Ivefore - instructions for use, doses, side effects, contraindications

Pharmacodynamics:Synthetic glucocorticosteroid drug (GCS). Dehydrogenated analog hydrocortisone. Has anti-inflammatory, anti-allergic, anti-shock and immunosuppressive action. Interacts with specific cytoplasmic receptors and forms a complex penetrating into the nucleus of the cell and stimulating the synthesis of mRNA; the latter induces the formation of proteins, incl. lipocortin, mediating cellular effects. Lipocortin depresses the phospholipase A2, suppresses the liberation of arachidonic acid and inhibits the biosynthesis of endoperoxides, prostaglandins, leukotrienes, contributing to inflammation processes, allergies, etc. The anti-inflammatory effect is associated with the inhibition of eosinophil release 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 and membranes of organelles (especially lysosomal).

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

The antiallergic effect is caused by a decrease in the number of circulating eosinophils, which leads to a decrease in the release of mediators of immediate allergy; reduces the effect of mediators of allergy on effector cells.

Immunodepressive effect is due to inhibition of the release of cytokines (interleukin-1,2, gamma-interferon) from lymphocytes and macrophages. Protein metabolism: reduces the amount of protein in the plasma (due to globulins) with an increase in the albumin / globulin ratio, increases the synthesis of albumins in the liver and kidneys; enhances protein catabolism in muscle tissue.

Lipid metabolism: increases synthesis of higher fatty acids and triglycerides, redistributes fat (accumulation of fat 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-phosphatase, leading to an increase in the intake of glucose from the liver into the blood; increases the activity of phosphoenolpyruvate carboxylase and the synthesis of aminotransferases leading to the activation of gluconeogenesis.

Water-electrolytic exchange: retards sodium (Na+) and water in the body, stimulates the excretion of potassium (K +) (mineralocorticoid activity), reduces the absorption of calcium

(Ca²⁺ ) from the gastrointestinal tract, shows antagonistic action in relation to vitamin D: "washing away" calcium from bones and increasing its renal excretion.

Suppresses the synthesis and secretion of ACTH and, again, the synthesis of endogenous GCS.

Pharmacokinetics:Methylprednisolone sodium succinate is well soluble in water, well absorbed and has a quick and lasting effect. After intramuscular injection, the absorption is complete and fast enough. Bioavailability with intramuscular injection - 89%. Binding to plasma proteins is about 62%. The maximum concentration of methylprednisolone in the blood plasma (about 20 μg / ml) is reached about 15 minutes after IV injection 30 mg / kg body weight for 20 minutes, or 1 g for 30-60 minutes. After a / m introduction of 40 mg after 2 hours, the maximum concentration of methylprednisolone in the blood plasma is equal to 34 μg / 100 ml. The half-life of plasma is approximately 2.3-4 hours, the duration of action is 12-36 hours. After the / m administration, the drug is present in the blood plasma for a longer period than after intravenous administration, if an equivalent amount of methylprednisolone is administered.Taking into account the mechanism of action of glucocorticosteroids, it can be considered that these differences are of minimal clinical significance.

Metabolized, mainly in the liver. Its metabolites (keto- and hydroxy compounds) are hormonally inactive and are excreted mainly by the kidneys. About 85% of the administered dose is excreted within 24 hours by the kidneys and about 10% by the intestine.

Indications:

- Endocrine disorders - acute failure of the adrenal cortex.

- Rheumatic diseases: acute rheumatism; Collagenosis - with exacerbation or maintenance therapy with systemic lupus erythematosus.

- Dermatological diseases - pemphigus, severe erythema multiforme, exfoliative dermatitis, diffuse neurodermatitis, severe psoriasis, severe seborrheic dermatitis.

- Bronchial asthma, asthmatic status.

- Allergic diseases - severe or resistant to standard therapy: atopic dermatitis, serum sickness, hypersensitivity to medicines, laryngeal edema, urticaria, anaphylactic shock.

- Diseases of the gastrointestinal tract - an acute stage of ulcerative colitis.

- Edema of the brain - to treat cerebral edema caused by brain tumors, head injuries, craniocerebral operations.

- Organ transplantation - to prevent the reaction of rejection of the transplanted organ.

- Severe shock (hemorrhagic, traumatic, septic) resistant to standard therapy.

- Reduction of inflammatory phenomena and prevention of cicatricial narrowing during poisoning with cauterizing fluids.

