Properties
What is it?
Ibuprofen-Akos Trade name: Ibuprofen International Nonproprietary Name: Ibuprofen Chemical name: (2RS)-2-[4-(2-methylpropyl)phenyl]-propionic acid Dosage form: Film-coated tablet Composition: 1 tablet contains: Core: Active substance: Ibuprofen - 400 mg. Excipients: Povidone (Kollidon 90 F), microcrystalline cellulose, talc, crospovidone (Kollidon CL, Kollidon CL-F), calcium stearate, colloidal silicon dioxide (Aerosil), corn starch. Coating: Hypromellose (hydroxypropyl methylcellulose), titanium dioxide, macrogol 4000 (polyethylene oxide 4000, polyethylene glycol 4000). Description: Tablets are white or almost white, biconvex oval tablets, film-coated. The cross-section shows a single layer of white or almost white color. Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID). Pharmacological properties Pharmacodynamics The mechanism of action of ibuprofen, a propionic acid derivative from the group of non-steroidal anti-inflammatory drugs (NSAIDs), is due to the inhibition of prostaglandin synthesis - mediators of pain, inflammation, and hyperthermic reactions. It non-selectively blocks cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), thereby inhibiting prostaglandin synthesis. It has a rapid analgesic (pain-relieving), antipyretic, and anti-inflammatory effect. In addition, ibuprofen reversibly inhibits platelet aggregation. The analgesic effect of the drug lasts up to 8 hours. Pharmacokinetics Ibuprofen is rapidly and almost completely absorbed from the gastrointestinal tract, with maximum plasma concentration reached 1-2 hours after administration, and in synovial fluid - 3 hours. It binds to plasma proteins by 99%. It slowly penetrates into the joint cavity, accumulates in the synovial tissue, and forms a higher concentration there than in plasma. Ibuprofen is mainly metabolized in the liver. The half-life (T1/2) from plasma is 2-3 hours. It is excreted by the kidneys in the form of metabolites (no more than 1% is excreted unchanged), and to a lesser extent with bile. Ibuprofen is completely excreted within 24 hours. Indications for use Ibuprofen is used for headaches, migraines, toothaches, painful menstruation, neuralgia, back pain, muscle, rheumatic, and joint pain; also for fever in influenza and colds. Contraindications - Hypersensitivity to ibuprofen or any of the excipients of the preparation; - Complete or incomplete combination with bronchial asthma, recurrent nasal polyposis and paranasal sinuses, and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in history); - Erosive and ulcerative diseases of the gastrointestinal tract (including gastric and duodenal ulcer, Crohn's disease, ulcerative colitis) or active phase of gastrointestinal bleeding or history (two or more confirmed episodes of ulcerative disease or gastrointestinal bleeding). - History of gastrointestinal bleeding or perforation of an ulcer provoked by the use of non-steroidal anti-inflammatory drugs; - Severe heart failure (NYHA Class IV - New York Heart Association classification) - Severe liver failure or active liver disease; - Severe renal failure (creatinine clearance < 30 ml/min), confirmed hyperkalemia; - Decompensated heart failure; - Postoperative period after coronary artery bypass grafting; cerebrovascular or other bleeding; - Hemophilia and other blood clotting disorders (including hypocoagulation), hemorrhagic diathesis; - Pregnancy for more than 20 weeks; - Children under 12 years of age. Precautions: If you have any of the conditions listed in this section, consult your doctor before using the preparation. Simultaneous use of other non-steroidal anti-inflammatory drugs, a single episode of gastric and duodenal ulcer or gastrointestinal bleeding in history; gastritis, enteritis, colitis, Helicobacter pylori infection, ulcerative colitis; bronchial asthma or allergic diseases in the acute stage or in history - bronchospasm may develop; systemic lupus erythematosus or mixed connective tissue disease (Sharpe's syndrome) - increased risk of aseptic meningitis; renal failure, including dehydration (creatinine clearance 30-60 ml/min), nephrotic syndrome, liver failure, liver cirrhosis with portal hypertension, hyperbilirubinemia, arterial hypertension and/or heart failure, cerebrovascular diseases, blood diseases of unknown etiology (leukopenia and anemia), severe somatic diseases, dyslipidemia/hyperlipidemia, peripheral arterial