Why is there no Prednisolone in pharmacies? What to replace it with? Application and dosage. Composition, release forms and pharmacological action

Pharmacological action

Synthetic glucocorticosteroid (GCS), dehydrogenated analogue of hydrocortisone. It has anti-inflammatory, immunosuppressive and antiallergic effects.

Easily penetrating into target cells, it interacts with GCS receptors in the cytoplasm. Free receptors are usually associated with the so-called. heat shock protein (HSP90). After joining the GCS receptors, the structure of HSP90 changes and it leaves the receptor. The latter moves to the cell nucleus. The multilateral effect of steroids is due to the presence of the so-called. glucocorticoid response elements (CRE) in the promoter regions of several genes, some of which are “turned off” as a result of the attachment of receptors to their CRE, while others are in an active state. A key role in this complex process is played by the ubiquitous so-called. intracellular transcription factor Nf-kB. Various inflammatory mediators activate Nf-kB to trigger cytokine production. GCS induce transcription of the IkB protein, which captures activated Nf-kB and forms an inactive cytoplasmic complex with it. In addition, steroids activate lipocortins, which are representatives of another family of proteins, and enhance the transcription of β 2 receptor genes. The essence of the action of lipocortins is to inhibit the chain of reactions leading to the formation of prostaglandins, leukotrienes and platelet activating factor. These mediators usually increase vascular permeability, leading to tissue edema, migration of leukocytes and formation of fibrin deposits.

Prednisolone has an effect on all stages inflammatory process, among which the inhibition of phospholipase A 2 and the blockade of the formation of arachidonic acid by stimulating the synthesis of an inhibitor polypeptide, the so-called, are especially important. lipocortin-1 with subsequent suppression of the biosynthesis of inflammatory mediators, the so-called. pleiotropic cytokines of the reaction of the acute phase of inflammation: interleukin-1, TNF-α, as well as interleukins-4 and 5. In addition, it blocks the transcription of genes for such inflammatory enzymes as NO synthetase and cyclooxygenase. Suppresses the functions of neutrophils and macrophages, incl. release of chemical mediators and their effects on capillaries. Prednisolone stabilizes cell and organelle membranes (especially liposomal ones) and increases their resistance to various damaging factors. Blocking inflammatory reactions in connective tissue, prevents the formation of scar tissue.

Suppresses inflammatory process Regardless of its etiology, it has a beneficial effect in case of an excessive or “useless” inflammatory reaction, but is dangerous in infections due to the suppression of the protective inflammatory process.

The immunosuppressive effect is due to the effect of prednisolone on numerous targets, among which suppression of cytokine secretion is particularly important. Prednisolone suppresses the proliferation of lymphocytes, incl. leukemia lymphocytes, the expression of MHC II on macrophages and adhesion molecules of endothelial cells, causes eosinopenia and prevents eosinophil degranulation and neutrophil adhesion, prevents the release of cytokines by cells (mainly interleukin-2 and γ-interferon) and the secretion and release of prostaglandin E, and also blocks in fibroblasts collagen synthesis. Large doses of glucocorticosteroids suppress antibody production.

Hinders development allergic reactions. Reduces the number of circulating eosinophils, basophils and the release of immediate allergy mediators. The interaction of allergens with antibodies remains unchanged, but the damaging effects of inflammation are absent.

The drug affects various types of metabolism in the human body.

Carbohydrate metabolism: prednisolone activates gluconeogenesis (increased absorption of carbohydrates from the gastrointestinal tract, increased activity of glucose-6-phosphatase and phosphoenol-pyruvate kinase with an increase in the flow of glucose from the liver into the blood), while peripheral glucose utilization (transport of glucose across the cell membrane) may decrease, leading to hyperglycemia and sometimes glycosuria. Latent diabetes manifests itself, this effect can be used as a test to identify the prediabetic stage of the disease.

Protein metabolism: anabolism decreases (decrease in the amount of globulins, increase in albumin synthesis in the liver and kidneys, increase in the albumin/globulin ratio) with the same or even increased intensity of catabolic processes, which leads to a negative nitrogen balance with atrophy muscle tissue. Possible osteoporosis due to decreased protein matrix bone tissue, growth retardation in children, skin atrophy, which with increased capillary fragility leads to increased skin vulnerability and the formation of stretch marks. Healing of wounds and peptic ulcers is slowed down and occurs with the formation of fibrous tissue.

Fat metabolism: the synthesis of higher fatty acids and triglycerides is enhanced with the deposition of fat in the shoulder girdle, on the face and abdomen and its mobilization from the subcutaneous fatty tissue of the extremities, followed by hypercholesterolemia.

Water-electrolyte metabolism (mineralocorticoid effects): sodium retention in the renal tubules increases, potassium excretion in the urine increases. Prednisolone reduces hypercalcemia with excessive absorption of calcium from the gastrointestinal tract (sarcoidosis, vitamin D intoxication), increases urinary calcium excretion with possible stone formation.

Suppresses feedback hypothalamic-pituitary-adrenocorticoid system at long-term use(followed by delayed recovery), which, with abrupt cessation of treatment, leads to the development of adrenocorticoid insufficiency in the patient: it suppresses the synthesis and secretion of ACTH by the pituitary gland, thereby inhibiting the synthesis of endogenous glucocorticoid (and androgenic) hormones by the adrenal glands.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved within 1-2 hours. Bioavailability is 82±13%. The binding to blood proteins reaches 90-95%, with most of prednisolone bound to transcortin (cortisol-binding globulin) and albumin.

Metabolism occurs mainly in the liver and partly in the kidneys, small intestine, and bronchi. Oxidized forms are glucuronidated or sulfated. 20% is excreted by the kidneys unchanged, the rest in the form of free and conjugated metabolites. T 1/2 is 2-3 hours (2.2±0.5).

Prednisolone crosses the placental barrier and is excreted in small amounts in breast milk.

Indications

- rheumatic fever, rheumatic carditis, minor chorea;

- systemic connective tissue diseases (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis);

— multiple sclerosis;

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

bronchial asthma, status asthmaticus;

— interstitial lung diseases (acute alveolitis, pulmonary fibrosis, stage II-III sarcoidosis);

— lung cancer (in combination with cytostatics);

- berylliosis, aspiration pneumonia (in combination with specific therapy), eosinophilic Loeffler's pneumonia;

- tuberculosis (pulmonary tuberculosis, tuberculous meningitis) - in combination with specific therapy;

- primary and secondary adrenal insufficiency (including conditions after removal of the adrenal glands);

congenital hyperplasia adrenal glands;

- adrenogenital syndrome;

- subacute thyroiditis;

- acute and chronic allergic diseases(drug and food allergies, serum sickness, hay fever, atopic dermatitis, contact dermatitis involving a large surface of the body, urticaria, allergic rhinitis, Quincke's edema, Stevens-Johnson syndrome, toxicoderma);

- hepatitis;

- hypoglycemic conditions;

— autoimmune diseases (incl. acute glomerulonephritis);

nephrotic syndrome;

- inflammatory diseases of the gastrointestinal tract (nonspecific ulcerative colitis, Crohn's disease, local enteritis);

- diseases of the blood and hematopoietic organs (agranulocytosis, panmyelopathy, multiple myeloma, acute lympho- and myeloid leukemia, lymphogranulomatosis, thrombocytopenic purpura, secondary thrombocytopenia in adults, autoimmune hemolytic anemia, erythroblastopenia, congenital erythroid hypoplastic anemia);

- autoimmune and other skin diseases (eczema, seborrheic dermatitis, psoriasis, Lyell's syndrome, bullous dermatitis herpetiformis, pemphigus, exfoliative dermatitis);

- cerebral edema postoperative, post-radiation, post-traumatic, with a brain tumor (use after parenteral glucocorticosteroids);

— eye diseases, incl. allergic and autoimmune (sympathetic ophthalmia, allergic forms conjunctivitis, allergic corneal ulcers, non-purulent keratitis, iridocyclitis, iritis, severe sluggish anterior and posterior uveitis, choroiditis, neuritis optic nerve);

— prevention of transplant rejection reactions;

- hypercalcemia due to oncological diseases;

- for the prevention and relief of nausea and vomiting during cytostatic therapy.

Dosage regimen

Take orally, without chewing and with a small amount of liquid. The dose is selected individually. When prescribing, the circadian rhythm of GCS secretion should be taken into account: most of the dose (2/3) or the entire dose should be taken at morning hours, around 8 a.m., and 1/3 in the evening. Treatment is stopped slowly, gradually reducing the dose.

For adults: at acute conditions and as a replacement therapy, the initial daily dose is 20-30 mg, the maintenance daily dose is 5-10 mg. If necessary, the initial daily dose can be 15-100 mg, maintenance - 5-15 mg/day.

For children: the initial daily dose is 1-2 mg/kg body weight and is distributed into 4-6 doses, the maintenance daily dose is 300-600 mcg/kg.

Side effect

The incidence and severity of side effects depend on the duration of treatment, the dose of the drug and taking into account the daily rhythm of GCS synthesis.

