sustanon steroid


Sustanon steroid- methylated derivative ftorprednizolona. Has anti-inflammatory, antiallergic, desensitizing, immunosuppressive, antishock and antitoxic action, increases the sensitivity of the beta-adrenergic receptors to endogenous catecholamines. Interacts sustanon steroid with specific cytoplasmic receptors (receptors for glucocorticosteroids have all tissues, many of them especially in the liver) to form a complex that induces the formation of proteins (including enzymes, to regulate vital cell processes.)
The protein sharing reduces the amount of globulin plasma albumin increases synthesis in the liver and kidneys (with increase of 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 (mobilization of the subcutaneous tissue of limbs and fat accumulation mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
Carbohydrate metabolism : It contributes to the development of hyperglycemia. Water-eletrolitny sharing delays Na + and water in the body, stimulate the excretion of K + (mineralocorticoid activity) reduces the absorption of Ca2 + from the gastrointestinal tract, causing “washout” of bone calcium, and increasing its renal excretion, reduces bone mineralization.
Anti-inflammatory effect associated with inhibition of the release of eosinophils and mast cell mediators of inflammation; lipokortinov inducing formation and reduce the number of mast cells that produce hyaluronic acid; with sustanon steroid decreasing capillary permeability; stabilization of cell membranes (particularly lysosomal) membranes and organelles. Acts on all phases of the inflammatory process: inhibits prostaglandin synthesis (Pg) to arachidonic acid level (Lipokortin inhibits phospholipase A2 suppresses liberatiou arachidonic acid inhibits the biosynthesis endoperekisey, leukotrienes promoting inflammation, allergies, etc.), Synthesis of “proinflammatory cytokine” ( interleukin 1, tumor necrosis factor alpha, and others).; increases the stability of the cell membrane to the action of various damaging factors.
Immunosuppressive effect is due to the called involution of lymphoid tissue, inhibition of lymphocyte proliferation (especially T cells), suppression of the migration of B cells, and the interaction of T and B lymphocytes, inhibition of the release of cytokines (IL-1, 2;. gamma interferon) of lymphocytes and macrophages and the decrease in antibody formation
Antiallergic effect is due to a decrease of synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils, histamine and other biologically active substances, reducing the number of circulating basophils suppress development. lymphoid and connective tissues, reduce the number of T and B lymphocytes, mast cells, effector cells, reducing sensitivity to the mediators of allergy, inhibition of antibody production, changes in the immune response.
In obstructive diseases of action lies principally in the airways, the inflammation inhibition, prevention or a decrease in the severity of mucosal edema, reduction of eosinophil infiltration submucosal bronchial epithelium layer and deposition in the bronchial mucosa of circulating immune complexes, as well as braking and erozirovaniya desquamation mucosa. It increases the sensitivity of the beta-adrenergic receptors of the bronchi of small and medium caliber to endogenous catecholamines and exogenous sympathomimetic, reduces the viscosity of mucus by reducing its production. Hinders connective tissue reaction in the course of the inflammatory process and reduces the possibility of the formation of scar tissue.
Inhibits the synthesis and secretion of ACTH and the second – the synthesis of endogenous corticosteroids.
The peculiarity of the action -. A significant inhibition of the pituitary gland and the almost complete lack of activity mineralokortikosteroidnoy
doses of 1-1.5 mg / day oppress the function of the adrenal cortex; biological half-life -. 32-72 hours (the duration of suppression of the hypothalamic-pituitary-adrenal cortical substance)
By virtue of glucocorticoid activity of Sustanon steroid 0.5 mg corresponds to about 3.5 mg of prednisone (or prednisolone), 15 mg of hydrocortisone or cortisone 17.5 mg.

Pharmacokinetics
The blood is associated (60-70%) with specific protein carrier – transcortin. Easily it passes through the blood-tissue barriers (including the blood-brain and placental). It is metabolized in the liver (mainly by conjugation with glucuronic acid and sulfuric acid) to inactive metabolites. Report the news (a small part of -laktiruyuschimi glands). The half-life of Sustanon steroid in plasma – 3-5 hours.