- Hematological diseases - acquired autoimmune hemolytic anemia, congenital hypoplastic anemia, erythroblastopenia, idiopathic thrombocytopenic purpura in adults, secondary thrombocytopenia in adults.

- For palliative treatment of tumorous diseases, including acute or chronic leukemia and lymphoma in adults, acute leukemia in children.

Contraindications:For short-term use according to vital indications, the only contraindication is hypersensitivity to the Ivepred. It is not recommended to use the drug in patients with acute and subacute myocardial infarction, as the use of glucocorticosteroids in them can lead to the spread of a necrosis,slowing the formation of scar tissue and, as a result, to the rupture of the heart muscle.

This preparation contains benzyl alcohol. It is established that benzyl alcohol can cause a "suffocation syndrome" with a fatal outcome in premature newborns. The drug is not recommended for use in newborns.

Carefully:

Precautions should be used when the drug immunodeficiency (including AIDS or HIV), diseases of the cardiovascular system (including recent myocardial infarction, severe chronic cardiac insufficiency, arterial hypertension), severe chronic renal failure and liver failure, urolithiasis, recently established intestinal anastomosis, gastric ulcer and duodenal ulcer, ulcerative colitis, with the threat of perforation, diverticulitis, esophagitis, gastritis , Peptic ulcer, diabetes (including predisposition), and parasitic infectious diseases of viral, fungal or bacterial origin (currently or recently transferred, and including the recent contact with the patient); closed-angle glaucoma, hyperlipidemia, hyperthyroidism,hypothyroidism, Cushing's disease, hypoalbuminemia or conditions predisposing to its occurrence (cirrhosis, nephrotic syndrome), myasthenia gravis, osteoporosis, acute psychosis, obesity (III-IV st).

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

Pregnancy and lactation:When pregnancy (especially in the first trimester) is used for life indications. Since glucocorticosteroids pass into breast milk, if it is necessary to use the drug during breastfeeding, it is recommended to stop breastfeeding.

Dosing and Administration:

The drug is used intravenously (jet or drip) or intramuscularly.

The dose of the drug and the duration of treatment are determined by the attending physician, depending on the severity of the disease and the tolerability of the treatment.

In acute adrenocortical insufficiency, a single dose of the drug is 100-200 mg, daily 300-400 mg.

In severe allergic reactions, Ivered is administered in a daily dose of 100-200 mg for 3-16 days.

In bronchial asthma, the drug is administered depending on the severity of the disease andefficiency of complex treatment from 75 to 675 mg for a course of treatment from 3 to 16 days; in severe cases, the dose may be increased to 1,400 mg per treatment course and more with a gradual dose reduction.

With asthmatic status, Ivered is administered at a dose of 500-1200 mg per day, followed by a decrease to 300 mg per day and a transition to maintenance doses.

In the case of shock resistant to standard therapy, Ivefore, at the beginning of therapy, is usually injected intravenously and then switched to intravenous drip. If the arterial pressure does not increase within 10-20 minutes, repeat the fluid administration of the drug. After excretion from the shock state, intravenous drip administration is continued until blood pressure stabilizes. Single dose is 50-150 mg (in severe cases - up to 400 mg). Repeated drug is administered after 3-4 hours. The daily dose can be 300-1200 mg (with a subsequent dose reduction).

When immunosuppression - to prevent the reaction of rejection of the transplanted organ (especially the kidneys) during transplantations - Ivered is used in doses of 0.5 g to 2 g intravenously every 24-48 hours.

With edema of the brain - 40-125 mg every 4-6 hours intravenously or intramuscularly for 4-7 days (until the patient's condition is stabilized).

With rheumatoid arthritis and systemic lupus erythematosus, Ivered is administered in addition to the systemic administration of the drug at a dose of 75-125 mg per day for not more than 7-10 days. When poisoning with cauterizing liquids with burns of the digestive tract and upper respiratory tract is prescribed in a dose of 75-400 mg per day for 3-18 days. Ivepred is used as an additional therapy for patients with ulcerative colitis, with doses of 20 mg to 40 mg administered intravenously drip 3-7 times a week for 2 or more weeks.

In other conditions, the initial dose may vary from 10 mg to 40 mg, depending on the clinical picture. Large doses are usually applied for a short period of time. Children are prescribed in a dose of 0.8-1.5 mg / kg of body weight per day.

With the impossibility of intravenous administration, Ivered is administered intramuscularly in the same doses. Dose reduction and discontinuation of drug treatment should always be done gradually.

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

These doses must always be strictly individual. The drug should not be mixed with other drugs in the same syringe.

