Universal reference book for medicines
Name of the drug: DEXAMETHASONE

Active substance: dexamethasone

Type: GCS for injection

Manufacturer: SHREYA LIFE SCIENCES (India)
Composition, form of production and packaging
The injection solution is
clear, colorless or pale yellow.

1 amp.

dexamethasone sodium phosphate (in terms of dexamethasone phosphate) 4 mg

Excipients: methylparaben, propylparaben, sodium metabisulphite, disodium edetate, sodium hydroxide, water d / u.

1 ml - ampoules of dark glass (25) - cardboard boxes.

1 ml - bottles of dark glass (25) - carton boxes.

The injection solution is clear, colorless or pale yellow.

1 ml of 1 amp.

dexamethasone sodium phosphate (in terms of dexamethasone phosphate) 4 mg 8 mg

Excipients: methylparaben, propylparaben, sodium metabisulphite, disodium edetate, sodium hydroxide, water d / u.

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

2 ml - bottles of dark glass (25) - carton boxes.

INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

Synthetic glucocorticoid (GCS), methylated derivative of fluoride prednisolone.
Has anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are present in all tissues, especially in the liver), with the formation of a complex inducing the formation of proteins (including enzymes that regulate vital processes in cells.)

Protein metabolism: reduces the number of globulins in plasma, increases the synthesis of albumin 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 synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of ​​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); promotes the development of hyperglycemia.
Water-electrolyte metabolism: retards 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 the suppression of the release of eosinophils and mast cells by inflammatory mediators;
inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. It acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin depresses phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, promoting 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.
Immunosuppressive effect is caused by induced lymphoid tissue involution, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, 2, gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies.

The antiallergic effect develops as a result of a decrease in the synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in 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 mediators of allergy, inhibition of antibody formation, changes in the immune response of the body.
In obstructive airway diseases, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of mucosal edema, a decrease in the 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 bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS.

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 pituitary function and a virtually complete absence of 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 oppression of the hypothalamic-pituitary-cortical adrenal gland system).
The strength of the glucocorticoid activity of 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

Blood is bound (60-70%) with a specific transporter protein - transcortin.
Easily passes through gistogematicheskie barriers (including through hemato-encephalic and placental).
Metabolised in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites.

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

Diseases requiring the introduction of high-speed GCS, as well as cases where oral administration of 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, operational, toxic) - with ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;

- edema of the brain (with a brain tumor, craniocerebral trauma, 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, with the impossibility of oral treatment;
- 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 injection): allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, irit, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after corneal transplantation;

- local application (in the area of ​​pathological education): keloids, discoid lupus erythematosus, annular granuloma.

DOSING MODE

The dosage regimen is individual and depends on the indications, the patient's condition and his reaction to therapy.
The drug is administered iv in a slow stream or drip (with acute and urgent conditions); in / m; possibly also local (in pathological education) introduction. To prepare a solution for intravenous drip infusion, an isotonic solution of sodium chloride or a 5% dextrose solution should be used.
In an acute period with various diseases and at the beginning of therapy, Dexamethasone is used in higher doses.
During the day, you can inject 4 to 20 mg of Dexamethasone 3-4 times.
Doses of the drug for children (IM):

The dose of the drug for substitution therapy (with adrenal cortex insufficiency) is 0.0233 mg / kg body weight or 0.67 mg / m 2 body surface area, divided into 3 doses, every 3rd day or 0.00776 - 0.01165 mg / kg body weight or 0.233 - 0.335 mg / m 2 body surface area daily.
For other indications, the recommended dose is from 0.02776 to 0.16665 mg / kg body weight or 0.833 to 5 mg / m 2 body surface area every 12-24 hours.
When the effect is achieved, the dose is reduced to a maintenance dose or until the treatment is discontinued.
The duration of parenteral use is usually 3-4 days, then switch to maintenance therapy with dexamethasone in tablets.
Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute adrenocortical insufficiency.

SIDE EFFECT

Usually Dexamethasone is well tolerated.
It has a low mineralocorticoid activity, i.e. its effect on water-electrolyte exchange is small. As a rule, low and medium doses of Dexamethasone do not cause delays in sodium and water in the body, increased excretion of potassium. The following side effects are described:
On the part of the endocrine system: a decrease in glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae) , delay in sexual development in children.

On the part of the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal wall, increased or decreased appetite, digestive disorders, flatulence, hiccough.
In rare cases - increased activity of hepatic transaminases and alkaline phosphatase.
From the cardiovascular 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, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing 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 anxiety, insomnia, dizziness, vertigo, pseudotumor, cerebral palsy, headache, convulsions.

From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial, fungal or viral eye infections, trophic corneal changes, exophthalmos, sudden loss of vision (for parenteral administration in the head, neck, nasal shells, scalp, possibly the deposition of drug crystals in the vessels of the eye).

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

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

On the part of the musculoskeletal system: slowing growth 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 thigh bone), rupture of the tendons of muscles, steroid myopathy, (atrophy).

On the part of the skin and mucous membranes: delayed healing of wounds, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, propensity to develop pyoderma and candidiasis.

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

Local with parenteral administration: burning, numbness, pain, tingling at the injection site, infection at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site;
atrophy of the skin and subcutaneous tissue with the / m introduction (especially dangerous is the introduction to the deltoid muscle).
Other: development or exacerbation of infections (the emergence of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, blood flushing to the face, withdrawal syndrome.

CONTRAINDICATIONS

For short-term use according to vital indications, the only contraindication is hypersensitivity to dexamethasone or the components of the drug.

In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.

