Dexamethasone, 4 mg/ml 1 ml 10 pcs

Pharmacological action

Pharmacodynamics

It interacts with specific cytoplasmic receptors and forms a complex penetrating into the cell nucleus and stimulating mRNA synthesis: the latter induces formation of proteins, including lipocortin, mediating cellular effects. Lipocortin inhibits phospholipase A2, suppresses arachidonic acid liberation and inhibits the biosynthesis of endoperoxides, PG, leukotrienes, contributing to the processes of inflammation, allergy, etc.

Inhibits the release of inflammatory mediators from eosinophils and mast cells. Inhibits the activity of hyaluronidase, collagenase and proteases, normalizes the functions of the intercellular matrix of cartilage and bone tissue. It decreases capillary permeability, stabilizes cell membranes, including lysosomal membranes, inhibits release of cytokines (interleukins and gamma interferon) from lymphocytes and macrophages, causes involution of lymphoid tissue. Restores sensitivity of adrenoreceptors to catecholamines. Accelerates protein catabolism, decreases glucose utilization by peripheral tissues and increases gluconeogenesis in the liver. Reduces absorption and increases calcium excretion; inhibits sodium (and water) ACTH secretion.

Pharmacokinetics

In intravenous administration binds to specific carrier protein – transcortin – by 70-80%; in high doses of the drug binding to proteins is reduced to 60-70% due to transcortin saturation. Passes easily through histohematic barriers, including the blood-brain and placental ones. When ingested, it is rapidly and completely absorbed mainly in the proximal small intestine; absorption in the distal part is approximately half that in the proximal part. The absorption is reached within 1-2 hours. It is biotransformed in the liver, mainly by conjugation with glucuronic and sulfuric acids, to inactive metabolites.

The blood elimination half-life of T1/2 is 3-5 hours, the biological half-life is 36-54 hours. During parenteral administration it is metabolized faster and, correspondingly, pharmacological effects are shorter. It is excreted mainly with urine (a small part is excreted by lactating glands) as 17-ketosteroids, glucuroids and sulfates. About 15% of dexamethasone is excreted unchanged in the urine. When applied to the skin absorption is determined by many factors (skin integrity, presence of occlusive dressing, dosage form, etc.) and varies greatly.

Indications

• .Addison’s disease, congenital adrenal hypoplasia, adrenal insufficiency (usually in combination with mineralocorticoids), adrenogenital syndrome, thyroiditis (acute, subacute), hypothyroidism, tumor hypercalcemia, shock (anaphylactic, posttraumatic, postoperative, cardiogenic, hemotransfusion and others.), rheumatoid arthritis in the acute phase, acute rheumatic heart disease, collagenosis (rheumatic diseases, disseminated lupus erythematosus, etc.).), inflammatory and degenerative joint disease (arthritis, tendovaginitis, bursitis, epicondylitis, styloiditis, osteochondrosis, osteoarthritis, Bechterew disease, etc.), myositis, infectious-allergic bronchial asthma, asthmatic status, anaphylactoid reactions, including.
• brain edema (with tumors, brain injury, neurosurgery, brain hemorrhage, encephalitis, meningitis, radiation-induced lung injury);
• unspecific ulcerative colitis, hepatitis, sarcoidosis, berylliosis, disseminated tuberculosis (only in combination with antituberculosis drugs), Leffler disease, etc. severe respiratory diseases;
• anemia (autoimmune, hemolytic, congenital, hypoplastic, idiopathic, erythroblastopenia), idiopathic thrombocytopenic purpura (in adults), secondary thrombocytopenia, lymphoma (Hodgkins and non-Hodgkins), leukemia, lympholeukosis (acute, chronic), agranulocytosis, plasmacytoma, etc. blood diseases;
• nephrotic syndrome, severe infectious diseases (must be combined with antibiotics), severe inflammatory processes after eye trauma and surgery.

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Active ingredient

Dexamethasone

Composition

Active ingredient:

dexamethasone sodium phosphate (in terms of dexamethasone phosphate) – 4.0 mg in 1 ml.

How to take, the dosage

It is indicated for intravenous, intramuscular, intraarticular, periarticular and retrobulbar administration.

Adults in acute and emergency conditions are administered by IV slowly, by trickle or drip, or intravenously at a dose of 4-20 mg 3-4 times a day. The maximum single dose is 80 mg.

The maintenance dose is 0.2-9 mg per day. The course of treatment lasts 3-4 days and then we switch to oral dexamethasone administration.

