Prednisolone Nycomed - instructions for use, dose, side effects, contraindications

Prednisolone Nycomed is a synthetic glucocorticosteroid drug, a dehydrated analog of hydrocortisone. Has anti-inflammatory, antiallergic, immunosuppressive effect, increases the sensitivity of beta-adrenoreceptors to endogenous catecholamines.

Interacts with the cytoplasmic receptors of glucocorticosteroids (GCS) (GCC receptors are present in all tissues, especially in the liver), with the formation of a complex,inducing the formation of proteins (including enzymes that regulate vital processes in cells).

Protein metabolism: reduces the number of globulins in the plasma, increases the synthesis of albumin in the liver and kidneys (with an increase in the albumin / globulin ratio in the blood plasma), reduces synthesis and enhances protein catabolism in muscle tissue.

Lipid metabolism: increases the synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat occurs mainly in the area of the shoulder girdle, face, abdomen), leads to the development of hypercholesterolemia.

Carbohydrate metabolism: increases the absorption of carbohydrates from the gastrointestinal tract; increases the activity of glucose-6-fosfatazy (increase of glucose from the liver into the blood); increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases (activation of gluconeogenesis); promotes the development of hyperglycemia.

Water-electrolyte exchange: retards sodium and water in the body, stimulates the excretion of potassium (mineralocorticoid activity), reduces the absorption of calcium from the gastrointestinal tract, reduces the mineralization of bone tissue.

Anti-inflammatory effect is associated with the suppression of the release of eosinophils and mast cells by inflammatory mediators; inducing the formation of lipocortins and reducing the number of mast cells that produce hyaluronic acid; with a decrease in the permeability of capillaries; stabilization of cell membranes (especially lysosomal) and membranes of organelles. Acts on all phases of the inflammatory process: inhibits prostaglandin synthesis at the level of arachidonic acid (Lipokortin inhibits phospholipase A2 inhibits the release of arachidonic acid and endoperekisey inhibits biosynthesis of the leukotrienes contribute to inflammation, allergies, etc.), Synthesis of "proinflammatory cytokine" (interleukin1, tumor necrosis factor alpha, etc.); increases the stability of the cell membrane, to the action of various damaging factors.

Immunodepressive effect is caused by involution of lymphoid tissue, suppression of lymphocyte proliferation (especially T-lymphocytes), suppression of B-lymphocyte migration and interaction of T and B lymphocytes, inhibition of release of cytokines (interleukin-1, 2; gamma-interferon) from lymphocytes and macrophages and a decrease in the formation of antibodies.

Antiallergic effect develops as a result of a decrease in the synthesis and secretion of mediators of allergy, inhibition of release from sensitized mast cells and basophils of histamine and other biologically active substances, a decrease in the number of circulating basophils, T- and B-lymphocytes, mast cells; suppression of the development of lymphoid and connective tissue, reducing the sensitivity of effector cells to mediators of allergy; oppression of antibody formation, changes in the immune response of the body.

In obstructive airway diseases the effect is mainly due to inhibition of inflammatory processes,prevention or reduction of the degree of edema of the mucous membranes, a decrease in the eosinophilic infiltration of the submucosal layer of the bronchial epithelium and the deposition of circulating immune complexes in the bronchial mucosa, as well as inhibition of erosion and desquamation of the mucosa. Increases the sensitivity of beta-adrenergic receptors of small and medium-sized bronchial tubes to endogenous catecholamines and exogenous sympathomimetics, reduces the viscosity of mucus by reducing its production.

Suppresses the synthesis and secretion of adrenocorticotropic hormone (ACTH) and again - the synthesis of endogenous GCS.

It inhibits connective tissue reactions during the inflammatory process and reduces the possibility of scar tissue formation.

Pharmacokinetics:

Up to 90% of prednisolone binds to plasma proteins: transcortin (globulin binding corticosteroids) and albumins. Prednisolone metabolized in the liver, partially in the kidney and other tissues, mainly by conjugation with glucuronic and sulfuric acids. Metabolites are inactive.

