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

Excipients: lactose 58.00 mg, corn starch 41.105 mg, silicon colloidal dioxide 1.00 mg, stearic acid 2.20 mg, carboxymethyl sodium starch 2.20 mg, magnesium stearate 0.250 mg, purified water (removed during production).

Description:

White or almost white round, flat tablets with bevelled edges, with a dividing risk on one side.

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 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 inblood); 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, 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 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:

Ingestion prednisolone well absorbed from the gastrointestinal tract. The maximum concentration in the blood is reached after 1-1.5 hours after oral administration. 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. The half-life from plasma after oral administration is 2-4 hours.

Indications:

- Systemic diseases of connective tissue (systemic lupus erythematosus, scleroderma, nodular periarteritis, dermatomyositis, rheumatoid arthritis);

- acute and chronic inflammatory diseases of the joints - gouty and psoriatic arthritis, osteoarthritis (including post-traumatic), polyarthritis (including senile), humeropathy periarthritis, ankylosing spondylitis (Bechterew's disease), juvenile arthritis, Still's syndrome in adults, bursitis, nonspecific tenosynovitis, synovitis and epicondylitis;

- acute rheumatism, rheumatic carditis, small chorea;

- bronchial asthma, asthmatic status;

- acute and chronic allergic diseases - incl. allergic reactions to medicines and food products, serum sickness, urticaria, allergic rhinitis, Quincke's edema, drug exanthema, pollinosis, etc .;

- diseases of the skin - pemphigus, psoriasis, eczema, atopic dermatitis (common neurodermatitis), contracted dermatitis (with damage to the large surface of the skin), toxicermy, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous herpetiform dermatitis, Stevens-Johnson syndrome ;

- cerebral edema (including on the background of a brain tumor or associated with surgery, radiation therapy or head trauma) after previous parenteral administration;

- allergic eye diseases - allergic forms of conjunctivitis;

- inflammatory diseases of the eyes - sympathetic ophthalmia, severe sluggish anterior and posterior uveitis, optic neuritis;

- primary or secondary adrenal insufficiency (including the condition after removal of the adrenal glands);

- congenital adrenal hyperplasia);

- kidney disease of autoimmune genesis (including acute glomerulonephritis);

- nephrotic syndrome;

- subacute thyroiditis;

- blood diseases and hematopoiesis system - agranulocytosis, panmyelopathy, autoimmune hemolytic anemia, lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, erythroblastopenia (erythrocyte anemia), congenital (erythroid) hypoplastic anemia;

- lung diseases - acute alveolitis, pulmonary fibrosis, sarcoidosis II-III st;

- tuberculous meningitis, fulminant or disseminated pulmonary tuberculosis, aspiration pneumonia (in combination with specific chemotherapy);

- berylliosis, Leffler's syndrome (not amenable to other therapy); lung cancer (in combination with cytostatics);

- multiple sclerosis;

- gastrointestinal diseases - ulcerative colitis, Crohn's disease, local enteritis;

- hepatitis;

- hypoglycemic conditions;

- prevention of graft rejection during organ transplantation;

- hypercalcemia on the background of cancer, nausea and vomiting during cytostatic therapy;

- myeloma disease.

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, newly created anastomosis of the intestine, ulcerative colitis with perforation or abscessing threat, diverticulitis.

- Parasitic and infectious diseases of viral,fungal or bacterial nature (ongoing or recent, 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 post vaccination), lymphadenitis after BCG vaccination.

- Immunodeficiency conditions (including AIDS or HIV infection).

- Diseases of the cardiovascular system, incl. recently suffered 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, 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:

During pregnancy (especially in I trimester) are used only for vital indications.

Since glucocorticosteroids pass 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.

The entire daily dose of the drug is recommended to take a single or double daily dose - every other day, taking into account the circadian rhythm of the endogenous secretion of glucocorticosteroids in the interval from 6 to 8 am. A high daily dose can be divided into 2-4 doses, with a large dose taken in the morning. Tablets should be taken during or immediately after meals, with a small amount of liquid.

In acute conditions and as a replacement therapy, adults are prescribed in an initial dose of 20-30 mg / day, the maintenance dose is 5-10 mg / day.If necessary, the initial dose may be 15-100 mg / day, supporting - 5-15 mg / day.

For children, the initial dose is 1-2 mg / kg of body weight per day in 4-6 receptions, supporting - 300-600 mcg / kg per day.

When the therapeutic effect is obtained, the dose is gradually reduced - 5 mg, then 2.5 mg at intervals of 3-5 days, canceling at first later receptions. With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy can not be stopped suddenly! The withdrawal of the maintenance dose is slower the longer the glucocorticosteroid therapy is used.

In case of stressful influences (infection, allergic reaction, trauma, surgery, mental overload), the dose of Prednisolone should be temporarily increased (in 1,5-3, and in severe cases - 5-10 times) in order to avoid exacerbation of the underlying disease.

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 cardiovascular system: arrhythmias, bradycardia (up to cardiac arrest); development (in predisposed patients) or increased heart failure, ECG changes 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, a tendency to develop secondary bacterial, fungal or viral infections of the eyes, trophic changes in the cornea, exophthalmos.

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

Due to mineralocorticoid activity - fluid and sodium retention in the body (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 epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures,aseptic necrosis of the head of the humerus and femur), 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, acne, striae, a tendency to develop pyoderma and candidiasis.

Allergic reactions: skin rash, itching, anaphylactic shock.

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 simultaneous administration 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 of carbonic anhydrase) and amphotericin B can lead to increased excretion of K⁺ 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) -increased risk of erosive and ulcerative lesions in the gastrointestinal tract and development of bleeding (in combination with NSAIDs in the treatment of arthritis may reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect);

- 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 is reduced;

- vitamin D - its effect on the absorption of Ca decreases²⁺ in the intestine; 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.

Simultaneous administration of antacids reduces the absorption 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 level.

In order to reduce side effects, antacids can be prescribed, as well as increased intake of K⁺ in 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.

Patients should be monitored carefully during the year after the end of long-term therapy with Prednisolone in connection with the possible development of a relative insufficiency of the adrenal cortex in stressful situations.

In case of sudden cancellation, especially in case of previous application of high doses, the development of the "withdrawal" syndrome (anorexia, nausea,generalized musculo-skeletal pain, general weakness), as well as an exacerbation of the disease, which was appointed 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:

Tablets, 5 mg.

Packaging:

For 100 tablets in a plastic bag, along with the instructions for use are placed in a plastic bottle with a screw cap.

Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.

In a place inaccessible to children.

Shelf life:

4 years.

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

Terms of leave from pharmacies:On prescription

Registration number:П N011484 / 01

Date of registration:30.03.2010

The owner of the registration certificate:Ipka Laboratories Ltd.Ipka Laboratories Ltd. India

Manufacturer: & nbsp

IPCA LABORATORIES, Ltd. India

Representation: & nbspIPKA LABORATORIES LTD. IPKA LABORATORIES LTD. India

Information update date: & nbsp28.08.2015

Illustrated instructions

Instructions

Prednisolone (Prednisolon )