The instruction for medical use of medicine Brufenum the Trade name Brufenum the International unlicensed name Ibuprofen Dosage Form of the Granule sparkling 600 mg contains Structure of 1 sachet: active agent – an ibuprofen of 600 mg, excipients: malic acid, sodium saccharinate, sucrose, povidone (To value from 29 to 32), orange fragrance, sodium lauryl sulfate, Natrii hydrocarbonas, sodium a carbonate anhydrous. The description of the Granule of white color, the size from small to large with an orange smell. Pharmacotherapeutic group Anti-inflammatory and antirheumatic drugs. Non-steroidal anti-inflammatory drugs. Propionic acid derivatives. Ibuprofen. The ATX M01A E01 code the Pharmacological Pharmacokinetics Ibuprofen properties represents racemic mix [+] S- and [-] R-enantiomerov. The ibuprofen is quickly absorbed from a GIT, at the same time the bioavailability is 80-90%. Peak concentration in blood serum are reached within 1-2 hours after reception. Researches with use of standard food show that it does not affect substantially the general bioavailability. The ibuprofen substantially contacts proteins of blood plasma (99%). The volume of distribution of an ibuprofen is insignificant – 0.12-0.2 l/kg for adults. The ibuprofen is quickly metabolized in a liver by means of P450 cytochrome enzymes, mainly CYP2C9, with formation of two main inactive metabolites — 2 hydroxyibuprofens and 3 carboxyibuprofens. About 90% of the accepted dose of an ibuprofen can be found in urine in the form of oxidizing metabolites and their glucuronic conjugates. The insignificant quantity of an ibuprofen is removed with urine in not changed look. Removal with urine is fast and full. Elimination half-life — about 2 hours. The ibuprofen is almost completely brought out of an organism in 24 hours after reception of the last dose. Patients of advanced age in the absence of a renal failure were observed only small, clinically insignificant differences in a pharmacokinetic profile and removal with urine between patients of young and advanced age. Children System exposure of an ibuprofen at use in therapeutic doses according to body weight (from 5mg/kg to 10mg/kg body weights) to children aged from 1 year same, as at adults. Children aged from 3 months up to 2.5 years have a volume of distribution (l/kg) and clearance (l/kg/h) of an ibuprofen above, than at children aged from 2.5 years up to 12 years. A renal failure At patients with a moderate renal failure the increased level (S) – an ibuprofen in blood plasma, the increased value of the size AUC (S) – an ibuprofen and the increased values of an enantiomeric ratio of AUC (S/R) in comparison with healthy volunteers of control group was observed. At patients with an end-stage of a renal failure on dialysis the average free fraction of an ibuprofen made about 3% in comparison with, about, 1% at healthy volunteers. Serious violations of function of kidneys can lead to accumulation of metabolites of an ibuprofen. The importance of this effect is unknown. Metabolites can be removed by means of a hemodialysis (see the sections Route of Administration and Doses, Contraindications, Special Instructions). A liver failure Presence of an alcoholic liver disease in a slight or moderate liver failure had no significant effect on change of pharmacokinetic parameters. At the patients with cirrhosis and a moderate liver failure (6 — 10 points on a scale of Chayld-Pyyu) receiving treatment by a racemic ibuprofen the increase in elimination half-life on average was observed twice, and the value of an enantiomeric ratio of AUC (S/R) was much lower in comparison with healthy volunteers of control group that indicates disturbance of metabolic transformation (R) – an ibuprofen in active (S) – an enantiomer (see the sections Route of Administration and Doses, Contraindications, Special Instructions). The pharmacodynamics the Ibuprofen, active ingredient of Brufenum — derivative propionic acid, non-steroidal anti-inflammatory drug (NPVS) has analgetic, anti-inflammatory and febrifugal activity. It is considered that therapeutic effects of drug are caused by its inhibiting effect on enzyme cyclooxygenase that leads to the significant decrease in synthesis of prostaglandins. These properties provide relief of symptoms of inflammation, pain, fever. Experimental data allow to assume that the ibuprofen can suppress competitively influence of low doses of acetylsalicylic acid / aspirin on aggregation of thrombocytes when both drugs are appointed at the same time. In some pharmakodinamichesky researches at single reception of an ibuprofen in a dose of 400 mg within 8 hours to or 30 minutes after intake of acetylsalicylic acid / aspirin in shape with fast release of drug (in a dose of 81 