Dexamethasone 4 mg, 1 ml, 25 pcs

Active substance:

dexamethasone (in the form of sodium phosphate) 4 mg

Dexamethasone-Vial is a glucocorticosteroid (GCS) - a methylated derivative of fluoroprednisolone, inhibits the release of interleukin-1, interleukin-2, interferon gamma from lymphocytes and macrophages. It has anti-inflammatory, anti-allergic, desensitizing, anti-shock, anti-toxic and immunosuppressive effects.

Suppresses the release of adrenocorticotropic hormone (ACTH) and beta-lipotropin by the pituitary gland, but does not reduce the content of circulating beta-endorphin. Inhibits the secretion of thyroid-stimulating hormone (TTT) and follicle-stimulating hormone (FSH).

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

Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus and stimulates mRNA synthesis; 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, which promote inflammation and allergies.

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

Lipid metabolism: increases the synthesis of higher fatty acids and thyroglobulin (TG), 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 digestive tract; increases the activity of glucose-6-phosphatase, leading 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 metabolism: detains 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, "flushes" 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; inducing the formation of lipocortin and decreasing the number of mast cells that produce hyaluronic acid; and also with a decrease in capillary permeability; stabilization of cell membranes and membranes of organelles (especially lysosomal).

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, 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 , decrease in the sensitivity of effector cells to mediators of allergy, inhibition of antibody production, changes in the body's immune response.

In chronic obstructive pulmonary diseases (COPD), the action is based mainly on inhibition of inflammatory processes, inhibition of the development or prevention of edema of the mucous membranes, inhibition of eosinophilic infiltration of the submucous layer of the bronchial epithelium, deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and inhibition of erosion mucous membrane.

Increases the sensitivity of small and medium-sized bronchial beta-adrenergic receptors to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by inhibiting or reducing its production.

The anti-shock and antitoxic effect is associated with an increase in blood pressure (BP) (due to an increase in the concentration of circulating catecholamines and restoration of the sensitivity of adrenergic receptors to them, as well as vasoconstriction), a decrease in vascular wall permeability, membrane protective properties, 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 and interleukin-2, interferon gamma) from lymphocytes and macrophages.

Suppresses the synthesis and secretion of ACTH and, secondarily, 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 function of the pituitary gland and an almost complete absence of mineralocorticosteroid activity. Doses of 1-1.5 mg / day inhibit the adrenal cortex; biological half-life - 32-72 hours (duration of suppression of the hypothalamic-pituitary-adrenal system).

In terms of the strength of glucocorticosteroid 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

After i / m injection, it is absorbed slowly, the maximum plasma content is after 7-9 hours.

Communication with plasma proteins - 80%. Penetrates the blood-brain and placental barriers.

Metabolized in the liver. T1 / 2 - 3-5 hours. It is excreted by the kidneys (a small part - by the lactating glands).

• shock (burn, traumatic, operational, toxic) if other therapy is ineffective;
• allergic reactions (acute, severe forms), blood transfusion shock, anaphylactic shock, anaphylactoid reactions;
• cerebral edema (including against the background of a brain tumor or associated with surgery, radiation therapy, or head injury);
• bronchial asthma (severe form), asthmatic status;
• systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);
• acute suprarenal insufficiency;
• thyrotoxic crisis;
• acute hepatitis, hepatic coma;
• poisoning with cauterizing fluids (reducing inflammation and preventing scarring).

For short-term use for "vital" indications, the only contraindication is hypersensitivity.

For intra-articular 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 in history), as well as a general infectious disease, pronounced periarticular osteoporosis, no signs of inflammation in the joint (the so-called "dry" joint, for example, in osteoarthritis without synovitis), pronounced 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 ...

Carefully:

• 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), chickenpox, measles; amebiasis, strongyloidosis (established or suspected) systemic mycosis; active and latent tuberculosis. Application for severe infectious diseases is permissible only against the background of specific therapy;
• post-vaccination period (a period lasting 8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;
• immunodeficiency states (including AIDS or HIV infection);
• diseases of the gastrointestinal tract: gastric ulcer and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, newly 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, it is possible to spread the focus of necrosis, slow 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;
• severe chronic renal and / or hepatic failure, nephrourolithiasis;
• hypoalbuminemia and conditions predisposing to its occurrence;
• systemic osteoporosis, myasthenia gravis, acute psychosis, obesity (III-IV grade), poliomyelitis (except for the form of bulbar encephalitis), open- and closed-angle glaucoma.

For intra-articular administration: general serious condition of the patient, ineffectiveness (or short duration) of the action of 2 previous injections (taking into account the individual properties of the GCS used).

