Hirumat - instructions for use, dose, side effects, contraindications

Auxiliary Ingredients: cellulose microcrystalline 20 mg, corn starch 136.44 mg, talc 10 mg, magnesium stearate 10 mg, silicon dioxide colloid 6.06 mg, carboxy and methyl starch sodium 10 mg.

Description:White or almost white oval biconvex tablets with a risk on one side.

Pharmacotherapeutic group:Analgesic combined (NSAIDs + analgesic non-narcotic)

ATX: & nbsp

M.01.A.E.51 Ibuprofen in combination with other drugs

Pharmacodynamics:

Combined drug.

The effect of the drug is due to its constituent components.

Ibuprofen - Non-steroidal anti-inflammatory drug (NSAID), has analgesic, anti-inflammatory, antipyretic effect. Inhibiting cyclooxygenase (COX) I and 2, disrupts the metabolism of arachidonic acid, reduces the number of prostaglandins (mediators of pain, inflammation and hyperthermia), both in the inflammatory focus and in healthy tissues, suppresses the exudative and proliferative phases of inflammation.

Paracetamol - indiscriminately blocks COX, mainly in the central nervous system, weakly affects the water-salt metabolism and mucosa of the gastrointestinal tract (GI tract). Has analgesic and antipyretic effect. In inflamed tissues, peroxidases neutralize the effect of paracetamol on COX 1 and 2, which explains the low anti-inflammatory effect. The effectiveness of the combination is higher than that of the individual components. Relieves arthralgia at rest and during movement, reduces morning stiffness and swelling of joints, promotes an increase in the volume of movements.

Pharmacokinetics:

Ibuprofen. It is well absorbed from the gastrointestinal tract. Absorption slightly decreases when taking the drug after a meal.Time to reach the maximum concentration (TCmax) when administered on an empty stomach - 45 minutes, when taken after meals - 1,5-2,5 h, in synovial fluid - 2-3 h (the concentration of ibuprofen is higher than in blood plasma). The connection with plasma proteins is 90%.

Exposed to the systemic and post-systemic metabolism in the liver. After absorption about 60% of pharmacologically inactive Rform of ibuprofen is slowly transformed into an active S-form. In the metabolism of the drug takes part isoenzyme cytochrome P-450 CYP2C9.

Has a two-phase kinetics of elimination with a half-life (T_|/2) 2-2.5 hours. It is excreted by the kidneys (in unchanged form not more than 1%) and to a lesser extent - with bile.

Paracetamol. Absorption is high. TS_max is achieved after 0.5-2 hours. The maximum concentration in the blood plasma is 5-20 μg / ml. Connection with plasma proteins - 15%. Penetrates through the blood-brain barrier. Less than 1% of the dose of paracetamol taken by the lactating mother falls into the breast milk. The therapeutically effective concentration of paracetamol in plasma is achieved when it is administered at a dose of 10-15 mg / kg.

Metabolised in the liver (90-95%): 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites,which are conjugated with glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. In the metabolism of paracetamol is also involved isoenzyme cytochrome P-450 CYP2E1.

T1 / 2 1-4 h. It is excreted by the kidneys in the form of metabolites, only 3% in unchanged form. In elderly patients, the clearance of the drug decreases and increases T1 / 2.

Indications:

- headache (including migraine);

- toothache;

- algodismenorea (painful menstruation);

- neuralgia;

- myalgia (muscle pain);

- back pain;

- joint pain, pain syndrome with inflammatory and degenerative

diseases of the musculoskeletal system;

- pain with bruises, sprains, dislocations, fractures;

- post-traumatic and postoperative pain syndrome;

febrile conditions (fever).

The drug is used as a symptomatic treatment of acute respiratory diseases ("colds") and influenza: febrile conditions (fever), headache, muscle pain.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use; on the progression of the disease is not affected.

Contraindications:Hypersensitivity, gastric and duodenal ulcer (in the acute phase), severe hepatic and / or renal failure, diseases of the hematopoiesis, deficiency of glucose-6-phosphate dehydrogenase; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in anamnesis); gastrointestinal bleeding; condition after aortocoronary bypass surgery; confirmed hyperkalemia, pregnancy, lactation, children under 18 years of age.

Carefully:

Bronchial asthma, bronchospasm, chronic heart failure, viral hepatitis, alcoholic liver damage, hepatic and / or renal failure, benign hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson and Rotor syndrome), liver cirrhosis with portal hypertension, nephrotic syndrome; diabetes, peripheral arterial disease, gastric and duodenal ulcer (in history); gastritis, enteritis, colitis, and advanced age.

Pregnancy and lactation:

Dosing and Administration:

Inside, wash down with water.

The dosage regimen is set individually, depending on the indications.

Usually the initial dose is 1 tablet 3 times a day after meals. The maximum single dose - 2 tablets, the maximum daily - 6 tablets.

In case of violations of kidney or liver function, the break between doses is not 1 less than 8 hours.

Duration of treatment without medical supervision should not exceed 5 days when prescribed as an anesthetic and 3 days - as an antipyretic.

Side effects:

From the digestive system: dyspepsia, diarrhea, erosive and ulcerative lesions of the digestive tract, bleeding from the digestive tract, impaired liver function, NSAID-gastropathy (nausea, vomiting, abdominal pain, heartburn, decreased appetite, flatulence, pain and discomfort in the epigastric region), irritation, dry mucous oral cavity or pain in the mouth, ulceration of the gingival mucosa, aphthous stomatitis, pancreatitis, constipation, hepatitis.

