Prednisolone tablets 5mg, No. 100

• Rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, bronchial asthma, status asthma, acute and chronic allergic diseases, anaphylactic shock, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome;

• hepatitis, hepatic coma, hypoglycemic conditions, lipoid nephrosis;

• agranulocytosis, various forms of leukemia, lymphogranulomatosis, thrombocytopenic purpura, hemolytic anemia;

• chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, SLE, erythroderma, alopecia.

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 may be 15-100 mg / day, the maintenance dose is 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 doses, the maintenance dose is 300-600 ?g / kg / day.

Tablets 1 tab.

prednisolone 5 mg

Hypersensitivity to prednisone.

pharmachologic effect

GKS. Suppresses the function of leukocytes and tissue macrophages. Limits the migration of leukocytes to the area of ??inflammation. Violates the ability of macrophages to phagocytosis, as well as the formation of interleukin-1. Promotes the stabilization of 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 A2, 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; inhibits the formation of antibodies.

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

When applied directly to the 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 storage of glycogen, stimulating the activity of glycogen synthetase and the synthesis of glucose from the products of protein metabolism. An increase in blood glucose activates the release of insulin.

Prednisolone inhibits the uptake of glucose by fat cells, which leads to the activation of lipolysis. However, due to the increase in insulin secretion, lipogenesis is stimulated, which contributes to the accumulation of fat.

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's syndrome are the main factors limiting long-term GCS therapy. As a result of the catabolic effect, it is possible to suppress growth in children.

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

With systemic use, the therapeutic activity of prednisolone is due to its anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

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

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. Cmax in plasma is noted after 90 minutes. In plasma, most of prednisolone binds to transcortin (cortisol-binding globulin). It is metabolized mainly in the liver.

T1 / 2 is about 200 min. It is excreted by the kidneys unchanged - 20%.

Side effect

From the endocrine system: menstrual irregularities, suppression of adrenal function, Itsenko-Cushing's syndrome, suppression of the function of the pituitary-adrenal system, decreased carbohydrate tolerance, steroid diabetes or manifestation of latent diabetes mellitus, growth retardation in children, delayed sexual development in children.

From the digestive system: nausea, vomiting, steroid stomach and duodenal ulcer, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases, an increase in the activity of hepatic transaminases and alkaline phosphatase.

From the side of metabolism: negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, increased body weight, increased sweating.

From the side of the cardiovascular system: loss of potassium, hypokalemic alkalosis, arrhythmia, bradycardia (up to cardiac arrest); steroid myopathy, heart failure (development or worsening of symptoms), ECG changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute myocardial infarction - the spread of the focus of necrosis, slowing down the formation of scar tissue, which can lead to rupture of the heart muscle.

On the part of the musculoskeletal system: growth retardation and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (very rarely - pathological fractures, aseptic necrosis of the humerus and femur head), muscle tendon rupture, muscle weakness, steroid myopathy, reduction muscle mass (atrophy).

From the nervous system: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, cerebellar pseudotumor, seizures.

From the side of the organ of vision: posterior subcapsular cataract, increased intraocular pressure (with possible damage to the optic nerve), trophic changes in the cornea, exophthalmos, a tendency to develop a secondary infection (bacterial, fungal, viral).

On the part of the skin and subcutaneous fat: petechiae, ecchymosis, thinning and fragility of the skin, hyper- or hypopigmentation, acne, striae, a tendency to develop pyoderma and candidiasis.

Reactions due to immunosuppressive action: slowing down the regeneration processes, reducing resistance to infections.

With parenteral administration: in isolated cases, anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of the skin and subcutaneous tissue, exacerbation after intrasynovial use, Charcot-type arthropathy, sterile abscesses, when introduced into the foci on the head - blindness.

Application during pregnancy and lactation

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

Application for violations of liver function

Use with caution in severe chronic liver failure.

Application for impaired renal function

Use with caution in severe chronic renal failure.