From the digestive system: increased acidity gastric juice, nausea, vomiting, hiccups, flatulence, indigestion, decreased or increased appetite, steroid ulcers in the gastrointestinal tract, erosive esophagitis, perforation of the stomach or intestinal wall, bleeding from ulcers, pancreatitis, hepatomegaly, in in rare cases- increased activity of liver transaminases and alkaline phosphatase.

From the cardiovascular system: arterial hypertension, bradycardia, cardiac arrest, arrhythmia, ECG changes characteristic of hypokalemia, worsening or development of heart failure (in patients predisposed to it), myocardial dystrophy, in acute and subacute myocardial infarction, spread of necrosis, slowing down the formation of scar tissue and a tendency to myocardial rupture.

From the blood coagulation system: increased blood clotting, thrombus formation, thromboembolism.

Metabolism: negative nitrogen balance (catabolic effect), bulimia, weight gain.

From the side of water-electrolyte balance: increased potassium excretion, hypokalemic syndrome (hypokalemia, myalgia, muscle spasms, unusual weakness), sodium and water retention in the body with the formation of peripheral edema, hypernatremia, increased calcium excretion, hypocalcemia.

From the musculoskeletal system: decreased muscle mass (atrophy), muscle weakness, steroid myopathy, osteoporosis, very rarely - vertebral compression fractures, pathological fractures of long bones, aseptic necrosis humeral head and femur, rupture of muscle tendons, slower growth and ossification processes in children (premature closure of epiphyseal growth zones).

Dermatological reactions: ecchymosis, skin thinning, hyper- or hypopigmentation, facial skin hyperemia, allergic dermatitis, steroid acne, petechiae, increased sweating.

From the side of the central nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, nervousness, anxiety, insomnia, convulsions, epilepsy, cranial hypertension, dizziness, headache, cerebellar pseudotumor.

From the endocrine system: dysmenorrhea, amenorrhea, delayed sexual development in children, hyperlipoproteinemia, hirsutism, Itsenko-Cushing syndrome, adrenal insufficiency up to atrophy of the adrenal cortex, especially affecting during stress: trauma, surgery, concomitant diseases, decreased glucose tolerance, manifestation of latent diabetes mellitus, hyperglycemia up to steroid diabetes, withdrawal syndrome, increased activity of the renin-angiotensin-aldosterone system.

From the side of the organ of vision: development of secondary bacterial, viral and fungal eye diseases, posterior subcapsular steroid cataract, manifestation of latent glaucoma with possible damage to the optic nerve, trophic changes in the cornea, exophthalmos.

From the outside immune system : increased fatigue, decreased resistance to infections, exacerbation of infections (which is facilitated by the simultaneous use of immunosuppressants and vaccines), delayed wound healing, generalized or local allergic skin rash, itching, steroid vasculitis, anaphylactic shock.

Contraindications for use

In case of short-term use of the drug for health reasons, the only contraindication is hypersensitivity to the components of the drug.

The drug should be prescribed with caution for the following diseases and conditions:

- peptic ulcer and duodenum;

- acute or latent peptic ulcer;

- esophagitis;

- gastritis;

- diverticulitis;

- newly created intestinal anastomosis;

- nonspecific ulcerative colitis with the threat of perforation or abscess formation;

- predisposition to thromboembolism;

- spicy and subacute infarction myocardium;

- severe chronic heart failure;

- arterial hypertension;

- systemic mycoses;

- bacterial and fungal infections (active or recent, including contact with a patient);

— active and latent forms of tuberculosis;

- perivaccination period (8 weeks before vaccination and 2 weeks after it);

— lymphadenitis after BCG vaccination;

— immunodeficiency states (including HIV infection and AIDS);

— diabetes mellitus (including decreased glucose tolerance);

— Itsenko-Cushing's disease;

- hypothyroidism;

- hyperthyroidism;

mental disorders(For example, acute psychosis);

- polio (except for bulbar encephalitis);

- myasthenia gravis;

— stage III-IV obesity;

- severe chronic renal and/or liver failure;

- nephrolithiasis;

— hypoalbuminemia and conditions predisposing to its occurrence;

- glaucoma;

- systemic osteoporosis.

Use during pregnancy and breastfeeding

Renders adverse effect for pregnancy in animals.

During pregnancy (especially in the first trimester), prednisolone is used only for health reasons. In cases where the use of GCS is irreplaceable, women with a normal pregnancy can receive treatment similar to that prescribed to non-pregnant women. Long-term prednisolone therapy during pregnancy may be associated with a small risk of developing a gothic palate and delay intrauterine development fetus Taking the drug in the third trimester of pregnancy can lead to atrophy of the fetal adrenal cortex, which leads to the need for replacement therapy in the newborn.

During breastfeeding, glucocorticosteroids are taken with caution, since small quantities they pass into breast milk. In order to identify signs of possible adrenal suppression, the condition of children whose mothers take pharmacological doses of steroids should be carefully monitored.

Use in children

Children with bronchial asthma are contraindicated in the use of prednisolone simultaneously with sympathomimetic aerosols.

Overdose

Symptoms: increased side effects.

Drug interactions

Children with bronchial asthma are contraindicated in the use of Prednisolone simultaneously with sympathomimetic aerosols.

With the simultaneous administration of Prednisolone and indirect anticoagulants, the anticoagulant effect of the latter may be weakened, or less often, enhanced. Dose adjustment is necessary.

The combination of Prednisolone with anticoagulants and thrombolytics increases the risk of developing ulcerative bleeding from the gastrointestinal tract.

The simultaneous use of Prednisolone with salicylates increases the likelihood of gastrointestinal bleeding.

Simultaneous use with acetylsalicylic acid is accompanied by accelerated excretion and a decrease in its concentration in the blood, and when Prednisolone is discontinued, an increase in the content of salicylates in the blood with the likelihood of side effects.

The combination of Prednisolone with diuretics, especially thiazide derivatives and carbonic anhydrase inhibitors, amphotericin B, can aggravate disturbances in electrolyte metabolism, incl. increase potassium excretion (when prescribed with amphotericin B, the risk of heart failure may also increase).

The combination of Prednisolone with sodium-containing drugs leads to edema and increased blood pressure.

Concomitant use of Prednisolone with antihypertensive drugs, antidiabetic drugs and insulin reduces their effectiveness, with cardiac glycosides - increases the risk of developing glycoside intoxication with the development ventricular extrasystole as a result of hypokalemia.

Hormonal contraceptives enhance the effect of Prednisolone.

The simultaneous use of Prednisolone and ethanol or NSAIDs increases the risk of erosive and ulcerative lesions and bleeding from the gastrointestinal tract (a dose reduction of the drug may be required).

The appearance of hirsutism, acne and edema is facilitated by the simultaneous use of Prednisolone with other steroid hormonal drugs (androgens, estrogens, oral contraceptives and anabolic steroids).

Simultaneous use with hormonal contraceptives accompanied by an increase in the effect of Prednisolone due to a decrease in the clearance of the latter.

The risk of developing cataracts increases with simultaneous use of Prednisolone with antipsychotics, carbutamide and azathioprine.

Simultaneous use with inducers of microsomal liver enzymes (phenytoin and barbiturates, ephedrine, rifampicin, theophylline) leads to a decrease in the concentration and weakening of the effect of Prednisolone.

Simultaneous use of Prednisolone with M-anticholinergics, incl. antihistamines, tricyclic antidepressants and nitrates increase intraocular pressure.

Taking Prednisolone with paziquatel leads to a decrease in the concentration of the latter.

Concomitant use with paracetamol increases the hepatotoxic effect as a result of induction of liver enzymes and the formation of a toxic metabolite of paracetamol.

Simultaneous intake with vitamin D reduces the effect of the latter on the absorption of calcium in the intestine.

When taken simultaneously with growth hormone the effectiveness of the latter decreases.

Metabolism increases and the concentrations of isoniazid and mexelitine in the blood decrease when taken simultaneously with Prednisolone, especially in slow acetylators.

Carbonic anhydrase inhibitors and loop diuretics when prescribed together with Prednisolone, they can contribute to the development of osteoporosis.

Indomethacin displaces prednisolone from its binding to albumin and promotes the development of osteoporosis.

Ergocalciferol and parathyroid hormone prevent the development of prednisolone osteopathy.

ACTH enhances the effect of Prednisolone.

Cyclosporine and ketoconazole, slowing down the metabolism of Prednisolone, in some cases increase its toxicity.

When taken concomitantly with mitotane and other inhibitors of adrenal function, an increase in the dose of Prednisolone may be required.

Simultaneous use with live antiviral vaccines and other types of immunization promotes the activation of viruses with the development of infectious diseases.

Antacids reduce the absorption of Prednisolone.

Antithyroid drugs reduce, and thyroid hormones increase, the clearance of Prednisolone.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

Storage conditions

List B.

Store at a temperature of 15 to 30 °C, protected from light and out of reach of children.

