Instructions Ibuprofen film-coated tablets 200 mg No. 30
Composition
active ingredient: ibuprofen;
1 tablet contains 200 mg of ibuprofen;
excipients: potato starch, magnesium stearate, povidone, opadry II pink 85F34660 (mixture of substances: polyvinyl alcohol, titanium dioxide E 171, polyethylene glycol
3350, talc, carmoisine E 122, sunset yellow FCF E 110).
Dosage form
Film-coated tablets.
Main physicochemical properties: round, film-coated tablets with a biconvex surface, from light pink to dark pink in color. When broken, when viewed under a magnifying glass, a core surrounded by one continuous layer is visible.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory and antirheumatic drugs. Propionic acid derivatives. ATC code M01A E01.
Pharmacological properties
Pharmacodynamics.
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID), a propionic acid derivative, which has demonstrated its effectiveness by inhibiting prostaglandin synthesis. In humans, ibuprofen reduces inflammatory pain, swelling, and fever. It has pronounced analgesic, antipyretic, and anti-inflammatory effects. In addition, ibuprofen reversibly inhibits platelet aggregation.
Experimental data suggest that ibuprofen may competitively inhibit the effect of low-dose aspirin (acetylsalicylic acid) on platelet aggregation when these drugs are administered concomitantly. Some pharmacodynamic studies have shown that when single doses of ibuprofen 400 mg are administered within 8 hours before or within
A reduction in the effect of aspirin (acetylsalicylic acid) on thromboxane formation or platelet aggregation was observed 30 minutes after administration of immediate-release aspirin (81 mg). Although there is uncertainty about the extrapolation of these findings to the clinical situation, it cannot be ruled out that regular long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid. With non-systematic use of ibuprofen, such a clinically significant effect is considered unlikely.
Pharmacokinetics.
After administration, ibuprofen is rapidly absorbed from the gastrointestinal tract and binds to plasma proteins.
The maximum concentration of the active substance in the blood plasma is reached 45 minutes after administration on an empty stomach, in the synovial fluid - 3 hours after administration. In the case of using this drug during food intake, peak levels are observed 1-2 hours after administration. Ibuprofen is metabolized in the liver, excreted by the kidneys in unchanged form or in the form of metabolites. The half-life is almost 2 hours.
No significant differences in the pharmacokinetic profile are observed in elderly patients.
Indication
Symptomatic therapy of headache and toothache, dysmenorrhea, neuralgia, back pain, joint pain, muscle pain, rheumatic pain, as well as symptoms of colds and flu.
Contraindication
- Hypersensitivity to ibuprofen or to any of the other components of the drug.
- Allergic reactions (e.g., bronchial asthma, rhinitis, angioedema, or urticaria) after using ibuprofen, acetylsalicylic acid (aspirin), or other nonsteroidal anti-inflammatory drugs in history.
- Gastric and duodenal ulcer, active bleeding or history of recurrence (two or more severe episodes of confirmed ulcer or bleeding).
- History of gastrointestinal bleeding or perforation of the gastrointestinal wall associated with the use of NSAIDs.
- Severe heart failure (NYHA class IV), severe liver dysfunction or severe renal dysfunction.
- The last trimester of pregnancy.
- Active inflammatory bowel disease.
- Hemorrhagic diathesis or other blood clotting disorders.
Interaction with other medicinal products and other types of interactions
In general, caution should be exercised when using NSAIDs in combination with other drugs that may increase the risk of gastrointestinal ulcers, gastrointestinal bleeding, or worsening of renal function.
Ibuprofen, like other nonsteroidal anti-inflammatory drugs (NSAIDs), should not be used in combination with:
- acetylsalicylic acid (aspirin), as this increases the risk of adverse reactions, except in cases where aspirin (dose not exceeding 75 mg per day) has been prescribed by a doctor.
