Prednisolone

Active material: Prednisolone
When ATH: H02AB06
CCF: GCS for injection
When CSF: 04.01
Manufacturer: M.J.BIOPHARM Pvt.Ltd. (India)

Pharmaceutical form, composition and packaging

Solution for in / and the / m clear, colorless or slightly yellow or greenish-yellow.

Excipients: nicotinamide, disodium эdetat, sodium bisulfite, Sodium hydroxide (to maintain the pH level), water d / and.

1 ml – colorless glass vials (3) – trays, plastic (1) – packs cardboard.
1 ml – vials of dark glass (3) – trays, plastic (1) – packs cardboard.

Pills round, flat, beveled the edges, white, with Valium on one side.

Excipients: sodium carboxymethyl, starch, lactose, magnesium stearate, talc, microcrystalline cellulose.

100 PC. – plastic bags.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

GCS. It inhibits the function of leukocytes and tissue macrophages. Limit the migration of leukocytes to inflammation. Violates the ability of macrophages to phagocytosis, as well as the formation of interleukin-1. Contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. Decreases capillary permeability, caused by the release of histamine. Inhibits the activity of fibroblasts and collagen formation.

Inhibits the activity of phospholipase A₂, which leads to suppression of the synthesis of prostaglandins and leukotrienes. It suppresses the release of COX (especially COX-2), which also helps to reduce the production of prostaglandins.

It reduces the number of circulating lymphocytes (T- and B-cells), monotsitov, eosinophils and basophils as a result of their displacement from the vascular tissue into the lymphoid; suppresses the formation of antibodies.

Prednisone suppresses the release of pituitary ACTH and β-lipotropina, but it does not reduce the level of circulating β-endorphin. It inhibits the secretion of TSH and FSH.

When the immediate application of the receptacles has a vasoconstrictor effect.

Prednisone has a pronounced dose-dependent effects on carbohydrate metabolism, protein and fat. Stimuliruet gluconeogenesis, facilitates the capture of amino acids liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver increases glycogen deposition of prednisone, stimulating the activity of glycogen synthesis and glucose from products of protein metabolism. Increased blood glucose activates the secretion of insulin.

Prednisone suppresses the capture of glucose fat cells, leading to activation of lipolysis. However, due to an increase in insulin secretion are stimulated lipogenesis, that contributes to the accumulation of fat.

It has catabolic effect in the lymphoid tissue and connective, muscle, fat tissue, skin, bone. To a lesser extent than hydrocortisone, effect on vodno-elektrolitnogo Exchange processes: promotes the excretion of potassium ions and calcium, delay in the body of sodium ions and water. Osteoporosis and Cushing's syndrome are the main factors, limits the duration of therapy with corticosteroids. As a result of catabolic actions may suppress growth in children.

High doses of prednisone may increase excitability of brain tissue and contributes to lowering the threshold sudorojna preparedness. Stimulates excess production of hydrochloric acid and pepsin in the stomach, that leads to the development of peptic ulcers.

The systems use therapeutic activity of prednisone due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative effects.

External and local application of therapeutic activity of prednisone due to anti-inflammatory, anti-allergic and antiexudativ (thanks vasoconstrictor effect) action.

Compared to gidrokortizonom anti-inflammatory activity of prednisone in 4 times, mineralokortikoidnaja activity 0.6 half.

Pharmacokinetics

The ingestion well absorbed from the digestive tract. C_max in plasma observed after 90 m. In the most part plasma prednisone is associated with transkortinom (kortizolsvjazyvajushhim globulin). It is metabolized primarily in the liver.

T_1/2 is about 200 m. Excreted by the kidneys in unchanged form – 20%.

Testimony

For the reception inside and the parenteral use: rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, bronchial asthma, asthmatic status, acute and chronic allergic diseases, anaphylactic shock, Addison's disease, acute adrenal insufficiency, congenital adrenal hyperplasia; hepatitis, pechenochnaya coma, hypoglycemic states, lipoid nephrosis; agranulocytosis, various forms of leukemia, limfogranulematoz, trombotsitopenicheskaya purpura, gemoliticheskaya anemia; chorea; pemphigus, eczema, itch, exfoliative dermatitis, psoriasis, prurigo, seborrheic dermatitis, SLE, erythroderma, alopecia.

