Index of drugs

Glucocorticosteroids should be used only symptomatically, except for endocrine disorders when used in substitution treatment.Endocrine disorders - primary or secondary under adrenal insufficiency (in certain circumstances, in combination with mineralocorticosteroids); acute adrenal insufficiency (may be necessary in combination with mineralocorticosteroids); treatment of the shock state: induced by adrenal insufficiency or shock not responding to conventional treatment, if confirmed or suspected adrenal insufficiency (in cases when mineralocorticosteroids are inadvisable); before surgery and in case of severe illness or injury, in patients diagnosed with adrenal insufficiency or reduced levels of adrenal hormones; congenital adrenal hyperplasia; unhealthy thyroiditis; hypercalcemia in the course of cancer.Rheumatic diseases - short-term supportive treatment during an episode of exacerbation or deterioration of health in the course of: post-traumatic osteoarthritis; inflammation of the synovium in the course of osteoarthritis; rheumatoid arthritis, including juvenile rheumatoid arthritis; acute and subacute bursitis; necrotic inflammation; acute non-specific inflammation of the tendon sheath; acute gouty arthritis; psoriatic arthritis; ankylosing spondylitis.Systemic connective tissue diseases - during an exacerbation or as maintenance treatment in the course of: systemic lupus erythematosus (and lupus nephritis); acute rheumatic myocarditis; systemic polymyositis and dermatomyositis; nodular arteritis; Goodpasture syndrome.Dermatological diseases: pemphigus; severe erythema multiforme (Stevens-Johnson syndrome); exfoliative dermatitis; severe form of psoriasis; blister dermatitis dermatitis; severe form of seborrheic dermatitis; mycosis fungoides.Allergic diseases - treatment of serious allergic diseases, when other methods of treatment are ineffective: bronchial asthma; contact eczema; atopic dermatitis; serum sickness; seasonal or perennial allergic rhinitis; hypersensitivity reaction to drugs; urticarial reactions after transfusion; acute non-inflammatory larynx edema (the drug of the first choice is epinephrine).Eye diseases - severe acute and chronic allergic and inflammatory processes including the eye and its appendages: ophthalmia; iritis, iritis and iridocyclitis; choroid and retinal choritis; diffuse posterior uveitis and choroiditis; optic neuritis; sympathetic uveitis; inflammation within the anterior segment of the eye; allergic conjunctivitis; allergic peripheral corneal ulcers; keratitis.Diseases of the digestive tract - as a systemic treatment in exacerbation of the course of: ulcerative colitis; Leśniowski-Crohn's disease.Respiratory system diseases: symptomatic sarcoidosis; berylliosis; fulminant or disseminated pulmonary tuberculosis, simultaneously with appropriate treatment with tuberculosis medicine; Loefler syndrome that can not be treated by other means; aspiration pneumonia; moderate or severe pneumonia caused byPneumocystis carinii in patients with AIDS (as adjunctive therapy when given during the first 72 hours of initial treatment againstPneumocystis). Haematological diseases: acquired (autoimmune) haemolytic anemia; idiopathic thrombocytopenic purpura in adults (intravenous administration only, intramuscular administration contraindicated); secondary thrombocytopenia in adults; deficiency of erythroblasts in the bone marrow; congenital hypoplastic anemia.Cancers - palliative treatment: leukemia and lymphomas in adults; acute leukemia in children; improving the quality of life of patients with terminal cancer.edema - to induce diuresis or remission of proteinuria in the nephrotic syndrome without uremia.In neurology: brain edema associated with the presence of a tumor - primary or metastatic and / or associated with surgery or radiotherapy; exacerbation in the course of multiple sclerosis; acute spinal cord injuries (treatment should be started within 8 hours of injury).Other indications: tuberculous meningitis with a subarachnoid or subarachnoid subtype block together with appropriate anti-tuberculosis therapy; trichinosis with involvement of the nervous system or myocardium; organ transplantation; prevention of nausea and vomiting associated with cancer chemotherapy.

One vial contains 40 mg, 125 mg, 250 mg, 500 mg or 1.0 g methylprednisolone as the sodium succinate.

Synthetic glucocorticosteroid with a strong anti-inflammatory effect (about 5-fold higher than hydrocortisone), immunosuppressive action and minimal mineralocorticoid activity. It works at the DNA level, modifying the synthesis of certain enzymes, therefore the maximum pharmacological activity occurs later than reaching the peak concentration in the blood. Clinical response is generally observed 4-6 hours after administration; in the treatment of asthma the first beneficial effects can occur after 1-2 h. T_0,5 drug in the blood is from 2.3 to 4 h and does not depend on the route of administration. The biological half-life ranges from 12 to 36 h. The intracellular activity of glucocorticoids leads to a clear difference between the half-life in blood and the pharmacological half-life. Pharmacological activity persists despite the decrease in blood concentration to undetectable. The duration of anti-inflammatory activity of glucocorticoids corresponds approximately to the duration of suppression of the hypothalamic-pituitary-adrenal axis. Methylprednisolone is metabolised in the liver with the participation of CYP3A4. Metabolites are excreted mainly in the urine in the form of glucuronides, sulphates and free compounds.

