Prednisolone - instructions for use, dose, side effects, contraindications

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 albumin 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 (increased 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 acts on all stages of the inflammatory process: it inhibits the synthesis of prostaglandins at the level of arachidonic acid (lipocortin depresses phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, leukotrienes that promote 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 decreased synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils, histamine, and others. bioactive substances, reducing the number of circulating basophils, suppression of lymphoid and connective tissues, reduce the number of T and B lymphocytes, mast cells, reducing the sensitivity of the effector cells to the mediators of allergy, inhibition of antibody production, changes in the immune response.

In obstructive airway diseases effect is due mainly the inhibition of inflammatory processes, prevention or reduction of severity of mucosal edema, reduction of eosinophil infiltration bronchial epithelium submucosal layer and deposition in the bronchial mucosa of circulating immune complexes and erozirovaniya inhibition and mucosal desquamation. 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:

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

- alaryngic reactions (acute severe forms), blood transfusion shock, anaphylactic shock, anaphylactoid reactions;

- aboutbrain tissue (including on the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma);

- brohnhialnaya asthma (severe form), asthmatic status;

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

- aboutadrenal insufficiency;

- tiritoksichesky crisis;

- abouthepatitis, hepatic coma;

- Reduction of inflammatory phenomena and prevention of cicatricial narrowing (when poisoning with 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 - 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 the patient) - herpes simplex, herpes zoster (viremicheskaya 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.

- Immunodeficiency (including AIDS or HIV infection).

- Diseases of the cardiovascular system (including 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).

- Endocrine diseases - diabetes (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itenko-Cushing's disease, obesity (III-IV c).

- Severe chronic renal and / or hepatic insufficiency, nephrourolythiasis.

- Hypoalbuminemia and conditions predisposing to its occurrence.

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

- Pregnancy.

Pregnancy and lactation:

When pregnancy (especially in the first trimester) is used only for life indications.

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 the drug and the duration of treatment is determined by the doctor individually, depending on the indications and severity of the disease. Prednisolone injected 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 single dose of the drug is 100 - 200 mg, daily 300-400 mg.

In severe allergic reactions Prednisolone injected 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 is administered at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and 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 25 to 75 mg of 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 administered in addition to the system receiving the drug in doses of 75-125 mg per day is not more than 7-10 days.

With acute hepatitis Prednisolone is administered at 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 prescribe a dose of 75-400 mg per day 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: depression of glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, oppression of the adrenal gland function, Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delay in 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 side of 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 possibly the deposition of drug crystals 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 - sodium and fluid retention (peripheral edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue).

From the side of the musculoskeletal system: slowing growth and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and thigh bone), rupture of the tendons of muscles, steroid myopathy, decrease in 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:

The pharmaceutical incompatibility of prednisolone with other intravenously administered drugs is possible - it is recommended to administer 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 effect on absorption is reduced Ca²⁺in the intestine;

- somatotropic hormone - It 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 may 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 the patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia. that can have diagnostic value.

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

Form release / dosage:A solution for intravenous and intramuscular administration, 30 mg / ml.

Packaging:In ampoules of light brown glass of 1 ml.

3 ampoules on a plastic pallet, 1 pallet together with instructions for use are placed in a cardboard box.

Storage conditions:In a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C. Do not freeze.

Shelf life:3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-000078

Date of registration:18.01.2010

The owner of the registration certificate:ELFA NPC, CJSC ELFA NPC, CJSC Russia

Manufacturer: & nbsp

INDUS PHARMA, PVT. Ltd. India

Information update date: & nbsp29.08.2015

Illustrated instructions

Instructions

Prednisolone (Prednisolon )