For intraarticular administration: chronic polyarthritis, posttravmaticheskiy arthritis, osteoarthritis of large joints, certain rheumatic joints, arthrosis.

For introduction into the tissue infiltration: epicondylitis, tendinitis, ʙursit, frozen shoulder, keloid, işialgii, Dupuytren's Contracture, rheumatic and similar joints and various tissues.

For the use in ophthalmology: allergic, chronic and atypical conjunctivitis and blepharitis; corneal inflammation in the mucosa intact; acute and chronic inflammation of the anterior segment of the choroid, Sclera and jepisklery; sympathetic branch inflammation of the eyeball; after injuries and operations during prolonged stimulation of eyeballs.

Dosage regimen

The ingestion for replacement therapy in adults, the initial dose is 20-30 mg / day, maintenance dose – 5-10 mg / day. If necessary, the initial dose may be 15-100 mg / day, supports – 5-15 mg / day. Daily dose should be reduced gradually. For children initial dose of 1-2 mg / kg / day 4-6 receptions, supports – 300-600 ug / kg / day.

When the/m or/in a dose of, multiplicity and duration of application are determined individually.

When vnutrisustavnom the introduction of large joints applied dose 25-50 mg, for the joints of medium size – 10-25 mg, for small joints – 5-10 mg. For introduction into the tissue infiltration depending on the severity of the condition and size of the affected area apply a dose of 5 to 50 mg.

Topically applied in ophthalmology 3 times / day, a course of treatment – no more 14 days; in dermatology – 1-3 times / day.

Side effect

On the part of the endocrine system: menstrual irregularities, adrenal suppression, Cushing's syndrome, Suppression of the pituitary-adrenal system functions, reduced tolerance to carbohydrates, steroidnyi diabetes or manifestation of latent diabetes mellitus, growth retardation in children, delayed sexual development in children.

From the digestive system: nausea, vomiting, Steroid ulcers of the stomach and duodenum, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, Ikotech. In rare cases, – increase in liver transaminases and alkaline phosphatase.

Metabolism: nitrogenous negative balance due to protein catabolism, increased calcium excretion from the body, hypocalcemia, weight gain, increased perspiration.

Cardio-vascular system: potassium loss, hypokalemic alkalosis, arrhythmia, bradycardia (up to heart failure); steroidnaya myopathy, heart failure (development or increased symptoms), ECG changes, typical of hypokalemia, increased blood pressure, hypercoagulation, thrombosis. In patients with acute myocardial infarction – spread necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

On the part of the musculoskeletal system: slowing growth and ossification processes in children (premature closure of the epiphyseal growth zones), osteoporosis (rarely – pathological fractures, aseptic necrosis of the humeral head and femur), muscle tendon rupture, muscular weakness, steroidnaya myopathy, decrease in muscle mass (atrophy).

CNS: headache, intracranial hypertension, delirium, disorientation, euphoria, hallucinations, affective insanity, depression, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, seizures.

On the part of the organ of vision: zadnyaya subkapsulyarnaya cataracts, increased intraocular pressure (with the possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, the propensity for development of secondary infection (bacterial, fungal, viral).

Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, Hyper- or hypopigmentation, acne, striae, propensity to development of pyoderma and candidiasis.

Reaction, due to the influence of immunodepressive: slowing the regeneration processes, reduced resistance to infections.

For parenteral administration: in rare cases anaphylactic or allergic reaction, Hyper- or hypopigmentation, atrophy of the skin and subcutaneous tissue, aggravation after intrasinovial'nogo application, arthropathy, Charcot type, sterile abscesses, When introduced into the pockets on the head – blindness.

Contraindications

For short-term use for health reasons – hypersensitivity to prednizolonu.

For intraarticular administration and the introduction of directly to the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infectious (septic) inflammation in the joints and periarticular infections (incl. history), as well as common infectious disease, marked periarticular osteoporosis, no signs of inflammation in the joint (“dry” joint, eg osteoarthritis without synovitis), marked bone destruction and deformity of the joint (sharp narrowing of the joint space, ankiloz), instability of the joint as a result of arthritis, aseptic necrosis of the formative joint epiphyses of bones.

For outdoor use: Bacterial, Viral, fungal skin diseases, lupus, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), childhood (to 2 years, itching in the anal area – to 12 years), Rosacea, acne vulgaris, perioral dermatitis.

