Metipred - glucocorticosteroid with immunosuppressive, anti-inflammatory action.
Release form and composition
Metipred is available in the following dosage forms:
- Lyophilisate for preparation of a solution for intravenous and intramuscular administration: hygroscopic, white or slightly yellowish lyophilized powder (in vials of 250 mg, complete with solvent in ampoules or without it, 1 bottle in a carton box);
- Tablets: flat, white to almost white in color, round, with a transverse dividing line and a beveled edge on one side; On one side of the tablets, 16 mg each contains the code “ORN 346” (in dark glass bottles of 30 and 100 pcs., 1 bottle in a cardboard pack; in polyethylene containers of 30 and 100 pcs., 1 container in a carton pack; in plastic containers of 30 pcs., 1 container in a carton box).
The composition of 1 bottle with lyophilisate includes:
- Active ingredient: methylprednisolone - 250 mg (in the form of sodium succinate);
- Auxiliary component: sodium hydroxide.
Solvent: water for injection - 4 ml.
The composition of 1 tablet includes:
- Active ingredient: methylprednisolone - 4 or 16 mg;
- Auxiliary components: talc, lactose monohydrate, purified water, corn starch, gelatin, magnesium stearate.
Indications for use
Metabread in tablet form is used to treat the following diseases / conditions:
- Asthmatic status, bronchial asthma;
- Systemic diseases of the connective tissue: systemic lupus erythematosus, rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma;
- Small chorea, rheumatic carditis, acute rheumatism;
- Acute and chronic inflammatory diseases: epicondylitis, synovitis, nonspecific tenosynovitis, bursitis, Stilla disease in adults, juvenile arthritis, Bechterew's disease, shoulder scapular periarthritis, polyarthritis (including senile), osteoarthritis (including post traumatic), psoriatic and gouty arthritis;
- Primary or secondary adrenal insufficiency (including condition after removal of the adrenal glands);
- Allergic diseases (acute and chronic), including allergic reactions to drugs and food, pollinosis, exanthema drug, angioedema, allergic rhinitis, urticaria, serum sickness;
- Congenital adrenal hyperplasia;
- Skin diseases: Stevens-Johnson syndrome, bullous herpetiform dermatitis, Lyell's syndrome, exfoliative dermatitis, seborrheic dermatitis, toksidermiya, contract dermatitis (with damage to the large surface of the skin), atopic dermatitis (common neurodermatitis), eczema, psoriasis, vesicle.
- Pulmonary tuberculosis, tuberculous meningitis, aspiration pneumonia (in combination with specific chemotherapy);
- Cerebral edema (including with a brain tumor or associated with a head injury, radiation therapy or surgery) after prior parenteral administration of glucocorticosteroids;
- Allergic diseases of the eye (allergic forms of conjunctivitis);
- Inflammatory diseases of the eye: optic neuritis, severe sluggish anterior and posterior uveitis, sympathetic ophthalmia;
- Lung cancer (in combination with cytostatics);
- Autoimmune kidney diseases (including acute glomerulonephritis);
- Nephrotic syndrome;
- Subacute thyroiditis;
- Multiple sclerosis;
- Diseases of the blood and hematopoietic system: congenital (erythroid) hypoplastic anemia, elictionary of aprons aesthesia (erythrocytic anemia), secondary thrombocytopenia in adults, thrombocytopenic purpura, Hodgkin's lymphoma, myeloid and lymphoid leukemia, autoimmune, lymphogranulomatosis, myeloid and lymphoid leukemia
- Interstitial lung diseases: stage II-III sarcoidosis, pulmonary fibrosis, acute alveolitis;
- Hypoglycemic states;
- Berylliosis, Leffler syndrome (not amenable to other therapy);
- Hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy;
- Graft rejection reactions during organ transplantation (prevention).
Metipred in the form of a lyophilisate is used to treat the following diseases / conditions:
- Acute adrenal insufficiency;
- Cerebral edema, including on the background of a brain tumor or associated with radiation therapy, surgery or head injury;
- Acute hepatitis, hepatic coma;
- Shock conditions (cardiogenic, toxic, operative, traumatic, burn) with the ineffectiveness of other symptomatic treatment, plasma-substituting drugs and vasoconstrictor drugs;
- Allergic reactions (acute severe forms), anaphylactoid reactions, anaphylactic shock, blood transfusion shock;
- Thyrotoxic crisis;
- Bronchial asthma (severe), asthmatic status;
- Systemic lupus erythematosus, rheumatoid arthritis;
- Reduction of inflammation and prevention of cicatricial contractions (in case of poisoning with cauterizing liquids).
The only contraindication for short-term treatment with metipred for vital reasons is hypersensitivity to the components included in its composition.
The use of glucocorticosteroids in children during the growth period is allowed only by absolute indications and under close medical supervision.
