Dexamethasone injections - when they are needed, indications and precautions for injections. Dexamethasone - what is it prescribed for

Dexamethasone is a drug belonging to the group of glucocorticosteroids and is hormonal agent. It is widely used in medicine, in its various fields. It is produced in the form of a solution, which is used for injection intravenously, intramuscularly and for instillation into the conjunctiva of the eyes. When Dexamethasone is needed, why these injections are prescribed and how they act on the body - this issue needs to be sorted out in as much detail as possible.

Preparations of this group are used according to the indications and as prescribed by the doctor. Otherwise, you can cause irreparable harm to the body.

Composition, action

Dexamethasone is hormonal drug.

Dexamethasone is a homologue of hydrocortisone, a hormone produced by the adrenal cortex. It interacts with glucocorticoid receptors, regulates the exchange of sodium, potassium, water balance and glucose homeostasis. Stimulates the production of enzyme proteins in the liver, acts on the synthesis of mediators of inflammation and allergies, inhibits their formation. As a result, the agent gives an anti-inflammatory, anti-allergic, immunosuppressive, anti-shock effect.

When administered intramuscularly therapeutic effect observed after 8 hours, after intravenous infusion faster. The effect persists from 3 days to 3 weeks when administered locally, 17-28 days after intravenous administration.

Dexamethasone has a strong anti-inflammatory and anti-allergic effect. It is 35 times more effective than cortisone.

Each 1 ml ampoule contains 4 mg of dexamethasone and additional components - disodium edetate, glycerin, buffered phosphate solution, purified water.

Indications

The drug is indicated for systemic treatment diseases in which local therapy or oral medications are ineffective or impossible. This tool is used as an independent tool or in combination with others.


Glucocorticosteroids are prescribed for diseases of the joints and muscles.

The list of indications for this drug is very wide. As for diseases of the joints and muscles, it is indicated for such diagnoses:

  • and juvenile arthritis s;
  • tendovaginitis;
  • bursitis;
  • osteochondrosis;
  • osteoarthritis;
  • synovitis;

The remedy is prescribed in cases of development of shock - post-traumatic, anaphylactic, and also arising from surgical interventions Oh.

Important! To relieve inflammation of the joints, Dexamethasone solution in some cases is injected directly into the joint bag.

Contraindications

The main prohibition for the use of this drug is hypersensitivity to the substance.

Do not prescribe intra-articular injections in such cases:

  • joint instability;
  • recent arthroplasty;
  • pathological bleeding(including those provoked by taking anticoagulants);
  • bone fractures affecting the joint;
  • periarticular osteoporosis;
  • infection in the joint capsule or adjacent tissues.

Intramuscular and intravenous injections have the following contraindications:

  • active tuberculosis;
  • liver disease (cirrhosis, hepatitis);
  • thrombocytopenic purpura;
  • acute infectious diseases caused by viruses, bacteria, fungi;
  • acute psychosis.

Dosage

Inside the vein and muscle, the drug is administered with a syringe or by drip with glucose or saline. Moreover, mixing these substances in the same vial or syringe that will be used for infusion is impossible.

At the beginning of treatment, a dose of 0.5 to 9 mg of Dexamethasone is established. Within 24 hours, from 4 to 20 mg of the substance is administered 3-4 times. The duration of the course of droppers or injections with this drug is 3-4 days. After the patient is transferred to the same medicine in the form of tablets.

For injection directly into the joint, the recommended dose varies from 0.4 to 4 mg of the substance at a time. You can inject again after 12 to 16 weeks. In total, no more than four such procedures are allowed per year for each joint. Simultaneous infusion into two joints is permitted.

Important! The use of the drug intra-articular more than 34 times a year can lead to the destruction of cartilage.

The dosage for each joint is calculated individually and depends on the degree of the disease. For large joints single dose varies from 2 to 4 mg at a time, for small ones - from 0.8 to 1 mg.

For injection into the affected area, the dosage does not differ from the amount for infusion into the joint, and for the tissues surrounding the joint, it is possible to use from 2 to 6 mg at a time.

Overdose

Excessive administration of the drug can cause an overdose, which is manifested by an increase in 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

Due to the property of the drug to retain water, sodium, excrete potassium and calcium, edema may occur.


Dexamethasone may cause side effects various organs and body systems.

In addition, the following events are likely:

Rarely seen allergic manifestations- itching, rash on the skin.

Dexamethasone during pregnancy

Treatment with this drug during the period of gestation is prescribed only for vital indications when the benefits to the woman far outweigh the risks to the fetus. Corticosteroids are able to cross the placenta, so newborns whose mothers underwent such therapy should be carefully monitored.