For the use in ophthalmology: Bacterial, Viral, fungal diseases of the eye, ocular tuberculosis, trachoma, violation of the integrity of the epithelium of the eye.

Pregnancy and lactation

When pregnancy (especially in the I trimester) used only for health reasons. If you must use during lactation should be carefully weighed the expected benefit of treatment for mother and child at risk.

Cautions

C use caution when parasitic and infectious diseases virus, fungal or bacterial origin (currently or recently transferred, including the recent contact with a patient) – herpes simplex, herpes zoster (viremicheskaya phase), enable vetryanaya, kor, ameʙiaz, strongiloidoz (or suspected), systemic mycosis; active and latent tuberculosis. Application for serious infectious diseases is permissible only against the background of specific therapy.

Be wary of during the 8 weeks before and 2 weeks after vaccination, when lymphadenitis after BCG vaccination, with immunodeficiency (incl. AIDS or HIV-infection).

To apply caution in diseases of the DIGESTIVE TRACT: gastric ulcer and duodenal ulcer, эzofagite, gastritis, acute or latent peptic ulcer, recently established intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess, diverticulum.

To apply caution in diseases of cardiovascular system, incl. after recent myocardial infarction (in patients with acute and subacute myocardial infarction may spread necrosis, slowing the formation of scar tissue and thereby break the heart muscle), In decompensated chronic heart failure, hypertension, giperlipidemii), in endocrine diseases – diabetes (incl. violation of carbohydrate tolerance), thyrotoxicosis, gipotireoze, Cushing's disease, in severe chronic renal and / or hepatic insufficiency, nefrourolitiaze, with hypoalbuminemia and conditions, predisposing to its occurrence, at systemic osteoporosis, myasthenia, Ostrom psychosis, obesity (III-IV degrees), when polio (except bulbar form of encephalitis), openly- and angle-closure glaucoma.

If necessary, intra-articular introduction to apply caution in patients with a common grave condition, ineffectiveness (or short-term) actions 2 predыduschyh introduced (taking into account the individual properties used GCS).

During treatment (especially long) you must observe ophthalmologist, monitoring ad vodno-elektrolitnogo balance and, as well as paintings peripheral blood, glucose; in order to reduce the side effects of anabolic steroids can be assigned, antibiotics, and increase the flow of potassium in the body (diet, potassium supplements). It is recommended to clarify the need for the introduction of ACTH after a course of prednisolone (After the skin test!).

When Addison disease should avoid simultaneous application with barbituratami.

After the end of treatment, you may experience withdrawal syndrome, adrenal insufficiency, as well as exacerbation of disease, the prednisone was appointed.

When intercurrent infections, septic conditions and tuberculosis, must be simultaneous antibiotic.

Children in the period of growth of the SCS should apply only in absolute condition and under close supervision of a physician.

Naruzhno should not be applied more 14 days. If the ordinary or pink ugrah may exacerbate diseases.

Drug Interactions

If you are applying to prednisolone antikoagulyantami may increase protivosvertyvajushhego the last action.

If you are applying with salicilatami increases the likelihood of bleeding.

Together with the use of diuretics is perhaps worsening violations elektrolitnogo Exchange.

Together with the use of hypoglycemic drugs decreases the speed of lowering blood glucose levels.

Together with the use of cardiac glycosides amplified risk of Glycoside intoxication.

If you are applying with rifampitsinom possible weakening of therapeutic action rifampitina.

If you are applying gipotenziveh funds may reduce their effectiveness.

Together with the use of coumarin derivatives possible weakening of antikoaguljantnogo effect.

Together with the use of rifampicin, phenytoin, barbiturates possible weakening of prednisolone.

Together with the use of hormonal contraceptives – strengthening of prednisolone.

When acetylsalicylic acid – reduction of Salicylates in the blood.

If you are applying to praziquantel may reduce its concentration in the blood.

The appearance of HIRSUTISM and acne promotes the simultaneous use of other MCS, androgens, estrogen, oral contraceptives and steroid anabolic steroids. The risk of developing cataracts increases when applied on a background of GKS antipsychotic means, karbutamida and azatioprina.

Simultaneous with the m-holinoblokatorami (including antihistamines, tricyclic antidepressants), nitrates promotes increase of intraocular pressure.