mg) influence of acetylsalicylic acid / aspirin on formation of thromboxane or aggregation of thrombocytes decreased. Though there are inaccuracies concerning extrapolation of experimental data on a clinical situation, it is impossible to exclude probability that regular prolonged use of an ibuprofen can reduce cardiotyre-tread effect of low doses of acetylsalicylic acid / aspirin. Clinically significant effects are improbable at irregular use of an ibuprofen (see the section Medicinal Interactions). Indications – the pseudorheumatism, including the juvenile arthritis or Stilla-Shoffar’s disease ankylosing a spondylitis, an osteoarthritis and other not rheumatoid (seronegative) arthropathies and acute gouty arthritis – extraarticular rheumatic and periartikulyarny defeats, such as humeroscapular periarthritis (capsulitis), bursitis, tendinitis, tendosinovit also lower back pain – damages of soft tissues, for example stretching and tension of sheaves – reduction of mild and moderate pain, for example, at primary dysmenorrhea, tooth and postoperative pain, pain after an epiziotomiya, postnatal pain and symptomatic treatment of a headache, including migraine – a hyperthermia the Route of administration and doses of the Dose Side effects can be minimized at use of a minimal effective dose during the shortest span necessary for control over symptoms (see the section Special Instructions). Before use it is necessary to dissolve carefully granules in enough water that there was no burning sensation in a mouth or in a throat. For achievement of faster action, it is recommended to take the drug on a hungry stomach. Patients with a sensitive stomach are recommended to take the drug after a meal. Adults and teenagers (18 years are more senior) the Recommended dose makes 1200-1800 mg/days, divided into several receptions. To some patients there can be enough 600–1200 mg/days. In hard and sharp cases the increase in a dose up to the termination of a sharp phase of a disease is possible. At the same time the maximum daily dose should not exceed 2400 mg which are applied in stages. Patients of advanced age Are not present need for change of a dose if function of a liver or kidneys is not broken. In an abnormal liver function or kidneys the dose of drug should be selected individually and with care. Children Brufenum in this pharmaceutical form is contraindicated for use for children. Side effects Side reactions about which it was reported in connection with reception of an ibuprofen are similar it at use of other NPVS. The most widespread side effects are connected with digestive tract. Nausea, vomiting, diarrhea, a meteorism, a constipation, dyspepsia, an abdominal pain, a melena, a hematemesis, a stomacace, gastrointestinal bleedings and exacerbation of colitis and Crohn’s disease (see the section Contraindications) were recorded after reception of an ibuprofen. Gastritis, a duodenum ulcer, a peptic ulcer of a stomach and gastrointestinal perforation were less often observed. At administration of drug there can be a temporary burning sensation in a mouth or in a throat. Disturbances from the immune system At use of an ibuprofen it was reported about cases of development of reactions of hypersensitivity. They can include: (a) nonspecific allergic reactions and an acute anaphylaxis, (b) reactions of airways, including asthma, exacerbation of asthma, a bronchospasm or an asthma and also (c) various skin reactions, including rash of various types, naggers, urticaria, a purpura, a Quincke’s disease and, in rare instances a multiformny erythema and bullous dermatitis (including Stephen-Johnson’s syndrome and toxic epidermal a necrolysis). Infections and invasions Are described cases of aggravation of the inflammations of skin caused by infections (for example, development of a necrotizing fasciitis), at use of NPVP. If during use of an ibuprofen for the patient symptoms of an infection arise or worsen, it is necessary to see a doctor immediately. Disturbances from skin and hypodermic cellulose In exceptional cases can arise serious skin infections and disturbances from outside soft fabrics against the background of chicken pox (see also Infections and invasions) Disturbances from a cardiovascular system Results of clinical trials demonstrate that use of an ibuprofen, especially in a high dose (2400 mg/day), can be connected with insignificant increase in risk of arterial trombotichesky complications (for example, a myocardial infarction and a stroke) (see the section Special Instructions). Side reactions are distributed on emergence frequency: very frequent ≥ 1/10, frequent ≥1/100 to ≤1/10, infrequent ≥1/1000 to ≤ 1/100, rare ≥1/10000 to ≤ 1/1000, very rare ˂ 1/10000, frequency is unknown (it is impossible