When ingestion dianabol steroids rapidly absorbed, absorption is more than 70%. It has the effect of “first pass”.
In intramuscular absorption – full and fast enough. Bioavailability after intramuscular administration – 89%.
Time to reach maximum plasma concentration (Sshah) after intake – 1.5 h after intramuscular administration – 0.5-1 hour. C max after intravenous administration at a dose of 30 mg / kg for 20 minutes, or intravenous drip at a dose of 1 g for 30-60 minutes, up to 20 mcg / ml. Following intramuscular administration of 40 mg after about 2 hours Sshah reached, component 34 ug / ml.
Relationship to plasma proteins -. 62%, regardless of the dose (only binds to albumin)
The half-life of blood plasma after oral administration is about 3.3 hours , by parenteral injection – 2.3-4 hours, and probably does not depend on the route of administration. Due to the intracellular activity revealed a pronounced difference between the half-life of methylprednisolone and plasma half-life of the organism as a whole (about 12-36 hours). Pharmacotherapeutic effect persists even when it is not determined blood levels of the drug.
Metabolized primarily in the liver, metabolites (ll-keto and 20-hydroxy compounds) do not possess the GCS activity and derived primarily by the kidneys (approximately 85% of the administered dose is detected within 24 hours in urine and about 10% – in feces). It penetrates through the blood-brain barrier and the placental barrier. The metabolites are found in breast milk.
- Systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis).
- Acute and chronic inflammatory joint disease – gout and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis (including senile), frozen shoulder, ankylosing spovdiloartrit (ankylosing spondylitis), juvenile arthritis, Still’s syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis and epicondylitis.
- Acute rheumatic fever, rheumatic carditis, chorea.
- Bronchial asthma, asthmatic status.
- Acute and chronic allergic diseases – including allergic reactions to drugs and pshtsevye products, serum sickness, urticaria, allergic rhinitis, angioedema, drug rash, hay fever and others.
- Skin diseases – pemphigus, psoriasis, eczema, atopic dermatitis (common neurodermatitis), contract dermatitis (with the defeat of a large surface of the skin), drug reaction, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell’s syndrome), bullous dermatitis herpetiformis, Stevens-Johnson syndrome .
- Cerebral edema (including on the background of a brain tumor or associated with surgery, radiation therapy, or head injury) after a preliminary parenteral corticosteroids.
- Allergic eye disease – allergic form of conjunctivitis.
- Inflammatory diseases of the eye – sympathetic ophthalmia, severe lingering front and rear uveitis, optic neuritis.
- Primary or secondary adrenocortical insufficiency (including the state after the removal of the adrenal glands).
- Congenital adrenal hyperplasia.
- Kidney disease of autoimmune origin (including acute glomerulonephritis).
- Nephrotic syndrome.
- Subacute thyroiditis.
- Diseases of the blood and hematopoietic system – agranulocytosis, panmielopatiya, autoimmune hemolytic anemia, lymphoma and myeloid leukemia, limfogranulomatoz, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocytic anemia), congenital (erythroid) hypoplastic anemia.
- Interstitial lung disease – acute alveolitis, pulmonary fibrosis, sarcoidosis II-III art.
- TB meningitis, pulmonary tuberculosis, aspiration pneumonia (in combination with a specific chemotherapy).
- Beryllium, Loeffler’s syndrome (not amenable to other therapy.); lung cancer (in combination with cytostatics).
- Multiple sclerosis.
- Ulcerative colitis, Crohn’s disease, a local enteritis.
- Hepatitis, hypoglycemic state.
- Prevention of transplant rejection in organ transplants.
- Hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy.
- Multiple myeloma.
Emergency therapy for conditions requiring a rapid increase in the concentration of glucocorticoids in the body:
- A state of shock (burns, traumatic, operational, toxic, cardiogenic) – the ineffectiveness vasoconstrictor, plasma-drugs and other symptomatic therapy.
- Allergic reactions (acute severe), transfusion shock, anaphylactic shock, anaphylactoid reactions.
- Cerebral edema (including on the background of a brain tumor or associated with surgery, radiation therapy, or head injury).
- Bronchial asthma (severe), asthmatic status.
- Systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis).
- Acute adrenal insufficiency.
- Thyrotoxic crisis.
- Acute hepatitis, hepatic coma.
- Decrease inflammation and prevent scarring restrictions (for poisoning cauterizing liquids).
For short-term use for health reasons only contraindication is hypersensitivity to methylprednisolone or components of the drug.
