Prednisolonum

General characteristics. Structure:

Active agent: Prednisolonum of 5 mg; 1 mg.

Pharmacological properties:

GKS. Suppresses functions of leukocytes and fabric macrophages. Limits migration of leukocytes to the area of an inflammation. Breaks ability of macrophages to phagocytosis, and also to education interleykina-1. Promotes stabilization of lizosomalny membranes, reducing thereby concentration of proteolytic enzymes in the field of an inflammation. Reduces the permeability of capillaries caused by release of a histamine. Suppresses activity of fibroblasts and formation of collagen.
Inhibits activity of a phospholipase of A2 that leads to suppression of synthesis of prostaglandins and leukotrienes. Suppresses release of TsOG (mainly TsOG-2) that also promotes reduction of production of prostaglandins.
Reduces number of the circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophiles owing to their movement from a vascular bed to an adenoid tissue; suppresses antibody formation.
Prednisolonum suppresses release by a hypophysis of AKTG and β-lipotropin, but does not reduce the level of the circulating β-endorphine.......... Oppresses secretion of TTG and FSG.
At direct application renders vasopressor effect on vessels.
Prednisolonum possesses the expressed dozozavisimy action on metabolism of carbohydrates, proteins and fats. Stimulates a gluconeogenesis, promotes capture of amino acids a liver and kidneys and increases activity of enzymes of a gluconeogenesis. In a liver Prednisolonum strengthens deposition of a glycogen, stimulating activity of a glikogensintetaza and synthesis of glucose from products of protein metabolism. Increase in content of glucose in blood activates release of insulin.
Prednisolonum suppresses glucose capture by lipoblasts that leads to activation of a lipolysis. However owing to increase in secretion of insulin there is a stimulation of a lipogenesis that promotes fat accumulation.
Has catabolic effect in adenoid and connecting tissue, muscles, fatty tissue, skin, a bone tissue. To a lesser extent than the hydrocortisone, influences processes of water and electrolytic exchange: promotes removal of potassium ions and calcium, a delay in an organism of ions of sodium and water. Osteoporosis and an Icenco-Cushing syndrome are the main factors limiting long therapy of GKS. As a result of catabolic action suppression of growth at children is possible.
In high doses Prednisolonum can increase excitability of tissues of brain and promotes reduction of the threshold of convulsive readiness. Stimulates excess products of hydrochloric acid and pepsin in a stomach that leads to development of a round ulcer.
At system use therapeutic activity of Prednisolonum is caused by antiinflammatory, antiallergic, immunodepressive and anti-proliferative effect.
At external and topical administration therapeutic activity of Prednisolonum is caused antiinflammatory, antiallergic and anti-exudative (thanks to vasopressor effect) by action.
In comparison with a hydrocortisone antiinflammatory activity of Prednisolonum is 4 times more, mineralokortikoidny activity is 0.6 times less.

Pharmacokinetics. At intake it is well soaked up from a GIT. Cmax in plasma is noted in 90 min. In plasma the most part of Prednisolonum contacts transcortinum (kortizolsvyazyvayushchy globulin). It is metabolized preferential in a liver.
T1/2 makes about 200 min. It is removed by kidneys in not changed look - 20%.

Indications to use:

For intake and parenteral use: rheumatism; pseudorheumatism, dermatomyositis, nodular periarteritis, scleroderma, Bekhterev's disease, bronchial asthma, asthmatic status, acute and chronic allergic diseases, acute anaphylaxis, Addison's disease, acute insufficiency of bark of adrenal glands, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic states, lipoid nephrosis; agranulocytosis, various forms of leukemia, lymphogranulomatosis, Werlhof's disease, hemolitic anemia; hysterical chorea; pemphigus, eczema, itch, exfoliative dermatitis, psoriasis, prurigo, seborrheal dermatitis, hard currency, erythrosis, alopecia.

For intra joint introduction: chronic polyarthritis, posttraumatic arthritis, osteoarthritis of large joints, rheumatic damages of separate joints, arthroses.

For infiltration introduction to fabrics: epicondylitis, tendovaginitis, bursitis, humeroscapular periarthritis, keloids, ischialgia, palmar fibromatosis, damages of joints and various fabrics, rheumatic and similar to them.

For use in ophthalmology: 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 inflammation of an eyeglobe; after injuries and operations at long irritation of eyeglobes.