 

Indications for use:

Diseases that require a rapid-acting glucocorticosteroid, as well as cases when oral administration of the drug can not be:

  • endocrine diseases: acute adrenal insufficiency, primary or secondary adrenocortical insufficiency, congenital hyperplasia nadpochechkikov bark, subacute thyroiditis;
  • shock (burns, traumatic, operational, toxic) – the ineffectiveness vasoconstrictor, plasma-drugs and other symptomatic therapy;
  • cerebral edema (swelling of the brain, head trauma, neurosurgical intervention, stroke, encephalitis, meningitis, radiation injury);
  • asthmatic status; severe bronchospasm (exacerbation of asthma, chronic obstructive bronchitis);
  • severe allergic reaction, anaphylactic shock;
  • rheumatic diseases;
  • systemic connective tissue disease;
  • acute severe dermatoses;
  • malignancies: palliative treatment of leukemia and lymphomas in adults; acute leukemia in children; hypercalcemia in patients with malignant tumors, failing oral treatment;
  • blood diseases: acute hemolytic anemia, agranulocytosis, idiopathic thrombocytopenic purpura in adults;
  • severe infectious disease (in conjunction with antibiotics);
  • in ophthalmic practice (subconjunctival, retrobulbar or parabulbarno introduction): allergic conjunctivitis, keratitis, keratoconjunctivitis without epithelial damage, iritis, iridocyclitis, blepharitis, Blepharoconjunctivitis, scleritis, episcleritis, inflammation after eye injuries and surgical interventions, sympathetic ophthalmia, immunosuppressive treatment after transplantation cornea;
  • local application (to the pathological formation): keloids, discoid lupus erythematosus, granuloma annulare.

    Contraindications
    The only contraindication for short-term use for health reasons is the increased sensitivity to Sustanon steroid or components of the drug.
    The children in the period of growth GCS should be used only if absolutely indicated and under particularly close supervision of your doctor.
    Precautions drug should be used for the following diseases and conditions:
    Diseases gastrointestinal tract – stomach and duodenal ulcer disease, esophagitis, gastritis, acute or latent peptic ulcer, recently established intestinal anastomosis, ulcerative colitis, with the threat of perforation or abscess, diverticulitis.
    Parasitic and infectious diseases of viral, fungal or bacterial origin (occurring currently or recently transferred, including the recent contact with a patient) – herpes simplex, herpes zoster (viremicheskaya phase), chicken pox, measles; amoebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis. Application for serious infectious diseases is admissible only against the background of specific therapy.
    Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination. Immunodeficiency (including AIDS or HIV infection).
    Diseases of the cardiovascular system, including recent myocardial infarction (in patients with acute and subacute myocardial infarction may spread necrosis, slowing the formation of scar tissue and, as a consequence – the gap of the heart muscle), severe chronic heart failure, hypertension, hyperlipidemia.
    Endocrine diseases – diabetes (in including breach of tolerance to carbohydrates), hyperthyroidism, hypothyroidism, Cushing’s disease, obesity (III-IV cent.).
    Severe chronic renal and / or hepatic insufficiency, nefrourolitiaz. Hypoalbuminemia and conditions predisposing to its occurrence (liver cirrhosis, nephrotic syndrome).
    Systemic osteoporosis, myasthenia gravis, acute psychosis, polio (excluding the bulbar form of encephalitis), open-and-closure glaucoma, pregnancy.

    Dosage and administration
    Dosage is individual and depends on the indication, the patient’s condition and response to therapy. The drug is administered by slow intravenous bolus or infusion (for acute and urgent conditions);intramuscularly; it is also possible locally (in the pathological formation) administration. In order to prepare the solution for I / drip infusion to be used isotonic sodium chloride or 5% dextrose solution.
    In the acute period in various diseases and early therapy Deksamed used in higher doses. During the day may be administered from 4 to 20 mg 3-4 times Deksameda. Doses for children (intramuscularly)Dose in replacement therapy (for adrenocortical insufficiency) is 0.0233 mg / kg body weight or 0.67 mg / m 2 body surface area, divided into 3 doses every third day or 0,00776-0,01165 mg / kg body weight or 0,233-0,335 mg / m 2 body surface area daily. For other indications the recommended dose is from 0.02776 to 0.16665 mg / kg body weight or 0.833 – 5 mg / m 2 body surface area once every 12-24 hours.Upon reaching effect reduce the dose to maintenance or to discontinuation of treatment. Duration of parenteral use is usually 3-4 days, then move on to maintenance therapy with Sustanon steroid tablets.Long-term use of high doses of the drug requires a gradual reduction of the dose to prevent the development of acute adrenal insufficiency.