It is excreted with bile and urine by glomerular filtration and is reabsorbed by tubules by 80-90%. 20% of the dose is excreted by the kidneys unchanged.The half-life from the plasma after intravenous administration is 2-3.5 hours.

Indications:

- Shock (burn, traumatic, operational, toxic, cardiogenic) - with ineffectiveness of other therapy;

- alaryngic reactions (acute, severe forms), blood transfusion shock, anaphylactic shock, anaphylactoid reactions;

- aboutbrain tissue (including on the background of a brain tumor or associated with surgical intervention, radiation therapy or head trauma);

- brohnhialnaya asthma (severe form), asthmatic status;

- fromsystemic connective tissue diseases (systemic lupus erythematosus, rheumatoid arthritis);

- aboutstria insufficiency of the adrenal cortex;

- tiritoksichesky crisis;

- abouthepatitis, hepatic coma;

- Reduction of inflammatory phenomena and prevention of cicatricial narrowing (when poisoning with cauterizing fluids).

Contraindications:

- Hypersensitivity to prednisolone and other steroids or to any auxiliary substance (see Composition);

- systemic fungal infections;

- lactation.

In children during the growth period, SCS should be used only in absolute indications and under the strictest supervision of the attending physician.

Carefully:

Carefully the drug should be prescribed in the following diseases and conditions:

- diseases of the gastrointestinal tract - peptic ulcer of the stomach and duodenum, esophagitis, gastritis, acute or latent peptic ulcer, newly created intestinal anastomosis, ulcerative colitis with perforation or abscessing, diverticulitis;

- parasitic and infectious diseases of a viral, fungal or bacterial nature (current or recent, including recent contact with a patient) - herpes simplex, herpes zoster (viremic phase), chicken pox, measles; amebiasis, strongyloidiasis; systemic mycosis; active or latent tuberculosis. The use in severe infectious diseases is permissible only against the background of specific antimicrobial therapy;

- pre- and post-vaccination period (8 weeks before and 2 weeks after vaccination), lymphadenitis after BCG vaccination;

- immunodeficiency states (including AIDS or HIV infection);

- diseases of the cardiovascular system, incl. recently suffered myocardial infarction (in patients with acute and subacute myocardial infarction it is possible to spread the focus of necrosis, slow the formation of scar tissue and, as a result, break the heart muscle),severe chronic heart failure, hypertension, hyperlipidemia, concomitant treatment with diuretics that excrete potassium;

- endocrine diseases - diabetes mellitus (including a violation of carbohydrate tolerance), thyrotoxicosis, hypothyroidism, hyperparathyroidism, Itenko-Cushing's disease, obesity (III-IV item);

- severe chronic renal and / or hepatic insufficiency, nephrourolythiasis;

- hypoalbuminemia and conditions predisposing to its occurrence;

- systemic osteoporosis, myasthenia gravis gravis, acute psychosis, poliomyelitis (with the exception of the form of bulbar encephalitis), open and closed angle glaucoma, lymphatic tumors, latent epilepsy;

- pregnancy.

Pregnancy and lactation:

During pregnancy (especially in the first trimester) is used only for life indications.

With prolonged therapy during pregnancy, the possibility of impaired fetal growth is not ruled out. In the case of use in the III trimester of pregnancy, there is a risk of atrophy of the adrenal cortex in the fetus, which may require replacement therapy in the newborn.

It is impossible to exclude the risk of teratogenic effect glycerol formulations in the recommended doses of the drug.

Since glucocorticosteroids penetrate into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Dosing and Administration:

The dose of the drug and the duration of treatment is determined by the physician individually depending on the indications and severity of the disease.

Intravenously (intravenously) or intramuscularly (in / m) - 460 mg per day.

In / in, with shock - 30-90 (up to 150-300) mg. If the IV infusion is difficult, you can in / m, deep (a slower absorption). If necessary, repeated administration of 30-60 mg IV or IM is possible. If a history of psychosis, do not prescribe large doses.