to estimate frequency on the available data) Often – a headache, dizziness – dyspepsia, diarrhea, nausea, vomiting, an abdominal pain, a meteorism, a constipation, a melena, a hematemesis, gastrointestinal bleeding – rash – fatigue Infrequently – rhinitis – insomnia, concern – a parasthesia, drowsiness – deterioration in sight – deterioration in hearing, noise or a ring in ears, vertigo – asthma, a bronchospasm, otdyshka-gastritis, an ulcer of a duodenum and stomach ulcer, a stomacace, gastrointestinal perforation – hepatitis, jaundice, an abnormal liver function – urticaria, an itching, a purpura, a Quincke’s disease, photosensitivity – a toxic nephropathy in various forms, including tubulointerstitsialny nephrite, a nephrotic syndrome, a renal failure Seldom – an acute anaphylaxis – a depression and confusion of consciousness – retrobulbar neuritis – a toxic neuropathy of an optic nerve – hypostasis Very seldom – aseptic meningitis – a leukopenia, thrombocytopenia, aplastic anemia, a neutropenia, an agranulocytosis and hemolytic anemia – severe general reactions of hypersensitivity which proyalyatsya by edema of face, language and a throat, dispnoe, heartbeat acceleration, falling of arterial blood pressure (anaphylaxis, a Quincke’s disease or heavy shock). – pancreatitis – a liver failure – heavy skin reactions, for example, a multiformny erythema, bullous reactions, including Stephens-Johnson’s syndrome and a toxic epidermal necrolysis – a warm neostatochnost, a myocardial infarction (see the section Special Instructions) – arterial hypertension Frequency is unknown – colitis and Crohn’s disease of the Contraindication – hypersensitivity to active agent or other components of drug – asthma, urticaria or other allergic reactions after intake of acetylsalicylic acid / aspirin or other non-steroidal anti-inflammatory drugs (NPVS) in the anamnesis – heavy heart failure (the IV functional class by criteria of the New York Association of heart (NYHA). – a heavy liver failure – a heavy renal failure (glomerular filtration rate & lt, 30 ml/min.) – the states which are followed by the increased risk of developing bleedings or active bleeding – the gastrointestinal bleeding or perforation connected with reception of NPVS in the anamnesis – the acute or postponed earlier ulcer colitis, Crohn’s disease, a recurrent round ulcer or gastrointestinal bleeding, (existence in the anamnesis of two the confirmed episodes of a canker or bleeding independent from each other) – the third trimester of pregnancy – children’s and teenage age up to 18 years – the lactation period Medicinal interactions It is necessary to be careful at co-administration with the following drugs because of possible medicinal interaction at some patients. Other NPVS, including selection TsOG-2 inhibitors. It is necessary to avoid co-administration with other NPVS, including selection TsOG-2 inhibitors, because of risk of development of additive effects (see the section Special Instructions). Cardiac glycosides. NPVS can cause exacerbation of heart failure, reduction in the rate of glomerular filtration and increase in level of cardiac glycosides in blood plasma. Corticosteroids. Increase in risk of gastrointestinal ulcers or bleedings when assigning with NPVS. Anticoagulants. NPVS can enhance effects of anticoagulants, such as warfarin. Antithrombocytic drugs and selective serotonin reuptake inhibitors. NPVS increase risk of gastrointestinal bleeding. Acetylsalicylic acid / aspirin. As well as when prescribing other drugs containing NPVS, the concomitant use of an ibuprofen and acetylsalicylic acid / aspirin usually is not recommended because of risk of increase in side reactions. Experimental data demonstrate that the ibuprofen can oppress competitively influence of low doses of acetylsalicylic acid / aspirin on aggregation of thrombocytes at co-administration. However, despite ambiguities concerning a possibility of extrapolation of these data on a clinical situation, it is impossible to exclude probability that regular prolonged use of an ibuprofen can reduce cardiotyre-tread effect of low doses of acetylsalicylic acid. At irregular reception of an ibuprofen clinically significant effects are absent (see the section Pharmacodynamics). Lithium. NPVS can reduce lithium removal. Antihypertensive drugs, β-blockers and diuretics. NPVS can reduce effect of antihypertensive drugs, such as APF inhibitors, antagonists of receptors of angiotensin II, β-blockers and diuretics. Diuretics can increase risk of nephrotoxicity of NPVS also. Methotrexate. NPVS can suppress canalicular secretion of a methotrexate and reduce clearance of a methotrexate. Cyclosporine. NPVS increase risk of nephrotoxicity. Takrolimus. Increase in risk of