Best before date:

Do not use after the expiration date stated on the packaging.

Use for liver dysfunction

Use with caution in severe liver failure.

The drug has a more pronounced effect in cases of liver cirrhosis.

Use for renal impairment

Use with caution in severe renal failure.

Use in elderly patients

There is no data on the use of the drug in elderly patients.

Special instructions

Before starting treatment, the patient should be carefully examined to identify possible contraindications. In the future, during treatment, especially long-term treatment, it is necessary to periodically repeat the examination with a study of the state of the cardiovascular system and water-electrolyte metabolism, an X-ray examination of the lungs, a study of the stomach and duodenum, the urinary system, as well as a picture of peripheral blood and blood sugar levels and urine, the organ of vision.

Treatment of children with glucocorticosteroids during the growth period is possible only according to absolute indications and with careful supervision of the attending physician.

Children receiving Prednisolone therapy and who have been in contact with patients with measles or chickenpox are prescribed specific immunoglobulins prophylactically.

During treatment with Prednisolone, you should refrain from immunization.

If there is a history of psychosis, high doses of Prednisolone should be prescribed under strict medical supervision.

For diabetes mellitus, Prednisolone is prescribed only for absolute indications. In order to reduce side effects You can prescribe anabolic steroids, increase the intake of potassium in the body (diet, potassium supplements).

For severe infectious diseases the use of Prednisolone is permissible only against the background of specific therapy.

In the case of intercurrent infections, septic conditions and tuberculosis, simultaneous chemotherapy or antibiotic therapy is necessary.

The drug has a more pronounced effect in the case of hypothyroidism and liver cirrhosis.

In Addison's disease, the simultaneous use of Prednisolone and barbiturates should be avoided, since this combination can provoke acute adrenal insufficiency (Addisonian crisis).

If treatment with Prednisolone is abruptly stopped, especially after using high doses of the drug, withdrawal syndrome or exacerbation of the underlying disease for which Prednisolone was used may develop. To avoid the development of withdrawal syndrome (decreased appetite, nausea, lethargy, generalized bone- muscle pain, general weakness), drug withdrawal is carried out over several days, gradually reducing the dose.

After discontinuation of the drug, a state of relative insufficiency of the adrenal cortex persists for several months, so monitoring of the patient should be continued. If stressful situations arise during prednisolone withdrawal, glucocorticoid drugs are prescribed temporarily and according to indications, if necessary, in combination with mineralocorticosteroids.

Due to its weak mineralocorticoid effect in adrenal insufficiency, Prednisolone is used in combination with mineralocorticoids.

For latent infections of the kidneys and urinary tract, Prednisolone provokes leukocyturia, which may have diagnostic value.

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

Prednisolone is a synthetic glucocorticoid hormone (glucocorticosteroid), similar in its spectrum of therapeutic activity to those normally produced in the human body by the adrenal glands.

Glucocorticosteroids, including Prednisolone, are used orally in the form of tablets, systemically in the form of injections, and topically - ointment is applied to the skin and eyes. The drug has anti-inflammatory, antiallergic, antishock, antiexudative, antiproliferative, antipruritic and immunosuppressive effects.

In this article we will look at why doctors prescribe the drug Prednisolone, including instructions for use, analogues and prices for this drug in pharmacies. If you have already used Prednisolone, leave your feedback in the comments.

Composition and release form

Clinical and pharmacological group: GCS for oral use.

  • Active ingredient: 1 ml of solution contains prednisolone sodium phosphate in terms of prednisolone - 30 mg;
  • Excipients: sodium hydrogen phosphate anhydrous, sodium dihydrogen phosphate dihydrate, propylene glycol, water for injection.

Release form: 1 ml or 2 ml of drug solution in an ampoule. 3, 5 or 10 ampoules per pack.

What is Prednisolone used for?

Inflammatory joint diseases:

  • acute and subacute bursitis;
  • epicondylitis;
  • acute tendovaginitis;
  • post-traumatic osteoarthritis.

Oncological diseases:

  • acute and chronic leukemia;
  • lymphomas;
  • breast cancer;
  • prostate cancer;
  • multiple myeloma.

Rheumatic diseases:

  • rheumatoid arthritis, juvenile rheumatoid arthritis (in cases resistant to other treatment methods);
  • psoriatic arthritis;
  • ankylosing spondylitis;
  • acute gouty arthritis;
  • acute rheumatic fever;
  • myocarditis (including rheumatic);
  • dermatomyositis;
  • systemic lupus erythematosus;
  • granulomatous giant cell mesoarteritis;
  • systemic scleroderma;
  • periarteritis nodosa;
  • relapsing polychondritis;
  • polymyalgia rheumatica (Horton's disease);
  • systemic vasculitis.

Endocrinological diseases:

  • adrenal insufficiency: primary (Addison's disease) and secondary;
  • adrenogenital syndrome (congenital adrenal hyperplasia);
  • acute adrenal insufficiency;
  • before surgical interventions and in severe illnesses and injuries in patients with adrenal insufficiency;
  • subacute thyroiditis.

Severe allergic diseases resistant to other therapy:

  • contact dermatitis;
  • atopic dermatitis;
  • serum sickness;
  • hypersensitivity reactions to drugs;
  • permanent or seasonal allergic rhinitis;
  • anaphylactic reactions;
  • angioedema.

Dermatological diseases:

  • exfoliative dermatitis;
  • bullous dermatitis herpetiformis;
  • severe seborrheic dermatitis;
  • severe erythema multiforme (Stevens-Johnson syndrome);
  • mycosis fungoides;
  • pemphigus;
  • severe psoriasis;
  • severe forms of eczema;
  • pemphigoid.

Hematological diseases:

  • acquired autoimmune hemolytic anemia;
  • congenital aplastic anemia;
  • idiopathic thrombocytopenic purpura (Werlhof's disease) in adults;
  • hemolysis.

Liver diseases:

  • alcoholic hepatitis with encephalopathy;
  • chronic active hepatitis.

Neurological diseases:

  • tuberculous meningitis with subarachnoid block;
  • multiple sclerosis in the acute phase;
  • myasthenia gravis.

Eye diseases (severe acute and chronic allergic and inflammatory processes):

  • severe sluggish anterior and posterior uveitis;
  • optic neuritis;
  • sympathetic ophthalmia.

Respiratory diseases:

  • bronchial asthma;
  • berylliosis;
  • Loeffler's syndrome;
  • symptomatic sarcoidosis;
  • fulminant or disseminated pulmonary tuberculosis (in combination with anti-tuberculosis chemotherapy);
  • chronic pulmonary emphysema (resistant to treatment with aminophylline and beta-agonists).

During organ and tissue transplantation to prevent and treat graft rejection (in combination with other immunosuppressive drugs).

Pharmacological action

Prednisolone is synthetic analogue The hormones cortisone and hydrocortisone secreted by the adrenal cortex. Prednisolone is 4-5 times more active than cortisone and 3-4 times more active than hydrocortisone when used orally. Unlike cortisone and hydrocortisone, prednisolone does not cause noticeable sodium and water retention and only slightly increases potassium excretion.

The drug has a pronounced anti-inflammatory, anti-allergic, anti-exudative, anti-shock, anti-toxic effect.

Instructions for use

The dosage regimen is set individually depending on the indications, the effectiveness of therapy and the patient’s condition. In accordance with the daily rhythm of secretion of endogenous glucocorticoids, the drug is recommended to be taken once a day in the morning. In some cases, more frequent use of the drug is required. After achieving the desired therapeutic effect, it is recommended to gradually reduce the dose to the minimum effective.

  1. Prednisolone tablets. At the beginning of therapy for acute and severe conditions, you should take 50–75 mg (10–15 tablets) per day, and for chronic diseases – 20–30 mg per day (4–6 tablets). After normalization of the condition, the dosage of Prednisolone is reduced to 5–15 mg per day and the tablets are continued. The duration of treatment is determined by the doctor and depends on general condition person and the effectiveness of therapy.
  2. Prednisolone ampoules. In case of shock, 50–150 mg of Prednisolone (2–5 ml of 3% (30 mg/ml) solution) is administered at a time. The same amount of solution is reintroduced every 3 to 4 hours during the first day. After this, the doctor determines whether it is necessary to continue Prednisolone injections or whether they can be stopped. In case of acute adrenal and liver failure, as well as allergic reactions, 100–200 mg of Prednisolone is administered every 8 hours. For status asthmaticus, 500–1200 mg of Prednisolone is administered once, on the second day the dosage is reduced to 300 mg, on the third day to 150 mg and on the fourth day to 100 mg. On days 5–6, Prednisolone can be discontinued if status asthmaticus does not recur.

  3. Prednisolone ointment. The ointment is applied in a thin layer to the affected areas of the skin 1 - 3 times a day for 6 - 14 days. The use of the ointment should be discontinued as soon as the therapeutic effect is achieved. It is not recommended to apply the ointment under a tight bandage, as this may cause the absorption of a large amount of ointment into the bloodstream with the development of systemic side effects. The ointment should not be used for longer than 14 days without breaks.

