Hayrumat

General characteristics. Structure:

Active ingredients: 400 mg of an ibuprofen, 325 mg of paracetamol.

Excipients: cellulose microcrystallic, starch corn, talc, magnesium stearate, silicon dioxide colloid, sodium carboxymethylstarch.

Pharmacological properties:

Pharmacodynamics. The combined drug which effect is caused by effects of the components which are its part. The ibuprofen - NPVP, has analgeziruyushchy, antiinflammatory and febrifugal effect. Oppressing TsOG-1 and TsOG-2, breaks metabolism of arachidonic acid, reduces amount of prostaglandins (mediators of pain, an inflammation and hyper thermal reaction), both in the inflammation center, and in healthy fabrics, suppresses exudative and proliferative phases of an inflammation.

Paracetamol not selectively blocks TsOG, is preferential in TsNS, poorly influences a water salt metabolism and a condition of a mucous membrane of a GIT. Has analgeziruyushchy and febrifugal effect. In the inflamed fabrics of peroxidase neutralize influence of paracetamol on TsOG 1 and 2 that explains low antiinflammatory effect.

Efficiency of a combination is higher, than separate components. Weakens an arthralgia at rest and at the movement, reduces morning constraint and a swelling of joints, promotes increase in volume of movements.

Pharmacokinetics. Ibuprofen. Absorption and distribution. It is well absorbed from a GIT. Absorption slightly decreases at administration of drug after food. Time of achievement of Cmax at reception on an empty stomach - 45 min., at reception after food - 1.5-2.5 h, in synovial fluid - 2-3 h (concentration of an ibuprofen is higher, than in a blood plasma). Linkng with proteins of plasma - 90%.

Metabolism and removal. Is exposed to presistemny and post-system metabolism in a liver. After absorption about 60% pharmacological of an inactive R-form of an ibuprofen are slowly transformed to an active S-form. The isoenzyme of P450 CYP2C9 cytochrome takes part in metabolism of drug.

Has two-phase kinetics of elimination from T1/2 2-2.5 h. It is removed by kidneys (in not changed look no more than 1%) and to a lesser extent - with bile.

Paracetamol. Absorption and distribution. Absorption is high. Time of achievement of Cmax makes 0.5-2 h Cmax in a blood plasma - 5-20 mkg/ml. Linkng with proteins of plasma - 15%. Gets through GEB. Less than 1% from the accepted nursing mother of a dose of paracetamol come to breast milk. Therapeutic effective concentration of paracetamol in plasma is reached at its appointment in a dose of 10-15 mg/kg.

Metabolism and removal. It is metabolized in a liver (90-95%): 80% enter conjugation tests with glucuronic acid and sulfates with formation of inactive metabolites; 17% are exposed to a hydroxylation with formation of 8 active metabolites which conjugate with glutathione with formation of already inactive metabolites. At a lack of glutathione these metabolites can block fermental systems of hepatocytes and cause their necrosis. Also the isoenzyme of P450 CYP2E1 cytochrome participates in metabolism of paracetamol.

T1/2 - 1-4 h. Only 3% in not changed look are removed by kidneys in the form of metabolites.

At elderly patients the clearance of drug decreases and T1/2 increases.

Indications to use:

— a weak and moderate pain syndrome of various origin (head and a dentagra, neuralgia, pain at backbone osteochondrosis, an arthralgia, a mialgiya, a tendovaginitis, a bursitis, pain at traumatic injury of muscles, sheaves, sinews, painful periods, postoperative pains);

— fever at infectious and inflammatory diseases (including diseases of upper respiratory tracts and ENT organs - tonsillitis, pharyngitis, a tracheobronchitis, sinusitis, otitis);

— a joint syndrome (a pseudorheumatism, including juvenile, the osteoarthrosis ankylosing a spondylitis, gouty arthritis).

Route of administration and doses:

Drug should be accepted inside, after food, washing down with water.

The mode of dosing is set individually depending on indications.

At the beginning of therapy appoint on 1 таб. 3 times/days. The maximum single dose — 2 таб., the maximum daily - 6 таб.

At renal failures or a liver the break between receptions has to make not less than 8 h.

Treatment duration without medical control should not exceed 5 days at appointment as anesthetic and 3 days - as an antipyretic.

Features of use:

Use at pregnancy and feeding by a breast. Drug is contraindicated to use at pregnancy and in the period of a lactation.

Use at abnormal liver functions. It is contraindicated at a heavy liver failure. With care it is necessary to use drug at a viral hepatitis, alcoholic damage of a liver, a liver failure, high-quality hyperbilirubinemias (Gilbert's syndrome, the Cudgel Johnson and the Rotor), cirrhosis with portal hypertensia.

At abnormal liver functions the break between receptions has to make not less than 8 h.

Use at renal failures. It is contraindicated at a heavy renal failure. With care it is necessary to use drug at a renal failure, a nephrotic syndrome.

At renal failures the break between receptions has to make not less than 8 h.

Use for children. It is contraindicated to children up to 18 years.

Use for elderly patients. With care it is necessary to use drug at patients of advanced age.

Special instructions. At simultaneous use with anticoagulants of indirect action control of coagulant system of blood is necessary.

At drug use more than 5-7 days it is necessary to control indicators of peripheral blood and a functional condition of a liver.

At emergence of symptoms of the NPVP-gastropathy the careful control including carrying out an ezofagogastroduodenoskopiya, blood test with definition of hemoglobin and a hematocrit, the analysis a calla on the occult blood is shown.

In need of definition of 17 ketosteroids drug should be cancelled for 48 h prior to a research. Paracetamol distorts results of laboratory researches of content of glucose and uric acid in a blood plasma.