Experimental data suggest that ibuprofen may competitively inhibit the effect of low-dose aspirin (acetylsalicylic acid) on platelet aggregation when used concomitantly. Although there is uncertainty about the extrapolation of these data to the clinical situation, it cannot be excluded that regular long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid. With non-systematic use of ibuprofen, such a clinically significant effect is considered unlikely;
Ibuprofen should be used with caution in combination with the following drugs:
Anticoagulants: nonsteroidal anti-inflammatory drugs may increase the effect of anticoagulants such as warfarin;
Antihypertensives (ACE inhibitors and angiotensin II antagonists) and diuretics: NSAIDs may reduce the therapeutic effect of these drugs. 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 angiotensin II antagonist and drugs that inhibit cyclooxygenase may lead to further deterioration of renal function, including possible acute renal failure, which is usually reversible. These interactions should be considered in patients receiving coxibs concomitantly with ACE inhibitors or angiotensin II antagonists. Therefore, such combinations should be used with caution, especially in the elderly. If treatment is necessary, it should be ensured that the patient is adequately hydrated and that renal function should be monitored at the start of combination therapy and periodically thereafter. Diuretics increase the risk of nephrotoxic effects of NSAIDs;
corticosteroids: increase the risk of ulcers and bleeding in the gastrointestinal tract;
Antiplatelet agents and selective serotonin reuptake inhibitors: increase the risk of gastrointestinal bleeding;
cardiac glycosides: NSAIDs may exacerbate heart failure, reduce glomerular filtration rate, and increase plasma glycoside levels;
Lithium and methotrexate: there is evidence of a potential increase in plasma levels of lithium and methotrexate;
cyclosporine: increased risk of nephrotoxicity;
Mifepristone: NSAIDs should not be taken for 8–12 days after mifepristone administration, as this may lead to a decrease in the effect of mifepristone;
Tacrolimus: increased risk of nephrotoxicity with concomitant use of NSAIDs with tacrolimus;
Zidovudine: Increased risk of hematological toxicity with concomitant use of zidovudine and NSAIDs. There is evidence of an increased risk of hemarthrosis and hematoma in HIV-infected patients with hemophilia when treated concomitantly with zidovudine and ibuprofen.
Quinolone antibiotics: Concomitant use of ibuprofen and quinolone antibiotics increases the risk of seizures.
Application features
The side effects associated with ibuprofen can be reduced by using the minimum effective dose for a short period of time necessary to treat symptoms.
Elderly patients have an increased incidence of adverse reactions to NSAIDs, especially gastrointestinal bleeding and perforation, which can be fatal.
Effects on the respiratory system.
Bronchospasm may occur in patients with bronchial asthma, patients with allergic diseases, and patients with a history of bronchospasm.
Other NSAIDs.
The concomitant use of ibuprofen with other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided as this increases the risk of adverse reactions.
Systemic lupus erythematosus and mixed connective tissue disease.
Ibuprofen should be used with caution in systemic lupus erythematosus and mixed connective tissue disease due to an increased risk of aseptic meningitis.
Cases of aseptic meningitis have been reported with ibuprofen. Although this effect is more likely in patients with systemic lupus erythematosus and other connective tissue diseases, such cases have also been reported in some patients without chronic diseases, so this should be taken into account when using this drug.
Effects on the cardiovascular and cerebrovascular systems.
Patients with a history of hypertension and/or heart failure should start treatment with caution (consultation with a doctor is necessary), since cases of fluid retention, hypertension and edema have been reported with ibuprofen therapy, as with other NSAIDs.
Ibuprofen use, especially at high doses (2400 mg daily), and long-term use, slightly increases the risk of arterial thrombotic events (e.g. myocardial infarction or stroke). However, there is no evidence of an association between low-dose ibuprofen use (e.g. less than 1200 mg daily) and an increased risk of myocardial infarction.
Patients with uncontrolled hypertension, congestive heart failure (NYHA class II-III), established ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease should be treated with ibuprofen only after careful clinical assessment. High doses (2400 mg/day) should be avoided.
Cases of Kounis syndrome have been reported in patients treated with ibuprofen. Kounis syndrome is manifested by cardiovascular symptoms associated with narrowing of the coronary arteries due to an allergic or hypersensitivity reaction, which can lead to myocardial infarction.
Kidney/liver effects.
Caution should be exercised in patients with renal insufficiency due to the possibility of worsening of renal function. Ibuprofen should be used with caution in patients with renal or hepatic disease, and especially during concomitant therapy with diuretics, since inhibition of prostaglandins may lead to fluid retention and further deterioration of renal function. In such patients, the lowest possible dose of ibuprofen should be used and renal function should be monitored regularly. In case of dehydration, adequate fluid intake should be ensured. There is a risk of renal insufficiency in children (from 6 years of age) and adolescents with dehydration.
In general, the systematic use of analgesics, especially combinations of different analgesics, can lead to long-term kidney damage with the risk of renal failure (analgesic nephropathy). The highest risk of this reaction exists in elderly patients, patients with renal failure, heart failure and liver failure, as well as in those receiving diuretics or ACE inhibitors. After discontinuation of NSAID therapy, a return to the state observed before treatment is usually achieved.