With caution, the drug should be administered in the following conditions and conditions:

- gastrointestinal diseases - peptic ulcer of stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing threat, diverticulitis;

- parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles;
amebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis. The use in severe infectious diseases is permissible only against the background of specific therapy.
- pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;

- immunodeficiency conditions (including AIDS or HIV infection);

- diseases of the cardiovascular system (including recently transferred myocardial infarction - in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia);

- endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV century)

- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;

- 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;

- Pregnancy.

PREGNANCY AND LACTATION

In pregnancy (especially in the first trimester), the drug can be used only when the expected therapeutic effect exceeds 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 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 treatment with the drug during breastfeeding, then breastfeeding should be discontinued.

APPLICATION FOR FUNCTIONS OF THE LIVER

Contraindications: severe chronic renal failure, nephrourolythiasis.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindications: severe chronic liver failure.

APPLICATION FOR CHILDREN

In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.

SPECIAL INSTRUCTIONS

During treatment with dexamethasone (especially long-term) it is necessary to observe the oculist, monitor blood pressure and the state of water-electrolyte balance, as well as patterns of peripheral blood and blood glucose levels.

To reduce side effects, antacids can be prescribed, and K + intake should be increased (diet, potassium preparations).
Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.
The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis.
The drug may enhance existing emotional instability or psychotic disorders.When referring to psychoses in an anamnesis, Dexamethasone is given in high doses under strict doctor's supervision.
With caution should be used in acute and subacute myocardial infarction - possibly spreading the focus of necrosis, slowing the formation of scar tissue and rupture of the heart muscle.

In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids.
It should be carefully monitored for patients within a year after the end of long-term therapy with Dexamethasone in connection with the possible development of a relative insufficiency of the adrenal cortex in stressful situations.
With the sudden cancellation, particularly in the case of the prior use of high doses may develop the syndrome of "lifting" (anorexia, nausea, lethargy, generalized musculoskeletal pain, fatigue), as well as worsening of the disease, about which he was appointed Dexamethasone.
During treatment Dexamethasone should not be vaccinated in connection with a reduction in its efficiency (immune response).
Assigning Dexamethasone with intercurrent infections, septic conditions, and tuberculosis, treatment with antibiotics is necessary to simultaneously bactericidal action.
In children, during long-term treatment Dexamethasone careful observation of the dynamics of growth and development.
Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.
Due to the weak mineralocorticoid effect for replacement therapy for adrenal insufficiency Dexamethasone is used in combination with a mineralocorticoid.
Patients with diabetes should monitor blood glucose content and correct treatment if necessary.
Shows the X-ray control of the osteo-articular system (spine images, brushes).
Patients with latent infectious diseases of the urinary tract Dexamethasone can cause pyuria, which may be of diagnostic value.
Dexamethasone increases the content of 11- and 17-metabolites oksiketokortikosteroidov.
OVERDOSE

May increase the side effects described above.
It is necessary to reduce the dose of dexamethasone.
Treatment is symptomatic.
DRUG INTERACTION

Possible pharmaceutical dexamethasone incompatibility with other I / administered drugs - it is recommended to be administered separately from other drugs (in / bolus or through a dropper, etc., as a second solution.). When mixed with a solution of dexamethasone heparin precipitate formed.
Simultaneous with dexamethasone:
- inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;
- diuretics (especially thiazide and carbonic anhydrase inhibitors) and amphotericin B - can lead to increased excretion of K + and increase the risk of heart failure;
- a sodium-containing drugs- to the development of edema and high blood pressure;
- cardiac glycosides - worsening their tolerance and increases the likelihood of ventricular ekstrasitolii (due to induced hypokalemia);
- indirect antikoagupyantami - weakens (less amplifies) their effect (dose required correction);
- anticoagulants and thrombolytics - increases the risk of bleeding from ulcers in the gastrointestinal tract;
- ethanol and NSAID - enhanced risk of erosive ulcerous lesions in the gastrointestinal tract and of bleeding (in combination with NSAIDs for the treatment of arthritis may be reduced dose glucocorticosteroids for therapeutic effect summation);
-paracetamol - increases the risk of hepatotoxicity (liver enzyme induction and formation of a toxic metabolite of acetaminophen);
- acetylsalicylic acid - accelerates its excretion and lowers blood concentration (cases dexamethasone salicylates blood increases, and increases the risk of side effects);
- insulin and peroralnymi hypoglycemic drugs, antihypertensive agents - their efficiency is reduced;
- Vitamin D - decreases its effect on the absorption of Ca 2+ in the intestine;
- STH - reduces the effectiveness of the latter, and with praziquantel - its concentration;
-M-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrate - contributes to the intraocular pressure;
- isoniazid and mexiletine - increases their metabolism (especially in the "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 side effects.
ACTH increases the effects of dexamethasone.
Ergocalciferol and parathyroid hormone hinder the development of osteopathy caused by dexamethasone.
Cyclosporine and ketoconazole, slowing down the metabolism of dexamethasone, may in some cases increase its toxicity.
Simultaneous with the appointment of androgens and anabolic steroid drug dexamethasone contributes to the development of peripheral edema and hirsutism, 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 adrenocortical function may necessitate increasing the dose of dexamethasone.
While the use of live virus vaccines and immunization compared to other types of activation increases the risk of viruses and the development of infections.
Antipsychotic drugs (neuroleptics) and azathioprine increases the risk of developing cataracts in the appointment of dexamethasone.
While the use of antithyroid drugs decreases, and a thyroid hormone - increased clearance dexamethasone.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. Store at a temperature not higher than 25 ° C in the reach of children.
Do not freeze. Shelf life - 3 years. Do not use after the expiry date printed on the package.
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