Corticosteroids are also secreted from breast milk and may suppress the production natural hormones in a newborn, which leads to negative consequences. Therefore, for the period of treatment with Dexamethasone, breastfeeding is stopped.

special instructions


Treatment with Dexamethasone requires compliance with certain rules.

At the time of treatment with this drug is required complete failure from the use of alcohol, it is forbidden to conduct preventive vaccinations patient. Preventive measures should be observed if there has been contact with a patient with a viral or infectious disease - SARS, measles, chicken pox.

Termination of therapy is carried out gradually. Abrupt rejection from the drug can cause a withdrawal syndrome, which is manifested by an increase in body temperature, muscle pain, arthralgia, general deterioration.

If treatment with this remedy is necessary for a child, then the dose is calculated based on the surface area of ​​\u200b\u200bhis body. A long course of such treatment requires observation and analysis of the dynamics of growth, development of children, control of hormones and blood glucose levels.

Analogues

If it is necessary to replace Dexamethasone, then drugs are prescribed either containing the same active substance or similar in effect.

Dexamethasone is found in:

  • Dexazon;
  • Dexamed;
  • Dexaven.

Important! In action with this drug, other drugs from the GCS group are similar, but only a doctor should select them, since the active substances are different.

Price

The cost of the drug in ampoules for injection is different. For 25 ampoules of 1 ml with 4 mg active substance you need to pay from 210 rubles. The price may vary depending on the manufacturer of the drug and the place of its sale.

Round tablets white or almost white color with a flat surface, with a risk on one side and a chamfer.

Pharmacotherapeutic group

Corticosteroids for systemic use. Glucocorticosteroids. Dexamethasone.

ATX code H02AB02

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Pharmacological properties

Pharmacokinetics

Dexamethasone is rapidly and almost completely absorbed by oral administration. The bioavailability of dexamethasone is 80%. After oral intake Cmax in blood plasma was noted after 1-2 hours; after a single dose, the effect lasts approximately 66 hours.

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

Replacement therapy for primary and secondary (pituitary) adrenal insufficiency

Congenital adrenal hyperplasia

Subacute thyroiditis and severe forms 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 medicines and food products

serum sickness, drug exanthema

Hives, 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

Ulcerative colitis, Crohn's disease, localized enteritis

Sarcoidosis (symptomatic)

Acute toxic bronchiolitis, Chronical bronchitis, bronchial 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 diseases of autoimmune origin (incl. 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

Dosage and administration

With long-term oral administration of high doses of dexamethasone, the drug is recommended to be taken with meals, and antacids should be taken between meals. During the day, it is recommended to use taking into account daily fluctuations in endogenous secretion of glucocorticoids in the range from 6 to 8 am.

Adults

The recommended starting dose for adults is 0.5 mg to 9 mg per day. Maximum daily dose- 10-15 mg. The daily dose can be divided into 2-4 doses. The usual maintenance dose is 0.5 mg to 3 mg per day.

The initial dose of dexamethasone should be used until a therapeutic effect is achieved, then it is gradually reduced (usually by 0.5 mg in 3 days) to a maintenance dose of 2 - 4.5 or more mg / day. If high-dose therapy continues for more than a few days, the dose of the drug is gradually reduced over the next few days or over a longer period. Minimum effective dose- 0.5-1 mg / day. Doses are set individually for each patient, depending on the nature of the disease, the expected duration of treatment, the tolerability of the drug and the patient's response to therapy. The duration of Dexamethasone use ranges from 5-7 days to several 2-3 months or more. Treatment is stopped gradually.

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Side effects

Decreased glucose tolerance, "steroid" diabetes or manifestation of the latent diabetes

Itsenko-Cushing syndrome, weight gain

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

- "steroid" gastric ulcer and duodenum, erosive esophagitis, bleeding and perforation gastrointestinal tract

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

Hypercoagulability, 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 parenteral administration possible deposition of crystals of the drug in the vessels of the eye), posterior subcapsular cataract, increased intraocular pressure With possible damage optic nerve, trophic changes in the cornea, exophthalmos, development of secondary bacterial, fungal or viral infections eye

Negative nitrogen balance (increased protein breakdown), hyperlipoproteinemia

Increased sweating

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

Deceleration of growth 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, tendency to develop pyoderma and candidiasis

Petechiae, ecchymosis, skin thinning, hyper- or hypopigmentation, steroid acne, striae

generalized and local allergic reactions

Reduced immunity, development or exacerbation of infections

Leukocyturia

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

Syndrome "cancellation"

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

heavy arterial hypertension

Severe renal failure

Obesity III - IV degree

Active form of tuberculosis

Acute psychoses

Pregnancy and lactation

Cirrhosis of the liver or chronic hepatitis

Children's age up to 6 years

Drug Interactions

Simultaneous use of Dexamethasone and painkillers (non-steroidal anti-inflammatory drugs), antihypertensives, antidiabetic drugs, antiepileptic drugs, diuretics, anticoagulants, anti-asthma aerosols or ritodrine may increase or decrease its effect and / or cause unwanted action. Therefore, these drugs should not be used simultaneously.

