Producer: Ranbaxy Laboratories Ltd, Ind. Area (Ranbaksi Laboratoriz Ltd, Indus Erea) India
Code of automatic telephone exchange: M01AE51
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active agents: ibuprofen of 400 mg, paracetamol of 325 mg
Excipients: calcium hydrophosphate, starch corn, the povidone, talc purified isopropanol *
Film cover: dye опадрай orange 06G53189 (gipromelloza 5 Wednesday, gipromelloza 15 Wednesday, titanium dioxide, dye sunset yellow, macrogoal, propylene glycol, sodium lauryl sulfate), water очищенная*.
* it is lost in the course of production
The combined drug. Has anesthetic, antiinflammatory and febrifugal effect. The mechanism of antiinflammatory action of an ibuprofen is caused by activity inhibition циклогеназ (TsOG) with the subsequent suppression of synthesis of prostaglandins.
Paracetamol - non-narcotic analgesic, blocks TsOG preferential in TsNS, influencing the centers of pain and thermal control, has analgeziruyushchy and febrifugal effect.
Pharmacokinetics. The ibuprofen is well absorbed from a stomach. Tmax – about 1 hour. Absorption slightly decreases at administration of drug after food. About 99% contact proteins of plasma. The ibuprofen is slowly distributed in synovial fluid and brought out of it more slowly, than out of plasma. Is exposed to metabolism in a liver, mainly by a hydroxylation and a carboxylation of isobutyl group. CYP2C9 isoenzyme takes part in metabolism of drug. After absorption about 60% pharmacological of an inactive R-form of an ibuprofen are slowly transformed to an active S-form. Has two-phase kinetics of elimination. Elimination half-life (T?) makes 2-3 hours of plasma. To 90% of a dose it can be revealed in urine in the form of metabolites and their conjugates. Less than 1% are excreted in not changed view with urine and, to a lesser extent, with bile. The ibuprofen is completely removed in 24 hours.
Paracetamol is quickly soaked up from a GIT. Achievement time With max in 0,5-2 hours. It is evenly distributed in organism liquids. Communication with proteins of plasma variable within 15%. Gets through GEB. Is exposed to metabolism 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 at conjugation with glutathione form inactive metabolites. At a lack of glutathione these metabolites can block fermental systems of hepatocytes and cause their necrosis. CYP2E1 isoenzyme participates in metabolism of paracetamol. T 1/2 1-4 hours. Only 3% in not changed look are removed by kidneys in the form of conjugates, and. At elderly patients the clearance of paracetamol decreases and T1/2 increases.
Indications to use:
Feverish reaction at acute respiratory diseases, flu, post-inoculative reactions and other infectious and inflammatory diseases.
Pain syndrome of weak or moderate intensity, including: head and a dentagra, migraine, neuralgia, a lumbago, a mialgiya, a fibrositis, a tendovaginitis, an arthralgia at a pseudorheumatism, an osteoarthrosis, gout, a spondylarthritis, etc., pain at diseases the ENT SPECIALIST – bodies, at injuries of soft tissues and the basic motive device (stretchings, bruises, dislocations, fractures and др), postoperative pain, альгодисменорея.
Route of administration and doses:
Drug is accepted inside after food.
Adults and children are more senior than 15 years: drug is accepted on 1 tablet by 3-4 times a day with an interval of 6-8 hours (no more than 4 times a day!).
Children from 12 to 15 years (body weight more than 40 kg): on 1 tablet 3 times a day.
If fever remains more than 3 days, it is necessary to consult to the doctor.
Duration of treatment is defined by the doctor depending on therapeutic effect and the nature of a disease.
Features of use:
Treatment by drug should be carried out in a minimal effective dose, minimum possible short course.
During treatment control of a picture of peripheral blood and a functional condition of a liver and kidneys is necessary. At emergence of symptoms of a gastropathy the careful control including carrying out an ezofagogastroduodenoskopiya, blood test with definition of hemoglobin, a hematocrit, the analysis a calla on the occult blood is shown. For the prevention of development of the NPVP-gastropathy it is recommended to combine with prostaglandin E drugs (мизопростол). Patients have to abstain from all types of activity requiring special attention, bystry mental and motor reaction. During treatment alcohol intake (ethanol) is not recommended.
At a concomitant use with indirect anticoagulants it is necessary to control coagulant system of blood.
At drug use side effects are observed seldom, however emergence of the following side effects is possible:
Digestive tract: NPVP a gastropathy (nausea, vomiting, heartburn, abdominal pains, a lock, a meteorism, a loss of appetite, it is rare – ulcerations mucous a GIT, in some cases are complicated by bleeding and perforation), irritation or dryness of a mucous membrane of an oral cavity, mouth pain, an ulceration of a mucous membrane of gums,
Gepato-biliarnaya system: hepatitis
Allergic reactions: skin rash (usually erythematic or small tortoiseshell), skin itch, Quincke's edema, anaphylactoid reactions, acute anaphylaxis, bronchospasm or диспноэ, fever, mnogoformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), eosinophilia, allergic rhinitis.
Cardiovascular system: heart failure, tachycardia, increase in arterial pressure.
Central and peripheral nervous system: a headache, dizziness, sleeplessness, uneasiness, nervousness and irritability, psychomotor excitement, drowsiness, a depression confusion of consciousness, a hallucination, it is rare - aseptic meningitis (more often at patients with autoimmune diseases)
Bodies of a hemopoiesis: anemia (including hemolitic, aplastic), thrombocytopenia and Werlhof's disease, agranulocytosis, leukopenia.
