DEXAMETHASONE PILLS 0.5 MG

Mechanism of action

GKS. Suppresses the function of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. Violates the ability of macrophages to phagocytosis, as well as the formation of interleukin-1. It contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to histamine release. Suppresses the activity of fibroblasts and the formation of collagen.
Inhibits the activity of phospholipase A2, which leads to the suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed to the lymphoid tissue; inhibits the formation of antibodies.
Dexamethasone inhibits pituitary ACTH and b-lipotropin, but does not reduce the level of circulating b-endorphin. It inhibits the secretion of TSH and FSH.
With the direct application of the vessels has a vasoconstrictor effect.
Dexamethasone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats.Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys, increases the activity of gluconeogenesis enzymes. In the liver, Dexamethasone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose activates insulin secretion.
Dexamethasone inhibits glucose uptake by fat cells, which leads to the activation of lipolysis. However, due to an increase in insulin secretion, lipogenesis is stimulated, which leads to fat accumulation.
It has a catabolic effect in the lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. Osteoporosis and Cushing's syndrome are the main factors limiting the long-term therapy of SCS. As a result of the catabolic effect, growth can be suppressed in children.
In high doses, dexamethasone may increase the excitability of brain tissue and help lower the threshold of convulsive readiness. Stimulates excessive production of hydrochloric acid and pepsin in the stomach, which contributes to the development of peptic ulcers.
With systemic use, the therapeutic activity of dexamethasone is due to the anti-inflammatory, anti-allergic, immunosuppressive and anti-proliferative effects.
When applied topically and locally, the therapeutic activity of dexamethasone is due to anti-inflammatory,antiallergic and antiexudative (due to vasoconstrictor effect) action.
On anti-inflammatory activity exceeds Hydrocortisone 30 times, does not possess mineralocorticoid activity.

Metabolized in the liver. The half-life is 2-3 hours. Excreted by the kidneys.
When applied topically in ophthalmology, it is absorbed through the cornea with intact epithelium in the moisture of the anterior chamber of the eye. When inflammation of the eye tissue or damage to the mucous membrane and cornea, the rate of absorption of dexamethasone increases significantly.

For oral administration: Addison's disease - Birmera; acute and subacute thyroiditis, hypothyroidism, progressive ophthalmopathy associated with thyrotoxicosis; bronchial asthma; rheumatoid arthritis in the acute phase; NK; connective tissue diseases; autoimmune hemolytic anemia, thrombocytopenia, aplasia and hypoplasia of the blood, agranulocytosis, serum sickness; acute erythroderma, pemphigus (normal), acute eczema (at the beginning of treatment); malignant tumors (as palliative therapy); congenital adrenogenital syndrome; swelling of the brain (usually after prior parenteral administration of GCS).
For parenteral administration: shock of various genesis; cerebral edema (with brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis,radiation injury); asthmatic status; severe allergic reactions (angioedema, bronchospasm, dermatosis, acute anaphylactic reaction to drugs, serum transfusions, pyrogenic reactions); acute hemolytic anemia, thrombocytopenia, acute lymphoblastic leukemia, agranulocytosis; severe infectious diseases (in combination with antibiotics); acute insufficiency of the adrenal cortex; spicy croup; diseases of the joints (shoulder-scapular periarthritis, epicondylitis, styloiditis, bursitis, tendovaginitis, compression neuropathy, osteochondrosis, arthritis of various etiologies, osteoarthritis).
For use in ophthalmic practice: non-purulent and allergic conjunctivitis, keratitis, keratoconjunctivitis without damage to the epithelium, iritis, iridocyclitis, blepharoconjunctivitis, blepharitis, episculitis, scleritis, inflammatory process after eye injuries and surgical procedures, sympathetic ophthalmus, scleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmus, scleritis, inflammation after eye injuries and surgical procedures, sympathetic ophthalmus, sylmatitis

Individual. Inside for serious diseases, at the beginning of treatment, up to 10-15 mg / day is prescribed, the maintenance dose may be 2 - 4.5 mg or more per day. The daily dose is divided into 2-3 doses. When used in small doses, dexamethasone is administered once in the morning.
In case of parenteral administration, it is introduced into / into a slow jet or drip (in acute and emergency conditions); in / m; periarticular and intraarticular administration is also possible.During the day, you can enter from 4 to 20 mg of dexamethasone 3-4 times. The duration of parenteral administration is usually 3-4 days, then switch to maintenance therapy with the oral form. In the acute period, with various diseases and at the beginning of treatment, dexamethasone is used in higher doses. When the effect is achieved, the dose is reduced at intervals of several days until the maintenance dose is reached or until the treatment is stopped.
When used in ophthalmology in acute conditions, instilled into the conjunctival sac 1-2 drops every 1-2 hours, then, with a decrease in inflammation, every 4-6 hours. Duration of treatment from 1-2 days to several weeks depending on the clinical course diseases.