During the period of treatment with Dexamethasone, you should refrain from alcoholic beverages.

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special instructions

With diabetes mellitus, tuberculosis, bacterial and amoebic dysentery, arterial hypertension, thromboembolism, cardiac and kidney failure, non-specific ulcerative colitis, diverticulitis, recently formed intestinal anastomosis, Dexamethasone should be used very carefully and if possible adequate treatment 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 with preventive purpose antacids.

GKS. Suppresses the functions of leukocytes and tissue macrophages.

A drug: DEXAMETHASONE (DEXAMETHASONE)

Active ingredient: dexamethasone
ATX code: H02AB02
KFG: GCS for injections
ICD-10 codes (indications): D59, D69.3, D70, E06, E25, E27.1, E27.2, E27.4, G93.6, H01.0, H10, H10.1, H10.5, H15.0, H15.1, H16, H16.2, H20.0, H20.1, H30, H44.1, J44, J45, J46, L20.8, L21, L40, L50, L51.1, L51.2, L91.0, L93. 0, M05, M07, M08, M30, M31, M32, M33, M34, M35, R57, R57.0, R57.8, T78.2, T78.3, T79.4, Z51.5
Reg. number: P N014442/01-2002
Date of registration: 18.11.08
The owner of the reg. acc.: SHREYA LIFE SCIENCES (India)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Injection transparent, colorless or pale yellow.

Excipients: methylparaben, propylparaben, sodium metabisulphite, disodium edetate, sodium hydroxide, water for injection.

2 ml - dark glass ampoules (25) - cardboard boxes.

2 ml - dark glass bottles (25) - cardboard boxes.

INSTRUCTIONS FOR USE FOR THE SPECIALIST.
The description of the drug was approved by the manufacturer in 2009.

PHARMACHOLOGIC EFFECT

Synthetic glucocorticoid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, anti-allergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.

Interacts with specific cytoplasmic receptors (there are receptors for corticosteroids in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells.)

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

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

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increased intake of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); contributes to the development of hyperglycemia.

Water-electrolyte metabolism: retains Na + and water in the body, stimulates the excretion of K + (mineralocorticoid activity), reduces the absorption of Ca + from the gastrointestinal tract, reduces the mineralization of bone tissue.

The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; inducing the formation of lipocortins and reducing the amount mast cells that produce hyaluronic acid; with a decrease in capillary permeability; stabilization cell membranes(especially lysosomal) and organelle membranes. It acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, which contribute to inflammation, allergies, etc.), the synthesis of "pro-inflammatory cytokines" ( interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

The immunosuppressive effect is due to the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T-lymphocytes), suppression of B-cell migration and the interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; interferon gamma) from lymphocytes and macrophages and decreased antibody production.

The antiallergic effect develops as a result of a decrease in the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils. active substances, reducing the number of circulating basophils, T- and B-lymphocytes, mast cells; suppression of the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to allergy mediators, inhibition of antibody formation, changes in the body's immune response.

For obstructive diseases respiratory tract the action is mainly due to the inhibition of inflammatory processes, the prevention or decrease in the severity of edema of the mucous membranes, the decrease in eosinophilic infiltration of the submucosal layer of the bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.

Suppresses the synthesis and secretion of ACTH and secondarily - the synthesis of endogenous corticosteroids.

It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

The peculiarity of the action is a significant inhibition of the function of the pituitary gland and practically complete absence mineralocorticosteroid activity.

Doses of 1-1.5 mg/day inhibit the function of the adrenal cortex; the biological half-life is 32-72 hours (the duration of the inhibition of the hypothalamus-pituitary-adrenal cortex system).

According to the strength of glucocorticoid activity, 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisolone), 15 mg of hydrocortisone, or 17.5 mg of cortisone.

PHARMACOKINETICS

Dexamethasone in the blood binds (60-70%) to a specific carrier protein - transcortin. Easily passes through histohematic barriers(including through the blood-brain and placental).

Metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites.

It is excreted by the kidneys (a small part - lactating glands). T 1/2 dexamethasone from plasma - 3-5 hours.