Preparation of injection solution: the solvent is added to the lyophilizate in the ampoule and the resulting solution is mixed with a different amount of the infusion solution-5% dextrose, isotonic saline or 5% dextrose in isotonic saline.

Side effects:

The frequency of development and severity of side effects depends on the duration of application, the amount of dose used, and the possibility of observing the circadian rhythm of the appointment of Iwepred.

When applying the Yvespred, the following may be noted:

From the endocrine system: depression of glucose tolerance, steroid diabetes mellitus or manifestation of latent diabetes mellitus, acne, suppression of adrenal function, Itenko-Cushing syndrome (lunar face, obesity of the pituitary type, hirsutism, increased blood pressure, dysmenorrhea, amenorrhea, muscle weakness, striae), delay in sexual development in children.

From the digestive system: nausea, vomiting, pancreatitis, steroid ulcer of the stomach and duodenum, erosive esophagitis, bleeding and perforation of the digestive tract, increased or decreased appetite, digestive disorders, flatulence, hiccups.

From the cardiovascular system: arrhythmias, bradycardia, cardiac arrest; exacerbation of phenomena or development of heart failure (in predisposed patients), ECG - changes characteristic of hypokalemia, increased blood pressure, hypercoagulation, thrombosis; in patients with acute and subacute myocardial infarction - the spread of the focus of necrosis, slowing the formation of scar tissue, which can lead to rupture of the heart muscle.

From the nervous system: delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, paranoia, increased intracranial pressure, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, headache.

From the side of the organ of vision: sudden loss of vision (with parenteral administration in the head, neck, nasal concha, scalp may precipitate crystals of the drug in the vessels of the eye), posterior subcapsular cataracts, increased intraocular pressure with possible damage to the optic nerve, propensity to develop secondary bacterial, fungal or viral infections eye, trophic changes of the cornea, exophthalmos.

From the side of metabolism: fluid retention and sodium (edema), hypernatremia, hypokalemic syndrome (hypokalemia, arrhythmia, myalgia or muscle spasm, unusual weakness), increased calcium excretion, hypocalcemia, weight gain, negative nitrogen balance (increased protein breakdown), increased sweating.

From the musculoskeletal system: slowing the growth and processes of ossification in children (premature closure of epiphyseal growth zones), osteoporosis (very rarely - pathological bone fractures, aseptic necrosis of bones), steroid myopathy, rupture of muscle tendons, reduction of muscle mass.

From the skin and mucous membranes: deterioration of wound healing, ecchymosis, thinning of the skin, hyper or hypopigmentation, steroid acne, a tendency to develop pyoderma and candidiasis.

Allergic reactions: generalized (skin rash, itching, anaphylactic shock), local allergic reactions.

Local for parenteral administration: burning, numbness, pain, tingling at the injection site, infections at the injection site, rarely - necrosis of surrounding tissues, scar formation at the injection site; atrophy of the skin and subcutaneous tissue with the / m introduction(especially dangerous is the introduction to the deltoid muscle).

Other: exacerbation of infections, increased activity of renin-angiotensin-

aldosterone system, withdrawal syndrome.

With IV introduction: arrhythmias, "tides" of blood to the face, seizures.

Overdose:It is possible to strengthen the above described side effects. It is necessary to reduce the dose of Iweprad. Treatment simtomatic.

Interaction:

Simultaneous use with phenobarbital, rifampicin, phenytoin or ephedrine leads to a weakening of the effect of the Iweprad.

Simultaneous use with diuretics (especially "loop") can lead to increased excretion of potassium from the body.

With a simultaneous appointment with cardiac glycosides, their tolerability worsens and the possibility of cardiac rhythm disturbance increases (due to hypokalemia caused).

Ivefore weakens (less intensifies) the effect of the coumarin derivatives, which requires correction of their dose.

Ivefore exacerbates the side effects of non-steroidal anti-inflammatory drugs (NSAIDs), especially their effect on the gastrointestinal tract (increased risk of erosive ulcerative lesions and bleeding from the gastrointestinal tract); reduces the concentration of NSAIDs in the serum, thereby reducing their effectiveness.

Carbonic anhydrase inhibitors: increase the risk of hypokalemia, osteoporosis.

�?вепред reduces the effectiveness of insulin and oral hypoglycemic drugs, antihypertensive drugs.

Ivepred reduces the concentration of praziquantel.

