Dexamethasone refers to synthetic drugs that are analogues of the hormones of the adrenal cortex - glucocorticosteroids. The action of the drug is similar to another hormone preparation - Prednisolone. Dexamethasone is produced by fluoridation and methylation of prednisolone.
So, let's talk about dexamethasone( in ampoules for injections, tablets, drops, etc.) of its instructions for use, price, reviews and analogues.
Features of the preparation
Composition of Dexamethasone
The main substance of the drug Dexamethasone is dexamethasone sodium phosphate, the amount of which is 4 mg per 1ml solution. Ampoules of dark glass contain 2 ml of solution, packed in cardboard boxes of 5 or 10 pieces( plastic boxes of 5 pieces).
Auxiliary substances of the injection solution are methyl and propyl derivatives of paraben, distilled water for injection, sodium salts of edetate and metabisulphite, sodium hydroxide.
Forms of dexamethasone release
Dexamethasone is registered in the following dosage forms:
- Ampoules with an injection solution for intramuscular and intravenous infusion of 2 ml.
- Dexamethasone tablets of 0.5 mg each.
- In ophthalmology - Oftan - 0,1% solution( eye drops).
- Glazed drops Dexamethasone with an active substance concentration of 0.1%.
Pharmacological action
Dexamethasone - a powerful immunosuppressant, has anti-inflammatory and anti-allergic effect. In the presence of the active substance, the receptor sensitivity of β-adrenoreceptors to adrenaline and norepinephrine produced by the adrenal medulla is increased.
- The drug activates the interaction with the cell membrane receptors, leading to the synthesis of proteins and enhancing the enzymatic activity. The greatest number of β-adrenergic receptors, dependent on Dexamethasone, is observed in the liver tissues.
- Protein metabolism. In muscle tissue, the breakdown of proteins is intensified against the background of a decrease in their synthesis. In the liver and kidneys, the ratio of albumins and globulins shifts toward the formation of albumins. In blood plasma, an increase in albumin synthesis and inhibition of the formation of globulins are also found.
- Lipid metabolism. Stimulates the synthesis of lipids from glycerol and higher fatty acids, promotes the development of hyperlipidemia. There is a redistribution of fat mass with its displacement in the body from the lower parts of the body( thighs, buttocks, pelvis) to the upper parts( face, chest and abdomen).
- Metabolism of carbohydrates. Stimulates active absorption of glucose in intestinal villi and gastric mucosa, removes glycogen from the liver and muscles into the blood, causing hyperglycemia. Activates the enzymatic activity of glucose-6-phosphatase, aminotransferases and phosphoenolpyruvate carboxylase.
- Metabolism of water and mineral elements. Promotes active retention of water and sodium ions in the body, increased renal excretion of potassium and calcium salts. Calcium ions are absorbed in the digestive system weaker, the process of mineralization of bone plates begins.
- Relieves inflammatory processes by reducing the synthesis of eosinophils and mast cells producing inflammatory mediators. Stimulates the synthesis of arachidonic acid, interleukin 1, prostaglandins. Increases the resistance of the cell membrane to chemical damage.
- The antiallergic and immunosuppressive effect of Dexamethasone is to reduce the differentiation of T-lymphocytes on suppressors, helpers and killers, decrease the interaction reactions of T and B lymphocytes, inhibit the activity of interleukin 2 and γ-interferon, and decrease the secretion of antibodies. There is an involution of lymphoid tissue, a decrease in the synthesis of mast cells and inhibition of secretion by basophils of mediators of allergy, histamine, etc. The result of the action of Dexamethasone is the transformation of the immune response.
The following video tells in some detail about the action of Dexamethasone:
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Pharmacodynamics
One ampoule of Dexamethasone causes oppression of the hypothalamic-pituitary-glcocortical system for 3 days. In an equivalent ratio, 0.5 mg of dexamethasone corresponds to the action of 3.5 mg of prednisolone, 15 mg of hydrocortisone, or 17.5 mg of Cortisone.