INDICATIONS

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

Endocrine diseases: acute insufficiency of the adrenal cortex, primary or secondary insufficiency of the adrenal cortex, congenital hyperplasia of the adrenal cortex, subacute thyroiditis;

Shock (burn, traumatic, surgical, toxic) - with inefficiency vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;

Cerebral edema (with a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury);

Asthmatic status; severe bronchospasm (exacerbation of bronchial asthma, chronic obstructive bronchitis);

severe allergic reactions, anaphylactic shock;

Rheumatic diseases;

Systemic connective tissue diseases;

Acute severe dermatoses;

Malignant diseases: palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; hypercalcemia in patients with malignant tumors, when oral treatment is not possible;

Blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;

Severe infectious diseases (in combination with antibiotics);

In ophthalmic practice (subconjunctival, retrobulbar or parabulbar administration): allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammation after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after corneal transplantation;

Local application (in the area of ​​pathological formation): keloids, discoid lupus erythematosus, granuloma annulare.

DOSING MODE

The dosage regimen is individual and depends on the indications, the patient's condition and his response to therapy. The drug is administered intravenously in a slow stream or drip (for acute and emergency conditions); i / m; possibly also local (in pathological formation) introduction. In order to prepare a solution for intravenous drip infusion, use isotonic solution sodium chloride or 5% dextrose solution.

AT acute period at various diseases and at the beginning of therapy Dexamethasone is used in higher doses. During the day, you can enter from 4 to 20 mg of Dexamethasone 3-4 times.

Doses of the drug Dexamethasone for children(w / m):

The dose of the drug during replacement therapy(with insufficiency of the adrenal cortex) is 0.0233 mg / kg of body weight or 0.67 mg / m 2 of body surface area, divided into 3 doses, every 3rd day or 0.00776 - 0.01165 mg / kg of body weight or 0.233 - 0.335 mg / m 2 body surface area daily. For other indications, the recommended dose is 0.02776 to 0.16665 mg/kg body weight or 0.833 to 5 mg/m2 body surface area every 12-24 hours.

When the effect is achieved, the dose is reduced to maintenance or until treatment is stopped. The duration of parenteral use is usually 3-4 days, then they switch to maintenance therapy with dexamethasone tablets.

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

SIDE EFFECTS of Dexamethasone

Dexamethasone is generally 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:

From the side endocrine systems s: reduced glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, adrenal suppression, Itsenko-Cushing syndrome (moon face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delayed sexual development in children.

From the side digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal tract wall, increased or decreased appetite, indigestion, flatulence, hiccups. AT rare cases- increased activity of hepatic transaminases and alkaline phosphatase.

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 myocardial infarction - the spread of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.

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

From the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, sudden loss vision (with parenteral administration in the head, neck, turbinates, scalp, crystals of the drug may be deposited in the vessels of the eye).

From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticoid activity- fluid and sodium retention (peripheral edema), hypnatremia, hypokalemia syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: 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, steroid myopathy, decreased muscle mass(atrophy).

From the 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.

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

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; skin atrophy and subcutaneous tissue with i / m administration (especially dangerous is the introduction into the deltoid muscle).

Others: 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.

CONTRAINDICATIONS DEXAMETHASONE

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

In children during the period of growth, GCS should be used only according to absolute readings and under the close supervision of the attending physician.

FROM caution the drug should be prescribed for the following diseases and states:

Diseases of the gastrointestinal tract - peptic ulcer stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis;

Pre- and post-vaccination period(8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;

Immunodeficiency states (including AIDS or HIV infection);

Diseases of the cardiovascular system (including recent myocardial infarction - in patients with acute and subacute myocardial infarction, the focus of necrosis may spread, slowing down the formation of scar tissue and, as a result, rupture of the heart muscle), severe chronic heart failure, arterial hypertension, hyperlipidemia);

Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, obesity (III-IV stage)

Severe chronic renal and/or liver failure, nephrourolithiasis;

Hypoalbuminemia and conditions predisposing to its occurrence;

Systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (with the exception of the form of bulbar encephalitis), open and angle-closure glaucoma;

Pregnancy.

PREGNANCY AND LACTATION

During pregnancy (especially in the first trimester), the drug can be used only when the expected healing effect exceeds potential risk for the fetus. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In the case of use at the end of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

If it is necessary to carry out drug treatment during breastfeeding then breastfeeding should be discontinued.

SPECIAL INSTRUCTIONS

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.

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). The food must be rich in proteins, vitamins, with limited content of fats, carbohydrates and salt.

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.

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.

In stressful situations during maintenance treatment (for example, surgical operations, 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.

With sudden withdrawal, 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, 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.

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

Due to the weak mineralocorticoid effect for replacement therapy in adrenal insufficiency, Dexamethasone is used in combination with mineralocorticoids.

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 (spine, hand) is shown.

Patients with latent infectious diseases of the kidneys and urinary tract Dexamethasone can cause leukocyturia, which may have diagnostic value.

