Prednisolone: instructions for using the medicine, structure, Contraindications ATC Code S01BA04
When ATH: S01BA04
Prednisolone: characteristic
Hormonal agents (glucocorticoid for systemic and topical). It is dehydrated analogue of hydrocortisone.
In medical practice, prednisolone and prednisolone hemisuccinate are used. (for I / O or the / m).
Prednisone is a white or white with weak yellowish white crystalline powder and odourless. Practically insoluble in water, Slightly soluble in alcohol, xloroforme, dioksane, methanol. Molecular weight 360,44.
Prednisolone gemisuktinat — white or white with kremovatam white crystalline powder and odourless. Soluble in water. Molecular weight 460,52.
Prednisolone: pharmachologic effect
Glucocorticoid, anti-inflammatory, antiallergic, protivoshokovoe, immunosuppressive.
Prednisolone: application
Parenteral administration. Acute allergic reactions; bronchial asthma, asthmatic status; prevention or treatment of thyrotoxic response and thyrotoxic crisis; shock, incl. resistant to other therapies; myocardial infarction; acute adrenal insufficiency; cirrhosis of the liver, acute hepatitis, acute renal failure; poisoning cauterizing liquids (to reduce inflammation and prevent scarring restrictions).
Intra: rheumatoid arthritis, Spondylitis, posttravmaticheskiy arthritis, osteoarthritis (when there are significant signs of joint inflammation, synovitis).
Pills. Systemic diseases of connective tissue (systemic lupus erythematosus, scleroderma, periarteritis nodosa, dermatomyositis, rheumatoid arthritis); acute and chronic inflammatory diseases of the joints: podagricheskiy and psoriaticheskiy arthritis, osteoarthritis (incl. posttraumatic), polyarthritis, frozen shoulder, ankylosing spondylitis (ankylosing spondylitis), yuvenilynыy arthritis, Still's syndrome in adults, ʙursit, nonspecific tenosynovitis, synovitis and epicondylitis; rheumatic fever, Acute rheumatic heart disease; bronchial asthma; acute and chronic allergic diseases: allergies to drugs and food, serum sickness, hives, nasal allergy, angioedema, drug rash, pollen disease; skin diseases: pemphigus, psoriasis, eczema, atopic dermatitis, atopic dermatitis, contact dermatitis (with damage to a large area of the skin), drug reaction, seborrheic dermatitis, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), bullous dermatitis herpetiformis, malignant exudative erythema (Stevens-Johnson syndrome); swelling of the brain (incl. amid brain tumor or associated with surgery, radiotherapy or head injury) after pre parenteral administration; congenital adrenal hyperplasia; primary or secondary adrenal insufficiency (incl. condition after the removal of the adrenal glands); kidney disease of autoimmune origin (incl. acute glomerulonephritis), nephrotic syndrome; subacute thyroiditis; diseases of the blood: agranulocytosis, panmyelopathy, autoimmunnaya gemoliticheskaya anemia, Congenital (erythroid) gipoplasticheskaya anemia, acute lymphatic- and myeloid leukemias, limfogranulematoz, multiple myeloma, trombotsitopenicheskaya purpura, secondary thrombocytopenia in adults, erythroblastopenia (эritrotsitarnaya anemia); lung diseases: Acute alveolitis, fibrosis lyegkikh, sarcoidosis II-III st.; tuberculous meningitis, pulmonary tuberculosis, inhalation pneumonia (in combination with a specific chemotherapy); berylliosis, Loffler's syndrome (not amenable to other therapy); lung cancer (in combination with cytostatics); multiple sclerosis; gastrointestinal diseases (to remove the patient from the critical state): yazvennыy colitis, Crohn's disease, Local enteritis; hepatitis; prevention of graft rejection; hypercalcemia on the background of cancer; nausea and vomiting during cytostatic therapy; ocular allergy: allergic corneal ulcers, allergic conjunctivitis form; inflammatory diseases of the eye: transferred ophtalmia, heavy sluggish front and posterior uveitis, optic neuritis.
Ointment: hives, atopic dermatitis, atopic dermatitis, simple chronic zoster (limited neurodermatitis), eczema, seborrheic dermatitis, discoid lupus erythematosus, simple and allergic dermatitis, drug reaction, erythroderma, psoriasis, alopecia; epicondylitis, tendosynovyt, ʙursit, frozen shoulder, keloid scars, işialgija.
Eye drops: non-infectious inflammatory diseases of the anterior segment of the eye-iritis, iridocyclitis, uveitis, episcleritis, scleritis, conjunctivitis, parenchymal and discoid keratitis without damage to the corneal epithelium, allergic conjunctivitis, blefarokonъyunktyvyt, .Aloe, inflammation after eye injuries and surgeries, transferred ophtalmia.
