Dexamethasone: instructions for use in adults and children. Instructions for use dexamethasone (dexamethason) solution Dexamethasone injections contraindications

DEXAMETHASONE instructions for use (injections in ampoules, eye drops, tablets). DEXAMETHASONE is a powerful synthetic glucocorticoid (containing adrenal cortex hormones and their synthetic analogues) drug designed to regulate protein, carbohydrate and mineral metabolism.

Dexamethasone instructions for use, reviews, analogs and forms of release (tablets 0.5 mg, injections in ampoules (solution for injection), eye drops oftan) drugs for the treatment of inflammation in adults, children and pregnancy.

Compound

• Active substance - dexamethasone sodium phosphate (in terms of dexamethasone phosphate) - 4.0 mg / 8.0 mg;
• Excipients - glycerin, disodium phosphate dihydrate, disodium edetate, water for injection.

Release forms

1. Tablets 0.5 mg;
2. Solution in ampoules for intravenous and intramuscular administration (injections for injections) 4 mg/ml;
3. Eye drops Oftan 0.1%;
4. Eye suspension 0.1%

DEXAMETHASONE instructions for use of the drug

Oral administration of Dexamethasone in the form of tablets involves the appointment of 10-15 mg of the drug per day at the initial stage of treatment, followed by a decrease in the daily dose to 2-4.5 mg with maintenance therapy. The instruction recommends dividing the daily dose of the drug Dexamethasone into 2-3 doses (after or during meals).

Maintenance small doses should be taken once a day, preferably in the morning. Dexamethasone in ampoules is intended for intravenous (drip or jet), intramuscular, periarticular and intraarticular administration. The recommended daily dose of Dexamethasone for these routes of administration is 4-20 mg. Dexamethasone in ampoules is usually used 3-4 times a day for 3-4 days, followed by switching to tablets.

Dexamethasone drops are used in ophthalmology: in acute conditions, 1-2 drops of the drug are instilled into conjunctival sac every 1-2 hours, with improvement - every 4-6 hours. Chronic processes involve the use of Dexamethasone drops 2 times a day.

The duration of treatment depends on the clinical course of the disease, so Dexamethasone drops can be used from several days to four weeks.

Indications for the use of Dexamethasone

Diseases requiring the introduction of fast-acting corticosteroids, as well as cases when oral intake the drug is not possible:

• Shock (burn, traumatic, surgical, toxic) - with the ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;
• Severe allergic reactions, anaphylactic shock;
• Blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;
• Endocrine diseases: acute insufficiency adrenal cortex, primary or secondary insufficiency, congenital hyperplasia, subacute thyroiditis;
• Local application (in the area of ​​pathological formation): keloids, discoid lupus erythematosus, granuloma annulare;
• Rheumatic diseases - Dexamethasone instructions for use;
• In ophthalmic practice (subconjunctival, retrobulbar or parabulbar administration): allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after transplantation cornea;
• Acute severe dermatoses;
• Malignant diseases: palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; hypercalcemia in patients suffering from malignant tumors, when oral treatment is not possible;
• heavy infectious diseases(in combination with antibiotics);
• Cerebral edema (with a tumor, traumatic brain injury, neurosurgical intervention, hemorrhage, encephalitis, meningitis, radiation injury);
• Systemic connective tissue diseases;
• Asthmatic status; severe bronchospasm (exacerbation of bronchial asthma, chronic obstructive bronchitis).

What are Dexamethasone tablets used for?

• With hypothyroidism (a condition with a persistent lack of thyroid hormones);
• At rheumatoid arthritis in the acute phase;
• With congenital adrenogenital syndrome (hyperfunction of the adrenal cortex and an increased content of androgens in the body);
• With Addison-Birmer disease (loss of the ability of the adrenal glands to produce hormones in sufficient quantities);
• With pemphigus (a skin disease that manifests itself in the form of blisters on the hands, genitals, mouth, etc.);
• In acute and subacute thyroiditis (inflammation of the thyroid gland);
• With acute erythroderma (reddening of the skin);
• With progressive ophthalmopathy (an increase in the volume of eye tissues) associated with thyrotoxicosis (intoxication with thyroid hormones);
• With acute eczema;
• In diseases of the connective tissue;
• At malignant tumors(symptomatic therapy);
• With autoimmune hemolytic anemia;
• With cerebral edema;
• With agranulocytosis (decrease in the level of neutrophils in the blood);
• With bronchial asthma;
• With serum sickness (immune reaction to foreign serum proteins).

What are Dexamethasone drops prescribed for?

• With scleritis (inflammation of the deep layers of the sclera of the eye);
• With keratitis (inflammation of the cornea of ​​\u200b\u200bthe eye);
• With sympathetic ophthalmia (inflammatory lesions of the eye);
• With non-purulent and allergic conjunctivitis (inflammation of the mucous membrane of the eye);
• With iritis (inflammation of the iris of the eye);
• With blepharitis (inflammation of the edges of the eyelids);
• In inflammatory processes after eye injuries or operations;
• With iridocyclitis (inflammation of the iris and ciliary body);
• With episcleritis (inflammation of the connective tissue between the conjunctiva and the sclera);
• With keratoconjunctivitis (simultaneous inflammation of the conjunctiva and cornea of ​​the eye) without damage to the epithelium.

Why are injections prescribed in ampoules Dexamethasone

• With acute hemolytic anemia;
• With acute insufficiency of the adrenal cortex;
• With asthmatic status;
• Acute lymphoblastic leukemia (malignant disease that affects the bone marrow, spleen, The lymph nodes, thymus and other organs). Dexamethasone instructions for use;
• With cerebral edema;
• With severe infectious diseases;
• In shock various genesis;
• With diseases of the joints;
• With thrombocytopenia;
• With severe allergic reactions;
• With acute croup (inflammation of the larynx and upper respiratory tract);
• with agranulocytosis.

Contraindications

For short-term use for health reasons, the only contraindication is hypersensitivity to dexamethasone or the components of the drug.

In children during the period of growth, corticosteroids should be used only according to absolute indications and under the most careful supervision of the attending physician.

Carefully the drug should be prescribed for the following diseases and conditions:

The therapeutic and toxic effects of Dexamethasone are reduced by barbiturates, phenytoin, rifabutin, carbamazepine, ephedrine and aminoglutethimide, rifampicin (accelerate metabolism); somatotropin; antacids (reduce absorption), enhance - estrogen-containing oral contraceptives. Simultaneous use with cyclosporine increases the risk of seizures in children.

The risk of arrhythmias and hypokalemia is increased by cardiac glycosides and diuretics, the likelihood of edema and arterial hypertension - sodium-containing drugs and nutritional supplements, severe hypokalemia, heart failure and osteoporosis - amphotericin B and carbonic anhydrase inhibitors; the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract - non-steroidal anti-inflammatory drugs. Dexamethasone instructions for use.

When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of virus activation and infection.

Simultaneous use with thiazide diuretics, furosemide, ethacrynic acid, carbonic anhydrase inhibitors, amphotericin B can lead to severe hypokalemia, which can increase the toxic effects of cardiac glycosides and non-depolarizing muscle relaxants.

Weakens the hypoglycemic activity of insulin and oral antidiabetic agents; anticoagulant - coumarins; diuretic - diuretic diuretics; immunotropic - vaccination (suppresses antibody production).

It worsens the tolerance of cardiac glycosides (causes a potassium deficiency), reduces the concentration of salicylates and praziquantel in the blood. May increase the concentration of glucose in the blood, which requires dose adjustment of hypoglycemic drugs, sulfonylurea derivatives, asparaginase.

GCS increase the clearance of salicylates, so after the abolition of Dexamethasone, it is necessary to reduce the dose of salicylates. When used simultaneously with indomethacin, the Dexamethasone suppression test may give false negative results.

Dosage and administration

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

In order to prepare for intravenous drip infusion, an isotonic sodium chloride solution or a 5% dextrose solution should be used. The introduction of high doses of dexamethasone can be continued only until the patient's condition stabilizes, which usually does not exceed 48 to 72 hours.

Adults with acute and emergency conditions administered in / in slowly, stream or drip, or / m at a dose of 4-20 mg 3-4 times a day. The maximum single dose is 80 mg. Maintenance dose - 0.2-9 mg per day. The course of treatment is 3-4 days, then they switch to oral administration of Dexamethasone. Children - in / m at a dose of 0.02776-0.16665 mg / kg every 12-24 hours.

