Brufen SR, 800 mg 28 pcs
€10.85 €9.49
ATX: M.01.A.E.01 Ibuprofen
Ibuprofen is a propionic acid derivative, a nonsteroidal anti-inflammatory drug (NSAID) that has analgesic, anti-inflammatory and antipyretic effects. The therapeutic effect of the drug is due to inhibition of cyclooxygenase enzyme, which leads to a significant decrease in the synthesis of prostaglandins. These properties provide elimination of symptoms of inflammation, pain and fever.
Experimental data show that concomitant use of ibuprofen may inhibit the effect of low doses of acetylsalicylic acid on platelet aggregation. In a single study, a single dose of ibuprofen 400 mg for 8 hours before or within 30 minutes of immediate-release acetylsalicylic acid (81 mg) was observed to reduce the effect of acetylsalicylic acid on thromboxane formation or platelet aggregation.
Because of the limitations of these data and the imprecision in extrapolating ex vivo data to the clinical situation, however, reliable conclusions regarding the continued use of ibuprofen cannot be drawn. The development of clinically significant effects is considered unlikely with episodic use of ibuprofen.
Pharmacokinetics:
Ibuprofen is a racemic mixture of [+]S- and [-]R-enantiomers. Studies have shown that food intake has no significant effect on overall bioavailability.
Absorption
Ibuprofen is rapidly absorbed in the gastrointestinal tract, bioavailability is 80 – 90%, time to maximum concentration (TCmax) in plasma when using the drug form of immediate release – 1-2 hours. Prolonged dosage form of ibuprofen 800 mg tablets provides a gradual release of the active substance, with a slower release rate compared to the dosage form of immediate release and a decrease in the value of maximum concentration (Cmax) in blood plasma, which is reached approximately 3 hours after the use of ibuprofen. As a result of the prolonged absorption phase, plasma concentrations of ibuprofen are maintained longer in the systemic bloodstream.
Thus, ibuprofen 800 mg tablets with prolonged action only once a day. A comparison of the pharmacokinetic profile of two 800 mg sustained-release ibuprofen tablets and 400 mg immediate-release ibuprofen tablets taken four times daily showed that the sustained-release dosage form provided a reduced range of differences between Cmax and threshold concentrations of immediate-release tablets and maintained higher mean plasma concentrations after 5, 10, 15 and 24 hours. The area under the curve “concentration – time” (AUC) was similar for immediate release tablets and prolonged release tablets.
Distribution
Ibuprofen is intensively bound to blood plasma proteins (99%). The volume of distribution (Vd) of ibuprofen is small and is approximately 0.12 – 0.2 L/kg in adults.
Metabolism
Ibuprofen is rapidly metabolized in the liver with the participation of cytochrome P450 isoenzymes, primarily CYP2C9, to form two major inactive metabolites – 2-hydroxyibuprofen and 3-carboxyibuprofen. When ibuprofen is administered orally, slightly less than 90% of the ingested dose of ibuprofen may be detected in the urine as oxidative metabolites and their glucuron conjugates. A small amount of ibuprofen is excreted unchanged in the urine.
Excretion
Excretion of ibuprofen through the kidneys is fast and complete. The elimination half-life (T1/2) of immediately-released forms is about two hours. Ibuprofen is almost completely eliminated from the body 24 hours after the last dose.
Special patient groups
Patients of the elderly
In elderly patients in the absence of renal failure only small, clinically insignificant differences in the pharmacokinetic profile and urinary excretion compared to younger patients are observed. Renal failure
In patients with moderate renal failure, elevated plasma (S)-ibuprofen levels, elevated AUC (S)-ibuprofen values and elevated enantiomeric AUC (S/R) ratio values were observed compared to healthy control patients. In patients with end-stage renal failure who were on dialysis, the mean free fraction of ibuprofen was about 3% compared to 1% in healthy volunteers. Serious renal dysfunction can lead to accumulation of ibuprofen metabolites. The significance of this effect is unknown. Metabolites may be excreted by hemodialysis.
