Pharmacological properties
Pharmacodynamics. Ibuprom - NSAID, a derivative of phenylpropionic acid. It has analgesic, antipyretic and anti-inflammatory effects. The mechanism of action is to inhibit the synthesis of prostaglandins - mediators of pain, inflammation and temperature reactions. In addition, ibuprofen can inhibit platelet aggregation.
Pharmacokinetics. When taken orally, ibuprofen is rapidly and well absorbed from the gastrointestinal tract - partly in the stomach and then completely in the small intestine. The bioavailability of ibuprofen is 71%.
The onset of the therapeutic effect of Ibuprom Max in symptomatic treatment occurs within 15-30 minutes after administration.
The capsule of the drug Ibuprom Extra contains 400 mg of ibuprofen, which is in a hydrophilic solvent. The active substance is contained in a gelatin capsule. During digestion, the gelatin shell disintegrates in gastric juice, releasing ibuprofen, ready for immediate absorption. C max in blood plasma is reached already 30 minutes after administration.
When using tablets, C max is reached 1-2 hours after administration (when taken on an empty stomach - after 45 minutes).
Comparative studies with ibuprofen capsules 400 mg and tablets 2 × 200 mg showed that C max in blood plasma was achieved almost 3 times faster with capsules (32.5 min) than with tablets (90 min). Thus, the analgesic effect of Ibuprom Extra occurs almost 3 times faster than with ibuprofen tablets.
C max of the active substance in the synovial fluid is reached 3 hours after application.
Ibuprofen is metabolized in the liver, turning into carboxylated and hydroxylated derivatives. It is excreted by the kidneys (90%) in unchanged form and in the form of metabolites, as well as with bile. T ½ in healthy people is about 2 hours, in patients with liver and / or kidney diseases - 1.8-3.5 hours. In the elderly, there are no significant differences in the pharmacokinetic profile. Binding to plasma proteins is 99%.
Indication
Symptomatic therapy for headache and toothache, dysmenorrhea (menstrual pain), back pain, joint pain, muscle pain, rheumatic pain, as well as cold and flu symptoms.
Ibuprom Max and Ibuprom Extra also: migraine, neuralgia.
Application
For oral administration. Elderly people do not require special dose selection, except in cases of severe renal or hepatic insufficiency. Patients with mild or moderate renal and hepatic impairment do not require dose adjustment. If symptoms of the disease persist for more than 3 days, you should consult a doctor to clarify the diagnosis and correct the treatment regimen.
Ibuprom, tablets 200 mg. The minimum effective dose should be used for a short period (no more than 5 days) necessary to eliminate pain symptoms, or no more than 3 days to eliminate fever symptoms. If it is necessary to use the drug for more than 5 days (if symptoms do not disappear), you should consult a doctor for advice.
The drug is prescribed for adults and children weighing 20 kg (from 6 years of age). Usually used at a rate of 20 to 30 mg/kg of body weight per day. Do not exceed the dose of 30 mg/kg/day.
Children weighing 20-30 kg (aged 6 to 11 years) are prescribed a dose of 200 mg (1 tablet), a second dose, if necessary, is taken after 6 hours, but in no case should more than 600 mg (3 tablets) be used per day.
Adults and children weighing 30 kg are prescribed 200-400 mg (1-2 tablets) every 4-6 hours as needed. The tablets are washed down with water. Do not use more than 1200 mg (6 tablets) within 24 hours.
Ibuprofen is taken during or after meals, without chewing. Patients with increased stomach sensitivity are recommended to take the drug with meals.
The duration of treatment is determined individually depending on the course of the disease and the patient's condition.
Ibuprom Sprint Caps. For adults and children weighing ≥40 kg, the recommended initial dose is 1-2 capsules, then, if necessary, 1-2 capsules (200-400 mg ibuprofen) every 4-6 hours. Do not use more than 6 capsules (1200 mg) within 24 hours.
Children weighing ≤39 kg. The drug can be used in children weighing 20 kg (approximately 6 years). The maximum daily dose of ibuprofen is 20-30 mg/kg body weight, divided into 3-4 doses with an interval of 6-8 hours. Do not exceed the maximum permissible daily dose.
Children weighing 20-29 kg: the recommended starting dose is 1 capsule (equivalent to 200 mg ibuprofen). The maximum daily dose is 3 capsules (equivalent to 600 mg ibuprofen).
