Trade name of the drug: Dexamethasone Active ingredient (INN): sodium dexamethasone phosphate Dosage form: solution for injection Composition: 1 ml of the drug contains: active substance: dexamethasone sodium phosphate (equivalent to dexamethasone phosphate 4.00 mg); excipients: sodium methylparaben (as a preservative) 1,8 mg, sodium propylparaben (as a preservative)..0.2 mg, water for injection up to 1.00 ml. Description: transparent colorless liquid. Pharmacotherapeutic group: Glucocorticosteroid. ATX Code: H02AB02
Pharmacological properties Pharmacodynamics Synthetic glucocorticoid (GCS), a methylated derivative of fluoroprednisolone. It has an anti-inflammatory, anti-allergic, immunosuppressive effect, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines. It interacts with specific cytoplasmic receptors (there are receptors for GCS in all tissues, especially a lot of them in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells.) Protein metabolism: reduces the amount of globulins in plasma, increases the synthesis of albumins in the liver and kidneys (with an increase in the albumin/globulin ratio), reduces the synthesis and enhances protein catabolism in muscle tissue. Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia. Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase (increased glucose intake from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia. Water-electrolyte metabolism: delays Na+ and water in the body, stimulates the excretion of K+ (mineralocorticoid activity), reduces the absorption of Ca+ from the gastrointestinal tract, reduces the mineralization of bone tissue. The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells; inducing the formation of lipocortins and reducing the number of mast cells producing hyaluronic acid; with a decrease in capillary permeability; stabilization of cell membranes (especially lysosomal) and organelle membranes. It acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin inhibits phospholipase A2, inhibits the release of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, contributing to the processes of inflammation, allergies, etc.), the synthesis of "pro-inflammatory cytokines" (interleukin 1, tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors. The immunosuppressive effect is caused by the involution of lymphoid tissue, inhibition of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T- and B-lymphocytes, inhibition of the release of cytokines (interleukin-1, 2; gamma interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies. The antiallergic effect develops as a result of reducing the synthesis and secretion of allergy mediators, inhibiting the release of histamine and other biologically active substances from sensitized mast cells and basophils, reducing the number of circulating basophils, T- and B-lymphocytes, mast cells; suppressing the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to allergy mediators, inhibiting antibody formation, changes in the immune response of the body. In obstructive diseases of the respiratory tract, the effect is mainly due to inhibition of inflammatory processes, prevention or reduction of the severity of edema of the mucous membranes, reduction of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of small and medium-sized bronchial beta-adrenoreceptors to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production. Suppresses the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous GCS. Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation. The peculiarity of the action is a significant inhibition of pituitary function and the almost complete absence of mineralocorticosteroid activity. Doses of 1-1.5 mg / day inhibit the function of the adrenal cortex; the biological half-life is 32-72 hours (the duration of suppression of the hypothalamus-pituitary-adrenal cortex). According to the strength of glucocorticoid activity, 0.5 mg of dexamethasone corresponds to approximately 3.5 mg of prednisone (or prednisone), 15 mg of hydrocortisone or 17.5 mg of cortisone. Pharmacokinetics It binds in the blood (60-70%) with a specific carrier protein - transcortin. It easily passes through histohematic barriers (including through hemato-encephalic and placental). It is metabolized in the liver (mainly by conjugation with glucuronic and sulfuric acids) to inactive metabolites. It is excreted by the kidneys (a small part - by the lactating glands). T1/2 dexamethasone from plasma - 3-5 hours.
Indications for use Diseases requiring the introduction of fast−acting GCS, as well as cases when oral administration of the drug is impossible: - endocrine diseases: acute insufficiency of the adrenal cortex, primary or secondary insufficiency of the adrenal cortex, congenital hyperplasia of the adrenal cortex, subacute thyroiditis; − shock (burn, traumatic, surgical, toxic) - with the ineffectiveness of vasoconstrictors, plasma replacement drugs and other symptomatic therapy; − cerebral edema (with a brain tumor, traumatic brain injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, radiation damage); − asthmatic status; severe bronchospasm (exacerbation of bronchial asthma, chronic obstructive bronchitis); − severe allergic reactions, anaphylactic shock; − rheumatic diseases; − systemic connective tissue diseases; − acute severe dermatoses; − malignant diseases: palliative treatment of leukemia and lymphoma in adult patients; acute leukemia in children; hypercalcemia in patients suffering from malignant tumors, if oral treatment is not possible; − blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults; − severe infectious diseases (in combination with antibiotics); − in ophthalmological practice (subconjunctival, retrobulbar or parabulbar administration): allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharitis, blepharoconjunctivitis, scleritis, episcleritis, inflammatory process after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after corneal transplantation; − local application (in the field of pathological education): keloids, discoid lupus erythematosus, annular granuloma.