Liver failure
The presence of alcoholic liver disease in mild to moderate liver failure had no significant effect on pharmacokinetic parameters.
Patients with cirrhosis and moderate liver failure (6-10 Child-Pugh scores) treated with racemic ibuprofen showed a 2-fold increase in T1/2, on average, and the enantiomeric AUC (S/R) value was significantly lower compared to healthy control group patients, indicating impaired metabolic transformation of (R)-ibuprofen to the active (S)-enantiomer.
Indications
Inflammatory and degenerative diseases: rheumatoid arthritis, including juvenile rheumatoid arthritis or Still’s syndrome, osteoarthritis, joint syndrome in gout exacerbation, psoriatic arthritis, Bechterew disease (ankylosing spondylitis), spondylosis.
Diseases of the periarticular tissues including rheumatic: periarthritis (capsulitis), bursitis, tendinitis, tenosynovitis, tendovaginitis, low back pain, radiculitis.
Padded tissue injuries: traumatic inflammation of soft tissues and locomotor system, sprains and strains, bruises.
Mild to moderate pain relief in: headache, toothache, primary dysmenorrhea, post-operative pain, migraine, panniculitis, neuralgia, myalgia.
Inflammatory processes in the pelvis: adnexitis, algodysmenorrhea.
Active ingredient
Ibuprofen
Composition
Active ingredient:
Ibuprofen – 800 mg.
Excipients:
xanthan gum – 196.8 mg;
povidone – 25.9 mg;
stearic acid – 10.3 mg;
colloidal silicon dioxide – 3.0 mg,
Hypromellose – 16.0 mg;
Opadry white M-1-7111B – 5.0 mg;
Talc – 3.0 mg;
Opacode S-1- 9460HV brown ink – traces.
How to take, the dosage
Ingestion, after a meal. Tablets should be swallowed whole, without chewing, with plenty of water.
Adults and children 12 years of age and older: The recommended dose is 2 tablets Brufen CP once a day, preferably before bedtime. In severe and acute conditions, the maximum daily dose is 3 tablets taken separately. The maximum daily dose is 2400 mg.
Elderly patients: With normal renal and hepatic function, dosage regimen adjustment in elderly patients is not required. In patients with impaired renal and/or hepatic function the dose should be adjusted individually. In this group of patients the dosing should be conducted with caution.
Interaction
Because of reported drug interactions in some patients, Brufen CP should be used with caution in patients taking any of the following medications:
Concomitant use of ibuprofen with the following medications: | Possible effects | |
Other NSAIDs, including selective cyclooxygenase-2 inhibitors | Concurrent use with other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided due to possible additive effects. | |
Heart glycosides | NSAIDs may worsen the course of heart failure, decrease glomerular filtration rate, and increase plasma concentrations of cardiac glycosides. | |
Glucocorticosteroids | The use of NSAIDs increases the risk of GI ulcers or bleeding. | |
Anticoagulants | NSAIDs may increase the effect of anticoagulants such as warfarin or heparin. In case of concomitant use, it is recommended to monitor blood clotting parameters. | |
Probenecid | Drugs containing probenecid may delay excretion of ibuprofen. | |
Antiplatelet agents and selective serotonin reuptake inhibitors (SSRIs) (e.g., clopidogrel, ticlopidine) | The use of NSAIDs increases the risk of gastrointestinal bleeding. | |
Acetylsalicylic acid | As with other drugs containing NSAIDs, concomitant use of ibuprofen and acetylsalicylic acid is not recommended because the risk of adverse effects increases. Experimental data show that concomitant use of ibuprofen may inhibit the effect of low doses of acetylsalicylic acid on platelet aggregation. However, due to the limitations of these data and the imprecision in extrapolating ex vivo data to the clinical situation, reliable conclusions regarding the continued use of ibuprofen cannot be drawn. The development of clinically significant effects is considered unlikely with episodic use of ibuprofen. | |
Lithium preparations | NSAIDs may decrease lithium excretion. | |
Hypotensive agents, beta-adrenoblockers, and diuretics | NSAIDs may reduce the antihypertensive effects of hypotensive agents, including ACE inhibitors, angiotensin II receptor antagonists, beta-adrenoblockers and diuretics. Also, diuretics may increase the risk of nephrotoxic effects of NSAIDs. | |