Prednisolone in tablets and solution is optimally administered from 6 to 8 am, and during these hours all or most of the daily dose should be taken (at least 2/3). Whenever stressful situation in a person taking glucocorticoids, Prednisolone should be administered until this effect of stress wears off.

If a person has suffered from psychosis in the past, then high dosages of Prednisolone should only be taken under the supervision of a doctor.

Contraindications

Severe forms of hypertension (persistent rise in blood pressure), diabetes mellitus and Itsenko-Cushing's disease, pregnancy, stage III circulatory failure, acute endocarditis (inflammation of the internal cavities of the heart), psychosis, nephritis (inflammation of the kidneys), osteoporosis, gastric and duodenal ulcers guts, recently previous operations, syphilis, active form tuberculosis, old age.

Prednisolone is prescribed for diabetes mellitus with caution and only for absolute indications or for the treatment of insulin resistance (lack of response and insulin administration) associated with a high titer of anti-insulin antibodies. For infectious diseases and tuberculosis, the drug should be used only in combination with antibiotics or drugs for the treatment of tuberculosis.

Special instructions

Treatment with Prednisolone should be discontinued gradually. Dose reduction is carried out by weekly reducing the dose used by ⅛ or taking the last dose every other day and reducing it by ⅕ (this method is faster).

At fast way on a day without Prednisolone, the patient is recommended to stimulate the adrenal glands using UHF or DQV on their projection, take ascorbic acid (500 mg/day), administer insulin in increasing doses (starting - 4 units, then increase it by 2 units for each dose; the highest dose is 16 units).


If Prednisolone is prescribed for bronchial asthma, it is recommended to switch to inhaled steroids. If the indication for use is an autoimmune disease, use mild cytostatics.

Side effects

The drug has certain side effects:


Weight gain, potassium deficiency (hypokalemia), growth retardation in children, Cushing's syndrome (moon face), increased blood pressure, thrombosis, muscle atrophy, thinning skin, digestive disorders, nausea. From the nervous system, manifestations such as depression, hallucinations, decreased visual acuity, general weakness, and headache are possible.

The above symptoms are possible, but they do not appear in every case. In general, the drug is well tolerated by patients, even with long-term use.

Overdose

With an overdose of Prednisolone, a sharp increase in side effects is observed. Due to the fact that mechanical blood purification does not give the desired result, it is recommended drug withdrawal symptoms.

During pregnancy and lactation

Prednisolone is contraindicated at any stage of pregnancy and lactation. IN the latter case the use of the drug is possible only after complete refusal from breastfeeding throughout the course of treatment and only when urgently needed.

Analogs

Analogs of Prednisolone in composition for dosage forms for systemic use: Prednisolone Nycomed (in ampoules), Prednisolone Nycomed in tablets, Prednisolone Bufus (solution), Medopred (solution), Prednisol (solution).

Prices

The average price of PREDNISOONE tablets in pharmacies (Moscow) is 100 rubles.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

instrukciya-po-primeneniyu.com

Prednisolone tablets belong to the pharmacological group of drugs - oral glucocorticosteroids for oral use. They have a pronounced anti-inflammatory pharmacological effect and are used for various systemic pathologies, primarily associated with autoimmune pathological process.

Prednisolone tablets have a round, flat-cylindrical shape and white. There is a chamfer on one side for easy breaking of the tablet in half. The main active ingredient of the drug is prednisolone. Its content in 1 tablet is 5 mg. It also includes auxiliary components, which include:

  • Magnesium stearate.
  • Potato starch.
  • Lactose.
  • Gelatin.

The tablets are packaged in dark glass bottles in the amount of 30 pieces. A cardboard box contains one bottle of tablets and instructions for the drug.

The active ingredient of Prednisolone tablets is a synthetic chemical derivative of glucocorticosteroids (hormones of the adrenal cortex that perform various biological functions in the body). It has a pronounced anti-inflammatory effect, which is realized through several mechanisms:

  • Inhibition (suppression) of the enzyme phospholipase A 2, which catalyzes the synthesis of prostaglandins from arachidonic acid at the site of the inflammatory reaction. Prostaglandins are the main mediators of inflammation. They are responsible for development pain, tissue swelling and hyperemia. By blocking the phospholipase A2 enzyme with prednisolone, the concentration of prostaglandins and the severity of the inflammatory reaction decreases.
  • Inhibition of the accumulation of immune system cells in tissues that are responsible for the inflammatory process (leukocytes, lymphocytes, tissue macrophages).
  • Blocking the binding of antibodies produced by B lymphocytes and plasma cells to specific receptors in tissues.

Prednisolone also has the ability to immunosuppress; it significantly reduces the functional activity of the immune system as a whole. However, the mechanism of this effect remains not fully understood to date. Prednisolone also enhances the reabsorption of water and sodium ions in the distal parts of the renal tubules, increases the catabolism (breakdown) of proteins in the human body, inhibits the synthesis of bone tissue, affects the redistribution of subcutaneous fatty tissue, and increases the concentration of glucose in the blood.


and long-term intake of prednisolone into the human body, according to the feedback principle, the production of ACTH (adrenocorticotropic hormone) in the pituitary gland, which is responsible for the functional activity of the adrenal glands, decreases. Therefore, after long-term use of Prednisolone tablets, a period of time of at least 1 month is required to restore normal functioning.

After taking a Prednisolone tablet orally, the active substance is quickly absorbed into the systemic bloodstream from the digestive tract, however, more time may be required to develop a therapeutic effect. long period time (usually taking the tablets over several times according to the dosage). Prednisolone is evenly distributed in tissues, where it acts on various cell receptors, providing a therapeutic effect. The active substance is metabolized and excreted primarily by the liver.

Today there is a significant amount of medical indications to the use of Prednisolone tablets, these include:

  • Endocrinological pathology - congenital adrenal hypoplasia (adrenogenital syndrome), primary or secondary insufficiency of the adrenal cortex, as replacement therapy before surgery in patients with adrenal insufficiency, autoimmune thyroiditis (inflammation thyroid gland due to the production of antibodies by the immune system to its cells).
  • Severe allergic pathology that cannot be treated with others medicines– contact dermatitis, serum sickness, anaphylactic shock, angioedema, allergic rhinitis, hypersensitivity reaction to various drugs.
  • Rheumatic systemic diseases in which connective tissue is affected due to an autoimmune process - rheumatism, rheumatoid arthritis, ankylosing spondylitis (ankylosing spondylitis), psoriatic arthritis, acute gouty arthritis, systemic lupus erythematosus, systemic scleroderma, dermatomyositis, systemic vasculitis, mesoarteritis, periarteritis nodosa.
  • Skin diseases - severe erythema multiforme (Stevens-Johnson disease), severe psoriasis, eczema, pemphigus, fungal skin lesions, seborrheic, exfoliative dermatitis, bullous dermatitis herpetiformis, pemphigoid.
  • Pathology of the blood system - autoimmune hemolytic anemia (acquired), hemolysis (destruction of red blood cells), congenital aplastic anemia, Werlhof's disease (idiopathic thrombocytopenic purpura).
  • Some liver diseases - chronic hepatitis in the active stage, alcoholic liver damage.
  • Inflammatory pathology of joints - bursitis in the acute and subacute course, acute tendovaginitis, epicondylitis, osteoarthritis developing as a result of injury.
  • Malignant neoplasms (oncological pathology) – breast cancer in women, prostate cancer in men, multiple myeloma, various types of lymphomas, acute and chronic leukemia.
  • Neurological pathology – tuberculous meningitis, myasthenia gravis (muscle weakness), multiple sclerosis in the active stage.
  • Eye pathology – a severe form of sluggish posterior uveitis in the active stage, sympathetic ophthalmopathy, optic neuritis.
  • Heart pathology – pericarditis.
  • Diseases of the respiratory system - berylliosis, chronic emphysema, bronchial asthma, symptomatic sarcoidosis, disseminated pulmonary tuberculosis.

Prednisolone tablets are also used to prevent tissue rejection after organ transplantation in transplantology.

Since the drug is used primarily for the treatment of severe pathologies, the list of contraindications is small:

  • Hypersensitivity to the active substance of the drug.
  • The development of severe systemic fungal infections, in which additional suppression of the immune system leads to their progression.

Before prescribing Prednisolone tablets, the doctor must make sure that there are no contraindications.

Prednisolone tablets are intended for oral use. They are used orally, usually after meals, once a day, which is associated with the daily rhythm of glucocorticosteroid secretion by the adrenal cortex (sometimes, if necessary, the frequency of taking tablets can be increased). The dose is set by the doctor individually, which depends on the type, severity and characteristics of the pathological process in the patient’s body. After achieving the required therapeutic effect, the dose is gradually reduced until it is maintained. The average daily dose for an adult varies between 5-60 mg. The maximum daily dose should not exceed 200 mg (used for acute multiple sclerosis for 7 days, then the dose is gradually reduced to 80 mg per day). For children, the dosage is set at the rate of 0.14 mg of prednisolone per 1 kg of the child’s body weight. If you miss a pill, you should take it as quickly as possible.

