International generic name

Methylprednisolone

Drug form and composition

Powder for solution for injection and solvent. One ampoule of 2 ml contains 6.31 mg; 15.78 mg or 40 mg Methylprednisolone (powder for solution for injection); one ampoule of 1 ml contains 1ml Sterilised water for injections (solvent). One ampoule of 5 ml contains 125 mg Methylprednisolone (powder for solution for injection); one ampoule of 2 ml contains 2 ml Sterilised water for injections (solvent). One ampoule of 10 ml contains 250 mg Methylprednisolone (powder for solution for injection); one ampoule of 5 ml contains 5 ml Sterilised water for injections (solvent).

Indications

The preparation is used in following conditions: endocrine disorders - acute adrenocortical insufficiency; collagenosis - during an exacerbation or as a maintaining treatment in lupus erythematosus; dermatology diseases - pemphigus, severe erythema multiforme, exfoliative dermatitis, generalized neurodermatitis, severe psoriasis, severe seborrhea dermatitis; allergy - severe or resistant to conventional treatment diseases, including bronchial asthma, atopic dermatitis, serum disease, drug hypersensitivity, larungeal edema, urticaria, anaphylaxis; gastrointestinal diseases - acute ulcerous colitis; intracranial edema - intracranial edema due to brain neoplasms, head injuries, intracranial surgery; organ transplantation - to prevent rejection of the transplant; acute rheumatic fever; severe shock - hemorrhagic, traumatic, allergic, septic (infections with severe intoxication); pseudocrup; following esophageal injuries by corrosive agents, in order to prevent esophageal strictures.

Dosage and administration

Methylprednisolon is applied intramuscularly or intravenously as follows: In shock - 125 mg every 2-6 hours or 250 mg every 4-6 hours or 30 mg per kg body weight every 24 hours. It could be applied as an intravenous infusion for 10-30 minutes, but not less. As an immunosuppressive agent (for prevention of transplant rejection) Methylprednisolon is used in dose 0.5-2 g intravenously every 24-48 hours. In intracranial edema - 40-125 mg every 4-6 hours intravenously or intramuscularly for 4-7 days (until the condition is stabilized). In other diseases the initial dose varies between 10 and 40 mg, depending on the clinical manifestation. High doses are usually used for a short time. In children the therapeutic dose varies between 0.8 and 1.5 mg per kg body weight. Method of preparation of the solution for injection: the solvent is added to the powder and prepared solution is diluted in desired volume infusion solution - 5% dextrose, isotonic saline or 5% solution of dextrose in saline. Discontinuation of the treatment should be made with gradually reduction of the dose. The preparation should not be mixed with other medicines in the syringe!

Contraindications

Hypersensitivity to the preparation; acute psychoses; latent or active tuberculosis; herpes simplex infection; keratitis. Relative contraindications for application include: active and latent peptic ulcer; Cushing’s syndrome; diverticulosis; recent intestinal anastomoses; osteoporosis; glaucoma; renal insufficiency; diabetes mellitus; hypertension; local and systemic infections (including varicella vaccine); fungal infections and other exanthematous diseases; immunosuppressive conditions; pregnancy (particularly during the first trimester).

Special warnings and precautions

Corticosteroids may cause a blood pressure elevation, water and salt retention, and increased excretion of potassium and calcium. In this reason during the treatment a diet with reduced salt and increased potassium and calcium content is advisable. The corticosteroid therapy may conceal a brain hemorrhage. Long-term treatment may lead to an increase of the stomach acidity with resultant peptic ulcers. Long-term hormonal treatment frequently leads to diminish the activity of the suprarenal gland function and dimensions reduction. The preparation should not be injected in the deltoid muscle, as a high risk of subcutaneous atrophy exists. Following the discontinuation of the treatment the patient should be monitored for a long time, as a risk of abrupt severe relapse of the disease exists. During the pregnancy and lactation, as well as in women in term a careful consideration of the risk/benefit ratio should be made.

Drug interactions

Concomitant administration of cardiac glycosides may potentiate their activity (due to increased excretion of potassium). Simultaneous treatment with saluretics may exacerbate the hypokalemia. Methylprednisolon reduces the effect of oral antidiabetics and anticoagulants. The Methylprednisolon action is inhibited in simultaneous administration of barbiturates, rifampicin, and phenytoin, because the latter preparations induce its metabolism. In concomitant treatment with salicylates or other nonsteroidal anti-inflammatory drugs the risk of gastrointestinal complications becomes higher. Methylprednisolon should be avoided during immunization.

Adverse reactions

Following adverse reactions may appear: cardiovascular system - hypertension, thrombosis, thromboembolia, and vasculitis; CNS - depression, fear, irritability, insomnia, euphoria, convulsions (in children), mental disorders; gastrointestinal system - ulcer disease exacerbation, pancreatitis; endocrine system - glucose tolerance disorders, glycose serum level elevation, atrophy of the suprarenal gland, Cushing-like syndrome, amenorrhoea, hirsutism, sexual impotence, hypoparathyroidism, grout retardation; urinary system - proteinuria or hematuria, reduced creatine clearance; skin - rash, contact dermatitis, steroidal akne, abdominal striae, reduced skin pigmentation, hypertrichosis, wound recovery retardation; blood - lymphopenia, aplastic anemia, thrombocytopenia, bleeding time shortness; other - increase of the intraocular pressure, cataract, moon-like face, edemas, increased potassium excretion, muscular weakness, osteoporosis.

Pharmacological mechanisms

Methylprednisolon is a synthetic derivative of prednisolon. It exerts more powerful antiexudative, anti-inflammatory, antiallergic, and anti-shock effects, compared to prednisolon. It inhibits proliferation of the connective tissue cells. Its mineralcorticoid activity is weak. The effect appears about 4 times more rapidly, compared to prednisolon. The preparation is well absorbed and exerts fast and continuos effect.

Supplied

5 or 10 ampoules of 2 ml (6.31 mg); 15.78 mg (powder for solution for injection), and 5 or 10 ampoules of 1 ml (solvent). 10 ampoules of 40 mg (powder for solution for injection), and 10 ampoules of 1 ml (solvent). 5 ampoules of 5 ml (125 mg) - powder for solution for injection, and 5 ampoules of 2 ml (solvent). 5 ampoules of 10 ml (250 mg) - powder for solution for injection, and 5 ampoules of 5 ml (solvent).

Expiry

5 years.