Children from 2 to 12 months - 2-3 mg / kg, from 1 to 14 years - 1-2 mg / kg IM; in / in is injected slowly (within 3 min). If necessary, this dose can be repeated after 20-30 minutes.

Children are considered particularly at risk for growth retardation (see sections "Special instructions" and "Side effects"). The dose should be reduced gradually to the lowest dose, which will ensure the maintenance of a satisfactory clinical response to treatment and a minimum of adverse effects.

After relief of acute condition, Prednisolone Nycomed is prescribed inside tablets, followed by a gradual decrease in dose.

With prolonged use of the drug, the daily dose should be reduced gradually. Long-term therapy can not be stopped suddenly!

The preparation is a ready-made solution. Do not dilute it in any infusion and injection solutions!

Instructions for the use of ampoules with a break point:

1. Place the tip of the ampoule point to the top. Gently tapping your finger and shaking the ampoule, letting the solution from the tip of the ampoule drain down.

2. Position the tip of the ampoule point to the top. Break the tip down.

Side effects:

The frequency of development and the severity of unwanted adverse reactions (NDP) depends on the duration of application, the amount of dose used and the possibility of observing the circadian rhythm of prednisolone.

Classification of CPD by frequency of development: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000); frequency is unknown (can not be estimated from available data).

When applying Prednisolone may be noted:

Disorders from the endocrine system

Very often: withdrawal syndrome due to adrenocortical insufficiency (headache, pain, nausea, dizziness, anorexia, weakness, changes in emotional state, apathy and inadequate response to stressful situations (see section "Special instructions")), "steroid" sugar diabetes with a low sensitivity to insulin, an increase in blood glucose in patients already suffering from diabetes; growth retardation in children due to impaired growth hormone secretion and decreased sensitivity to growth hormone.

Often: hypokalemia due to mineralocorticoid effect, amenorrhea in women of childbearing age, decreased or increased appetite, weight gain.

Rarely: changes in thyroid function.

Very rarely: ketoacidosis and hyperosmolar coma, manifestation of latent hyperparathyroidism, acceleration of porphyria development, tumor lysis syndrome (see section "Special instructions").

The frequency is unknown: increased excretion of calcium, hypocalcemia, negative nitrogen balance (increased protein breakdown), insufficiency of the adrenal cortex (starting with inhibition of the hypothalamus and ending with a true atrophy of the adrenal cortex) (see below).(See "Special instructions"), Itenko-Cushing syndrome (lunar face, pituitary obesity, hirsutism, increased blood pressure, dysmenorrhea, muscle weakness, striae) (see "Special instructions"), increased concentration of cholesterol, triglycerides and lipoproteins, violation of glucose tolerance.

Disorders from the gastrointestinal tract

Often: Candidiasis of the oral mucosa; risk of perforation of the organs of the gastrointestinal tract in colitis, ileitis, diverticulitis.

Infrequently: peptic ulcers in patients treated with acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (NSAIDs), gastrointestinal bleeding (0.5%).

Very rarely: pancreatitis after long-term treatment with high doses.

The frequency is unknown: nausea, vomiting, flatulence, hiccough.

Disorders from the cardiovascular system

Often: arterial hypertension (due to sodium retention, which leads to fluid retention), aggravation of chronic heart failure (as a result of sodium retention).

Very rarely: cardiomyopathy with an increased risk of decreasing the minute volume of the heart, arrhythmia due to hypokalemia, acute cardiovascular failure (see section "Special instructions").

The frequency is unknown: bradycardia (right up to cardiac arrest). In patients with acute and subacute myocardial infarction - the proliferation of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

Disorders of the psyche

Often: euphoria, depression, "steroid" psychosis.

Infrequently: insomnia, mood swings, personality changes, manic syndrome (see section "Special instructions") and hallucinations.

Disturbances from the nervous system

Rarely: a violation of cognitive functions (eg, weakening memory), epidural lipomatosis.