The children in the period of growth GCS should be used only if absolutely indicated and under particularly close supervision of your doctor.
The drug should be prescribed in the following diseases and conditions:
- gastrointestinal disease – gastric ulcer and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, recently established intestinal anastomosis, ulcerative colitis, with the threat of perforation or abscess, diverticulitis;
- parasitic and infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, including the recent contact with a patient) is a simple herpes, herpes zoster (viremicheskaya phase), chicken pox, measles; amoebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis. Application for serious infectious diseases is admissible only against the background of specific therapy;
- Pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination,
- immunodeficiency (including AIDS or HIV infection);
- diseases of the cardiovascular system (including recent myocardial infarction – in patients with acute and subacute myocardial infarction may spread necrosis, slowing the formation of scar tissue and, as a consequence – the gap of the heart muscle), severe chronic heart failure, arterial hypertension, hyperlipidemia);
- endocrine diseases – diabetes mellitus (including breach of tolerance to carbohydrates), hyperthyroidism, hypothyroidism, Cushing’s disease, obesity (III-IV cent.);
- severe chronic renal and / or hepatic insufficiency, nefrourolitiaz;
- hypoalbuminemia and conditions predisposing to its occurrence;
- systemic osteoporosis, myasthenia gravis, acute psychosis, polio (excluding the bulbar form of encephalitis), open-and-closure glaucoma;
Use during pregnancy and breast-feeding
During pregnancy (especially in I trimester) apply only for health reasons.
Since steroids penetrate into breast milk, if necessary, use during breast-feeding, breast-feeding is recommended to stop.
Dosage and administration
The dose and duration of treatment is determined by the doctor individually, depending on the indication and the severity of the disease. Pills. All the daily dose is recommended to be taken orally once or double daily dose – a day in view of the circadian rhythm of endogenous secretion of glucocorticoids in the range of 6 to 8 am The high daily dose can be divided into 2-4 reception, with the morning dose should be taken large. The tablets should be taken during or directly after a meal, with a small amount of liquid. The initial dose may be 4 mg to 48 mg per day of methylprednisolone, depending on the nature of the disease. In less severe disease usually sufficient use of lower doses, although individual patients may require higher doses. High doses may be required in such diseases and conditions such as multiple sclerosis (200 mg / day), brain edema (200-1000 mg / day), and organ transplantation (up to 7 mg / kg / day). If after a reasonable period of time not received a satisfactory clinical effect, the drug should be discontinued and the patient to assign another type of therapy. Children dose determined by the physician based on weight or body surface. When adrenal insufficiency – inside the 0.18 mg / kg or 3.33 mg / m² per day in 3 divided doses, other testimony -as 0,42-1,67 mg / kg or 12.5-50 mg / m² .m per day in 3 divided doses. Chronic administration of the drug daily dose should be reduced gradually.Duration of therapy should not be stopped abruptly! Parenteral drug is administered as a slow intravenous bolus dianabol steroids injection or intravenous infusion and intramuscular injection. Preparation of the solution. A solution for injection is prepared by adding the solvent to the vial with lyophilized prior to use. The mixed solution contains 62.5 mg / ml Methylprednisolone. As an additional therapy for life-threatening conditions are administered 30 mg / kg body weight / in for at least 30 min. The introduction of this dose can be repeated every 4-6 hours for a maximum of 48 hours. Pulse therapy in the treatment of diseases for which effective GCS therapy in exacerbations of the disease and / or ineffectiveness of standard therapy. The recommended regimen:
- Rheumatic diseases: 1 g / day / in for 1-4 days or 1 year / month / in 6 months
- Systemic lupus erythematosus: 1 g / day / in 3 days
- Multiple sclerosis: 1 g / day / in for 3 or 5 days
- Edematous conditions, such as glomerulonephritis, lupus nephritis: 30 mg / kg / day over a 4 days or 1 g / day for 3, 5 or 7 days
Dose mentioned above should be administered for at least 30 minutes, the introduction can be repeated, if within one week after treatment has been achieved to improve, or if required by the patient’s condition. Cancer in the terminal phase – to improve the quality of life: is administered 125 mg / day / per day for up to 8 weeks. Prevention of nausea and vomiting associated with chemotherapy for cancer.chemotherapy, characterized by little or srednevyrazhennym emetic action , administered 250 mg / in for at least 5 min for 1 hour before administration of a chemotherapeutic drug at the beginning of chemotherapy, as well as after its completion. Chemotherapy, characterized by severe emetic action , administered 250 mg / in for at least 5 minutes, combined with appropriate doses of metoclopramide or butyrophenone for 1 hour prior to administration of the chemotherapy drug, followed by 250 mg / in at the beginning of chemotherapy and after the . For other indications the initial dose is 10-500 mg w / w depending on the nature of the disease. For short course in severe acute conditions may require higher doses. Initial dose not exceeding 250 mg, to be administered in / for at least 5 minutes, more than 250 mg dose is administered for at least 30 min. Subsequent doses are administered in / in or / m, and the length of intervals between administrations depends on the reaction of the patient to therapy and on his clinical condition. Babies be administered a lower dose (but not less than 0.5 mg / kg / day), but at dose selection in the first place take into account the severity of the condition and the patient’s response to therapy rather than age and body weight.