Methotrexate | NSAIDs may inhibit tubular secretion of methotrexate and decrease methotrexate clearance. | |
Cyclosporine | The use of NSAIDs increases the risk of nephrotoxicity. | |
Tacrolimus | Simultaneous use of NSAIDs and tacrolimus may increase the risk of nephrotoxicity. | |
Zidovudine | Concomitant use of NSAIDs and zidovudine increases the risk of hematologic toxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive patients with hemophilia who received concomitant treatment with zidovudine and ibuprofen. | |
Quinolone antibiotics | Data from animal studies suggest that NSAIDs may increase the risk of seizures associated with quinolone antibiotics. Patients taking NSAIDs and quinolones may be at increased risk of seizures. | |
CYP2C9 isoenzyme inhibitors | Concurrent use of ibuprofen and CYP2C9 isoenzyme inhibitors may enhance the effects of ibuprofen (a CYP2C9 isoenzyme substrate). During the study with voriconazole and fluconazole (CYP2C9 isoenzyme inhibitors) it was shown that 8(+)-ibuprofen content in the body was increased by about 80-100%. When concomitant use with CYP2C9 isoenzyme inhibitors, consider reducing the dose of ibuprofen, in particular when using ibuprofen in high doses with voriconazole or fluconazole. | |
Sulfonylurea drugs | NSAIDs may increase the effects of sulfonylurea drugs. Rare cases of hypoglycemia have been reported in patients concomitantly taking sulfonylureas and ibuprofen. | |
Colestiramine | Simultaneous use of ibuprofen and colestiramine may decrease the absorption of ibuprofen in the GI tract. However, the clinical significance of this phenomenon is unknown. | |
Aminoglycosides | NSAIDs may decrease excretion of aminoglycosides. | |
Herbal extracts | Simultaneous use of NSAIDs and ginkgo biloba extract may increase the risk of bleeding. | |
Mifepristone | Due to the antiprostaglandin properties of NSAIDs, including acetylsalicylic acid, it is theoretically possible that the effectiveness of the drug may decrease. Limited data suggest that concomitant use of NSAIDs on the day of prostaglandin administration has no adverse effect on mifepristone efficacy or prostaglandin action on cervix or uterine contractions, and does not reduce the clinical effectiveness of medical termination of pregnancy. |
Special Instructions
Gastrointestinal bleeding, ulcers and perforations
Use Brufen CP with caution in patients with a history of penthic ulcers and other gastrointestinal conditions, as exacerbation of these conditions is possible.
Cases of gastrointestinal bleeding, ulceration or perforation have been reported with all NSAIDs during any treatment period. These adverse events may be life-threatening and may occur in the presence/absence of warning symptoms or a history of serious gastrointestinal disease. The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing doses of Brufen CP in patients with peptic ulcer disease, especially those with a history of bleeding or perforation, and in the elderly. In these patients, treatment should be started with the lowest dose.
In this group of patients, as well as in patients requiring concomitant therapy with low-dose acetylsalicylic acid or other drugs that may increase the risk of gastrointestinal disease, combination therapy with gastroprotectors (such as misoprostol or proton pump inhibitors) should be considered.
Simultaneous use of Brufen CP and other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors, should be avoided due to increased risk of ulceration or bleeding.
Patients with a history of gastrointestinal disease, especially elderly patients, should report any unusual abdominal symptoms (especially gastrointestinal bleeding) during initial treatment.
Caution should be exercised when using Brufen CP in patients concomitantly receiving medications that may increase the risk of ulceration or bleeding, such as oral glucocorticosteroids, anticoagulants (including warfarin), selective serotonin reuptake inhibitors or antiaggregant drugs, including acetylsalicylic acid.
If gastrointestinal bleeding or ulceration occurs, therapy with Brufen CP should be discontinued.
