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Pharmacology
Pharmacological action - anti-inflammatory, anti-allergic, immunosuppressive, anti-shock, glucocorticoid.
Interacts with specific cytoplasmic receptors and forms a complex that penetrates the cell nucleus; causes the expression or depression of mRNA, changing the formation of proteins on ribosomes, incl. lipocortin mediating cellular effects. Lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, PGs, leukotrienes, which promote inflammation, allergies, etc. It prevents the release of inflammatory mediators from eosinophils and mast cells. It inhibits the activity of hyaluronidase, collagenase and proteases, normalizes the functions of the extracellular matrix of cartilage and bone tissue. Reduces capillary permeability, stabilizes cell membranes, incl. lysosomal, inhibits the release of cytokines (interleukins 1 and 2, interferon gamma) from lymphocytes and macrophages. Affects all phases of inflammation, the antiproliferative effect is due to inhibition of the migration of monocytes into the inflammatory focus and the proliferation of fibroblasts. It causes involution of lymphoid tissue and lymphopenia, which leads to immunosuppression. In addition to reducing the number of T-lymphocytes, their effect on B-lymphocytes decreases and the production of immunoglobulins is inhibited. The effect on the complement system is to reduce the formation and increase the breakdown of its components. Antiallergic effect is a consequence of inhibition of synthesis and secretion of allergy mediators and a decrease in the number of basophils. Restores the sensitivity of adrenergic receptors to catecholamines. Accelerates protein catabolism and reduces their content in plasma, reduces glucose utilization by peripheral tissues and increases gluconeogenesis in the liver. Stimulates the formation of enzyme proteins in the liver, surfactant, fibrinogen, erythropoietin, lipomodulin. Causes the redistribution of fat (increases lipolysis of adipose tissue of the extremities and fat deposition in the upper half of the body and on the face). Promotes the formation of higher fatty acids and triglycerides. Decreases absorption and increases calcium excretion; delays sodium and water, the secretion of ACTH. Has an anti-shock effect.
After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract, Tmax - 1–2 hours. In the blood it binds (60–70%) to a specific carrier protein - transcortin. Easily passes through the histohematological barriers, including the BBB and placental. It is biotransformed in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. T1 / 2 from plasma - 3-4.5 hours, T1 / 2 from tissues - 36-54 hours. It is excreted by the kidneys and through the intestines, penetrates into breast milk.
After instillation into the conjunctival sac, it penetrates well into the epithelium of the cornea and the conjunctiva, while therapeutic concentrations of drugs are created in the aqueous humor of the eye. With inflammation or damage to the mucous membrane, the rate of penetration increases.
Application of the substance Dexamethasone
For systemic use (parenteral and oral)
Shock (burn, anaphylactic, post-traumatic, postoperative, toxic, cardiogenic, blood transfusion, etc.); edema of the brain (including with tumors, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation injury); bronchial asthma, asthmatic status; systemic connective tissue diseases (including systemic lupus erythematosus, rheumatoid arthritis, scleroderma, periarteritis nodosa, dermatomyositis); thyrotoxic crisis; hepatic coma; poisoning with cauterizing fluids (in order to reduce inflammation and prevent scarring); acute and chronic inflammatory diseases of the joints, incl. gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis, periarthritis of the shoulder scapula, ankylosing spondylitis (ankylosing spondylitis), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tendosynovitis, synovitis, epicondylitis; rheumatic fever, acute rheumatic heart disease; acute and chronic allergic diseases: allergic reactions to drugs and foods, serum sickness, urticaria, allergic rhinitis, hay fever, angioedema, drug exanthema; skin diseases: pemphigus, psoriasis, dermatitis (contact dermatitis affecting a large surface of the skin, atopic, exfoliative, bullous herpetiformis, seborrheic, etc.), eczema, toxidermia, toxic epidermal necrolysis (Lyell's syndrome), malignant exudative erythema (Stevens-Jones syndrome ); allergic eye diseases: allergic corneal ulcers, allergic forms of conjunctivitis; inflammatory eye diseases: sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis; primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands); congenital adrenal hyperplasia; kidney disease of autoimmune genesis (including acute glomerulonephritis), nephrotic syndrome; subacute thyroiditis; diseases of the hematopoietic organs: agranulocytosis, panmyelopathy, anemia (including autoimmune hemolytic, congenital hypoplastic, erythroblastopenia), idiopathic thrombocytopenic purpura, secondary thrombocytopenia in adults, lymphoma (Hodgkin's, non-Hodgkin's, lymphoma), leukemia lung diseases: acute alveolitis, pulmonary fibrosis, sarcoidosis II – III stage; tuberculous meningitis, pulmonary tuberculosis, aspiration pneumonia (only in combination with specific therapy); beryllium disease, Loeffler's syndrome (resistant to other therapy); lung cancer (in combination with cytostatics); multiple sclerosis; diseases of the gastrointestinal tract (to remove the patient from a critical state): ulcerative colitis, Crohn's disease, local enteritis; hepatitis; prevention of graft rejection reaction; tumor hypercalcemia, nausea and vomiting during cytostatic therapy; multiple myeloma; conducting a test in the differential diagnosis of hyperplasia (hyperfunction) and tumors of the adrenal cortex.