As with other NSAIDs, ibuprofen may cause a small, transient increase in certain liver function tests, as well as a significant increase in AST and ALT levels. In the event of a significant increase in these values, treatment should be discontinued.
With prolonged use of ibuprofen, liver function tests, kidney function, and hematological function/blood count should be regularly checked.
Impact on fertility in women.
There is insufficient evidence that drugs that inhibit cyclooxygenase/prostaglandin synthesis can cause impairment of female reproductive function through effects on ovulation. This effect is reversible after discontinuation of treatment.
Effect on the gastrointestinal tract.
NSAIDs should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), as their condition may be exacerbated.
There are reports of cases of gastrointestinal bleeding, perforation, ulceration, which can be fatal, occurring at any stage of treatment with NSAIDs, regardless of the presence of warning symptoms or the presence of severe gastrointestinal disorders in history.
The risk of gastrointestinal bleeding, perforation or ulceration increases with increasing doses of NSAIDs in patients with a history of peptic ulcer disease, especially complicated by bleeding or perforation, and in the elderly. Elderly patients are at increased risk of serious consequences due to side effects. These patients should be started on the lowest dose. In such patients, as well as in patients who require concomitant use of low doses of acetylsalicylic acid or other drugs that may increase the risk from the gastrointestinal tract, combination therapy with protective drugs (e.g. misoprostol or proton pump inhibitors) is recommended.
Patients with a history of gastrointestinal toxicity, particularly elderly patients, should be informed of any unusual abdominal symptoms from the gastrointestinal tract (especially gastrointestinal bleeding), particularly at the beginning of treatment.
With prolonged use of analgesics in high doses, headaches may occur that cannot be treated by increasing the dose of the drug. Prolonged use of any analgesic for the treatment of headaches may worsen this condition. In such cases, a doctor should be consulted and treatment should be discontinued. The possibility of drug overuse headache should be considered in patients who suffer from frequent or daily headaches despite (or because of) regular use of headache medications.
The drug should be used with caution in patients receiving concomitant therapy with drugs that increase the risk of ulcers or bleeding, including oral corticosteroids, anticoagulants (e.g. warfarin), selective serotonin reuptake inhibitors or antiplatelet agents (e.g. acetylsalicylic acid).
In the event of gastrointestinal bleeding or ulceration in patients receiving ibuprofen, treatment should be discontinued immediately.
Skin and subcutaneous tissue reactions.
If signs and symptoms suggestive of these reactions occur, ibuprofen should be discontinued immediately and alternative treatment considered (if necessary).
In exceptional cases, chickenpox can cause severe skin and soft tissue infections. At this time, the effect of NSAIDs on the worsening of these infections cannot be excluded, therefore it is recommended to avoid the use of ibuprofen in case of chickenpox.
Masking the symptoms of underlying infections.
Ibuprofen may mask the symptoms of an infectious disease, which may delay the initiation of appropriate treatment and thus complicate the course of the disease. This has been observed in bacterial community-acquired pneumonia and bacterial complications of varicella. When ibuprofen is used for fever or for pain relief in an infection, monitoring for the presence of an infectious disease is recommended. In the setting of outpatient treatment, the patient should seek medical advice if symptoms persist or worsen.
The medicine contains the dyes carmoisine E 122 and sunset yellow FCF E 110, which may cause allergic reactions.
Use during pregnancy or breastfeeding
Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryonal/fetal development. Epidemiological data suggest an increased risk of miscarriage, congenital heart defects and gastroschisis following the use of prostaglandin synthesis inhibitors in early pregnancy. The absolute risk of cardiovascular malformations increased from less than 1% to approximately 1.5%. The risk is believed to increase with increasing dose and duration of therapy.
In animals, the use of prostaglandin synthesis inhibitors has resulted in an increase in pre- and post-implantation loss and embryo/fetal lethality. In addition, an increased incidence of various malformations, including cardiovascular malformations, has been reported in animals treated with prostaglandin synthesis inhibitors during the period of organogenesis.
From the 20th week of pregnancy onwards, the use of ibuprofen may cause oligohydramnios due to fetal renal dysfunction. This disorder may occur shortly after the start of treatment and is usually reversible after discontinuation of treatment. In addition, there have been reports of narrowing of the ductus arteriosus in the fetus after the use of ibuprofen in the second trimester of pregnancy, which in most cases resolved after discontinuation of treatment.