1. Soft tissues: 2 to 6 mg;
2. Large joints (eg. knee-joint): 2 to 4 mg;
3. Articular bags: 2 to 3 mg;
4. Small joints (eg, interphalangeal, temporal joint): 0.8 to 1 mg;
5. Nerve ganglia: 1 to 2 mg;
6. Tendons: 0.4 to 1 mg.

The drug is prescribed repeatedly with an interval of 3 days to 3 weeks as needed; the maximum dose for adults is 80 mg per day. In shock, adults - in / in 20 mg once, then 3 mg / kg for 24 hours as a continuous infusion or in / in a single dose of 2-6 mg / kg, or in / in 40 mg every 2- 6 o'clock.

With cerebral edema (adults) - 10 mg IV, then 4 mg every 6 hours / m until symptoms disappear; the dose is reduced after 2-4 days and gradually - within 5-7 days - stop treatment. In case of insufficiency of the adrenal cortex (children) in / m at 0.0233 mg / kg (0.67 / mg / m2) per day in 3 injections every third 24 hours, or daily at 0.00776-0.01165 mg / kg ( 0.233-0.335 mg/m2) per day.

In an acute allergic reaction or exacerbation of a chronic allergic disease, dexamethasone should be prescribed according to the following schedule, taking into account the combination of parenteral and oral administration: dexamethasone instructions for use injection solution 4 mg / ml: 1 day, 1 or 2 ml (4 or 8 mg ) intramuscularly; dexamethasone tablets 0.75 mg: the second and third days, 4 pieces in 2 doses per day, the fourth - 2 pieces in 2 doses, the fifth and sixth days - 1 pc. daily, on the seventh - without treatment, day 8 - observation.

Side effects

Dexamethasone is usually well tolerated. It has low mineralocorticoid activity, i.e. its effect on water-electrolyte metabolism is small. As a rule, low and medium doses of Dexamethasone do not cause sodium and water retention in the body, increased potassium excretion.

The following side effects have been described:

1. From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral infections eye, trophic changes in the cornea, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, turbinates, scalp, crystals of the drug may be deposited in the vessels of the eye);
2. From the side skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, a tendency to develop pyoderma and candidiasis;
3. On the part of the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes, suppression of adrenal function, Itsenko-Cushing's syndrome (moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delayed sexual development in children;
4. From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), excessive sweating. Due to mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypnatremia, hypokalemia syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue);
5. On the part of the musculoskeletal system: growth retardation and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely, pathological bone fractures, aseptic necrosis of the head of the humerus and femur), rupture of muscle tendons, steroid myopathy, decreased muscle mass(atrophy). Dexamethasone instructions for use;
6. From the side of cardio-vascular system: 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, hypercoagulability, thrombosis. In patients with acute and subacute infarction myocardium - the spread of the focus of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle;
7. From the side digestive system: nausea, vomiting, pancreatitis, steroid gastric ulcer and duodenum, erosive esophagitis, gastrointestinal bleeding and wall perforation gastrointestinal tract, increase or decrease in appetite, indigestion, flatulence, hiccups. V rare cases- increased activity of hepatic transaminases and alkaline phosphatase;
8. From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.

allergic reactions: skin rash, itching, anaphylactic shock, local allergic reactions.

Local for parenteral administration: burning, numbness, pain, tingling and infection at the injection site, rarely - necrosis of surrounding tissues, scarring; atrophy of the skin and subcutaneous tissue with intramuscular injection (it is especially dangerous to inject into the deltoid muscle).

Other: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, "flushing" of blood to the face, "withdrawal" syndrome.

The price of the drug DEXAMETHASONE

• Dexamethasone, tablets 0.5 mg, 10 pcs. - 45 rubles;
• Dexamethasone, eye drops 0.1%, 5 ml - 34 rubles;
• Dexamethasone, ampoules 4 mg, 1 ml, 25 pcs. - 202 rubles;
• Dexamethasone solution for injections 4 mg/ml 1 ml ampoules, 25 pcs. 144 rubles;
• Dexamethasone eye drops, 10 ml - 82 rubles.

special instructions

• Caution should be used in acute and subacute myocardial infarction - it is possible to spread the focus of necrosis, slow the formation of scar tissue and rupture the heart muscle;
• During treatment with Dexamethasone, vaccination should not be carried out due to a decrease in its effectiveness (immune response).
  When prescribing Dexamethasone for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics;
• Patients with latent infectious diseases of the kidneys and urinary tract Dexamethasone can cause leukocyturia, which may be of diagnostic value;
• With sudden cancellation, especially in the case of previous use of high doses, the development of a “withdrawal” syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness) is possible, as well as an exacerbation of the disease for which Dexamethasone was prescribed;
• During treatment with Dexamethasone (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure and the state of water and electrolyte balance, as well as pictures of peripheral blood and blood glucose levels;
• Children during long-term treatment Dexamethasone requires careful monitoring of the dynamics of growth and development. Children who during the treatment period were in contact with patients with measles or chicken pox, prophylactically prescribe specific immunoglobulins.
  Due to the weak mineralocorticoid effect on replacement therapy with adrenal insufficiency, Dexamethasone is used in combination with mineralocorticoids;
• Dexamethasone increases the content of metabolites of 11- and 17-hydroxyketocorticosteroids;
• In order to reduce side effects you can prescribe antacids, and you should also increase the intake of K + in the body (diet, potassium supplements). Food should be rich in proteins, vitamins, with limited content of fats, carbohydrates and salt;
• In patients with diabetes mellitus, blood glucose levels should be monitored and, if necessary, therapy should be adjusted.
  X-ray control of the osteoarticular system (images of the spine, hand) is shown;
• The effect of the drug is enhanced in patients with hypothyroidism and cirrhosis of the liver. The drug may increase existing emotional instability or psychotic disorders. When indicating a history of psychosis, Dexamethasone in high doses is prescribed under the strict supervision of a physician;
• In stressful situations during maintenance treatment (for example, surgery, trauma or infectious diseases), the dose of the drug should be adjusted due to an increase in the need for glucocorticosteroids. Patients should be closely monitored for a year after the end of long-term therapy with Dexamethasone due to possible development relative insufficiency of the adrenal cortex in stressful situations. Dexamethasone instructions for use.

Video review of the drug DEXAMETHASONE (DEXAMETHASONE)

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Dexamethasone ampoules 4 mg, 1 ml, 25 pcs. - the average price is 185 rubles.

Dexamethasone is a drug that has anti-inflammatory and immunosuppressive effects. Solution for intravenous and intramuscular injection, is a clear, colorless or light yellow liquid.

• Latin name: Dexamethasone
• ATX code: S01BA01
• Active substance: Dexamethasone (Dexamethasone)
• Manufacturer: RUE “Belmedpreparaty” (Republic of Belarus), JSC “Lekhim-Kharkov”, PJSC “Farmak”, CJSC FF “Darnitsa” (Ukraine)

Compound

Active substance:

Dexamethasone sodium phosphate (dexamethasone phosphate disodium salt) in terms of 100% substance - 4.0 mg.

Excipients:

• glycerol (distilled glycerin) - 22.5 mg;
• disodium edetate (trilon B) - 0.1 mg;
• sodium hydrogen phosphate dodecahydrate (sodium phosphate disubstituted 12-water) - 0.8 mg;
• water for injection - up to 1 ml.

pharmachologic effect

Dexamethasone is a hormonal drug with anti-allergic, anti-inflammatory, immunosuppressive, desensitizing, antitoxic, anti-shock activity.

Able to interact with specific cytoplasmic receptors:

1. forms a complex that penetrates the cell nucleus and stimulates mRNA synthesis;
2. the latter induces the formation of proteins, incl. lipocortin mediating cellular effects. Lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the biosynthesis of endoperoxides, prostaglandins, leukotrienes, which promote inflammation, allergies, and others.

Dexamethasone eye drops also have anti-allergic, anti-exudative and anti-inflammatory effects.

Pharmacodynamics and pharmacokinetics

The use of Dexamethasone makes it possible to increase the sensitivity of the proteins of the outer cell membrane (beta-adrenergic receptors) to endogenous catecholamines (mediators of intercellular interaction).