Dexamethasone increases the content of metabolites of 11- and 17-hydroxyketocorticosteroids.

OVERDOSE

It is possible to increase the side effects described above.

It is necessary to reduce the dose of Dexamethasone. Treatment is symptomatic.

DRUG INTERACTIONS

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(phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;

- diuretics(especially thiazides and carbonic anhydrase inhibitors) and amphotericin B may lead to increased excretion of K + from the body and an increase in the risk of developing heart failure;

- with sodium preparations- 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- increased risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding (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);

- 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 (with the abolition of dexamethasone, the level of salicylates in the blood increases and the risk of side effects increases);

- insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness decreases;

- vitamin D - its effect on the absorption of Ca 2+ in the intestine decreases;

- somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration;

- M-anticholinergics(including antihistamines and tricyclic antidepressants) and nitrates - promotes an 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.

Indomethacin, displacing dexamethasone from its association with albumin, increases the risk of its development. side effects.

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.

Concomitant administration of androgens and steroids anabolic drugs with dexamethasone promotes the development of peripheral edema and hirsutism, 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.

TERMS AND CONDITIONS OF DISCOUNT FROM PHARMACIES

The drug is dispensed by prescription.

Price - 107 rubles BUY

TERMS AND CONDITIONS OF STORAGE

List B. Store at a temperature not exceeding 25 ° C, out of the reach of children. Do not freeze. Shelf life - 3 years. Do not use after the expiry date stated on the packaging.

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

Once in the cytoplasm, it interacts with its receptors, resulting in the formation of a complex that, penetrating into the cell nucleus, enhances the synthesis of messenger RNA. Available in the form of tablets and injection solutions. Belongs to the category of life necessary funds, dispensed by prescription.

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

Application of the drug

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

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

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

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

Dexamethasone during pregnancy

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

Mode of application

Dexamethasone is used according to an individually drawn up plan. It is taken orally (tablets), by injection, conjunctival.

  • Tablets for adults. Taken after or during meals, from 2-3 to 10-15 mg per day (depending on the doctor's instructions).
  • Tablets for children. 3-4 times a day, depending on the body weight of the child.
  • Injections for adults. For emergency assistance- from 4 to 20 mg, up to 4 times a day. In case of shock, a loading dose of 20 mg is used, then 3 mg per 1 kg of body weight during the day.
  • Injections for children. Calculated based on body weight.
  • At ophthalmic diseases- up to 2 drops every hour, after - every 5-6 hours (if the condition is acute). In other cases - up to 2 drops 3 times a day. The course is usually a couple of weeks.

Contraindications

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

Side effects and overdose

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

Catad_pgroup Systemic corticosteroids

Catad_pgroup Preparations for ophthalmology

Dexamethasone tablets - official instruction by application

INSTRUCTIONS for medical use drug

Registration number:

Tradename:

Dexamethasone

International non-proprietary name:

Dexamethasone

Dosage form:

tablets

Composition per tablet.

Active substance:
Dexamethasone -0.0005 g

Excipients:
- to obtain a tablet weighing 0.15 g
potato starch -0.0340 g
sucrose (sugar) -0.1140 g
ancient acid -0.0015 g

Description

Tablets are white, ploskotsilindricheskie with a chamfer.

Pharmacological group:

glucocorticosteroid.

ATC Code:

H02AB02

Pharmacological properties

Pharmacodynamics
Dexamethasone is a synthetic glucocorticosteroid (GCS), a methylated derivative of fluoroprednisolone. It has anti-inflammatory, anti-allergic, desensitizing, immunosuppressive, anti-shock and anti-toxic effects.

It inhibits the secretion of thyroid-stimulating hormone and follicle-stimulating hormone.

Increases the excitability of the central nervous system, reduces the number of lymphocytes and eosinophils, increases the number of red blood cells (stimulates the production of erythropoietins).

Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus, stimulates the synthesis of matrix ribonucleic acid (mRNA); 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 synthesis of endoperoxides, prostaglandins, leukotrienes. contributing to the processes of inflammation, allergies and others.

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

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

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase, which leads to an increase in the flow of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases, leading to the activation of gluconeogenesis.

Water-electrolyte exchange; retains sodium ions and water in the body, stimulates the excretion of potassium ions (mineralocorticosteroid activity), reduces the absorption of calcium ions from the gastrointestinal tract, "washes out" calcium ions from the bones, increases the excretion of calcium ions by the kidneys.

The anti-inflammatory effect is 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; stabilization of cell membranes and organelle membranes (especially lysosomal ones).