Use in elderly patients

Use with caution in elderly patients in order to avoid the risk of exacerbation of chronic diseases.

special instructions

Use with caution in parasitic and infectious diseases of a viral, fungal or bacterial nature (currently or recently transferred, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chickenpox, measles, amebiasis, strongyloidosis (established or suspect), systemic mycosis; active and latent tuberculosis. Application for severe infectious diseases is permissible only against the background of specific therapy.

Use with caution within 8 weeks before and 2 weeks after vaccination, with lymphadenitis after BCG vaccination, with immunodeficiency conditions (including AIDS or HIV infection).

Use with caution in diseases of the gastrointestinal tract: gastric ulcer and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess formation, diverticulitis.

Use with caution in diseases of the cardiovascular system, incl. after a recent myocardial infarction (in patients with acute and subacute myocardial infarction, it is possible to spread the focus of necrosis, slow down the formation of scar tissue and, as a result, rupture of the heart muscle), with decompensated chronic heart failure, arterial hypertension, hyperlipidemia), with endocrine diseases - diabetes mellitus ( including impaired carbohydrate tolerance), thyrotoxicosis, hypothyroidism, Itsenko-Cushing's disease, with severe chronic renal and / or hepatic failure, nephrourolithiasis, with hypoalbuminemia and conditions predisposing to its occurrence, with systemic osteoporosis, psychosis, myasthenia gravis , obesity (III-IV degree), with poliomyelitis (except for the form of bulbar encephalitis),open and closed angle glaucoma.

If necessary, intra-articular administration should be used with caution in patients with a general serious condition, ineffectiveness (or short duration) of the action of 2 previous injections (taking into account the individual properties of the GCS used).

During treatment (especially long-term), it is necessary to observe an ophthalmologist, control blood pressure and water-electrolyte balance, as well as pictures of peripheral blood, blood glucose; in order to reduce side effects, you can prescribe anabolic steroids, antibiotics, and also increase the intake of potassium into the body (diet, potassium preparations). It is recommended to clarify the need for ACTH administration after a course of treatment with prednisolone (after a skin test!).

In Addison's disease, concomitant use with barbiturates should be avoided.

After discontinuation of treatment, withdrawal syndrome, adrenal insufficiency, as well as exacerbation of the disease, for which prednisolone was prescribed, may occur.

With intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously carry out antibiotic therapy.

In children during the period of growth, GCS should be used only for absolute indications and under the close supervision of a physician.

Drug interactions

With simultaneous use with salicylates, an increase in the likelihood of bleeding is possible.

With simultaneous use with diuretics, it is possible to aggravate electrolyte metabolism disorders.

With simultaneous use with hypoglycemic drugs, the rate of decrease in blood glucose levels decreases.

With simultaneous use with cardiac glycosides, the risk of developing glycosidic intoxication increases.

With simultaneous use with rifampicin, the therapeutic effect of rifampicin may be weakened.

With the simultaneous use of antihypertensive drugs, their effectiveness may decrease.

With the simultaneous use of coumarin derivatives, the anticoagulant effect may be weakened.

With the simultaneous use of rifampicin, phenytoin, barbiturates, the effect of prednisolone may be weakened.

With the simultaneous use of hormonal contraceptives - an increase in the action of prednisone.

With the simultaneous use of acetylsalicylic acid, it is possible to reduce the content of salicylates in the blood.

With the simultaneous use of praziquantel, it is possible to reduce its concentration in the blood.

The appearance of hirsutism and acne is facilitated by the simultaneous use of other GCS, androgens, estrogens, oral contraceptives and steroid anabolic steroids. The risk of developing cataracts increases when antipsychotics, carbutamide and azathioprine are used against the background of GCS.

Simultaneous administration with m-anticholinergics (including antihistamines, tricyclic antidepressants), nitrates contributes to the development of an increase in intraocular pressure.