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

On the part of the digestive system: nausea, vomiting, pancreatitis, "steroid" ulcers of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - increased activity of "hepatic" transaminases and alkaline phosphatase.

On the part of the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of chronic heart failure, ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus 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 anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, headache, convulsions.

From the sensory organs: sudden loss of vision (with parenteral administration in the region of the head, neck, nasal concha, scalp, 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, 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, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating.

Due to mineralocorticosteroid activity - fluid and sodium ion retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

On the part of 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 humerus and femur head), muscle tendon rupture, "steroid" myopathy, decreased muscle mass (atrophy).

On the part of 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: generalized (skin rash, itching of the skin, anaphylactic shock), local allergic reactions.

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

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

With the on / in the introduction: arrhythmias, "hot flushes" of blood to the face, convulsions.

With intracranial administration - epistaxis.

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

Dexamethasone is pharmaceutically incompatible with other drugs (it can form insoluble compounds).

Dexamethasone increases the toxicity of cardiac glycosides (because of the resulting hypokalemia, the risk of arrhythmias increases). Accelerates the excretion of acetylsalicylic acid, reduces the content of its metabolites in the blood (when dexamethasone is canceled, 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 immunization, 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 hepatotoxic effects of 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 GCS can increase the severity and duration of muscle blockade against the background of muscle relaxants.

In high doses, it reduces the effect of somatropin.

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 GCS.

Reduces the concentration of praziquantel in the blood.

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

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

NSAIDs and ethanol increase the risk of ulceration of the gastrointestinal mucosa and bleeding; in combination with NSAIDs for the treatment of arthritis, it is possible to reduce the dose of GCS due to the summation of the therapeutic effect.

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

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

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

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

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

Immunosuppressants increase the risk of infections and lymphoma or other lymphoproliferative disorders associated with Epstein-Barr virus.

Estrogens (including oral estrogen-containing contraceptives) reduce the clearance of GCS, lengthen 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 can increase the severity of depression caused by taking GCS (not indicated for the treatment of these side effects).

The risk of developing cataracts increases when used against the background of other GCS, antipsychotic drugs (neuroleptics), carbutamide and azathioprine.

Concomitant administration with m-anticholinergics (including antihistamines, tricyclic antidepressants) and nitrates contributes to the development of increased intraocular pressure.

With simultaneous interthecal use with iofendilate, the risk of developing arachnoiditis increases.

The dosage regimen is individual and depends on the indications, the patient's condition and his response to therapy. The drug is injected intravenously slowly in a stream or drip (in acute and urgent conditions); intramuscularly; local (in pathological education) introduction is also possible. In order to prepare a solution for intravenous (IV) drip infusion, use isotonic sodium chloride solution or 5% dextrose solution.

Dexamethasone sodium phosphate: intra-articular, in the lesion - 0.2-6 mg, repeated 1 every 3 days or 3 weeks.

V / m or / in - 0.5-9 mg / day.

For the treatment of cerebral edema - 10 mg in the first administration, then 4 mg IM every 6 hours until the symptoms disappear. The dose can be reduced after 2-4 days with gradual cancellation within 5-7 days after elimination of cerebral edema. The maintenance dose is 2 mg 3 times a day.

For the treatment of shock - intravenous 20 mg in the first injection, then 3 mg / kg in 24 hours as an intravenous infusion or intravenous jet - from 2 to 6 mg / kg as a single injection or 40 mg as a single dose injections given every 2-6 hours; possible intravenous administration of 1 mg / kg once. Shock therapy should be canceled as soon as the patient's condition stabilizes, the usual duration is no more than 2-3 days.

Allergic diseases - intramuscularly in the first injection of 4-8 mg. Further treatment is carried out with oral dosage forms.

For nausea and vomiting during chemotherapy - 8-20 mg intravenously 5-15 minutes before the chemotherapy session. Further chemotherapy should be given with oral dosage forms.

For the treatment of respiratory distress syndrome of newborns - intramuscular injection of 5 mg every 12 hours, then from the seventh day every 24 hours. The maximum daily dose is 80 mg.

For children: for the treatment of adrenal insufficiency - IM at 23 μg / kg (0.67 mg / m2) every 3 days, or 7.8-12 μg / kg (0.23-0.34 mg / m2 / day), or 28-170 μg / kg (0.83-5 mg / m2) every 12-24 hours.

Symptoms : increased blood pressure, edema, peptic ulcer, hyperglycemia, impaired consciousness.

Treatment:  symptomatic, no specific antidote.