The antiallergic effect develops as a result of suppression of the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, and a decrease in the number of circulating basophils. suppression of the development of lymphoid and connective tissue, a decrease in the number of T- and B-lymphocytes, mast cells, a decrease in the sensitivity of effector cells to allergy mediators, inhibition of antibody production, changes in the body's immune response.

In chronic obstructive pulmonary disease, the action is mainly based on inhibition of inflammatory processes, inhibition of development or prevention of edema of the mucous membranes, inhibition of eosinophilic infiltration of the submucosal layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, and inhibition of erosion and desquamation of the mucous membrane. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.

The anti-shock and anti-toxic effect is associated with an increase in blood pressure (due to an increase in the concentration of circulating catecholamines and the restoration of adrenoreceptor sensitivity to them, as well as vasoconstriction), a decrease in the permeability of the vascular wall, membrane-protective properties, and activation of liver enzymes involved in the metabolism of endo- and xenobiotics.

The immunosuppressive effect is due to inhibition of the release of cytokines (interleukin-1, interleukin-2; interferon gamma) from lymphocytes and macrophages.

Suppresses the synthesis and secretion of adrenocorticotropic hormone (ACTH). and secondarily - the synthesis of endogenous glucocorticosteroids.

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

The strength of glucocorticoid activity of 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisolone, 15 mg of hydrocortisone or 17.5 mg of cortisone for oral dosage forms.

Pharmacokinetics
After oral administration, it is rapidly and completely absorbed, the maximum concentration of dexamethasone in blood plasma is 1-2 hours. In the blood, it binds (60-70%) to a specific carrier protein - transcortin. Easily passes through histohematic barriers (including through the blood-brain and placental barriers). Metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. It is excreted by the kidneys (a small part - lactating glands). The half-life is 3-5 hours.

Indications for use:

Systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis).

Acute and chronic inflammatory diseases of the joints: gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, humeroscapular periarthritis, ankylosing spondylitis (Bechterew's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tendosynovitis, synovitis and epicondylitis.

Rheumatic fever, acute rheumatic fever.

Acute and chronic allergic diseases: allergic reactions to drugs and food, serum sickness, urticaria, allergic rhinitis, angioedema, drug exanthema, hay fever.

Skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis, diffuse neurodermatitis. contact dermatitis (with damage to a large surface of the skin), toxidermia, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous dermatitis herpetiformis, malignant exudative erythema (Stevens-Johnson Syndrome).

Cerebral edema (including against the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma) after prior parenteral administration.

Allergic eye diseases: allergic corneal ulcers, allergic forms 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 diseases of autoimmune origin (including acute glomerulonephritis): nephrotic syndrome.

Subacute thyroiditis.

Diseases of the hematopoietic organs - agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, acute lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia.

Lung diseases: acute alveolitis. pulmonary fibrosis, stage II-III sarcoidosis. Bronchial asthma (with bronchial asthma the drug is prescribed only for severe course, ineffectiveness or inability to take inhaled glucocorticosteroids).

Tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy).

Beryllium, Loeffler's syndrome (not amenable to other therapy).

Lung cancer (in combination with cytostatics).

Multiple sclerosis.

Diseases of the gastrointestinal tract: ulcerative colitis, Crohn's disease, local enteritis.

Prevention of graft rejection as part of complex therapy.

Hypercalcemia in the background oncological diseases, nausea and vomiting during cytostatic therapy.

Myeloma.

Conducting a test at differential diagnosis hyperplasia (hyperfunction) and tumors of the adrenal cortex.

Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency states (including acquired immunodeficiency syndrome or human immunodeficiency virus (HIV infection).

Diseases of the gastrointestinal tract: peptic ulcer of the stomach and 12 duodenal ulcer. esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis

Diseases of the cardiovascular system, incl. recent myocardial infarction (in patients with acute and subacute myocardial infarction, the focus of necrosis may spread, slowing down the formation of scar tissue and, as a result, rupture of the heart muscle), decompensated chronic heart failure, arterial hypertension, hyperlipidemia.

Endocrine diseases - diabetes mellitus (including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease. obesity (1II-1V stage).

Severe chronic renal and / or liver failure, nephrourolithiasis.

Hypoalbuminemia and conditions predisposing to its occurrence.

Systemic osteoporosis, myasthenia gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open- and closed-angle glaucoma, lactation period.

Use during pregnancy and during breastfeeding

During pregnancy, the drug is used only in cases where the potential benefit to the mother outweighs the potential risk to the fetus. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In case of application in III trimester pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn. If it is necessary to carry out treatment with the drug during breastfeeding, then breastfeeding should be discontinued.

Dosage and administration:

Inside, in individually selected doses, the value of which is determined by the type of disease. the degree of its activity and the nature of the patient's response.