The drug should be avoided during the first and second trimesters of pregnancy. NSAIDs should not be used during the first and second trimesters of pregnancy unless the potential benefit to the patient outweighs the potential risk to the fetus. In women attempting to conceive and during the first and second trimesters of pregnancy, the lowest possible dose should be used for the shortest duration possible. Antenatal monitoring for oligohydramnios and narrowing of the ductus arteriosus may be appropriate if ibuprofen exposure has occurred for several days, starting from the 20th week of gestation. Ibuprofen should be discontinued if oligohydramnios or narrowing of the ductus arteriosus is detected.
All prostaglandin synthesis inhibitors, when used during the third trimester of pregnancy, pose risks:
- for the fetus: cardiopulmonary toxicity (characterized by premature narrowing/closure of the ductus arteriosus and pulmonary hypertension); renal dysfunction (see above), which may progress to renal failure, accompanied by oligohydramnios;
- for the mother and newborn: increased bleeding time, antiplatelet effect, which can develop even at very low doses; inhibition of uterine contractions, leading to delayed or prolonged labor.
The drug is contraindicated in the third trimester of pregnancy (see section "Contraindications").
In limited studies, ibuprofen has been found in breast milk at very low concentrations, so it is unlikely that it could negatively affect a breastfed infant.
Ability to influence reaction speed when driving vehicles or other mechanisms
When used in accordance with the recommended doses and duration of treatment, the drug does not affect the reaction speed when driving vehicles or other mechanisms.
Method of administration and doses
For short-term oral use only. The tablets should be swallowed whole with water.
The lowest effective dose should be used for the shortest time necessary to relieve symptoms (see section "Special instructions for use"). If it is necessary to use the drug for more than 5 days (if symptoms persist or worsen), you should consult a doctor for advice.
The drug is prescribed to adults and children weighing more than 20 kg (from 6 years of age). The recommended daily dose of the drug is 20–30 mg/kg of body weight. Do not exceed a dose of 30 mg/kg of body weight per day.
Adults and children weighing more than 30 kg: 200–400 mg (1–2 tablets) per dose. Repeat the dose every 4–6 hours if necessary. Do not exceed 1200 mg (6 tablets) in 24 hours.
Elderly people do not require special dosage.
Children: Do not use in children weighing less than 20 kg and under 6 years of age.
Overdose
Most reported cases of overdose have been asymptomatic. The risk of symptoms occurs with ibuprofen doses above 80-100 mg/kg.
The use of the drug in children in doses exceeding 400 mg/kg may cause symptoms of intoxication. In adults, the dose effect is less pronounced. The half-life in overdose is 1.5–3 hours.
Symptoms. Symptoms of overdose occur within 4 hours of administration. In most patients, the use of clinically significant amounts of nonsteroidal anti-inflammatory drugs has caused only nausea, vomiting, epigastric pain or, very rarely, diarrhea. Tinnitus, headache and gastrointestinal bleeding may also occur. In more severe poisoning, toxic lesions of the central nervous system may occur in the form of vertigo, dizziness, lethargy, drowsiness, sometimes - nervous excitement, ataxia, disorientation or coma. Sometimes patients have convulsions. In more severe poisoning, hyperkalemia, metabolic acidosis and an increase in prothrombin time/INR (international normalized ratio) may occur, presumably due to interaction with blood clotting factors circulating in the bloodstream. Moderate to severe symptoms such as acute renal failure, liver damage, hypotension, hypothermia, cyanosis, dyspnoea/acute respiratory distress syndrome and short-term apnoea episodes (in children after administration of large amounts of the drug) have been observed rarely. Exacerbation of asthma may occur in patients with bronchial asthma. Nystagmus, blurred vision and loss of consciousness are possible.
Treatment. There is no specific antidote. Treatment may be symptomatic and supportive, and may include maintaining a patent airway and monitoring cardiac function and vital signs until the patient is stable. When small amounts of the drug are ingested (less than 50 mg/kg ibuprofen), water is recommended to minimize gastrointestinal upset. Oral administration of activated charcoal or gastric lavage is recommended within 1 hour of ingestion of a potentially toxic dose. If ibuprofen has already been absorbed, alkaline agents may be used to help eliminate acidic ibuprofen in the urine. The benefit of measures such as forced diuresis, hemodialysis, and hemoperfusion has not been proven, as ibuprofen is highly bound to plasma proteins. Diazepam or lorazepam should be administered intravenously for frequent or prolonged muscle spasms. Bronchodilators should be used in cases of bronchial asthma. You should consult a doctor for medical advice.