Prednisolone: Contraindications
Hypersensitivity (for short-term use of the system for health is the only contraindication).
For systemic use: parasitic and infectious diseases of viral, fungal or bacterial origin (currently without appropriate chemotherapy 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. Immunodeficiency states (incl. AIDS or HIV infection), post-vaccination period (period duration 8 Sun and up 2 weeks after vaccination), lymphadenitis after BCG vaccination; gastrointestinal diseases (incl. gastric ulcer and duodenal ulcer, esophagitis, gastritis, acute or latent peptic ulcer, recently established intestinal anastomosis, ulcerative colitis with the threat of perforation or abscess, diverticulitis); diseases of the cardiovascular system, incl. recent myocardial infarction (in patients with acute and subacute myocardial infarction may spread necrosis, slowing the formation of scar tissue and, thereby, rupture of the heart muscle), decompensated chronic heart failure, arterial hypertension, hyperlipidemia; endocrine diseases: diabetes (incl. violation of carbohydrate tolerance), thyrotoxicosis, gipotireoz, pituitary basophilia; severe chronic renal and / or hepatic insufficiency, nefrourolitiaz; hypoalbuminemia and condition, predisposing to its occurrence; systemic osteoporosis, myasthenia gravis, acute psychosis, Obesity III-IV Art., polio (except bulbar form of encephalitis), openly- zakrыtougolynaya and glaucoma, pregnancy, lactation.
For intraarticular administration: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), chressustavnoy fracture, infectious (septic) inflammation in the joints and periarticular infections (incl. history), common infectious disease, marked periarticular osteoporosis, no signs of inflammation in the joint (T. N. "Dry" joint, such as osteoarthritis without signs of 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, pregnancy.
When applied to the skin: Bacterial, Viral, fungal skin diseases, cutaneous manifestations of syphilis, lupus, skin tumors, acne vulgaris, rosacea (possible worsening of the disease), pregnancy.
Eye drops: viral and fungal diseases of the eye, acute purulent conjunctivitis, purulent infection of the mucous membrane of the eyes and eyelids, purulent corneal ulcer, viral conjunctivitis, trachoma, glaucoma, violation of the integrity of the corneal epithelium; Tuberculosis eyes; condition after the removal of a foreign body of the cornea.
Prednisolone: use during pregnancy and lactation
The use of corticosteroids during pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety of not performed). Women of childbearing age should be warned about the potential risk to the fetus (Corticosteroids cross the placenta). It should be carefully monitored for newborns, whose mothers during pregnancy were treated with corticosteroids (adrenal insufficiency may develop in the fetus and newborn).
Do not use often, large doses, over a long period of time. Nursing women should stop any breastfeeding, or use of drugs, especially in high doses (corticosteroids penetrate into breast milk and could suppress growth, production of endogenous corticosteroids and cause undesirable effects in the newborn).
Prednisolone shown to be teratogenic in many species of animals, get it in doses, equivalent dose for humans. In studies in pregnant mice, rats and rabbits there were an increase in the incidence of cleft palate in the offspring.
Prednisolone: side effects
The frequency and severity of side effects depend on the way, the duration of use, the dosage used and the possibility of compliance circadian rhythm of destination PM.
Systemic effects
Metabolism: delay Na+ and body fluid, kaliopenia, hypokalemic alkalosis, negative nitrogen balance as a result of protein catabolism, giperglikemiâ, glycosuria, weight gain.
On the part of the endocrine system: secondary adrenal and hypothalamic-pituitary insufficiency (particularly during times of stress, such as illness, trauma, surgery); Cushing's syndrome; growth suppression in children; menstrual irregularities; reduced tolerance to carbohydrates; a manifestation of latent diabetes mellitus, increase the need for insulin or oral antidiabetic drugs in patients with diabetes.
Cardio-vascular system and blood (hematopoiesis, hemostasis): increased blood pressure, development (in predisposed patients) or increased severity of chronic heart failure, hypercoagulation, thrombosis, ECG changes, typical of hypokalemia; in patients with acute and subacute myocardial infarction is necrosis lesion distribution, slowing the formation of scar tissue with a possible rupture of the heart muscle, occlusive disease.
On the part of the musculoskeletal system: muscular weakness, steroidnaya myopathy, loss of muscle mass, osteoporosis, a compression fracture of the spine, aseptic necrosis of the femoral head and the shoulder bones, pathological fractures of long bones.
From the digestive tract: steroid ulcer with possible perforation and hemorrhage, pancreatitis, flatulence, ulcerative esophagitis, indigestion, nausea, vomiting, increased appetite.
