Instructions for use Ibuprofen-Darnitsa tablets 200 mg No. 50
Composition
active ingredient: ibuprofen;
1 tablet contains 200 mg of ibuprofen;
Excipients: microcrystalline cellulose, croscarmellose sodium, colloidal anhydrous silicon dioxide, corn starch, magnesium stearate.
Dosage form
Pills.
Main physicochemical properties: tablets of white or almost white color, round shape, with a biconvex surface.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory and antirheumatic drugs. Propionic acid derivatives.
ATX 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 the synthesis of prostaglandins - mediators of pain and inflammation. Ibuprofen has 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 used concomitantly. Some pharmacodynamic studies have shown that single doses of ibuprofen 400 mg administered within 8 hours before or within 30 minutes after immediate-release aspirin (81 mg) reduced the effect of aspirin (acetylsalicylic acid) on thromboxane formation or platelet aggregation. 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. Such a clinically significant effect is unlikely with non-systematic use of ibuprofen.
Ibuprofen relieves pain, reduces inflammation, and lowers fever.
Pharmacokinetics
Ibuprofen is rapidly absorbed from the gastrointestinal tract and binds to plasma proteins.
The maximum concentration in the blood serum is determined 45 minutes after administration on an empty stomach. In the case of using this drug with food, 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. In elderly patients, no significant differences in the pharmacokinetic profile are observed.
Indication
Symptomatic treatment of headache, toothache, dysmenorrhea, neuralgia, back pain, joint pain, muscle pain, rheumatic pain, as well as treatment of cold and flu symptoms.
Contraindication
Hypersensitivity to ibuprofen or to any of the excipients. History of hypersensitivity reactions (such as asthma, rhinitis, angioedema or urticaria) after taking ibuprofen, acetylsalicylic acid (aspirin) or other NSAIDs. Gastric and duodenal ulcer/bleeding in active form 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 renal failure or severe hepatic failure. Active inflammatory bowel disease. Hemorrhagic diathesis or other blood clotting disorders. Last trimester of pregnancy.
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 deterioration of renal function.
Ibuprofen, like other NSAIDs, should not be used in combination with:
acetylsalicylic acid (aspirin), as this may increase the risk of adverse reactions, unless aspirin (dose not exceeding 75 mg per day) has been prescribed by a doctor. Experimental data suggest that ibuprofen may inhibit the antiplatelet effect of low-dose aspirin when used concomitantly. However, the limited data and uncertainty regarding the extrapolation of ex vivo data to the clinical picture do not allow firm conclusions to be drawn regarding the systematic use of ibuprofen. Therefore, such clinically significant effects are considered unlikely with non-systematic use of ibuprofen; other NSAIDs, including selective cyclooxygenase-2 inhibitors. The simultaneous use of two or more NSAIDs should be avoided, as this may increase the risk of adverse effects.
Anticoagulants: NSAIDs may enhance the effect of anticoagulants such as warfarin; Antihypertensives (ACE inhibitors and angiotensin II antagonists) and diuretics: NSAIDs may reduce the effect of these medicinal products. 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 medicinal products 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, ensure that the patient is adequately hydrated and consider the need to monitor renal function at the beginning of combination therapy and periodically thereafter.
Diuretics may increase the risk of nephrotoxicity of NSAIDs; corticosteroids: increased risk of ulceration and bleeding in the gastrointestinal tract; antiplatelet agents and selective serotonin reuptake inhibitors: increased risk of gastrointestinal bleeding; cardiac glycosides: NSAIDs may exacerbate cardiac dysfunction, reduce glomerular filtration rate and increase plasma glycoside levels; lithium: there is evidence of a potential increase in plasma lithium levels; methotrexate: there is a possibility of increased plasma methotrexate levels; cyclosporine: increased risk of nephrotoxicity; mifepristone: NSAIDs should not be used earlier than 8–12 days after mifepristone administration, as they may reduce its effectiveness; tacrolimus: there is a possible increased risk of nephrotoxicity with concomitant use of NSAIDs with tacrolimus; Zidovudine: 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 treated with zidovudine and ibuprofen. Quinolone antibiotics: Patients receiving ibuprofen and quinolone antibiotics may be at increased risk of convulsions.
Application features
Side effects associated with ibuprofen can be minimized by using the lowest effective dose necessary to treat symptoms for the shortest period of time.
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 who suffer from bronchial asthma or allergic diseases or have a history of these diseases.
