Active substancePrednisolonePrednisolone
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  • Dosage form: & nbspinjection
    Composition:

    In 1 ml of solution contains:

    active substance: prednisolone sodium phosphate (in terms of prednisolone) 30 mg;

    Excipients: nicotinamide, sodium metabisulphite, disodium edetate, sodium hydroxide, water for injection.

    Description:

    Transparent solution, colorless or slightly yellowish or greenish-yellowish in color.

    Pharmacotherapeutic group:glucocorticosteroid
    ATX: & nbsp

    H.02.A.B.06   Prednisolone

    Pharmacodynamics:

    Prednisolone is a synthetic glucocorticoid drug, a dehydrated analog of hydrocortisone. Has anti-inflammatory, antiallergic, immunosuppressive action, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

    Interacts with specific cytoplasmic receptors (receptors for glucocorticosteroids (GCS) are present in all tissues, especially in the liver), with the formation of a complex inducing the formation of proteins (including enzymes that regulate vital processes in cells.)

    Protein metabolism: reduces the number of globulins in plasma, increases the synthesis of albumins in the liver and kidneys (with increasing albumin / globulin ratio), reduces synthesis and enhances protein catabolism in muscle tissue.

    Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of ​​the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

    Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-phosphatase(increase in the intake of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.

    Water-electrolyte exchange: delays Na+ and water in the body, stimulates the excretion of K + (mineralocorticoid activity), reduces the absorption of Ca2+ from the gastrointestinal tract, reduces the mineralization of bone tissue.

    Anti-inflammatory effect is associated with the suppression of the release of eosinophils and mast cells by inflammatory mediators; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. It works on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins (Pg) at the level of arachidonic acid (lipocortin depresses phospholipase A2, inhibits the liberation of arachidonic acid and inhibits the biosynthesis of endoperexides, leukotrienes, promoting inflammation, allergies, etc.), the synthesis of "pro-inflammatory cytokines" (interleukin-1,tumor necrosis factor alpha, etc.); increases the resistance of the cell membrane to the action of various damaging factors.

    Immunodepressive effect is caused by involution of lymphoid tissue, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-cell migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, 2, gamma-interferon) from lymphocytes and macrophages and a decrease the formation of antibodies.

    Antiallergic effect develops as a result of reduced synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in the number of circulating basophils, T- and B-lymphocytes, mast cells; suppression of the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to mediators of allergy, inhibition of antibody formation, changes in the immune response of the body.

    In obstructive airway diseases the effect is mainly due to the inhibition of inflammatory processes, the prevention or reduction of the degree of edema of the mucous membranes,a decrease in the eosinophilic infiltration of the submucosal layer of the bronchial epithelium and the 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 bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.

    Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS.

    It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

    Pharmacokinetics:

    Up to 90% of the drug binds to plasma proteins: transcortin (cortisol-binding globulin) and albumins. Prednisolone metabolized in the liver, partially in the kidneys and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.

    It is excreted with bile and urine by glomerular filtration and is reabsorbed by tubules by 80-90%. 20% of the dose is excreted by the kidneys unchanged. Half-life from the plasma after intravenous administration is 2-3 hours.

    Indications:

    Prednisolone is used for emergency therapy in conditions requiring a rapid increase in the concentration of glucocorticosteroids in the body:

    - shock conditions (burn, traumatic, operational, toxic, cardiogenic) - with ineffectiveness of vasoconstrictors, plasma-substituting drugs and other symptomatic therapy;

    - allergic reaction (acute severe), transfusion shock, anaphylactic shock, anaphylactoid reactions;

    - brain edema (including on the background of a brain tumor or associated with surgery, radiation therapy, or head injury);

    - bronchial asthma (severe form), asthmatic status;

    - systemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);

    - acute adrenal insufficiency;

    - thyrotoxic crisis;

    - acute hepatitis, hepatic coma;

    - Reduction of inflammatory phenomena and prevention of cicatricial narrowing (with poisoning by cauterizing fluids).

    Contraindications:

    For short-term use according to vital indications, the only contraindication is hypersensitivity to Prednisolone or the components of the drug.

    In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.

    Carefully:

    Carefully the drug should be prescribed in the following diseases and conditions:

    - Diseases of the gastrointestinal tract - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis;

    - Parazitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis; systemic mycosis; active and latent tuberculosis. The use in severe infectious diseases is permissible only against the background of specific therapy;

    - Pre-and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;

    - andmmunodeficitnye status (including AIDS or HIV infection);

    - zabortion of the cardiovascular system (including the recently transferred myocardial infarction - in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle), severe chronic heart failure, arterial hypertension, hyperlipidemia);

    - endokrinnye diseases - diabetes (including a violation of tolerance to carbohydrates), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV c);

    - tsevere chronic renal and / or hepatic insufficiency, nephrourolythiasis;

    - gialoalbuminemia and conditions predisposing to its occurrence;

    - fromsystemic osteoporosis, myasthenia gravis gravis, acute psychosis, poliomyelitis (except for the form of bulbar encephalitis), open and closed angle glaucoma;

    - bVariability.

