Ibuprofen-Darnitsa

General characteristics. Structure:

Active ingredient: 1 tablet contains 200 mg of an ibuprofen (in terms of 100% dry matter);

excipients: cellulose microcrystallic, sodium of a kroskarmeloz, silicon dioxide colloid anhydrous, starch corn, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Non-steroidal anti-inflammatory drug with anesthetic, antiinflammatory and febrifugal actions. The mechanism of action of an ibuprofen is caused by braking of biosynthesis of prostaglandins by non-selective inhibition of TsOG-1 and TsOG-2, and also reduction of formation of other mediators of pain and an inflammation. Reversibly inhibits aggregation of thrombocytes.

Pharmacokinetics. At intake the ibuprofen is quickly and completely adsorbed. Bioavailability makes 80%. Contacts proteins of a blood plasma for 99%. The concomitant use of food umenyyoshat absorption speed. Time of achievement of the maximum concentration in blood (Tmax) makes 45-90 minutes. Slowly gets into a joint cavity, being late in synovial fabric and creating in it big concentration, than in plasma. The elimination half-life (T1/2) makes about 2 hours. The general clearance – 0,75 ml/(min.). Distribution volume – 0,15 l/kg. At elderly people (65 years are more senior) the elimination half-life of drug increases, the general clearance decreases. The ibuprofen is metabolized in a liver by oxidation with formation of inactive oxyforms. Removal of an ibuprofen is carried out generally by kidneys,

including 50-60% of the entered dose – in the form of the conjugated metabolites, less than 10% – in not changed look and in the form of inactive oxyforms. The insignificant quantity is distinguished with bile.

The analgesic effect after single use of drug remains within 8 hours.

Pharmaceutical characteristics.

Main physical and chemical properties:

tablets of white or almost white color, round form, with a biconvex surface. On a surface of a tablet the mramornost is allowed.

Indications to use:

Headache, dentagra, migraine, dysmenorrhea, neuralgia, dorsodynia, joints, muscles, rheumatic pain, and also feverish conditions and symptoms of cold and flu.

Route of administration and doses:

The mode of dosing is set individually taking into account intensity of a pain syndrome. To adults and children 12 years usually are more senior appoint 1-2 tablets (200-400 mg of an ibuprofen) 3-4 times a day after food. The recommended initial dose makes 2 tablets (400 mg of an ibuprofen). The highest daily dose – 1200 mg. Drug is intended for symptomatic stopping of a pain syndrome, but if symptoms of a disease remain more than 3 days, are followed by high temperature, a headache or other phenomena, it is necessary to specify the diagnosis and in addition to correct the scheme of treatment.

Features of use:

It is necessary to be careful at purpose of drug the patient suffering gastyority, enteritis, colitis, chronic hepatitis, chronic heart failure. At patients with a renal failure treatment should be carried out with care and in the minimum dose under constant control of functional renal tests.

Side effects can be reduced by incontinuous use of a minimal effective dose necessary (sufficient) for treatment of symptoms.

Influence on cardiovascular and cerebrovascular system. Use of an ibuprofen, especially in high doses (1200 mg daily), and also can lead its prolonged use to slight increase of risk of emergence of arterial trombotichesky complications (for example, a myocardial infarction or a stroke). In general data of epidemiological researches do not demonstrate that the low dose of an ibuprofen can lead to increase in risk of development of a myocardial infarction.

The bronchospasm can arise at patients who have allergic diseases now and/or had a bronchospasm in the anamnesis.

People of advanced age are in the field of the increased risk of emergence of serious effects owing to development of side effects.

System lupus erythematosus and general diseases of connecting fabric – the increased risk of emergence of aseptic meningitis.

Symptoms of increase in arterial pressure and/or heart failure in connection with a heavy abnormal liver function can worsen and/or there can be a liquid delay.

There are not enough proofs that medicines which inhibit synthesis of cyclooxygenases/prostaglandins can cause deterioration in reproductive function in women by means of influence on process of an ovulation. This phenomenon at the termination of treatment is reversible.

At use of all non-steroidal anti-inflammatory drugs there can be bleedings in a digestive tract, an ulcer or perforation which can lead to death during all treatment, at existence or lack of symptoms of deterioration or serious cardiovascular events in the anamnesis.

Patients at whom gastrointestinal frustration were observed and also people of advanced age have to report about any unusual abdominal symptoms (especially about bleedings from digestive tract) in an initiation of treatment.

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

Taking into account possible side effect drug is carefully appointed to the drivers of motor transport and persons who are engaged in potentially dangerous types of activity.