Respiratory disorders
Caution should be exercised when using Brufen CP in patients with bronchial asthma, chronic rhinitis or allergic diseases, including a history of bronchospasm, urticaria or angioedema have been reported in this group of patients.
Heart failure, renal and hepatic impairment
Caution should be exercised when using Brufen CP in patients with renal, hepatic or cardiac impairment, as taking NSAIDs may lead to worsening of renal function. Simultaneous treatment with several analgesics further increases this risk. In patients with renal, hepatic or cardiac insufficiency, the minimum effective dose should be used for the shortest possible period of time and renal function should be monitored, especially during long-term treatment.
Cardiovascular and cerebrovascular disorders
Use Brufen CP with caution in patients with a history of heart failure or arterial hypertension, as cases of edema have been reported with ibuprofen.
Data from epidemiologic studies suggest that use of ibuprofen at a high dose (2400 mg daily) and with long-term treatment may be associated with a small increase in the risk of arterial thrombotic complications, including myocardial infarction or stroke. Epidemiological studies have not shown that the use of ibuprofen at a low dose (< 1200 mg per day) is associated with an increased risk of arterial thrombotic complications, in particular myocardial infarction.
Therapy with Brufen CP in patients with uncontrolled arterial hypertension, heart failure, CHD, peripheral artery disease and/or cerebrovascular disease should only be undertaken after a thorough benefit/risk assessment. Similar assessment should also be performed before prescribing long-term treatment for patients with cardiovascular risk factors (such as arterial hypertension, hyperlipidemia, diabetes mellitus, smoking).
Dermatological disorders
Very rare cases of serious skin reactions, including life-threatening, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis have been reported when using NSAIDs. Patients are at greatest risk of developing these reactions during the initial phase of therapy. In most cases, the reaction develops during the first month of treatment. If skin rash, mucosal lesions or any other signs of hypersensitivity first appear, Brufen CP should be discontinued.
Renal disorders
Caution should be exercised when initiating therapy with Brufen CP in patients with significant dehydration. There is a risk of renal failure, especially in children and adolescents with dehydration.
Prolonged use of ibuprofen, as well as other NSAIDs, has resulted in the development of medullary renal necrosis and other pathological changes in the kidneys. Also renal toxicity was observed in patients in whom “renal” prostaglandins play a compensatory role in maintaining renal perfusion. Use of NSAIDs in this group of patients may lead to a dose-dependent decrease in prostaglandin production and, secondarily, in renal blood flow, which may cause renal failure.
Patients with impaired renal function, heart failure, impaired liver function, those taking diuretics, ACE inhibitors, as well as elderly patients are at increased risk of this reaction. After discontinuation of NSAIDs, there is usually a recovery before treatment.
Hematologic disorders
Brufen CP, like other NSAIDs, may inhibit platelet aggregation and increase bleeding time in healthy patients.
Aseptic meningitis
Aseptic meningitis has rarely developed in patients treated with ibuprofen. Although aseptic meningitis is most likely to occur in patients with systemic lupus erythematosus and related connective tissue diseases, cases of aseptic meningitis have been reported in patients without this chronic disease.
Elderly patients
In elderly patients, the use of NSAIDs may be accompanied by an increased incidence of adverse reactions, especially perforation and gastrointestinal bleeding, which may be life-threatening.
May affect responsiveness. During treatment, caution should be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and rapid psychomotor reactions.
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Synopsis
White oblong, film-coated tablets with “BRUFEN RETARD” printed on one side in red-brown.
Contraindications
– complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including history). In anamnesis);
– severe heart insufficiency;
– severe hepatic insufficiency;
– active liver disease;
– severe renal insufficiency (CK <30 ml/min);
– progressive renal disease;
– haemophilia and other coagulation disorders (including
– hemophilia and other blood clotting disorders (including hypocoagulation), hemorrhagic diathesis;
– gastrointestinal bleeding or perforations in anamnesis, associated with previous use of NSAIDs;
– ulcerative colitis, Crohn’s disease, recurrent ulcer disease or gastrointestinal bleeding (determined by two or more separate episodes of confirmed ulcer or bleeding), including in anamnesis;
– condition after aortocoronary bypass;
– confirmed hyperkalemia;
– inflammatory bowel disease;
– intracranial hemorrhage;
– pregnancy (III trimester);
– breastfeeding period;
– children under 12 years old.