Respiratory system: asthma, bronchospasm.
Sense bodys: hearing disorder (ring or sonitus), vision disorder (toxic optic neuritis, illegibility of sight or diplopia, dryness and irritation of eyes, chemosis and century of allergic genesis, scotoma)
Urinary system: acute renal failure, allergic nephrite, nephrotic syndrome (hypostases), polyuria, cystitis
Laboratory indicators: a bleeding time, concentration of creatinine in serum, activity of hepatic "transaminases" (can increase); concentration of glucose in serum, clearance of creatinine, a hematocrit or hemoglobin (can decrease).
Interaction with other medicines:
Inductors of a microsomal oxidation (Phenytoinum, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase products of hydroxylated active metabolites, increasing risk of development of heavy hepatotoxic reactions.
Inhibitors of a microsomal oxidation reduce risk of a hepatotoxic action.
Reduces hypotensive activity of vazodilatator (in т.ч blockers of "slow" calcium channels and APF inhibitors), natriyurichesky and diuretic - furosemide and Hydrochlorthiazidum. Reduces efficiency of uricosuric medicines, strengthens action of indirect antikoagulyantn, antiagregant, fibrinolitik (increase in risk of emergence of hemorrhagic complications), ulcerogenic action with bleedings of glucocorticosteroids, colchicine, estrogen, ethanol; strengthens effect of peroral hypoglycemic medicines and insulin.
Antacids and Colestyraminum reduce absorption of an ibuprofen. Increases concentration in blood of digoxin, drugs of lithium and a methotrexate
Caffeine strengthens analgeziruyushchy effect.
At co-administration active component of Brustan - the ibuprofen reduces antiinflammatory and antiagregantny effect of acetylsalicylic acid (ASK) (after the beginning of reception of an ibuprofen increase in frequency of development of acute coronary insufficiency in the patients receiving small doses of ASK as antiagregantny means is possible).
At appointment with anticoagulants and thrombolytic medicines (alteplazy, Streptokinasa, an urokinase), inhibitors of the return serotonin reuptake (tsitalopramy, fluoxetine, paroksetiny, sertraline) the risk of development serious a GIT of bleedings increases.
Tsefamandol, цефаперазон, цефотетан, valproic acid, пликамицин increase the frequency of development of a prothrombinopenia.
Myelotoxic drugs strengthen manifestations of a gematotoksichnost of drug.
Cyclosporine and drugs of gold strengthen influence of an ibuprofen on synthesis of prostaglandins in kidneys that is shown by increase in nephrotoxicity. The ibuprofen increases plasma concentration of cyclosporine and probability of development of its gepatotoksichny effects. The medicines blocking canalicular secretion reduce removal and increase plasma concentration of an ibuprofen.
Hypersensitivity to an ibuprofen, paracetamol, acetylsalicylic acid or other NPVP, and also to other components of drug;
The instruction in the anamnesis on the bronkhoobstruktion attack, a small tortoiseshell, rhinitis provoked by reception of acetylsalicylic acid (salicylates) or other NPVP (a full or incomplete syndrome of intolerance of acetylsalicylic acid: rinosinusit, a small tortoiseshell, polyps mucous a nose, bronchial asthma).
The period after performing aortocoronary shunting
Erosive язвеннное damage of a GIT, active gastric bleeding
Inflammatory diseases of intestines
Condition of hypocoagulation, cerebrovascular bleedings
The expressed renal and/or liver failure, the confirmed hyperpotassemia;
Pregnancy III trimester, lactation period;
Children's age up to 12 years (this dosage form)
With care: congestive heart failure, arterial hypertension, coronary heart disease, cerebrovascular diseases, a dislipidemiya, a diabetes mellitus, diseases of peripheral arteries, smoking, frequent alcohol intake, hyperbilirubinemias, cirrhosis with portal hypertensia, a liver and/or renal failure, a nephrotic syndrome, pregnancy I and II trimesters, advanced age, deficit glyukozo-6-fosfatdegidrogenazy, a peptic ulcer of a stomach and a 12-perstny gut (in the anamnesis), gastritis, diseases of blood of not clear etiology (a leukopenia and anemia).
Pregnancy and period of a lactation.
Drug is contraindicated in the III trimester of pregnancy. Use in I and II trimester, the period of a lactation has to be discussed with the attending physician.
Problems of emergence of overdose arise very seldom, however, at accidental overdose it is necessary to see a doctor immediately.
Symptoms: abdominal pains, nausea, vomiting, headache, sonitus, metabolic acidosis, coma, acute renal failure, lowering of arterial pressure, bradycardia, tachycardia.
Emergence of hepatotoxic effect with development of the gepatonekroz connected with paracetamol is possible.
Treatment: a gastric lavage (only within an hour after reception), absorbent carbon, alkaline drink, an artificial diuresis, introduction of donators of SH-group and predecessors of synthesis of glutathione – methionine and N-Acetylcysteinum. Need for holding additional therapeutic actions (further administration of methionine, in/in introduction of N-Acetylcysteinum) is defined depending on concentration of paracetamol in blood, and also from time which passed after its reception. Besides, symptomatic therapy is shown.
To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use drug after expiry date.
According to the recipe
Tablets are film coated: On 10 tablets in the blister from the aluminum foil covered with a vinylchloride polymeric film; on 1 blister together with the application instruction in a cardboard pack.