Nurofen^® Express (Tablets, Capsules, Gel) Instructions for Use

ATC Code

M01AE01 (Ibuprofen)

Active Substance

Ibuprofen (Rec.INN registered by WHO)

Clinical-Pharmacological Group

NSAID

Pharmacotherapeutic Group

NSAID

Pharmacological Action

The mechanism of action of ibuprofen, a propionic acid derivative from the NSAID group, is due to the inhibition of prostaglandin synthesis – mediators of pain, inflammation, and hyperthermic reaction.

It non-selectively blocks COX-1 and COX-2, thereby inhibiting prostaglandin synthesis. It has a rapid targeted effect against pain (analgesic), antipyretic and anti-inflammatory effect. Furthermore, Ibuprofen reversibly inhibits platelet aggregation.

Pharmacokinetics

Absorption and Distribution

Absorption is high; it is rapidly and almost completely absorbed from the gastrointestinal tract. After taking 2 capsules of the drug on an empty stomach, Ibuprofen is detected in blood plasma within 10 minutes; C_max of ibuprofen in blood plasma is reached within 30-40 minutes, which is twice as fast as after taking an equivalent dose of the drug Nurofen^® in the form of 200 mg film-coated tablets. Taking the drug with food may increase T_max.

Plasma protein binding is more than 90%. It slowly penetrates into the joint cavity, is retained in the synovial fluid, creating higher concentrations there than in blood plasma. In limited studies, Ibuprofen was detected in breast milk in very low concentrations.

Metabolism and Excretion

After absorption, about 60% of the pharmacologically inactive R-form slowly transforms into the active S-form. It is metabolized in the liver. T_1/2 is 2 hours. It is excreted by the kidneys (unchanged, no more than 1%) and, to a lesser extent, with bile.

Pharmacokinetics in Special Patient Groups

In elderly people, no significant differences in the pharmacokinetic profile of the drug were found compared to younger people.

Indications

• Headache;
• Migraine;
• Toothache;
• Painful menstruation;
• Neuralgia;
• Back pain;
• Muscle pain;
• Rheumatic pain;
• Febrile condition in influenza and colds.

ICD codes

Dosage Regimen

Capsules

The drug is taken orally. The capsule should be swallowed whole without chewing, with water.

Nurofen^® Express is intended only for short-term use.

For adults and children over 12 years old, it is recommended to take 200 mg (1 capsule) 3-4 times/day. The interval between doses of the drug should be 6-8 hours.

To achieve a faster therapeutic effect in adults, the dose can be increased to 400 mg (2 capsules) up to 3 times/day.

The maximum daily dose is 1200 mg.

The maximum daily dose for children aged 12-17 years is 1000 mg.

If symptoms persist or worsen when taking the drug for 2-3 days, the patient must discontinue treatment and consult a doctor.

Tablets

Take orally. The individual dosing regimen depends on the indications, severity of clinical manifestations, and the patient’s age.

A single dose for adults and children over 6 years old is 200-400 mg. It can be taken 3-4 times a day.

The maximum daily dose for adults is 1200 mg; for children aged 12-17 years – 1000 mg; for children aged 6 to 12 years – 800 mg.

For children under 6 years of age, the dose depends on the child’s age and body weight. The maximum daily dose should not exceed 30 mg/kg of body weight with intervals between doses of 6-8 hours.

Gel

For external use. Apply to the affected area 2-3 times/day.

Adverse Reactions

The risk of side effects can be minimized by taking the drug for a short course, at the minimum effective dose necessary to relieve symptoms.

Side effects are predominantly dose-dependent.

The following adverse reactions were noted with short-term use of ibuprofen in doses not exceeding 1200 mg/day (6 capsules). When treating chronic conditions and with long-term use, other adverse reactions may occur.

The assessment of the frequency of adverse reactions is based on the following criteria: very common (≥1/10), common (from ≥1/100 to <1/10), uncommon (from ≥1/1000 to <1/100), rare (from ≥1/10,000 to <1/1000), very rare (<1/10,000), frequency unknown (insufficient data to estimate frequency).

Blood and lymphatic system disorders: very rare – hematopoietic disorders (anemia, leukopenia, aplastic anemia, hemolytic anemia, thrombocytopenia, pancytopenia, agranulocytosis). The first symptoms of such disorders are fever, sore throat, superficial mouth ulcers, flu-like symptoms, severe weakness, nosebleeds and subcutaneous hemorrhages, bleeding and bruising of unknown etiology.

