Instructions for Nurofen Express Ultracap capsules 200mg No. 16
Composition
active ingredient: ibuprofen; 1 capsule contains ibuprofen 200 mg;
excipients: macrogol 600, potassium hydroxide, gelatin, sorbitol (E 420), ponceau 4R (E 124), Opacod WB white NS-78-18011, purified water.
Dosage form
Soft capsules.
Main physicochemical properties: red oval transparent soft gelatin capsules with the logo "NUROFEN" printed in white ink.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory and antirheumatic drugs. Propionic acid derivatives. ATC code M01A E01.
Pharmacological properties
Pharmacodynamics.
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.
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 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 considered unlikely with non-systematic use of ibuprofen.
Pharmacokinetics.
After oral administration, ibuprofen is rapidly absorbed from the gastrointestinal tract. The maximum concentration of the active substance in the blood plasma is determined 1-2 hours after administration. Ibuprofen is metabolized in the liver, excreted by the kidneys (90%) in an unchanged form and in the form of metabolites, as well as with bile. The half-life in healthy people is almost 1.8 hours, in patients with liver and kidney diseases - 1.8-3.5 hours. Ibuprofen actively (99%) binds to blood plasma proteins, slowly penetrates into the synovial cavities, where its concentration can remain high, while the concentration in the blood plasma decreases.
In two pharmacokinetic studies, the time to maximum plasma concentration (Tmax) for ibuprofen tablets was 60 and 90 minutes, compared to 35 and 40 minutes, respectively, for Nurofen® Express Ultracaps, soft capsules. The mean Cmax is reached twice as quickly for Nurofen® Express Ultracaps compared to the normal release formulation (Nurofen, tablets). Ibuprofen is detected in plasma for more than 8 hours after administration of Nurofen® Express Ultracaps.
Indication
Symptomatic treatment of headache, toothache and periodic menstrual pain. Fever and muscle pain with colds.
Contraindication
§ Hypersensitivity to ibuprofen or to any of the components of the drug.
§ Patients with a history of bronchospasm, asthma, rhinitis, angioedema or skin rash associated with the use of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs).
§ The use of Nurofen® Express Ultracap concomitantly with other NSAIDs, including selective cyclooxygenase-2 (COX-2) inhibitors, should be avoided.
§ Patients with a history of gastrointestinal bleeding or perforation after NSAID use.
Current or history of peptic ulcer/bleeding (two or more distinct episodes of ulcer exacerbation or bleeding).
Patients with severe renal, hepatic or cardiac (NYHA class IV) insufficiency.
§ Children weighing less than 20 kg.
§ Patients with cerebrovascular or other active forms of bleeding.
§ Patients with unclear etiology of hematopoietic disorders.
§ Patients with dehydration caused by vomiting, diarrhea, or insufficient fluid intake.
§ Last trimester of pregnancy.
Interaction with other medicinal products and other types of interactions
Ibuprofen (like other NSAIDs) should be used with caution in concomitant treatment with the following drugs:
other NSAIDs, including salicylates: increased risk of gastrointestinal ulcers and bleeding;
digoxin: the blood plasma level of both drugs increases;
corticosteroids: increased risk of gastrointestinal bleeding or ulceration;
antithrombotic agents: the risk of gastrointestinal bleeding increases;
Anticoagulants: NSAIDs may enhance the effects of anticoagulants, such as warfarin;
antiplatelet and selective serotonin inhibitors: the risk of gastrointestinal bleeding may increase;
Experimental data suggest that ibuprofen may inhibit the effect of low-dose acetylsalicylic acid (aspirin) on platelet aggregation when used concomitantly. However, limitations in extrapolating these data to the clinical situation prevent definitive conclusions that regular long-term use of ibuprofen may reduce the cardioprotective effect of low-dose acetylsalicylic acid. Such clinically significant effects are considered unlikely with non-systematic use of ibuprofen;
Antihypertensives and diuretics: NSAIDs may reduce the therapeutic effect of these drugs; in patients with impaired renal function, the simultaneous use of ACE inhibitors, beta-blockers or angiotensin-II receptor antagonists and agents that inhibit cyclooxygenase may lead to further deterioration of renal function. Therefore, the combination of drugs should be used with caution, especially in elderly patients;
Lithium and methotrexate: there is evidence of a potential increase in plasma levels of lithium and methotrexate;
Probenecid and sulfinpyrazone: may delay the elimination of ibuprofen;
potassium-sparing diuretics: may lead to hyperkalemia (checking the level of potassium in the blood plasma is recommended);
cyclosporine and tacrolimus: increased risk of nephrotoxicity;
zidovudine: there is evidence of an increased risk of hemarthrosis and hematoma in HIV-infected patients receiving concomitant treatment with zidovudine and ibuprofen;
sulfonylurea: it is necessary to monitor blood glucose levels;
Quinoline antibiotics: there may be a risk of seizures.
