site;
• loss of vision.

Important! With prolonged intra-articular injection there is a risk of tendon rupture.

Other

The drug is sold by prescription. Shelf life – 2 years from the date of production. Store in the refrigerator or at room temperature (not higher than 25 degrees).

• Instructions for use Dexamethasone
• Composition of the drug Dexamethasone
• Indications for the drug Dexamethasone
• Storage conditions for the drug Dexamethasone
• Shelf life of Dexamethasone

ATX Code: Hormones for systemic use (excluding sex hormones and insulins) (H) > Corticosteroids for systemic use (H02) > Corticosteroids for systemic use (H02A) > Glucocorticoids (H02AB) > Dexamethasone (H02AB02)

Release form, composition and packaging

Injection transparent, colorless or slightly yellowish.

Excipients: glycerol, disodium edetate, disodium hydrogen phosphate dihydrate, d/i water.

1 ml - ampoules (25) - cardboard boxes.

Description of the drug DEXAMETHASONE solution created in 2010 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Belarus. Update date: 06/08/2011

pharmachologic effect

Dexamethasone is a synthetic adrenal hormone (corticosteroid) with glucocorticoid activity. It has anti-inflammatory and immunosuppressive effects, and also affects energy metabolism, glucose homeostasis, and (through a negative feedback effect) the secretion of hypothalamic releasing hormone and trophic hormone of the adenohypophysis.

Pharmacokinetics

After intravenous administration, dexamethasone phosphate reaches Cmax in plasma within 5 minutes and one hour after intramuscular injection. After local application as an injection into a joint or soft tissue (wound), absorption is slightly lower than after intramuscular administration. After IV application, the onset of action occurs quickly; after IM application, the clinical effect is achieved after 8 hours. The effect lasts for a long time: 17-28 days after IM application, and 3 days - 3 weeks after topical application. The biological half-life of dexamethasone is 24-72 hours. In plasma and synovial fluid, dexamethasone phosphate is quickly converted into dexamethasone. The drug is primarily metabolized in the liver, but is also metabolized in the kidneys and other tissues. Mainly excreted in urine.

Indications for use

Dexamethasone is prescribed IV or IM in emergency cases, or when internal use is not possible.

Endocrine disorders: replacement therapy for primary and secondary (pituitary) adrenocortical insufficiency (except for acute insufficiency, where it is better to use cortisone and hydrocortisone, due to their stronger mineralocorticoid effect);

Rheumatic diseases: rheumatoid arthritis, including adolescent chronic arthritis, and extra-articular manifestations of rheumatoid arthritis (rheumatic lungs, cardiac changes, ocular changes, cutaneous vasculitis), Systemic connective tissue diseases, vasculitic syndromes.

Skin diseases: pemphigus, severe exudative erythema multiforme (Stevens-Johnson syndrome), exfoliative dermatitis, bullous dermatitis herpetiformis, exudative erythema (severe), erythema nodosum, seborrheic dermatitis (severe), psoriasis (severe), urticaria (not responding to standard treatment), fungal mycosis, dermatomyositis, scleroderma, Quincke's edema.

Allergic diseases (not responding to conventional treatment): asthma, contact dermatitis, atopic dermatitis, serum sickness, allergic rhinitis, drug allergies, urticaria after blood transfusion.

Eye diseases: diseases that threaten vision (acute central chorioretinitis, retrobulbar neuritis), allergic diseases (conjunctivitis, uveitis, scleritis, keratitis, inflammation of the iris), systemic immune diseases (sarcoidosis, temporal arteritis), proliferative changes in the orbit (endocrine ophthalmopathy, false tumor) , sympathetic ophthalmia, immunosuppressive therapy for corneal transplantation.

The drug is applied systemically or locally (subconjunctival, retrobulbar or parabulbar application)

Gastrointestinal diseases: ulcerative colitis (severe exacerbation), Crohn's disease (severe exacerbation), chronic autoimmune hepatitis, rejection reaction after liver transplantation.

Respiratory diseases: sarcoidosis (symptomatic), acute toxic bronchiolitis, chronic bronchitis and asthma (acute attack of the disease), pulmonary tuberculosis accompanied by severe general weakness (in combination with appropriate anti-tuberculosis therapy), berylliosis (granulomatous inflammation), radiation or aspiration pneumonitis.