Very rarely: manifestation of latent epilepsy, pseudotumor of the brain (benign intracranial hypertension with symptoms such as headache, blurred vision and visual impairment).

The frequency is unknown: delirium, disorientation, paranoia, increased intracranial pressure, nervousness or anxiety, dizziness, vertigo, convulsions.

Disturbances on the part of the organ of sight

Very rarely: chorioretinopathy.

The frequency is unknown: the propensity to develop secondary bacterial, fungal or viral infections of the eyes, trophic changes in the cornea, increased intraocular pressure, posterior subcapsular cataract, glaucoma, exophthalmos.

Disturbances from musculoskeletal and connective tissue

Very often: myopathy (10%) when treated with high doses.

Infrequent: avascular aseptic necrosis of bone tissue.

Very rarely: tendonopathies, especially the Achilles tendon and tendons of the quadriceps femoris (see section "Interaction").

The frequency is unknown: osteoporosis with associated symptoms such as back pain, decreased mobility, acute pain, compression fractures of the vertebrae and decreased vertebrae height, fractures of long bones (see section "Special instructions"), pathological bone fractures, aseptic necrosis of the head of the shoulder and femoral bone, decreased muscle mass (atrophy).

Disturbances from the skin and subcutaneous tissues

Often: fungal infections that affect the skin and mucous membranes, striae, acne, ecchymosis (ecchymosis) and petechiae, dermatitis, ecchymosis, facial erythema, atrophy, hirsutism, wound healing, increased sweating, telangiectasia and thinning of the skin.

Very rarely: epidermal necrolysis, Stevens-Johnson syndrome.

Frequency unknown: hyper or hypopigmentation.

Immune system disorders

Very often: an immunosuppressive and anti-inflammatory effect, leading to masking or exacerbation of the existing disease (see section "Special instructions"). Infrequently: allergic reactions (skin rash, itching, local allergic reactions).

The frequency is unknown: anaphylactic shock.

Infectious and parasitic diseases

Very often: increased susceptibility to infection, aggravation of existing infection, activation of latent infection and masking of infection symptoms due to immunosuppressive and anti-inflammatory effect of prednisolone (see section "Special instructions").

Violations of the blood and lymphatic system

Very often: a decrease in the number of eosinophils and lymphocytes.

Often: increase in the number of leukocytes and platelets.

Rarely: the risk of thrombosis due to increased blood coagulability.

Disturbances from the respiratory system, chest and mediastinal organs

Very often: lung abscess in patients with lung cancer (12%).

Often: increased risk of developing tuberculosis.

Infrequent: myopathy, affecting the respiratory muscles.

Violation of the kidneys and urinary tract

Often: nocturnal polyuria.

Infrequent: the formation of urinary stones due to increased excretion of calcium and phosphate.

Frequency unknown: leukocyturia.

Laboratory and instrumental data

Rarely: increased activity of "liver" transaminases and alkaline phosphatase.

General disorders and disorders at the site of administration

The frequency is unknown: burning, numbness, pain, tingling at the injection site, infections at the injection site, necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue with intramuscular injection (especially dangerous introduction to the deltoid muscle), with intravenous injection: "hot flashes".

Overdose:

It is possible to increase dose-dependent side effects. It is necessary to reduce the dose of Prednisolon Nycomed. Treatment is symptomatic.

Interaction:

Possible pharmaceutical incompatibility of prednisolone with other intravenously administered drugs - it is recommended to inject it separately from other drugs (intravenously bolus, or through another dropper, as a second solution). When mixing the solution of prednisolone with heparin a precipitate forms.