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 diseases
Ibuprofen should be used with caution in patients with systemic lupus erythematosus and mixed connective tissue disease due to an increased risk of aseptic meningitis. Cases of aseptic meningitis have been reported in association with ibuprofen. Although this effect is more likely in patients with systemic lupus erythematosus and other connective tissue diseases, it has also been reported in some patients without chronic diseases, and this should be taken into account when using this medicinal product.
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.
Clinical trial and epidemiological data suggest that the use of ibuprofen, especially at high doses (2400 mg/day), and in long-term use 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 low-dose ibuprofen (e.g. ≤ 1200 mg/day) may be associated with 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.
The clinical picture should also be carefully assessed before starting long-term treatment in patients with risk factors for cardiovascular complications (such as hypertension, hyperlipidemia, diabetes mellitus, smoking), especially if high doses of ibuprofen (2400 mg per day) are required.
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, 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, the condition that was observed before treatment usually returns.
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 checked regularly.
Impact on fertility in women
There is limited evidence that drugs that inhibit cyclooxygenase/prostaglandin synthesis may affect ovulation. This effect is reversible upon discontinuation of treatment.
Effects 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 if complicated by bleeding or perforation, and in the elderly. These patients should be started on the lowest dose.
Combination therapy with protective drugs (such as misoprostol or proton pump inhibitors) is recommended for these patients, as well as for patients who require concomitant use of low-dose acetylsalicylic acid or other drugs that may increase gastrointestinal risk.
Patients with a history of gastrointestinal toxicity, particularly elderly patients, should be informed of any unusual gastrointestinal symptoms (especially gastrointestinal bleeding), particularly at the beginning of treatment.
Prolonged use of any painkiller for headache may worsen this condition. In such cases, a doctor should be consulted and treatment should be discontinued. The possibility of medication overuse headache should be considered in patients who suffer from frequent or daily headaches despite (or because of) regular use of headache medications.
Caution should be exercised when treating patients who are taking concomitant medications that may increase the risk of ulceration or bleeding, such as oral corticosteroids, anticoagulants (e.g. warfarin), selective serotonin reuptake inhibitors or antiplatelet agents (e.g. aspirin).
In the event of gastrointestinal bleeding or ulceration in patients receiving ibuprofen, treatment should be discontinued immediately.
Skin and subcutaneous tissue disorders
Very rarely, severe skin reactions, which can be fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis, may occur with NSAIDs. The risk of such reactions is highest at the beginning of therapy, in most cases they began within the first month of treatment. Ibuprofen should be discontinued at the first sign of skin rash, pathological changes in the mucous membranes or any other sign of hypersensitivity.
In exceptional cases, chickenpox can cause severe skin and soft tissue infections. At present, it cannot be excluded that NSAIDs may worsen these infections, and it is therefore recommended that the drug be avoided in case of chickenpox.
Important information about excipients
This medicine contains 6.8 mg sodium, i.e. essentially sodium-free.
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 or working with other mechanisms.
Use during pregnancy or breastfeeding
The use of the drug should be avoided during the first and second trimesters of pregnancy. The drug is contraindicated in the third trimester of pregnancy.
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 exposure to prostaglandin synthesis inhibitors in early pregnancy. The risk is believed to increase with increasing dose and duration of therapy.
NSAIDs should not be used during the first and second trimesters of pregnancy unless the potential benefit to the patient justifies the potential risk to the fetus. If ibuprofen is used by a woman attempting to conceive, or during the first and second trimesters of pregnancy, the lowest possible dose should be used for the shortest duration possible.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may pose the following risks:
for the fetus: cardiopulmonary toxicity (characterized by premature closure of the ductus arteriosus and pulmonary hypertension); renal dysfunction, which may progress to renal failure, accompanied by oligohydramnios; for the mother and newborn at the end of pregnancy: possible increase in bleeding time, antiplatelet effect, which may develop even at very low doses; inhibition of uterine contractions, leading to delay or prolongation of labor.
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.
Method of administration and doses
For short-term oral use only. The tablets should be swallowed whole with water and not chewed.
The lowest effective dose necessary to control symptoms should be used for the shortest possible time. If symptoms persist for more than 5 days after starting treatment or worsen, a doctor should be consulted.
The drug is prescribed for adults and children weighing more than 20 kg (approximately 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.
Children weighing 20 to 30 kg (ages 6 to 11 years): 200 mg (1 tablet) per dose. Repeat dose if necessary after 6 hours. Do not exceed 600 mg (3 tablets) per day.
Adults and children weighing more than 30 kg: 200–400 mg (1–2 tablets) per dose. Repeat dose if necessary after 4–6 hours. Do not exceed 1200 mg (6 tablets) per day.
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
Symptoms of overdose occur within 4 hours after administration.