Hematological diseases: congenital or acquired chronic pure aplastic anemia, autoimmune hemolytic anemia, secondary thrombocytopenia in adults, erythroblastopenia, acute lymphoblastic leukemia (induction therapy), idiopathic thrombocytopenic purpura (intravenous use only;

Kidney diseases: immunosuppressive therapy for kidney transplantation, induction of diuresis or reduction of proteinuria in idiopathic nephrotic syndrome (without uremia) and renal disorders in systemic lupus erythematosus.

Malignant diseases: palliative treatment of leukemia and lymphoma in adults, acute leukemia in children, hypercalcemia in patients suffering from malignant diseases.

Brain edema: cerebral edema caused by primary or metastatic brain tumors, neurosurgery, or traumatic brain injury.

Shock: shock not responding to classical therapy, shock in patients with adrenal insufficiency, anaphylactic shock (intravenously after the use of adrenaline), before surgery to prevent shock in cases of adrenal insufficiency or suspected adrenal insufficiency.

Other indications: tuberculous meningitis with subarachnoid block (in combination with appropriate anti-tuberculosis therapy), trichinosis with neurological symptoms and myocardial damage, cystic tumor of the aponeurosis or tendon (ganglion).

Indications for intra-articular injection of dexamethasone or injection into soft tissues: rheumatoid arthritis (severe inflammation of a single joint), ankylosing spondylitis (if the inflamed joints do not respond to conventional therapy), psoriatic arthritis (oligoarticular injury or tenosynovitis), monoarthritis (after pumping out fluid from the joint), osteoarthritis of the joints (only in the case of synovitis and exudate) , extra-articular rheumatism (epicondylitis, tenosynovitis, bursitis).

Local application (introduction into the wound): keloids, hypertrophic, inflamed wounds with infiltration in lichen, psoriasis, granuloma annulare, sclerosing folliculitis, discoid lupus erythematosus and cutaneous sarcoidosis, localized alopecia.

Dosage regimen

The dose is set individually depending on the disease, the expected duration of treatment, corticoid tolerance and the body's response. The injection solution can be prescribed intravenously (in the form of injections or infusions with glucose or saline), intramuscularly or locally (into a joint, into a wound, into soft tissues).

Parenteral use. Dexamethasone is used parenterally in emergency cases, in cases where oral therapy is not possible and for conditions indicated in the indications. The injection solution is prescribed intravenously or intramuscularly, or in the form of intravenous infusion (with glucose or saline solution).

Recommended average initial daily doses for IV or IM administration are 0.5 mg–0.9 mg or more as needed. The dexamethasone dosage is initially administered until clinical response is achieved, then the dosage is gradually reduced to the lowest level at which the dose remains clinically effective. If treatment with high doses continues for more than a few days, the dose should be reduced over several consecutive days or even over a longer period of time.

Local application. The recommended single dose of dexamethasone for intra-articular administration is 0.4 mg-4 mg. The dosage depends on the size of the affected joint. The usual dosage of dexamethasone for large joints is 2 mg-4 mg and 0.8 mg-1 mg for small joints. Intra-articular administration can be repeated after 3-4 months. The usual dosage of dexamethasone for administration into the bursa is 2 mg-3 mg, into the tendon sheath - 0.4 mg-1 mg and for the tendons - 1 mg-2 mg.

For injection into the wound, the same dosage of dexamethasone is used as for intra-articular injection. Dexamethasone can be administered into no more than two wounds at a time. Recommended doses for infiltration into soft tissues (periarticular) are 2-6 mg of dexamethasone.

Dosage for children. The recommended dose for intramuscular administration during replacement therapy is 0.02 mg/kg body weight or 0.67 mg/m2 body surface, divided into three doses, every third day, or 0.008 mg–0.01 mg/kg body weight, or 0.2 mg - 0.3 mg/m2 body surface daily.

Side effects

Like all drugs, Dexamethasone can cause side effects, although these may not occur in every patient taking the drug.

Side effects that may occur during treatment with dexamethasone phosphate are classified into groups depending on the frequency of occurrence:

• very common (≥1/10), frequent (≥1/100 to< 1/10), нечастые (≥ 1/1000 до < 1/100), редкие (≥ 1/10000 до < 1/1000), очень редкие (<1/10000), неизвестные (не могут быть оценены по доступным данным).