With short-term use of Prednisolone tablets, side effects develop extremely rarely. With longer use of the drug, the development of negative reactions from various organs and systems is possible:

  • Digestive system - steroid ulcer of the stomach or duodenum, associated with the fact that prednisolone inhibits the synthesis of prostaglandins of the digestive tract, which perform protective function, perforation of an ulcer or bleeding from it, periodic nausea, vomiting, increased appetite, inflammation of the pancreas (pancreatitis), esophagus (esophagitis) with the formation of ulcers in it, disruption of the digestive process, increased gas formation in the intestines (flatulence).
  • Nervous system - increased intracranial pressure, which is accompanied by congestive optic disc syndrome (more often develops in children), sleep disturbances, convulsions, severe dizziness, headache, fainting.
  • Endocrine system - disruption of the functional activity of the adrenal cortex (adrenal insufficiency), suppression of the growth process in children, increased blood sugar (hyperglycemia), menstrual irregularities in women, manifestation of latent (latent) diabetes mellitus, hirsutism (increased hair growth of the skin, which is especially noticeable in women).
  • Water-electrolyte balance is the retention of water and salts in the body, accompanied by an increase in blood pressure, as well as the development of circulatory failure.
  • Musculoskeletal system - muscle weakness, increased bone fragility (osteoporosis), which causes subsequent pathological fractures, including compression fractures of some vertebrae.
  • Skin and subcutaneous tissue– thinning (atrophy) of the skin, stretch marks on it, deterioration of wound healing, erythema (redness of the skin), increased sweating (hyperhidrosis), the appearance of acne, pinpoint hemorrhages on the skin (petechiae).
  • Eyes – cataracts, increased intraocular pressure, which subsequently develops glaucoma, exophthalmos.
  • Higher nervous activity– symptoms of psychosis may appear, especially in the first 2 weeks after starting to take Prednisolone tablets, more often develops in women and in people with systemic lupus erythematosus.
  • Metabolism is a negative nitrogen balance in the body, which is caused by increased destruction of proteins and an increase in body weight.
  • Indicators laboratory research– a decrease in the number of leukocytes (leukopenia), platelets (thrombopenia), an increase in the level of calcium in the blood, urine, an increase in the level of triglycerides, total cholesterol, as well as low and very low density lipoproteins.
  • Allergic reactions - rarely, while taking Prednisolone tablets, the development of anaphylactic shock with multiple organ failure and a progressive decrease in blood pressure is possible.

If side effects develop, the doctor decides whether to discontinue Prednisolone tablets on an individual basis, depending on their type, nature and severity.

Prednisolone tablets are prescribed only by a doctor; they are prescription drugs. The specialist must take into account special instructions regarding the use of the drug before prescribing it, these include:

  • If a patient has a systemic fungal infection while taking Prednisolone tablets, its course may progress, since they suppress the activity of the immune system.
  • When the patient’s body is exposed to stress factors, it is recommended to switch to parenteral forms of glucocorticosteroids, which are administered intravenously or intramuscularly.
  • Sudden withdrawal of Prednisolone tablets is excluded, as this can lead to the development of acute adrenal insufficiency, so the dosage is reduced gradually.
  • Against the background of the use of the drug, the manifestation of diabetes mellitus, as well as the latent course of amebiasis (in persons with signs of intestinal infection lower parts of the digestive tract, as well as those arriving from tropical countries, before prescribing Prednisolone tablets, a test for dysenteric amoebiasis is required).
  • Long-term use of Prednisolone tablets may result in the development of glaucoma, so periodic examination by an ophthalmologist is required, as well as measurement of intraocular pressure.
  • The use of the drug in high doses requires periodic monitoring of blood pressure levels, as well as the patient’s weight.
  • For patients with tuberculosis, the drug can be prescribed only when the disseminated form has a fulminant course.
  • Vaccination of the patient with vaccines containing live but weakened pathogenic microorganisms (bacteria, viruses) during treatment with the drug is excluded.
  • Against the background of liver cirrhosis, as well as in patients with concomitant hyperthyroidism (increased activity of the thyroid gland), the therapeutic effect of the drug is enhanced.
  • With caution, Prednisolone tablets are prescribed to patients with hypoprothrombinemia, with nonspecific ulcerative colitis, the presence of an abscess (limited purulent cavity) of any location.
  • With long-term use of the drug, the risk of developing osteoporosis (increased bone fragility) associated with calcium leaching increases significantly.
  • Taking tablets after meals significantly reduces the risk of complications from the digestive system.
  • When prescribing Prednisolone tablets, it is imperative to monitor their growth and development indicators.
  • In men, the drug may lead to a decrease in the number of sperm per unit volume of semen.
  • Pregnant women should use the drug with caution and only for health reasons.
  • Prednisolone tablets can interact with a significant number of drugs from other pharmacological groups.
  • Data on the effect of the drug on the speed of psychomotor reactions are not provided, however, due to the possible development of side effects from the nervous system during its use, it is better to abandon the potential dangerous species activities.

Prednisolone tablets are sold in pharmacies only with a doctor's prescription. Their independent use is not allowed.

The risk of overdose increases significantly with long-term use of Prednisolone. This is manifested by an increase in systemic blood pressure, the development of peripheral edema, and the appearance or intensification of side effects. In this case, the drug is temporarily stopped and then the dosage is reduced.

For Prednisolone tablets, structural analogs are the drugs Decortin, Prednisone, Medopred.

The shelf life of Prednisolone tablets is 3 years. They must be stored in a dry, dark, cool place, out of reach of children, in the original original packaging.

The average cost of Prednisolone tablets in Moscow pharmacies varies between 66-68 rubles.

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Indications for use of Prednisolone

Indications for prescribing Prednisolone are the following diseases of the spinal column:

  • Injuries to nerves and joints in the spine
  • Osteoarthritis
  • Inflammation of the spinal cord or its membranes
  • Osteochondrosis
  • Arthritis of non-infectious origin
  • Ankylosing spondylitis
  • Swelling of muscles, nerves and other structures of the spinal column
  • No effect from drug therapy spine
  • Injuries of the spine, its joints, blood vessels and nerves, as well as the spinal cord
  • Severe pain in the spine

Contraindications to the use of Prednisolone

Contraindications to prescribing Prednisolone are the following conditions in the patient:

  • Lactation period
  • During pregnancy (especially before 12 weeks of gestation)
  • Tuberculosis
  • Cushing's disease or syndrome
  • Nephritis
  • Hypertension
  • Allergy to the drug and its components
  • Endocarditis, acute form
  • Syphilis
  • Heart failure stage 3
  • Ulcers in the stomach or intestines

How Prednisolone works

Prednisolone is one of the most active drugs this group. Among the effects of the drug on the human body, the main ones are anti-inflammatory, analgesic, decongestant and antitoxic. The drug also potentiates the actions of other medications prescribed for the treatment of spinal diseases.

Such properties of the drug are due to the fact that it affects hormone-receptor compounds, penetrates the cell nucleus, and reduces the production of certain enzymes and other chemical compounds.

Instructions for use of Prednisolone

Prednisolone in tablet form

The drug is administered orally with sufficient quantity liquids. The first dose is usually 20-30 mg per dose, 1 time per day. As a maintenance dose, 5-10 mg per day is usually sufficient. Maximum daily dosage medicine is 100 mg. The duration of treatment depends on the patient’s condition and is selected strictly individually. The dose of the drug must be reduced gradually over several days or weeks.

For children, if necessary, Prednisolone is prescribed 1 mg per kg of the child’s weight per day, divided into 4-6 doses. As a maintenance dosage, 300-600 mcg per kg of baby’s weight per day is sufficient.

Prednisolone in the form of a solution for injection

It can be administered either intramuscularly (deep into the gluteal muscle) or intravenously. The first injection is usually 30-45 mg. If necessary, do a second one the next day - 30-60 mg. After this, they switch to tablet form.

Children from 2 to 12 months are prescribed 2-3 mg per kg, from 1 year to 14 years - 1-2 mg per kg. Over 14 years old - adult dosage.

You can also do intra-articular injections - 10 mg of Prednisolone in one joint once.

Prednisolone in ointment form for external use

The ointment is applied to the affected area of ​​the spine 1-2 times a day. The course of treatment is 10-14 days.

Side effects of Prednisolone

Side effects of Prednisolone include the following manifestations in the patient:

  • Increased body hair (hirsutism) in women
  • Obesity
  • Menstrual irregularities
  • Pathological fractures due to increased bone fragility (with frequent and long-term use)
  • Adrenal insufficiency
  • Increased blood glucose
  • Ulcerations on the mucous membrane of the gastrointestinal tract, especially in the stomach
  • Sexual dysfunction

If such symptoms occur, symptomatic treatment. If the patient's health condition allows, then Prednisolone is discontinued.