The average daily dose is 0.75-9 mg. AT severe cases may also apply large doses divided into 3-4 doses. The maximum daily dose is usually 15 mg. After achieving a therapeutic effect, the dose is gradually reduced (usually by 0.5 mg in 3 days) to a maintenance dose of 2-4.5 mg / day. The minimum effective dose is 0.5-1 mg / day.

Children (depending on age) are prescribed 83.3-333.3 mcg / kg or 2.5-10 mg / sq. m / day in 3-4 doses.

The duration of dexamethasone use depends on the nature of the pathological process and the effectiveness of treatment and ranges from several days to several months or more. Treatment is stopped gradually (at the end, several injections of corticotropin are prescribed).

With bronchial asthma, rheumatoid arthritis, ulcerative colitis - 1.5-3 mg / day; with systemic lupus erythematosus - 2-4.5 mg / day; with oncohematological diseases - 7.5-10 mg.

For the treatment of acute allergic diseases it is advisable to combine parenteral and oral administration: 1 day - 4-8 mg parenterally; Day 2 - inside. 4 mg 3 times a day; 3, 4 day - inside. 4 mg 2 times a day; 5. Day 6 - 4 mg / day. inside; Day 7 - drug withdrawal.

Dexamethasone test (Liddle test). It is carried out in the form of small and large tests. With a small test, dexamethasone is given to the patient at 0.5 mg every 6 hours during the day (i.e. at 8 am, at 2 20 pm and 2 am). Urine for the determination of 17-hydroxycorticosteroids or free cortisol is collected from 8 am to 8 am 2 days before the appointment of dexamethasone and also 2 days at the same time intervals after taking the indicated doses of dexamethasone. These doses of dexamethasone inhibit the formation of corticosteroids in almost all apparently healthy individuals. 6 hours after the last dose of dexamethasone, plasma cortisol levels are below 135-138 nmol/l (less than 4.5-5 µg/100 ml). Reducing the excretion of 17-hydroxycorticosteroids below 3 mg / day. and free cortisol below 54-55 nmol / day (below 19-20 mcg / day) excludes hyperfunction of the adrenal cortex. At persons. suffering from Itsenko-Cushing's disease or syndrome, no changes in corticosteroid secretion are noted during a small test.

When conducting a large test, dexamethasone is prescribed 2 mg every 6 hours for 2 days (i.e. 8 mg dexamethasone per day). Urine is also collected to determine 17-hydroxycorticosteroids or free cortisol (if necessary, determine free cortisol in plasma). With Itsenko-Cushing's disease, there is a decrease in the excretion of 17-hydroxycorticosteroids or free cortisol by 50% or more, while with tumors of the adrenal glands or adrenocorticotropic-ectopic (or corticoliberin-ectopic) syndrome, the excretion of corticosteroids does not change. In some patients with adrenocorticotropic-ectopic syndrome, a decrease in the excretion of corticosteroids is not detected even after taking dexamethasone at a dose of 32 mg / day.

Side effect

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 compliance. circadian rhythm destination. Dexamethasone is generally 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:

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

From the digestive system: nausea, vomiting, pancreatitis, "steroid" gastric and duodenal ulcer, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases, an increase in the activity of "liver" transaminases and alkaline phosphatase .

From the side of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, electrocardiographic changes characteristic of hypokalemia, increased blood pressure, hypercoagulability, 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.

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

From the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos.

From the side of metabolism: increased excretion of calcium ions, hypocalcemia. weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

Caused by mineralocorticosteroid activity- retention of fluid and sodium ions (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the musculoskeletal system: growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely - pathological fractures bones, aseptic necrosis of the head of the humerus and femur), rupture of the tendons of the muscles, "steroid" myopathy, a decrease in muscle mass (atrophy).

From the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis. thinning of the skin, atrophy of the skin and subcutaneous tissue, hyper- or hypopigmentation, "steroid" acne, striae. tendency to develop pyoderma and candidiasis.

Allergic reactions: generalized (skin rash, skin itching, anaphylactic shock), local allergic reactions.

Others: development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia. withdrawal syndrome.

Overdose

It is possible to increase dose-dependent side effects, with the exception of allergic reactions. It is necessary to reduce the dose of dexamethasone. Treatment is symptomatic.

Interaction with other drugs

Dexamethasone increases the toxicity of cardiac glycosides (due to the resulting hypokalemia, the risk of developing arrhythmias increases).

Accelerates excretion acetylsalicylic acid, reduces its concentration in the blood (with the abolition of dexamethasone, the concentration of salicylates in the blood increases and the risk of side effects increases).

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

Increases the metabolism of isoniazid, mexiletine (especially in "fast acetylators"), which leads to a decrease in their plasma concentrations.