    Pregnancy and lactation:

    During pregnancy (especially in I trimester) are used only for vital indications. With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In the case of use in the III trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

    Since glucocorticosteroids penetrate into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

    Dosing and Administration:

    The dose of Prednisolone and the duration of treatment are set by the doctor individually, depending on the indications and severity of the disease.

    Prednisolone is administered intravenously (by drip or jet) or by intramuscular injection. Intravenously, the drug is usually injected first with a stream, then drip.

    In acute adrenal insufficiency a single dose of the drug is 100-200 mg, daily 300-400 mg.

    In severe allergic reactions Prednisolone is administered in a daily dose of 100-200 mg for 3-16 days.

    With bronchial asthma the drug is administered depending on the severity of the disease and the effectiveness of complex treatment from 75 to 675 mg for a course of treatment from 3 to 16 days; in severe cases, the dose may be increased to 1,400 mg per treatment course and more with a gradual dose reduction.

    With asthmatic status Prednisolone injected at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and the transition to maintenance doses.

    With thyrotoxic crisis Introduce 100 mg of the drug in a daily dose of 200-300 mg; if necessary, the daily dose can be increased to 1000 mg. The duration of administration depends on the therapeutic effect, usually up to 6 days.

    In shock, resistant to standard therapy, Prednisolone At the beginning of therapy, injections are usually given, after which they pass to a drip introduction. If the arterial pressure does not increase within 10-20 minutes, repeat the fluid administration of the drug. After excretion from the shock state, drip administration continues until blood pressure stabilizes. Single dose is 50-150 mg (in severe cases - up to 400 mg). Repeated drug is administered after 3-4 hours. The daily dose can be 300-1200 mg (with a subsequent dose reduction).

    In acute hepatic-renal insufficiency (for acute poisoning, in the postoperative and postpartum periods, etc.) Prednisolone administered at 25-75 mg per day; in the presence of indications, the daily dose can be increased to 300-1500 mg per day or more.

    With rheumatoid arthritis and systemic lupus erythematosus Prednisolone is administered in addition to the systemic administration of the drug at a dose of 75-125 mg per day for not more than 7-10 days.

    With acute hepatitis Prednisolone Enter 75-100 mg per day for 7-10 days.

    When poisoning with cauterizing liquids with burns of the digestive tract and upper respiratory tract Prednisolone is prescribed in a dose of 75-400 mg per day is for 3-18 days.

    If intravenous injection is not possible Prednisolone administered intramuscularly in the same doses. After relief of acute condition is prescribed inside Prednisolone in tablets, followed by a gradual decrease in the dose.

    With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy can not be stopped suddenly!

    Side effects:

    The frequency of development and severity of side effects depends on the duration of the application, the amount of dose used and the possibility of observing the circadian rhythm of prescription of prednisolone.

    When applying Prednisolone may be noted:

    From the endocrine system: Impaired glucose tolerance, steroid diabetes or a manifestation of latent diabetes mellitus, adrenal suppression, Cushing's syndrome (moon face, obesity, pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae) delayed sexual development in children.

    From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, gastrointestinal bleeding and perforation of the gastrointestinal wall, increased or decreased appetite, digestive disorders, flatulence, hiccough. In rare cases - increased activity of "liver" transaminases and alkaline phosphatase.

    From the cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased 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 the focus of 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, cerebral palsy, headache, convulsions.

    From the sense organs: posterior subcapsular cataract, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial, fungal or viral infections of the eyes, trophic corneal changes, exophthalmos, sudden loss of vision (with parenteral administration in the head, neck, nasal concha, scalp it is possible to deposit crystals of the drug in the vessels of the eye).

    From the side of metabolism: increased excretion of calcium, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

    Due to 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 - pathological fractures, aseptic necrosis of the humeral head and femur), rupture of tendons of muscles, steroid myopathy, loss of muscle mass (atrophy).

    From the skin and mucous membranes: delayed healing of wounds, petechiae, ecchymosis, thinning of the skin, hyper or hypopigmentation, steroid acne, striae, propensity to develop pyoderma and candidiasis.

    Allergic reactions: skin rash, itching, anaphylactic shock, local allergic reactions.

    Local reactions with parenteral administration: burning, numbness, pain, tingling at the injection site, infections at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue with the / m introduction (especially dangerous is the introduction to the deltoid muscle).

    Other: development or exacerbation of infections (the emergence of this side effect is facilitated by jointly used immunosuppressants and vaccination), leukocyturia, withdrawal syndrome.

    Overdose:

    It is possible to strengthen the above described side effects. It is necessary to reduce the dose of Prednisolone. Treatment is symptomatic.

    Interaction:

    Possible pharmaceutical incompatibility of Prednisolone with other intravenously administered drugs - it is recommended to inject it separately from other drugs (iv bolus, or through another drip as a second solution).When mixing the solution of prednisolone with heparin a precipitate forms.