Immune system disorders: uncommon – hypersensitivity reactions – nonspecific allergic reactions and anaphylactic reactions, respiratory tract reactions (bronchial asthma, including its exacerbation, bronchospasm, shortness of breath, dyspnea), skin reactions (itching, urticaria, purpura, angioedema, exfoliative and bullous dermatoses, including toxic epidermal necrolysis (Lyell’s syndrome), Stevens-Johnson syndrome, erythema multiforme), allergic rhinitis, eosinophilia; very rare – severe hypersensitivity reactions, including facial, tongue and laryngeal swelling, shortness of breath, tachycardia, arterial hypotension (anaphylaxis, angioedema or severe anaphylactic shock).

Gastrointestinal disorders: uncommon – abdominal pain, nausea, dyspepsia (including heartburn, bloating); rare – diarrhea, flatulence, constipation, vomiting; very rare – peptic ulcer, perforation or gastrointestinal bleeding, melena, hematemesis, in some cases fatal, especially in elderly patients, ulcerative stomatitis, gastritis; frequency unknown – exacerbation of colitis and Crohn’s disease.

Hepatobiliary disorders very rare – liver function disorders (especially with long-term use), hepatitis and jaundice.

Renal and urinary disorders: very rare – acute renal failure (compensated and decompensated) especially with long-term use, in combination with increased plasma urea concentration and the appearance of edema, hematuria and proteinuria, nephritic syndrome, nephrotic syndrome, papillary necrosis, interstitial nephritis, cystitis.

Nervous system disorders: uncommon – headache; very rare – aseptic meningitis.

Cardiac disorders: frequency unknown – heart failure, peripheral edema, with long-term use increased risk of thrombotic complications (e.g., myocardial infarction), increased blood pressure.

Respiratory, thoracic and mediastinal disorders: frequency unknown – bronchial asthma, bronchospasm, shortness of breath.

General disorders and administration site conditions very rare – edema, including peripheral.

Investigations: possible decrease in hematocrit or hemoglobin; bleeding time may increase; plasma glucose concentration may decrease; creatinine clearance may decrease; serum creatinine concentration may increase; liver transaminase activity may increase.

If side effects occur, discontinue the drug and consult a doctor.

Contraindications

• Hypersensitivity to ibuprofen or any of the components of the drug;
• Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses, and intolerance to acetylsalicylic acid or other NSAIDs (including in history);
• Erosive and ulcerative diseases of the gastrointestinal tract (including peptic ulcer of the stomach and duodenum, Crohn’s disease, ulcerative colitis) or ulcer bleeding in the active phase or in history (two or more confirmed episodes of peptic ulcer or ulcer bleeding);
• History of gastrointestinal ulcer bleeding or perforation provoked by the use of NSAIDs;
• Severe hepatic failure or active liver disease;
• Severe renal failure (creatinine clearance <30 ml/min), confirmed hyperkalemia;
• Severe heart failure (NYHA class IV);
• Decompensated heart failure;
• Period after coronary artery bypass graft surgery;
• Cerebrovascular or other bleeding;
• Hemophilia and other blood clotting disorders (including hypocoagulation);
• Hemorrhagic diathesis;
• Fructose intolerance;
• Third trimester of pregnancy;
• Children under 12 years of age.

With caution

In the presence of the conditions listed in this section, the patient should consult a doctor before using the drug.

Concomitant use of other NSAIDs, history of a single episode of gastric ulcer or gastrointestinal ulcer bleeding; gastritis, enteritis, colitis, presence of Helicobacter pylori infection, ulcerative colitis; bronchial asthma or allergic diseases in the exacerbation phase or in history – bronchospasm may develop; systemic lupus erythematosus or mixed connective tissue disease (Sharp’s syndrome) – increased risk of aseptic meningitis; chickenpox; renal failure, including with dehydration (creatinine clearance less than 30-60 ml/min), nephrotic syndrome, hepatic failure, liver cirrhosis with portal hypertension, hyperbilirubinemia, arterial hypertension and/or heart failure, cerebrovascular diseases, blood diseases of unclear etiology (leukopenia and anemia), severe somatic diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, frequent alcohol consumption, simultaneous use of drugs that may increase the risk of ulcers or bleeding, in particular, oral corticosteroids (including prednisolone), anticoagulants (including warfarin), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline) or antiplatelet agents (including acetylsalicylic acid, clopidogrel), first and second trimesters of pregnancy, breastfeeding period, elderly age.

