Instructions for use dexamethasone (dexamethasone). Dexamethasone injections - when they are needed, indications and precautions for administering Dexamethasone injections instructions for use 0

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Characteristics of the substance Dexamethasone

Hormonal agent (glucocorticoid for systemic and topical use). Fluorinated hydrocortisone homologue.

Dexamethasone is a white or almost white, odorless crystalline powder. Solubility in water (25 °C): 10 mg/100 ml; soluble in acetone, ethanol, chloroform. Molecular weight 392.47.

Dexamethasone sodium phosphate is a white or slightly yellow crystalline powder. Easily soluble in water and very hygroscopic. Molecular weight 516.41.

Pharmacology

pharmachologic effect- anti-inflammatory, anti-allergic, immunosuppressive, anti-shock, glucocorticoid.

Interacts with specific cytoplasmic receptors and forms a complex that penetrates into the cell nucleus; causes expression or depression of mRNA, changing the formation of proteins on ribosomes, incl. lipocortin mediating cellular effects. Lipocortin inhibits phospholipase A 2 , inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, PG, leukotrienes, which promote inflammation, allergies, etc. It prevents the release of inflammatory mediators from eosinophils and mast cells. It inhibits the activity of hyaluronidase, collagenase and proteases, normalizes the functions of the intercellular matrix of cartilage and bone tissue. Reduces capillary permeability, stabilizes cell membranes, incl. lysosomal, inhibits the release of cytokines (interleukins 1 and 2, interferon gamma) from lymphocytes and macrophages. It affects all phases of inflammation, the antiproliferative effect is due to inhibition of monocyte migration to the inflammatory focus and fibroblast proliferation. Causes involution of lymphoid tissue and lymphopenia, which causes immunosuppression. In addition to reducing the number of T-lymphocytes, their influence on B-lymphocytes is reduced and the production of immunoglobulins is inhibited. The effect on the complement system is to reduce the formation and increase the breakdown of its components. The antiallergic effect is a consequence of inhibition of the synthesis and secretion of allergy mediators and a decrease in the number of basophils. Restores the sensitivity of adrenergic receptors to catecholamines. Accelerates protein catabolism and reduces their content in plasma, reduces the utilization of glucose by peripheral tissues and increases gluconeogenesis in the liver. Stimulates the formation of enzyme proteins in the liver, surfactant, fibrinogen, erythropoietin, lipomodulin. Causes redistribution of fat (increases lipolysis of adipose tissue of the extremities and fat deposition in the upper half of the body and on the face). Promotes the formation of higher fatty acids and triglycerides. Reduces absorption and increases excretion of calcium; delays sodium and water, ACTH secretion. Has anti-shock effect.

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract, T max - 1-2 hours. In the blood, it binds (60-70%) to a specific carrier protein - transcortin. Easily passes through histohematic barriers, including the BBB and placental. Biotransformed in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. T 1/2 from plasma - 3-4.5 hours, T 1/2 from tissues - 36-54 hours. Excreted by the kidneys and through the intestines, penetrates into breast milk.

After instillation into the conjunctival sac, it penetrates well into the epithelium of the cornea and conjunctiva, while therapeutic concentrations of drugs are created in the aqueous humor of the eye. With inflammation or damage to the mucous membrane, the rate of penetration increases.

The use of the substance Dexamethasone

For systemic use (parenterally and orally)

Shock (burn, anaphylactic, post-traumatic, postoperative, toxic, cardiogenic, blood transfusion, etc.); cerebral edema (including with tumors, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); bronchial asthma, asthmatic status; systemic diseases connective tissue(including systemic lupus erythematosus, rheumatoid arthritis, scleroderma, periarteritis nodosa, dermatomyositis); thyrotoxic crisis; hepatic coma; poisoning with caustic fluids (in order to reduce inflammation and prevent cicatricial narrowing); acute and chronic inflammatory diseases joints, incl. gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, humeroscapular periarthritis, ankylosing spondylitis (Bekhterev's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tendosynovitis, synovitis, epicondylitis; rheumatic fever, acute rheumatic heart disease; acute and chronic allergic diseases: allergic reactions on drugs and food products, serum sickness, urticaria, allergic rhinitis, hay fever, angioedema, drug exanthema; skin diseases: pemphigus, psoriasis, dermatitis (contact dermatitis with damage to a large surface of the skin, atopic, exfoliative, bullous herpetiform, seborrheic, etc.), eczema, toxidermia, toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema(Stevens-Johnson syndrome); allergic eye diseases: allergic corneal ulcers, allergic forms of conjunctivitis; inflammatory eye diseases: sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis; primary or secondary adrenal insufficiency (including condition after removal of the adrenal glands); congenital adrenal hyperplasia; kidney disease of autoimmune origin (including acute glomerulonephritis), nephrotic syndrome; subacute thyroiditis; diseases of the hematopoietic organs: agranulocytosis, panmyelopathy, anemia (including autoimmune hemolytic, congenital hypoplastic, erythroblastopenia), idiopathic thrombocytopenic purpura, secondary thrombocytopenia in adults, lymphoma (Hodgkin's, non-Hodgkin's), leukemia, lymphocytic leukemia (acute, chronic); lung diseases: acute alveolitis, pulmonary fibrosis, sarcoidosis stage II-III; tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (only in combination with specific therapy); berylliosis, Leffler's syndrome (resistant to other therapy); lung cancer(in combination with cytostatics); multiple sclerosis; diseases of the gastrointestinal tract (to remove the patient from a critical condition): ulcerative colitis, Crohn's disease, local enteritis; hepatitis; prevention of graft rejection; tumor hypercalcemia, nausea and vomiting during cytostatic therapy; myeloma; testing at differential diagnosis hyperplasia (hyperfunction) and tumors of the adrenal cortex.