Cytochrome CYP2C9 inhibitor: may increase the effects of ibuprofen, such as voriconazole or fluconazole.
Application features
Side effects can be reduced by using the minimum effective dose needed to treat symptoms for a short period of time.
The drug should be used with caution in patients with:
systemic lupus erythematosus and systemic connective tissue diseases;
congenital disorder of porphyrin metabolism (e.g. acute intermittent porphyria);
a history of hypertension and/or heart failure, which were accompanied by fluid retention and edema during the use of NSAIDs;
impaired kidney and/or liver function;
immediately after operations.
This medicinal product contains sorbitol. It is not recommended for use in patients with hereditary fructose intolerance.
Allergic reactions are possible due to the presence of Ponceau 4R in the composition of the drug.
Elderly people are at increased risk of adverse reactions to NSAIDs, especially gastrointestinal bleeding and perforation, which can be fatal.
Gastrointestinal bleeding, ulceration or perforation, which can be fatal, has been reported with all NSAIDs and regardless of duration of treatment, with or without a history of serious gastrointestinal events.
Increasing the dose of NSAIDs, older age, and a history of peptic ulcer disease are risk factors for gastrointestinal adverse reactions. During treatment in these cases, it is recommended to use the minimum effective dose.
Combination therapy with protective drugs (e.g. misoprostol or proton pump inhibitors) should be considered, especially for patients requiring long-term use of low doses of acetylsalicylic acid or other drugs that may increase the risk of gastrointestinal side effects.
Clinical trial data suggest that ibuprofen use, particularly at high doses (2400 mg/day), may be associated with an increased risk of arterial thrombotic events (e.g. myocardial infarction or stroke). Overall, epidemiological data do not suggest that low-dose ibuprofen use (e.g. ≤ 1200 mg/day) is associated with 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.
The clinical picture should also be carefully assessed before starting long-term treatment in patients with risk factors for cardiovascular complications (e.g. hypertension, hyperlipidemia, diabetes mellitus, smoking), especially if high doses of ibuprofen (2400 mg per day) are required.
Cases of Kounis syndrome have been reported in patients treated with ibuprofen. Kounis syndrome is defined as cardiovascular symptoms caused by an allergic or hypersensitivity reaction associated with narrowing of the coronary arteries, potentially leading to myocardial infarction.
The drug should be used with caution in patients receiving concomitant therapy with drugs that may increase the risk of peptic ulcer or bleeding, in particular oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors or antiplatelet agents such as acetylsalicylic acid.
NSAIDs should be used with caution in patients with a history of ulcerative colitis or Crohn's disease, as their condition may worsen.
Severe skin adverse reactions
Severe cutaneous adverse reactions (SCARs), including exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), drug-induced eosinophilia with systemic symptoms (DRESS) and acute generalised exanthematous pustulosis (AGEP), which can be life-threatening or fatal, have been reported with ibuprofen (see section 4.8). Most of these reactions occurred within the first month of treatment.
If signs and symptoms suggestive of these reactions occur, ibuprofen should be discontinued immediately and alternative treatment considered (if necessary).
Masking the symptoms of underlying infections.
Nurofen® Express Ultracap may mask the symptoms of an infectious disease, which may delay the initiation of appropriate treatment and thereby complicate the course of the disease. This has been observed in bacterial community-acquired pneumonia and bacterial complications of chickenpox. When Nurofen® Express Ultracap is used for fever or to relieve pain in an infection, monitoring for the infectious disease is recommended. In outpatient settings, the patient should consult a doctor if symptoms persist or worsen.
Patients who have or have had bronchial asthma or allergic diseases may experience bronchospasm.
With prolonged use of painkillers in large doses, a headache may occur, which cannot be treated by increasing the dose of the drug.
Prolonged and uncontrolled use of painkillers, especially combinations of different painkilling active ingredients, can lead to chronic kidney damage with the risk of kidney failure (analgesic nephropathy).
