Dexamethasone solution for intravenous and intramuscular administration of 4 mg ampoules 1 ml 25 pcs
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Active ingredients
Dexamethasone
Release form
Solution
Composition
Active ingredient: Dexamethasone (Dexamethasone) Active ingredient concentration (mg): 4
Pharmacological effect
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 the release of ACTH pituitary and β-lipotropin, but does not reduce the level of circulating β-endorphin. It inhibits the secretion of TSH and FSH. When directly applied to the vessels, it 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 lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term therapy of corticosteroids.As a result of the catabolic action, growth suppression in children is possible. At 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, therapeutic activity of dexamethasone is due to anti-inflammatory, antiallergic, immunosuppressive and anti-proliferative effect. ) action. By anti-inflammatory ak exceeds hydrocortisone by 30 times, does not possess mineralocorticoid activity.
Pharmacokinetics
Plasma protein binding is 60-70%. Penetrates histohematogenous barriers. In a small amount excreted in breast milk. Metabolized in the liver. T1 / 2 is 2-3 hours. It is excreted by the kidneys. When applied locally in ophthalmology, it is absorbed through the cornea with the intact epithelium into 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.
Indications
Increased nervous irritability, insomnia, irritability.
Contraindications
For short-term use for vital reasons, the only Contraindications are hypersensitivity. For intra-articular administration: previous arthroplasty, pathological bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture of the bone, infectious (septic) inflammation in the joint and periarticular infections (including). history), as well as a common infectious disease, marked periarticular osteoporosis, the absence of signs of inflammation in the joint (so-called dry joint, for example in osteoarthritis without synovitis), severe bone destruction and joint deformity (sharp joint space narrowing, ankylosis), joint instability as an outcome of arthritis, aseptic necrosis of bone-forming epiphyses.
Use during pregnancy and lactation
With caution should be used for parasitic and infectious diseases of viral, fungal or bacterial nature (currently or recently transferred, including recent contact with the patient) - herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amebiasis, strongyloidosis (established or suspect), systemic mycosis; active and latent tuberculosis. Use in severe infectious diseases is permissible only against the background of specific therapy. It should be used with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, and with immunodeficiency states (including AIDS or HIV infection). С caution should be used in diseases of the gastrointestinal tract: gastric ulcer and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, a newly created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscessing, diverticulitis. It should be used with caution in diseases of the cardiovascular system, including after a recent myocardial infarction (patients with acute and subacute myocardial infarction may spread necrosis, slow the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, hypertension, hyperlipidemia), with endocrine diseases - diabetes mellitus ( including violation of tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and / or liver failure, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, myasthenia, acute psychosis, obesity (III-IV degree), with polio (except for the form of bulbar encephalitis), open-and-closed-angle glaucoma. caution should be used in patients with general severe condition, inefficiency (or short duration) of the action of 2 previous injections (taking into account the individual properties of the used GCS). Before and during treatment of corticosteroids, it is necessary to control the complete blood count, glycemia level and electrolyte content in plasma. In intercurrent infections,septic conditions and tuberculosis; simultaneous antibiotic therapy is necessary. Dexamethasone-induced relative adrenal insufficiency may persist for several months after its withdrawal. Given this, when stressful situations occur during this period, hormone therapy is resumed with the simultaneous appointment of salts and / or mineralocorticoids. When using dexamethasone in patients with herpes, the cornea should be borne in mind that it can be perforated. During treatment, it is necessary to control intraocular pressure and the state of the cornea. When dexamethasone is abruptly canceled, especially in the case of previous 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, relative adrenal insufficiency may persist. If during this period there are stressful situations, they are prescribed (if indicated) for the time of GCS, if necessary in combination with mineralocorticoids. In the period of treatment, control of blood pressure, water and electrolyte balance, pictures of peripheral blood and blood glucose levels, as well as observation of an oculist are required. during prolonged 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.