For topical application

Intraarticular, periarticular. Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, Reiter's disease, osteoarthritis (if present) pronounced signs inflammation of the joint, synovitis).

Conjunctival. Conjunctivitis (non-purulent and allergic), keratitis, keratoconjunctivitis (without damage to the epithelium), iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, episcleritis, scleritis, uveitis of various origins, retinitis, optic neuritis, retrobulbar neuritis, superficial corneal trauma various etiologies(after complete epithelialization of the cornea), inflammatory processes after eye injuries and eye operations, sympathetic ophthalmia.

Into the external auditory canal. Allergic and inflammatory diseases of the ear, incl. otitis.

Contraindications

Hypersensitivity (for short-term systemic use for health reasons is the only contraindication).

For intra-articular injection. Unstable joints, previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), transarticular bone fracture, infected lesions of the joints, periarticular soft tissues and intervertebral spaces, severe periarticular osteoporosis.

Eye forms. Viral, fungal and tubercular lesions of the eyes, incl. keratitis caused by herpes simplex, viral conjunctivitis, acute purulent eye infection (in the absence of antibiotic therapy), violation of the integrity of the corneal epithelium, trachoma, glaucoma.

Ear forms. Perforation of the tympanic membrane.

Application restrictions

For systemic use (parenterally and orally): Itsenko-Cushing's disease, obesity III-IV degree, convulsive conditions, hypoalbuminemia and conditions predisposing to its occurrence; open angle glaucoma.

For intra-articular administration: the general serious condition of the patient, the inefficiency or short duration of the action of the two previous injections (taking into account the individual properties of the glucocorticoids used).

Use during pregnancy and lactation

The use of corticosteroids during pregnancy is possible if the expected effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled safety studies have not been conducted). Women of childbearing age should be warned of the potential risk to the fetus (corticosteroids pass through the placenta). It is necessary to carefully monitor newborns whose mothers received corticosteroids during pregnancy (the development of adrenal insufficiency in the fetus and newborn is possible).

Dexamethasone has been shown to be teratogenic in mice and rabbits after topical ophthalmic applications of multiple therapeutic doses.

In mice, corticosteroids cause fetal resorption and a specific disorder, the development of a cleft palate in offspring. In rabbits, corticosteroids cause fetal resorption and multiple disorders, incl. anomalies in the development of the head, ear, limbs, palate, etc.

Breastfeeding women are advised to stop either breast-feeding, or the use of drugs, especially in high doses (corticosteroids penetrate into breast milk and can inhibit growth, the production of endogenous corticosteroids and cause unwanted effects in a newborn).

It should be borne in mind that when topical application glucocorticoids are systemically absorbed.

Side effects of Dexamethasone

The frequency of development and severity of side effects depend on the duration of use, the size of the dose used and the possibility of observing the circadian rhythm of drug administration.

System effects

From the side nervous system and sense organs: delirium (confusion, agitation, anxiety), disorientation, euphoria, hallucinations, manic/depressive episode, depression or paranoia, increased intracranial pressure with congestive optic papilla syndrome (brain pseudotumor - more common in children, usually after too rapid dose reduction, symptoms — headache, blurred vision or double vision); sleep disturbance, dizziness, vertigo, headache; sudden loss of vision (with parenteral administration in the head, neck, turbinates, scalp), formation of posterior subcapsular cataracts, increased intraocular pressure with possible damage optic nerve, glaucoma, steroid exophthalmos, development of secondary fungal or viral infections eye.

From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): arterial hypertension, development of chronic heart failure (in predisposed patients), myocardial dystrophy, hypercoagulability, thrombosis, ECG changes characteristic of hypokalemia; when administered parenterally: flushes of blood to the face.

From the digestive tract: nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract, pancreatitis, erosive esophagitis, hiccups, increase / decrease in appetite.

From the side of metabolism: retention of Na + and water (peripheral edema), hypokalemia, hypocalcemia, negative nitrogen balance due to protein catabolism, weight gain.

From the endocrine system: suppression of the function of the adrenal cortex, decreased glucose tolerance, steroid diabetes mellitus or the manifestation of latent diabetes mellitus, Itsenko-Cushing's syndrome, hirsutism, irregular menstruation, growth retardation in children.

From the musculoskeletal system: muscle weakness, steroid myopathy, decreased muscle mass, osteoporosis (including spontaneous bone fractures, aseptic necrosis of the femoral head), tendon rupture; pain in muscles or joints, back; when administered intraarticularly: increased joint pain.

From the side of the skin: steroid acne, striae, thinning of the skin, petechiae and ecchymosis, delayed wound healing, increased sweating.

Allergic reactions: skin rash, hives, swelling of the face, stridor or shortness of breath, anaphylactic shock.

Others: decreased immunity and activation of infectious diseases, withdrawal syndrome (anorexia, nausea, lethargy, abdominal pain, general weakness, etc.).

Local reactions with parenteral administration: burning, numbness, pain, paresthesia and infection at the injection site, scarring at the injection site; hyper- or hypopigmentation; atrophy of the skin and subcutaneous tissue (with i / m administration).