disease, smoking, frequent alcohol consumption, phenylketonuria or phenylalanine intolerance, simultaneous use of drugs that may increase the risk of ulcers or bleeding, especially simultaneous use of oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), selective serotonin reuptake inhibitors (including acetylsalicylic acid, clopidogrel), pregnancy I-II trimester, lactation, elderly age. Use during pregnancy and breastfeeding Use of the preparation should be avoided from the 20th week of pregnancy; if necessary, the preparation should be taken after consulting a doctor. Non-steroidal anti-inflammatory drugs should not be used by women from the 20th week of pregnancy due to the possible development of oligohydramnios and/or kidney disease in newborns (neonatal kidney dysfunction). There is evidence that small amounts of ibuprofen can pass into breast milk without any negative impact on the infant's health, so breastfeeding usually does not need to be discontinued with short-term use of the medication. If long-term use of the preparation is necessary, consult a doctor to decide whether to discontinue breastfeeding during the period of medication use. Dosage and administration Adults, the elderly, and children over 12 years of age: The daily dose is 1200 mg (should not exceed 3 tablets of 400 mg in 24 hours). Tablets should be taken with water, preferably during or after meals. Do not take more often than every 4 hours. Do not exceed the indicated dose! The course of treatment should not exceed 5 days without consulting a doctor. If symptoms persist, consult a doctor. Do not use in children under 12 years of age without consulting a doctor. Side effects The risk of side effects can be minimized if the preparation is taken for a short course, at the lowest effective dose necessary to eliminate symptoms. In the elderly, there is an increased incidence of adverse reactions, especially gastrointestinal bleeding and perforation, in some cases fatal, against the background of NSAID use. Side effects are primarily dose-dependent. In particular, the risk of developing gastrointestinal bleeding depends on the dose range and duration of treatment. The following side effects were observed with short-term use of ibuprofen at doses not exceeding 1200 mg per day (3 tablets of 400 mg). Other adverse reactions may develop during the treatment of chronic diseases and with long-term use. The frequency of adverse reactions is assessed based on the following criteria: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), rare (≥ 1/10,000 to < 1/1000), very rare (< 1/10,000), frequency unknown (data for frequency assessment are not available). Disorders of the blood and lymphatic system Very rarely: Hematopoietic disorders (anemia, leukopenia, aplastic anemia, hemolytic anemia, thrombocytopenia, pancytopenia, agranulocytosis). The first symptoms of such disorders are fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe weakness, nosebleeds and subcutaneous hemorrhages, bleeding and bruising of unknown etiology. Immune system disorders Rarely: Hypersensitivity reactions - non-specific allergic reactions and anaphylactic reactions, respiratory tract reactions (including bronchial asthma, its exacerbation, bronchospasm, shortness of breath, dyspnea), skin reactions (itching, urticaria, purpura, angioedema, exfoliative and bullous dermatoses, including toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, erythema multiforme), allergic rhinitis, eosinophilia. Very rarely: Severe hypersensitivity reactions, including swelling of the face, tongue, and throat, shortness of breath, tachycardia, arterial hypotension (anaphylaxis, angioedema, or severe anaphylactic shock). Gastrointestinal disorders Uncommon: Abdominal pain, nausea, dyspepsia (including heartburn, bloating). Rarely: Diarrhea, flatulence, constipation, vomiting. Very rarely: Peptic ulcer, perforation or gastrointestinal bleeding, melena, hematemesis, in some cases fatal, especially in elderly patients, ulcerative stomatitis, gastritis. Frequency unknown: Exacerbation of colitis and Crohn's disease. Liver and biliary tract disorders Very rarely: Impaired liver function, increased activity of "liver" transaminases, hepatitis and jaundice. Kidney and urinary tract disorders Very rarely: Acute renal failure (compensated and decompensated), especially with prolonged use, with an increase in urea concentration in blood plasma