Route of administration and doses:

At intake for the replacing therapy at adults the initial dose makes 20-30 mg/days, a maintenance dose - 5-10 mg/days. If necessary the initial dose can make 15-100 mg/days, supporting - 5-15 mg/days. The daily dose should be reduced gradually. For children the initial dose makes 1-2 mg/kg/days in 4-6 receptions, supporting - 300-600 mkg/kg/days.

At in oil or in introduction the dose, frequency rate and duration of use are defined individually.

At intra joint introduction to large joints apply a dose of 25-50 mg, to joints of average size - 10-25 mg, to small joints - 5-10 mg. Depending on disease severity and the size of area of defeat apply doses from 5 to 50 mg to infiltration introduction to fabrics.

Locally in ophthalmology apply 3 times/days, a course of treatment - no more than 14 days; in dermatology - 1-3 times/days.

Features of use:

With care to apply at parasitic and infectious diseases of the virus, fungal or bacterial nature (now or recently postponed, including recent contact with the patient) - the herpes simplex surrounding herpes (a viremichesky phase), the chicken pox, measles, the amebiasis, a strongyloidosis (established or suspected), system mycosis; active and latent tuberculosis. Use at serious infectious diseases is admissible only against the background of specific therapy.

With care to apply within 8 weeks to and 2 weeks after vaccination, at lymphadenitis after BTsZh inoculation, at immunodeficiency (including AIDS or HIV contamination).

With care to apply at gastrointestinal diseases: a peptic ulcer of a stomach and a duodenum, an esophagitis, gastritis, an acute or latent round ulcer, recently created intestines anastomosis, nonspecific ulcer colitis with threat of perforation or abscessing, a diverticulitis.

With care to apply at diseases of cardiovascular system, including after recently postponed myocardial infarction (at patients with an acute and subacute myocardial infarction distribution of the center of a necrosis, delay of formation of cicatricial fabric and thereof a rupture of a cardiac muscle is possible), at dekompensirovanny chronic heart failure, arterial hypertension, a lipidemia), at endocrine diseases - a diabetes mellitus (including disturbance of tolerance to carbohydrates), a thyrotoxicosis, a hypothyroidism, Itsenko-Cushing's disease, at a heavy chronic renal and/or liver failure, a nefrourolitiaza, at the hypoalbuminemia and states contributing to its emergence at system osteoporosis, a myasthenia, acute psychosis, obesity (the III-IV degree), at poliomyelitis (except for a form of bulbar encephalitis), open and closed-angle glaucoma.

In need of intra joint introduction with care to apply at patients with the general serious condition, inefficiencies (or short durations) actions of 2 previous introductions (taking into account individual properties of the applied GKS).

During treatment (especially long) observation of the oculist, control of the ABP 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 appoint anabolic steroids, antibiotics, and also to increase intake of potassium in an organism (a diet, potassium drugs). It is recommended to specify need of introduction of AKTG after a course of treatment Prednisolonum (after conducting skin test!).

At Addison's disease it is necessary to avoid simultaneous use with barbiturates.

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.

At intercurrent infections, septic states and tuberculosis, simultaneous performing antibiotic treatment is necessary.

At children in a growth period of GKS it is necessary to apply only according to absolute indications and under careful control of the doctor.

Outwardly it is not necessary to apply more than 14 days. In case of use at ordinary or pink eels the exacerbation of a disease is possible.

Side effects:

From endocrine system: disturbances of a menstrual cycle, oppression of function of adrenal glands, an Icenco-Cushing syndrome, suppression of function of pituitary and adrenal system, decrease in tolerance to carbohydrates, steroid diabetes or manifestation of a latent diabetes mellitus, delay of growth at children, a delay of sexual development at children.

From the alimentary system: nausea, vomiting, steroid stomach ulcer and duodenum, pancreatitis, esophagitis, bleedings and perforation of a GIT, increase or loss of appetite, meteorism, hiccups. In rare instances - increase in activity of hepatic transaminases and ShchF.

From a metabolism: negative nitrogenous balance because of a catabolism of proteins, the sweating increased removal of calcium from an organism, a hypocalcemia, increase in body weight, increased.

From cardiovascular system: potassium loss, a gipokaliyemichesky alkalosis, arrhythmia, bradycardia (up to a cardiac standstill); a steroid myopathy, heart failure (development or strengthening of symptoms), changes on the ECG characteristic of a hypopotassemia, increase in the ABP, hypercoagulation, fibrinferments. Patients with an acute myocardial infarction have a distribution of the center of a necrosis, delay of formation of cicatricial fabric that can lead to a rupture of a cardiac muscle.