Pharmacokinetics
In the blood plasma, Dexamethasone binds to the transporterin transport protein. Hematoencephalic and hematoplacental barriers are not retained. Decomposition of the drug substance is made by the liver before the complex compound of glucuronic and sulfuric acids.
The half-life of the hormonal drug is 5 hours. Excretion of the inactive metabolite is via the mammary glands( during feeding) and excretory system.
And now let's find out what dexamethasone is for.
Indications
Intramuscular injection of a hormonal drug is performed in conditions of impossibility of oral intake or hormone replacement therapy in acute shortage of glucocorticosteroids. This occurs in the following cases:
- of hormonal abnormalities with a deficiency of the adrenal cortex, inflammation in the thyroid gland - subacute thyroiditis;
- shock therapy with the inefficient effect of antispasmodics and other agents that remove the symptoms of shock;
- neurological surgeries, brain trauma, other types of brain damage with the symptom of puffiness;
- attacks of bronchial asthma and acute obstructive bronchitis;
- severe allergy with a threat of anaphylactic shock;
- acute leakage of dermatoses;
- rheumatism of various organs;
- pathologies of connective tissue development;
- agranulocytosis and other hematological pathologies;
- malignant neoplasms, in children with malignant systemic hemoblastosis;
- severe course of stagnant phenomena in the lungs and infectious processes;
- topical use during lupus erythematosus, etc.;
- in the practice of oculists in the treatment of inflammation of many structures of the eyeball and mucous membranes.
Pregnant women may receive dexamethasone in case of:
- the threat of premature birth;
- of a rare hereditary disease of the fetus - underdevelopment of the cortical layer of the adrenal glands;
- anaphylactic shock and other conditions of each person falling into the conditions of a threat to life.
Instruction for use
The drug is administered by intramuscular or intravenous infusion. In the case of drip administration, Dexamethasone is mixed in a solution of dextrose or isotonic sodium chloride solution.
Local application is possible. The maximum daily dose of a hormonal drug is 20 mg per day. The daily dose is divided 3-4 times. In the initial treatment period, the dosage of dexamethasone increases until the desired effect is achieved, in the future the dose is reduced. The possibility of prolonged use is limited because of the threat of atrophy of the cortical layer of the adrenal glands.
The video below provides instructions for the use of Dexamethasone in the form of eye drops:
Contraindications
The drug is contraindicated for individual intolerance and severe hepatic insufficiency. With special care and vigilant control of the attending physician drug dexamethasone is administered to women during pregnancy, children and adults with:
- pathologies of the digestive system ulcerative;
- infectious diseases;
- for people with HIV and AIDS;
- chronic liver and kidney disease;
- cardiovascular pathologies, especially during the course of acute myocardial infarction;
- disorders of hormonal secretion;
- period before and after vaccination of lymphadenitis and brucellosis;
- osteoporosis, glaucoma.
Side effects of
Usually no side effects from dexamethasone from the body's somatic systems are observed.
- In some cases, exacerbations of diabetes mellitus, hypertension, delayed sexual development are noted.
- On the part of the gastrointestinal tract, disorders and perforation of the mucous membranes of the digestive organs are sometimes noted.
- Local allergic reaction, slow healing of wounds, excessive sweating, increased excretion of calcium, increased fatigue are not excluded.
Special instructions
High doses of Dexamethasone are prescribed with close supervision by the attending physician. After discontinuing the drug, be sure to monitor the patient's well-being in a clinical setting.
During the use of the drug should adhere to the diet and monitor the enrichment of the diet with calcium, potassium and proteins.
Reviews
Reviews and comments of doctors and patients, when they are summarized, speak about the rapid action of the drug. But associated with the unprofessional administration of the drug face and neck redness may be associated with too rapid injection.
The following video presents a review of Dexamethasone from a woman with severe joint pain:
Analogues
In total, there are 31 analogues of Dexamethasone. The most popular of them are Oftan Dexamethasone, Dexacort, Dexazon, Maxidex, etc.