Dexamethasone regulates protein metabolism, reducing synthesis and increasing muscle tissue protein catabolism, reducing the amount of globulins in plasma, increasing albumin synthesis in the liver and kidneys. Influencing carbohydrate metabolism Dexamethasone promotes the absorption of carbohydrates from the digestive tract, increases the flow of glucose into the blood from the liver, the development of hyperglycemia, which in turn activates the production of insulin. The participation of Dexamethasone in water-electrolyte metabolism is manifested in a decrease in mineralization bone tissue, sodium and water retention in the body, a decrease in calcium absorption from the gastrointestinal tract.

The anti-inflammatory and anti-allergic properties of Dexamethasone are 35 times more active than those of cortisone.

In the blood, it binds (60-70%) to a specific protein - the carrier - transcortin. Easily passes through histohematic barriers (including through the blood-brain barrier and placental). It is excreted in a small amount from breast milk. Metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. Excreted through the kidneys.

Indications for use

The instruction recommends using Dexamethasone tablets in the following cases:

• acute and subacute thyroiditis (inflammation of the thyroid gland);
• hypothyroidism (a condition with a persistent lack of thyroid hormones);
• progressive ophthalmopathy (an increase in the volume of eye tissues) associated with thyrotoxicosis (intoxication with thyroid hormones);
• Addison-Birmer disease (loss of the ability of the adrenal glands to produce hormones in sufficient quantities);
• bronchial asthma;
• connective tissue diseases;
• rheumatoid arthritis in the acute phase;
• autoimmune hemolytic anemia;
• serum sickness (immune reaction to foreign serum proteins);
• agranulocytosis (decrease in the level of neutrophils in the blood);
• acute erythroderma (redness of the skin);
• pemphigus (skin disease that manifests itself in the form of blisters on the hands, genitals, mouth, etc.);
• acute eczema;
• malignant tumors (symptomatic therapy);
• cerebral edema;
• congenital adrenogenital syndrome (hyperfunction of the adrenal cortex and increased levels of androgens in the body).

Dexamethasone in ampoules is used for:

• shock of various origins;
• asthmatic status;
• cerebral edema;
• severe allergic reactions;
• acute hemolytic anemia;
• thrombocytopenia;
• agranulocytosis;
• acute lymphoblastic leukemia (a malignant disease affecting the bone marrow, spleen, lymph nodes, thymus and other organs);
• severe infectious diseases;
• acute croup (inflammation of the larynx and upper respiratory tract);
• acute insufficiency of the adrenal cortex; joint diseases.

Dexamethasone drops are used in ophthalmic practice for:

• non-purulent and allergic conjunctivitis (inflammation of the mucous membrane of the eye);
• keratitis (inflammation of the cornea of ​​the eye);
• keratoconjunctivitis (simultaneous inflammation of the conjunctiva and cornea of ​​the eye) without damage to the epithelium;
• iritis (inflammation of the iris);
• iridocyclitis (inflammation of the iris and ciliary body); blepharitis (inflammation of the edges of the eyelids);
• scleritis (inflammation of the deep layers of the sclera of the eye);
• episcleritis (inflammation of the connective tissue between the conjunctiva and the sclera); inflammatory processes after eye injuries or operations;
• sympathetic ophthalmia (inflammatory lesions of the eye).

Application instruction of Dexamethasone

At the initial stage of treatment, the use of Dexamethasone (orally) in the form of tablets is preferred at 10-15 mg of the drug per day, followed by a decrease in the daily dose to 2-4.5 mg with maintenance therapy.

The daily dose of Dexamethasone is recommended to be divided into 2-3 doses (during or after meals). Maintenance small doses should be taken once a day, preferably in the morning.

Dexamethasone in ampoules is intended for intravenous (drip or jet), intramuscular, periarticular and intraarticular administration. The recommended daily dose of Dexamethasone for these routes of administration is 4-20 mg. Dexamethasone in ampoules is usually used 3-4 times a day for 3-4 days, followed by switching to tablets.

Dexamethasone drops are used in ophthalmology: in acute conditions, 1-2 drops of the drug are instilled into the conjunctival sac every 1-2 hours, when the condition improves, every 4-6 hours.

Chronic processes involve the use of Dexamethasone drops 2 times a day. The duration of treatment depends on the clinical course of the disease, so Dexamethasone drops can be used from several days to four weeks.

Use during pregnancy

The use of Dexamethasone during pregnancy is possible only for health reasons, if the expected benefit of therapy for the mother outweighs the potential risk associated with treatment.
If it is necessary to carry out drug treatment during breastfeeding then breastfeeding should be discontinued.

Overdose

Excessive administration of the drug can cause an overdose, which is manifested by increased side effects, as well as hypercortisolism syndrome (Cushing's Syndrome).

Therapy is symptomatic, at the same time a dose reduction or drug withdrawal is required for a while.

Side effects

According to the instructions, Dexamethasone can cause the following reactions:

• decreased glucose tolerance, suppression of adrenal function, steroid diabetes mellitus, Itsenko-Cushing's syndrome;
• hypocalcemia, hypokalemia, hyponatremia, increased calcium excretion, weight gain, increased sweating;
• increased intracranial pressure, anxiety, depression, paranoia, dizziness, headache, convulsions;
• vomiting, nausea, steroid ulcer, pancreatitis, erosive esophagitis, hiccups, flatulence;
• bradycardia, arrhythmias, increased blood pressure;
• exophthalmos, trophic changes in the cornea, a tendency to develop eye infections, increased intraocular pressure, posterior subcapsular cataract;
• slowing down of ossification in children, rupture of tendons of muscles, osteoporosis, decrease in muscle mass, steroid myopathy; dermatological and allergic reactions.

Contraindications for use

The use of Dexamethasone is contraindicated in those patients who have a very hypersensitivity to the components of the drug.

The drug is incompatible with other drugs, since it can form insoluble compounds with them.

The solution for injection can be mixed in such cases:

1. only with 5% glucose solution;
2. NaCl solution 0.9%.

Release form

1. In ampoules of 1 ml or 2 ml in package No. 10,
2. In ampoules of 1 ml or 2 ml in blisters No. 5×1, No. 5×2.

Storage conditions and shelf life

In a place protected from light at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Shelf life - 2 years.

Dexamethasone analogs

Analogues of solution and tablets:

• Dexazon,
• Dexamethasone-Vial,
• Dexamed,
• Megadexan,
• Dexamethasone-Ferrein.

Similar preparations for eye drops:

• Dexamethasone-LANS,
• Dexapos,
• Ozurdex,
• Maxidex,
• Dexamethasone long.

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

Hormonal preparations have multidirectional action. They not only normalize the work of the endocrine system, but also stabilize the functioning of individual organs and systems. An example of such a drug is Dexamethasone (injections) - not all patients know why and how they are prescribed.

Dexamethasone (shots) - what is it prescribed for?

Dexamethasone is related to hormonal drugs. This medicine is a synthetic analogue of adrenal hormones. It is used for insufficient work of these glands and for other pathological conditions. If you turn to the instructions for the drug Dexamethasone, injections, indications for use, the following are indicated there:

• diseases of the joints, muscles (, myositis);
• cerebral edema;
• dermatosis;
• liver disease;
• pathology of the visual apparatus;
• oncological diseases;
• blood diseases.

Dexamethasone (shots) - why is it prescribed for adults?

The range of disorders for which the drug is used is wide. Dexamethasone injections intramuscularly help to quickly stop the allergic reaction, the developed cerebral edema. Doctors talk about the positive effect of treating severe infectious diseases when Dexamethasone is used along with an antibiotic. This drug has a systemic effect on the body. Telling patients about Dexamethasone, injections, for which the drug is prescribed, doctors point out the following effect of the drug:

• elimination of shock;

• removal of inflammation;
• regulation of metabolism;
• reduced allegorical reaction;
• reduction of toxic effects on the body during the infectious process.

Dexamethasone (shots) - why is it prescribed to children?

Dexamethasone, injection, is rarely prescribed for children. So, the drug can be used when vaccinated with live vaccines, if the child has a predisposition to developing allergies. As part of complex therapy, the drug is used for Itsenko-Cushing's syndrome, a disease accompanied by a malfunction of the adrenal glands. Injections for children are not prescribed in case of violation of the blood coagulation system. Among the main pathologies in which the use of Dexamethasone is indicated:

• severe skin lesions, dermatoses;
• Crohn's disease;
• hemolytic anemia;
• glomerulonephritis.

