Conditions that require systemic or local treatment with glucocorticosteroids, such as inflammatory and systemic rheumatic diseases, autoimmune diseases, allergic conditions, anaphylactic shock, severe asthma, transplant rejection. In combination with cytostatic drugs for the treatment of various types of leukemias, lymphomas, myelomas and breast cancer; in combination therapy with these drugs has antiemetic effect.
Composition:
1 tabl contains 4 mg or 16 mg of methylprednisolone. The preparation contains lactose.
Action:
Synthetic glucocorticosteroid with a strong anti-inflammatory effect (about 5-fold higher than hydrocortisone) and immunosuppressive and weak mineralocorticoid (slightly enhances salt and water retention). Glucocorticosteroids inhibit the synthesis of many protein enzymes involved in rheumatoid arthritis and cytokines that play an important role in immune and inflammatory processes. The effect of these complex activities is the weakening of the inflammatory and immune response. Glucocorticoids, including methyl Prednisolone, inhibit or eliminate the tissue response to various stimuli, including radioactive, mechanical, chemical, infectious and immunological factors. In this way, they reduce symptoms without affecting the underlying disease. The drug inhibits the secretion of ACTH, the production of endogenous cortisol, and in the case of prolonged use causes partial cessation of the adrenal cortex. It also participates in the metabolism of carbohydrates, Calcium, vitamin D, proteins and fats, causing an increase in the level of Glucose in the blood. reduction of bone mineral density, muscular atrophy and disturbances in lipid metabolism. The oral bioavailability is usually> 80%, but during high-dose treatment, it may be reduced to 60%. Maximum plasma concentrations occur within 1 to 2 hours after oral administration. It binds to plasma albumin approximately 77%. It is metabolized to inactive metabolites, its total clearance is about 6.5 ml / kg / min, and the period of biological half-reduction of anti-inflammatory action is from 18 to 36 hours. About 5% is excreted unchanged in urine. The drug passes through the placenta and is excreted into breast milk, it can be removed from the body during dialysis.
Contraindications:
Hypersensitivity to the components of the preparation. Tuberculosis and other acute / chronic viral or bacterial infections without parallel specific antimicrobial or chemotherapy treatment. Systemic fungal infections.
Precautions:
In children, the use of the drug should be limited to the minimum dose used as short as possible due to delayed growth. Especially cautiously use in patients with hypertension, congestive heart failure, psychiatric disorders, diabetes (in the patient or members of his family), pancreatitis, gastrointestinal disorders (such as peptic ulcer, segmental ileitis, ulcerative colitis or diverticulitis - an increased risk of bleeding and perforation), osteoporosis, glaucoma and risk factors for thrombosis, blood coagulation disorders. In patients with hypothyroidism or liver damage, it may be necessary to reduce the dose due to the stronger effect of the drug. When used with anticoagulants, salicylates, and prostaglandin inhibitors, there is an increased risk of stomach ulceration and gastrointestinal bleeding. During treatment with glucocorticosteroids, it is also possible to weaken the anticoagulant effect. Therefore, it is necessary to monitor INR, especially when changing treatment. Administration of corticosteroids may lead to the disclosure of latent hyperparathyroidism. In case of disease or surgical injury, the dose should be increased if necessary or another glucocorticosteroid should be administered due to adrenocortical insufficiency, which may last for several months after the end of treatment. The risk of osteoporosis-induced glucocorticosteroids can be reduced to a minimum using the dose corresponding to the lowest therapeutic level.In patients with known osteoporosis or risk factors for osteoporosis, prophylactic parallel therapy should be considered, eg using bisphosphonates. Exercise caution in elderly patients due to the increased risk of, for example, gastric ulceration, osteoporosis or skin ulceration. The medicinal product contains lactose. Patients with rare hereditary disorders such as galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose should not take this medicine.
Pregnancy and lactation:
The drug passes the placenta barrier and is excreted into breast milk. In individual cases, delayed fetal development and slight narrowing of the ductus arteriosus during pregnancy with the drug were observed. A low risk of congenital malformations, such as cleft palate, has been observed. The drug can be used during pregnancy only if absolutely necessary after a careful assessment of the expected benefits of treatment against possible risk to the fetus. However, you should not give up treatment for which there are clear indications. If long-term treatment with corticosteroids is terminated during pregnancy, treatment should be discontinued gradually. In some cases (eg, adrenocortical insufficiency replacement therapy), it may be necessary to continue treatment and even increase the doses used. Newborns born to mothers who during pregnancy received significant doses of corticosteroids should be observed for the presence of adrenal insufficiency. Breastfeeding during prolonged systemic treatment with glucocorticosteroids is not recommended.
Side effects:
Corticosteroids can exacerbate existing infections and mask the symptoms of infection: they can delay wound healing and cause scarring. Posteroid adrenal insufficiency may occur, symptoms of Cushing's syndrome, growth retardation in children, amenorrhea, decreased sperm count, hypertension, increased risk of atherosclerosis, thrombosis and vasculitis; bleeding and perforation (in the course of peptic ulcer disease, pancreatitis, segmental ileitis and ulcerative colitis), striae and trophic changes of the skin, petechiae, purpura, acne, hirsutism, fibrosis, myopathy and muscle weakness, impaired glucose tolerance to diabetes mellitus , osteoporosis, aseptic osteonecrosis, cataracts, glaucoma, psychiatric disorders (depression, dementia, psychosis), mood changes (from slight euphoria to mild manic states), intracranial hypertension and fits, increased risk of urolithiasis, allergic reactions (including anaphylactic shock) ). In order to minimize side effects, the entire daily dose should be taken in the morning, according to the circadian rhythm of endogenous cortisol production.
Dosage:
The initial dose depends on the severity of the disease being treated and is 16-96 mg / day. Maintenance dose usually 4-12 mg per day and is given once in the morning. With long-term use, it may be appropriate to take one dose every other day. In the treatment of children, it is recommended to use lower doses of the drug.