Dosage and administration
Intra-articular, in the lesion - 0.2–6 mg, repeated 1 time in 3 days or 3 weeks. Intra-intramuscularly or intravenously - 0.5–9 mg / day. For the treatment of cerebral edema - 10 mg in the first injection, later 4 mg intramuscularly every 6 hours until symptoms disappear. The dose can be reduced in 2-4 days with a gradual abolition in the period of 5-7 days after elimination of cerebral edema. The maintenance dose is 2 mg 3 times / day. For the treatment of shock - intravenous 20 mg in the first injection, then 3 mg / kg for 24 hours in the form of intravenous infusions or intravenous fluids - from 2 to 6 mg / kg as a single injection or 40 mg as a single injection, administered every 2-6 hours; perhaps intravenous administration of 1 mg / kg once.Shock therapy should be canceled as soon as the patient's condition stabilizes, the usual duration is no more than 2-3 days. Allergic diseases - intramuscularly in the first injection of 4-8 mg. Further treatment is carried out with oral dosage forms. For nausea and vomiting, during chemotherapy, 8-20 mg intravenously, 5-15 minutes before the chemotherapy session. Further chemotherapy should be carried out using oral dosage forms. For the treatment of respiratory distress syndrome of the newborn - intramuscularly 4 administrations of 5 mg every 12 hours for two days. The maximum daily dose is 80 mg. For children: for the treatment of adrenal insufficiency - intramuscularly of 23 mg / kg (0.67 mg / sq. m) every 3 days, or 7.8-12 mg / kg (0.23-0.34 mg / sq. m / day), or 28-170 mg / kg (0.83-5 mg / sq m) every 12-24 hours
Side effects
With simultaneous use with antipsychotics, bukarbanom, azathioprine, there is a risk of developing cataracts; with anticholinergic agents - risk of developing glaucoma. When used simultaneously with dexamethasone, the effectiveness of insulin and oral hypoglycemic drugs is reduced. When used simultaneously with hormonal contraceptives, androgens, estrogens, anabolic steroids, hirsutism, acne, and chromomas are possible. excretion of potassium; with NSAIDs (including acetylsalicylic acid) - the incidence of erosive and ulcerative lesions and bleeding from the gastrointestinal tract increases. If used simultaneously with oral anticoagulants, a weakening of the anticoagulant effect is possible. potassium deficiency. When used simultaneously with aminoglutethimide, it is possible to reduce or inhibit the effects of dexamethasone; with carbamazepine - may decrease the action of dexamethasone; with ephedrine - increased excretion of dexamethasone from the body; with imatinib - a decrease in plasma concentration of imatinib is possible due to the induction of its metabolism and an increase in excretion from the body. With simultaneous use of itraconazole, the effects of dexamethasone are enhanced; with methotrexate - may increase hepatotoxicity; with praziquantel - perhaps a decrease in the concentration of praziquantel in the blood. When used simultaneously with rifampicin, phenytoin,barbiturates may weaken the effects of dexamethasone due to the increase in its elimination from the body.
Interaction with other drugs
Precautionary measures
special instructions
The frequency of development and severity of side effects depend on the duration of use, the size of the dose used and the ability to comply with the circadian rhythm of administration. From the side of metabolism: sodium retention and water in the body; hypokalemia; hypokalemic alkolosis; negative nitrogen balance due to increased protein catabolism, increased appetite, weight gain. From the cardiovascular system: a higher risk of thrombosis (especially in immobilized patients), arrhythmias, high blood pressure, development or worsening of chronic heart failure, myocardiodystrophy, Steroid vasculitis. From the musculoskeletal system: muscle weakness, steroid myopathy, muscle loss, osteoporosis, vertebra compression fractures Aseptic necrosis of the femoral head and humeral bones, pathological fractures of the long bones. From the digestive system: nausea, vomiting, erosive and ulcerative lesions of the gastrointestinal tract (which can cause perforations and bleeding), hepatomegaly, pancreatitis, ulcerative esophagitis. Dermatological reactions: thinning and vulnerability of the skin, petechiae and subcutaneous hemorrhages, ecchymosis, stretch marks, steroid acne, delayed wound healing, increased sweating. From the central nervous system: increased uma dizziness, dizziness, headache, mental disorders, convulsions and false symptoms of a brain tumor (increased intracranial pressure with a stagnant optic nerve head). On the part of the endocrine system: reduced glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes, adrenal gland function Itsenko-Cushing syndrome (moon face, pituitary type obesity, hirsutism, high blood pressure, dysmenorrhea, amenorrhea, myasthenia, strii), delayed sexual development detey.So in the organs of: posterior subcapsular cataracts, increased intraocular pressure, ekzoftalm.Pobochnye effectsassociated with immunosuppressive action: more frequent occurrence of infections and aggravation of their severity. Others: allergic reactions. Local reactions (at the injection site): hyperpigmentation and leukoderma, atrophy of the subcutaneous tissue and skin, aseptic abscess, hyperemia at the injection site, arthropathy.