Prednizolon-Darnitsa, the tab. on 0.005 g No. 40

General characteristics. Structure:

Active ingredient: prednisolone;

1 tablet contains Prednisolonum 5 mg;

excipients: lactose monohydrate, potato starch, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Prednisolonum – the dehydrogenated hydrocortisone analog. Renders the antiinflammatory, antiallergic, desensibilizing, antishock and immunodepressive effect.

At Prednisolonum use effects of drug are implemented through stabilization of cellular membranes, braking of accumulation of macrophages, reduction of migration of leukocytes, decrease in permeability of capillaries that interferes with formation of hypostases. Prednisolonum oppresses phagocytosis, influences metabolism of arachidonic acid, and also synthesis and release of mediators of an inflammation. Immunosuppressive effect of Prednisolonum is caused by oppression of activity of T - and V-lymphocytes, reduction of maintenance of a complement in blood, and also oppression of products and effects interleykina-2. Shows katabolitichesky action, increases glucose level in blood. Shows some mineralkortikoidny activity, increases a reabsorption in renal tubules of Na + and waters, a conclusion from an organism of K+ and Sa + raises, in particular at increase in their level in a blood plasma. Prednisolonum oppresses synthesis and secretion by a hypophysis of adrenocorticotropic hormones and for the second time – glucocorticosteroids adrenal glands.

Pharmacokinetics. It is quickly soaked up from digestive tract. Has high bioavailability. Time of achievement of the maximum concentration in a blood plasma – 1–1,5 hours. The most part of drug (90%) communicates kortizolsvyazyvayushchy globulin – transcortinum and albumine. It is metabolized in a liver, kidneys, a small intestine, bronchial tubes. The oxidized forms of Prednisolonum glyukuronizirutsya or sulphated. An elimination half-life (T1/2) – 2-4 hours. It is removed by kidneys generally in the form of metabolites, to 20% in not changed look.

Pharmaceutical characteristics.

Main physical and chemical properties: tablets of white color, a ploskotsilindrichesky form with a facet.

Indications to use:

Rheumatic fever, rheumatic carditis, hysterical chorea.

General diseases of connecting fabric (system lupus erythematosus, scleroderma, nodular periarteritis, dermatomyositis).

Multiple sclerosis.

Acute and chronic inflammatory diseases of joints (a pseudorheumatism, the juvenile arthritis ankylosing a spondylarthritis, gouty and psoriasis arthritises, polyarthritis, a humeroscapular periarthritis, an osteoarthritis (including posttraumatic), Steel's syndrome at adults, the bursitis, nonspecific tendosinovit, a synovitis, an epicondylitis);

Bronchial asthma, asthmatic status.

Intersticial diseases of lungs (acute alveolitis, pneumosclerosis, sarcoidosis      of the II-III degree); lung cancer (in a combination with cytostatics), a berylliosis, aspiration pneumonia (in a combination to specific therapy), eosinophilic pneumonia of Leffler, tuberculosis (a pulmonary tuberculosis, tubercular meningitis) – in a combination to specific therapy.

Primary and secondary insufficiency of adrenal glands (including states after removal of adrenal glands), an inborn adrenal struma, an adrenogenital syndrome, a subacute thyroiditis.

Acute and chronic allergic diseases (medicinal and food allergies, a serum disease, pollinosis, atopic dermatitis, contact dermatitis with involvement of a big body surface, urticaria, allergic rhinitis, a Quincke's edema, Stephens-Johnson's syndrome, a toksikodermiya).

Hepatitis.

Hypoglycemic states.

Autoimmune diseases (including acute glomerulonephritis).

Nephrotic syndrome.

Inflammatory gastrointestinal diseases (nonspecific ulcer colitis, disease Krone, local enteritis).

Diseases of blood and bodies of a hemopoiesis (an agranulocytosis, a panmyelopathia, a multiple myeloma, an acute lympho-and myeloid leukosis, a lymphogranulomatosis, a Werlhof's disease, secondary thrombocytopenia at adults, autoimmune hemolitic anemia, an eritroblastopeniya, inborn erythroidal hypoplastic anemia).

Autoimmune and other skin diseases (eczema, seborrheal dermatitis, psoriasis, Lyell's disease, violent herpetiform dermatitis, pemphigus, exfoliative dermatitis).

Wet brain is post-operational, post-radiation, posttraumatic, brain tumors (to apply after parenteral glucocorticosteroids).

Diseases of eyes, including allergic and autoimmune (sympathetic ophthalmia, allergic forms of conjunctivitis, allergic helcoma, not purulent keratitis, iridocyclitis, iritis, heavy slow lobbies and back uveites, choroiditis, neuritis of an optic nerve).

Prevention of reactions of graft rejection.

Hypercalcemia against the background of oncological diseases.