Increases the risk of developing hepatitis toxic action paracetamol (induction of "liver" enzymes and the formation of a toxic metabolite of paracetamol).

Increases (with prolonged therapy) the content of folic acid.

Hypokalemia caused by glucocorticosteroids can increase the severity and duration of muscle blockade against the background of muscle relaxants,

In high doses, it reduces the effect of somatropin.

Antacids reduce the absorption of glucocorticosteroids.

Dexamethasone reduces the effect of hypoglycemic drugs: enhances the anticoagulant effect of coumarin derivatives.

Weakens the effect of vitamin D on the absorption of calcium ions in the intestinal lumen. Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by glucocorticosteroids.

Reduces the concentration of praziquantsla in the blood.

Cyclosporine (inhibits metabolism) and ketoconazole (reduces clearance) increase toxicity.

Thiazide diuretics, carbonic anhydrase inhibitors. other glucocorticosteroids and amphotericin B increase the risk of hypokalemia. sodium-containing drugs - edema and increased blood pressure.

Non-steroidal anti-inflammatory drugs and ethanol increase the risk of developing ulceration of the gastrointestinal mucosa, bleeding, in combination with non-steroidal anti-inflammatory drugs for 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 its side effects.

Amphotericin B and carbonic anhydrase inhibitors increase the risk of osteoporosis.

The therapeutic effect of glucocorticosteroids is reduced under the influence of phenytoin. barbiturates, ephedrine, theophylline, rifampicin and other inducers of "liver" microsomal enzymes (increased metabolic rate).

Mitotan and other inhibitors of adrenal function may necessitate an increase in the dose of glucocorticosteroids.

The clearance of glucocorticosteroids increases against the background of thyroid hormones.

Immunosuppressants increase the risk of developing infections and lymphoma or other lymphoproliferative disorders caused by the Epstein-Barr virus.

Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of glucocorticosteroids, prolong the half-life and their therapeutic and toxic effects.

The appearance of hirsutism and acne is facilitated by the simultaneous use of other steroid hormonal drugs - androgens, estrogens, anabolic steroids, oral contraceptives.

Tricyclic antidepressants may increase the severity of depression caused by taking glucocorticosteroids (not indicated for the treatment of these side effects).

The risk of developing cataracts increases when used in combination with other glucocorticosteroids. antipsychotic drugs (neuroleptics), carbutamide and azathioprine.

Simultaneous administration with m-anticholinergics (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of an increase in intraocular pressure.

special instructions

Before starting and during glucocorticosteroid therapy, it is necessary to control general analysis blood, glycemia and plasma electrolytes.

When prescribing dexamethasone for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics.

With daily use, by 5 months of treatment, atrophy of the adrenal cortex develops.

May mask some symptoms of infections: it is useless to carry out immunization during treatment.

With the sudden cancellation of glucocorticosteroids, especially in the case of previous use of high doses. there is a syndrome of "cancellation" of glucocorticosteroids (not due to hypocorticism): loss of appetite, nausea, lethargy, generalized musculoskeletal pain, asthenia, and acute adrenal insufficiency (lowering blood pressure, arrhythmia, sweating, weakness, oligoanuria, vomiting, abdominal pain, diarrhea, hallucinations, fainting, coma).

After cancellation, relative insufficiency of the adrenal cortex persists for several months. If stressful situations arise during this period, glucocorticosteroids are prescribed (according to indications) for a while, if necessary in combination with mineralocorticosteroids.

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

During treatment with dexamethasone (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure and water and electrolyte balance, as well as pictures of peripheral blood and glycemia. To reduce side effects, you can prescribe anabolic steroid, antacids. as well as increase the intake of potassium ions in the body (diet, potassium preparations). Food should be rich in potassium ions, proteins, vitamins, containing a small amount fats, carbohydrates and salt.

In children during the period of growth, glucocorticoids should be used only according to absolute indications and iodine with especially careful supervision of the attending physician.

The ability to influence the rate of reactions when driving vehicles or working with other mechanisms.

Care should be taken when driving vehicles and engaging in other potentially dangerous species activities requiring increased concentration attention and speed of psychomotor reactions, as the drug can cause dizziness, etc. Side effects, which may affect these abilities.

Release form:

Tablets 0.5 mg.
10 tablets in a blister pack of film and foil.
5, 10 blister packs with instructions for use in a cardboard pack

Storage conditions:

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

Best before date:

4 years. Do not use after the expiry date stated on the package.

Holiday conditions

Released by prescription.

Manufacturer/organization accepting claims

CJSC "Production Pharmaceutical Company Update"
633623, Novosibirsk region, r.p. Suzun, st. Komissara Zyatkova, 18:
630071. Novosibirsk, Leninsky district, st. Station, d. 80
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