    Simultaneous prescription of prednisolone with:

    - inducers of "hepatic" microsomal enzymes (phenobarbital, rifampicin, phenytoin, theophylline, ephedrine) leads to a decrease in its concentration;

    - diuretics (especially "thiazide" and inhibitors carbonic anhydrase) and amphotericin B - can lead to increased excretion of K + from the body and an increased risk of developing heart failure;

    - with sodium-containing preparations - to the development of edema and increased blood pressure;

    - cardiac glycosides - their tolerance is worsened and the likelihood of developing ventricular extrasystole (due to induced hypokalemia) increases;

    - indirect anticoagulants - weakens (less intensifies) their effect (dose adjustment is required);

    - anticoagulants and thrombolytics - Increased risk of bleeding from ulcers in the gastrointestinal tract;

    - ethanol and non-steroidal anti-inflammatory drugs (NSAIDs) - the risk of erosive and ulcerative lesions in the gastrointestinal tract and the development of bleeding increases (in combination with NSAIDs, a reduction in the dose of glucocorticosteroids due to the summation of the therapeutic effect is possible in the treatment of arthritis);

    - paracetamol - The risk of hepatotoxicity increases (induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol);

    - acetylsalicylic acid - accelerates its removal and reduces the concentration in the blood (with the withdrawal of prednisolone, the level of salicylates in the blood increases and the risk of side effects increases);

    - insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness decreases;

    - vitamin D - its influence on absorption of Ca2 + in the intestine decreases;

    - somatotropic hormone - reduces the effectiveness of the latter, and with praziquantel - its concentration;

    - M-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates - promotes increased intraocular pressure;

    - isoniazid and mexiletine - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations.

    Inhibitors of carbonic anhydrase and looped diuretics can increase the risk of osteoporosis.

    Indomethacin, displacing prednisolone from association with albumin, increases the risk of developing its side effects.

    ACTH increases the effect of prednisolone.

    Ergocalciferol and parathyroid hormone interfere with the development of osteopathy caused by prednisolone.

    Cyclosporine and ketoconazole, slowing the metabolism of prednisolone, can in some cases increase its toxicity.

    Simultaneous appointment of androgens and steroid anabolic drugs with prednisolone promotes the development of peripheral edema and hirsutism, the appearance of acne.

    Estrogens and oral estrogen-containing contraceptives reduce the clearance of prednisolone, which may be accompanied by an increase in the severity of its action.

    Mitotane and other inhibitors of adrenal cortex function may necessitate an increase in the dose of prednisolone.

    With simultaneous use with live antiviral vaccines and against other types of immunizations, increases the risk of virus activation and the development of infections.

    Antipsychotic drugs (antipsychotics) and azathioprine increase the risk of developing cataracts in the appointment of prednisolone.

    With simultaneous use with antithyroid drugs is reduced, and with thyroid hormones - increases the clearance of prednisolone.

    Special instructions:

    During treatment with prednisolone (especially prolonged), it is necessary to observe the oculist, control blood pressure, condition of water electrolyte balance, as well as patterns of peripheral blood and blood glucose levels.

    In order to reduce side effects, antacids can be prescribed, as well as increase the intake of K + into the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.

    The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug can enhance existing emotional instability or psychotic disorders. When referring to a psychosis in an anamnesis Prednisolone in high doses prescribed under the strict supervision of a doctor.

    With caution should be used in acute and subacute myocardial infarction - possibly spreading the focus of necrosis, slowing the formation of scar tissue and rupture of the heart muscle.

    In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids.

    In case of sudden cancellation, especially in case of prior application of high doses, it is possible to develop the "withdrawal" syndrome (anorexia, nausea, block, generalized musculoskeletal pain, general weakness), as well as an exacerbation of the disease for which it was prescribed Prednisolone.

    During treatment Prednisolone should not be vaccinated due to a decrease in its effectiveness (immune response).

    Assigning Prednisolone with intercurrent infections, septic states and tuberculosis, it is necessary to simultaneously perform antibiotic treatment of bactericidal action.

    In children during prolonged treatment with prednisolone, careful monitoring of the dynamics of growth and development is necessary. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.

    Due to a weak mineralocorticoid effect for replacement therapy with adrenal insufficiency Prednisolone used in combination with mineralocorticoids.

    Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.

    An x-ray control of the osteoarticular system (images of the spine, hands) is shown.

    Prednisolone in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which can have diagnostic value.

    Prednisolone increases the metabolites content of 11- and 17-oxyketocorticosteroids.

    Form release / dosage:

    Solution for injection, 30 mg / ml.

    Packaging:

    In ampoules of 1 ml.

    By 3, 5, 10 ampoules in a plastic pallet.

    For 1, 2 pallets, together with the instructions for use are placed in a cardboard box.

    Storage conditions:

    At a temperature not higher than 25 ° C, out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014426 / 01-2002
    Date of registration:19.11.2008
    The owner of the registration certificate:Shraya Life Senses Pvt. Ltd.Shraya Life Senses Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspSHREYA LIFE SENENSIZ Pvt.Ltd. SHREYA LIFE SENENSIZ Pvt.Ltd. India
    Information update date: & nbsp29.08.2015
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