For prevention and elimination of nausea, vomiting at cytostatic therapy.

Route of administration and doses:

Dosing is established individually. At appointment it is necessary to consider a circadian rhythm of secretion of glucocorticoids: it is necessary to accept the most part of a dose (2/3) or all dose in the morning, about 8 h morning, and 1/3 – in the evening.

Adult.

At acute states and as replacement therapy drug appoint in a dose 20-30 mg a day with gradual transition to the supporting daily dose to 5-10 mg. If necessary the initial dose can make 15-100 mg/days, and a maintenance dose – 5-15 mg/days.

To children.

The initial dose of drug for children makes 1-2 mg/kg/days and the maintenance dose – 300-600 mkg/kg/days is distributed on 4-6 receptions, and.

Drug is used inside, without chewing and washing down with a small amount of liquid. Treatment is stopped slowly, gradually reducing a dose.

Features of use:

Use during pregnancy or feeding by a breast.

Controlled researches on pregnant women were not conducted. During pregnancy (especially in Ι a trimester) use is possible if the advantage for mother exceeds risk for a fruit. At use of drug during feeding by a breast it is necessary to remember that Prednisolonum gets into breast milk.

Children.

Drug is used in pediatric practice.

Before an initiation of treatment of the patient it is necessary to inspect regarding identification of possible contraindications. Clinical inspection has to include a research of cardiovascular system, X-ray inspection of lungs, a research of a stomach and duodenum; systems of urination, organs of sight. Laboratory inspection has to include: the general blood test, concentration of glucose in blood and urine, electrolytes in a blood plasma.

At treatment glucocorticoids recommend to control regularly arterial pressure for a long time, to determine glucose level in urine and blood, to carry out the analysis a calla on the occult blood, analyses of indicators of a fibrillation, radiological control of a backbone, ophthalmologic inspection (1 time in   3 months).

Children who during treatment were in contact with patients with measles or chicken pox as prevention should appoint specific immunoglobulins (  for 10 days after contact).

During treatment it is not necessary to carry out immunization.

If during treatment by glucocorticoids patients have unusual stressful situations, increase in a dose of high-speed corticosteroids to, in time and after a stressful situation is recommended.

During treatment by Prednisolonum it is not necessary to take alcohol.

Depending on duration of treatment and a dose, perhaps negative impact of drug on calcium metabolism. Prevention of osteoporosis is recommended that is especially important in the presence at patients of risk factors (including – family tendency, advanced age, a postmenopause, insufficient consumption of protein and calcium, excessive smoking, alcohol overconsumption, and also decrease in physical activity). Prevention is based on sufficient consumption of calcium and vitamin D, and also includes physical activity.

For reduction of side effects of therapy Prednisolonum justified is purpose of the corresponding diet.

When using high doses of Prednisolonum throughout the long period (30 mg/days within at least 4 weeks) there can be reversible disturbances of a spermatogenesis remaining for several months after the medicine reception termination.

At patients who received Prednisolonum doses above physiological (about 7,5 mg of Prednisolonum or an equivalent) more than 3 weeks, it is necessary to stop treatment by Prednisolonum gradually. Treatment needs to be stopped gradually even if it lasted less than 3 weeks, at such groups of patients:

–  the patients passing a repeated course of treatment Prednisolonum;

–  patients to whom the repeated course of treatment was appointed for a year after prolonged treatment (months, years);

–  the patients receiving more than 40 mg/days of Prednisolonum or an equivalent;

–  patients with epinephral insufficiency which reason exogenous reception of corticosteroids is not.

After the termination of treatment emergence of a withdrawal, insufficiency of adrenal glands, and also an exacerbation of a disease concerning which Prednisolonum was appointed is possible. If after the end of treatment Prednisolonum observes functional insufficiency of adrenal glands, it is necessary to resume immediately administration of drug, and to carry out reduction of a dose very slowly and with care (for example, the daily dose needs to be reduced by 2-3 mg within 7-10 days).

The atrophy of bark of adrenal glands develops at long therapy and can remain for many years after the treatment termination.

The steroid-induced secondary adrenal insufficiency can be reduced to the dose, minimum as a result of gradual reduction. This type of insufficiency can remain within several months after the end of therapy therefore at any stressful situation which arose during this period it is necessary to resume therapy by corticosteroids.

At sudden cancellation, especially in case of the previous use of high doses, there is a withdrawal which is shown by fever, a loss of appetite, nausea, vomiting, diarrhea, block, dizziness, generalizuyemy musculoskeletal pains, an adynamy.

Because of danger of development of a hypercorticoidism the new course of treatment Prednisolonum within several months always needs to be begun with a cortisone after the carried-out earlier prolonged treatment with low initial doses (except for acute states, life-threatening).

At children in a growth period glucocorticosteroids can be applied only according to absolute indications and under especially careful observation of the attending physician.

