Prednisolonum

General characteristics. Structure:

Active ingredient: 5 mg of Prednisolonum in 1 tablet.

Drug renders antiinflammatory, antiallergic, immunodepressive, antishock effect.

Pharmacological properties:

Pharmacodynamics. Drug is a synthetic analog of the hormones emitted by bark of adrenal glands. Raises products of the lipokortin inhibiting A2 phospholipase and reduces synthesis of products of metabolism of arachidonic acid – cyclic endoperoxides, prostaglandins, thromboxane. Stabilizes membranes of lysosomes, inhibits hyaluronidase synthesis, reduces products of lymphokines and slows down migration of macrophages.

The antiallergic effect is caused by reduction of number of basophiles, direct inhibition of secretion and synthesis of mediators of an immediate allergy. Causes a lymphopenia and involution of an adenoid tissue, than immunosuppression is caused. Has antishock properties, strengthens action of catecholamines and recovers sensitivity of receptors to catecholamines. Reduces amount of protein in plasma, strengthens a protein catabolism in muscular tissue, increases its synthesis in a liver.

Promotes formation of higher fatty acids and triglycerides, fat redistribution. Increases a resorption of carbohydrates from digestive tract, activity of glyukozo-6-phosphatase and a fosfoyenolpiruvatkinaza that leads to mobilization of glucose in a blood stream and to strengthening of a gluconeogenesis. Detains sodium and water and promotes removal of potassium due to mineralokortikoidny action. Reduces absorption of calcium in intestines, increases its washing away from bones and excretion kidneys. Suppresses activity of fibroblasts and formation of collagen.

Pharmacokinetics. At intake it is well soaked up from digestive tract. The maximum concentration in a blood plasma is reached in 60-90 minutes after reception. In plasma of 90% of Prednisolonum is in the connected look (with transcortinum and albumine). Gets through a placental barrier and in small amounts it is found in breast milk. It Biotransformirutsya preferential in a liver by oxidation; the oxidized forms glyukuronizirutsya or sulphated. Biotransformation occurs also in kidneys, a small bowel, bronchial tubes. The elimination half-life makes 2-4 h. It is removed by kidneys – 20% in not changed look.

Indications to use:

Acute rheumatic fever, pseudorheumatism, system lupus erythematosus, dermatomyositis, system vasculites, system scleroderma, Bekhterev's disease, hysterical chorea; Addison's disease, acute insufficiency of bark of adrenal glands, adrenogenital syndrome; nonspecific ulcer colitis, disease Krone, hepatitis, hepatic coma; glomerulonephritis, lipoid nephrosis; agranulocytosis, various forms of a leukosis, lymphogranulomatosis, Werlhof's disease, hemolitic anemia; prevention of reaction of graft rejection; bronchial asthma; acute and chronic allergic diseases, pemphigus, eczema, itch, exfoliative dermatitis, psoriasis, prurigo, eczema, seborrheal dermatitis, erythrosis, psoriasis, alopecia; allergic, chronic and atypical conjunctivitis and blepharitis; a cornea inflammation at the unimpaired mucous; acute and chronic inflammation of a front piece of a choroid, sclera and episclera; sympathetic ophthalmia.

Route of administration and doses:

Tablets of Prednisolonum are appointed inside. The dose is selected individually. At appointment it is necessary to consider a day-night secretory rhythm of glucocorticosteroids: appoint big in the morning (or all) a part of a dose. Treatment is stopped slowly, gradually reducing a dose.

At intake as replacement therapy the initial dose for adults makes 20-30 mg/days (4-6 tablets), a maintenance dose – 5-10 mg/days (1-2 tablets). If necessary the initial dose can make 15-100 mg/days (3-20 tablets), supporting – 5-15 mg/days (1-3 tablets). The daily dose should be reduced gradually. For children the initial dose makes 1-2 mg/kg/days for 4-6 receptions, supporting – 0,3-0,6 mg/kg/days.

The highest daily dose for adults makes 0,1 g.

Features of use:

During treatment (especially long) observation of the oculist, control of arterial pressure and water and electrolytic balance, and also a picture of peripheral blood, glucose in blood is necessary. For the purpose of reduction of side effects it is possible to increase intake of potassium in an organism (a diet, potassium drugs).

With care apply at patients with the instruction on psychoses in the anamnesis; at nonspecific infections on condition of a simultaneous himio-or an antibioticotherapia.

At a diabetes mellitus use is possible only at absolute indications or for the prevention of estimated resistance to insulin. At latent forms of tuberculosis Prednisolonum can be applied only in combination with antituberculous remedies. At Addison's disease it is necessary to avoid simultaneous use with barbiturates.

Treatment by Prednisolonum has to be carried out in the presence of accurate indications and under careful medical control.

After the termination of treatment emergence of a withdrawal, adrenal insufficiency, and also an exacerbation of a disease concerning which Prednisolonum was appointed is possible.

Pregnancy and lactation: at pregnancy (especially in the I trimester) apply only according to vital indications. In need of use in the period of a lactation it is necessary to weigh carefully expected advantage of treatment for mother and risk for the child.

Drug does not influence ability to manage vehicles and the machine equipment.