Side effects associated with short-term dexamethasone treatment include:

Side effects associated with long-term dexamethasone treatment include:

The following side effects associated with dexamethasone may also occur:

Frequent:	adrenal insufficiency and atrophy (weakened response to stress), Cushing's syndrome, irregular menstruation, excessive hair growth (hirsutism), transition from latent to clinical diabetes, sodium and water retention, increased potassium loss, muscle weakness, steroid myopathy ( muscle weakness due to muscle catabolism), slow wound healing, stretch marks, pinpoint or large skin hemorrhages, increased sweating, acne, suppressed response to skin tests.
Uncommon:	Swelling of the brain due to very high blood pressure (hypertensive encephalopathy), papilledema, increased intracranial pressure (benign intracranial hypertension), dizziness, headache, personality and behavior changes, insomnia, irritability, abnormal increase in muscle activity (hyperkinesia ), depression, nausea, hiccups, stomach and duodenal ulcers, increased intraocular pressure.
Rare:	Blockage of blood vessels by a clot, changes in the blood picture, rash, spasm of the bronchial muscles (bronchospasm), hypersensitivity reactions, psychosis, impotence.
Very rare:	Heart rhythm disturbances, heart failure, rupture of the heart muscle in patients after a recent heart attack (myocardial infarction), seizures, hypokalemic alkalosis (renal response to high potassium deficiency or loss), negative nitrogen balance due to protein breakdown, inflammation of the esophagus (esophagitis), perforation of a gastrointestinal ulcer and gastrointestinal bleeding (hematemesis, melena), perforation of the gallbladder, intestinal perforation in patients with chronic inflammatory bowel disease, swelling of the face, lips, throat and/or tongue that leads to difficulty breathing or swallowing (angioedema), allergic dermatitis, vertebral compression fracture, tendon ruptures (especially with concomitant use of quinolones), articular cartilage damage and necrosis bones (associated with frequent intra-articular injections), urticaria, protrusion of the eyeballs (exophthalmos), edema, hyper- or hypopigmentation skin, atrophy of the skin or subcutaneous tissue, sterile local inflammation (abscess), redness of the skin.

Contraindications for use

Hypersensitivity to the active substance or other ingredients of the drug.

Acute viral, bacterial and systemic fungal infections (without appropriate treatment). Cushing's syndrome.

Vaccination using live vaccine.

Breastfeeding period (except in emergency cases).

IM use is contraindicated in patients with severe hemostatic disorders.

special instructions

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.

Overdose

Symptoms. Case reports of acute overdose or death due to acute overdose are rare. Overdose can, usually after only a few weeks of use, lead to most of the side effects mentioned, especially Cushing's syndrome.

Treatment. There is no known specific antidote. Treatment is supportive and symptomatic. Hemodialysis is not effective in accelerating the elimination of dexamethasone from the body.

Drug interactions

The simultaneous use of dexamethasone and nonsteroidal anti-inflammatory drugs increases the risk of gastrointestinal bleeding and ulcers. The effect of dexamethasone is reduced by the simultaneous administration of drugs that activate the CYP3A4 enzyme (for example, phenytoin, phenobarbitone, carbamazepine, primidone, rifabutin, rifampicin) or increase the clearance of glucocorticoids (ephedrine and aminoglutethimide); therefore, in these cases, an increase in the dose of dexamethasone is necessary.

Dexamethasone reduces the therapeutic effect of antidiabetic drugs, antihypertensive drugs, praziquantel and natriuretics (the dosage of these drugs should be increased), but potentiates the activity of heparin, albendazole and kaliuretics (if necessary, the dosage of these drugs should be decreased). Dexamethasone may alter the effect of coumarin anticoagulants; therefore, more frequent monitoring of prothrombin time is recommended during concurrent use.

Concomitant use of high doses of glucocorticoids and betag receptor agonists increases the risk of hypokalemia. Patients with hypokalemia have increased arrhythmogenicity and toxicity of cardiac glycosides.

Antacids reduce the absorption of dexamethasone in the stomach. The effect of combined use of dexamethasone with food and alcohol has not been studied; however, concomitant use with medications and foods high in sodium is not recommended. Smoking does not affect the pharmacokinetics of dexamethasone. Glucocorticoids accelerate the renal clearance of salicylates, so it is sometimes difficult to achieve therapeutic serum concentrations of salicylates. Caution should be exercised in patients who have had their dexamethasone dose tapered as increased serum salicylate concentrations and salicylate toxicity may occur.