Eye forms: with prolonged use (more than 3 weeks), an increase in intraocular pressure and / or the development of glaucoma with damage to the optic nerve, a decrease in visual acuity and loss of visual fields, the formation of posterior subcapsular cataracts, thinning and perforation of the cornea; the spread of herpetic and bacterial infection is possible; in patients with hypersensitivity to dexamethasone or benzalkonium chloride, conjunctivitis and blepharitis may develop.

Dexamethasone is a drug that belongs to the group of corticosteroids. There are many pathologies that require the use of this medicinal product.

It is sometimes used to treat even infants, but only in cases where it is necessary to take urgent measures that will save the child's life (for example, when, or when other medicines have not had the desired therapeutic effect. At the same time, be sure to constantly be under the supervision of a doctor.

Features of the drug

The medicine is available in several dosage forms: in the form of injections, tablets and drops. Dexamethasone is usually given to children in injectable or tablet form.

The active ingredient is dexamethasone phosphate. With regard to the additional ingredients of the drug, it must be said that the composition of the drug depends on its form:

  1. In the injectable form 4 mg of active ingredient per 1 ml of solution is included, and a small amount of glycerin, propylene glycol, a buffered phosphate solution, and water are observed as concomitant components.
  2. in tablet form is 0.5 mg active substance, as well as lactose, silicon and residual amounts of magnesium stearate.
  3. IN eye drops is the main active ingredient weighing 1 mg per milliliter of solution, as well as small amounts of boric acid, sodium tetraborate, water and preservatives.

Active substance able to pass into cells and increase the synthesis of ribonucleic acid. Due to the inhibition of phospholipase, there is an increase in the production of arachidonic acids, as well as the biosynthesis of endoperoxide, mediators of an inflammatory allergic reaction and pain syndrome.

As a result of the action of the drug, there is a decrease in the amount of protease, hyaluronidase and collagenase in a small amount or in the absence of it, which leads to the following:

  1. Improving the functioning of bone and cartilage tissues.
  2. Decreased capillary permeability.
  3. Correction of stabilization of cell membranes.
  4. Retention of water and sodium in the body.
  5. Increased protein catabolism, glucose utilization, and increased glycogen release from the liver.

When taking the tablet form of Dexamethasone for children, almost complete absorption of the drug into the blood from the stomach is observed. At the same time, the percentage of binding to blood proteins is not too high, it reaches an average of no more than 80%, and bioavailability is no more than 70%. The active substance is able to act inside the cells.

The effect may appear already after a few minutes from the moment of administration, but the maximum effect is achieved on average after 2 hours. The duration of the therapeutic effect of the drug can be 3 days.

When using the injectable form, the effect of the drug can occur much faster. This is largely due to the lack of time required for the absorption of the drug. The drug penetrates the blood-brain barrier, thereby affecting the organs of the central nervous system.
The drug is excreted in the urine through the urinary system.

Dexamethasone is incompatible with other drugs.

Indications and contraindications

Dexamethasone can be used for various pathologies, but due to possible side effects, as well as the presence of a large number of contraindications, including childhood, it is not used so often. Basically, its use is justified only in cases where there is a threat to life. AND childhood here is no exception.

Among the indications in which there is an acute threat to life, there are:

  1. Anaphylactic shock, manifested by a sharp drop blood pressure, disruption of the heart and other vital organs.
  2. Severe allergic reaction in the form of.
  3. cerebral edema, as a result of a traumatic brain injury, an infectious process, the presence of a tumor process in the skull area.
  4. Toxic state associated with a massive burn, a consequence of pain or traumatic shock, acute blood loss.
  5. Acute deficiency adrenal apparatus.

Dexamethasone in children is also used for the following chronic diseases:

  • severe course, clinic of severe bronchospasm;
  • severe autoimmune pathologies such as rheumatoid arthritis or systemic lupus erythematosus;
  • expressed;
  • Crohn's disease or ulcerative colitis with severe dysfunction of the digestive tract;
  • hemolytic anemia or other pathologies of the blood system;
  • glomerulonephritis;
  • severe infectious processes;
  • malignant lesions.

Among the contraindications, in which even acute processes will not be an indication for the appointment of this drug, we should highlight:

  • increased sensitivity of the body to the components of the drug;
  • allergy to dexamethasone;
  • acute diseases that can be caused by bacterial, viral, and fungal infections;
  • condition associated with direct vaccination, especially after BCG vaccination;
  • pathologies of the cornea, accompanied by a violation of its integrity;
  • Itsenko-Cushing's syndrome;
  • inflammatory diseases of the digestive tract, especially associated with the presence of erosive and ulcerative defects (gastritis, stomach ulcers or duodenum);
  • tuberculosis and other chronic infectious processes;
  • pathologies of the nervous system, accompanied by convulsions, epilepsy;
  • diseases of the endocrine system, especially thyroid gland(hypothyroidism or thyroiditis).

Dexamethasone should be taken with caution in case of impaired liver function.

For the treatment of severe nasal congestion in children, difficulty breathing due to allergies, Dexamethasone drops are sometimes prescribed for instillation into the nose. Such an unusual use of the drug relieves swelling well, eliminates inflammation, and facilitates the baby's breathing.

Possible side effects

Side effects are a common problem with Dexamethasone in children. The most common reactions include:

  1. allergic reaction in response to the introduction of the drug, which most often has the form of urticaria, eczema or rashes of a different nature.
  2. Violation of the nervous system such as headache, dizziness, neuropathy, etc.
  3. Damage to the digestive tract. It can be manifested by the appearance or complication of pancreatitis, gastritis, as well as peptic ulcer stomach and duodenum.
  4. Children have incorrect or long-term use Dexamethasone can cause growth retardation of both the whole organism and individual systems. That is why in babies taking Dexamethasone, there are acquired heart defects, serious disturbances in work internal organs, underdevelopment or lag in the development of the sex glands and organs of the reproductive system.
  5. The appearance of a specific appearance associated with an increase in body weight, water retention in the body, atrophy of the muscular apparatus.
  6. Mental disorders.
  7. Skin change with their depletion and the appearance of striae and cicatricial changes.
  8. Development of cataracts and glaucoma.

