Instructions for Gofen 400 soft capsules 400 mg blister No. 60
Composition
active ingredient: ibuprofen;
1 soft capsule contains 400 mg of ibuprofen;
excipients: polyethylene glycol 600, potassium hydroxide, purified water;
Gelatin capsule: gelatin, non-crystallizing sorbitol solution (E 420), purified water.
Dosage form
Soft capsules.
Main physicochemical properties: oblong soft capsules with a transparent shell of natural color, the contents of the capsule are a transparent, colorless oily liquid.
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 in 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 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 acetylsalicylic acid (81 mg) have been shown to reduce the effect of acetylsalicylic acid (aspirin) 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 considered unlikely with non-systematic use of ibuprofen.
Pharmacokinetics
When taken orally, ibuprofen is rapidly absorbed, partially in the stomach and then completely in the small intestine.
After metabolism in the liver (hydroxylation, carboxylation, conjugation), pharmacologically inactive metabolites are completely excreted mainly in the urine (90%), as well as in the bile. The half-life in healthy volunteers, as well as in patients with liver and kidney diseases, is 1.8–3.5 hours. Binding to plasma proteins is approximately 99%. With oral administration of the usual release dosage form, the maximum concentration in the blood plasma is reached after 1–2 hours. Ibuprofen is detected in the plasma for more than 8 hours after taking the drug.
Indication
Symptomatic treatment of mild to moderate pain of various origins (headache, toothache, painful menstruation), including colds and fever.
Contraindication
Hypersensitivity to ibuprofen or to any of the components of the drug. Hypersensitivity reactions (e.g. bronchial asthma, rhinitis, angioedema or urticaria) previously observed after taking ibuprofen, acetylsalicylic acid (aspirin) or other NSAIDs. Gastric ulcer/bleeding in active form or recurrent in history (two or more severe episodes of ulcer or bleeding). Gastrointestinal bleeding or perforation associated with the use of NSAIDs in history. Severe hepatic impairment, severe renal impairment, severe heart failure (class IV according to the NYHA classification). Last trimester of pregnancy. Cerebrovascular or other bleeding in the active phase. Hemorrhagic diathesis or blood clotting disorders. Hematopoietic disorders of unknown etiology. Severe dehydration (caused by vomiting, diarrhea, or insufficient fluid intake).
Interaction with other medicinal products and other types of interactions
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 effect of low-dose acetylsalicylic acid (aspirin) on platelet aggregation when used concomitantly. However, the limitations of extrapolation of these data to the clinical situation do not allow definitive conclusions to be drawn that regular long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid. With non-systematic use of ibuprofen, such clinically significant effects are considered unlikely; other NSAIDs, including selective cyclooxygenase-2 inhibitors:
The simultaneous use of several NSAIDs may increase the risk of gastrointestinal ulcers and bleeding due to a synergistic effect. Therefore, concomitant use of ibuprofen with other NSAIDs should be avoided.
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 diuretics and other antihypertensive 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. Therefore, such combinations should be prescribed with caution, especially in elderly patients. If long-term 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 of ibuprofen and potassium-sparing diuretics may lead to hyperkalemia (serum potassium monitoring is recommended); corticosteroids: increased risk of gastrointestinal ulcers and bleeding; antiplatelet agents and selective serotonin reuptake inhibitors: may increase the 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: use of ibuprofen within 24 hours before or after methotrexate administration may lead to increased methotrexate concentrations and increased toxicity; 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: possible increased risk of nephrotoxicity with concomitant use of NSAIDs and tacrolimus; zidovudine: an increased risk of haematological toxicity is known 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; quinolone antibiotics: concomitant use with ibuprofen may increase the risk of convulsions; sulfonylureas: blood glucose monitoring is recommended as a precautionary measure when used concomitantly; probenecid and sulfinpyrazone: may delay the excretion of ibuprofen.
Application features
The side effects of ibuprofen and the entire group of NSAIDs in general can be reduced by using the minimum 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.
