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

Active ingredient

Composition

Active ingredient:

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

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use

Similarities