    Side effects
    usually Deksamed well tolerated. It has low mineralocorticoid activity, i.e. its effect on water and electrolyte metabolism is low. Typically, the low and medium dose Deksameda not cause a delay of sodium and water in the body, increased excretion of potassium. We describe the following side effects: On the part of the endocrine system: reduction of glucose tolerance, steroid diabetes or a manifestation of latent diabetes mellitus, adrenal suppression, Cushing’s syndrome (moon face, obesity, pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae) delayed sexual development in children. from the digestive system: nausea, vomiting, pancreatitis, steroid stomach ulcers and duodenal ulcers, erosive esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases – increased activity of “liver” transaminases and alkaline phosphatase, Cardio-vascular system: arrhythmia, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased severity of blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction – the spread 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 cerebellum, headache, convulsions. From the senses: the sudden loss of vision (for parenteral administration in the area of the head, neck, nasal turbinate, the scalp may be the deposition of crystals of the drug in the vessels of the eye ), posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, the propensity to develop secondary bacterial, fungal or viral eye infections, trophic changes of the cornea, exophthalmos. On the part of metabolism: increased excretion of calcium, hypocalcemia, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating. Conditional mineralocorticoid activity – delay of fluid and sodium (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue). From the musculoskeletal system:slowing growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rare -patologicheskie fractures, aseptic necrosis of the humeral head and femur), rupture of tendons of muscles, steroid myopathy, reduced muscle mass (atrophy). from the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, acne, striae, susceptibility to the development of pyoderma and candidiasis. allergic reactions: generalized (skin rash, pruritus, anaphylactic shock), local allergic reactions. Local: burning, numbness, pain, tingling, redness at the injection site, infection at the injection site, rarely – necrosis of surrounding tissue, scarring at the injection site; atrophy of the skin and subcutaneous tissue with the / m introduction (especially dangerous administration in the deltoid muscle). Other: development or exacerbation of infection (the appearance of this side effect contribute jointly used immunosuppressants and vaccination), leucocyturia. . syndrome “cancel” on / in the introduction: arrhythmia, “tides” of blood to the face, convulsions.

    Overdose

    may be increased side effects described above. It is necessary to reduce the dose Deksameda. Treatment is symptomatic.

    Interaction with other drugs
    is possible Deksameda pharmaceutical incompatibility with other intravenously administered drugs – it is recommended to be administered separately from other drugs (in / bolus or through an IV, etc., as the second solution.). When mixed with a solution of Sustanon steroid heparin precipitate formed.