and the development of edema, hematuria and proteinuria, nephritic syndrome, nephrotic syndrome, papillary necrosis, interstitial nephritis, cystitis. Nervous system disorders Uncommon: Headache. Very rarely: Aseptic meningitis. Cardiovascular system disorders Frequency unknown: Heart failure, peripheral edema, prolonged use increases the risk of thrombotic complications (e.g., myocardial infarction), increased blood pressure. Respiratory and mediastinal disorders Frequency unknown: Bronchial asthma, bronchospasm, shortness of breath. Laboratory indicators - Hematocrit or hemoglobin (may decrease); - Bleeding time (may increase); - Plasma glucose concentration (may decrease); - Creatinine clearance (may decrease); - Plasma creatinine concentration (may increase); - "Liver" transaminase activity (may increase). If side effects develop, discontinue the preparation and consult a doctor. Overdose Do not exceed the indicated dose. In case of overdose, seek medical attention or the nearest medical facility immediately. Take the medication package with you. Symptoms: Abdominal pain, nausea, vomiting, lethargy, drowsiness, depression, headache, tinnitus, metabolic acidosis, coma, acute renal failure, decreased blood pressure, bradycardia, tachycardia, atrial fibrillation, respiratory arrest. Treatment: Gastric lavage (only within one hour of ingestion), activated charcoal, alkaline drink, forced diuresis, symptomatic therapy (correction of acid-base balance, blood pressure). Interactions with other medicinal products Simultaneous use of ibuprofen with the following medicinal products should be avoided: - Acetylsalicylic acid: except for low doses of acetylsalicylic acid prescribed by a doctor (not more than 75 mg per day), as combined use may increase the risk of side effects. With simultaneous use of ibuprofen, the anti-inflammatory and antiplatelet effect of acetylsalicylic acid is reduced (an increase in the incidence of acute coronary insufficiency may occur in patients taking low doses of acetylsalicylic acid as an antiplatelet agent after starting ibuprofen); - Other non-steroidal anti-inflammatory drugs, especially COX-2 selective inhibitors: Simultaneous use of two or more drugs from the NSAID group should be avoided due to the possible increased risk of side effects; Use with caution with the following preparations: - Anticoagulants and thrombolytic agents: Non-steroidal anti-inflammatory drugs can enhance the action of anticoagulants, especially warfarin, and thrombolytic agents; - Antihypertensive agents (ACE inhibitors and angiotensin II antagonists) and diuretics: Non-steroidal anti-inflammatory drugs can reduce the effect of drugs in these groups. In some patients with impaired renal function (e.g., in patients with dehydration or elderly patients with impaired renal function), the simultaneous use of ACE inhibitors or angiotensin II antagonists and cyclooxygenase inhibitors may lead to deterioration of renal function, including the development of acute renal failure (usually reversible). This interaction should be considered in patients taking COX inhibitors together with ACE inhibitors or angiotensin II antagonists. In this regard, the combined use of the above-mentioned agents should be prescribed with caution, especially in the elderly. Dehydration should be prevented in patients, and monitoring of renal function should be considered after the start of such combination therapy and periodically thereafter. Diuretics and ACE inhibitors can increase the nephrotoxicity of NSAIDs; - Glucocorticosteroids: Increased risk of gastrointestinal ulcers and gastrointestinal bleeding; - Antiplatelet agents and selective serotonin reuptake inhibitors: Increased risk of gastrointestinal bleeding. - Cardiac glycosides: Simultaneous use of NSAIDs and cardiac glycosides can lead to worsening of heart failure, decreased glomerular filtration rate, and increased concentration of cardiac glycosides in blood plasma; - Lithium preparations: There is evidence of an increased probability of increased lithium concentration in blood plasma against the background of NSAID use; - Methotrexate: There is evidence of an increased probability of increased methotrexate concentration in blood plasma against the background of NSAID use; - Cyclosporine: Increased risk of nephrotoxicity with simultaneous administration of NSAIDs and cyclosporine; - Mifepristone: NSAID intake should