Conditions / diseases in which metipred should be used with caution:
- Diseases of the gastrointestinal tract: diverticulitis, ulcerative colitis with the threat of perforation or abscess, recently created intestinal anastomosis, acute or latent peptic ulcer, gastritis, esophagitis, peptic ulcer and duodenal ulcer;
- Infectious (bacterial, fungal or viral origin) and parasitic diseases (currently or recently suffered, including recent contact with a patient): systemic mycosis, strongyloidosis, amoebiasis, measles, chicken pox, herpes zoster (viraemic phase), herpes simplex; latent and active tuberculosis (use for severe infectious diseases is permissible only against the background of specific treatment);
- Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after vaccination of Bacillus Calmette-Guerin (BCG), immunodeficiency states (including acquired immunodeficiency syndrome or HIV infection);
- Cardiovascular diseases (including recent myocardial infarction; in patients with acute and subacute myocardial infarction, necrosis can spread, slowing the formation of scar tissue and, as a consequence, rupture of the heart muscle), hyperlipidemia, arterial hypertension, severe chronic heart failure;
- Endocrine diseases: obesity (grade III-IV), Itsenko-Kyching disease, hypothyroidism, thyrotoxicosis, diabetes mellitus (including impaired carbohydrate tolerance);
- Severe chronic renal and / or hepatic failure, nephroluritiasis;
- Hypoalbuminemia and conditions predisposing to its occurrence;
- Open-angle and angle-closure glaucoma, systemic osteoporosis, poliomyelitis (with the exception of the form of bulbar encephalitis), acute psychosis, myasthenia gravis;
Dosing and Administration
Tablets are taken orally during or after a meal, washed down with a small amount of liquid. A full daily dose of the drug should be taken once; double daily dose - every other day, taking into account the circadian rhythm of endogenous glucocorticosteroid secretion in the range from 6 to 8 am; A high daily dose can be divided into 2-4 doses, while in the morning it is recommended to take most of it.
The initial dose of Metipred, depending on the nature of the disease, can vary from 4 mg to 48 mg per day. In cases of less serious diseases, in most cases lower doses are sufficient, although individual patients may require higher doses. Increased doses of the drug may also be required for multiple sclerosis (200 mg per day), brain edema (200-1000 mg per day), organ transplantation (up to 7 mg per 1 kg of body weight per day). If there is no satisfactory clinical effect after a sufficient period of time, Metipred should be canceled and another therapy should be prescribed.
The dosage of the drug for children is determined by the doctor taking into account the mass or surface of the body. In adrenal insufficiency, 0.18 mg is prescribed per 1 kg of body weight or 3.33 mg per 1 m² per day, divided into 3 doses; with other indications - 0.42-1.67 mg per 1 kg of body weight or 12.5-50 mg per 1 m² per day, divided into 3 doses.
In cases of long-term medication, the daily dose is recommended to be reduced gradually. Long-term treatment should not be stopped suddenly.
The solution prepared from the lyophilisate is administered in the form of intramuscular injections, slow intravenous jet injections or intravenous infusions.
To prepare the solution immediately before use should be in a vial of lyophilized add solvent. The finished solution contains 62.5 mg / ml methylprednisolone.
In life-threatening conditions as an additional therapy, the drug is administered intravenously at a dose of 30 mg per kg of body weight every 4–6 hours for no more than 48 hours within 30 minutes.
Dosing regimen for pulse therapy for the treatment of diseases in which the use of glucocorticosteroids is effective, for exacerbations of diseases and / or the ineffectiveness of standard treatment:
- Rheumatic diseases: 1000 mg per day intravenously for 1-4 days or 1000 mg per month intravenously for 6 months;
- Systemic lupus erythematosus: 1000 mg daily intravenously for 3 days;
- Multiple sclerosis: 1000 mg per day intravenously for 3 or 5 days;
- Edematous conditions (for example, glomerulonephritis, lupus nephritis): 30 mg per 1 kg of body weight intravenously every other day for 4 days or 1000 mg per day for 3, 5 or 7 days.
The above dose is recommended to be administered within 30 minutes (no less). Repeated injections are allowed in cases where no improvement has been achieved within 7 days after treatment, or if the patient’s condition requires it.
In case of cancer, 125 mg of Metipred per day is administered intravenously daily for 56 days to improve the quality of life of the patient in the terminal stage.
In cases of chemotherapy characterized by a slight or moderate emetic effect, 250 mg of the solution is injected intravenously for 5 minutes (at least) 1 hour before the use of the chemotherapeutic drug, at the beginning of chemotherapy, as well as after it. In cases of chemotherapy characterized by a pronounced emetic effect, 250 mg of the drug is administered intravenously for 5 minutes (at least) in combination with appropriate doses of butyrophenone or metoclopramide 1 hour before the chemotherapy drug is administered, then 250 mg of solution is administered at the beginning of chemotherapy intravenously.
The initial dose for other indications is administered intravenously and ranges from 10 to 500 mg (depending on the nature of the disease).