From a musculoskeletal system: delay of growth and processes of ossification at children (premature closing of epiphyseal regions of growth), osteoporosis (it is very rare - pathological changes, an aseptic necrosis of a head humeral and a femur), a rupture of sinews of muscles, muscular weakness, a steroid myopathy, reduction of muscle bulk (atrophy).

From TsNS: headache, increase in intracranial pressure, delirium, disorientation, euphoria, hallucinations, maniac-depressive psychosis, depression, nervousness or concern, sleeplessness, dizziness, вертиго, cerebellum pseudoneoplasm, convulsive attacks.

From an organ of sight: a back subkapsulyarny cataract, increase in intraocular pressure (with possible injury of an optic nerve), trophic changes of a cornea, an exophthalmos, tendency to development of consecutive infection (bacterial, fungal, virus).

Dermatological reactions: petechias, ecchymomas, thinning and fragility of skin, hyper - or hypopigmentation, eels, striya, tendency to development of a pyoderma and candidiases.

The reactions caused by an immunodepressive effect: delay of processes of regeneration, decrease in resistance to infections.

At parenteral administration: in isolated cases anaphylactic and allergic reactions, hyper - or hypopigmentation, an atrophy of skin and hypodermic cellulose, an aggravation after intrasinovialny use, an arthropathy like Sharko, sterile abscesses, at introduction to the centers on the head - a blindness.

Interaction with other medicines:

At simultaneous use with salicylates increase in probability of developing of bleedings is possible.

At simultaneous use with diuretics aggravation of disturbances of electrolytic exchange is possible.

At simultaneous use with hypoglycemic drugs the speed of decrease in level of glucose in blood decreases.

At simultaneous use with cardiac glycosides the risk of development of glikozidny intoxication amplifies.

At simultaneous use with rifampicin weakening of therapeutic effect of rifampicin is possible.

At simultaneous use of antihypertensives decrease in their efficiency is possible.

At simultaneous use of derivatives of coumarin easing of anticoagulating effect is possible.

At simultaneous use of rifampicin, Phenytoinum, barbiturates weakening of effect of Prednisolonum is possible.

At simultaneous use of hormonal contraceptives - strengthening of effect of Prednisolonum.

At simultaneous use of acetylsalicylic acid decrease in content of salicylates in blood is possible.

At simultaneous use of a prazikvantel reduction of its concentration in blood is possible.

Emergence of a hirsutism and eels is promoted by simultaneous use of other GKS, androgens, estrogen, oral contraceptives and steroid anabolic steroids. The risk of development of a cataract increases at use against the background of GKS of antipsychotic means, Carbutamidum and Azathioprinum.

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

Contraindications:

For short-term use according to vital indications - hypersensitivity to Prednisolonum.
For intra joint introduction and introduction directly to the defeat center: the previous arthroplasty, pathological bleeding (endogenous or caused by use of anticoagulants), an intra joint fracture of a bone, infectious (septic) inflammatory process in a joint and periartikulyarny infections (including in the anamnesis), and also the general infectious disease, the osteoporosis expressed circumarticular, lack of signs of an inflammation in a joint (Sukhoi a joint, for example at an osteoarthrosis without synovitis), the expressed bone destruction and deformation of a joint (sharp narrowing of a joint crack, an anchylosis), instability of a joint as an arthritis outcome, an aseptic necrosis of the epiphysis of bones creating a joint.
For external use: bacterial, viral, fungus skin diseases, a tuberculosis cutis, skin displays of syphilis, skin tumor, the postvaccinal period, disturbance of integrity of integuments (an ulcer, a wound), children's age (up to 2 years, at an itch in the field of an anus - up to 12 years), a rozatsea, vulgar eels, perioral dermatitis.

For use in ophthalmology: bacterial, viral, fungus diseases of eyes, tubercular damage of eyes, trachoma, disturbance of integrity of an eye epithelium.

Use at pregnancy and feeding by a breast
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.

Use at abnormal liver functions
With care to apply at a heavy chronic liver failure.

Use at renal failures
With care to apply at a heavy chronic renal failure.

Use for children
At children in a growth period of GKS it is necessary to apply only according to absolute indications and under careful control of the doctor.
Contraindication for external use: children's age (up to 2 years, at an itch in the field of an anus - up to 12 years).

Overdose:

There are no data.

Storage conditions:

List B. To store in the dry, protected from light place, at a temperature not above 25 °C.
To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets of 5 mg; 1 mg.: 30, 60, 100 or 120 pieces.