When taken together with oral contraceptives, the half-life of glucocorticoids may increase, which enhances their biological effect and increases the incidence of side effects.

The combined use of ritodrine and dexamethasone during childbirth is contraindicated, as this may lead to maternal death due to pulmonary edema. Concomitant use of dexamethasone and thalidomide may cause toxicodermal necrolysis.

Interactions with possible beneficial therapeutic effects. Concomitant use of dexamethasone and metoclopromide, diphenhydramine, prochlorperazine, or 5-HT 3 receptor antagonists (serotonin or 5-hydroxytryptamine type 3 receptors, such as ondansetron or granisetron) is effective for the prevention of nausea and vomiting caused by chemotherapy (cisplatin, cyclophosphamide, methotrexate, fluorouracil ).

Dexamethasone refers to synthetic drugs that are analogues of hormones of the adrenal cortex - glucocorticosteroids. The effect of the drug is similar to another hormonal drug -. Dexamethasone is obtained by fluoridation and methylation of Prednisolone.

So, let's talk about dexamethasone (in ampoules for injections, tablets, drops, etc.), its instructions for use, price, reviews and analogues.

Features of the drug

Composition of Dexamethasone

The main substance of the drug Dexamethasone is dexamethasone sodium phosphate, the amount of which is 4 mg per 1 ml of solution. Dark glass ampoules contain 2 ml of solution, packed in cardboard boxes of 5 or 10 pieces (plastic boxes of 5 pieces).

Excipients of the injection solution are methyl and propyl derivatives of paraben, distilled water for injection, sodium salts of edetate and metabisulfite, sodium hydroxide.

Dexamethasone release forms

Dexamethasone is registered in the following dosage forms:

1. Ampoules with injection solution for intramuscular and intravenous infusion, 2 ml each.
2. Dexamethasone tablets 0.5 mg.
3. In ophthalmology – Oftan – 0.1% solution (eye drops).
4. Dexamethasone eye drops with an active substance concentration of 0.1%.

pharmachologic effect

Dexamethasone is a powerful immunosuppressant with anti-inflammatory and antiallergic effects. In the presence of the active substance, the receptor sensitivity of β-adrenergic receptors to adrenaline and noradrenaline produced by the adrenal medulla increases.

• The drug activates interaction with cell membrane receptors, leading to protein synthesis and enhancing enzymatic activity. The largest number of Dexamethasone-dependent β-adrenergic receptors is observed in liver tissue.
• Protein metabolism. In muscle tissue, the breakdown of proteins increases against the background of a decrease in their synthesis. In the liver and kidneys, the ratio of albumins and globulins shifts towards the formation of albumins. Increased albumin synthesis and inhibition of globulin formation are also found in blood plasma.
• Lipid metabolism. Stimulates the synthesis of lipids from glycerol and higher fatty acids, promotes the development of hyperlipidemia. There is a redistribution of fat mass with its displacement in the body from the lower parts of the body (hips, buttocks, pelvis) to the upper parts (face, chest and abdomen).
• Metabolism of carbohydrates. Stimulates the active absorption of glucose in the intestinal villi and gastric mucosa, removes glycogen from the liver and muscles into the blood, causing hyperglycemia. Activates the enzymatic activity of glucose-6-phosphatase, aminotransferases and phosphoenolpyruvate carboxylase.
• Metabolism of water and mineral elements. Promotes active retention of water and sodium ions in the body, enhancing renal excretion of potassium and calcium salts. Calcium ions are less absorbed in the digestive system, and the process of mineralization of bone plates begins.
• Relieves inflammatory processes by reducing the synthesis of eosinophils and mast cells that produce inflammatory mediators. Stimulates the synthesis of arachidonic acid, interleukin 1, prostaglandins. Increases the resistance of cell membranes to chemical damage.
• The antiallergic and immunosuppressive effect of Dexamethasone is to reduce the differentiation of T-lymphocytes into suppressors, helpers and killers, reduce the reactions of interaction between T and B lymphocytes, inhibit the activity of interleukin 2 and γ-interferon, and reduce the secretion of antibodies. There is an involution of lymphoid tissue, a decrease in the synthesis of mast cells and inhibition of the secretion of allergy mediators, histamine, etc. by basophils. The result of the influence of Dexamethasone is the transformation of the immune response.