Instructions for the use of Dexamethasone for children in the form of injections, tablets and drops

The dosage of the drug in children and not only should be calculated only by a specialist, based on pathological condition patient, the severity of the process, as well as the age of the patient and his body weight.
The method of administration and dose of Dexamethasone for children depends on the form of the drug and indications.

Using injection form the drug prescription by a doctor may be as follows: with the development of an acute condition, which is an emergency, a calculation is made from 0.02 mg per 1 kg of body weight. In some cases, the dosage may be increased to 0.16 mg per 1 kg. In this case, it is necessary to take into account the dosing regimen and frequency of administration. The minimum duration between injections is 12 hours. In some cases, a single injection of Dexamethasone intramuscularly or intravenously is used. In acute adrenal insufficiency, it is permissible to increase the dosage to 0.2-0.3 mg per kilogram of body weight until the condition stabilizes.

In the form of tablets with inflammatory, allergic or other chronic pathologies Dexamethasone, a dosage of 0.25 mg, is divided into three or four doses per day. The maximum daily dosage can reach 2 mg.

In the form of eye drops Dexamethasone is allowed to take in the amount of one drop up to 3 times a day. The duration of therapy can be up to a week. In the case of a severe or chronic process, an individual increase in the duration of use of this medicinal product is possible.

The drug in liquid form in ampoules is often used for inhalation in children with inflammation of the respiratory tract (for example, with bronchitis, laryngitis, bronchial obstruction). For children, the following dosage is used: 0.5 ml of the drug is mixed with 2-3 ml of saline. Inhalations are done 3 times a day for 3-7 days.

How much and how to store

The price of Dexamethasone depends not only on the type of pharmacy and the manufacturer, but also dosage form. The average cost of a tablet form is about 50 rubles. The injection form can reach a price of about 200 rubles. The cost of eye drops is about 70 rubles. The drug is dispensed from the pharmacy only with a doctor's prescription.

The drug can be stored in the form of tablets and injections for five years from the date of manufacture, and the shelf life for drops is three years, but only on condition that the vial is sealed. After opening, the drops must be used within 3 weeks.
The optimum temperature regime should not exceed 25 degrees Celsius. It is necessary to protect the drug from exposure to sunlight.

  • 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 the complete absence of 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 (contribute 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, and 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 with high risk development of 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 administering the lowest effective dose for the shortest duration and by administering 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.

    At diabetes, tuberculosis, bacterial and amoebic dysentery, arterial hypertension, thromboembolism, cardiac 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 long-term 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 antacids for prophylactic purposes.

    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.

INN: Dexamethasone

Manufacturer: Krka, d.d., Novo Mesto

Anatomical-therapeutic-chemical classification: Dexamethasone

Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 003394

Registration period: 05.08.2016 - 05.08.2021

Instruction

Tradename

Dexamethasone

International non-proprietary name

Dexamethasone

Dosage form

Solution for injection, 4 mg/ml

Composition

One ampoule contains

active substance- dexamethasone sodium phosphate 4.37 mg (equivalent to dexamethasone phosphate 4.00 mg),

inexcipients: glycerin, disodium edetate, sodium hydrogen phosphate dihydrate, water for injection.

Description

Clear, colorless to light yellow solution

Pharmacotherapeutic group

Corticosteroids for systemic use. Glucocorticosteroids. Dexamethasone.

ATX code H02AB02

Pharmacological properties

Pharmacokinetics

After intravenous administration, the drug begins to act quickly, and after intramuscular administration, the clinical effect is achieved after 8 hours. The action of the drug is prolonged and lasts from 17 to 28 days after intramuscular injection and from 3 days to 3 weeks after local application (in the affected area). A dose of 0.75 mg dexamethasone is equivalent to a dose of 4 mg methylprednisolone and triamcinolone, 5 mg prednisone and prednisolone, 20 mg hydrocortisone, and 25 mg cortisone. In plasma, about 77% of dexamethasone binds to plasma proteins, and the majority is converted to albumin. Only a minimal amount of dexamethasone binds to non-albumin proteins. Dexamethasone is a fat soluble compound. The drug is initially metabolized in the liver. Small amounts of dexamethasone are metabolized in the kidneys and other organs. The predominant excretion occurs through the urine. The half-life (T1 \ 2) is about 190 minutes.

Pharmacodynamics

Dexamethasone is a synthetic adrenal hormone (corticosteroid) with glucocorticoid action. The drug has a pronounced anti-inflammatory, anti-allergic and desensitizing effect, has immunosuppressive activity.

To date, enough information has been accumulated on the mechanism of action of glucocorticoids to imagine how they act at the cellular level. There are two well-defined receptor systems found in the cytoplasm of cells. Through glucocorticoid receptors, corticosteroids exert anti-inflammatory and immunosuppressive effects and regulate glucose homeostasis; through mineralocorticoid receptors, they regulate sodium and potassium metabolism, as well as water and electrolyte balance.