Side effects:

At use of drug development of side reactions from the following systems and bodies is possible:

from the central nervous system and peripheral nervous system: headache, dizziness, sleeplessness, excitement, irritability, disorientation, feeling of strong fatigue, aseptic meningitis;

from sense bodys: vision disorder, sonitus;

from digestive tract: an abdominal pain, dyspepsia, heartburn, nausea, vomiting, anorexia, a meteorism, diarrhea, a lock, a round ulcer, perforation and hemorrhage in digestive tract, a melena, vomiting blood, cankers of an oral cavity, an exacerbation of ulcer colitis and disease Krone;

from a liver and bilious ways: disturbance of functions of a liver, jaundice, hepatitis;

from cardiovascular system: heart failure, stenocardia, hypertensia;

from system of blood: disturbance of a hemogenesis (thrombocytopenia, a granulocytopenia, anemia, hemolitic anemia, aplastic anemia, a leukopenia, a pancytopenia, an agranulocytosis), decrease in level of hemoglobin and a hematocrit, hemorrhage under skin and nasal bleedings;

from system of a respiratory organs: pharyngalgia, asthma, bronchospasm, dispny, goose breathing;

from an urinary system: a renal failure, the papillary necrosis which is characterized increase in level of urea of blood, hypostases of extremities, a liquid delay, increase in arterial pressure;

from skin: itch, various enanthesis. In isolated cases possible development of such serious side reactions as a violent rash, Stephens-Johnson's syndrome, a multiformny erythema, an epidermal necrolysis;

from immune system: hypersensitivity reactions, small tortoiseshell, nape muscle tension;

allergic reactions: skin allergic reactions, bronkhoobstruktivny syndrome, Quincke's edema, exacerbation of asthma, Quincke's disease, face edema, throats and language, tachycardia, arterial hypotension, shock;

from an organism in general: fervescence.

Interaction with other medicines:

Antigipertenzivy means, inhibitors of an angiotensin-converting enzyme – at simultaneous use the anti-hypertensive effect decreases.

Diuretics (furosemide and hypothiazid) – at simultaneous use with an ibuprofen the diuretic effect decreases, natriydiuretichesky activity decreases, nephrotoxicity of NPVS increases.

Cardiac glycosides – at simultaneous use with NPVS the exacerbation of heart failure, reduction in the rate of glomerular filtering and increase in concentration of cardiac glycosides in a blood plasma is possible.

Lithium drugs – at simultaneous use elimination of drugs of lithium decreases and their toxicity and concentration in a blood plasma increases.

The methotrexate – at simultaneous use decreases elimination of a methotrexate and its toxicity and concentration in a blood plasma increases.

Cyclosporine – at simultaneous use with NPVS raises nephrotoxicity.

Mifepristone – use of NPVS is allowed only in 8-12 days after mifepristone cancellation as NPVS reduce effect of mifepristone.

Glucocorticosteroids and other NPVS – at simultaneous use the risk of development of hemorrhages in digestive tract increases.

Anticoagulants – at simultaneous use effect of anticoagulants amplifies.

Anticoagulants of coumarinic type and alcohol – at simultaneous use the risk of emergence of hemorrhagic complications increases.

Analgetics – simultaneous use of two and more NPVS is forbidden.

Antibiotics of a hinolonovy row – NPVS can increase risk of development of the convulsions connected with reception of hinolon.

Caffeine – at simultaneous use amplifies analgeziruyushchy effect of an ibuprofen.

Phenytoinum – at simultaneous use raises concentration of Phenytoinum in a blood plasma.

Zidovudine – there are proofs of increase in risk of emergence of a hemarthrosis and a hematoma at HIV-positive patients who apply the accompanying treatment by a zidovudine and an ibuprofen.

Contraindications:

–  Hypersensitivity to any of drug components, to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;

–  use of drug with the accompanying non-steroidal anti-inflammatory drugs, including specific inhibitors of cyclooxygenase-2;

–  digestive tract erosive cankers in a phase of an aggravation or in the anamnesis, the nonspecific ulcer colitis, bleeding from upper parts of digestive tract or a perforation in the anamnesis connected with the previous treatment by non-steroidal anti-inflammatory drugs;

– heavy abnormal liver functions and kidneys;

– bronchial asthma;

– leukopenia, thrombocytopenia;

– arterial hypertension, heart failure;

–  diseases of an optic nerve, disturbance of color sight;

–   The III trimester of pregnancy, is not recommended to apply an ibuprofen for the first 6 months of pregnancy; feeding period breast;

–  children's age up to 12 years.

Use during pregnancy or feeding by a breast.

Drug is contraindicated in ІІІ a trimester of pregnancy and during feeding by a breast.

In spite of the fact that researches did not prove teratogenic action at animals, it is not recommended to apply an ibuprofen during the first 6 months of pregnancy.

During treatment it is necessary to stop feeding by a breast.

Children.

Drug is appointed to children from 12 years.

Overdose:

Most of patients at overdose by drug had symptoms: nausea, vomiting, a headache, a sonitus, pain in epigastriums, diarrhea, hemorrhages in digestive tract. In cases of more serious poisonings with drug perhaps toxic influence on a nervous system which is shown by drowsiness, block, sudden excitement, a disorientation, convulsions and a coma. Also cases of a renal failure, a liver failure, bradycardia, tachycardia were observed. At a serious poisoning there can be a metabolic acidosis; the raised prothrombin ratio, perhaps, owing to influence on factors of coagulation of the circulating blood is observed.

At patients with asthma the exacerbation of a disease is possible.

Treatment. The termination of administration of drug, a gastric lavage (only for the first hour after reception), reception of absorbent carbon, an artificial diuresis and symptomatic therapy (at gastrointestinal bleeding, unstable arterial pressure), correction of electrolytic balance. In case of developing of convulsions it is necessary to appoint diazepam or lorazepam. Patients with bronchial asthma should appoint bronchodilators.

Storage conditions:

Period of validity. 2 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 5 blister strip packagings in a pack.