nephrotoxicity when assigning NPVS to the patients accepting takrolimus is possible. Zidovudine. NPVS increase risk of hematologic toxicity. There are proofs of increase in risk of developing a hemarthrosis and hematomas at the HIV-positive patients having hemophilia when assigning an ibuprofen against the background of reception of a zidovudine. Hinolonovy antibiotics. The data obtained on animals specify that NPVS can increase risk of appearance of the spasms connected with reception of hinolon. The patients accepting at the same time NPVS and hinolona have the increased risk of developing spasms. CYP2C9 inhibitors. Co-administration of an ibuprofen with CYP2C9 inhibitors can increase exposure of an ibuprofen (CYP2C9 substrate). During one research it was shown that vorikonazol and flukonazol (CYP2C9 inhibitors) increased exposure of S (+) – an ibuprofen approximately for 80-100%. It is necessary to provide an ibuprofen dose decline at co-administration with CYP2C9 inhibitors, especially when assigning high doses of Brufenum to the patients accepting vorikonazol or flukonazol. Sulphonylurea. NPVS can exponentiate effects of drugs of sulphonylurea. It was seldom reported about development of a hypoglycemia in the patients accepting sulphonylurea when prescribing Brufenum. Holestiramin. Co-administration of an ibuprofen and holestiramin can reduce absorption of an ibuprofen in a GIT. However the clinical value of it is unknown Aminoglycosides. NPVS can reduce removal of aminoglycosides. Extracts of herbs. The ginkgo of a bilob can exponentiate the risk of bleedings connected with NPVS. Mifepristone. Reduction of efficiency of medicine can theoretically happen because of the NPVS antiprostaglandinovy properties. Limited data allow to assume that simultaneous use of NPVS in day of use of prostaglandin does not distort effect of mifepristone or prostaglandin on changes a neck of the uterus or contractility
of an atka and does not reduce clinical performance of medicamentous termination of pregnancy. Special instructions General measures of precaution Undesirable effects can be minimized, using the lowest effective dose during the minimum span necessary for control over symptoms (see the section Special Instructions). As well as at use of other NPVS, reception of an ibuprofen can mask infection symptoms. Brufenum contains sucrose. To patients with such rare hereditary diseases, such as intolerance of fructose, glyukozo-galaktozny malabsorption or insufficiency of sucrose-isomaltase it is not necessary to take this medicine. Each sachet Brufenum contains sodium. Patients on a diet with control of content of sodium should take it into account. Patients of advanced age At patients of advanced age the frequency of development of side reactions at use of NPVS are higher, especially gastrointestinal bleeding and perforation which can be lethal. The Ibuprofen should appoint gastrointestinal bleeding, ulceration and perforation with care the patients having a round ulcer and other diseases of the digestive tract (DT) in the anamnesis as these states can become aggravated (see the section Contraindications). About development of gastrointestinal bleeding, ulcer or perforation it was reported at use of all NPVS during any span during treatment. These side reactions can be lethal and develop with or without symptoms harbingers irrespective of existence in the anamnesis of serious pathology of a GIT. Risk of developing gastrointestinal bleeding, ulcer or perforation is higher at increase in doses of an ibuprofen at patients with the ulcer which was especially complicated by bleeding or perforation in the anamnesis and at patients of advanced age. Such patients have to begin treatment with the lowest available dose. It is necessary to consider the possibility of co-administration to such patients of protective drugs (for example, a mizoprostol or inhibitors of a proton pomp), as well as to the patients who are at the same time accepting acetylsalicylic acid / aspirin in a low dose or other drugs increasing risk of damage of a GIT (see the section Medicinal Interactions). It is necessary to avoid co-administration of an ibuprofen and other NPVS, including selection inhibitors of cyclooxygenase-2 (TsOG-2), because of the increased risk of formation of ulcers and bleedings (see the section Medicinal Interactions). Patients, especially advanced age, with gastrointestinal diseases in the anamnesis have to report about any unusual abdominal symptoms (especially about gastrointestinal bleeding) at the initial stages of treatment. With care should appoint an ibuprofen the patients receiving the accompanying treatment by drugs which can increase risk of developing an ulcer or bleeding as, for example, oral