Method of administration and dosage The dosage regimen is individual and depends on the indications, the patient's condition and his reaction to therapy. The drug is administered intravenously slowly in a jet or drip (in acute and urgent conditions); in / m; local (in pathological formation) administration is also possible. In order to prepare a solution for intravenous infusion, an isotonic sodium chloride solution or a 5% dextrose solution should be used. In the acute period with various diseases and at the beginning of therapy, Dexamethasone is used in higher doses. During the day, you can inject from 4 to 20 mg of Dexamethasone 3-4 times. Doses of the drug for children (in / m): The dose of the drug during replacement therapy (in case of adrenal cortex insufficiency) is 0.0233 mg / kg of body weight or 0.67 mg / m2 of body surface area, divided into 3 doses, every 3rd day or 0.00776 - 0.01165 mg / kg of body weight or 0.233 - 0.335 mg / m2 of body surface area daily. For other indications, the recommended dose ranges from 0.02776 to 0.16665 mg/ kg of body weight or 0.833 - 5 mg/ m2 of body surface area every 12-24 hours. When the effect is achieved, the dose is reduced to maintenance or to discontinuation of treatment. The duration of parenteral administration is usually 3-4 days, then they switch to maintenance therapy with dexamethasone in tablets. Long-term use of high doses of the drug requires a gradual dose reduction in order to prevent the development of acute insufficiency of the adrenal cortex.
Side effects Dexamethasone is usually well tolerated. It has low mineralocorticoid activity, i.e. its effect on water-electrolyte metabolism is small. As a rule, low and medium doses of Dexamethasone do not cause sodium and water retention in the body, increased potassium excretion. The following side effects are described: From the endocrine system: decreased glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, suppression of adrenal function, Itsenko-Cushing syndrome (moon-shaped face, pituitary type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delayed sexual development in children. From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal tract wall, increased or decreased appetite, violationdigestion, flatulence, hiccups. In rare cases, increased activity of hepatic transaminases and alkaline phosphatase. From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of heart failure, changes on the electrocardiogram characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle. From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor of the cerebellum, headache, convulsions. From the sensory organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, a tendency to develop secondary bacterial, fungal or viral eye infections, trophic changes in the cornea, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, nasal conchs, scalp, deposition of crystals of the drug in the vessels is possible eyes). From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased breakdown of proteins), increased sweating. Caused by mineralocorticoid activity - fluid and sodium retention (peripheral edema), hypocrine anemia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue). From the musculoskeletal system: slowing down of growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur), muscle tendon rupture, steroid myopathy, decreased muscle mass (atrophy). From the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, a tendency to develop pyoderma and candidiasis. Allergic reactions: skin rash, itching, anaphylactic shock, local allergic reactions. Local with parenteral administration: burning, numbness, pain, tingling at the injection site, infections at the injection site, rarely - necrosis of surrounding tissues, scarring at the injection site; atrophy of the skin and subcutaneous tissue during intravenous administration (especially dangerous injection into the deltoid muscle). Others: the development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, "flushes" of blood to the face, "withdrawal" syndrome.
Contraindications For short-term use for vital indications, the only contraindication is hypersensitivity to dexamethasone or the components of the drug. In children during the growth period, GCS should be used only according to absolute indications and under the very careful supervision of the attending physician. With caution , the drug should be prescribed for the following diseases and conditions: − gastrointestinal diseases - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, recently created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess, diverticulitis; − parasitic and infectious diseases of viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chickenpox, measles; amoebiasis, strongyloidosis; systemic mycosis; active and latent tuberculosis. Use in severe infectious diseases is permissible only against the background of specific therapy. − pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination; − diseases of the cardiovascular system (including recent myocardial infarction - in patients with acute and subacute myocardial infarction, the spread of the necrosis focus, slowing of scar tissue formation and, consequently, rupture of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia is possible); − endocrine diseases - diabetes mellitus (including impaired tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, obesity (III-IV art.) − severe chronic renal and/or hepatic insufficiency, nephrourolithiasis; − ischemic osteoporosis, myasthenia gravis, acute psychosis, polio (except for the form of bulbar encephalitis), open- and closed-angle glaucoma;
Drug interactions Pharmaceutical incompatibility of dexamethasone with other intravenous drugs is possible - it is recommended to administer it separately from other drugs (in / in bolus, or through another dropper, as a second solution). When dexamethasone solution is mixed with heparin, a precipitate is formed. Simultaneous administration of dexamethasone with: inducers of hepatic microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration; diuretics (especially thiazide and carbonic anhydrase inhibitors) and amphotericin B - may lead to increased excretion of K+ from the body and increase the risk of heart failure; with sodium-containing drugs - to the development of edema and increased blood pressure; cardiac glycosides - their tolerability worsens and the likelihood of ventricular extrasitol development increases (due to hypokalemia caused); indirect anticoagulants - weakens (less often strengthens) their effect (dose adjustment is required); anticoagulants and thrombolytics - increases the risk of bleeding from ulcers in the gastrointestinal tract; ethanol and NSAIDs - the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs in the treatment of arthritis, it is possible to reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect); paracetamol - increases the risk of hepatotoxicity (induction of liver enzymes and the formation of a toxic metabolite of paracetamol); acetylsalicylic acid - accelerates its excretion and reduces the concentration in the blood (with the abolition of dexamethasone, the level of salicylates in the blood increases and the risk of side effects increases); insulin and oral hypoglycemic drugs, hypotensive agents - their effectiveness decreases; vitamin D - reduces its effect on the absorption of Ca2+ in the intestine; somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration; M-holinoblockers (including antihistamines and tricyclic antidepressants) and nitrates - helps to increase intraocular pressure; isoniazid and mexiletine - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations. Carbonic anhydrase inhibitors and loop diuretics may increase the risk of osteoporosis. Indomethacin, displacing dexamethasone from the connection with albumins, increases the risk of its side effects. ACTH enhances the effect of dexamethasone. Ergocalciferol and parathyroid hormone prevent the development of osteopathy caused by dexamethasone. Cyclosporine and ketoconazole, slowing down the metabolism of dexamethasone, can in some cases increase its toxicity. Simultaneous administration of androgens and steroid anabolic drugs with dexamethasone contributes to the development of peripheral edema and hirsutism, the appearance of acne.