Talking about such a dosage form as Dexamethasone, injections, for which the drug is prescribed, it is necessary to note the possibility of local administration of the drug. Injections are often carried out in a neoplasm in soft tissues, a joint, and even in the eye. In rare cases, with severe and persistent hypothermia, Dexamethasone is used as part of a lytic mixture (administered together with Analgin and Diphenhydramine).

Dexamethasone (shots) - why is it prescribed for pregnant women?

When carrying a child, the drug is used with caution. It helps the body future mother fight high levels of androgens in the blood - male hormones that can provoke a miscarriage. Under the influence of Dexamethasone, there is a decrease in the synthesis of testosterone. The drug can be used throughout the entire gestation period.

In each case, experts determine individually the need for the use of the drug. When Dexamethasone is prescribed, injections, indications for the use of the drug during pregnancy are always associated with the threat of interruption of gestation. The drug is used carefully: its components penetrate the placental barrier, so they can affect the fetus.

Dexamethasone (injections) - why is it prescribed for cancer patients?

Often in the list of prescriptions for patients with oncology there is Dexamethasone, a solution for injection. It is used in the tumor-like process in the brain as a complex therapy drug. It allows you to improve the general condition of the patient: relieve swelling, reduce inflammation. The systematic use of the drug helps to normalize intracranial pressure, relieve the patient from severe, prolonged headaches. Dosage, frequency and duration of therapy are set individually, taking into account the stage of the pathological process.

Dexamethasone and Diclofenac injection together

The drug for injection Dexamethasone in some cases can be used together with another drug - Diclofenac. This medication has a pronounced anti-inflammatory and analgesic effect and is actively used in inflammatory processes of various localization. To enhance its effect, doctors may prescribe Diclofenac and Dexamethasone at the same time. This combination of drugs is recommended for use in:

• treatment of osteochondrosis, rheumatoid arthritis;
• inflammation of the joints, soft tissues with severe pain;
• neuralgia, neuritis;
• painful sensations against the background of sciatica, spondyloarthritis.

The decision on the appropriateness of such therapy is made by the doctor. Dosage, frequency of administration are set individually, based on the general well-being of the patient, clinical picture diseases. More often, doctors use the following proportion: 75 mg of Diclofenac and 4 mg of Dexamethasone.

How to dilute Dexamethasone for injection?

For the correct administration of the drug Dexamethasone (injections), the instruction states the need for preliminary dilution of the drug. As a solvent, physiological saline is often used - 0.9% sodium chloride. It is also allowed to dilute the drug with glucose. However, in this case it is necessary to take into account metabolic processes in organism. For certain diseases, Dexamethasone injections (for which it is indicated above) are not diluted with glucose (diabetes mellitus, for example).

Dexamethasone Injections - Dosage

Having found out what effect the injection of Dexamethasone has on the body, for which the drug is prescribed, it is necessary to indicate the features of the dosage of the drug. It is worth noting that all appointments are carried out exclusively by a doctor: he calculates the dosage, frequency of administration of the drug and the duration of therapy. These parameters completely depend on the nature of the pathology, the stage of the disease and the clinical picture.

So, for adults, Dexamethasone is prescribed as follows:

• in emergencies - intravenously, slowly at a dosage of 4-20 mg, up to 4 times a day (maximum single dose 80 mg);
• to maintain body functions, as part of complex therapy - 0.2–9 mg of the drug per day;
• in shock - intravenously 20 mg Dexamethasone once, then at the rate of 3 mg / kg of body weight for 24 hours;
• with cerebral edema - 10 mg intravenously, then 4 mg every 6 hours.

The drug is rarely prescribed to children. Dosage calculation - 0.02776–0.16665 mg / kg. The indication for the use of the drug is insufficiency of the adrenal cortex. With this disease, Dexamethasone is used as follows:

• 0.0233 mg / kg (0.67 / mg / m2) per day with an interval of 3 days;
• at daily intake- 0.00776–0.01165 mg/kg per day.

• Instructions for use Dexamethasone
• Ingredients of Dexamethasone
• Indications for Dexamethasone
• Dexamethasone storage conditions
• Dexamethasone expiration date

ATC 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

solution for injections. 4 mg/1 ml: amp. 5, 10 or 25 pcs.
Reg. No: RK-LS-5-No. 020631 dated 06/11/2014 - Current

Injection colorless or slightly brown, transparent.

Excipients: water for injection, creatinine, sodium citrate, disodium edetate dihydrate, sodium hydroxide solution 1 M.

1 ml - dark glass ampoules (5) - blister packs (1) - cardboard packs.
1 ml - dark glass ampoules (5) - blister packs (2) - cardboard packs.
1 ml - dark glass ampoules (5) - blister packs (5) - cardboard packs.

Description of the medicinal product DEXAMETHASONE created in 2014 on the basis of instructions posted on the official website of the Ministry of Health of the Republic of Kazakhstan. Date of update: 08/25/2014

pharmachologic effect

Synthetic glucocorticoid drug. It has a pronounced anti-inflammatory, anti-allergic and desensitizing effect, has immunosuppressive activity. Slightly retains sodium and water in the body. These effects are associated with inhibition of the release of inflammatory mediators by eosinophils; induction of the formation of lipocortins and a decrease in the number of mast cells that produce hyaluronic acid; with a decrease in capillary permeability; inhibition of cyclooxygenase activity (mainly COX-2) and prostaglandin synthesis; stabilization of cell membranes (especially lysosomal). The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-I, II, gamma-interferon) from lymphocytes and macrophages. The main effect on metabolism is associated with protein catabolism, an increase in gluconeogenesis in the liver and a decrease in glucose utilization by peripheral tissues. The drug inhibits the activity of vitamin D, which leads to a decrease in calcium absorption and an increase in its excretion from the body. Dexamethasone inhibits the synthesis and secretion of adrenocorticotropic hormone and, secondarily, the synthesis of endogenous glucocorticoids. A feature of the action of the drug is a significant inhibition of the function of the pituitary gland and complete absence mineralocorticoid activity.

Pharmacokinetics

Dexamethasone phosphate is a long-acting glucocorticosteroid. After i / m administration, it is rapidly absorbed from the injection site and distributed in the tissues with blood flow. Approximately 80% of the drug binds to plasma proteins. It penetrates well through the blood-brain and other blood-tissue barriers. Cmax of dexamethasone in the liquor is observed 4 hours after the / in the introduction and is 15-20% of the concentration in the blood plasma. After intravenous administration, a specific effect appears after 2 hours and lasts for 6-24 hours. Dexamethasone is metabolized in the liver much more slowly than cortisone. T1 / 2 from blood plasma - about 3-4.5 hours. About 80% of the administered dexamethasone is eliminated by the kidneys in the form of glucuronide for 24 hours.

Indications for use

• shock of various origins (anaphylactic, post-traumatic, postoperative, cardiogenic, blood transfusion, etc.);
• cerebral edema (with brain tumors, traumatic brain injury, neurosurgical operations, cerebral hemorrhage, meningitis, encephalitis, radiation injuries);
• asthmatic status;
• severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction to medications, serum transfusion, pyrogenic reactions);
• acute hemolytic anemia;
• thrombocytopenia;
• agranulocytosis;
• acute lymphoblastic leukemia;
• severe infectious diseases (in combination with antibiotics);
• acute insufficiency of the adrenal cortex;
• joint diseases (humeroscapular periarthritis, epicondylitis, bursitis, tendovaginitis, osteochondrosis, arthritis of various etiologies, osteoarthritis);
• rheumatoid diseases;
• collagenoses.

Dexamethasone, solution for injection, 4 mg/ml, is used in acute and emergency conditions in which parenteral administration is vital. The drug is intended for short-term use according to vital indications.

Dosing regimen

The dosage regimen is individual and depends on the indications, the severity of the disease and the patient's response to therapy. The drug is administered intramuscularly, intramuscularly by jet or drip, it is also possible periarticular or intraarticular administration. In order to prepare a solution for intravenous drip infusion, isotonic sodium chloride solution, 5% glucose solution or Ringer's solution should be used.