Side effects:

Frequency of development and expressiveness of side effects depend on duration of use and size of the used drug dose.

From endocrine system: Itsenko's syndrome - Cushing, increase in body weight, a hyperglycemia up to development of steroid diabetes, exhaustion (up to an atrophy) functions of bark of adrenal glands, a delay of sexual development at children.

From the alimentary system: nausea, vomiting, increase in acidity of a gastric juice, ulcerogenic action, increase or loss of appetite, meteorism, hiccups.

From a metabolism: increase in removal of potassium, a sodium delay in an organism with formation of hypostases, negative nitrogenous balance.

From cardiovascular system: arterial hypertension, arrhythmias, bradycardia.

From coagulant system of blood: increase in coagulability of blood.

From a musculoskeletal system: a "steroid" myopathy, decrease in muscle bulk, osteoporosis, an aseptic necrosis of bones, delay of growth and processes of ossification at children.

From integuments and mucous membranes: the slowed-down healing of wounds, petechias, ecchymomas, thinning of skin, hyper - or hypopigmentation, eels, striya, tendency to development of a pyoderma and candidiases.

From an organ of sight: steroid cataract, provoking of latent glaucoma.

From a nervous system: mental disorders.

Allergic reactions: generalized (skin rash, skin itch, acute anaphylaxis), local allergic reactions.

Others: decrease in resilience to infections, a syndrome of "cancellation".

Interaction with other medicines:

Prednisolonum increases toxicity of cardiac glycosides (because of the arising hypopotassemia the risk of development of arrhythmias increases). Accelerates removal of acetylsalicylic acid, reduces its concentration in blood (at Prednisolonum cancellation concentration of salicylates in blood increases and the risk of development of by-effects increases).

At simultaneous use with live antiviral vaccines and against the background of other types of immunization increases risk of activation of viruses and development of infections.

Increases metabolism of an isoniazid, meksiletin that leads to decrease in their plasma concentration. Increases risk of development of hepatotoxic reactions of paracetamol (owing to induction of "hepatic" enzymes and formation of a toxic metabolite of paracetamol). Increases (at long therapy) the content of folic acid.

The hypopotassemia arising at Prednisolonum reception can increase expressiveness and duration of muscular blockade against the background of use of muscle relaxants. In high doses reduces effect of Somatotropinum.

Reduces effect of hypoglycemic drugs, strengthens anticoagulating action of derivatives of coumarin. Weakens influence of vitamin D on absorption of calcium in an intestines gleam. Reduces concentration of a prazikvantel in blood.

Antacids reduce Prednisolonum absorption. Cyclosporine (metabolism oppresses) and кетоконазол (reduces clearance) increase its toxicity.

Thiazide diuretics, karboangidraza inhibitors, other glucocorticosteroids and Amphotericinum In increase risk of development of a hypopotassemia, the Na+-containing drugs – hypostases and increase in arterial pressure.

Non-steroidal anti-inflammatory drugs and ethanol increase danger of development of an ulceration of a mucous membrane of digestive tract and bleeding. In Prednisolonum combination with non-steroidal anti-inflammatory drugs summation of antiinflammatory effect is observed. Indometacin, forcing out Prednisolonum from communication with albumine, increases risk of development of its side effects.

Amphotericinum In and inhibitors of a karboangidraza increase risk of development of osteoporosis. Therapeutic effect of Prednisolonum decreases under the influence of Phenytoinum, barbiturates, ephedrine, theophylline, rifampicin and other inductors of "hepatic" microsomal enzymes (increase in speed of metabolism). Mitotanum and other inhibitors of function of bark of adrenal glands can cause need of increase in a dose of Prednisolonum.

The clearance of Prednisolonum increases against the background of reception of hormones of a thyroid gland. Immunodepressants increase risk of development of infections. Estrogen (including oral estrogensoderzhashchy contraceptives) reduces clearance of Prednisolonum, extends an elimination half-life and therapeutic and toxic effects.

Emergence of a hirsutism and eels at reception of Prednisolonum is promoted by simultaneous use of other steroid hormonal drugs – androgens, estrogen, anabolic steroids, oral contraceptives.

Tricyclic antidepressants can increase expressiveness of the depression caused by Prednisolonum reception. The risk of development of a cataract increases at use of Prednisolonum against the background of neuroleptics, Carbutamidum and Azathioprinum.

Co-administration with M-holinoblokatorami (including antihistaminic drugs, tricyclic antidepressants), nitrates promotes development of increase in intraocular pressure.

Contraindications:

Hypersensitivity, stomach ulcer or a 12-perstny gut in an aggravation phase, a dekompensirovanny diabetes mellitus, heavy arterial hypertension, osteoporosis, Itsenko-Cushing's disease, the vaccination period, an active form of tuberculosis, glaucoma, system mycoses, an acute viral infection, productive symptomatology at mental diseases, viral and bacterial diseases of eyes, primary glaucoma, cornea diseases with damage of an epithelium, bacterial, fungal, virus damages of skin, tuberculosis, syphilis, skin tumors.

Issue conditions:

According to the recipe

Packaging:

Tablets of 5 mg in a blister strip packaging No. 10x5.