Indications for use

Dexamethasone is administered intravenously or intramuscularly in acute cases or when oral therapy is not possible:

    replacement therapy for primary and secondary (pituitary) adrenal insufficiency

    congenital adrenal hyperplasia

    subacute thyroiditis and severe forms of postradiation thyroiditis

    rheumatic fever

    acute rheumatic heart disease

    pemphigus, psoriasis, dermatitis (contact dermatitis affecting a large surface of the skin, atopic, exfoliative, bullous herpetiform, seborrheic, etc.), eczema

    toxidermia, toxic epidermal necrolysis (Lyell's syndrome)

    malignant exudative erythema (Stevens-Johnson syndrome)

    allergic reactions to drugs and food

    serum sickness, drug exanthema

    urticaria, angioedema

    allergic rhinitis, hay fever

    diseases that threaten the loss of vision (acute central chorioretinitis, inflammation of the optic nerve)

    allergic conditions (conjunctivitis, uveitis, scleritis, keratitis, iritis)

    systemic immune diseases (sarcoidosis, temporal arteritis)

    proliferative changes in the orbit (endocrine ophthalmopathy, pseudotumors)

    sympathetic ophthalmia

    immunosuppressive therapy in corneal transplantation

The drug is used systemically or locally (in the form of subconjunctival, retrobulbar or parabulbar injections):

    ulcerative colitis

    Crohn's disease

    local enteritis

    sarcoidosis (symptomatic)

    acute toxic bronchiolitis

    chronic bronchitis and asthma (exacerbations)

    agranulocytosis, panmyelopathy, anemia (including autoimmune hemolytic, congenital hypoplastic, erythroblastopenia)

    idiopathic thrombocytopenic purpura

    secondary thrombocytopenia in adults, lymphoma (Hodgkin's, non-Hodgkin's)

    leukemia, lymphocytic leukemia (acute, chronic)

    kidney disease of autoimmune origin (including acute glomerulonephritis)

    nephrotic syndrome

    palliative care for leukemia and lymphoma in adults

    acute leukemia in children

    hypercalcemia in malignant neoplasms

    cerebral edema due to primary tumors or metastases to the brain, due to craniotomy or head trauma.

Shock of various origins

    shock not responding to standard therapy

    shock in patients with adrenal insufficiency

    anaphylactic shock (intravenously, after the introduction of adrenaline)

Other indications

Indications for intra-articular administration of dexamethasone or injection into soft tissues:

    rheumatoid arthritis (severe inflammation in a single joint)

    ankylosing spondylitis (when inflamed joints do not respond to standard therapy)

    psoriatic arthritis (oligoarticular lesion and tendosynovitis)

    monoarthritis (after removal of intra-articular fluid)

    osteoarthritis (only in the presence of exudate and synovitis)

    extra-articular rheumatism (epicondylitis, tendosynovitis, bursitis)

Local administration (injections into the lesion):

  • hypertrophic, inflamed, and infiltrated lesions of lichen, psoriasis, granuloma annulare, sclerosing folliculitis, discoid lupus, and cutaneous sarcoidosis

    localized alopecia

Dosage and administration

Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, the tolerability of corticosteroids and the patient's response to therapy.

Parenteral application

The solution for injection is administered intravenously or intramuscularly, as well as in the form of intravenous infusions (with glucose or saline).

The recommended average initial daily dose for intravenous or intramuscular administration varies from 0.5 mg to 9 mg and, if necessary, more. The initial dose of dexamethasone should be used until the clinical effect is achieved; then the dose is gradually reduced to the minimum effective. During the day, you can enter from 4 to 20 mg of Dexamethasone 3-4 times. The duration of parenteral administration is usually 3-4 days, then they switch to maintenance therapy with the oral form of the drug.

Local administration

The recommended single dose of dexamethasone for intra-articular administration is from 0.4 mg to 4 mg. Intra-articular injection can be repeated after 3-4 months. Injections into the same joint can only be done 3-4 times in a lifetime, and injections into more than two joints at the same time should not be made. More frequent administration of dexamethasone can lead to damage to intra-articular cartilage and bone necrosis. The dose depends on the size of the affected joint. The usual dose of dexamethasone is 2 mg to 4 mg for large joints and 0.8 mg to 1 mg for small joints.

The usual dose of dexamethasone for intraarticular capsule is 2 mg to 3 mg, for the introduction into the tendon sheath - from 0.4 mg to 1 mg, and for tendons - from 1 mg to 2 mg.

When administered to limited lesions, the same doses of dexamethasone are used as for intra-articular administration. The drug can be administered simultaneously, at most, in two foci.

Dosing in children

When administered intramuscularly, the dose for replacement therapy is 0.02 mg / kg of body weight or 0.67 mg / m2 of body surface area, which is divided into 3 injections with an interval of 2 days, or from 0.008 mg to 0.01 mg / kg of body weight body or 0.2 mg to 0.3 mg/m2 of body surface area daily. For other indications, the recommended dose is 0.02 mg to 0.1 mg/kg body weight, or 0.8 mg to 5 mg/m2 body surface area, every 12 to 24 hours.