Adults in / in, / m administered from 4 to 20 mg 3-4 times / day. The maximum daily dose is 80 mg. In acute life-threatening situations, high dosages may be necessary. The duration of parenteral use is 3-4 days, then they switch to maintenance therapy with the oral form of the drug. When the effect is achieved, the dose is reduced over several days until a maintenance dose is reached (on average 3-6 mg / day, depending on the severity of the disease) or until treatment is stopped with continuous monitoring of the patient. Rapid intravenous administration of massive doses of glucocorticoids can cause cardiovascular collapse:

• The injection is made slowly, over several minutes.

Cerebral edema (adults): initial dose of 8-16 mg intravenously, followed by 5 mg intravenously or intramuscularly every 6 hours until a satisfactory result is achieved. In brain surgery, these dosages may be needed for several days after the operation. After that, the dosage should be gradually reduced. Continuous treatment may counteract the increase in intracranial pressure associated with a brain tumor.

children appoint in / m. The dose of the drug is usually from 0.2 mg / kg / day to 0.4 mg / kg / day. Treatment should be reduced to the minimum dose in the shortest possible period of time.
With intra-articular administration, the dose depends on the degree of inflammation, the size and location of the affected area. The drug is administered once every 3-5 days (for the synovial bag) and once every 2-3 weeks (for the joint).

Inject no more than 3-4 times in the same joint and no more than 2 joints at the same time. More frequent administration of dexamethasone can damage articular cartilage. Intra-articular injections must be carried out under strictly sterile conditions.

Side effects

Dexamethasone is generally well tolerated. It has low mineralocorticoid activity:

• its effect on water-electrolyte metabolism is small. As a rule, low and medium doses of Dexamethasone do not cause sodium and water retention in the body, increased potassium excretion.

With a single injection:

• nausea, vomiting;
• arrhythmias, bradycardia, up to cardiac arrest;
• arterial hypotension, collapse (especially with the rapid introduction of large doses of the drug);
• decreased glucose tolerance;
• decrease in immunity.

With prolonged therapy:

• steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing's syndrome, delayed sexual development in children, dysfunction of sex hormones (impaired menstrual cycle, amenorrhea, hirsutism, impotence);
• pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, indigestion, flatulence, hiccups, in rare cases - increased activity of hepatic transaminases and alkaline phosphatase, hepatomegaly;
• myocardial dystrophy, development 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;
• delirium, confusion, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure with disc edema (brain pseudotumor - more common in children, usually after too rapid dose reduction, symptoms - headache, blurred vision or double vision) , exacerbation of epilepsy, mental dependence, anxiety, sleep disturbances, dizziness, headache, convulsions, amnesia, cognitive impairment;
• increased intraocular pressure, glaucoma, swelling of the optic nerve head, posterior subcapsular cataract, thinning of the cornea or sclera, exacerbation of bacterial, fungal or viral eye diseases, exophthalmos, sudden loss of vision (with parenteral administration, crystals of the drug may be deposited in the vessels of the eye);
• increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance, increased sweating;
• fluid and sodium retention (peripheral edema), hypernatremia, hypokalemic alkalosis;
• growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely, pathological bone fractures, aseptic necrosis of the head of the humerus and femur), muscle tendon rupture, proximal myopathy, decreased muscle mass (atrophy). Increased pain in the joint, swelling of the joint, painless destruction of the joint, Charcot's arthropathy (with intra-articular injection);
• delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, a tendency to develop pyoderma and candidiasis;
• hypersensitivity, including anaphylactic shock, local allergic reactions - skin rash, itching. Transient burning or tingling in the perineal region after intravenous injection of large doses of phosphate corticosteroids.

Local for parenteral administration:

• burning, numbness, pain, tingling at the injection site, infection at the injection site, rarely - necrosis of surrounding tissues, scarring at the injection site; atrophy of the skin and subcutaneous tissue with intramuscular injection (especially dangerous is the introduction into the deltoid muscle);
• development or exacerbation of infections (contributed to jointly used immunosuppressants and vaccination), leukocytosis, leukocyturia, flushing, withdrawal syndrome, risk of thrombosis and infections.

Contraindications for use

• hypersensitivity to dexamethasone or auxiliary components of the drug;
• systemic infection, unless a specific antibiotic therapy;
• for periarticular or intraarticular administration: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular bone fracture, infectious (septic) inflammatory process in the joint and periarticular infections (including history), as well as a general infectious disease, bacteremia, systemic fungal infection, pronounced periarticular osteoporosis, no signs of inflammation in the joint ("dry" joint, for example, in osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp narrowing of the joint space, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of the epiphyses of the bones forming the joint, injection site infections (eg, septic arthritis due to gonorrhea, tuberculosis).

In children during the period of growth, glucocorticosteroids should be used only according to absolute indications and under the most careful supervision of a physician.

Carefully

Particular attention is required when considering the use of systemic corticosteroids in patients with the following diseases and conditions, while frequent monitoring of the patient's condition is necessary:

Use during pregnancy and lactation

During pregnancy (especially in the first trimester) and during lactation, the drug is prescribed only if the expected therapeutic effect exceeds the potential risk to the fetus and child. With prolonged treatment during pregnancy, the possibility of disruption of fetal growth cannot be ruled out. In the case of use in the last months of pregnancy, there is a risk of developing atrophy of the adrenal cortex in the fetus, which in the future may require replacement therapy in the newborn.

special instructions

In post-marketing studies, very rare cases of tumor lysis syndrome have been reported in patients with hemoblastoses after using dexamethasone alone or in combination with other chemotherapeutic agents. Patients at high risk of developing tumor lysis syndrome should be closely monitored and appropriate precautions should be taken.

Patients and/or caregivers should be warned about the possibility of serious psychiatric side effects. Symptoms usually appear within a few days or weeks after starting treatment. The risk of these side effects is higher with high doses/systemic exposure, although the dose level does not predict the onset, severity or duration of the reaction. Most reactions disappear after dose reduction or discontinuation of the drug, although specific treatment is sometimes necessary. Patients and/or caregivers should seek medical attention if they are concerned about psychological symptoms, in particular depression, suicidal thoughts, although such reactions are not frequently reported. Particular attention should be paid to the use of systemic corticosteroids in patients with existing or a history of severe affective disorders, which include depressive, manic-depressive psychosis, previous steroid psychosis - treatment is carried out only for health reasons.

After parenteral administration of glucocorticoids, serious anaphylactic reactions, such as laryngeal edema, urticaria, bronchospasm, can occur, more often in patients with a history of allergies. If anaphylactic reactions occur, the following measures should be taken: urgently in / in the slow introduction of 0.1-0.5 ml of adrenaline (solution 1: 1000:

• 0.1–0.5 mg of adrenaline, depending on body weight), intravenous administration of aminophylline aminophylline and, if necessary, artificial respiration.

Side effects can be reduced by prescribing the lowest effective doses in short term and by administering a daily dose once in the morning. It is necessary to titrate the dose more often depending on the activity of the disease.

Patients with traumatic brain injury or stroke should not be given glucocorticoids, as this will not benefit and may even be harmful.

In diabetes mellitus, tuberculosis, bacterial and amoebic dysentery, arterial hypertension, thromboembolism, heart and kidney failure, ulcerative colitis, diverticulitis, recently formed intestinal anastomosis, Dexamethasone should be used very carefully and with adequate treatment of the underlying disease.

With the sudden withdrawal of the drug, especially in the case of high doses, a withdrawal syndrome of glucocorticosteroids occurs:

• anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness. Too rapid dose reduction after prolonged treatment can lead to acute adrenal insufficiency, arterial hypotension, death. After discontinuation of the drug for several months, relative insufficiency of the adrenal cortex may persist. If stressful situations arise during this period, temporarily glucocorticoids are prescribed, and if necessary, mineralocorticoids.

Before starting the use of the drug, it is desirable to examine the patient for the presence of ulcerative pathology of the gastrointestinal tract. Patients with a predisposition to the development of this pathology should be prescribed with preventive purpose antacids.

During treatment with the drug, the patient should follow a diet rich in potassium, protein, vitamins, with a reduced content of fats, carbohydrates and sodium.

As a result of the suppression of the inflammatory response and immune function by dexamethasone, susceptibility to infection increases. If the patient has intercurrent infections, a septic condition, treatment with Dexamethasone should be combined with antibiotic therapy.