There is a decrease in the production and release of adrenocorticotropic hormone by the pituitary gland and glucocorticoids by the adrenal cortex.

The following video talks in some detail about the action of Dexamethasone:

Pharmacodynamics

One ampoule of Dexamethasone causes inhibition of the hypothalamic-pituitary-glucocortical system for 3 days. In an equivalent ratio, 0.5 mg of Dexamethasone corresponds to the effect of 3.5 mg of Prednisolone, 15 mg of Hydrocortisone or 17.5 mg of Cortisone.

Pharmacokinetics

In the blood plasma, Dexamethasone binds to the transport protein transcortin. They are not blocked by the blood-brain and blood-placental barriers. The breakdown of the drug is carried out by the liver into a complex compound of glucuronic and sulfuric acids.

The half-life of the hormonal drug is 5 hours. Excretion of the inactive metabolite occurs through the mammary glands (during feeding) and the excretory system.

Now let's find out why dexamethasone is prescribed.

Indications

Intramuscular injection of a hormonal drug is performed in conditions where oral administration or hormone replacement therapy is impossible due to an acute shortage of glucocorticosteroids. This happens in the following cases:

• hormonal abnormalities due to deficiency of the adrenal cortex, inflammation in the thyroid gland - subacute thyroiditis;
• shock therapy when antispasmodics and other drugs that relieve symptoms of shock are not effective;
• neurological operations, brain injuries, other types of brain damage with symptoms of swelling;
• attacks of bronchial asthma and acute obstructive bronchitis;
• severe allergy with the threat of anaphylactic shock;
• acute course of dermatoses;
• rheumatism of various organs;
• pathologies of connective tissue development;
• agranulocytosis and other hematological pathologies;
• , in children - with malignant systemic;
• severe congestion in the lungs and infectious processes;
• local use during lupus erythematosus, etc.;
• in the practice of ophthalmologists in the treatment of inflammation of many structures of the eyeball and mucous membranes.

Pregnant women may receive Dexamethasone if:

• threats of premature birth;
• a rare hereditary disease of the fetus - underdevelopment of the adrenal cortex;
• anaphylactic shock and other conditions of each person falling into life-threatening conditions.

Instructions for use

The drug is administered by intramuscular or intravenous infusion. In the case of drip administration, Dexamethasone is mixed in a dextrose solution or isotonic sodium chloride solution.

Local application possible. The maximum daily dose of the hormonal drug is 20 mg per day. The daily dose is divided into 3-4 times. During the initial period of treatment, the dosage of dexamethasone is increased until the desired effect is achieved, and then the dose is reduced. The possibility of long-term use is limited due to the threat of atrophy of the adrenal cortex.

For children, the amount of the drug is calculated based on the child’s body weight. Per 1 kg of child’s body weight per day, no more than 0.00233 mg is allowed to be administered intramuscularly.

The video below provides instructions for using Dexamethasone in the form of eye drops:

Contraindications

The drug is contraindicated in case of individual intolerance and severe liver failure. With extreme caution and the constant supervision of the attending physician, dexamethasone is administered to women during pregnancy, children and adults for:

• pathologies of the digestive system of an ulcerative nature;
• infectious diseases;
• HIV – infected and suffering from AIDS;
• chronic liver and kidney diseases;
• cardiovascular pathologies, especially during the acute period;
• disorders of hormonal secretion;
• the period before and after vaccination of lymphadenitis and brucellosis;
• osteoporosis, glaucoma.

Side effects

Usually there are no side effects from dexamethasone from the somatic systems of the body.

• In some cases, exacerbations of diabetes mellitus and delayed sexual development were noted.
• From the gastrointestinal tract, disorders and perforation of the mucous membranes of the digestive organs are sometimes observed.
• A local allergic reaction, slow wound healing, excessive sweating, increased calcium excretion, and increased fatigue cannot be ruled out.

special instructions

High doses of Dexamethasone are prescribed with careful supervision by the attending physician. After discontinuation of the drug, be sure to monitor the patient’s well-being in a clinical setting.

While using the drug, you should adhere to a diet and ensure that your diet is enriched with calcium, potassium and proteins.