corticosteroids, anticoagulants, such as warfarin, selective serotonin reuptake inhibitors or antithrombocytic drugs as, for example, acetylsalicylic acid / aspirin (see the section Medicinal Interactions). In case of development of gastrointestinal bleeding or an ulcer in the patient receiving an ibuprofen, drug should be cancelled. Respiratory disorders With care the patients having bronchial asthma, chronic rhinitis or allergic diseases and also the patients having these diseases in the anamnesis as it was reported that the ibuprofen can cause a bronchospasm, urticaria, a Quincke’s disease in such patients should appoint an ibuprofen. Dysfunction of heart, kidneys and a liver With care the patients having dysfunction of heart, kidneys and a liver as use of NPVS can lead to deterioration in function of kidneys should appoint an ibuprofen. Regular intake of similar analgetics at the same time in addition increases risk of deterioration in function of kidneys. To the patients having dysfunction of heart, kidneys and a liver it is necessary to apply a drug minimal effective dose during the shortest span and to control function of kidneys, especially at the patients receiving long-term treatment (ms. Section Contraindications). The Ibuprofen patients should appoint cardiovascular and cerebral and vascular effects with care with heart failure or arterial hypertension in the anamnesis as it was reported about development of hypostases against the background of use of an ibuprofen. Clinical trials demonstrate that purpose of an ibuprofen, especially in a high dose (2400 mg a day) can be connected with small increase in risk of arterial trombotichesky complications (for example, a myocardial infarction or a stroke). In general, epidemiological researches do not allow to assume existence of communication between reception of an ibuprofen in a low dose (≤ 1200 mg a day) and the increased risk of arterial trombotichesky complications. Patients with the uncontrollable arterial hypertension, stagnant heart failure (the II-III functional class by criteria of NYHA) diagnosed by coronary heart disease, a disease of peripheral arteries and/or cerebrovascular diseases should appoint an ibuprofen after the careful analysis of a situation and also it is necessary to avoid use of high doses of an ibuprofen (2400 mg a day). The careful analysis of a situation is also necessary before long therapy by an ibuprofen of patients with risk factors of developing cardiovascular diseases (such as arterial hypertension, lipidemia, diabetes, smoking), especially in case of need reception of high doses of an ibuprofen (2400 mg a day). Dermatological effects Very seldom at use of NPVS it was reported about development of serious skin reactions some of which can be lethal, including exfoliative dermatitis, Stephens-Johnson’s syndrome and a toxic epidermal necrolysis. Presumably, the greatest risk of development of these reactions exists in an initiation of treatment. In most cases the beginning of reaction occurs within the first month of therapy. Reception of an ibuprofen should be stopped at the first appearance of rash on skin, injury of a mucous membrane or any other signs of hypersensitivity. Effects from kidneys With care it is necessary to begin treatment of an ibuprofen of patients with considerable dehydration. There is a risk of developing a renal failure, especially at children and teenagers with dehydration. As well as when assigning other NPVS, long reception of an ibuprofen can lead to papillary necrosis of kidneys and other pathological changes in kidneys. Toxic influence on kidneys was also observed at patients at whom renal prostaglandins played a compensatory role in maintenance of perfusion of kidneys. Purpose of NPVS to such patients can cause dose-dependent reduction of formation of prostaglandins and, again, reduction of a renal blood-groove that can lead to a renal failure. The patients with a renal failure, heart failure, liver dysfunction accepting diuretics and inhibitors of angiotensin-converting enzyme (APF) and also patients of advanced age treat group of high risk of development of such reaction. The termination of reception of NPVS usually is followed by restoration of the state preceding treatment. Hematologic effects the Ibuprofen, it is similar to other NPVS, can oppress aggregation of thrombocytes and extend a bleeding time at healthy people. Aseptic meningitis In rare instances at the patients receiving an ibuprofen developed aseptic meningitis. Though it is more probable at patients with a system lupus erythematosus and other diseases of connective tissue, was reported about development of this complication also at patients without the accompanying chronic diseases. Pregnancy and the period of