Chickenpox can be fatal in immunosuppressed patients. Patients who have not had chickenpox should avoid close personal contact with patients with chickenpox or herpes zoster, and in case of contact, seek urgent medical care.

• patients should be careful to avoid contact with people with measles and seek immediate medical attention if contact occurs.

Live vaccines should not be given to people with a weakened immune response. The immune response to other vaccines may be reduced.

If treatment with Dexamethasone is carried out 8 weeks before or within 2 weeks after active immunization (vaccination), then there may be a decrease or loss of the effect of immunization (suppresses antibody formation).

Pediatric use

In children during the period of growth, glucocorticosteroids should be used only for health reasons and under the most careful supervision of a physician. During long-term treatment, it is necessary to carefully monitor the dynamics of growth and development. To prevent disruption of growth processes during long-term treatment of children under the age of 14 years, it is advisable to take a 4-day break in treatment every 3 days.

Premature newborns:

• available data suggest the development of long-term adverse effects on the nervous system after early treatment (<96 ч) недоношенных детей с хроническими заболеваниями легких в начальной дозе 0.25 мг/кг 2 раза/сут.

Recent studies have suggested an association between the use of dexamethasone in premature infants and the development of cerebral palsy. In this regard, an individual approach to prescribing the drug is necessary, taking into account the risk / benefit assessment.

Use in the elderly

Common side effects of systemic corticosteroids may be associated with more serious consequences in the elderly, especially osteoporosis, hypertension, hypokalemia, diabetes mellitus, susceptibility to infection, and thinning of the skin.

Features of the influence of the drug on the ability to drive vehicles or potentially dangerous mechanisms

Since Dexamethasone can cause dizziness and headache, it is recommended that you refrain from driving a car and operating other potentially dangerous mechanisms when driving a motor vehicle or working with other mechanisms.

drug interaction

Pharmaceutical incompatibility of dexamethasone with other intravenous drugs is possible - it is recommended to administer it separately from other drugs (in / in a bolus, or through another dropper, as a second solution). When mixing a solution of dexamethasone with heparin, a precipitate forms.

Co-administration of dexamethasone with:

• inducers of hepatic microsomal enzymes(barbiturates, carbamazepine, primidone, rifabutin, rifampicin, phenytoin, phenylbutazone, theophylline, ephedrine, barbiturates) it is possible to weaken the effects of dexamethasone due to an increase in its excretion from the body;
• diuretics(especially thiazide and carbonic anhydrase inhibitors) and amphotericin B- may lead to increased excretion of potassium from the body and an increased risk of developing heart failure;
• sodium-containing drugs- to the development of edema and increased blood pressure;
• cardiac glycosides - their tolerance worsens and the likelihood of developing ventricular extrasitolia increases (due to the hypokalemia caused);
• indirect anticoagulants- weakens (rarely enhances) their effect (dose adjustment is required);
• anticoagulants and thrombolytics- increased risk of bleeding from ulcers in the gastrointestinal tract;
• ethanol and NSAIDs- the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs in the treatment of arthritis, it is possible to reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect). Indomethacin, displacing dexamethasone from its association with albumin, increases the risk of developing its side effects;
• paracetamol- increases the risk of developing hepatotoxicity (induction of liver enzymes and the formation of a toxic metabolite of paracetamol);
• acetylsalicylic acid- accelerates its excretion and reduces the concentration in the blood. When taking corticosteroids, the renal clearance of salicylates increases, so the abolition of corticosteroids can lead to intoxication of the body with salicylates;
• insulin and oral hypoglycemic drugs, antihypertensive drugs- their effectiveness decreases;
• vitamin D - its effect on the absorption of Ca 2+ in the intestine decreases;
• growth hormone- reduces the effectiveness of the latter;
• M-anticholinergics(including antihistamines and tricyclic antidepressants) and nitrates- promotes increase in intraocular pressure;
• isoniazid and mexiletin- increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.

Carbonic anhydrase inhibitors and loop diuretics may increase the risk of osteoporosis.

ACTH enhances the action of dexamethasone.

Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by dexamethasone.

Cyclosporine and ketoconazole, by slowing down the metabolism of dexamethasone, can in some cases increase its toxicity and increase the risk of seizures in children.

The simultaneous administration of androgens and steroid anabolic drugs with dexamethasone contributes to the development of peripheral edema, hirsutism, and the appearance of acne.

Estrogens and oral estrogen-containing contraceptives reduce the clearance of dexamethasone, which may be accompanied by an increase in the severity of its action.

Mitotane and other inhibitors of adrenal function may necessitate an increase in the dose of dexamethasone.

When used simultaneously with live antiviral vaccines and against the background of other types of immunization, it increases the risk of virus activation and the development of infections.

Antipsychotics (neuroleptics) and azathioprine increase the risk of developing cataracts with dexamethasone.

With simultaneous use with antithyroid drugs, it decreases, and with thyroid hormones, the clearance of dexamethasone increases.

With simultaneous use with drugs that increase the metabolic clearance of glucocorticoids (ephedrine and aminoglutethimide), it is possible to reduce or inhibit the effects of dexamethasone; with carbamazepine - a decrease in the effect of dexamethasone is possible; with imatinib, a decrease in the concentration of imatinib in blood plasma is possible due to the induction of its metabolism and increased excretion from the body.

With simultaneous use with antipsychotics, bucarban, azathioprine, there is a risk of developing cataracts.

With simultaneous use with methotrexate, it is possible to increase hepatotoxicity; with praziquantel - a decrease in the concentration of praziquantel in the blood is possible.

Immunosuppressants and cytostatics enhance the effect of dexamethasone.

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Compound

1 ml of the drug contains

active substance- dexamethasone sodium phosphate 4 mg in terms of dexamethasone phosphate 100% substance

Excipients: sodium chloride, sodium hydrogen phosphate dodecahydrate, disodium edetate, water for injection

Pharmacotherapeuticgroup

Corticosteroids for systemic use. Glucocorticosteroids. Dexamethasone

ATX code H02A B02

Pharmacological properties "type="checkbox">

Pharmacological properties

Pharmacokinetics

After intravenous administration, the maximum concentration of dexamethasone phosphate in blood plasma is reached in just 5 minutes, and after intramuscular administration - after 1 hour. When applied topically as an injection into the joints or soft tissues absorption is slower. The action of drugs begins quickly after intravenous administration. When administered intramuscularly, the clinical effect is observed 8 hours after administration. The drug acts for a long time: from 17 to 28 days after intramuscular injection and from 3 days to 3 weeks after local application. The biological half-life of dexamethasone is 24-72 hours. In plasma and synovial fluid, dexamethasone phosphate is rapidly converted to dexamethasone.

In plasma, approximately 77% of dexamethasone is protein bound, predominantly to albumin. Only a small amount of dexamethasone binds to other plasma proteins. Dexamethasone is a fat-soluble substance, so it penetrates into the inter- and intracellular space. Works in the central nervous system(hypothalamus, pituitary gland) by binding to membrane receptors. In peripheral tissues, it binds and acts through cytoplasmic receptors. Dexamethasone breaks down at the site of its action, i.e. in a cage. Dexamethasone is metabolized primarily in the liver. A small amount of dexamethasone is metabolized in the kidneys and other tissues. The main route of excretion is by the kidneys.

Pharmacodynamics

Dexamethasone is a synthetic hormone of the adrenal cortex (corticosteroid) that has a glucocorticoid effect. It has anti-inflammatory and immunosuppressive effects, and also affects energy metabolism, glucose metabolism and (due to negative feedback) on the secretion of the hypothalamic activating factor and the trophic hormone of the adenohypophysis.

The mechanism of action of glucocorticoids is still not fully understood. There are now a sufficient number of reports on the mechanism of action of glucocorticoids to confirm that they act at the cellular level. There are two well-defined receptor systems in the cytoplasm of cells. By binding to glucocorticoid receptors, corticoids have anti-inflammatory and immunosuppressive effects and regulate glucose metabolism, and by binding to mineralocorticoid receptors, they regulate sodium, potassium, and fluid and electrolyte balance.