The simultaneous use of prednisolone with:

inducers of microsomal liver enzymes (barbiturates, phenytoin, theophylline, rifampicin, ephedrine) leads to a decrease in its concentration;
diuretics (especially "thiazide" and inhibitors carbonic anhydrase) and amphotericin B - can lead to increased excretion from the body of potassium and an increased risk of developing heart failure;
inhibitors of carbonic anhydrase and "loop" diuretics may increase the risk of osteoporosis;
fluoroquinolones - increased risk of rupture of tendons;
sodium-containing drugs - to the development of edema and increased blood pressure;
cardiac glycosides - increases the toxicity of cardiac glycosides (due to occurring hypokalemia increases the risk of arrhythmias);
indirect anticoagulants - weakens (less intensifies) their effect (dose adjustment is required);
anticoagulants and thrombolytics - increased risk of bleeding from ulcers in the gastrointestinal tract;
ethanol and non-steroidal anti-inflammatory drugs (NSAIDs) - increased risk of erosive and ulcerative lesions in the gastrointestinal tract and development of bleeding (in combination with NSAIDs in the treatment of arthritis may reduce the dose of glucocorticosteroids due to the summation of the therapeutic effect);
indomethacin - increased risk of side effects of prednisolone (displacement by indomethacin of prednisolone from bond with albumins);
paracetamol - increased risk of hepatotoxicity (induction of microsomal liver enzymes and the formation of a toxic metabolite of paracetamol);
acetylsalicylic acid - accelerates its excretion and reduces the concentration in the blood (With the withdrawal of prednisolone, the level of salicylates in the blood increases and the risk of side effects increases), increases the risk of gastrointestinal bleeding and ulceration;
insulin and oral hypoglycemic drugs, antihypertensive drugs - their effectiveness decreases;
vitamin D - its effect on the absorption of calcium ions (Ca²⁺) in the intestine;
a somatotropic hormone - It reduces the effectiveness of the latter, and with praziquantel - its concentration;
M-holinoblokatorami (including antihistamines and tricyclic antidepressants) and nitrates - promotes increased intraocular pressure;
neuromuscular blocking (for example, pancuronium bromide) - lowering the effectiveness of blocking neuromuscular transmission; increased risk of myopathy with prolonged simultaneous application;
isoniazid and mexiletine - increases their metabolism (especially in "slow" acetylators), which leads to a decrease in their plasma concentrations;
quetiapine - a decrease in the concentration of quetiapine in the blood serum;
methotrexate, licorice preparations - increases the risk of side effects of prednisolone.

Corticotropin strengthens the action of prednisolone.

Ergocalciferol and parathyroid hormone prevent the development of osteopathy, caused by prednisolone.

Cyclosporine and ketoconazole, slowing the metabolism of prednisolone, can in some cases increase its toxicity.

Simultaneous application androgen and steroid anabolic drugs with prednisolone promotes the development of peripheral edema and hirsutism, the appearance of acne.

Estrogens and oral estrogen-containing contraceptives reduce the metabolism of prednisolone in the liver, which increases the risk of side effects of glucocorticosteroids.

Mitotan and other inhibitors of adrenal cortex function may necessitate an increase in the dose of prednisolone.

With simultaneous application with live antiviral vaccines and against the background of other types of immunizations increases the risk of virus activation and the development of infections.

Immunosuppressive drugs increase the risk of infection and lymphoma or other lymphoproliferative disorders associated with the Epstein-Barr virus.

Antipsychotic drugs (antipsychotics) and azathioprine increase the risk of developing cataracts in the appointment of prednisolone.

When used simultaneously with antithyroid drugs decreases, and with thyroid hormones - The clearance of prednisolone rises.

Special instructions:

During treatment with Prednisolon Nycomed (especially prolonged), an ophthalmologist should be monitored, blood pressure monitored, water electrolyte balance status, and peripheral blood and blood glucose levels monitored. Patients should be observed in order to detect suppression of the hypothalamic-pituitary-adrenal system (GTI) (insufficiency of the adrenal cortex), Itenko-Cushing syndrome, hyperglycemia and glucosuria.

In order to reduce side effects, it is possible to prescribe antacids, and also to increase the intake of potassium in the body (diet, potassium preparations). Food should be rich in proteins, vitamins, with a restriction of fat, carbohydrates and table salt.

The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug may enhance existing emotional instability or psychotic disorders. When referring to a psychosis in an anamnesis, prednisolone Nycomed in high doses is prescribed under the strict supervision of a doctor.