begin no earlier than 8-12 days after mifepristone intake, as NSAIDs can reduce the effect of mifepristone; - Tacrolimus: With simultaneous administration of NSAIDs and tacrolimus, the risk of nephrotoxicity may increase; - Zidovudine: Simultaneous use of NSAIDs and zidovudine can lead to increased hematotoxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive patients with hemophilia undergoing concomitant treatment with zidovudine and ibuprofen; - Quinolone antibiotics: In patients receiving concomitant treatment with NSAIDs and quinolone antibiotics, the risk of seizures may increase; - Myelotoxic drugs: Increased hematotoxicity; - Cefamandole, Cefoperazone, Cefotetan, Valproic acid, Plicamycin: Increased incidence of hypoprothrombinemia; - Drugs that block tubular secretion: Decreased excretion and increased plasma concentration of ibuprofen; - Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants): Increased production of hydroxylated active metabolites, risk of severe intoxication; - Inhibitors of microsomal oxidation: Reduced risk of hepatotoxicity; - Oral hypoglycemic agents and insulin, sulfonylurea derivatives: Enhanced effect of drugs; - Antacids and cholestyramine: Decreased absorption; - Uricosuric drugs: Decreased effect of drugs; - Caffeine: Enhanced analgesic effect. Special instructions It is recommended to take the preparation for the shortest possible course and at the minimum effective dose necessary to eliminate symptoms. If you need to take the preparation for more than 10 days, you should consult a doctor. In patients with bronchial asthma or allergic diseases in the acute stage, as well as in patients with a history of bronchial asthma/allergic diseases, the preparation may provoke bronchospasm. In patients with systemic lupus erythematosus or mixed connective tissue disease, the use of the preparation is associated with an increased risk of aseptic meningitis. During long-term treatment, it is necessary to monitor the peripheral blood count and the functional state of the liver and kidneys. In case of symptoms of gastropathy, careful monitoring is necessary, including esophagogastroduodenoscopy, complete blood count (hemoglobin determination), stool analysis for occult blood. If 17-ketosteroids need to be determined, the preparation should be discontinued 48 hours before the study. Alcohol consumption is not recommended during treatment. Patients with renal failure should consult a doctor before using the preparation, as there is a risk of deterioration of renal function. Patients with hypertension, including those with a history and/or chronic heart failure, should consult a doctor before using the preparation, as the preparation may cause fluid retention, increased blood pressure, and edema. In patients with uncontrolled hypertension, congestive heart failure of NYHA class II-III, coronary artery disease, peripheral arterial and/or cerebrovascular disease, ibuprofen should be prescribed only after careful assessment of the benefit-risk ratio and after ibuprofen use. High doses of ibuprofen (≥ 2400 mg/day) should be avoided. The use of NSAIDs in patients with chickenpox may be associated with an increased risk of severe purulent complications of infectious and inflammatory diseases of the skin and subcutaneous fat (e.g., necrotizing fasciitis). In this regard, it is recommended to discontinue the use of the preparation for chickenpox. Information for women planning pregnancy: The preparation inhibits cyclooxygenase and prostaglandin synthesis, affects ovulation, disrupts female reproductive function (reversible after discontinuation of treatment). Effect of the medicinal product on the ability to drive vehicles and operate machinery Patients who experience dizziness, drowsiness, lethargy, or visual disturbances while taking ibuprofen should avoid driving or operating machinery. Dosage form Film-coated tablets 400 mg. 10 tablets in a contour cell package made of polyvinyl chloride film and printed aluminum foil. 5 contour cell packages together with the instructions for use are placed in a cardboard box. Storage conditions Store at a temperature not exceeding 30°C in the original packaging (cardboard box). Keep out of reach of children. Shelf life 3 years. Do not use after the expiry date. Dispensing category: Pharmaceutical product group III, available without a prescription. See also: Ibuprofen - Ibuprofen 400 mg 20 tablets