For the skin: Hyper- or hypopigmentation, subcutaneous and each atrophy, abscess, atrophic band, acne, delayed wound healing, thinning of the skin, petechiae and ecchymosis, эritema, increased sweating.
From the nervous system and sensory organs: mental disorders, such as delirium, disorientation, euphoria, hallucinations, depression; increased intracranial pressure syndrome stagnant nipples optic nerve (pseudotumor of the brain — more often in children, usually after too rapid dose reduction, the symptoms — headache, deterioration of visual acuity or double vision); sleep disturbance, dizziness, vertigo, headache; sudden loss of vision (by parenteral administration in the head, Neck, turbinates, Scalp), posterior subcapsular cataract formation, increase of intraocular pressure with possible damage to the optic nerve, glaucoma; steroid exophthalmos.
Allergic reactions: Generalized (atopic dermatitis, hives, anaphylactic shock) and local.
Other: generalized weakness, masking of symptoms of communicable diseases, swoon, withdrawal.
When applied to the skin: steroid acne, purpura, teleangiэktazii, burning and itching of the skin, irritation and dryness of the skin; long-term use and / or applied to a large surface may be a manifestation of systemic side effects, development of Cushing (In these cases, supersede ointment); prolonged use of ointment may also develop secondary infections of skin lesions, atrophic changes, hypertryhoza.
Eye drops: with long-term use is increased intraocular pressure, damage to the optic nerve, posterior subcapsular cataract formation, the severity of the violation and the narrowing of the field of view (blurring or loss of vision, sore eyes, nausea, dizziness), with the thinning of the cornea — the risk of perforation; rarely is the spread of viral or fungal eye diseases.
Prednisolone: interaction
With simultaneous application of cardiac glycosides, and prednisolone because of the emerging hypokalemia increases the risk of cardiac arrhythmias. Barbiturates, antiepileptic drugs (phenytoin, Carbamazepine), rifampicin accelerates metabolism of glucocorticoids (by induction of microsomal enzymes), weaken their action. Antihistamines weaken the effect of prednisolone. Thiazide diuretics, Amphotericin B, carbonic anhydrase inhibitors increase the risk of severe hypokalaemia, On+-contain HP-edema and ad. When using prednisolone and paracetamol increases the risk of hepatotoxicity. Oral contraceptive formulations, containing estrogen, may alter protein binding and metabolism of prednisolone, reducing clearance and increasing T1/2, strengthening, thus, the therapeutic and toxic effects of prednisolone. When concomitant administration of prednisolone and anticoagulants (coumarin derivatives, indandiona, Heparin) possible weakening of the anticoagulant action of the past; the dose should be verified on the basis of the definition of PV. Tricyclic antidepressants may enhance mental disorders, associated with taking prednisone, incl. severity of depression (should not be prescribed for the treatment of these disorders). Prednisone oslablyaet hypohlykemycheskoe Action peroralnыh protyvodyabetycheskyh LS, insulin. Immunosuppressive drugs increase the risk of infection, lymphomas and other lymphoproliferative disorders. NSAIDs, acetylsalicylic acid, Alcohol increases the risk of ulcers and bleeding from the gastrointestinal tract. During the period of immunosuppressive doses of corticosteroids and vaccines, containing live viruses, replication of viruses and development of viral diseases, reduction in antibody production (concurrent use is not recommended). When applied with other vaccines — may increase the risk of neurological complications and reduced production of antibodies. Increases (prolonged use) folate. It increases the likelihood of disturbances on the background electrolyte metabolism diuretics.
Prednisolone: overdose
The risk of overdose increases with long-term use of prednisone, especially in large doses.
Symptoms: increased blood pressure, peripheral edema, increased side effects of the drug.
Treatment of acute overdose: immediate gastric lavage or induction of vomiting, specific antidote is not found.
Treatment of chronic overdose: should reduce the dose of the drug.
Prednisolone: Dosing and Administration
Inside, parenterally (I /, / m), vnutrisustavno, outwardly. The route of administration and dosage regimen are selected individually depending on the nature and severity of the disease, patient's condition and response to therapy.
Inside (All or most of the dose administered in the morning). During replacement therapy initial dose of 20-30 mg/day, supporting-5-10 mg/day. If necessary, use a higher dose. Treatment stopped slowly, gradually reducing the dose. For children initial dose-1-2 mg/kg body weight per day for 4-6 receptions, supporting-0.3-0.6 mg/kg/day.
In large joints injected 25-50 mg, in the joints average is 10-25 mg, small-5-10 mg. For tissue infiltration — from 5 to 50 mg, intralesional at Dupuytren's contracture.