No cases of overdose have been reported. If the prescribed dose is exceeded and any signs of intoxication occur, it is recommended to consult a doctor and take symptomatic treatment.

Special instructions

During lactation, it is necessary to avoid breastfeeding for the entire period of treatment with Prednisolone. Prednisolone is contraindicated during pregnancy under 12 weeks. At a later date, it will only be possible if absolutely necessary.

Children are allowed to take Prednisolone, but they should stick to it as much as possible. exact dosages and take the drug only when absolutely necessary.

Alcoholic drinks do not affect the way Prednisolone works in the body.

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Composition and release form

The following types of medicine are produced:

  • Solution for intravenous and intramuscular administration 30 mg/ml - 1 ml; 15 mg/ml - 2 ml.
  • Tablets 1 and 5 mg.
  • Ointment for external therapy 0.5%.
  • Eye drops 0.5%.

The composition of Prednisolone in ampoules includes the active substance at a concentration of 30 mg/ml, as well as sodium pyrosulfate (additive E223), disodium edetate, nicotinamide, sodium hydroxide, and water.

Prednisolone tablets, which help the medicine for many indications, include: 1 or 5 mg of the active substance and excipients.

Prednisolone ointment contains 0.05 g of active substance, soft white paraffin, glycerin, stearic acid, methyl and propyl parahydroxybenzoate, Cremophor A25 and A6, purified water.

Pharmacological properties

The drug (ointment, drops, injections, tablets) Prednisolone, which helps with complex pathologies, has a pronounced anti-inflammatory, anti-allergic, anti-exudative, anti-shock, anti-toxic effect. The anti-inflammatory effect of prednisolone is achieved mainly with the participation of cytosolic glucocorticosteroid receptors.

The hormone-receptor complex, penetrating into the nucleus of the skin target cells (keratinocytes, fibroblasts, lymphocytes), enhances the expression of genes encoding the synthesis of lipocortins, which inhibit phospholipase A2 and reduce the synthesis of arachidonic acid metabolic products, cyclic endoperoxides, prostaglandins and thromboxane.

The antiproliferative effect of prednisolone is associated with inhibition of the synthesis of nucleic acids (primarily DNA) in the cells of the basal layer of the epidermis and fibroblasts of the dermis. The antiallergic effect of the drug is due to a decrease in the number of basophils, direct inhibition of the synthesis and secretion of biologically active substances.

When taken orally, it is well absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is reached 90 minutes after administration.

Prednisolone - hormonal or not?

Prednisolone is a hormonal drug for local and systemic use with an average duration of action. The drug is 4-5 times more active than cortisone and 3-4 times more active than hydrocortisone when administered orally. Unlike cortisone and hydrocortisone, prednisolone does not cause noticeable sodium and water retention and only slightly increases potassium excretion.

Medicine Prednisolone: ​​what helps

Indications for use of tablets and solution for injection

Systemic use is advisable for:

  • hepatitis;
  • eosinophilic and aspiration pneumonia, tuberculous meningitis, pulmonary tuberculosis (as an addition to specific therapy);
  • autoimmune and other skin diseases (including Dühring's disease, psoriasis, eczema, pemphigus, Lyell's syndrome, exfoliative dermatitis);
  • multiple sclerosis;
  • granulomatous thyroiditis;
  • lung cancer (with cytostatics);
  • acute and chronic diseases that are accompanied by inflammation in the joints and periarticular tissue;
  • allergic diseases;
  • cerebral edema;
  • inflammatory diseases of the gastrointestinal tract;
  • status asthmaticus and asthma;
  • minor chorea, rheumatic fever, rheumatic carditis;
  • hypercalcemia developing against the background of cancer.
  • diseases of the hematopoietic organs and blood (leukemia, anemia and diseases associated with damage to the hemostatic system);
  • congenital adrenal hyperplasia (CAH) or dysfunction of their cortex;
  • diffuse connective tissue diseases;
  • hypoglycemic conditions;
  • nephrotic syndrome;
  • autoimmune diseases;
  • interstitial diseases of the lung tissue (fibrosis, acute alveolitis, sarcoidosis, etc.);
  • primary and secondary hypocortisolism(including after adrenalectomy);
  • eye diseases (including autoimmune and allergic; including uveitis, allergic ulcerative keratitis, allergic conjunctivitis, sympathetic ophthalmia, choroiditis, iridocyclitis, non-purulent keratitis, etc.).

Indications for the use of injections are emergency conditions, for example, an acute attack of food allergies or anaphylactic shock. After several days of parenteral use, the patient is usually transferred to the tablet form of Prednisolone.

Indications for the use of tablets are chronic and severe pathologies (for example, bronchial asthma).

Prednisolone solution and tablets are also used to prevent transplant rejection and relieve nausea/vomiting in patients receiving cytostatics.

Why are eye drops prescribed?

Eye drops are prescribed to relieve inflammation of a non-infectious nature affecting the anterior segment of the eye, as well as inflammation that develops after an eye injury or ophthalmic surgery.

Local use of Prednisolone is justified for the following eye diseases:

  • iritis;
  • scleritis;
  • blepharitis;
  • keratitis;
  • episcleritis;
  • sympathetic ophthalmia;
  • iridocyclitis;
  • blepharoconjunctivitis;
  • allergic conjunctivitis;
  • uveitis

Prednisolone ointment: what is it prescribed for?

As an external agent, prednisolone is used for allergies and for the treatment of inflammatory skin diseases non-microbial etiology. Indications for use of the ointment are as follows:

  • dermatitis (contact, allergic and atopic);
  • discoid lupus erythematosus;
  • psoriasis;
  • eczema;
  • limited neurodermatitis;
  • hives;
  • erythroderma;
  • toxicoderma.

Contraindications

The instructions prohibit the use of Prednisolone in the following cases:

  • peptic ulcer of the stomach and duodenum;
  • active form of tuberculosis;
  • nephritis (kidney inflammation);
  • acute endocarditis (inflammation of the internal cavities of the heart);
  • severe forms of hypertension (persistent rise in blood pressure);
  • diabetes mellitus and Itsenko-Cushing's disease;
  • osteoporosis;
  • recent operations;
  • psychoses;
  • old age;
  • syphilis,
  • circulatory failure stage III,
  • pregnancy.

Prednisolone: ​​instructions for use

Injections

The solution is administered intravenously, intramuscularly and intraarticularly. The method of administration and dosage of Prednisolone (Prednisolone Nycomed, Prednisolone hemisuccinate) are selected individually by the attending physician, taking into account the type of pathology, the severity of the patient’s condition, and the location of the affected organ.

In severe and life-threatening conditions, the patient is prescribed pulse therapy using ultra-high doses for a short period of time. For 3-5 days, he is given 1-2 g of prednisolone daily by intravenous drip infusion. The duration of the procedure is from 30 minutes to 1 hour.

During treatment, the dosage is adjusted depending on the patient's response to therapy. It is considered optimal to administer Prednisolone intravenously. For intra-articular administration, ampoules with Prednisolone are used only in cases where the tissue inside the joint is affected by the pathological process.

Positive dynamics are a reason to transfer the patient to tablets or suppositories with prednisolone. Treatment with tablets is continued until stable remission develops. If it is not possible to administer Prednisolone intravenously, the medicine should be injected deep into the muscle. However, it should be borne in mind that with this method it is absorbed more slowly.

Depending on the pathology, the dose can range from 30-1200 mg/day. (with its subsequent decrease).

Children aged from two months to 1 year are administered from 2 to 3 mg/kg. Dosage for children from one to 14 years of age is 1-2 mg/kg (as a slow, 3-minute intramuscular injection). If necessary, after 20-30 minutes the medicine is re-administered in the same dose.

If a large joint is affected, 25 to 50 mg of prednisolone is injected into it. From 10 to 25 mg is injected into medium-sized joints, and from 5 to 10 mg into small joints.

Instructions for use of Prednisolone tablets

The patient is transferred to taking tablets, following the principle of gradual withdrawal of GCS.

If HRT is used, the patient is prescribed 20 to 30 mg of prednisolone per day. Maintenance dose - from 5 to 10 mg/day. For some pathologies - for example, with nephrotic syndrome - it is advisable to prescribe higher doses.

For children, the starting dose is 1-2 mg/kg/day. (it should be divided into 4-6 doses), maintenance - from 0.3 to 0.6 mg/kg/day. When prescribing, the daily secretory rhythm of endogenous steroid hormones is taken into account.

Using eye drops

Instillations of the drug are carried out 3 times a day, instilling 1-2 drops of solution into the conjunctival cavity of the affected eye. IN acute phase diseases, the instillation procedure can be repeated every 2-4 hours.

For patients who have undergone ophthalmic surgery, drops are prescribed 3-5 days after surgery.

Prednisolone ointment: instructions for use

The ointment is a means of external therapy. It should be applied to the affected areas of the skin in a thin layer from 1 to 3 times a day. An occlusive dressing can be applied to limited pathological lesions to enhance the effect.