Adverse reactions
The following adverse reactions have been observed with short-term use of ibuprofen in non-prescription doses. Other adverse reactions may occur with chronic disease treatment and long-term use. The most frequently observed adverse reactions are gastrointestinal. Adverse reactions are mostly dose-dependent, in particular the risk of gastrointestinal bleeding depends on the dose and duration of treatment.
Adverse reactions associated with the use of ibuprofen are classified by system organ class and frequency. The frequency is defined as follows: very common (≥1/10); common (≥1/100 and <1/10); uncommon (≥1/1000 and <1/100); rare (≥1/10000 and <1/1000); very rare (<1/10000); frequency unknown (frequency cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
From the blood and lymphatic system:
very rare: blood disorders (anemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis). The first signs are fever, sore throat, superficial ulcers in the mouth, flu-like symptoms, severe exhaustion, unexplained bleeding and hematomas of unknown etiology.
On the part of the immune system:
Hypersensitivity reactions1; uncommon: urticaria and pruritus; very rare: severe hypersensitivity reactions, symptoms of which may include swelling of the face, tongue and larynx, dyspnoea, tachycardia, hypotension (anaphylactic reaction, angioedema or severe shock); frequency unknown: airway reactivity including bronchial asthma, exacerbation of asthma, bronchospasm or dyspnoea.
From the nervous system:
uncommon: headache; very rare: aseptic meningitis2.
From the side of the cardiac system:
frequency unknown: heart failure, edema, Kounis syndrome.
Clinical trial data and epidemiological data suggest that the use of ibuprofen, especially at high doses of 2400 mg per day and with long-term treatment, may be associated with a slightly increased risk of arterial thrombotic complications (e.g. myocardial infarction or stroke).
From the vascular system:
frequency unknown: arterial hypertension.
Infrequent: abdominal pain, nausea, dyspepsia; Rare: diarrhea, flatulence, constipation and vomiting; Very rare: gastric and duodenal ulcers, perforations or gastrointestinal bleeding, melena, haematemesis, sometimes fatal (especially in elderly patients), ulcerative stomatitis, gastritis;
frequency unknown: exacerbation of colitis and Crohn's disease.
On the part of the liver:
very rare: liver dysfunction.
Skin and subcutaneous tissue disorders:
infrequently: various skin rashes;
very rare: severe skin reactions including Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis and toxic epidermal necrolysis;
frequency unknown: drug reaction with eosinophilia and systemic symptoms (DRESS syndrome), acute generalized exanthematous pustulosis, photosensitivity reactions.
From the respiratory tract and mediastinal organs:
frequency unknown: airway reactivity, including asthma, bronchospasm, or dyspnea.
From the kidneys and urinary system:
very rare: acute renal failure, papillonecrosis, especially with prolonged use, associated with increased serum urea levels, and edema; frequency unknown: renal failure.
Laboratory studies:
very rare: decreased hemoglobin level.
Description of selected adverse reactions.
1 Hypersensitivity reactions have been reported following treatment with ibuprofen. These reactions include (a) non-specific allergic reactions and anaphylaxis, (b) respiratory tract reactions including bronchial asthma, exacerbation of asthma, bronchospasm or dyspnoea, or (c) various skin disorders including rashes of various types, pruritus, urticaria, purpura, angioedema and, less commonly, exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).
2 The mechanism of pathogenesis of drug-induced aseptic meningitis is not fully understood. However, available data on aseptic meningitis associated with NSAIDs suggest a hypersensitivity reaction (due to temporal relationship to drug intake and resolution of symptoms after drug withdrawal). In particular, isolated cases of symptoms of aseptic meningitis (such as neck stiffness, headache, nausea, vomiting, fever or disorientation) have been observed during treatment with ibuprofen in patients with pre-existing autoimmune disorders (such as systemic lupus erythematosus, mixed connective tissue disease).
Reporting adverse reactions after registration of a medicinal product is of great importance. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of a medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
10 tablets in a blister, 1 or 3 or 5 blisters in a pack.
Vacation category
Without a prescription.
Producer
JSC "VITAMINS".
Location of the manufacturer and its business address.
Ukraine, 20300, Cherkasy region, Uman city, Uspenska st., 31.
Applicant.
JSC "VITAMINS".
Location of the applicant and/or the applicant's representative.
Ukraine, 20300, Cherkasy region, Uman city, Uspenska st., 31.