A single episode of gastrointestinal erosive-ulcer disease in the anamnesis (including peptic ulcer); concurrent use of oral GBS (including prednisolone).Prednisolone), anticoagulants (incl.anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline); long-term use of NSAIDs; bronchial asthma, chronic rhinitis or allergic diseases (including history); liver failure and/or chronic renal failure (creatinine clearance 30-60 ml/min); heart failure; arterial hypertension; coronary heart disease; cerebrovascular disease; dyslipidemia/hyperlipidemia; diabetes; peripheral artery disease; smoking; presence of H. pylori; frequent use of alcohol; severe somatic diseases; systemic lupus erythematosus or other autoimmune connective tissue diseases (increased risk of aseptic meningitis); blood diseases of unclear etiology (leukopenia and anemia); cirrhosis with portal hypertension; nephrotic syndrome; hyperbilirubinemia; gastritis; enteritis; colitis; dehydration state; pregnancy (I-II trimester), old age.
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Side effects
The side effects observed with ibuprofen are common to the entire class of NSAIDs. Unwanted effects can be minimized by using the lowest effective dose for the short period of time needed to relieve symptoms.
All adverse reactions considered to have at least a possible association with ibuprofen use are presented by organ system and frequency of occurrence: Very common (≥1/10), common (≥1/100 to < 1/10), infrequent (≥1/1000 to < 1/100), rare (≥1/10000 to < 1/1000), very rare (< 1/10000) and frequency unknown (cannot estimate frequency based on available data).
An organ system | Frequency | Unintended effect | |
Infectious diseases1 | Infrequent | Rhinitis | |
Aseptic meningitis | |||
Disorders of the blood and lymphatic system | Rarely | Anemia (including hemolytic, aplastic) Thrombocytopenia Neutropenia Agranulocytosis /p> Leukopenia | |
Immune system disorders | Rarely | Anaphylactic reaction | |
Mental disorders | Infrequent | Insomnia Anxiety | |
Rarely | Depression Confusion | Frequency unknown | Hallucinations |
Nervous system disorders | Frequent | Headache Dizziness | |
Infrequent | Paresthesia Sleepiness | Rarely | Optic neuritis |
Visual disturbances | Infrequent | Visual disturbances | |
Rarely | Toxic optical neuropathy | ||
Hearing and labyrinth disorders | Infrequent | Hearing impairment /p> Ringing or tinnitus Vertigo | |
Heart disturbances | p> Very rare | Worsening heart failure Myocardial infarction | |
Very rare | Increased blood pressure < | ||
Respiratory, thoracic, and mediastinal disorders | Infrequent | Aggravation of bronchial asthma Bronchospasm Dyspnea | |
Gastrointestinal (GI) disorders | Often | ||
Infrequent | Gastritis Gastric and/or duodenal ulcer Eraging of oral mucosa /p> Gastrointestinal mucosal perforation | ||
Very rare | Pancreatitis | ||
Frequency unknown | Aggravation of colitis and Crohn’s disease Aphthous stomatitis | ||
Disorders of the liver and biliary tract | Infrequent /td> | Hepatitis Jaundice Impaired liver function | |
Very rarely | Hepatic failure | ||
Skin and subcutaneous tissue disorders2 | Often | Skin rash | |
Infrequent | Urticaria Cutaneous itching Hemorrhagic rash Angioneurotic edema Photosensitization | ||
Very rare | Multiform exudative erythema Bullous dermatosis (incl.ч. Stevens-Johnson syndrome) Toxic epidermal necrolysis (Lyell syndrome) | ||
Renal and urinary tract disorders | Infrequent | Tubulointerstitial nephritis (including.ч. Allergic nephritis) Nephrotic syndrome Renal failure | |
General disorders | . Often | Elevated fatigue | |
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1 – cases of exacerbation of inflammation caused by infections (e.g., development of necrotizing fasciitis) have been described when using NSAIDs. If when using ibuprofen the patient shows signs of infection or the course of infection worsens, the patient should immediately consult a physician.