When used in children over one year of age, the drug should be used for the shortest possible course. You should also exclude measures that enhance the absorption and resorption of prednisolone (occlusive, fixing, warming dressings).

How long can you take Prednisolone?

Glucocorticosteroid therapy is aimed at achieving maximum effect with the lowest possible doses.

The duration of treatment depends on the patient's diagnosis and individual response to treatment. In some cases, the course lasts up to 6 days; with HRT it lasts for months. The duration of external therapy using Prednisolone ointment is usually from 6 to 14 days.

Side effect

Using the drug can cause the following negative reactions in the body:

  • acne;
  • convulsions;
  • osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of the head of the humerus and femur);
  • trophic changes in the cornea;
  • disorientation;
  • delayed sexual development in children;
  • increased intracranial pressure;
  • skin rash;
  • hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness and fatigue);
  • insomnia;
  • suppression of adrenal function;
  • steroid ulcer of the stomach and duodenum;
  • fluid and sodium retention in the body (peripheral edema);
  • hallucinations;
  • increased calcium excretion;
  • nausea, vomiting;
  • weight gain;
  • decreased glucose tolerance;
  • increased blood pressure;
  • gastrointestinal bleeding and perforation of the gastrointestinal tract wall;
  • ECG changes characteristic of hypokalemia;
  • increased or decreased appetite;
  • increased intraocular pressure with possible damage optic nerve;
  • muscle tendon rupture;
  • euphoria;
  • striae;
  • flatulence;
  • Itsenko-Cushing syndrome (moon-shaped face, pituitary-type obesity, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, stretch marks);
  • increased sweating;
  • dizziness;
  • nervousness or restlessness;
  • manic-depressive psychosis;
  • steroid diabetes mellitus or manifestation of latent diabetes mellitus;
  • slower growth and ossification processes in children (premature closure of epiphyseal growth zones);
  • arrhythmias;
  • erosive esophagitis;
  • development or exacerbation of infections (the appearance of this side effect is facilitated by jointly used immunosuppressants and vaccination);
  • anaphylactic shock;
  • tendency to develop secondary bacterial, fungal or viral eye infections;
  • hiccups;
  • paranoia;
  • withdrawal syndrome;
  • depression;
  • headache;
  • bradycardia (up to cardiac arrest);
  • indigestion;
  • decreased muscle mass (atrophy);
  • delayed wound healing.

Signs of withdrawal syndrome

One of the consequences of the use of GCS may be “withdrawal syndrome”. Its severity depends on functional state adrenal cortex. In mild cases, after stopping treatment with Prednisolone, malaise, weakness, fatigue, muscle pain, loss of appetite, hyperthermia, and exacerbation of the underlying disease are possible.

In severe cases, the patient may develop a hypoadrenal crisis, which is accompanied by vomiting, convulsions, and collapse. Without the introduction of GCS into short terms death occurs from acute cardiovascular failure.

How to “get off” Prednisone?

Treatment with Prednisolone should be discontinued gradually. Dose reduction is carried out by weekly reducing the dose used by 1/8 or taking the last dose every other day and reducing it by 1/5 (this method is faster).

With the fast method, on a day without Prednisolone, the patient is shown stimulation of the adrenal glands using UHF or DQV on their projection, taking ascorbic acid (500 mg/day), administering insulin in increasing doses (starting - 4 units, then for each dose it is increased by 2 units; highest dose - 16 units).

Insulin should be injected before breakfast, and the person should remain under observation for 6 hours after the injection.

If Prednisolone is prescribed for bronchial asthma, it is recommended to switch to inhaled steroids. If the indication for use is an autoimmune disease, use mild cytostatics.

During pregnancy and breastfeeding

Prescription of GCS during pregnancy and women childbearing age permissible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Women of childbearing age should be informed of the potential risks of GC therapy to the fetus.

Prednisolone is excreted in breast milk and can cause undesirable effects in a breastfed baby (growth retardation or inhibition of the production of endogenous adrenal hormones). If it is necessary to use the drug during lactation, breastfeeding should be stopped.

During pregnancy, especially in the first trimester, prednisolone should be prescribed with extreme caution.

Special instructions

Treatment with Prednisolone should be stopped slowly, gradually reducing the dose. For patients with a history of psychosis, high doses are allowed to be prescribed only under the strict supervision of a physician.

Analogues of the drug Prednisolone

Structural analogues of the active substance:

  • Solyu-Decortin H25.
  • Solyu-Decortin N50.
  • Prednisolone 5 mg Yenapharm.
  • Prednisolone Nycomed.
  • Prednisolone buffus.
  • Decortin N20.
  • Decortin N5.
  • Solyu-Decortin N250.
  • Prednisolone sodium phosphate.
  • Prednisolone-Ferein.
  • Prednisol.
  • Decortin H50.
  • Medopred.
  • Prednisolone hemisuccinate.

Similar drugs with a similar mechanism of action:

  • Betamethasone.
  • Triamcinolone.
  • Kenalog.
  • Flosteron.
  • Dexamed.
  • Hydrocortisone.
  • Dexazone.
  • Dexamethasone.
  • Rectodelt.
  • Lemod.
  • Deltason.
  • Medrol.
  • Metipred.

Price

In Moscow and St. Petersburg, you can buy the drug Prednisolone for 26-110 rubles. Its price in Kyiv reaches 30-50 hryvnia. Pharmacies offer to purchase tablets in Minsk for 1-3 bel. rubles The price in Kazakhstan is 1200 tenge.


Analogues of the drug prednisolone are presented, in accordance with medical terminology, called “synonyms” - drugs that are interchangeable in their effects on the body, containing one or more identical active ingredients. When selecting synonyms, consider not only their cost, but also the country of production and the reputation of the manufacturer.

Description of the drug

Prednisolone- GKS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. It disrupts the ability of macrophages to phagocytose, as well as to form interleukin-1. Helps stabilize lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to the release of histamine. Suppresses fibroblast activity and collagen formation.

Inhibits the activity of phospholipase A 2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.

Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses the formation of antibodies.

Prednisolone suppresses the release of ACTH and β-lipotropin by the pituitary gland, but does not reduce the level of circulating β-endorphin. Inhibits the secretion of TSH and FSH.

When directly applied to blood vessels, it has a vasoconstrictor effect.

Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys and increases the activity of gluconeogenesis enzymes. In the liver, prednisolone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose levels activates the release of insulin.

Prednisolone inhibits the uptake of glucose into fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which promotes fat accumulation.

It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone, it affects the processes of water-electrolyte metabolism: it promotes the excretion of potassium and calcium ions, the retention of sodium and water ions in the body. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, growth suppression in children is possible.

In high doses, prednisolone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.

For systemic use therapeutic activity prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

When external and local application The therapeutic activity of prednisolone is due to its anti-inflammatory, antiallergic and antiexudative (due to the vasoconstrictor effect) effect.

Compared with hydrocortisone, the anti-inflammatory activity of prednisolone is 4 times greater, mineralocorticoid activity is 0.6 times less.

List of analogues

Pay attention! The list contains synonyms of Prednisolone having similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by your doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from Eastern Europe: KRKA, Gedeon Richter, Actavis, Egis, Lek, Hexal, Teva, Zentiva.


Release form(by popularity)Price, rub.
Ointment 0.5% - 10g Altaivit (Altaivitamins CJSC (Russia)16
30mg / 1ml No. 3 amp Induspharma (Elfa NPC CJSC (Russia)32
0.5% 15g ointment (Sintez OJSC (Russia)35.20
5mg No. 100 tab GR (Gedeon Richter OJSC (Hungary)111.70
Tab 5mg N100 GR (Gedeon Richter Romania A.O. (Romania)114.40
R - r for v / ven. and v / mouse. input 30 mg/ml 1 ml ampoule, 10 pcs. (Medokemi Ltd, Cyprus)182
Amp 30mg / 1ml N1 Agio (Agio Pharmaceuticals Ltd (India)24.60
30mg/ml 1ml No. 3 r - r i/v i/m Agio. ..6870 (Agio Pharmaceuticals Ltd (India)25
Tablets 5 mg, 30 pcs. (Nycomed, Norway)44
Ampoules 25 mg/ml, 1 ml, 3 pcs. (Nycomed, Norway)53
Ampoules 25 mg/ml, 1 ml, 50 pcs. (Nycomed, Norway)452

Reviews

Below are the results of surveys of site visitors about the drug prednisolone. They reflect the personal feelings of those surveyed and cannot be used as an official recommendation for treatment with this drug. We strongly recommend that you contact a qualified medical specialist to select a personal course of treatment.