Children weighing 30-39 kg: the recommended initial dose is 1 capsule (equivalent to 200 mg ibuprofen). The maximum daily dose is 4 capsules (equivalent to 800 mg ibuprofen).
Capsules are usually taken during meals, without chewing and with water.
Ibuprom Max. For short-term use. Regardless of meals.
Adults and children over 12 years of age: 1 tablet every 4-6 hours. The tablets should be taken with water. Do not take more than 3 tablets in 24 hours. The maximum daily dose is 1200 mg.
Ibuprom Extra. Adults and children over 12 years of age: 1 capsule every 4 hours after meals. No more than 3 capsules per day (maximum daily dose - 1200 mg in several doses). Capsules should not be chewed.
Contraindication
Hypersensitivity to ibuprofen or any of the components of the drug. allergic reactions (urticaria, rhinitis, angioedema, urticaria) associated with the use of the drug, acetylsalicylic acid or other non-steroidal anti-inflammatory drugs. hemorrhagic diathesis. use of the drug simultaneously with other NSAIDs, including specific COX-2 inhibitors. gastrointestinal bleeding or perforation in history, associated with the use of non-steroidal anti-inflammatory drugs. gastric ulcer and / or bleeding in active form or recurrences in history (≥2 clear episodes of exacerbation of gastric / duodenal ulcer or bleeding). severe renal, cardiac or hepatic failure, coronary artery disease or severe heart failure. cerebrovascular or other forms of bleeding. bleeding of unclear etiology. dehydration caused by vomiting, diarrhea or insufficient fluid intake. disorders of blood formation or blood clotting. children weighing 20 kg.
Side effects
Edema, increased heart rate, and heart failure have been reported when treated in combination with other NSAIDs.
The use of ibuprofen (especially in high doses of 2400 mg daily), as well as long-term use, may lead to a small increased risk of arterial thrombotic events (e.g. myocardial infarction or stroke).
Hypersensitivity reactions have been reported: non-specific allergic reactions, anaphylaxis and respiratory tract reactivity, e.g. asthma, exacerbation of asthma, bronchospasm, dyspnoea, various skin reactions, e.g. rash, pruritus, urticaria, purpura, angioedema and very rarely exfoliative and bullous dermatitis (including epidermal necrolysis and erythema multiforme).
With long-term treatment for chronic conditions, additional side effects are possible.
The list of side effects below is related to side effects observed with short-term use of ibuprofen in over-the-counter preparations.
Adverse reactions occurring with the use of ibuprofen, as with other NSAIDs, are classified by organ system and frequency of occurrence: very common (≥1/10); common (≥1/100, 1/10); uncommon (≥1/1000, 1/100); rare (≥1/10,000, 1/1000); very rare (1/10,000) and unknown (cannot be estimated due to the limited available data).
On the part of the digestive system: infrequently - stomach pain, dyspepsia, nausea; rarely - diarrhea, flatulence, constipation and vomiting; very rarely - melena, bloody vomiting, sometimes fatal cases (especially in the elderly), ulcerative stomatitis, gastritis, pancreatitis, gastric / duodenal ulcer, perforation or gastrointestinal bleeding, which can in some cases lead to death (especially in the elderly), exacerbation of ulcerative colitis and Crohn's disease; unknown - heartburn, ulceration of the oral mucosa, esophagitis, development of diaphragmatic strictures of the intestine.
From the nervous system: infrequently - headache; rarely - aseptic meningitis (more often in patients with autoimmune diseases); very rarely - dizziness, irritability, nervousness, tinnitus, depression, drowsiness, insomnia, anxiety, psychomotor agitation, emotional instability, convulsions; paresthesia, confusion, hallucinations.
On the part of the respiratory system: unknown - respiratory distress.
Cardiovascular and cerebrovascular reactions: very rarely - edema, hypertension and heart failure have been reported in the treatment of NSAIDs; rarely - cerebrovascular complications, arterial hypotension, palpitations; unknown - increased heart rate; tachycardia, increased blood pressure, myocardial infarction.
From the urinary system: very rarely - acute renal failure, papillonecrosis, especially with prolonged use, in combination with increased blood urea and edema; unknown - renal failure, nephrotoxicity, including interstitial nephritis and nephrotic syndrome. Cystitis, hematuria, oliguria, polyuria, tubular necrosis, glomerulonephritis, allergic nephritis. Decreased urea secretion and edema.