Side effects

    decreased glucose tolerance, "steroidal" diabetes mellitus, or manifestation of latent diabetes mellitus

    Itsenko-Cushing's syndrome, weight gain

    hiccups, nausea, vomiting, increased or decreased appetite, flatulence, increased activity of "liver" transaminases and alkaline phosphatase, pancreatitis

    "steroid" ulcer of the stomach and duodenum, erosive zophagitis, bleeding and perforation of the gastrointestinal tract

    arrhythmias, bradycardia (up to cardiac arrest), development (in predisposed patients) or increased severity of chronic heart failure, increased blood pressure

    hypercoagulation, thrombosis

    delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia

    increased intracranial pressure, nervousness, anxiety, insomnia, headache, dizziness, convulsions, vertigo

    pseudotumor of the cerebellum

    sudden loss of vision (with parenteral administration, crystals of the drug may be deposited in the vessels of the eye), posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, trophic changes in the cornea, exophthalmos, development of secondary bacterial, fungal or viral eye infections

    negative nitrogen balance (increased protein breakdown), hyperlipoproteinemia

    increased sweating

    fluid and sodium retention (peripheral edema), hyperkalemia syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue)

    growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones)

    increased excretion of calcium, osteoporosis, pathological bone fractures, aseptic necrosis of the head of the humerus and femur, tendon rupture

    "steroid" myopathy, muscle atrophy

    delayed wound healing, a tendency to develop pyoderma and candidiasis

    petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation,

steroid acne, striae

    generalized and local allergic reactions

    decreased immunity, development or exacerbation of infections

    leukocyturia

    violation of the secretion of sex hormones (menstrual irregularities, hirsutism, impotence, delayed sexual development in children

    withdrawal syndrome

    burning, numbness, pain, paresthesias and infections, necrosis of surrounding tissues, scarring at the injection site, atrophy of the skin and subcutaneous tissue when administered intramuscularly (injection into the deltoid muscle is especially dangerous), arrhythmias, flushing of blood to the face, convulsions (with intravenous introduction), collapse (with the rapid introduction of large doses)

Contraindications

    hypersensitivity to the active substance or auxiliary components of the drug

    peptic ulcer of the stomach and duodenum

    osteoporosis

    acute viral, bacterial and systemic fungal infections (when appropriate therapy is not used)

    Cushing's syndrome

    pregnancy and lactation

    kidney failure

    cirrhosis of the liver or chronic hepatitis

    acute psychoses

    intramuscular injection is contraindicated in patients with severe disorders of hemostasis (idiopathic thrombocytopenic

    for use in ophthalmic practice: viral and fungal eye diseases

    acute form of purulent eye infection in the absence of a specific

therapy, corneal diseases associated with epithelial defects, trachoma, glaucoma

    active tuberculosis

Drug Interactions

The effectiveness of dexamethasone is reduced when taken concomitantly rifampicin, carbamazepine, phenobarbitone, phenytoin (diphenylhydantoin), primidone, ephedrine, or aminoglutethimide. Dexamethasone reduces the therapeutic effect hypoglycemic drugs, antihypertensive drugs, praziquantel and natriuretics; dexamethasone increases activity heparin, albendazole and kaliuretics. Dexamethasone may change the action coumarin anticoagulants.

Simultaneous use of dexamethasone and high doses glucocorticoids or agonists2-receptor increases the risk of developing hypokalemia. Higher arrhythmogenicity and toxicity of cardiac glycosides is noted in patients suffering from hypokalemia.

With the simultaneous use of oral contraceptives, the half-life of glucocorticoids may increase, which leads to an increase in their action and an increase in the number of side effects.

The simultaneous use of ritodrine and dexamethasone during labor is contraindicated, since this can lead to the death of the mother due to pulmonary edema.

Co-administration of dexamethasone and metoclopramide, diphenhydramine, 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 .

special instructions

Application in pediatrics

In children during long-term treatment, it is necessary to carefully monitor the dynamics of growth and development. In children during the period of growth, glucocorticosteroids should be used only for health reasons and under the most careful supervision of a physician. 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.

Children who are in contact with patients with measles, chickenpox during treatment are prescribed specific immunoglobulins.

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 subject to the possibility of adequate treatment of the underlying disease. If the patient had a history of psychosis, then treatment with glucocorticosteroids is carried out only for health reasons.

With the sudden withdrawal of the drug, especially in the case of high doses, there is a withdrawal syndrome of glucocorticosteroids: anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness. After discontinuation of the drug for several months, 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 antacids for prophylactic purposes.

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.

If the patient has intercurrent infections, a septic condition, treatment with Dexamethasone should be combined with antibiotic therapy.

If treatment with Dexamethasone is carried out for 8 weeks before and 2 weeks after active immunization (vaccination), then in this case the effect of immunization will be reduced or completely neutralized.

Patients with severe traumatic brain injury and ischemic cerebrovascular accident should be prescribed glucocorticoids with caution.

Features of influenceon the ability to drive a vehicle or potentially dangerous machinery

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.

Overdose

Symptoms: possible aggravation of side effects.

Treatment: should be canceled and symptomatic therapy prescribed. There is no specific antidote.

After the disappearance of symptoms of an overdose, the drug is resumed.

Release formand packaging

1 ml in dark glass ampoules with a white dot and a green ring for opening the ampoules. A self-adhesive label is attached to the ampoule.


Instructions for use of Dexamethasone indicate that this agent is included in the list of vital drugs and is a strong synthetic glucocorticosteroid with immunosuppressive, antitoxic and anti-inflammatory properties.

The basis of the drug is a synthetic analogue of the hormone produced by the adrenal cortex. It is this substance that allows you to regulate carbohydrate, protein, lipid and water-electrolyte metabolism in the body.

Dexamethasone injections and eye drops - description of the drug

Dexamethasone is a powerful hormonal agent, a corticosteroid (related to fluoroprednisolone), obtained synthetically. It has a wide range of therapeutic effects and exhibits the following properties:

  • anti-inflammatory;
  • antitoxic;
  • antishock;
  • immunosuppressive;
  • desensitizing.