Hypersensitivity to methylprednisolone or to any of the excipients. Systemic fungal infections. Do not administer. Administration of live or live attenuated vaccines is contraindicated in patients receiving doses of corticosteroids with immunosuppressive activity.

Glucocorticoids may mask the symptoms of infection and impair the body's defenses and increase the susceptibility to new infections, and infections may be more severe. Corticosteroids should be used with caution in patients with known parasitic infections, e.g.Strongyloides) or with suspicion of such infections (in such patients, immunosuppression after corticosteroids may lead to infection or worsening of the infection with the nematode and spread of the parasite in the body with extensive migration of larvae, often accompanied by severe intestinal inflammation and potentially deadly sepsis caused by Gram-negative bacteria). The role of corticosteroids in septic shock has been described as both beneficial and harmful. Recently, it has been suggested that corticosteroid supplementation has a beneficial effect in patients with advanced septic shock who have been diagnosed with adrenal insufficiency. However, they are not recommended for routine use in the treatment of septic shock, and a systematic review suggests that short-term use of high-dose corticosteroids is not warranted. However, a meta-analysis and review studies indicate that longer regimens (lasting 5-11 days) for low-dose corticosteroids may reduce mortality. Patients receiving immunosuppressive corticosteroids may receive inactivated vaccines derived from biogenetics; however, the response to these vaccines may be limited or may even be ineffective. Patients receiving non-immunosuppressant corticosteroid doses may undergo all required immunization procedures. The use of corticosteroids in people with active tuberculosis should be limited to cases of fulminant or disseminated disease where they are used to treat the disease in combination with appropriate anti-tuberculosis drugs. When administration of glucocorticoids is indicated in patients with latent tuberculosis or with a positive tuberculin test, close observation of patients is necessary as the disease may be reactivated; in these patients, chemoprophylaxis should be used during prolonged corticosteroid therapy. Patients receiving corticosteroids have been diagnosed with Kaposi's sarcoma; discontinuation of corticosteroids may lead to clinical remission. If severe stress occurs in patients undergoing corticosteroid therapy, it is advisable to increase the dosage of fast acting corticosteroids before and during the stressful situation.Long-term administration of therapeutic doses of corticosteroids may lead to inhibition of the hypothalamo-pituitary-adrenal axis, i.e. secondary adrenocortical insufficiency; it can be reduced by administering the drug in the schedule every other day. Sudden discontinuation of glucocorticoids may result in acute adrenal failure leading to death. Drug-induced secondary adrenal insufficiency can be minimized by gradually reducing the dose; this type of relative failure may persist for several months after discontinuation of treatment, therefore, in the event of a stressful situation, the implementation of hormone therapy should be considered. The "withdrawal syndrome" of steroids, which seemingly is not associated with adrenal insufficiency, may also occur after a sudden discontinuation of the drug (it is believed that the symptoms are rather the consequences of a sudden change in glucocorticoid concentration, not a small concentration thereof). Glucocorticosteroids should not be administered to patients with Cushing's disease (risk of worsening of the disease). Use with caution in patients with diabetes (latent diabetes mellitus or increased insulin requirements or oral antidiabetic medicines); with hypertension (increased hypertension) or other cardiovascular disorders (in the case of congestive heart failure administered only in case of clear indications); with a history of mental disorders (worsening of existing emotional instability or psychotic tendencies); with ulcerative enteritis, if there is a risk of perforation, or an abscess or other form of purulent infection, diverticulitis, fresh intestinal anastomoses, active or latent peptic ulcer disease; hypothyroidism (increased effect of the drug); with renal failure; with cirrhosis (increased activity of the drug); in the elderly (increased risk of osteoporosis, water retention and hypertension); with osteoporosis; with myasthenia or concomitantly treated with anticholinergics, including neuromuscular blockers, e.g. pancuronium (risk of acute myopathy); with hypersensitivity to any medicines in the past; with eye infection by virusHerpes simplex (risk of corneal perforation). Long-term use of corticosteroids may lead to the development of subcapsular rear cataract and nuclear cataract (especially in children), exophthalmos or increased intraocular pressure that can cause glaucoma with potential damage to the optic nerves; secondary fungal and viral infections of the eyeball may also develop more frequently. Methylprednisolone should not be used as a routine medicine for the treatment of head injuries. The solvent for solution for injection contains benzyl alcohol - a relationship has been reported between benzyl alcohol and lethal "air trapping syndrome" (respiratory distress, characterized by continuous constipation) in preterm infants. The development and development of infants and children undergoing long-term therapy should be closely observed In children given glucocorticoids prolonged, daily and in divided doses, the increase may be inhibited, therefore this regimen should be limited to the most severe indications: administration of glucocorticoids every 2 days usually eliminates or minimizes the occurrence of this side effect. Infants and children receiving corticosteroids they are exposed to increased intracranial pressure for a long time and pancreatitis may develop after high doses.