It is necessary to avoid simultaneous use of drug with other medicines containing paracetamol and/or NPVS.

During treatment reception of alkogolsoderzhashchy drinks is not recommended.

Influence on ability to driving of motor transport and to control of mechanisms. During use of drug it is necessary to be careful and avoid control of vehicles and occupation potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: the dispeptic phenomena, diarrhea, erosive cankers of a GIT, bleeding from a GIT, an abnormal liver function, the NPVP-gastropathy (nausea, vomiting, an abdominal pain, heartburn, a loss of appetite, a meteorism, pain and discomfort in epigastric area), irritation, dryness of a mucous membrane of an oral cavity or mouth pain, an ulceration of a mucous membrane of gums, aphthous stomatitis, pancreatitis, a lock, hepatitis.

From respiratory system: asthma, bronchospasm.

From sense bodys: decrease in hearing, ring or sonitus, reversible toxic optic neuritis, illegibility of visual perception or diplopia, dryness and irritation of eyes, chemosis and century (allergic genesis), scotoma.

From a nervous system: dizziness, headache, sleeplessness, uneasiness, nervousness and irritability, psychomotor arousing, drowsiness, depression, confusion of consciousness, hallucination; seldom - aseptic meningitis (is more often at patients with autoimmune diseases).

From cardiovascular system: development or aggravation of heart failure, tachycardia, increase in the ABP.

From an urinary system: acute renal failure, allergic nephrite, nephrotic syndrome (hypostases), polyuria, cystitis.

Allergic reactions: skin rash, itch, Quincke's disease, anaphylactoid reactions, acute anaphylaxis, bronchospasm, fever, mnogoformny exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), eosinophilia, allergic rhinitis.

From bodies of a hemopoiesis: anemia (including hemolitic, aplastic), thrombocytopenia and Werlhof's disease, agranulocytosis, leukopenia.

Others: hypostases, sweating strengthening.

Interaction with other medicines:

The combination to ethanol, GKS, corticotropin increases risk of an erosive canker of a GIT.

The ibuprofen strengthens action of straight lines (heparin) and indirect (derivatives of coumarin and an indandion) anticoagulants, trombolitik (an alteplaza, an anistreplaza, Streptokinasa, an urokinase), antiagregant, colchicine the risk of development of hemorrhagic complications increases.

Strengthens hypoglycemic effect of insulin and peroral hypoglycemic medicines.

Weakens effects of hypotensive medicines and diuretics (at the expense of inhibition of synthesis of renal prostaglandins).

Increases concentration in blood of digoxin, drugs of lithium and a methotrexate.

Caffeine strengthens analgeziruyushchy action of an ibuprofen.

Cyclosporine and drugs of gold increase nephrotoxicity.

Tsefamandol, цефоперазон, цефотетан, valproic acid, пликамицин increase the frequency of development of a prothrombinopenia.

Antacids and Colestyraminum reduce absorption of an ibuprofen.

Diflunisal increases plasma concentration of paracetamol for 50% that increases risk of development of a hepatotoxic.

Myelotoxic medicines strengthen manifestations of a gematotoksichnost of drug.

At simultaneous use with acetylsalicylic acid the ibuprofen reduces its antiinflammatory and antiagregantny action.

Inductors of a microsomal oxidation in a liver (Phenytoinum, ethanol, barbiturates, флумецинол, rifampicin, phenylbutazone, tricyclic antidepressants) increase products of hydroxylated active metabolites that causes a possibility of development of heavy intoxication at overdose.

Contraindications:

— a peptic ulcer of a stomach and duodenum (in an aggravation phase);

— heavy liver and/or renal failure;

— diseases of bodies of a hemopoiesis;

— deficit glyukozo-6-fosfatdegidrogenazy;

— full or incomplete combination of bronchial asthma,
the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid or other NPVP (including in the anamnesis);

— gastrointestinal bleeding;

— a state after performing aortocoronary shunting;

— the confirmed hyperpotassemia;

— pregnancy;

— lactation period;

— children's age up to 18 years;

— hypersensitivity to drug components.

With care it is necessary to use drug at bronchial asthma, a bronchospasm, chronic heart failure, a viral hepatitis, alcoholic damage of a liver, a liver and/or renal failure, high-quality hyperbilirubinemias (Gilbert's syndrome, the Cudgel Johnson and the Rotor), cirrhosis with portal hypertensia, a nephrotic syndrome, a diabetes mellitus, diseases of peripheral arteries, a peptic ulcer of a stomach and a duodenum (in the anamnesis), gastritis, enteritis, colitis, and also at patients of advanced age.

Overdose:

Symptoms: symptoms of an abnormal liver function under the influence of paracetamol can appear in 12-48 h after overdose. At heavy overdose - a liver failure with the progressing encephalopathy, a coma, death; an acute renal failure with a tubular necrosis (including in the absence of severe damage of a liver); arrhythmia, pancreatitis.

Treatment: introduction of donators of SH-group and predecessors of synthesis of glutathione: methionine in 8-9 h and Acetylcysteinum in 12 h after overdose. Need for holding additional therapeutic actions (further administration of methionine, in/in introduction of Acetylcysteinum) is defined depending on concentration of paracetamol in blood, and also from time which passed after its reception.

Storage conditions:

Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature from 8 °C to 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

5 pieces - blisters (1) - packs cardboard.
7 pieces - blisters (1) - packs cardboard.
7 pieces - blisters (10) - packs cardboard.
10 pieces - blisters (1) - packs cardboard.
10 pieces - blisters (5) - packs cardboard.
10 pieces - blisters (7) - packs cardboard.