Under the influence of the active substance, the sensitivity of β-adrenergic receptors (cell membrane proteins) to endogenous catecholamines increases.

Dexamethasone is directly involved in the regulation of metabolic processes in the body:

  1. Protein metabolism - helps to reduce the amount of globulins in plasma, while increasing protein catabolism in muscle tissue and accelerating the synthesis of albumin in the liver and kidneys.
  2. Carbohydrate metabolism - stimulates the production of insulin and contributes to the development of hyperglycemia due to the fact that it speeds up the absorption of carbohydrates from the digestive tract and activates the flow of glucose from the liver into the blood.
  3. Lipid metabolism - accelerates the synthesis of fatty acids and triglycerides, promotes the redistribution of fats, which begin to be deposited in the abdomen and shoulder girdle.
  4. Water-electrolyte metabolism - retains water and sodium in the body, slows down the absorption of calcium from the gastrointestinal tract, provokes the "washout" of calcium from the bones, reduces the mineralization of bone tissue.

The anti-inflammatory effect of the drug is achieved by reducing the permeability of small vessels, inhibiting the production of inflammatory mediators and the activity of eosinophils. Slowing down the severity of allergic reactions occurs due to a decrease in the synthesis of histamine and other biologically active substances that provoke the body's immune response.

Dexamethasone inhibits the production of certain hormones by the pituitary gland, its active substances, penetrating into cells, activate the production of ribonucleic acids and normalize the functions of the nervous system. In diseases of the respiratory tract, the drug exhibits an anti-inflammatory effect, reduces the severity of edema of the mucous membranes, reduces the viscosity of bronchial sputum, suppresses its production and facilitates breathing.

The anti-shock effect of the drug is based on its ability to increase blood pressure, the antitoxic effect is due to the acceleration of the excretion of decay products from the body.

Additionally, the drug prevents the formation of scar tissue, as it inhibits the formation of connective tissue reactions during the inflammatory process. The active substance easily penetrates the placental and blood-brain barrier, is metabolized in the liver, and excreted from the body by the kidneys.

Thus, the action of the drug is aimed at binding certain substances produced by the pituitary gland, participating in metabolic processes, affecting the central nervous system and the hematopoietic system. In fact, the action of Dexamethasone extends to the entire body.

Good to know

This is a very serious drug that, if used incorrectly, can provoke unwanted complications and systemic reactions, but in the hands of a professional it helps to cope with many diseases and significantly improve the general condition of the patient.

Dexamethasone release forms

The drug is produced in the following dosage forms:

  • Dexamethasone tablets (0.5 mg);
  • Dexamethasone in ampoules 4mg/ml (solution for intravenous and intramuscular injections);
  • Oftan - eye drops Dexamethasone (0.1%);
  • Ophthalmic suspension Dexamethasone (0.1%).

Each form of the drug has its own indications for use and features of use, which the doctor must take into account when prescribing.

Why is Dexamethasone prescribed?

The oral form of the drug (tablets) is used in the following conditions:

  • endocrine diseases (hypothyroidism, thyroiditis, progression of ophthalmopathy associated with thyrotoxicosis);
  • autoimmune pathologies (hemolytic anemia, hematopoietic disorders, serum sickness);
  • insufficiency of the adrenal cortex (acute, primary, secondary), hyperplasia of the adrenal cortex (congenital);
  • nonspecific ulcerative colitis (NUC);
  • exacerbation of rheumatoid arthritis;
  • skin diseases (acute eczema, erythroderma, pemphigus);
  • connective tissue diseases;
  • cerebral edema;
  • malignant tumors.

Dexamethasone injections are prescribed in the treatment of the following diseases:

  • severe infections (in combination with antibacterial agents);
  • shock states of various origins;
  • cerebral edema (due to traumatic brain injury, tumor, hemorrhage, radiation exposure, encephalitis or meningitis);
  • dangerous allergic reactions (angioedema, bronchospasm, anaphylactic and pyrogenic reactions);
  • joint diseases;
  • sharp croup;
  • exacerbation of bronchial asthma, obstructive bronchitis, accompanied by bronchospasm;
  • acute dermatoses in severe form;
  • blood diseases (hemolytic anemia, agranulocytosis, acute lymphoblastic leukemia, thrombocytopenia);
  • insufficiency of the adrenal cortex in acute form;
  • oncological diseases (lymphoma and leukemia, acute leukemia in children).

Dexamethasone eye drops and injections of this drug in ophthalmic practice are used for a wide range of pathological conditions (allergic conjunctivitis, keratoconjunctivitis, keratitis, iritis, iridocyclitis, blepharitis, etc.), are prescribed to eliminate the inflammatory process after surgical interventions and eye injuries, and are also used in as immunosuppressive therapy after corneal transplantation.

In addition, the drug in drops is instilled into the ear canal for allergic and inflammatory lesions of the ear.

Instructions for use

When taking Dexametosan tablets orally, the dosage and treatment regimen is selected by the doctor individually, taking into account the type of disease, the severity of the symptoms, the general condition of the patient and possible contraindications. In severe cases of the disease, at the initial stage of therapy, from 1 to 9 mg of the drug per day is prescribed, followed by a decrease in the daily dose to 0.5-3 mg at the stage of maintenance treatment.

The maximum dose of Dexamethasone should not exceed 15 mg/day. The daily dose of the drug is divided into three doses, it is best to take the medicine with meals. The duration of the course of treatment largely depends on the nature of the pathological process, the severity of the symptoms and how the sick person tolerates the drug. In some, especially severe cases, the duration of therapy with Dexamethasone can reach several months.