Special instructions During Dexamethasone treatment (especially long-term), it is necessary to monitor the oculist, monitor blood pressure and the state of the water-electrolyte balance, as well as the picture of peripheral blood and blood glucose levels. In order to reduce side effects, antacids can be prescribed, and the intake of K + in the body (diet, potassium preparations) should also be increased. The food should be rich in proteins, vitamins, with a limited content of fats, carbohydrates and table salt. The effect of the drug is enhanced in patients with hypothyroidism and cirrhosis of the liver. The drug may increase existing emotional instability or psychotic disorders. When indicating a history of psychosis, Dexamethasone in high doses is prescribed under strict medical supervision. With caution, it should be used in acute and subacute myocardial infarction - it is possible to spread the focus of necrosis, slow down the formation of scar tissue and rupture of the heart muscle. In stressful situations during supportive treatment (for example, surgical operations, trauma or infectious diseases), the dose of the drug should be adjusted due to an increased need for glucocorticosteroids. Patients should be carefully monitored for a year after the end of long-term therapy with Dexamethasone due to the possible development of relative insufficiency of the adrenal cortex in stressful situations. With sudden withdrawal, especially in the case of previous use of high doses, it is possible to develop a "withdrawal" syndrome (anorexia, nausea, lethargy, generalized musculoskeletal pain, general weakness), as well as an exacerbation of the disease for which Dexamethasone was prescribed. During treatment with Dexamethasone, vaccination should not be carried out due to a decrease in its effectiveness (immune response). Prescribing Dexamethasone for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously treat with bactericidal antibiotics. In children, during long-term treatment with Dexamethasone, careful monitoring of the dynamics of growth and development is necessary. Children who have been in contact with patients with measles or chickenpox during treatment are prophylactically prescribed specific immunoglobulins. As a result of weak mineralocorticoid, the enhancer may be used in combination with mineralocorticoid therapies. In the hospital, extravehicular diabetoma follow the control of blood glucose. Radiological control for the bone system is shown (photos, cysts). In the hospital, the patient was diagnosed with latent extravehicular infestations in the hospital, which may be of diagnostic importance. Dexamethasone was subsequently found to be metabolite 11 - and 17-oxyketocorticosteroid. Changes in steering and steering During pregnancy (especially in the first trimester), the drug can be used only when the expected therapeutic effect exceeds the potential risk to the fetus. In the case of oral therapies in the period of pregnancy, there is no possibility of fetal growth disorders. In the case of changes in the thread, there is a danger of atrophy of the root in the fetus, which may require the replacement therapies in the newborns. It is necessary to conduct the treatment of the preparation in the time of the tuber inskarming, it is the steering of the tuber after the termination.
Peredosis Possible amplification described in Urgench in extravehicular. You need to take dexamethasone. Treatment symptomatic.
Shape in aposematic 4 mg / mL in ampoule of 1 ml. On the Pyat ampul in contour-yacheykovuyuyu packakovka in plenki PVH and folgi alyuminiyevoy. Pyat contour-yacheykov penghakovok is housed in korobku, 25 ampul instead with instructions on medical procedure.
Feeding conditions Eat in the shelter of the world, at a temperature not in Urgench 25. Eat in an uncomplicated place.
Period meals 2 years. Do not change the actual length of time.
Terms of leave from pharmacy Recipe.
Manufacturer HARASHA PHARMA PVT. LTD., India
Owner registration certificates HARASHA PHARMA PVT. LTD., India
Name and address organizations making claims (proposals) for quality medicinal products of territories Republic of Uzbekistan «FUTURE-WORLD GROUP» Republic of Uzbekistan, Tashkent, Chilanzarsky r-n, str. Sanyat 13A. Tel.:+99891 134 94 14 E-mail: info.fwg@yandex.com