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 case of overdose is 1.5–3 hours.
Symptoms. In most patients, the use of clinically significant amounts of NSAIDs has caused nausea, vomiting, epigastric pain or, less commonly, diarrhea. Tinnitus, headache and gastrointestinal bleeding may also occur. In severe poisoning, toxic damage to the central nervous system is observed, manifested by drowsiness, vertigo, dizziness, lethargy, sometimes - an excited state, ataxia, disorientation or coma. Sometimes patients develop convulsions. In more severe poisoning, hyperkalemia, metabolic acidosis and an increase in prothrombin time/INR (presumably due to interaction with blood clotting factors circulating in the bloodstream) may occur. Acute renal failure and liver damage, hypotension, hypothermia, cyanosis, dyspnea/acute respiratory distress syndrome and short-term episodes of apnea (in children after administration of large amounts of the drug) may occur. 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 should be symptomatic and supportive, and include maintaining a patent airway and monitoring cardiac function and vital signs until the patient's condition is normal. When using small amounts of the drug (less than 50 mg/kg ibuprofen), drinking water is recommended to minimize gastrointestinal disturbances. Oral administration of activated charcoal or gastric lavage is recommended within 1 hour after taking a potentially toxic dose of the drug. The benefit of measures such as forced diuresis, hemodialysis and hemoperfusion has not been proven, since ibuprofen is highly bound to plasma proteins. In case of frequent or prolonged muscle spasms, treatment should be carried out with intravenous diazepam or lorazepam. In case of bronchial asthma, bronchodilators should be used. You should consult a doctor for medical advice.
Adverse reactions
Adverse reactions that have occurred with ibuprofen are listed below by system organ class and frequency. The frequency of adverse reactions is defined as follows: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000) and not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
The following adverse reactions are those observed with short-term use of ibuprofen at non-prescription doses. When treating chronic conditions, additional adverse effects may occur with long-term treatment.
The most frequently observed adverse reactions were gastrointestinal. Most adverse reactions are dose-dependent, in particular the risk of gastrointestinal bleeding depends on the dose and duration of treatment.
Respiratory, thoracic and mediastinal disorders: frequency unknown: airway reactivity, including asthma, bronchospasm or dyspnoea.
Gastrointestinal: uncommon: 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.
Hepatobiliary disorders: very rare: liver dysfunction.
Renal and urinary disorders: very rare: acute renal failure, papillonecrosis, especially with prolonged use, associated with increased serum urea levels, and edema; frequency unknown: renal failure.
Nervous system disorders: Uncommon: headache, aseptic meningitis. The pathogenic mechanism of drug-induced aseptic meningitis is not clear. Available data on aseptic meningitis associated with NSAIDs suggest a hypersensitivity reaction (due to temporal association with drug use and resolution of symptoms after drug withdrawal). In patients with autoimmune diseases (systemic lupus erythematosus and mixed connective tissue disease), isolated cases of symptoms of aseptic meningitis (rigidity of the neck muscles, headache, nausea, vomiting, fever or disorientation) have been observed.
Cardiovascular system: frequency unknown: arterial hypertension, heart failure, edema.
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).
Blood and lymphatic system disorders: very rare: haematopoietic disorders (including anaemia, leukopenia, thrombocytopenia, pancytopenia and agranulocytosis). The first signs of such disorders are fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe exhaustion, unexplained bleeding and haematomas of unknown etiology.
Immune system disorders: uncommon: hypersensitivity reactions accompanied by urticaria and pruritus; very rare: severe hypersensitivity reactions, symptoms of which may include swelling of the face, tongue and larynx, shortness of breath, tachycardia, arterial hypotension (anaphylaxis, angioedema or severe shock). Hypersensitivity reactions may include: non-specific allergic reactions and anaphylaxis, airway reactivity including bronchial asthma, exacerbation of asthma, bronchospasm and dyspnoea, or various forms of skin reactions including pruritus, urticaria, purpura, angioedema, and less commonly, exfoliative and bullous dermatoses including toxic epidermal necrolysis, Stevens-Johnson syndrome and erythema multiforme.
Skin and subcutaneous tissue disorders: uncommon: various skin rashes; very rare: severe forms of skin reactions such as bullous reactions, including Stevens-Johnson syndrome, erythema multiforme and toxic epidermal necrolysis, may occur.
Laboratory indicators: very rare: decrease in hemoglobin level.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after the marketing authorisation of a medicinal product is an important procedure. It allows for continued monitoring of the benefit-risk balance of the medicinal product in question. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a contour blister pack; 5 contour blister packs in a pack.
Vacation category
Without a prescription.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