From the respiratory system: shortness of breath, bronchospasm,

From the sense organs: hearing loss, ringing or noise in the ears, reversible toxic optic neuritis, blurred vision or diplopia, dry and irritated eyes, conjunctival edema and eyelids (allergic genesis), scotoma.

From the nervous system: dizziness, headache, insomnia, [anxiety, nervousness and irritability, psychomotor [agitation, drowsiness, depression, confusion, hallucinations,

rarely - aseptic meningitis (more often in patients with autoimmune diseases).

From the cardiovascular system: development or aggravation of heart failure, tachycardia, increased blood pressure.

From the urinary system: acute renal failure, allergic nephritis, nephrotic syndrome (edema), polyuria, cystitis.

Allergic reactions: skin rash, itching, angioedema, anaphylactoid reactions, anaphylactic shock, bronchospasm, fever, erythema multiforme exudative (including Stephen-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), eosinophilia, allergic rhinitis.

On the part of the organs of hematopoiesis: anemia (including hemolytic, aplastic), thrombocytopenia and thrombocytopenic purpura, agranulocytosis, and leukopenia.

Other: swelling, increased sweating.

Overdose:

Symptoms. Symptoms of liver dysfunction under the action of paracetamol may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia; pancreatitis.

Treatment. Introduction of donors of SH-groups and precursors of the synthesis of glutathione: methionine after 8-9 hours and acetylcysteine 12 hours after an overdose. The need for additional, therapeutic measures (continued methionine administration, intravenous acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.

Interaction:

The combination with ethanol, glucocorticosteroids, corticotropin increases the risk of erosive and ulcerative lesions of the digestive tract.

Ibuprofen enhances the effect of direct (heparin) and indirect (coumarin and indanedione derivatives) anticoagulants, thrombolytics (alteplase, anestreplase, streptokinase, urokinase), antiplatelet agents, colchicine - the risk of hemorrhagic complications increases.Strengthens the hypoglycemic effect of insulin and oral hypoglycemic drugs.

Weaken the effects of antihypertensive drugs and diuretics (by inhibiting the synthesis of renal prostaglandins). Increases the concentration in the blood of digoxin, lithium and methotrexate.

Caffeine increases the analgesic effect of ibuprofen. Cyclosporin and gold preparations increase nephrotoxicity. Cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin increase the frequency of hypoprothrombinemia.

Antacids and colestramine reduce the absorption of ibuprofen. Diflunisal increases the plasma concentration of paracetamol by 50%, which increases the risk of hepatotoxicity. Myelotoxic drugs increase the manifestation of hematotoxicity of the drug. With simultaneous use with acetylsalicylic acid ibuprofen reduces its anti-inflammatory and antiaggregant effect. Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites,which causes the possibility of severe intoxication in case of an overdose.

Special instructions:

At simultaneous application with anticoagulants of indirect action control of coagulating system of blood is necessary.

When using the drug for more than 5-7 days should be monitored

parameters of peripheral blood and the functional state of the liver.

When symptoms of NSAID-gastropathy appear, careful monitoring is performed, including esophagogastroduodenoscopy, a blood test with determination of hemoglobin and hematocrit, and analysis of feces for latent blood. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test. Paracetamol distorts the results of laboratory studies of glucose and uric acid in the blood plasma. The simultaneous use of the drug with other drugs containing paracetamol and / or non-steroidal anti-inflammatory agents. During the period of treatment, it is not recommended to take alcohol-containing drinks.

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

Be careful and avoid driving and potentially dangerous activities that require increased concentration attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 400 mg + 325 mg.

Packaging:

5, 7 or 10 tablets in PVC / Al blister or Al / Al blister.

1 blister for 5 tablets together with instructions for use in a pack of cardboard.

1, 2, 5 or 10 blisters of 10 tablets together with instructions for use in a pack of cardboard.

1 or 10 blisters for 7 tablets together with instructions for use in a cardboard pack.

1 or 2 blisters for 5, 7 or 10 tablets together with instructions for use in a cardboard package with perforations protected with a PVC film on the inside of the pack (2 perforations in the form of an oval on a pack of 5 tablets, 4 perforations in the form of an oval on a pack of 7 , 10, 14 or 20 tablets).

For hospitals:

100, 500, 1000 tablets per package polyethylene, 1 package together with instructions for use in a jar of high-density polyethylene. A label is attached to the jar.

Storage conditions:In a dry, dark place at a temperature of 8 ° C to 25 ° C.

Keep out of the reach of children.

Shelf life:3 years.Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001514

Date of registration:16.02.2012

The owner of the registration certificate:Rekitt Benckiser Helsar International Ltd.Rekitt Benckiser Helsar International Ltd. United Kingdom

Manufacturer: & nbsp

RECKITT BENCKISER HEALTHCARE INTERNATIONAL, Ltd. United Kingdom

Representation: & nbspREKITT BENKIZER HELSKER LTD. REKITT BENKIZER HELSKER LTD. United Kingdom

Information update date: & nbsp16.02.2012

Illustrated instructions

Instructions

Hyrumat (Hirumat)