In children – intravenously in dosage 0.02776-0.16665 mg/kg every 12-24 hours.

Intraarticularly (into the lesion area) or periarticularly (into soft tissues) to adults and adolescents is administered in dose 0.2-6 mg (2-8 mg) repeatedly at intervals of 3 days to 3 weeks as needed; maximum dose for adults is 80 mg daily.

In case of shock, adults – by IV 20 mg once, then by 3 mg/kg for 24 hours as a continuous infusion or by IV once 2-6 mg/kg, or by IV 40 mg every 2-6 hours.

In cerebral edema (adults) 10 mg intravenously, then 4 mg every 6 hours intravenously until symptoms disappear; the dose is reduced after 2-4 days and the treatment is gradually stopped within 5-7 days.

In adrenal cortex insufficiency (children), 0.0233 mg/kg (0.67/mg2) per day in 3 injections every third day, or daily 0.00776-0.01165 mg/kg (0.233-0.335 mg/m2) per day.

Interaction

Therapeutic and toxic effects of dexamethasone are reduced by barbiturates, phenytoin, rifampicin (accelerate metabolism); somatotropin; antacids (reduce absorption), enhance – estrogen-containing oral contraceptives.

The risk of arrhythmias and hypokalemia is increased by cardiac glycosides and diuretics; the risk of edema and arterial hypertension – by sodium-containing drugs and supplements; severe hypokalemia, heart failure and osteoporosis – by amphotericin B and carboangidase inhibitors; risk of erosive-ulcerative lesions and gastrointestinal bleeding – non-steroidal anti-inflammatory drugs.

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

Weakens hypoglycemic activity of insulin and oral antidiabetic agents; anticoagulant activity of coumarins; diuretic activity of diuretics; immunotropic activity of vaccines (suppresses antibody formation).

Worsens tolerance of cardiac glycosides (causes potassium deficiency), reduces the concentration of salicylates and praziquantel in blood.

Special Instructions

Restricted to use in: Peptic ulcers of the GI tract, peptic ulcer of the stomach and duodenum, esophagitis, gastritis, intestinal anastomosis (in the immediate anamnesis); congestive heart failure, arterial hypertension, thrombosis, diabetes, osteoporosis, Icenko-Cushing’s disease, acute renal and/or liver failure, psychosis, seizures, myasthenia gravis, open-angle glaucoma, AIDS, pregnancy, lactation.

Contraindications

Hypersensitivity, systemic mycoses, amoebic infections, infectious joint and periarticular soft tissue lesions, active tuberculosis, period before and after preventive vaccinations (especially antiviral), glaucoma, acute purulent eye infection (retrobulbar injection).

Side effects

• .Sodium and water retention, loss of potassium and calcium, edema, gastrointestinal erosive and ulcerative lesions (with aggravation of ulcer disease up to perforation, bleeding), hemorrhagic pancreatitis, GI atony, increased appetite, nausea and vomiting, hepatomegaly, muscle weakness, myopathy, osteoporosis, pathological fractures, tendon ruptures, arrhythmia, bradycardia, increased BP, congestive heart failure, myocardial infarction and dystrophy, Icenko-Cushing syndrome, hyperglycemia, hyperlipoproteinemia, negative nitrogen balance, dysmenorrhea, growth retardation in children, hirsutism, reduced immunity, suppression of regenerative and reparative processes, dizziness, headaches, mood disorders, psychosis, increased intracranial pressure, seizures, thinning and vulnerability of skin, petechiae, ecchymosis, stretch marks, erythema and changes in skin pigmentation, increased sweating, increased intraocular pressure, exophthalmus;
• thrombosis and thromboembolism, withdrawal syndrome (malaise, pain: head, abdominal, joint and muscle pains);
• depression, secondary adrenal insufficiency;
• often, allergic reactions (rash, itching).

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Overdose

Reports of acute toxic poisonings and/or deaths due to glucocorticoid overdose are extremely rare.

If adverse events develop – treatment is symptomatic, aimed at maintaining vital functions; Icenko-Cushing’s syndrome – aminoglutemide prescription.

Pregnancy use

Use during pregnancy is allowed if the expected effect of therapy exceeds the potential risk to the fetus. Breast-feeding should be stopped during the treatment.

Similarities

Oftan Dexamethasone, Maxidex, Dexamethasone-Vial, Dexamethasone, Megadexan