In combination with paracetamol leads to an increased risk of hepatotoxicity, due to the induction of hepatic enzymes and the formation of a toxic metabolite of paracetamol.

Simultaneous use of androgens, anabolic steroids contributes to the appearance of peripheral edema, hirsutism and acne; estrogens, oral contraceptives - leads to a decrease in clearance and increased action of Yvespeed, an increase in its toxic effects.

The risk of developing cataracts increases when applied against the background of Iwepred, antipsychotics (neuroleptics) and azathioprine.

Simultaneous administration with drugs with m-holinoblokiruyuschim action (including antihistamines, tricyclic antidepressants) and nitrates contribute to the development of glaucoma.

With simultaneous use with amphotericin B, the risk of developing heart failure increases.

In combination with anti-coagulants and thrombolytics, the risk of ulcers of the gastrointestinal tract and bleeding increases.

�?вепред increases the metabolism of mexiletine, reducing its concentration in the plasma. With simultaneous use with live antiviral vaccines and against other types of immunizations, increases the risk of virus activation and the development of infections. Sodium-containing drugs or supplements increase the likelihood of peripheral edema and increased blood pressure.

Special instructions:

Before starting treatment, the patient should be examined for possible contraindications. Clinical examination should include examination of the cardiovascular system, radiology examination of the lungs, examination of the stomach and duodenum, urinary system, vision organs; the control of the general analysis of a blood, a level of a glycemia, the maintenance of electrolytes in a plasma. The effect of the drug is enhanced in patients with hypothyroidism and liver cirrhosis. The drug can enhance existing emotional instability, mental disorders or psychosis. When referring to a psychosis in an anamnesis, Ivepren in high doses is prescribed under the strict supervision of a doctor.

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. It should be carefully monitored for patients within a year after the end of the long-term therapy of Iweprad 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, there may be a syndrome of "cancellation" (not caused by hypocorticism: anorexia, nausea, blocking, generalized musculoskeletal pain, general weakness); adrenal insufficiency; as well as the aggravation of the disease, in connection with which Ivered was appointed.

During the treatment of Yvepreda, vaccination should not be given due to a decrease in its effectiveness and possible neurological complications.

When prescribing Ivered for intercurrent infections, septic conditions and tuberculosis, it is necessary to simultaneously perform antibiotic treatment with bactericidal action.

Children during prolonged treatment need careful monitoring of the dynamics of growth and development. Children who were in contact with sick measles or chickenpox during the treatment period prophylactically prescribe specific immunoglobulins.

During treatment with Ivecred (especially long), it is necessary to observe the oculist, control blood pressure and water-electrolyte balance, as well as pictures of peripheral blood and glycemia. Food should be rich in potassium, proteins, vitamins, containing a small amount of fats, carbohydrates and salt.

Effect on the ability to drive transp. cf. and fur:During therapy, it is necessary to refrain from engaging in potentially dangerous activities that require increased attention, speed of motor and mental reactions (including from driving a car or controlling machinery).

Form release / dosage:

Lyophilizate for the preparation of a solution for intravenous and intramuscular administration, 500 mg and 1000 mg complete with a solvent (0.9% benzyl alcohol).

Packaging:

Lyophilizate for the preparation of a solution for intravenous and intramuscular administration, 500 mg and 1000 mg complete with a solvent (0.9% benzyl alcohol).

500 mg

Vial with preparation: 500 mg of methylprednisolone in a colorless glass vial of 20 ml of glass type I, sealed with a bromo-butyl plug of gray color and covered with an aluminum cap with a detachable polypropylene orange lid.

Ampoule with solvent: 4 ml of solvent in a colorless glass ampoule of 5 ml of glass type I, with a dark maroon band and a blue dot.

Ivefore 1000 mg

Vial with the drug: per 1000 mg of methylprednisolone in a colorless glass vial of 20 ml of type I glass, sealed with a bromo-butyl plug of gray color and covered with an aluminum cap with a detachable polypropylene lid of burgundy color.

Ampoule with solvent: 8 ml of solvent in a colorless glass ampoule of 10 ml of glass type I, with a violet stripe and a blue dot.

For 1 bottle with the drug and 1 ampoule with a solvent in one plastic pallet. One tray in a cardboard box with instructions for use.

Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years.

Terms of leave from pharmacies:On prescription

Registration number:LP-002113

Date of registration:28.06.2013

Expiration Date:28.06.2018

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Sun Pharmaceutical Industries, Ltd. India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp16.12.2016

Illustrated instructions

Instructions

And (Ivepred)