From the hepatobiliary system: very rarely - liver disorders; unknown - hepatic failure, acute hepatitis, with prolonged treatment hepatitis and jaundice may occur. Hepatonecrosis, pancreatitis, duodenitis, esophagitis, hepatorenal syndrome.
From the blood and lymphatic system: very rarely - disorders of the hematopoietic system (anemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis). The first signs are: high body temperature, sore throat, ulcers on the oral mucosa, flu symptoms, severe exhaustion, unexplained bleeding and bruising, ecchymosis, purpura, nosebleeds. With prolonged therapy, it is necessary to regularly monitor blood morphology parameters.
Immune system disorders: rhinitis. In patients with autoimmune disorders (e.g. systemic lupus erythematosus, systemic connective tissue diseases) treated with ibuprofen, isolated cases of symptoms of aseptic meningitis, such as stiff neck, headache, nausea, vomiting, fever or disorientation, have been observed.
On the part of the psyche: unknown - with prolonged use, depression, hallucinations, confusion, psychotic reactions, vertigo, insomnia, irritability, nervousness, excited state, emotional instability may occur.
On the part of the organ of vision: rarely - dryness of the mucous membrane of the eye; very rarely - blurred vision, impaired color perception, toxic amblyopia; unknown - with prolonged treatment, visual impairment, optic neuritis may occur.
On the part of the organ of hearing: hearing impairment, hearing loss, with prolonged use, ringing or tinnitus, dizziness are possible.
General disorders: hypersensitivity reactions in the form of urticaria and itching; severe hypersensitivity reactions with the following manifestations: swelling of the face, tongue and larynx, shortness of breath, tachycardia, decreased blood pressure (anaphylaxis, Quincke's edema, up to shock); aseptic meningitis; exacerbation of asthma and bronchospasm. Malaise and increased fatigue, decreased appetite, increased sweating.
Laboratory indicators: very rarely - a decrease in hemoglobin levels.
Infections: unknown - varicella virus.
Exacerbation of inflammation resulting from infection (e.g. cases of necrotizing fasciitis) associated with the use of nonsteroidal anti-inflammatory drugs. This may be associated with the mechanism of action of NSAIDs.
Special instructions
Do not use with other NSAIDs in patients with a history of angina and/or cardiac dysfunction, as fluid retention and edema associated with the use of nonsteroidal anti-inflammatory drugs may occur.
Use with caution in patients with asthma, as the drug may cause bronchospasm. In patients with a history of gastric/duodenal ulcer, taking the drug increases the likelihood of bleeding in the digestive tract. In the case of taking the drug in patients with impaired liver and kidney function, the activity of liver enzymes and the functional ability of the kidneys should be monitored. Use with caution in patients with systemic lupus erythematosus or connective tissue diseases, as there is a risk of developing aseptic meningitis; in patients with impaired porphyrin metabolism (for example, acute intermittent porphyria); in patients immediately after surgery.
With prolonged use of painkillers in large doses, a headache may occur, which cannot be treated by increasing the dose of the drug.
The manifestations of side effects related to the use of ibuprofen and the entire group of nonsteroidal anti-inflammatory drugs can generally be reduced by using the minimum effective dose necessary to treat symptoms for the minimum period.
Clinical trial and epidemiological data suggest that ibuprofen, especially at high doses (2400 mg/day), and long-term treatment may be associated with a small increased risk of arterial thrombotic events (e.g. myocardial infarction or stroke). Overall, epidemiological data do not suggest that ibuprofen at lower doses (e.g. ≤1200 mg/day) may be associated with an increased risk of myocardial infarction. In patients with uncontrolled hypertension, congestive heart failure diagnosed with coronary artery disease, peripheral arterial disease and/or cerebrovascular disease, long-term treatment should only be initiated by a physician after careful consideration. In individuals with significant risk factors for cardiovascular events (e.g. hypertension, hyperlipidemia, diabetes mellitus, smoking), long-term treatment with NSAIDs should only be initiated after consultation with a physician.
Prolonged use of NSAIDs may lead to a dose-dependent decrease in prostaglandin synthesis and may precipitate renal failure. Patients with impaired renal function, cardiac disease, hepatic impairment, diuretic therapy, and the elderly are at increased risk of this reaction. Renal function should be monitored in such patients.