For topical use
Intra-articular, periarticular. Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, Reiter's disease, osteoarthritis (in the presence of pronounced signs of joint inflammation, synovitis).
Conjunctival. Conjunctivitis (non-purulent and allergic), keratitis, keratoconjunctivitis (without damage to the epithelium), iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, episcleritis, scleritis, uveitis of various genesis, retinitis, neuritis of the superficial epulbaric neurology, retinitis cornea), inflammation after eye injuries and eye operations, sympathetic ophthalmia.
Into the external auditory canal. Allergic and inflammatory ear diseases, incl. otitis.
Dexamethasone in sports
Due to a sharp decrease in the secretion of catabolic hormones, in particular - cortisol, metabolism while taking dexamethasone sharply shifts towards anabolism. Against the background of even small doses of androgens, this can lead to significant gains in muscle mass. Sometimes weight gain goes only along the fatty pathway (dexamethasone increases the synthesis of fatty acids). And it is also possible to suppress the secretion of testosterone, which outside the "course" of AAS can simply result in a catastrophic "collapse" of muscle mass. So, if you have already decided on the use of dexamethasone, do it only against the background of the use of androgens and anabolic steroids. The use of dexamethasone also leads to a faster recovery after exercise - again by suppressing the secretion of catabolic hormones. So for strength athletes, it can be a very useful drug.
Very often sports are accompanied by pain in the joints or tendons, and this drug comes to the rescue, which has a high anti-inflammatory effect. He is able to eliminate all pains in just 24 hours. Regardless of their causality and local location.
If you use Dexamethasone slightly more than the minimum dosage, then it begins to retain water in the body. And with a small water retention in the body (somewhere between 1000-2000 ml), the lubricity of the joints improves, which has a positive effect on them. But with increasing dosage, water retention increases, which is accompanied by such negative effects as increased pressure and sluggishness.
Dexamethasone is suitable for those with a poor appetite. Since the more you eat. The faster you recover from workouts and the faster you gain muscle mass.
Dosage
In the case of using dexamethasone in bodybuilding, it is very important not to overdo the dosages. In this case, "more" only means "worse" - side effects begin to "come out" with just the same incredible force. In any case, it is worth stopping at the minimum - 0.5-1.5 mg (1-3 tablets) per day. The daily dose is taken once a day - in the morning after a meal, on the day free from training, or again after a meal, an hour and a half hours before training. During the "course" of dexamethasone, you should not use exogenous growth hormone, due to the ability of dexamethasone to greatly weaken the effect of the latter. Acceptance of dexamethasone should be carried out in short "courses" - it is better that their duration does not exceed 2-3 weeks. The most justified is the use of dexamethasone only on training days. In this case, it can be applied over a longer period of time.
Interaction
Reduce the therapeutic and toxic effects of barbiturates, phenytoin, rifampicin (speed up metabolism), growth hormone, antacids (reduce absorption), increase - estrogen-containing oral contraceptives, the risk of arrhythmias and hypokalemia - cardiac glycosides and diuretics, the likelihood of edema - and arterial hypertension severe hypokalemia, heart failure and osteoporosis - amphotericin B and carbonic anhydrase inhibitors, the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract - NSAIDs.
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. Weakens the hypoglycemic activity of insulin and oral antidiabetic agents, anticoagulant - coumarins, diuretic - diuretics, immunotropic - vaccination (suppresses antibody production). It impairs the tolerance of cardiac glycosides (causes potassium deficiency), reduces the concentration of salicylates and praziquantel in the blood.
SIDE EFFECTS
With regard to sports practice, a very unpleasant phenomenon is the increased risk of osteoporosis - fragility of bones may increase due to the fact that the drug exhibits an antagonistic effect in relation to vitamin D (there is a "leaching" of calcium from the bones). Also, with long-term use of dexamethasone, the ligaments not only become elastic, but soften, which, of course, should also be avoided.
Dexamethasone cannot be recommended for those who have a tendency to diabetes, and even more so for those suffering from this disease - the use of this drug increases insulin resistance. You should not use the drug for stomach or duodenal ulcers, as well as for renal failure. During infectious diseases, taking dexamethasone should be stopped.