There is some evidence that drugs that inhibit cyclooxygenase/prostaglandin synthesis may cause impairment of female fertility through effects on ovulation. This can be reversed by discontinuing these drugs.
Ibuprofen may temporarily inhibit blood/platelet function (platelet aggregation). Therefore, special monitoring is recommended in patients with bleeding disorders.
In case of prolonged use of the drug, it is necessary to regularly check liver function indicators, kidney function, as well as blood cell counts.
In case of chickenpox, treatment with the drug should be avoided.
Due to the simultaneous use of alcohol, side effects, especially those affecting the gastrointestinal tract or central nervous system, may be exacerbated after the use of NSAIDs.
NSAIDs can mask symptoms of infections and fever.
There is a risk of kidney failure in children and adolescents with dehydration.
Use during pregnancy or breastfeeding
Pregnancy. Prostaglandin synthesis inhibitors may have adverse effects on pregnant women and/or on the development of the embryo/foetus. Epidemiological data indicate an increased risk of miscarriage and cardiac malformations following the use of prostaglandin synthesis inhibitors in early pregnancy. The risk is believed to increase with increasing dose and duration of treatment.
From the 20th week of pregnancy, ibuprofen may cause oligohydramnios due to fetal renal dysfunction. This may occur shortly after initiation of treatment and is usually reversible after discontinuation of treatment. In addition, there have been reports of narrowing of the ductus arteriosus following treatment in the second trimester of pregnancy, most of which resolved after discontinuation of treatment. Therefore, ibuprofen should not be given during the first and second trimesters of pregnancy unless clearly necessary. If ibuprofen is used by a woman attempting to conceive or during the first and second trimesters of pregnancy, the dose should be kept as low and the duration of treatment as short as possible. Antenatal monitoring for oligohydramnios and narrowing of the ductus arteriosus should be considered after exposure to ibuprofen for several days from the 20th week of gestation. Nurofen® Express Ultracap should be discontinued if oligohydramnios or narrowing of the ductus arteriosus is detected.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may pose risks:
Risks to the fetus:
cardiopulmonary toxicity (premature narrowing/closure of the ductus arteriosus and pulmonary hypertension);
renal dysfunction (see above);
Risks for the mother at the end of pregnancy and for the newborn:
suppression of uterine contractions, leading to delayed or prolonged labor.
Therefore, Nurofen® Express Ultracap is contraindicated during the third trimester of pregnancy (see Section “Contraindications”).
Breastfeeding. Ibuprofen and its metabolites may pass into breast milk in low concentrations. No harmful effects on infants are known to date, therefore, as a rule, for short-term treatment of pain and fever at recommended doses, it is not necessary to discontinue breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
With short-term use, Nurofen® Express Ultracap has no or negligible effect on the ability to drive and use machines, but with long-term use, side effects from the central nervous system may occur, such as increased fatigue and dizziness.
Method of administration and doses
The lowest effective dose should be used for the shortest time necessary to relieve symptoms (see section "Special instructions").
The drug is recommended 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 at least 20 kg. The maximum daily dose of ibuprofen is 20–30 mg per kilogram of 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 to 39 kg: the recommended starting 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, with water.
Elderly people do not require special dose adjustment.
If symptoms persist for more than 3 days, and when used for pain relief for more than 4 days, you should consult a doctor for clarification of the diagnosis and adjustment of the treatment regimen. Undesirable effects can be minimized by using the lowest effective dose for the shortest period of time necessary to control symptoms.
Children. The use of the drug is contraindicated in children weighing less than 20 kg.
Overdose
In case of acute overdose, the symptoms depend on the amount of the drug taken and the time that has passed since its administration. The first symptoms that are usually observed are: nausea, vomiting, headache and dizziness, epigastric pain or, less often, diarrhea, drowsiness, nystagmus, blurred vision, tinnitus, gastrointestinal bleeding. In case of overdose, coma, arterial hypotension, hyperkalemia with cardiac arrhythmia, metabolic acidosis, increased body temperature, respiratory disorders and cyanosis, impaired renal function, liver damage may occur. Sometimes - agitation and disorientation, convulsions. After long-term administration, hemolytic anemia, granulocytopenia and thrombocytopenia may be observed sporadically.
If no more than 1 hour has passed after an acute overdose, it is recommended to induce vomiting, rinse the stomach, or take activated charcoal.