Effects on female fertility. There is limited evidence that medicinal products that inhibit cyclooxygenase/prostaglandin synthesis may affect ovulation. This is reversible after discontinuation of treatment. Long-term use (at doses of 2400 mg/day and for a duration of 10 days) of ibuprofen may impair female fertility and is not recommended in women attempting to conceive. In women who have difficulty conceiving or are undergoing investigation for infertility, this medicinal product should be discontinued.
The risk of gastrointestinal bleeding, perforation, ulceration increases with increasing doses of NSAIDs in patients with a history of gastric/duodenal ulcer, especially if complicated by bleeding or perforation, and in the elderly. These patients should start treatment with minimal doses. Caution should be exercised when treating patients receiving concomitant medications that may increase the risk of gastrotoxicity or bleeding, such as oral corticosteroids or anticoagulants (e.g. warfarin), or antiplatelet agents (e.g. acetylsalicylic acid). With prolonged treatment for these patients, as well as for those who require concomitant use of low doses of acetylsalicylic acid or other drugs that may increase the risk for the digestive tract, the doctor should consider prescribing combination therapy with misoprostol or proton pump inhibitors.
Patients with a history of gastrointestinal disorders, especially the elderly, should be informed of any unusual symptoms from the digestive tract, especially gastrointestinal bleeding at the beginning of treatment. In the event of gastrointestinal bleeding or gastric/duodenal ulceration in patients receiving ibuprofen, treatment should be discontinued immediately.
Skin and subcutaneous tissue disorders: Very rarely, severe skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, may occur in association with the use of NSAIDs. The highest risk of such reactions occurs during the first month of treatment. Ibuprofen should be discontinued at the first appearance of skin rash, mucosal lesions or any other sign of hypersensitivity.
Since the medicinal product contains lactose, patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.
Ibuprom. Do not use in patients with fructose intolerance, glucose-galactose malabsorption and/or sucrase-isomaltase. Patients with diabetes should take into account the presence of sugar in the preparation.
Ibuprom Sprin Caps and Ibuprom Extra contain sorbitol. The use of these drugs is not recommended in patients with hereditary fructose intolerance.
Ibuprom Max contains sucrose, patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not use this medicine.
Use during pregnancy or breastfeeding. Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryo/foetal development. Epidemiological studies have shown an increased risk of miscarriage and birth defects following exposure to prostaglandin synthesis inhibitors in early pregnancy. The risk is thought to increase with dose and duration of therapy. NSAIDs should not be used during the first two trimesters of pregnancy or during labour unless the potential benefit to the mother outweighs the potential risk to the foetus. In the third trimester of pregnancy, the use of any prostaglandin synthesis inhibitor may cause foetal effects such as cardiopulmonary toxicity (premature closure of the ductus arteriosus with pulmonary hypertension) and renal impairment, which may progress to renal failure with oligohydramnios. Ibuprofen is contraindicated in the third trimester of pregnancy due to the possibility of suppressing uterine contractile function, which may lead to an increase in the duration of labor with a tendency to increase bleeding in the mother and child, even when the drug is used in low doses.
Studies have shown that small amounts of ibuprofen are found in breast milk. NSAIDs should be avoided during breastfeeding if possible.
Children. Ibuprom and Ibuprom Sprint Caps are not used in children weighing 20 kg and under 6 years of age. Ibuprom Max and Ibuprom Extra are contraindicated in children under 12 years of age.
Ability to influence the speed of reaction when driving vehicles or other mechanisms. With short-term use of the drug, there is no need for precautions. When used in accordance with the recommended doses and duration of treatment, the drug does not affect the speed of reaction when driving vehicles or working with other mechanisms. Patients who experience dizziness, drowsiness, disorientation or visual impairment when using NSAIDs should refrain from driving vehicles or working with mechanisms.