The frequency and severity of side effects depend on the duration of application, size of the dosage used and the possibility of compliance circadian rhythm destination metipred.
When using metipred may occur: On the part of the endocrine system: reduction of glucose tolerance, dianabol steroids steroid diabetes or a manifestation of latent diabetes mellitus, depression adrenal glands, Cushing’s syndrome (moon face, obesity, pituitary ary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae) delayed sexual development in children. from the digestive system: nausea, vomiting, pancreatitis, steroid gastric and duodenal ulcers, erosive esophagitis, gastrointestinal bleeding and perforation of the wall of the gastrointestinal tract, increased or decreased appetite, indigestion, flatulence, hiccups. In rare cases – increase in the activity of “liver” transaminases and alkaline phosphatase. Cardio-vascular system: arrhythmia, bradycardia (up to cardiac arrest);development (in predisposed patients) or increased severity of heart failure, changes in the electrocardiogram, characteristic gilokaliemii, increased blood pressure, hypercoagulation, thrombosis. In patients with acute and subacute myocardial infarction – the spread necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle. From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, headache, convulsions. from the sensory organs: posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, the propensity to develop secondary bacterial, fungal or viral eye infections trophic changes of the cornea, exophthalmos, sudden loss of vision (for parenteral administration in the area of the head, neck, nasal turbinate, the scalp may be the deposition of crystals of the drug in the blood vessels of the eye). On the part of metabolism: increased excretion of calcium, gipokalydaemiya, increased body weight, negative nitrogen balance (increased protein breakdown), increased sweating. Conditional mineralocorticoid activity: fluid retention and sodium (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue). From the musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones), osteoporosis (very rare -patologicheskie fractures, aseptic necrosis of the humeral head and femur), rupture of tendons of muscles, steroid myopathy, reduced muscle mass (atrophy). from the skin and mucous membranes: delayed wound healing, petechiae, ecchymosis, thinning of the skin, hyper- or hypopigmentation, steroid acne, striae, susceptibility to the development of pyoderma and candidiasis. allergic reactions: skin rash, pruritus, anaphylactic shock, local allergic reactions. local at parenteral administration: a burning sensation, numbness, pain, tingling at the site of injection, infection at the injection site, rarely – necrosis of surrounding tissue, scarring at the injection site; atrophy of the skin and subcutaneous tissue when administered intramuscularly (particularly dangerous administration in the deltoid muscle). Other:development or exacerbation of infection (the appearance of this side effect contribute jointly used immunosuppressants and vaccination), leucocyturia, “cancellation” syndrome, “tides” of blood to the head.
may be increased side effects described above. It is necessary to reduce the dose metipred. Treatment – symptomatic.