The drug can be used during pregnancy only in case of absolute necessity. Some corticosteroids easily penetrate through the placenta. One retrospective study found an increased incidence of low birth weight in children whose mothers were treated with corticosteroids. Although in infants who were exposed to corticosteroidsin uterorarely there is a newborn adrenal insufficiency, infants treated with high doses of corticosteroids should be carefully observed and examined for adrenocortical insufficiency. In infants born to mothers treated with corticosteroids for a long time during pregnancy, development of cataracts has been observed. Corticosteroids are excreted in human milk and can inhibit growth and affect the production of endogenous glucocorticoids in breast-fed infants.It should only be given to nursing mothers when the benefits of treatment are considered to outweigh the potential risks to the child.

Common: infections, Cushing's syndrome, sodium retention, fluid retention, affective disorders (including depressed mood and euphoric mood, in children - sudden changes in mood, abnormal behavior, insomnia, irritability), subcapsular cataract, hypertension, peptic ulcer disease (with the possibility of follow-up perforation and bleeding), peripheral edema, subcutaneous or stromal blood haemorrhage, atrophy of the skin, acne, growth retardation (in children), osteoporosis, muscle weakness, impaired wound healing, decrease in potassium in the blood. Not known: opportunistic infections, hypersensitivity reactions (including anaphylactic reactions and anaphylactoid reactions with or without a cardiovascular collapse, cardiac arrest, bronchospasm), hypopituitarism, "steroid withdrawal syndrome" (anorexia, nausea, vomiting, lethargy) , headaches, fever, joint pain, exfoliation, muscle pain, weight loss and / or hypotension), hypokalemic alkalosis, impaired Glucose tolerance, dyslipidemia, increased insulin requirements or oral antidiabetic medications in diabetic patients, negative nitrogen balance (caused by catabolism of proteins), increased blood urea, increased appetite (which may lead to weight gain), lipomatosis, affective disorders (including emotional instability, psychological dependence, suicidal thoughts), psychotic disorders (including m anomalous arousal, delusions, hallucinations and schizophrenia or its deterioration), mental disorders, personality change, mood swings, confusion, abnormal behavior, anxiety, insomnia, irritability, convulsions, increased intracranial pressure (with edema of optic nerves), amnesia, disorder cognitive functions, dizziness, headache, glaucoma, exophthalmos, labyrinthine dizziness, congestive heart failure (in patients with increased risk), arrhythmia, hypotension, hiccups, intestinal perforation, gastric bleeding, pancreatitis, peritonitis, ulcerative oesophagitis, flatulence, oesophagitis, abdominal pain, diarrhea, dyspepsia, nausea, erythema, angioedema, pruritus, urticaria, ecchymosis, rash, hypertrichosis, excessive sweating, dermatoses, skin discoloration, pathological fractures, osteonecrosis, muscle atrophy neuropathic degeneration joints, myopathy, arthralgia, myalgia, irregular menstruation, injection site reactions, tiredness, malaise, decreased carbohydrate tolerance, increased ALT, AST, increased alkaline phosphatase in the blood, increased urine Calcium, increased intraocular pressure , inhibition of response to skin tests, tendon rupture (especially of the Achilles tendon), compression fractures.