Glucocorticoids dissolve in lipids and easily penetrate the target cells through the cell membrane. Binding of the hormone to the receptor leads to a change in the conformation of the receptor, which increases its affinity for DNA. The hormone/receptor complex enters the nucleus of the cell and binds to the regulatory center of the DNA molecule, also called the glucocorticoid response element (GRE). An activated receptor associated with GRE or with specific genes regulates mRNA transcription, which can be increased or decreased. The newly formed mRNA is transported to the ribosome, after which the formation of new proteins occurs. Depending on the target cells and the processes that take place in the cells, protein synthesis can be increased (for example, the formation of tyrosine transaminase in liver cells) or reduced (for example, the formation of IL-2 in lymphocytes). Since glucocorticoid receptors are found in all types of tissues, glucocorticoids can be considered to act on most cells in the body.

Indications for use

• shock of various origins
• cerebral edema (with brain tumors, traumatic brain injury, neurosurgical operations, cerebral hemorrhage, meningitis, encephalitis, radiation injuries)
• bronchial asthma, asthmatic status, severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction to medicines, administration of serum and antibiotics), pyrogenic reactions
• acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis, severe infectious diseases (in combination with antibiotics)
• acute adrenal insufficiency
• acute stenosing laryngotracheitis in children
• humeroscapular periarthritis, epicondylitis, bursitis, tendovaginitis, osteochondrosis, arthritis of various etiologies, osteoarthritis
• rheumatic diseases, collagenoses

Dexamethasone, solution for injection, 4 mg/ml, is used in acute and emergency conditions in which parenteral administration is vital. The drug is intended for short-term use according to vital indications.

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Dosage and administration

Assign to adults and children from birth.

The dosage regimen is individual and depends on the indications, the severity of the disease and the patient's response to therapy. The drug is administered intramuscularly, intravenously slowly in a stream or drip, it is also possible periarticular or intraarticular administration. In order to prepare a solution for intravenous drip infusion, isotonic sodium chloride solution, 5% glucose solution or Ringer's solution should be used.

Adults intravenously, intramuscularly administered from 4 to 20 mg 3-4 times / day. The maximum daily dose is 80 mg. In acute life-threatening situations, high dosages may be necessary. The duration of parenteral use is 3-4 days, then they switch to maintenance therapy with the oral form of the drug. When the effect is achieved, the dose is reduced over several days until a maintenance dose is reached (on average 3-6 mg / day, depending on the severity of the disease) or until treatment is stopped with continuous monitoring of the patient. Rapid intravenous administration of massive doses of glucocorticoids can cause cardiovascular collapse: the injection is performed slowly, over several minutes.

Cerebral edema (adults): an initial dose of 8-16 mg intravenously, followed by 5 mg intravenously or intramuscularly every 6 hours until a satisfactory result is achieved. In brain surgery, these dosages may be needed for several days after the operation. After that, the dosage should be gradually reduced. Continuous treatment may counteract the increase in intracranial pressure associated with a brain tumor.

children prescribe dexamethasone injections intramuscularly. The dose of the drug is usually from 0.2 mg / kg to 0.4 mg / kg per day. Treatment should be reduced to the minimum dose in the shortest possible period of time.

At intra-articular injection the dose depends on the degree of inflammation, the size and location of the affected area. The drug is administered once every 3-5 days (for the synovial bag) and once every 2-3 weeks (for the joint).

Inject no more than 3-4 times into the same joint and no more than 2 joints at the same time. More frequent administration of dexamethasone can damage articular cartilage. Intra-articular injections must be carried out under strictly sterile conditions.

Side effects "type="checkbox">

Side effects

• thromboembolism, a decrease in the number of monocytes and / or lymphocytes, leukocytosis, eosinophilia (as with other glucocorticoids), thrombocytopenia and non-thrombocytopenic purpura
• hypersensitivity reactions, rash, allergic dermatitis, urticaria, angioedema, bronchospasm and anaphylactic reactions, decreased immune response and increased susceptibility to infections
• polytopic ventricular extrasystole, paroxysmal bradycardia, heart failure, cardiac arrest, cardiac rupture in patients with recent myocardial infarction
• arterial hypertension, hypertensive encephalopathy
• after treatment, optic nerve edema and increased intracranial pressure (pseudotumor) may occur. There may also be neurological side effects such as dizziness (vertigo), convulsions and headache, sleep disturbances, confusion, nervousness, restlessness.
• changes in personality and behavior, which most often manifest as euphoria; such side effects: insomnia, irritability, hyperkinesia, depression and psychosis, as well as manic-depressive psychosis, delirium, disorientation, hallucinations, paranoia, mood lability, suicidal thoughts, worsening of schizophrenia, amnesia, worsening of epilepsy
• depression of function and atrophy of the adrenal glands (decrease in response to stress), Cushing's syndrome, growth retardation in children and adolescents, menstrual irregularities, amenorrhea, hirsutism, the transition of latent diabetes to a clinically active form, a decrease in carbohydrate tolerance, an increase in appetite and an increase in body weight, hypertriglyceridemia, obesity, increased need for insulin or oral antidiabetic agents in diabetic patients, negative nitrogen balance due to protein catabolism, hypokalemic alkalosis, sodium and water retention, increased potassium loss, hypocalcemia
• esophagitis, dyspepsia, nausea, vomiting, hiccups, peptic ulcers of the stomach and duodenum, ulcerative perforations and bleeding in the digestive tract (vomiting blood, melena), pancreatitis and perforation of the gallbladder and intestines (especially in patients with chronic inflammation intestines)
• muscle weakness, steroid myopathy (muscle weakness causes muscle catabolism), osteoporosis (increased calcium excretion) and compression fractures of the spine, fractures of tubular bones, aseptic osteonecrosis (more often - aseptic necrosis of the heads of the bones of the thighs and shoulders), tendon ruptures (especially with parallel some quinolones), articular cartilage damage and bone necrosis (due to intra-articular infection), premature closure of epiphyseal growth plates
• delayed wound healing, itching, thinning and sensitization of the skin, striae, petechiae and bruising, acne, telangiectasia, erythema, increased sweating, depressed reaction to skin tests
• elevated intraocular pressure, glaucoma, cataract or exophthalmos, thinning of the cornea, exacerbation of bacterial, fungal or viral eye infections
• development of opportunistic infections, recurrence of inactive tuberculosis
• impotence
• edema, hyper- or hypopigmentation of the skin, atrophy of the skin or subcutaneous layer, sterile abscess and redness of the skin, transient burning and stinging sensation in the perineum when administered intravenously or when administered at high doses
• with intramuscular injection, changes at the injection site, including swelling, burning, numbness, pain, paresthesia and infection at the injection site, rarely necrosis of surrounding tissues, scarring at the injection site, atrophy of the skin and subcutaneous tissue, with intramuscular injection (introduction into the deltoid is especially dangerous muscle)

With intravenous administration: arrhythmias, flushing of the face, convulsions.

With intracranial administration - nosebleeds.

With intra-articular injection - increased pain in the joint.

Signs of glucocorticoid withdrawal syndrome

In patients who have been treated with dexamethasone for a long time, withdrawal syndrome and cases of adrenal insufficiency, arterial hypotension or death may occur during a rapid dose reduction.

In some cases, withdrawal symptoms may be similar to those of worsening or relapse of the disease for which the patient was being treated.

If severe adverse reactions occur, treatment should be discontinued.

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Contraindications

• hypersensitivity to dexamethasone or to any other ingredient of the drug
• acute viral, bacterial or systemic fungal infections (unless appropriate therapy is used)
• Cushing's syndrome
• vaccination with a live vaccine
• intramuscular injection contraindicated in patients with severe bleeding disorders
• peptic ulcer of the stomach and duodenum
• osteoporosis
• pregnancy and lactation
• acute psychoses
• viral and fungal eye diseases, corneal diseases combined with epithelial defects
• trachoma, glaucoma
• active tuberculosis
• kidney failure
• cirrhosis of the liver and chronic hepatitis
• epilepsy
• topical administration is contraindicated in bacteremia, systemic fungal infections, in patients with unstable joints, infections at the site of application, including septic arthritis due to gonorrhea or tuberculosis.

Drug Interactions "type="checkbox">

Drug Interactions

Concurrent use of dexamethasone and non-steroidal anti-inflammatory drugs increases the risk of gastrointestinal bleeding and ulceration.

The effectiveness of dexamethasone is reduced if rifampicin, rifambutin, carbamazepine, phenobarbitone, phenytoin (diphenylhydantoin), primidone, ephedrine or aminoglutethimide are taken concomitantly, so the dose of dexamethasone in such combinations should be increased.