In cases of ibuprofen overdose, there is no antidote or specific treatment. Symptomatic treatment is based on monitoring vital functions with blood pressure measurement, ECG, and interpretation of symptoms indicating possible gastrointestinal bleeding, metabolic acidosis, and central nervous system disorders.
Side effects
The following is a list of adverse reactions that have been reported in people who have used ibuprofen for short-term treatment of mild to moderate pain and fever, as well as those observed with long-term high-dose therapy in patients with rheumatism.
Clinical trial data suggest that the use of ibuprofen, especially at a high dose of 2400 mg per day, may be associated with a slightly increased risk of arterial thrombotic complications (e.g. myocardial infarction or stroke).
The frequency of side effects is calculated as follows:
Very common: ≥1/10, common: ≥1/100, <1/10, uncommon: ≥1/1000, <1/100, rare: ≥1/10000, <1/1000, very rare: <1/10000, including isolated reports.
General disorders.
Uncommon: hypersensitivity in the form of urticaria and itching, increased sweating. Very rare: severe hypersensitivity reactions with the following manifestations: swelling of the face, tongue and larynx, shortness of breath, tachycardia, decreased blood pressure, anaphylactoid reactions (anaphylaxis, angioedema up to shock). Exacerbation of asthma and bronchospasm or dyspnoea, allergic rhinitis, eosinophilia.
From the sensory organs.
Rare: hearing impairment (hearing loss, ringing or tinnitus).
From the gastrointestinal tract.
Uncommon: abdominal pain, melena, haematemesis, dyspepsia and nausea.
Rare: diarrhea, flatulence, constipation and vomiting.
Very rare: heartburn, ulcerative stomatitis, gastritis, perforation or gastrointestinal bleeding (which may cause anemia), which can in some cases be fatal, especially in the elderly. Exacerbation of ulcerative colitis and Crohn's disease, oesophagitis, formation of intestinal diaphragmatic strictures. Irritation or dryness of the oral mucosa, gingival ulcers, aphthous stomatitis, pancreatitis.
Neurological disorders.
Uncommon: headache, dizziness, insomnia, anxiety, depression, nervousness and irritability or fatigue, psychomotor agitation, drowsiness, confusion, hallucinations;
rarely - aseptic meningitis (more often in patients with autoimmune diseases).
From the cardiovascular system.
Very rare: heart failure, tachycardia, increased blood pressure, vasculitis, myocardial infarction.
Not known: Kounis syndrome.
From the urinary system.
Very rare: decreased urea excretion and edema. Acute renal failure, allergic nephritis, glomerulonephritis, oliguria, polyuria, cystitis, hematuria. Papillonecrosis, especially with prolonged use. Increased serum urea levels.
On the part of the hepatobiliary system.
Very rare: liver dysfunction, especially with prolonged use. Hepatitis, pancreatitis, duodenitis, esophagitis.
From the blood and lymphatic system.
Very rare: disorders of the blood system (anemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis). The first signs are: high fever, sore throat, mouth ulcers, flu symptoms, severe exhaustion, nosebleeds and bruising.
From the skin and subcutaneous tissue.
Very rare: severe cutaneous adverse reactions (SCARs) (including erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis), alopecia.
Not known: drug-induced eosinophilia with systemic symptoms (DRESS syndrome); acute generalized exanthematous pustulosis; photosensitivity reactions.
From the immune system.
Uncommon: in patients with autoimmune disorders (systemic lupus erythematosus, systemic connective tissue diseases) during treatment with ibuprofen, isolated cases of symptoms of aseptic meningitis (rigidity of the occipital muscles, headache, nausea, vomiting, high fever or disorientation), swelling of the face, tongue and larynx, shortness of breath, tachycardia. Allergic reactions in the form of skin rashes, itching, bronchial asthma attacks, decreased blood pressure have been observed.
Infections and parasitic diseases.
Very rare: Exacerbation of inflammation associated with infection.
Laboratory tests: Rare: Decreased hemoglobin.
Expiration date
2 years.
Storage conditions
Store out of the reach of children at a temperature not exceeding 25 °C.
Packaging
4 or 10 capsules in a blister; 1 blister in a cardboard box.
8 capsules in a blister; 2 blisters in a cardboard box.
Vacation category
Without a prescription.
Producer
Reckitt Benckiser Healthcare International Limited.
Location of the manufacturer and address of its place of business. Nottingham site, Thane Road, Nottingham, NG90 2DB, United Kingdom