Respiratory effects. Bronchospasm may occur in patients with or with a history of bronchial asthma or allergic diseases. Other NSAIDs. Concomitant use of ibuprofen with other NSAIDs, including selective cyclooxygenase-2 inhibitors, increases the risk of adverse reactions and should be avoided. Systemic lupus erythematosus and mixed connective tissue diseases. Ibuprofen should be used with caution in patients with systemic lupus erythematosus and mixed connective tissue diseases due to an increased risk of aseptic meningitis. Porphyrin metabolism. Caution should be exercised in patients with congenital disorders of porphyrin metabolism (e.g. acute intermittent porphyria). 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 data and epidemiological data suggest that the use of ibuprofen, especially at high doses (2400 mg/day), may be associated with a slightly increased risk of arterial thrombotic events (e.g. myocardial infarction or stroke). Overall, epidemiological studies do not suggest that low-dose ibuprofen (e.g. ≤ 1200 mg/day) may lead to an increased risk of arterial thrombotic events.
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.
Effects on the kidneys. Ibuprofen should be used with caution in patients with impaired renal function, as renal function may deteriorate. Effects on the liver. Liver function may deteriorate. Surgery. Caution should be exercised immediately after major surgery. Effects on female fertility. There is limited evidence that medicinal products that inhibit cyclooxygenase/prostaglandin synthesis may impair female fertility by affecting ovulation in long-term use (applies to doses of 2400 mg per day and treatment durations exceeding 10 days). This is reversible after discontinuation of treatment. Effects on the gastrointestinal system. NSAIDs should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease) as these conditions may be exacerbated. There are reports of cases of gastrointestinal bleeding, perforation, ulceration, possibly 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, and ulceration increases with increasing doses of NSAIDs, in patients with a history of ulcer, especially complicated by bleeding or perforation, and in elderly patients. Such patients should start treatment with minimal doses. For such patients, as well as for those who require concomitant use of low-dose acetylsalicylic acid or other drugs that may increase the risk for the gastrointestinal tract, the need for combination therapy with protective drugs (e.g. misoprostol or proton pump inhibitors) should be considered.
Patients with a history of gastrointestinal disorders, especially elderly patients, should be informed of any unusual gastrointestinal symptoms (especially gastrointestinal bleeding), particularly at the beginning of treatment.
Caution should be exercised when treating patients receiving 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 effects. 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 early in therapy; in most cases, the onset of such reactions occurs within the first month of treatment. Ibuprofen should be discontinued at the first sign of skin rash, mucosal lesions or any other sign of hypersensitivity.
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.
Allergy: Caution should be exercised in patients with known allergic reactions to other substances, as these patients are also at increased risk of developing hypersensitivity reactions when using ibuprofen.
Patients suffering from hay fever, nasal polyps, chronic obstructive airways disease, or a history of allergic diseases are at increased risk of allergic reactions, which may manifest as asthma attacks (so-called analgesic asthma), angioedema, or urticaria.
This medicinal product contains sorbitol solution. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicinal product.
Other. Severe acute hypersensitivity reactions (e.g. anaphylactic shock) have been observed very rarely. At the first signs of a hypersensitivity reaction after use of the drug, therapy should be discontinued. In such cases, both symptomatic and specialized therapy should be carried out.
Ibuprofen may temporarily inhibit platelet function (affect platelet aggregation). Therefore, it is recommended to carefully monitor the condition of patients with blood clotting disorders.
With long-term use of the drug, it is necessary to regularly check liver and kidney function indicators, as well as check the blood picture.
Long-term use of any painkiller for headache may worsen this condition. If this condition is suspected or confirmed, consult a doctor and discontinue treatment. A diagnosis 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.
When using NSAIDs while drinking alcohol, the risk of adverse effects related to the active substance may increase, especially from the gastrointestinal tract or CNS.
Ability to influence reaction speed when driving vehicles or other mechanisms
Patients who experience dizziness, drowsiness or visual disturbances while taking ibuprofen should avoid driving or operating machinery. Single administration or short-term use of ibuprofen usually does not require any special precautions. This mainly applies to the simultaneous use of the drug with alcohol.
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
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 absolute risk of cardiovascular malformations increased from 1% to approximately 1.5%. The risk is believed to increase with increasing dose and duration of therapy.
NSAIDs should not be taken during the first two trimesters of pregnancy unless, in the opinion of the physician, the potential benefit to the patient outweighs 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 possible period of time.
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 the 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. Therefore, ibuprofen is contraindicated during the third trimester of pregnancy.
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.
Fertility.
The use of ibuprofen may affect female fertility. This effect is reversible upon discontinuation of treatment. Therefore, the use of ibuprofen is not recommended in women who have difficulty conceiving.