With caution should be used in acute and subacute myocardial infarction - possibly spreading the focus of necrosis, slowing the formation of scar tissue and rupture of the heart muscle.

In stressful situations during maintenance treatment (for example, surgical operations, trauma or infectious diseases), a correction of the dose of the drug should be made in connection with an increase in the need for glucocorticosteroids.

One should carefully monitor the patient within a year after the end of long-term therapy with Prednisolon Nycomed in connection with the possible development of a relative insufficiency of the adrenal cortex in stressful situations.

In case of sudden cancellation, especially in case of prior application of high doses, it is possible to develop a withdrawal syndrome (anorexia, nausea, inhibition, generalized musculoskeletal pain, general weakness), as well as an exacerbation of the disease, in which Prednisolon Nycomed was appointed.

During treatment with Prednisolone, Nycomed should not be vaccinated due to a decrease in her effectiveness (immune response).

When prescribing Prednisolone Nycomed with intercurrent infections, septic conditions and tuberculosis, antimicrobial treatment should be concurrently administered.

Prednisolone should be administered with caution in any known infectious disease or suspected of it (see Adverse Effect). Patients during treatment should avoid contact with patients with viral infections and immediately consult a doctor in case of contact with them.

At children during long treatment Prednisolonum Nycomed it is necessary careful monitoring of the dynamics of growth and development.

Due to a weak mineralocorticoid effect for replacement therapy with adrenal insufficiency Prednisolone Nycomed is used in combination with mineralocorticoids.

Prednisolone enhances gluconeogenesis. Approximately 20% of patients receiving treatment with high doses of glucocorticosteroids develop benign "steroid" diabetes mellitus with low sensitivity to insulin and a low renal threshold for glucose.The condition is reversible upon cancellation of therapy. Patients with diabetes should monitor blood glucose and, if necessary, correct therapy.

Prolonged treatment with prednisolone affects the metabolism of calcium and phosphate and increases the risk of osteoporosis. The loss of bone tissue, induced by glucocorticosteroids, can prevent the appointment of calcium and vitamin D₃. An x-ray control of the osteoarticular system is shown (photos of the spine, brushes).

Prednisolone Nycomed in patients with latent infectious diseases of the kidneys and urinary tract can cause leukocyturia, which can be of diagnostic significance.

Prednisolone Nycomed increases the metabolites of 11- and 17-oxyketocorticosteroids.

During immunosuppressive therapy with glucocorticosteroids, vaccination with live viral or bacterial vaccines is counter-indicative. A reduced immune response may allow a live attenuated vaccine to cause an infectious disease.

Effect on the ability to drive transp. cf. and fur:

During treatment, patients are advised to exercise caution when driving vehicles and taking other potentially hazardousActivities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular administration, 25 mg / ml.

Packaging:

1 ml is placed in colorless glass ampoules (type I, Eur.pharm.) With a break point.

3 ampoules per plastic contour mesh package. One contour pack with instructions for use is placed in a cardboard box.

5 ampoules per plastic contour mesh package. 5 contour packs with instructions for use are placed in a cardboard box.

10 ampoules per plastic contour mesh package. 5 contour packs with instructions for use are placed in a cardboard box.

Storage conditions:

In the dark place at a temperature of 18-25 ° C.

Even temporary storage of Prednisolone Nycomed in unsuitable conditions (for example, below 15 ° C) can lead to the formation of single crystals of prednisolone.

Do not use a solution containing crystals!

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015850 / 01

Date of registration:28.05.2009 / 17.06.2014

Expiration Date:Unlimited

Date of cancellation:2017-03-20

The owner of the registration certificate:Takeda Austria GmbHTakeda Austria GmbH Austria

Manufacturer: & nbsp

TAKEDA AUSTRIA GmbH Austria

Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.

Information update date: & nbsp22.03.2017

Illustrated instructions

Instructions

Prednisolone Nycomed (Prednisolon Nycomed)