a lactation Pregnancy Oppression of synthesis of prostaglandins can adversely influence a course of pregnancy and/or development of an embryo/fruit. Data of epidemiological researches allow to assume increase in risk of a miscarriage and development of heart diseases and a gastroshizis after use of inhibitors of synthesis of prostaglandin in the early stages of pregnancy. It is supposed that the risk increases with increase in a dose and duration of therapy. It is not necessary to appoint an ibuprofen in the first and second trimesters of pregnancy without emergency. In case of purpose of an ibuprofen the women planning pregnancy or in the first or second trimester of pregnancy should apply as it is possible a smaller dose during as it is possible a smaller span. Use of any inhibitors of prostaglandin in the third trimester of pregnancy can influence a fruit, causing development of cardiopulmonary toxicity (with premature closing of an arterial channel and pulmonary hypertensia), dysfunction of kidneys which can progress to a renal failure with oligogidramniony. At the end of pregnancy inhibitors of synthesis of prostaglandin can influence a condition of mother and newborn child with possible lengthening of a bleeding time, oppression of contractility of a uterus that can be followed by a delay and prolongation of childbirth. Thus, use of an ibuprofen in the third trimester of pregnancy is contraindicated. It is not recommended to appoint an ibuprofen to women during patrimonial activity. It can lead to a delay of the beginning of childbirth, lengthening of the period of childbirth and increase in tendency to bleeding at mother and the child. Use in the period of a lactation during limited number of researches the ibuprofen was defined in breast milk in very low concentration. The women nursing are not recommended to appoint an ibuprofen. The ibuprofen can affect female fertility therefore its use is not recommended to the women planning pregnancy. Women who do not manage to become pregnant or who are examined concerning infertility should consider the possibility of cancellation of an ibuprofen. Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms Treatment by an ibuprofen can influence time of reaction of patients that should be considered in need of special attention, for example, when driving or the operational equipment. Overdose Signs and symptoms of overdose at adults usually were not observed at doses lower than 100 mg/kg. However the supporting actions in certain cases can be required. Symptoms. At most of patients the symptoms of overdose develop within 4-6 hours after reception of a significant amount of an ibuprofen. The most frequent symptoms of overdose include: nausea, vomiting, abdominal pain, apathy and drowsiness. Manifestations from the central nervous system (CNS): a headache, a ring in ears, dizziness, spasms and a loss of consciousness. It was seldom reported about a nystagmus, a metabolic acidosis, a hypothermia, symptoms from kidneys, gastrointestinal bleeding, a coma, an apnoea and oppression of central nervous system and a respiratory system. It was reported about cardiovascular toxicity, including development of arterial hypotension, bradycardia and tachycardia. In cases of considerable overdose the development of a renal failure and injury of a liver is possible. The considerable overdose is usually well transferred if other drugs were not taken. Treatment. There is no specific antidote at overdose by an ibuprofen. In case of reception of the dose exceeding 400 mg/kg it is necessary to wash out a stomach and to take measures of the supporting treatment within an hour from the moment of reception. For obtaining the most relevant information it is necessary to address to local poison control center. A form of release and packing Sparkling granules in a sachet. On 30 sachets together with the instruction for medical use in the state and Russian languages put in a pack from cardboard. To Store storage conditions at a temperature not above 25 °C. To store out of children’s reach! 2 years not to use a period of storage after the expiry date specified on packing. Prescription status According to the prescription the Producer Abbvi of Neuter of l., Italy S.R. 148 Pontina km 52 snc, 04011 Campoverde di Aprilia, (LT) Owner of the registration certificate of Abbott Laboratories GmbH, Hanover, Germany Packer Abbvi of Neuter of l., Italy S.R. 148 Pontina km 52 snc, 04011 Campoverde di Aprilia, (LT) the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers on quality of products (goods) and responsible for post-registration observation of safety of medicine. Abbott Kazakhstan LLP 050059 Almaty, Dostyk Ave., 117/6, 2
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