Concomitant use with acetylsalicylic acid and other NSAIDs, including selective COX-2 inhibitors, may increase side effects, so this combination should be avoided, except in cases where a lower dose of acetylsalicylic acid (not higher than 75 mg/day) has been prescribed by a doctor. Experimental data indicate that, when used simultaneously, ibuprofen may inhibit the effect of acetylsalicylic acid in low doses on platelet aggregation. However, the limitations of these data give reason to believe that clinically significant effects are unlikely with unsystematic use of ibuprofen. Frequent use of the drug may inhibit the cardioprotective effect of acetylsalicylic acid. Increases the toxicity of methotrexate. In case of simultaneous use with corticosteroids, the risk of adverse reactions from the digestive tract (gastrointestinal bleeding or ulceration) increases. may inhibit the effect of diuretics (loop and thiazide diuretics) and antihypertensive drugs of the ACE inhibitor and β-adrenoceptor blocker group. enhances the effect of coumarin anticoagulants (e.g. warfarin). prolongs bleeding time in patients treated with zidovudine. there is evidence of an increased risk of hemarthrosis and hematoma in HIV-infected patients receiving concomitant treatment with zidovudine and ibuprofen. use of the drug in combination with lithium increases the concentration of the latter in the blood plasma.
In some patients with impaired renal function (e.g. dehydrated patients or elderly patients with compromised renal function), the concomitant use of an ACE inhibitor or an angiotensin II antagonist and drugs that inhibit COX may lead to further deterioration of renal function, including possible AKI, which is usually reversible. Therefore, such combinations should be prescribed with caution, especially in the elderly. If prolonged treatment is necessary, the patient should be adequately hydrated and consideration should be given to monitoring renal function at the beginning of the combination treatment and periodically thereafter.
Diuretics may increase the risk of nephrotoxicity of NSAIDs. Concomitant use with potassium-sparing diuretics may lead to hyperkalemia (plasma potassium monitoring is recommended).
There is an increased risk of haematological toxicity with concomitant use of zidovudine and NSAIDs. There is evidence of an increased risk of haemarthrosis and haematoma in HIV-infected patients with haemophilia when zidovudine and ibuprofen are used concomitantly.
Cardiac glycosides: NSAIDs may exacerbate cardiac dysfunction, reduce renal filtration function, and increase plasma glycoside levels.
Antiplatelet agents and selective serotonin reuptake inhibitors: The risk of gastrointestinal bleeding may be increased.
Cyclosporine, tacrolimus: possible increased risk of nephrotoxicity.
Mifepristone: NSAIDs should not be used earlier than 8-12 days after mifepristone administration, as they reduce its effectiveness.
Quinolone antibiotics: Concomitant use with ibuprofen may increase the risk of seizures.
Sulfonylurea drugs and phenytoin: possible enhancement of the effect. When used with sulfonylurea drugs, blood glucose levels should be monitored.
Ibuprofen should be used with caution in combination with digoxin - as a result, the blood plasma levels of both drugs increase.
Overdose
In case of acute overdose, the symptoms depend on the amount of the drug taken and the time elapsed since its administration. The first, usually observed, symptoms are: nausea, vomiting, headache and dizziness, epigastric pain, drowsiness, diarrhea, tinnitus, nystagmus, visual impairment, agitation, disorientation, convulsions, acute renal failure, liver damage, respiratory failure, cyanosis, prolonged prothrombin time. In case of overdose, coma, arterial hypotension, hyperkalemia with cardiac arrhythmia, metabolic acidosis, fever, respiratory system disorders and renal dysfunction may occur sporadically. After prolonged administration, hemolytic anemia, granulocytopenia and thrombocytopenia may occur sporadically.
Patients with bronchial asthma may experience an exacerbation of their condition.
The use of the drug in children at a dose above 400 mg/kg of body weight may lead to symptoms of intoxication. In adults, the effect is less pronounced. T ½ in case of overdose is 1.5-3 hours. If no more than 1 hour has passed since the acute overdose, it is recommended to induce vomiting, rinse the stomach or take activated charcoal. In case of frequent or prolonged seizures, diazepam or lorazepam should be administered intravenously. Patients with bronchial asthma should be prescribed bronchodilators.
In cases of ibuprofen overdose, there is no antidote or specific treatment. Symptomatic treatment is based on monitoring vital signs with blood pressure measurement, ECG, and interpretation of symptoms indicating possible gastrointestinal bleeding, metabolic acidosis, and central nervous system disorders.
Ibuprom. for packages with tablets in blisters: store at a temperature not exceeding 30 °C. for packages with tablets in bottles and sachets: does not require special storage conditions.
Ibuprom Sprint Caps. At a temperature not exceeding 25 °C.
Ibuprom Max. In the original packaging at a temperature not exceeding 30 °C.
Ibuprom Extra. At a temperature not exceeding 25 °C.