2 – In exceptional cases, serious skin infection and soft tissue abnormalities may occur with chickenpox infection.
3 – Evidence from clinical and epidemiologic studies suggests that use of ibuprofen (at a high dose of 2400 mg daily) and with long-term treatment may be associated with a small increase in the risk of arterial thrombotic complications, including myocardial infarction or stroke.
Overdose
Toxicity: In children and adults when taking ibuprofen in doses less than 100 mg/kg there are usually no signs and symptoms of toxicity. However, in some cases symptomatic therapy may be required. In children, the appearance of symptoms of toxicity has been observed after administration of ibuprofen in doses of 400 mg/kg or more. Most patients with ibuprofen overdose experience symptoms 4-6 hours after ingestion.
Symptoms: the most frequently reported symptoms of overdose are nausea, vomiting, abdominal pain, lethargy and drowsiness. Central nervous system (CNS) disorders include headache, tinnitus, dizziness, depression, seizures, and loss of consciousness. Nystagmus, metabolic acidosis, hypothermia, impaired renal function, gastrointestinal bleeding, coma, respiratory arrest, CNS and respiratory system suppression have also rarely been reported.
Cases of cardiovascular toxicity, including arterial hypotension, bradycardia and tachycardia, have been reported. In cases of significant overdose acute renal failure and liver damage are possible. Overdose with high doses of Brufen CP is usually well tolerated if no other drugs are taken at the same time.
Treatment: There is no specific antidote. In case of overdose, gastric lavage (within the first hour of ingestion) and supportive therapy are recommended. In the presence of symptoms of the gastrointestinal tract – antacid drugs. If arterial hypotension develops, intravenous infusion and, if required, inotropic support. Drinking, forced diuresis and symptomatic therapy (correction of COS, electrolyte balance, BP).
Pregnancy use
Reproduction, Pregnancy and Childbirth
In the first to second trimesters of pregnancy, Brufen CP should only be taken if strictly necessary and if the potential benefit to the mother outweighs the potential risk to the fetus and child. Use of Brufen CP in the third trimester of pregnancy is contraindicated and, as with the use of all prostaglandin synthesis inhibitors, carries the following risks to the fetus:
– cardiopulmonary toxicity (premature closure of the arterial duct and arterial hypertension);
– impaired renal function, with further possibility of renal failure and reduction of amniotic fluid volume.
During labor, ibuprofen, as well as all inhibitors of prostaglandin synthesis, exposes the mother and the newborn to the following risks:
– increased bleeding time;
– inhibition of uterine contractile activity, which may lead to a delay or increase the duration of labor.
In this regard, it is not recommended to take ibuprofen during labor activity. The use of ibuprofen may adversely affect female fertility and is not recommended for women planning pregnancy.
If ibuprofen is prescribed to women planning pregnancy, as well as in the I or II trimesters of pregnancy, the doses and duration of ibuprofen therapy should be reduced as much as possible. In women who have difficulty conceiving or who are undergoing infertility studies, consideration should be given to withdrawing ibuprofen therapy.
Breastfeeding
Due to the limited data available on the penetration of ibuprofen into breast milk at very low concentrations, use of Brufen CP while breastfeeding is not recommended.
Similarities
Nurofen, Nurofen Express, Ibuprofen, Dolgit, Ibuprofen-Chemopharm, Nurofen Forte, MIG 400, Faspik, Nurofen Express Lady, Nurofen Express Forte, Nurofen Kids, Next Uno Express, Nurofast
Weight | 0.540 kg |
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Shelf life | 3 years. Do not use the drug after the expiration date. |
Conditions of storage | At a temperature not higher than 25 ° C. Keep out of reach of children. |
Manufacturer | Famar A.V.E., Greece |
Medication form | sustained release tablets |
Brand | Famar A.V.E. |
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