Interactions between dexamethasone and all of the above drugs may interfere with the dexamethasone inhibition test. This must be taken into account when evaluating test results.

Injections Dexamethasone reduces the therapeutic effect of anticholinesterase drugs used in myasthenia gravis.

The combined use of dexamethasone and drugs that inhibit CYP 3A4 enzyme activity, such as ketoconazole, macrolide antibiotics, may cause an increase in the concentration of dexamethasone in serum and plasma. Dexamethasone is a moderate inducer of CYP 3A4. Co-administration with drugs that are metabolized by CYP3A4, such as indinavir, erythromycin, may increase their clearance, causing a decrease in serum concentrations.

Ketoconazole can inhibit the adrenal synthesis of glucocorticoids, thus, due to a decrease in the concentration of dexamethasone, adrenal insufficiency may develop.

Dexamethasone reduces the therapeutic effect of drugs for the treatment of diabetes mellitus, arterial hypertension, coumarin anticoagulants, praziquantel and natriuretics (therefore, the dose of these drugs must be increased); it increases the activity of heparin, albendazole and kaliuretics (the dose of these drugs should be reduced if necessary).

Dexamethasone can change the effect of coumarin anticoagulants, so when using this combination of drugs, you need to check the prothrombin time more often.

Concomitant use of dexamethasone and high doses of other glucocorticoids or β2-adrenergic agonists increases the risk of hypokalemia. In patients with hypokalemia, cardiac glycosides contribute more to rhythm disturbance and have greater toxicity.

Antacids reduce the absorption of dexamethasone from the stomach. The effect of dexamethasone when taken with food and alcohol has not been studied, but the simultaneous use of drugs and food with a high sodium content is not recommended. Smoking does not affect the pharmacokinetics of dexamethasone.

Glucocorticoids increase the renal clearance of salicylate, so it is sometimes difficult to obtain therapeutic serum concentrations of salicylates. Caution should be exercised in patients who gradually reduce the dose of corticosteroid, since this may lead to an increase in the concentration of salicylate in the blood serum and intoxication.

If oral contraceptives are used in parallel, the half-life of glucocorticoids may increase, which enhances their biological effect and may increase the risk of side effects.

Simultaneous use of ritodrine and dexamethasone is contraindicated during childbirth, as this can lead to pulmonary edema. Reported lethal outcome in a woman in labor due to the development of such a condition.

The simultaneous use of dexamethasone and thalidomide can cause toxic epidermal necrolysis.

Types of interaction that have therapeutic benefits: concomitant administration of dexamethasone and metoclopramide, diphenhydramide, prochlorperazine or 5-HT3 receptor antagonists (serotonin or 5-hydroxytryptamine type 3 receptors, such as ondansetron or granisetron) is effective in preventing nausea and vomiting caused by chemotherapy with cisplatin, cyclophosphamide, methotrexate, fluorouracil.

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special instructions

During parenteral treatment with corticoids, hypersensitivity reactions can rarely be observed, therefore, it is necessary to take appropriate measures before starting treatment with dexamethasone, taking into account the possibility of allergic reactions (especially in patients with a history of allergic reactions to any other drugs).

Patients treated with dexamethasone for a long time may experience a withdrawal syndrome (also without visible signs of adrenal insufficiency) upon discontinuation of treatment (fever, runny nose, conjunctival redness, headache, dizziness, drowsiness or irritability, muscle and joint pain, vomiting , weight loss, weakness, often also convulsions). Therefore, the dose of dexamethasone should be reduced gradually. Sudden discontinuation of treatment can be fatal.

If the patient is under severe stress (due to injury, surgery, or serious illness) during therapy, the dose of dexamethasone should be increased, and if this occurs during the cessation of treatment, hydrocortisone or cortisone should be used.

Patients who have been administered dexamethasone for a long time and who experience severe stress after discontinuation of therapy should be reinstated on dexamethasone, since the adrenal insufficiency caused by it can last for several months after discontinuation of treatment.

Treatment with dexamethasone or natural glucocorticoids may mask symptoms of an existing or new infection, as well as symptoms of intestinal perforation. Dexamethasone can exacerbate systemic fungal infection, latent amoebiasis, and pulmonary tuberculosis.

Caution and medical supervision are recommended in patients with osteoporosis, with arterial hypertension, heart failure, tuberculosis, glaucoma, hepatic or kidney failure, diabetes mellitus, active peptic ulcer, recent intestinal anastomosis, ulcerative colitis and epilepsy. Special care is required for patients during the first weeks after myocardial infarction, patients with thromboembolism, myasthenia gravis, hypothyroidism, psychosis or psychoneurosis, as well as elderly patients .

During treatment, an exacerbation of diabetes mellitus or a transition from a latent phase to clinical manifestations diabetes mellitus.

With prolonged treatment, it is necessary to control the level of potassium in the blood serum.

Vaccination with a live vaccine is contraindicated during treatment with dexamethasone. Vaccination with an inactivated viral or bacterial vaccine does not lead to the expected antibody synthesis and does not have the expected protective effect. Dexamethasone phosphate is usually not prescribed 8 weeks before vaccination and is not started earlier than 2 weeks after vaccination.

Patients who have been treated with high doses of dexamethasone for a long time and have never had measles should avoid contact with infected individuals; in case of accidental contact, prophylactic treatment with immunoglobulin is recommended.

The action of glucocorticoids is enhanced in patients with cirrhosis of the liver or hypothyroidism.

Severe mental reactions may accompany the systemic use of corticosteroids. Usually, symptoms appear a few days or weeks after the start of treatment. The risk of developing these symptoms increases with high doses. Most reactions resolve with dose reduction or drug withdrawal. It is necessary to observe and timely detect changes in the mental state, especially depressive mood, suicidal thoughts and intentions. With particular caution, corticosteroids should be used in patients with affective disorders present or in history, as well as in close relatives. The occurrence of undesirable effects can be prevented by using the minimum effective dose for the shortest period or by using the required daily dose of the drug 1 time in the morning.

Intra-articular use of dexamethasone can lead to systemic effects.

Frequent use may cause cartilage damage or bone necrosis.

Before intra-articular injection, synovial fluid must be removed from the joint and examined (check for infection). Injection of corticoids into infected joints should be avoided. If a joint infection develops after the injection, appropriate antibiotic therapy should be started.

Patients should be advised to avoid exertion on the affected joints until the inflammation has resolved.

Avoid injecting the drug into unstable joints.

Corticoids can interfere with the results of skin allergy tests.

Special precautions regarding excipients. The drug contains 1 mmol (23 mg) sodium per dose, which is a very small amount.

Incompatibility. The drug should not be mixed with other drugs, except for the following: 0.9% sodium chloride solution or 5% glucose solution.

When mixing dexamethasone with chlorpromazine, diphenhydramine, doxapram, doxorubicin, daunorubicin, idarubicin, hydromorphone, ondansetron, prochlorperazine, potassium nitrate and vancomycin, a precipitate forms.

Approximately 16% dexamethasone dissolves in 2.5% glucose solution and 0.9% sodium chloride solution with amikacin.

Some medicines, such as lorazepam, should be mixed with dexamethasone in glass vials rather than plastic bags (Lorazepam concentrations drop below 90% after 3-4 hours of storage in PVC bags at room temperature).

Some drugs, such as metapaminol, have a so-called "incompatibility that develops slowly" - it develops within a day when mixed with dexamethasone.

Dexamethasone with glycopyrolate: The pH of the final solution is 6.4, which is outside the stability range.

Use during pregnancy or lactation

The drug is contraindicated during pregnancy or during lactation

Application in pediatrics . Use in children from birth only if absolutely necessary. During treatment with dexamethasone, careful monitoring of the growth and development of children is necessary.

Features of the effect of the drug on the ability to drive vehicles or potentially dangerous mechanisms

Given that in sensitive patients when using the drug, there may be adverse reactions(dizziness, confusion, etc.), for the period of use of the drug, you should refrain from driving vehicles and performing other work that requires concentration.

Solution for injection 4 mg/ml 1 ml

Shelf life

Do not use the drug after the expiration date indicated on the package.

Terms of dispensing from pharmacies

On prescription

Manufacturer

PJSC "Farmak", Ukraine, 04080, Kiev, st. Frunze, 63.

Registration certificate holder

PJSC Farmak, Ukraine