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

In need of use of Prednisolonum against the background of reception of peroral gipoglikemiziruyushchy drugs or anticoagulants it is necessary to adjust the mode of dosing of the last.

It is necessary to control especially carefully electrolytic balance at the combined use of Prednisolonum with diuretics. At prolonged treatment Prednisolonum for the purpose of prevention of a hypopotassemia it is necessary to appoint drugs of potassium and the corresponding diet in connection with possible increase in intraocular pressure and development of ability of a subkapsulyarny cataract.

Use at serious infectious diseases is admissible only against the background of specific antimicrobic therapy.

Women during a menopause need to pass a research of rather possible developing of osteoporosis.

At Addison's disease it is necessary to avoid co-administration of barbiturates because of risk of development of acute adrenal insufficiency (addison crisis).

If are present at the anamnesis psoriasis, spasms, Prednisolonum it is necessary to apply only in minimal effective doses.

With extra care it is necessary to use drug at a liver and renal failure, migraine.

The special attention is required by a question of use of system corticosteroids for patients with the heavy affective frustration existing or available in the anamnesis which include depressive, maniac-depressive psychosis, the previous steroid psychosis. Patients and/or trustees have to be warned concerning a possibility of development of serious side effects from mentality. Symptoms are usually shown within several days or weeks after an initiation of treatment. The risk of emergence of these side effects is higher at use of high doses. The majority of reactions disappear after reduction of a dose or drug withdrawal though sometimes specific treatment is necessary. At development of similar symptoms it is necessary to see a doctor. Also mental disorders can be observed during cancellation of glucocorticoids.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Frequency of development and expressiveness of side effects depend on duration of use, size of the used dose and a possibility of observance of a circadian rhythm of appointment.

From cardiovascular system: arrhythmia, bradycardia, arterial hypertension, development or strengthening of displays of chronic heart failure, ECG change characteristic of a hypopotassemia. Patients with an acute and subacute 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 system of a kroviya of lymphatic system: a leukocyturia, the hypercoagulation leading to thromboses and thromboembolisms.

From a nervous system: headache, dizziness, cerebellum pseudoneoplasm, increase in intracranial pressure, spasm.

From bodies a zreniya:zadny subkapsulyarny cataract, increase in intraocular pressure with possible injury of an optic nerve, tendency to development of consecutive bacterial, fungal or viral infections of eyes, trophic changes of a cornea, an exophthalmos.

From the alimentary system: nausea, vomiting, pain in epigastriums, diarrhea, pancreatitis, "steroid" stomach ulcer and a duodenum, an erosive esophagitis, bleeding and perforation of digestive tract, increase or a loss of appetite, a meteorism, a hiccups. In rare instances – increase in activity of "hepatic" transaminases and an alkaline phosphatase.

From skin and hypodermic cellulose: delay of process of regeneration, a petechia, bruises, hematomas, ecchymomas, striya, thinning of skin, hyper - or hypopigmentation, eels, tendency to development of a pyoderma.

From a musculoskeletal system and connecting fabric: delay of growth and processes of ossification at children (premature closing of epiphyseal regions of growth), osteoporosis, is very rare – pathological fractures of bones, an aseptic necrosis of a head humeral and a femur, a rupture of sinews of muscles, a "steroid" myopathy, reduction of muscle bulk (atrophy).

From endocrine system: decrease in tolerance to glucose, a "steroid" diabetes mellitus or manifestation of a latent diabetes mellitus, oppression гипоталамо - pituitary and adrenal system, disturbance of a menstrual cycle, delay of growth at children and teenagers, a delay of sexual development at children, an Icenco-Cushing syndrome (a crescent-shaped face, obesity of pituitary type, a hirsutism, increase in arterial pressure, a dysmenorrhea, an amenorrhea, a myasthenia, striya).

From a metabolism: a hypocalcemia, negative nitrogenous balance (the increased disintegration of proteins), increase in body weight. The side effects caused by glucocorticosteroid activity of Prednisolonum: a delay of liquid and Na + (peripheral hypostases), a hypernatremia, a gipokaliyemichesky syndrome – arrhythmia, a mialgiya or a spasm of muscles, unusual weakness and fatigue.

Infections and invasions: decrease in resistance of an organism to infections.

From immune system: rash, itch, hyperemia, small tortoiseshell, Quincke's edema, acute anaphylaxis.

From mentality: delirium, disorientation, euphoria, hallucinations, maniac-depressive psychosis, depression, paranoia, nervousness, concern, sleeplessness.

Others: withdrawal, hypostases, aphthous ulcers, increase in risk of emergence of urolites.