Visitor survey results

Two visitors reported effectiveness


Your answer about side effects »

Two visitors reported cost estimates

Participants%
Not expensive1 50.0%
Dear1 50.0%

Your answer about the cost estimate »

Seven visitors reported frequency of intake per day

How often should you take Prednisolone?
Most respondents most often take this drug once a day. The report shows how often other survey participants take this drug.
Participants%
1 time per day4 57.1%
2 times a day3 42.9%

Your answer about the frequency of intake per day »

32 visitors reported dosage

Participants%
1-5mg20 62.5%
11-50mg6 18.8%
6-10mg4 12.5%
51-100mg2 6.2%

Your answer about dosage »

Three visitors reported an expiration date

How long does it take to take Prednisolone to feel an improvement in the patient’s condition?
In most cases, survey participants felt an improvement in their condition after 1 day. But this may not correspond to the period after which you will begin to improve. Check with your doctor for how long you need to take this medicine. The table below shows the results of the survey on the initiation of effective action.
Your answer about the start date »

Three visitors reported reception times

When is the best time to take Prednisolone? empty stomach, before, after or during meals?
Site users most often report that they take this medication before meals. However, your doctor may recommend a different time for you. The report shows when the remaining patients surveyed take their medication.
Your answer about the reception time »

56 visitors reported the patient's age


Your answer about the patient's age »

Visitor reviews


There are no reviews yet

Official instructions for use

There are contraindications! Read the instructions before use

The information on the page was verified by physician-therapist E.I. Vasilyeva.

Pharmacological action

GCS. Suppresses the functions of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ​​inflammation. It disrupts the ability of macrophages to phagocytose, as well as to form interleukin-1. Helps stabilize lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in the area of ​​inflammation. Reduces capillary permeability due to the release of histamine. Suppresses fibroblast activity and collagen formation.
Inhibits the activity of phospholipase A 2, which leads to suppression of the synthesis of prostaglandins and leukotrienes. Suppresses the release of COX (mainly COX-2), which also helps to reduce the production of prostaglandins.
Reduces the number of circulating lymphocytes (T- and B-cells), monocytes, eosinophils and basophils due to their movement from the vascular bed into the lymphoid tissue; suppresses the formation of antibodies.
Prednisolone suppresses the release of ACTH and b-lipotropin by the pituitary gland, but does not reduce the level of circulating b-endorphin. Inhibits the secretion of TSH and FSH.
When directly applied to blood vessels, it has a vasoconstrictor effect.
Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. Stimulates gluconeogenesis, promotes the uptake of amino acids by the liver and kidneys and increases the activity of gluconeogenesis enzymes. In the liver, prednisolone enhances the deposition of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from protein metabolism products. An increase in blood glucose levels activates the release of insulin.
Prednisolone inhibits the uptake of glucose into fat cells, which leads to activation of lipolysis. However, due to increased insulin secretion, lipogenesis is stimulated, which promotes fat accumulation.
It has a catabolic effect in lymphoid and connective tissue, muscles, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone, it affects the processes of water-electrolyte metabolism: it promotes the excretion of potassium and calcium ions, the retention of sodium and water ions in the body. Osteoporosis and Itsenko-Cushing syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, growth suppression in children is possible.
In high doses, prednisolone can increase the excitability of brain tissue and help lower the seizure threshold. Stimulates excess production of hydrochloric acid and pepsin in the stomach, which leads to the development of peptic ulcers.
When used systemically, the therapeutic activity of prednisolone is due to its anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.
When applied externally and locally, the therapeutic activity of prednisolone is due to its anti-inflammatory, antiallergic and antiexudative (due to the vasoconstrictor effect) effect.
Compared with hydrocortisone, the anti-inflammatory activity of prednisolone is 4 times greater, mineralocorticoid activity is 0.6 times less.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. The maximum plasma concentration is observed after 90 minutes. In plasma, most of the prednisolone is bound to transcortin (cortisol-binding globulin). Metabolized primarily in the liver.
The half-life is approximately 200 minutes. Excreted unchanged by the kidneys - 20%.

Indications

For oral and intramuscular use: rheumatism; rheumatoid arthritis; dermatomyositis; periarteritis nodosa; scleroderma; Bekhterev's disease; bronchial asthma, status asthmaticus; acute and chronic allergic diseases; Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis; agranulocytosis, various shapes leukemia, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, itching, exfoliative dermatitis, psoriasis, prurigo, eczema, seborrheic dermatitis, lupus erythematosus, erythroderma, psoriasis, alopecia.
For use in ophthalmology: allergic, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment choroid, sclera and episclera; sympathetic inflammation eyeball; after injuries and operations with prolonged irritation of the eyeballs.
For intra-articular administration: chronic polyarthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic lesions of individual joints, arthrosis.
For infiltration administration into tissues: epicondylitis, tendovaginitis, bursitis, humeroscapular periarthritis, keloids, sciatica, Dupuytren's contracture, rheumatic and similar lesions of joints and various tissues.

Dosage regimen

When taken orally for replacement therapy in adults, the initial dose is 20-30 mg/day, the maintenance dose is 5-10 mg/day. If necessary, the initial dose can be 15-100 mg/day, maintenance - 5-15 mg/day. The daily dose should be reduced gradually. For children, the initial dose is 1-2 mg/kg/day in 4-6 divided doses, maintenance dose is 300-600 mcg/kg/day.
When administered intramuscularly, the dose, frequency and duration of use are determined individually. With intra-articular injection into large joints a dose of 25-50 mg is used, for medium-sized joints - 10-25 mg, for small joints - 5-10 mg. For infiltration into tissue, depending on the severity of the disease and the size of the affected area, doses from 5 to 50 mg are used.
Used locally in ophthalmology 3 times a day, the course of treatment is no more than 14 days; in dermatology - 1-3 times/day.

Side effect

From the endocrine system: Itsenko-Cushing syndrome, weight gain. Hyperglycemia up to the development of steroid diabetes, depletion (up to atrophy) of the function of the adrenal cortex.
From the digestive system: increased acidity of gastric juice, ulcerogenic effect on the gastrointestinal tract.
Metabolism: increased excretion of potassium, sodium retention in the body with the formation of edema, negative nitrogen balance.
From the cardiovascular system: arterial hypertension.
From the blood coagulation system: increased blood clotting.
From the musculoskeletal system: osteoporosis, aseptic bone necrosis.
From the organ of vision: steroid cataract, provoking latent glaucoma.
From the side of the central nervous system: mental disorders.
Effects due to immunosuppressive effects: decreased resistance to infections, delayed wound healing.
When used externally: possible appearance of steroid acne, purpura, telangiectasia, as well as burning, itching, irritation, dry skin; with prolonged use and/or when applied to large surfaces of the skin, a resorptive effect may develop.
When applied topically: a slight burning sensation is possible.

Contraindications

Peptic ulcer stomach and duodenum, osteoporosis, Itsenko-Cushing syndrome, tendency to thromboembolism, renal failure, severe arterial hypertension, systemic mycoses, viral infections, vaccination period, active form of tuberculosis, glaucoma, productive symptoms in mental illness. Hypersensitivity to prednisolone.
Infiltration injection into lesions of the skin and tissues during chicken pox, specific infections, mycoses, with a local reaction to vaccination.
In ophthalmology - viral and bacterial diseases eye, primary glaucoma, corneal diseases with epithelial damage. In dermatology - bacterial, viral, fungal infections skin, tuberculosis, syphilis, skin tumors.

Pregnancy and lactation

During pregnancy (especially in the first trimester) it is used only for health reasons. If it is necessary to use it during lactation, the expected benefits of treatment for the mother and the risk for the child should be carefully weighed.

Special instructions

Not intended for intravenous administration. During the day, it is recommended to use it taking into account the circadian rhythm of endogenous secretion of GCS in the interval from 6 to 8 am.
Use with caution in patients with a history of psychosis; nonspecific infections subject to simultaneous chemotherapy or antibiotic therapy. For diabetes mellitus, use is possible only with absolute readings or to prevent suspected insulin resistance. For latent forms of tuberculosis, prednisolone can only be used in combination with anti-tuberculosis drugs.
During treatment (especially long-term), observation by an ophthalmologist, monitoring of blood pressure and water-electrolyte balance, as well as peripheral blood patterns and blood sugar levels are necessary; In order to reduce side effects, you can prescribe anabolic steroids, antibiotics, and also increase the intake of potassium in the body (diet, potassium supplements). It is recommended to clarify the need for ACTH administration after a course of treatment with prednisolone (after performing a skin test!). In Addison's disease, concomitant use with barbiturates should be avoided.
After cessation of treatment, withdrawal syndrome, adrenal insufficiency, and exacerbation of the disease for which prednisolone was prescribed may occur.
It should not be used externally for more than 14 days. If used for acne vulgaris or rosacea, an exacerbation of the disease is possible.

Prednisolone in the form of tablets, solution for injection, dry substance for injection, eye drops, ointments is included in the List of Vital and Essential Drugs.

Drug interactions

With the simultaneous use of prednisolone with anticoagulants, the anticoagulant effect of the latter may be enhanced; with salicylates - the likelihood of bleeding increases; with diuretics - possible aggravation of electrolyte metabolism disorders; with antidiabetic drugs - the rate of decrease in blood sugar decreases; with cardiac glycosides - the risk of developing glycoside intoxication increases; with rifampicin - weakening of the therapeutic effect of rifampicin.