Dexamethasone is a drug belonging to the group of glucocorticosteroids and is a hormonal agent.

It is widely used in medicine in various fields. It is produced in the form of a solution, which is used for injection intravenously, intramuscularly and for instillation into the conjunctiva of the eyes.

On this page you will find all the information about Dexamethasone: complete instructions for use for this drug, average prices in pharmacies, complete and incomplete analogues of the drug, as well as reviews of people who have already used Dexamethasone injections. Would you like to leave your opinion? Please write in the comments.

Clinical and pharmacological group

GCS for injection.

Conditions for dispensing from pharmacies

Dispensed with a doctor's prescription.

Prices

How much does Dexamethasone cost? The average price in pharmacies is 100 rubles.

Release form and composition

The drug solution, which is sold in pharmacies in ampoules, contains dexamethasone sodium phosphate. This active substance takes 4 or 8 mg.

The auxiliary components are glycerin, disodium phosphate dihydrate, disodium edetate and purified water to obtain a solution of the desired concentration. Dexamethasone solution for internal administration appears as a clear, colorless or yellowish liquid.

Pharmacological effect

Dexamethasone is a homologue of hydrocortisone, a hormone produced by the adrenal cortex.

It interacts with glucocorticoid receptors, regulates sodium and potassium metabolism, water balance and glucose homeostasis. Stimulates the production of enzyme proteins in the liver, affects the synthesis of mediators of inflammation and allergies, and inhibits their formation. As a result, the product gives an anti-inflammatory, anti-allergic, immunosuppressive, and anti-shock effect.

When administered intramuscularly, the therapeutic effect is observed after 8 hours, after intravenous infusion, faster. The effect lasts from 3 days to 3 weeks when administered locally, 17 - 28 days after administration intravenously. Dexamethasone has a strong anti-inflammatory and antiallergic effect. It is 35 times more effective than cortisone.

Why is Dexamethasone prescribed?

1. For gastrointestinal diseases: and ulcerative colitis.
2. For systemic connective tissue diseases: acute rheumatic carditis; .
3. For endocrine disorders: insufficiency of the adrenal cortex and their congenital hyperplasia; subacute form of inflammation of the thyroid gland.
4. For rheumatic diseases: bursitis; ; psoriatic and gouty arthritis; osteoarthritis; synovitis; nonspecific tenosynovitis; ankylosing spondylitis; epicondylitis accompanying osteoarthritis.
5. For allergic diseases: contact and atopic; status asthmaticus; serum sickness; allergies to food and certain medications; angioedema; (seasonal or chronic); ; associated with blood transfusion.
6. For skin diseases: severe erythema multiforme; pemphigus; exfoliative, bullous herpetiform and severe seborrheic dermatitis; fungoid mycosis; .
7. For eye diseases: optic neuritis; symptomatic ophthalmia; allergic corneal ulcers; keratitis; iridocyclitis; iritis; uveitis (anterior and posterior); allergic forms.
8. For respiratory diseases: Loeffler's syndrome; ; sarcoidosis 2nd-3rd degree; aspiration pneumonia; berylliosis.
9. For kidney diseases: impaired renal function associated with systemic wolf's lichen erythematosus; idiopathic nephrotic syndrome.
10. For malignant diseases: leukemia (acute) in children; lymphoma and leukemia in adults.
11. In case of shock: shock that cannot be treated with classical methods; anaphylactic shock; shock in patients suffering from insufficiency of the adrenal cortex.
12. For hematological diseases: idiopathic thrombocytopenic purpura; erythroblastopenia; congenital hypoplastic anemia; autoimmune hemolytic anemia; thrombocytopenia secondary.
13. For other indications: myocardial trichinosis; trichinosis with neurological signs; tuberculous meningitis.

Contraindications

The use of Dexamethasone is contraindicated in patients with hypersensitivity to the components of the drug.

The use of Dexamethasone by pregnant and lactating women, as well as children, should only be prescribed by a doctor after taking into account all possible risks.

Use during pregnancy and lactation

Dexamethasone in the form of tablets and drops is prohibited for use during pregnancy and lactation. If during breastfeeding there is a need for treatment with Dexamethasone, the child is transferred to artificial formula.

