Features of the drug
The main active ingredient in the medicine is methylprednisolone. Manufacturers offer metypred in the form:
- Lyophilisate. It is a white powder that may have a slight yellowish tint. It is packaged in 0.25 g bottles; in addition to the bottle, the kit includes an ampoule with a solvent. A solution is prepared from the drug for intramuscular or intravenous administration.
- Tablets. They may contain 4 or 16 mg of active substance. They are distinguished by their round shape, with a beveled edge on one side. Metipred 16 tablets are engraved “ORN 346”.
Metypred
Synthetic GCS. It has anti-inflammatory, antiallergic, immunosuppressive effects, increases the sensitivity of beta-adrenergic receptors to endogenous catecholamines.
Interacts with specific cytoplasmic receptors (receptors for GCS are found in all tissues, especially in the liver) to form a complex that induces the formation of proteins (including enzymes that regulate vital processes in cells).
The effect of methylprednisolone on protein metabolism: reduces the amount of globulins in plasma, increases the synthesis of albumins in the liver and kidneys (with an increase in the albumin/globulin ratio), reduces the synthesis and enhances protein catabolism in muscle tissue.
The effect of methylprednisolone on lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (fat accumulation occurs mainly in the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.
The effect of methylprednisolone on carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract, increases the activity of glucose-6-phosphatase (increases the flow of glucose from the liver into the blood), increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activates gluconeogenesis), promotes the development of hyperglycemia.
The effect of methylprednisolone on water-electrolyte metabolism: retains sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces calcium absorption from the gastrointestinal tract, reduces bone mineralization.
The anti-inflammatory effect is associated with inhibition of the release of inflammatory mediators by eosinophils and mast cells, induction of the formation of lipocortins and a decrease in the number of mast cells producing hyaluronic acid, with a decrease in capillary permeability, stabilization of cell membranes (especially lysosomal) and organelle membranes. Acts on all stages of the inflammatory process: inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin inhibits phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes, which also contribute to the processes of inflammation and allergies), the synthesis of pro-inflammatory cytokines (including including interleukin 1, tumor necrosis factor alpha), increases the resistance of the cell membrane to the action of various damaging factors.
The immunosuppressive effect is caused by the involution of lymphoid tissue, inhibition of the proliferation of lymphocytes (especially T lymphocytes), suppression of the migration of B cells and the interaction of T and B lymphocytes, inhibition of the release of cytokines (interleukin-1, 2, interferon gamma) from lymphocytes and macrophages and decreased antibody formation.
The antiallergic effect develops as a result of a decrease in the synthesis and secretion of allergy mediators, inhibition of the release of histamine and other biologically active substances from sensitized mast cells and basophils, a decrease in the number of circulating basophils, T- and B-lymphocytes, mast cells, suppression of the development of lymphoid and connective tissue, reduction sensitivity of effector cells to allergy mediators, inhibition of antibody formation, changes in the body's immune response.
In obstructive diseases of the respiratory tract, the effect is due mainly to inhibition of inflammatory processes, prevention or reduction of the severity of swelling of the mucous membranes, reduction of eosinophilic infiltration of the submucosal layer of the bronchial epithelium and deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchi to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.
Suppresses the synthesis and secretion of ACTH and, secondarily, the synthesis of endogenous corticosteroids.
Inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.
Prescription of the drug and contraindications
The drug metypred, the instructions for use confirm this, is used for various diseases in complex treatment. The list of indications is large, so only the attending physician should make a decision on drug therapy. Understanding what metypred is prescribed for, you should be aware that it also has contraindications. To eliminate negative reactions, they must be taken into account.
For short-term use, the only contraindication is hypersensitivity to the active substance and other components of the drug. This means that you need to carefully study the composition of the medicine before using it. Mitypred is not used for treatment when diagnosing tuberculosis. The drug is contraindicated for various infectious diseases: bacterial, fungal or viral.
Metypred should not be prescribed for treatment during pregnancy, as there is a risk of fetal death. It is recommended to use the medicine with caution when breastfeeding. Children are treated with the drug only if there are absolute indications under the strict supervision of a doctor.
Metypred should be used with extreme caution if you have the following diseases:
- Gastrointestinal tract.
- Of cardio-vascular system.
- Endocrine system.
- Kidney.
It is necessary to monitor the patient if treatment with metipred is carried out against the background of a diagnosis of hypoalbuminemia or conditions that can provoke its development. Careful monitoring of the patient's condition is necessary in case of glaucoma, mental disorders, osteoporosis and confirmation of parasitic infections.