Method of administration and doses
For oral use in adults and children aged 12 years and over with a body weight > 40 kg. For short-term use only. Undesirable effects can be minimized by using the lowest effective dose for the shortest period of time necessary to control symptoms.
Capsules should be taken preferably during or after meals, without chewing and with water.
The single dose for children aged 12 years and over with a body weight of > 40 kg and adults is 1 capsule (400 mg ibuprofen). If necessary, 1 capsule can be used every 6 hours. The maximum daily dose is 1200 mg (3 capsules per day). Use the minimum effective dose necessary to treat symptoms for the shortest possible period of time.
Elderly patients do not require special dose adjustment, except in cases of severe renal or hepatic insufficiency.
If the symptoms of the disease worsen or persist for more than 3 days, you should consult a doctor to clarify the diagnosis and adjust the treatment regimen. The duration of treatment is determined by the doctor individually, depending on the course of the disease and the patient's condition.
Children
Do not use in children under 12 years of age and weighing < 40 kg.
Overdose
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.
Treatment. Treatment should be symptomatic and supportive, and include maintaining a patent airway and monitoring cardiac and vital signs until the condition returns to normal. 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 administered to accelerate the excretion of acidic ibuprofen in the urine. Intravenous diazepam or lorazepam should be used for frequent or prolonged seizures. Bronchodilators should be used for the treatment of acute asthma.
Adverse reactions
The following adverse reactions have been observed with short-term use of ibuprofen at doses not exceeding 1200 mg per day. In the treatment of chronic diseases, additional adverse effects may occur with long-term use.
Adverse reactions that occurred with ibuprofen are listed by organ system and frequency of occurrence.
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 frequency unknown (cannot be estimated from the available data).
Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
The most common adverse reactions are gastrointestinal in nature and are mostly dose-dependent, in particular the risk of gastrointestinal bleeding, which is dose- and duration-dependent. Adverse reactions are less common when the maximum daily dose does not exceed 1200 mg.
Clinical trial data suggest that the use of ibuprofen, especially at high doses of 2400 mg per day, may be associated with a slightly increased risk of arterial thrombotic complications (such as myocardial infarction or stroke).
Blood and lymphatic system disorders: Very rare: haematopoietic disorders (anaemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis). The first signs are fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe exhaustion, unexplained bleeding and bruising.
Immune system disorders: Rare: hypersensitivity reactions including urticaria and pruritus; very rare: severe hypersensitivity reactions, symptoms of which may include swelling of the face, tongue and larynx, shortness of breath, tachycardia, hypotension, anaphylactic reactions, angioedema or severe shock; frequency unknown: airway reactivity including bronchial asthma, exacerbation of asthma, bronchospasm.
Nervous system disorders: Uncommon: headache; very rare: aseptic meningitis, some symptoms of which (rigidity of the occipital muscles, headache, nausea, vomiting, fever or disorientation) may occur in patients with existing autoimmune diseases such as systemic lupus erythematosus, mixed connective tissue disease; frequency unknown: dizziness, paresthesia, drowsiness.
From the side of the cardiovascular system. Frequency unknown: heart failure, edema.
Vascular disorders: Frequency unknown: arterial hypertension.
Gastrointestinal disorders: Uncommon: abdominal pain, nausea and dyspepsia; rare: diarrhoea, flatulence, constipation and vomiting; very rare: peptic ulcer, perforation or gastrointestinal bleeding, melena, haematemesis, sometimes fatal (especially in elderly patients), ulcerative stomatitis, gastritis; frequency unknown: exacerbation of colitis and Crohn's disease.
Hepatic disorders: Very rare: liver dysfunction.
Skin and subcutaneous tissue disorders: Rare: 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.
Renal and urinary disorders: Very rare: acute renal failure, papillonecrosis, especially with prolonged use, associated with increased serum urea levels, and edema.
Laboratory tests: Very rare: decreased hemoglobin.
Expiration date
2 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging.
Keep out of reach of children.
Packaging
10 capsules in a blister, 6 blisters in a cardboard box.
Vacation category
Without a prescription.
Producer
Mega Lifesciences Public Company Limited.
Location of the manufacturer and its business address
Factory 1 384, Moo 4, Soi 6, Bangpu Industrial Estate, Pattana 3 Road, Phraeksa, Mueang 10280 Samut Prakan Thailand.