In severe conditions, a short course of therapy may require the use of higher doses. The initial dose not exceeding 250 mg should be administered intravenously over 5 minutes (at least), a dose exceeding 250 mg - 30 minutes (at least). Next, the dose is administered intravenously or intramuscularly, keeping the interval between injections, determined depending on the clinical condition and the patient's response to treatment.
Children Metipred is recommended to use in smaller doses (but not less than 0.5 mg per 1 kg of body weight per day). In the first place, the selection of the dose should take into account the patient's response to therapy and the severity of his condition, and not body weight and age.
During the period of Metipred therapy, side effects may occur on the part of some body systems, namely:
- Endocrine system: delayed sexual development in children, Itsenko-Cushing syndrome, suppression of adrenal function, manifestation of latent diabetes, steroid diabetes, reduced glucose tolerance;
- Digestive system: hiccups, flatulence, indigestion and appetite, perforation of the gastrointestinal wall, gastrointestinal bleeding, erosive esophagitis, steroid ulcer of the stomach and duodenum, pancreatitis, nausea, vomiting; rarely, increased alkaline phosphatase and hepatic transaminase activity;
- Cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); predisposed patients may develop or increase the severity of heart failure, changes in the electrocardiogram, characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis; in patients with acute and subacute myocardial infarction - the spread of necrosis, slowing the formation of scar tissue, due to which the rupture of the heart muscle is possible;
- Central and peripheral nervous system: convulsions, headache, cerebellar pseudotumor, vertigo, dizziness, insomnia, anxiety, nervousness, increased intracranial pressure, paranoia, depression, manic-depressive psychosis, hallucinations, euphoria, disorientation, delirium;
- Sense organs: sudden loss of vision (with the introduction of a solution in the nasal conchs, head, scalp and neck, Metipred crystals in the eye vessels may be deposited), exophthalmos, trophic changes of the cornea, a tendency to develop secondary viral, fungal or bacterial infections of the eye, increased intraocular pressure with possible damage to the optic nerve, posterior subcapsular cataract;
- Metabolism: excessive sweating, negative nitrogen balance, weight gain, hypocalcemia, increased calcium excretion; side effects caused by mineralocorticoid activity - hypokalemic syndrome, hypernatremia, sodium and fluid retention;
- Musculoskeletal system: atrophy, steroid myopathy, muscle tendon rupture, osteoporosis (very rarely - aseptic necrosis of the femoral head and humerus, pathological bone fractures), growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones);
- Dermatological reactions: a tendency to the development of candidiasis and pyoderma, striae, steroid acne, hypo-or hyperpigmentation, thinning of the skin, ecchymosis, petechiae, delayed wound healing;
- Allergic reactions: local allergic reactions, anaphylactic shock, pruritus, rash;
- Local reactions with the introduction of the solution: infection of the injection site, tingling at the injection site, pain, numbness, burning sensation; rarely - atrophy of the skin and subcutaneous tissue when administered intramuscularly (introduction to the deltoid muscle is especially dangerous), scarring at the injection site, necrosis of the surrounding tissues;
- Others: flushing to the head, withdrawal syndrome, leukocyturia, the development or exacerbation of infections (the development of this side effect is facilitated by the jointly used immunosuppressants and vaccination).
During the period of drug therapy (especially long-term), observation of an oculist, control of blood pressure, a picture of peripheral blood, a state of water and electrolyte balance, and glucose concentration in the blood are required.
To reduce side effects, it is recommended to increase the intake of potassium in the body (potassium preparations, diet) and at the same time apply antacids. Food should be limited to the content of salt, carbohydrates and fats, rich in vitamins and proteins.
In patients with cirrhosis of the liver and hypothyroidism, the effect of Metipred is enhanced.
The drug may exacerbate existing psychotic disorders or emotional instability. When indications of psychosis in the history of high doses of the drug should be used under medical supervision.
In stressful situations during maintenance therapy (including infectious diseases, injuries, surgeries), it is recommended to adjust the dose of the drug due to the increased need for glucocorticosteroids.
In the case of abrupt withdrawal of the drug, especially with the previous use of high doses, the development of withdrawal syndrome and exacerbation of the disease, for which he was appointed, is possible.
For intercurrent infections, tuberculosis and septic conditions, it is recommended to use Metipred simultaneously with antibacterial drugs of bactericidal action.
With long-term treatment in children requires careful monitoring of the dynamics of growth and development. If the child was in contact with chickenpox or measles during the period of therapy, it is recommended to use specific immunoglobulins for prophylactic purposes.
Methylprednisolone has a high pharmacological activity, in this regard, only the attending physician can take into account the drug interaction of Metipred with the drugs taken simultaneously with it.
Terms and conditions of storage
Store in a dark place, out of reach of children, at a temperature up to 25 ° C.
The shelf life of the lyophilisate and tablets is 5 years.
The prepared solution is stored at a temperature of 15-20 ° C for 12 hours; the reconstituted solution is at a temperature of 2-8 ° C in a refrigerator for 24 hours.