On the part of the endocrine system: with short-term therapy - a decrease in glucose tolerance; with long-term therapy, it is possible to develop Itsenko-Cushing syndrome, hyperglycemia, including steroid diabetes, adrenal insufficiency, especially during stress (in trauma, surgery, concomitant diseases).
Metabolism: hyperlipoproteinemia, hepatomegaly.
Since the cardiovascular system: with short-term therapy - bradycardia, hypotension, collapse (especially with the rapid introduction of large doses), arrhythmias, cardiac arrest; with prolonged therapy possible myocardial dystrophy.
On the part of the central nervous system: with prolonged therapy, mood disorders, psychosis, increased intracranial pressure, dizziness, headaches, convulsions,
On the part of the organ of vision: increased intraocular pressure, posterior subcapsular cataract, exophthalmos. With prolonged use of dexamethasone in ophthalmic practice, it is possible to increase intraocular pressure; when the cornea is thinning, there is a danger of perforation.
On the part of the digestive system: nausea, vomiting, development of steroid gastric ulcer are possible with short-term therapy; with prolonged therapy, erosive and ulcerative lesions of the gastrointestinal tract, pancreatitis are possible.
On the part of the hematopoietic system: with prolonged therapy, increased thrombosis is possible.
Dermatological reactions: with prolonged therapy, erythema of the face, thinning and vulnerability of the skin, petechiae, ecchymosis, stretch marks, panniculitis, slow wound healing are possible.
Side effects associated with immunosuppressive effects: with short-term therapy - reduced immunity; with long-term therapy, infections may be more frequent and their severity will worsen.
Other: increased sweating.

Hypersensitivity to dexamethasone.
Systemic mycoses, infections of the joints and periarticular tissues, grade III-IV obesity (when administered orally).
For use in ophthalmic practice: viral and fungal diseases of the eye, an acute form of purulent eye infection in the absence of specific therapy, corneal diseases associated with epithelial defects, trachoma, glaucoma.

During pregnancy (especially in the first trimester), as well as during lactation, dexamethasone is used taking into account the expected therapeutic effect and the negative effect on the fetus. With prolonged therapy during pregnancy does not exclude the possibility of fetal growth disorders. 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.

It is used with caution in patients with NUC, with diverticulitis, recently created intestinal anastomosis, gastric ulcer and duodenal ulcer, renal failure, systemic osteoporosis, myasthenia, and arterial hypotension. Caution is also needed when using dexamethasone in patients with severe arterial hypertension, diabetes, mental illness and hypoalbuminemia. In hypothyroidism, as well as in liver cirrhosis, the effect of dexamethasone may be enhanced. With initial emotional instability or psychotic tendencies, these phenomena may intensify.
When applying dexamethasone in patients with herpes of the cornea should be borne in mind the possibility of perforation. During treatment, it is necessary to control the intraocular pressure and the state of the cornea.
With the sudden cancellation of dexamethasone, especially in the case of previous use in high doses, there is a so-called withdrawal syndrome (not caused by hypocorticism), manifested by anorexia, nausea, inhibition,generalized musculoskeletal pain, general weakness. After dexamethasone is canceled for a few months, the relative insufficiency of the adrenal cortex may persist. If during this period there are stressful situations, they are prescribed (according to indications) for the period of GCS, if necessary in combination with mineralocorticoids.
In children during long-term treatment, careful monitoring of the dynamics of growth and development is necessary. Children who were in contact with measles or chicken pox during the treatment period are prescribed specific immunoglobulins prophylactically.
Dexamethasone in the form of tablets, solution for injection and eye drops is included in the List of Vital and Essential Drugs.

With simultaneous use of dexamethasone with cardiac glycosides, the tolerance of the latter may be worsened due to potassium deficiency; with diuretics - perhaps increased excretion of potassium; with antidiabetic agents - hyperkalemia is possible; with coumarin derivatives - a weakening of the anticoagulant effect is possible; with rifampicin, phenytoin, barbiturates - it is possible to weaken the effect of dexamethasone; hormonal contraceptives - may increase the action of dexamethasone; with NSAIDs - the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract may be increased; with praziquantel - perhaps a decrease in its concentration in the blood.