Interaction with other drugs
is possible methylprednisolone pharmaceutical incompatibility with other intravenously administered drugs – it is recommended to be administered separately from other drugs (intravenous bolus or through an IV, etc., as the second solution.). Co-administration of methylprednisolone with:
- inducers “liver” microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, rifampicin, ephedrine) leads to a decrease in its concentration (increased metabolic rate);
- diuretics (especially “thiazide” and carbonic anhydrase inhibitors) and amphotericin B – may lead to increased excretion of potassium from the body and increase the risk of heart failure; carbonic anhydrase inhibitors, and “loop” diuretics may increase the risk of osteoporosis;
- with a sodium-containing drugs – to the development of edema and high blood pressure;
- cardiac glycosides – worsening their tolerance and increases the likelihood of ventricular ekstrasitolii (due to induced hypokalemia);
- indirect anticoagulants – weakens (strengthens rarely) their effect (dose adjustment is required);
- anticoagulants and thrombolytics – increases the risk of bleeding from ulcers in the gastrointestinal tract;
- ethanol, and nonsteroidal anti-inflammatory drugs (NSAIDs) – amplifies the risk of erosive and ulcerative lesions of the gastrointestinal tract and of bleeding (in combination with NSAIDs in the treatment of arthritis may reduce the dose of corticosteroids due to the summation of therapeutic effect);
- Indomethacin – increases the risk of side effects of methylprednisolone (methylprednisolone displacement of indomethacin from its association with albumin);
- paracetamol – increases the risk of hepatotoxicity (liver enzyme induction and formation of a toxic metabolite of acetaminophen);
- acetylsalicylic acid – accelerates its excretion and reduces the concentration in the blood (with the abolition of methylprednisolone salicylate level in the blood increases, and increases the risk of side effects);
- insulin and oral hypoglycemic agents, antihypertensive agents – their effectiveness is reduced;
- vitamin D – reduced its effects on calcium absorption in the intestine;
- STH – reduces the effectiveness of the latter, and with praziquantel – its concentration;
- M-holinoblokatorami (including antihistamines and tricyclic antidepressants), and nitrates – contributes to intraocular pressure;
- isoniazid and mexiletine – increases their metabolism (especially for “slow” acetylators), which leads to a decrease in their plasma concentrations. ACTH increases the effects of methylprednisolone.
Ergocalciferol and parathyroid hormone hinder the development of osteopathy, called methylprednisolone.
Cyclosporin and ketoconazole, slowing down the metabolism of methylprednisolone, can in some cases increase its toxicity.
Concurrent administration of androgen and steroid anabolic drugs with methylprednisolone contributes to the development of peripheral edema and hirsutism, acne.
Estrogens and plural estrogensoderzhaschie contraceptives reducing methylprednisolone clearance, which may be accompanied by increased expression of his actions.
Mitotane and other inhibitors of adrenocortical function may necessitate increasing the dose of methylprednisolone.
while the use of live virus vaccines, and in comparison with other types of immunization increases the risk of activation of viruses and the development of infections.
Immunosuppressive drugs increase the risk of the development of infections and lymphoma or other lymphoproliferative disorders associated with Epstein-Barr virus.
Antipsychotic drugs (neuroleptics) and azathioprine increases the risk of developing cataracts in the appointment of methylprednisolone.
Co-administration of antacids reduces absorption of methylprednisolone.
while the use of antithyroid drugs is reduced, and since thyroid hormones – increased clearance of methylprednisolone.
Store the prepared solution for parenteral administration should be at room temperature (15 ° -20 ° C) and used within 12 hours. If the prepared solution is stored in a refrigerator at 2 ° -8 ° C, it can be used within 24 hours.
During treatment dianabol steroids metipred (especially long) must be monitored ophthalmologist, blood pressure control, the state of water and electrolyte balance, as well as patterns of peripheral blood and blood glucose concentrations.
in order to reduce the side effects may be administered antacid and increase potassium intake of (diet, potassium supplements). Food should be rich in proteins, vitamins, with the restriction of fat, carbohydrates and salt.
The drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may exacerbate existing emotional instability or psychotic disorders. When referring to the history of psychoses in metipred at high doses prescribed under the strict supervision of a physician.
Caution should be used in acute and subacute myocardial infarction -perhaps spread necrosis, slowing the formation of scar tissue and rupture of the heart muscle.
In stressful situations during maintenance treatment (eg , surgery, trauma, or infectious diseases) should be carried out correction dose due to the increased need for glucocorticosteroids.
with the sudden cancellation, particularly in the case of the prior use of high doses may develop the syndrome of “cancellation” (anorexia, nausea, lethargy, generalized myshechno- skeletal pain, general weakness), as well as exacerbation of the disease, about which he was appointed metipred.
during treatment metipred should not be vaccinated due to the reduction of its effectiveness (immune response).
by assigning metipred during intercurrent infections, septic conditions, and tuberculosis, it is necessary at the same time to treat antibiotic bactericidal action.
The children during long-term treatment metipred careful observation of the dynamics of growth and development. Children who during the treatment period were in contact with patients with measles or chickenpox, prophylaxis prescribe specific immunoglobulins.
Due to the weak mineralocorticoid effect for replacement therapy in adrenal insufficiency metipred used in combination with a mineralocorticoid.
Diabetic patients should monitor blood glucose concentration and the need to adjust the dose of hypoglycemic agents.
Showed radiological control of bone and joint system (spine images, brushes).
metipred in patients with latent infectious diseases of kidneys and the urinary tract can cause pyuria, which may be of diagnostic value. Metipred increases the content of metabolites 11- and 17-oksiketokortikosteroidov. basic steroid cycle