Dexamethasone injections during pregnancy are given only for health reasons. For example, the drug may be prescribed when the immune system begins to perceive the embryo as a foreign body. Dexamethasone suppresses immune activity, which eliminates the threat of miscarriage and maintains pregnancy.

Instructions for use

The instructions for use indicate that the dosage regimen is individual and depends on the indications, the patient’s condition and his response to therapy.

1. The drug is administered intravenously in a slow stream or drip (for acute and emergency conditions); i/m; local (into the pathological formation) administration is also possible. To prepare a solution for intravenous drip infusion, you should use an isotonic sodium chloride solution or a 5% dextrose solution.
2. In the acute period for various diseases and at the beginning of therapy, Dexamethasone is used in higher doses. During the day, you can administer from 4 to 20 mg of Dexamethasone 3-4 times.

Doses of the drug for children (i.m.):

• The dose of the drug during replacement therapy (for adrenal insufficiency) is 0.0233 mg/kg body weight or 0.67 mg/m2 body surface area, divided into 3 doses, every 3rd day or 0.00776 – 0.01165 mg/kg body weight or 0.233 – 0.335 mg/m2 body surface area daily. For other indications, the recommended dose is from 0.02776 to 0.16665 mg/kg body weight or 0.833 to 5 mg/m2 body surface area every 12-24 hours.
• When the effect is achieved, the dose is reduced to maintenance or until treatment is stopped. The duration of parenteral use is usually 3-4 days, then they switch to maintenance therapy with dexamethasone tablets.

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

Side effects

During treatment with Dexamethasone in the form of injections, patients may experience the development of the following side effects:

1. From the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, skin thinning, hyper- or hypopigmentation, steroid acne, stretch marks, tendency to develop pyoderma and candidiasis;
2. From the senses: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, nasal turbinates, scalp possible deposition of drug crystals in the blood vessels of the eye);
3. Metabolism: increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating. Caused by mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypsarnatremia, hypokalemia syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue);
4. From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, stretch marks), delayed sexual development in children;
5. Cardiovascular systems: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of heart failure, changes in the electrocardiogram 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;
6. From the musculoskeletal system: slower growth and ossification processes in children (premature closure of the 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). Dexamethasone instructions for use;
7. From the 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.
8. From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the wall of the gastrointestinal tract, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases, increased activity of liver transaminases and alkaline phosphatase;

Overdose

If you use Dexamethasone too actively for several weeks, an overdose is possible, which is manifested by the symptoms listed among the side effects.

Treatment is carried out according to the manifested factors, and consists of reducing the dose or temporarily discontinuing the drug. In case of overdose, there is no special antidote; hemodialysis is not effective.

special instructions

1. For patients with liver abnormalities, Dexamethasone is prescribed with particular caution.
2. In order to reduce the risk of side effects, the patient should follow a diet high in potassium. Food should be rich in proteins, carbohydrate and salt intake should be slightly reduced.
3. During treatment with Dexamethasone, patients should constantly monitor blood pressure, the state of the visual organs, water and electrolyte balance and the clinical picture of the blood.
4. Treatment with the drug should not be stopped abruptly, as in this case the risk of developing withdrawal syndrome increases, a condition that is accompanied by an increase in the primary symptoms of the disease and suppression of adrenal function.
5. Patients with diabetes mellitus should constantly monitor blood glucose levels and, if necessary, adjust the daily dose of hypoglycemic drugs.
6. When using the drug in pediatric practice, you should carefully monitor the dynamics of the child's growth, since long-term use of the drug in large doses can lead to inhibition of the patient's growth.

Drug interactions

Instructions for use of Dexamethasone highlight the following drug interactions:

1. The ability to enhance the effect of antibiotics;
2. Phenobarbital, ephedrine reduce the effectiveness of the drug;
3. When taken with other glucocorticosteroids, there is an increased risk of hypokalemia;
4. When used with oral contraceptives, the half-life of Dexamethasone increases;
5. Ritodrine should not be used concomitantly with the drug in question due to the risk of death;
6. Dexamethasone reduces the effectiveness of hypoglycemic, anticoagulant, and antihypertensive medications;
7. To prevent nausea and vomiting after chemotherapy, it is recommended to use Dexamtheazone and Metoclopramide, Diphenhydramine, Prochlorperazine, Ondansetron, Granisetron simultaneously.