    Simultaneous with the appointment Deksameda with: inducers of “liver” microsomal enzymes (phenobarbital, rifampin, phenytoin, geofillin, ephedrine) leads to a decrease in its concentration; diuretics(especially “thiazide” and a carbonic anhydrase inhibitor) and amphotericin B may lead to increased excretion of K + ; with a sodium-containing drugs – the development of edema and high blood pressure;amphotericin B – increases the risk of developing heart failure, cardiac glycosides – worsening of their portability and increases the likelihood of developing ventricular arrhythmias (due to induced hypokalemia), indirect anticoagulants weakens (rarely strengthens) their effect ( required dose adjustment); anticoagulants and thrombolytics – increases the risk of bleeding from ulcers in the gastrointestinal tract, ethanol or non-steroidal anti-inflammatory drugs (NSAIDs) increases the risk of occurrence of erosive and ulcerative lesions of the gastrointestinal tract and of bleeding (in combination with NSAIDs at the treatment of arthritis may reduce the dose of corticosteroids due to the summation of therapeutic effect); paracetamol increases the risk of hepatotoxicity (induction of hepatic enzymes and the formation of toxic metabolites of paracetamol), acetylsalicylic acid, accelerates its excretion and reduces the concentration in the blood (with the abolition of Sustanon steroid salicylate level in the blood increases, and increases the risk of side effects), insulin and oral gipogilikemicheskimi drugs, antihypertensives – decreases their effectiveness. vitamin the D – reduces its impact on the absorption of Ca 2+ in the intestine.growth hormone reduces the effectiveness of the latter, and with praziquantel – its concentration; M holinoblokatorami (including antihistamines and tricyclic antidepressants), and nitrates contribute to increased intraocular pressure; isoniazid and mekselitinom increases their metabolism (especially in the “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 Deksamed from its association with albumin, increases the risk of its side effects. ACTH increases the effects Deksameda. Ergocalciferol and parathyroid hormone hinder the development of osteopathy caused Deksamedom. Cyclosporin and ketoconazole , slowing metabolism Deksameda, can in some cases increase its toxicity. Concurrent administration of androgen and steroid anabolic drugs with Deksamedom contributes to the development of peripheral edema and hirsutism, acne. Estrogens and oral estrogensoderzhaschie contraceptives reduced clearance Deksameda that may be associated with increased severity of his actions. Mitotane and other inhibitors of the function of the adrenal cortex may condition the need to increase the dose Deksameda. at simultaneous application with live virus vaccines and compared to other types of immunization increases the risk of activation of viruses and the development of . infections Antipsychotic drugs (neuroleptics) and azathioprine increases the risk of developing cataracts in the appointment Deksameda. while the use of antithyroid drugs is reduced, and a thyroid hormone – increased clearance Deksameda.

    Special instructions:

    Before treatment (if it is impossible because of the condition of urgency – in the course of treatment) the patient should be examined in order to identify possible contraindications. Clinical examination should include a study of the cardiovascular system, X-ray examination of the lungs, the study of gastric and duodenal ulcers, urinary system, organs of vision; control blood count, glucose and electrolytes in the blood plasma.
    During treatment Deksamedom (especially long) must be monitored ophthalmologist, blood pressure control and the state of water and electrolyte balance, as well as patterns of peripheral blood and the blood glucose level.
    In order to reduce the side effects should be to increase the flow of + organism (diet, potassium supplements). Food should be rich in proteins, vitamins, with the restriction of fat, carbohydrates and salt.
    The drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may exacerbate existing emotional instability or psychotic disorders. When referring to the history of psychoses in Deksamed in high doses administered under strict medical supervision. In stressful situations during maintenance therapy (eg, surgery, trauma, or infectious diseases) should be carried out correction dose due to an increase in the glucocorticosteroid needs. You should carefully monitor the patients for a year after the end of long-term therapy Deksamedom in connection with the possible development of relative adrenal insufficiency in stressful situations.
    With the sudden cancellation, particularly in the case of the prior use of high doses may develop the syndrome of “cancellation” (anorexia, nausea, lethargy , generalized musculoskeletal pain, general weakness), as well as exacerbation of the disease, about which he was appointed Deksamed.
    During treatment Deksamedom should not be vaccinated due to the reduction of its effectiveness (immune response). Appointing Deksamed during intercurrent infections, septic conditions, and tuberculosis, treatment with antibiotics is necessary to simultaneously bactericidal action.
    The children during long-term treatment Deksamedom careful observation of the dynamics of growth and development. Children who during the treatment period were in contact with patients with measles or chickenpox, prophylaxis prescribe specific immunoglobulins.
    Diabetic patients should monitor the content of blood glucose and correct treatment if necessary.
    Showed radiological control of bone and joint system (spine images, brushes) .
    patients with latent infectious diseases of kidneys and urinary tract infections can cause Deksamed leukocyturia that may have diagnostic value. Deksamed increases the content of metabolites 11- and 17-oksiketokortikosteroidov.

    Use during pregnancy and breast-feeding
    During pregnancy (especially in the first trimester), the drug can be used only when the expected therapeutic effect outweighs the potential risk to the fetus. When long-term therapy in pregnancy does not exclude the possibility of fetal growth. In the case of the end of pregnancy there is a risk of occurrence of atrophy of the adrenal cortex in the fetus, which may necessitate replacement therapy in the newborn.
    If you want to treat the drug during breastfeeding, the breast-feeding should be discontinued.

 

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