Interaction with other medicines:

At simultaneous use of Prednisolonum with other medicines perhaps:

with hormones of a thyroid gland, inductors of liver enzymes, in particular with barbiturates, Phenytoinum, pirimidony, carbamazepine, rifampicin – easing of effects of Prednisolonum as a result of increase in its system clearance;

with estrogen (including oral contraceptives which part estrogen is), cyclosporine, CYP3A4 inhibitors, in particular erythromycin, klaritromitsiny, ketokonazoly, diltiazem, aprepitanty, itrakonazoly, Oleandomycinum – strengthening of therapeutic and toxic effects of Prednisolonum;

with antacids – decrease in absorption;

with derivatives of salicylic acid and other nonsteroid antiinflammatory medicines – increase in probability of formation of ulcers of a mucous membrane of a stomach; Prednisolonum reduces the level of derivatives of salicylic acid in blood serum, increasing their renal clearance; drug increases risk of development of hepatotoxic reactions of paracetamol as a result of induction of "hepatic" enzymes and formation of its toxic metabolite;

with cardiac glycosides – strengthening of toxicity of the last, and as a result of the arising hypopotassemia – increase in risk of development of arrhythmias;

with hypoglycemic means – suppression of hypoglycemic effect of peroral antihyperglycemic means and insulin;

with hypotensive drugs – decrease in efficiency of the last;

with tricyclic antidepressants – strengthening of symptoms of the depression caused by Prednisolonum reception and increase in intraocular pressure;

with immunosuppressants – increase in risk of development of infections and a lymphoma or other limfoproliferativny disturbances connected with Epstein-Burra's virus;

with diuretics, purgatives, Amphotericinum In – increase in risk of development of a hypopotassemia; Prednisolonum strengthens risk of development of osteoporosis at simultaneous use with Amphotericinum and inhibitors of a karboangidraza;

with m-holinoblokatorami, antihistaminic medicines, nitrates – increase in intraocular pressure and decrease in efficiency of antihistaminic drugs;

with neuroleptics, Carbutamidum, Azathioprinum – increase in risk of development of a cataract;

with estrogen, anabolic drugs, oral contraceptives – manifestations of a hirsutism and eels;

with live antiviral vaccines and against the background of other types of immunizations – increase in risk of activation of viruses and development of infections;

with muscle relaxants against the background of a hypopotassemia – strengthening of signs and duration of muscular blockade against the background of use of muscle relaxants;

with antikholinesterazny means – emergence of muscular weakness at patients with a myasthenia (especially patients with a myasthenia have gravis);

with Mitotanum and other inhibitors of function of bark of adrenal glands – can cause increase in a dose of drug;

with antiemetics – strengthening of antiemetic effect;

with an isoniazid, meksiletiny, prazikvantely – decrease in their plasma concentration;

with Somatotropinum (in high doses) – decrease in effect of the last;

from ftorkhinolona – injury of a sinew;

with cyclosporine – cases of developing of spasms were noted. As simultaneous administration of these drugs causes mutual braking of metabolism probably that spasms and other side effects connected using each of these drugs both at monotherapy, and at their combined use can arise more often. Combined use can cause increase in concentration of other drugs in a blood plasma.

At long therapy Prednisolonum raises contents of folic acid.

Drug reduces influence of vitamin D on absorption of Ca2 + in an intestines cavity.

Contraindications:

Hypersensitivity to drug components.

The parasitic and infectious diseases of the virus, fungal or bacterial nature existing at the moment or which are recently postponed: the herpes simplex surrounding herpes (a viremichesky phase), chicken pox, measles; the amebiasis, a strongyloidosis (established or suspected); system mycosis; active and latent tuberculosis.

Postvaccinal period (duration of 10 weeks: 8 weeks to and 2 weeks after vaccination), lymphadenitis after BTsZh inoculation.

The immunodeficiency caused by HIV infection.

Digestive tract diseases: a peptic ulcer of a stomach and 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.

Diseases of cardiovascular system: recently postponed myocardial infarction, dekompensirovanny chronic heart failure, arterial hypertension, tendency to a clotting disease.

Diseases of endocrine system: a diabetes mellitus and disturbance of tolerance to carbohydrates, a thyrotoxicosis, a hypothyroidism, Itsenko-Cushing's disease.

Heavy chronic renal and/or liver failure, нефроуролитиаз. Hypoalbuminemia. System osteoporosis. gravis myasthenia. Acute psychosis. Obesity (III-IV Art.). Poliomyelitis (except for a form of bulbar encephalitis). Open and closed-angle glaucoma.

Overdose:

The risk of overdose increases at long use of drug, especially in high doses.

Symptoms: increase in arterial pressure, peripheral hypostases, increase in side effects.

Treatment of acute overdose: immediate gastric lavage or calling of vomiting. There is no specific antidote.

Treatment of chronic overdose: reduction of a dose of drug.

Storage conditions:

Period of validity. 3 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; on the 4th blister strip packagings in a pack.