In the form of intravenous or intramuscular injections or intravenous infusion. In the initial period of use, for emergency reasons, intravenous injection is preferred. The dose of methylprednisolone can be reduced in infants and children but should depend on the patient's condition and response to medication rather than on age or weight. The dose should not be less than 0.5 mg / kg / day.As supportive treatment in life-threatening conditions30 mg / kg intravenously for at least 30 min; this dose may be repeated in hospital conditions, every 4 to 6 h for 48 h, depending on clinical need."Interrupted therapy" in the case of very severe exacerbations of rheumatic diseases and (or) non-response to standard therapy (i.e., use of non-steroidal anti-inflammatory drugs, gold salts and penicillamine): 1g / day intravenously for 1, 2, 3 or 4 days or 1g / month. intravenously for 6 months. Large doses of corticosteroids may have an arrhythmogenic effect, therefore such treatment should only be carried out in hospitals equipped with an electrocardiograph and a defibrillator. The dose should be administered for at least 30 minutes and if no improvement is noted, it can be repeated within one week or in case of indications arising from the patient's condition.Systemic lupus erythematosus in the case of non-response to standard treatment (or during periods of exacerbation): 1 g / day for 3 days by direct intravenous injection, lasting at least 30 min.If no improvement occurs within one week after treatment, or if the patient's condition so requires, repeat the treatment.Multiple sclerosis if there is no response to standard treatment (or during periods of exacerbation): 1 g / day for 3 or 5 days by direct intravenous injection lasting at least 30 min. If no improvement occurs within one week after treatment, or if the patient's condition so requires, repeat the treatment.Diseases associated with edema, such as glomerulonephritis or lupus nephritis, in the absence of response to standard treatment (or during periods of exacerbation): 30 mg / kg. every other day for 4 days or 1 g / day for 3, 5 or 7 days, by direct intravenous injection lasting at least 30 min. If no improvement occurs within one week after treatment, or if the patient's condition so requires, repeat the treatment.Cancer in the terminal stage (to improve the quality of life): 125 mg / day intravenously for up to 8 weeksPrevention of nausea and vomiting associated with cancer chemotherapy: chemotherapy inducing mild to moderate vomiting - 250 mg intravenously for a minimum of 5 mins for 1 hour before chemotherapy, then at the start of chemotherapy and after chemotherapy (with the first dose of methylprednisolone to increase the effect, chlorinated phenothiazine may also be given); chemotherapy inducing severe vomiting: 250 mg intravenously over a minimum of 5 min in combination with appropriate doses of Metoclopramide or butyrophenone for 1 hour before chemotherapy, then 250 mg at the start of therapy and after completion of chemotherapy.Acute spinal cord injuries30 mg / kg in direct intravenous injection lasting at least 15 minutes, the preparation should be administered within 8 hours of injury, under continuous medical observation. It can be given by direct injection only if ECG is monitored and the defibrillator is available. Administration of high doses of methylprednisolone intravenously by direct intravenous injection (doses> 500 mg in less than 10 min) may cause arrhythmia, vascular collapse or cardiac arrest. After administration by intravenous injection, a 45-minute break should be observed, followed by continuous infusion of 5.4 mg / kg / h for 23 hours. To connect the infusion pump, choose a different venous access point than for direct intravenous injection.Pneumonia caused byPneumocistis carnini in patients with AIDS: treatment should be started within 72 hours of initial treatment directed againstPneumocystis. One possible scheme is to administer 40 mg intravenously over 6 to 12 hours with a gradual dose reduction for a maximum of 21 days or until the end of treatment againstPneumocystis. Due to the increased frequency of tuberculosis reactivation in AIDS patients, the use of antimycobacterial therapy should be considered if corticosteroids are used in the high-risk group. The patient should also be monitored for the activation of other latent infections.Other indications: initial dose of 10 to 500 mg, depending on the clinical condition. In the case of short-term treatment of severe acute conditions, i.e. bronchial asthma, serous disease, urticarial reactions after transfusion and acute deterioration in multiple sclerosis, higher doses may be required. The initial dose ≤ 250 mg should be administered intravenously over at least 5 minutes, while doses> 250 mg should be administered for at least 30 min. Subsequent doses may be administered intravenously or intramuscularly depending on the patient's response and clinical status. Steroid therapy is a supplement and not a replacement of conventional therapy.Notes on the use. Complications of glucocorticoid therapy depend on the dose and duration of treatment, therefore, taking into account the risk-benefit ratio, an individual decision as to the dose and duration of treatment should be made, and whether the drug should be given daily or in an intermittent schedule. The lowest effective dose should be used to monitor the condition of the patient during treatment and if the dose can be reduced, it should be reduced gradually. Treatment should be shortened whenever possible. If a period of spontaneous remission occurs in the course of a chronic disease, therapy should be discontinued.During prolonged therapy, routine laboratory tests should be performed regularly: urinalysis, postmeal glucose concentration, blood pressure and body mass measurement, and chest X-ray. Radiographs of the upper gastrointestinal tract are desirable in patients with a history of ulcers or significant indigestion. The possible discontinuation of long-term therapy should be under medical supervision (gradual discontinuation of treatment, assessment of adrenal cortex function). Do not administer the drug as an injection into the deltoid muscle due to the frequent occurrence of subcutaneous atrophy.