Dexamethasone intramuscularly and intravenously is prescribed for emergency conditions, as well as in situations where taking the drug in tablets is not possible. The solution for injection is also used for intraarticular and periarticular (periarticular) administration. In a vein, the drug is administered slowly (stream or drip).

According to the instructions, the drug can be administered up to four times a day, at a dose of 4 to 20 mg. When preparing a solution for a dropper, an isotonic solution of sodium chloride is used.

How much can I inject Dexamethasone? The duration of injections is usually no more than 4 days, after which they switch to taking the drug in tablet form. The peculiarity of therapy is that when acute conditions are relieved, Dexamethasone is used in higher doses, then, as it improves, the dosage is gradually reduced to maintenance, or the drug is completely canceled.

In ophthalmic practice, Dexamethasone eye drops for the relief of acute conditions are instilled into the conjunctival sac every 2 hours (1-2 drops each). Then, as the inflammatory process subsides, the interval between procedures is increased to 4-6 hours. The duration of treatment depends on the clinical picture of the disease and can last from 2 days to several weeks.

Dexamethasone in ampoules can be used for inhalation in acute inflammatory lesions of the upper respiratory tract (bronchitis, laryngitis). To do this, the drug should be diluted in saline in a ratio of 1:6 and the ready-made solution (in a volume of 4 ml) should be used for inhalation.

Dexamethasone for children

Is it possible to use Dexamethasone for children and how to use the drug correctly in the treatment of young patients? The optimal dosage of tablets should be selected by the attending physician, taking into account the severity of the underlying disease, the individual characteristics of the child, his age and weight. The standard daily dosage is from 2.5 to 10 mg, which is divided into several doses.

Inhalations with Dexamethasone for children are made at the rate of 0.5 ml of the drug per 3 ml of saline. Treatment usually lasts 7 days, the procedure is done three times a day.

During pregnancy

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

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

Contraindications

With short-term use of the drug for vital signs, the only limitation is the individual intolerance to dexamethasone or other components of the drug. In children, a hormonal agent should be used only according to indications and under the supervision of the attending physician.

Contraindications to the appointment of Dexamethasone injections are the following conditions:

Intra-articular injections are prohibited in case of instability of the joints, the presence of foci of infection in the joints and periarticular tissues, manifestations of osteoporosis, bleeding, previous arthroplasty.

In ophthalmology, Dexamethasone in the form of drops cannot be used for glaucoma, trachoma, corneal damage, viral, fungal or tuberculous eye damage. It is forbidden to instill the drug into the ear canal if the eardrum is damaged.

For the entire period of use of Dexamethasone, it is necessary to stop taking alcohol, since the combination of a hormonal agent with ethanol can provoke dangerous unpredictable consequences.

Adverse reactions

Dexamethasone is well tolerated by patients, but, like many hormonal agents, it can cause systemic adverse reactions. Their severity and frequency largely depend on the dosage and duration of the drug. In medical practice, the following side effects from the use of Dexamethasone are described:

From the side of the cardiovascular system - arrhythmias, slowing of the heartbeat (bradycardia), up to cardiac arrest, development or exacerbation of heart failure, increased blood pressure. In patients with myocardial infarction (acute and subacute), foci of necrosis may spread, which can lead to rupture of the heart muscle.

From the gastrointestinal tract - a violation of appetite and digestive processes, nausea, vomiting, flatulence, symptoms of pancreatitis, the formation of ulcers in the stomach and duodenum, perforation of the digestive system and internal bleeding.

Endocrine system - exacerbation of diabetes mellitus, increased pressure, obesity of the pituitary type, inhibition of the functions of the adrenal cortex, muscle weakness, painful menstruation, delayed sexual development in adolescents. Often there is a violation of metabolic processes, sodium fluid retention, leading to peripheral edema, weight gain, increased weakness and fatigue.

Nervous system - increased intracranial pressure, increased nervousness, anxiety in combination with headaches and dizziness, disorientation in space, depression, insomnia. In severe cases, convulsions, hallucinations, manifestations of paranoia or manic-depressive psychosis are possible.

Musculoskeletal system - growth retardation in children, osteoporosis leading to pathological bone fractures, tendon rupture, muscle atrophy.

On the part of the skin, there is a slow healing of wounds, the appearance of striae, acne, hyperpigmentation, thinning of the skin. Allergic reactions are possible, accompanied by skin itching, rashes, in rare cases, such a severe reaction as anaphylactic shock occurs.

Local reactions include a burning sensation and pain in the injection area, redness of the skin. Sometimes at the injection site, scarring, necrosis of surrounding tissues, and subcutaneous tissue atrophy are noted.

Analogues

Dexamethasone has quite a few structural analogues containing the same active ingredient. These include:

  • Dexaven;
  • Dexazon;
  • Dexamed;
  • Dexafar;
  • Dexamethasone - Nycomed;
  • Dexamethasone-Ferein;
  • Fortecortin etc.

Price

Dexamethasone is available without a doctor's prescription. Average prices for the drug in the pharmacy chain:

  • Dexamethasone tablets 0.5 mg (10 pcs) - from 38 rubles;
  • Dexamethasone solution in ampoules 4 mg / ml (25 ampoules) - from 180 rubles;
  • Dexamethasone eye drops - from 80 rubles.

Dexamethasone is inexpensive, but this does not mean that you need to self-medicate. It should be understood that this is a strong hormonal remedy with many side effects, which can only be used as directed and under the supervision of a doctor.