Metipred, instructions for use, focuses on this, and has other contraindications. The doctor must take them into account when prescribing the drug.
Indications for use of the drug Metipred
Conditions requiring systemic therapy with GCS are inflammatory and systemic rheumatic, autoimmune diseases, allergic conditions, anaphylactic shock, asthma and other lung diseases, as well as in order to reduce intracranial pressure (for example, with cerebral edema due to neoplasms), transplant rejection; some dermatological, hematological, hepatic, neurological (eg multiple sclerosis, myasthenia gravis), renal and gastrointestinal diseases (eg ulcerative colitis, Crohn's disease). Methylprednisolone is also used as an antiemetic in chemotherapy and as a component of regimens for the treatment of leukemia, lymphoma and malignant myeloma.
Treatment: recommended dosage
The dosage of the drug and the duration of treatment are determined individually. The tablets should be taken during or after meals. Take the medicine with a small amount of liquid.
The drug can be prescribed in an initial dosage of 4 mg - 48 mg per day. Such doses are used for various diseases that are mild. High doses (200-1000 mg/day) are prescribed for the following pathologies:
- Multiple sclerosis.
- Brain edema.
For organ transplantation, the dosage is calculated based on the patient’s body weight: 7 mg/kg/day. But if it is not possible to achieve the desired result after a certain time, then stop taking the drug and prescribe another type of therapy. For the treatment of children, if indicated, the dose of the drug is also calculated taking into account body weight.
The lyophilisate solution can be administered by intramuscular injection or intravenous infusion. The procedure involves slow injection. Moreover, if additional treatment is carried out in life-threatening cases, mitipred is administered intravenously over 30 minutes in an amount of 0.03 g/kg body weight every 6-8 hours. The procedures are repeated for no more than a day and a half.
After long-term therapy with the drug, you should not suddenly abandon the drug; the daily dose should be reduced gradually. Otherwise, a withdrawal effect may occur. This condition is characterized by depressive mood and aggression, increased fatigue and drowsiness.
Interactions of the drug Metypred
Metypred can potentiate the ulcerogenic effect of salicylates and other NSAIDs. Methylprednisolone may help reduce serum levels of salicylates by increasing their renal clearance. With the simultaneous use of methylprednisolone and anticoagulants, the risk of ulcerogenic effects and gastric bleeding increases. GCS can also reduce the severity of the action of anticoagulants. Thus, the dosage regimen of the latter must necessarily be accompanied by control of the international normalization index (INI). Parenteral administration of methylprednisolone potentiates the thrombolytic effect of vitamin K antagonists (fluindione, acenocoumarol). In patients with myasthenia gravis, the use of corticosteroids and anticholinesterase drugs can cause muscle weakness. Methylprednisolone may reduce the hypoglycemic effect of oral antidiabetic agents and insulin. Inducers of microsomal liver enzymes, such as barbiturates, phenytoin, primidone, carbamazepine and rifampicin, increase the systemic clearance of methylprednisolone, thereby reducing the severity of the effects of methylprednisolone by almost 2 times. CYP3A4 inhibitors, such as erythromycin, clarithromycin, ketoconazole, itraconazole and troleandomycin, increase plasma levels of methylprednisolone, which may increase its therapeutic and side effects. Estrogens can increase the effects of methylprednisolone by slowing its metabolism. It is not recommended to adjust the dose of methylprednisolone in women taking oral contraceptives, as this may not only prolong its half-life, but also lead to the development of immunosuppressive effects of methylprednisolone. Methylprednisolone may increase potassium excretion in patients receiving concomitant amphotericin, diuretics, and laxatives. Methylprednisolone has additive immunosuppressive properties, which may increase the therapeutic effects or the risk of various side effects when administered concomitantly with other immunosuppressives. Only some of these effects can be explained by pharmacokinetic interactions. GCS increase the effect of antiemetic drugs used to reduce the severity of side effects of emetogenic chemotherapy. Cases of seizures have been reported while taking methylprednisolone and cyclosporine. GCS may reduce the immune response to vaccination and increase the risk of neurological complications. The use of GCS in therapeutic (immunosuppressive) doses simultaneously with live viral vaccines may increase the risk of developing viral diseases. Two serious cases of acute myopathy have been reported in elderly patients receiving doxacurium chloride and high-dose methylprednisolone. With long-term therapy, GCS may reduce the effect of somatropin.