B / (usually first jet, then drip), if you can not / in the administered / m at the same doses. When a single dose of shock 0.05-0.15 g (in severe cases, to 0,4 g), again, through 3-4 h, daily dose of 0.3-1.2 g. In acute adrenal insufficiency single dose of 0.1-0.2 g, daily 0.3-0.4 g. When asthmatic status is administered by 0.5-1.2 g / day with subsequent dose reduction to 0,3-0,15-0,1 g / day. If severe allergic reactions is injected in a dose of 0.1-0.2 g/d.
Eye drops instilled in the conjunctival sac: 1-2 drops 3 once a day, In acute cases, medication is instilled every 2-4 hours. After eye surgery is prescribed only for 3-5 days after surgery.
Outwardly. The ointment is applied in a thin layer to the affected skin 1-3 times a day. The duration of treatment depends on the nature of the disease and the effectiveness of therapy, and is, usually, 6-14 Days. In limited areas to enhance the effect of occlusive dressings can be used.
Prednisolone: precautions
Appoint glucocorticoids need in the smallest doses and the minimum duration of time, required to achieve the desired therapeutic effect. In the appointment should take into account the daily circadian rhythm of endogenous secretion of glucocorticoids: in 6-8 h am appoint more (All or) of the dose.
In case of stress patients, We are on corticosteroid therapy, It is shown parenteral administration of corticosteroids to, during and after the stressful situation.
If you have a history of psychosis indicate high doses prescribed under strict medical supervision.
During treatment, especially with prolonged use, should carefully monitor the dynamics of growth and development in children, the need to monitor ophthalmologist, BP control, water and electrolyte balance, Blood Glucose, regular analyzes of the cells of peripheral blood.
The sudden discontinuation of treatment can cause the development of acute adrenal insufficiency; long-term use can not suddenly cancel the drug, the dose should be reduced gradually. With the sudden cancellation after long-term use may develop withdrawal, manifested by fever, myalgia and arthralgia, malaise. These symptoms may appear even in the case of, When not marked adrenal insufficiency.
Prednisolone may mask symptoms of infection, to reduce resistance to infection.
During treatment with eyedrops is necessary to control the intraocular pressure and the condition of the cornea.
In applying the ointment in children 1 and older need to limit the total duration of treatment and eliminating activities, leading to increased absorption and resorption (Warming, fixing and occlusive dressings). For the prevention of infectious skin lesions prednisolone ointment recommended given in combination with antibacterial and antifungal agents.
Prednisolone: interaction
Active substance | Description of interaction |
Akarʙoza | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; with a joint appointment is necessary to monitor the concentration of glucose in the blood. |
Acetylsalicylic acid | Increases (mutually) the risk of ulcer formation and gastrointestinal bleeding. Against the backdrop of the abolition of prednisolone (lowers plasma levels) concentration in the blood can rise, sometimes leading to toxic effects. |
Glimepiride | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; with a joint appointment is necessary to monitor the concentration of glucose in the blood. |
Glipizide | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; with a joint appointment is necessary to monitor the concentration of glucose in the blood. |
Digoxin | FMR: synergism. Against the background of prednisolone (increases the loss of potassium) It increases the probability of toxic manifestations (hypokalemia increases myocardial sensitivity to digoxin). |
Insulin aspart | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; with a joint appointment required glycemic control. |
Insulin dvuhfaznыy [human genetic engineering] | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; the combined appointment is necessary to control the level of glucose in the blood. |
Insulin soluble [pork monocomponent] | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; the combined use requires monitoring of blood glucose levels. |
Levothyroxine sodium | FKV. FMR. Against the background of weakened prednisolone (short, without the development of hypothyroidism) effect; because it reduces the concentration of thyroxine binding globulin, can decrease the content of levothyroxine associated plasma. |
Metformin | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; combined use requires monitoring of blood glucose levels. |
Pioglitazone | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; joint application requires monitoring of blood glucose levels. |
Protirelin | FMR: antagonizm. Against the background of the effect of prednisolone reduced (stimulating the secretion of thyroid-stimulating hormone). |
Repaglinide | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; with a joint appointment required monitoring of blood glucose. |
Rifampicin | FMR: antagonizm. It accelerates and reduces the effect of biotransformation. |
Rosiglitazone | FMR: antagonizm. Against the background of the effect of prednisolone is weakened; the combined use requires monitoring of blood glucose levels. |
Somatropin | FMR: antagonizm. Against the backdrop of prednisone effect is stimulation of growth-reduced. |
Cyclosporine | FKV. Reduces the clearance and prolongs the effect of. |