Use in Pregnancy and Lactation

The use of the drug is contraindicated in the third trimester of pregnancy. The use of the drug in the first and second trimesters of pregnancy should be avoided; if it is necessary to take the drug, consult a doctor.

There is evidence that Ibuprofen may pass into breast milk in small amounts without any negative consequences for the health of the breastfed infant, so usually with short-term use there is no need to stop breastfeeding. If long-term use of the drug is necessary, consult a doctor to decide on discontinuing breastfeeding during the period of drug use.

Information for women planning pregnancy these drugs suppress COX and prostaglandin synthesis, affect ovulation, disrupting female reproductive function (reversible after discontinuation of treatment).

Use in Hepatic Impairment

The drug is contraindicated in severe hepatic failure or active liver disease.

It should be prescribed with caution in hepatic failure, liver cirrhosis with portal hypertension.

Use in Renal Impairment

The drug is contraindicated in severe renal failure (creatinine clearance <30 ml/min).

It should be prescribed with caution in renal failure, including with dehydration (creatinine clearance less than 30-60 ml/min), nephrotic syndrome.

Pediatric Use

Contraindicated in children under 12 years of age.

Geriatric Use

Prescribe with caution to elderly patients.

Special Precautions

It is recommended to take the drug for the shortest possible course and at the minimum effective dose necessary to relieve symptoms.

During long-term treatment, monitoring of the peripheral blood picture and the functional state of the liver and kidneys is necessary.

If symptoms of gastropathy appear, careful monitoring is indicated, including esophagogastroduodenoscopy, complete blood count (hemoglobin determination), stool test for occult blood.

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study.

During treatment, ethanol intake is not recommended.

Patients with renal failure should consult a doctor before using the drug, as there is a risk of worsening renal function.

Patients with arterial hypertension, including in history, and/or chronic heart failure should consult a doctor before using the drug, as the drug may cause fluid retention, increased blood pressure and edema.

In patients with uncontrolled arterial hypertension, congestive heart failure NYHA class II-III, coronary artery disease, peripheral arterial diseases and/or cerebrovascular diseases, Ibuprofen should be prescribed only after careful assessment of the benefit-risk ratio, and the use of high doses of ibuprofen (≥2400 mg/day) should be avoided.

The use of NSAIDs in patients with chickenpox may be associated with an increased risk of severe purulent complications of infectious and inflammatory diseases of the skin and subcutaneous tissue (e.g., necrotizing fasciitis). Therefore, it is recommended to avoid using the drug for chickenpox.

Effect on ability to drive vehicles and operate machinery

Patients who experience dizziness, drowsiness, lethargy or visual disturbances when taking ibuprofen should avoid driving vehicles or operating machinery.

Overdose

In children, overdose symptoms may occur after taking a dose exceeding 400 mg/kg of body weight. In adults, the dose-dependent effect of overdose is less pronounced. The T_1/2 of the drug in overdose is 1.5-3 hours.

Symptoms: nausea, vomiting, epigastric pain or, less commonly, diarrhea, tinnitus, headache and gastrointestinal bleeding. In more severe cases, manifestations from the central nervous system are observed: drowsiness, rarely – agitation, convulsions, disorientation, coma. In cases of severe poisoning, metabolic acidosis and increased prothrombin time, renal failure, liver tissue damage, decreased blood pressure, respiratory depression and cyanosis may develop. In patients with bronchial asthma, exacerbation of this disease is possible.

Treatment is symptomatic, with mandatory provision of airway patency, monitoring of ECG and basic vital signs until the patient’s condition normalizes. Oral administration of activated charcoal or gastric lavage within 1 hour after taking a potentially toxic dose of ibuprofen is recommended. If Ibuprofen has already been absorbed, alkaline drinking may be prescribed to excrete the acidic derivative of ibuprofen by the kidneys, forced diuresis. Frequent or prolonged convulsions should be controlled by intravenous administration of diazepam or lorazepam. If bronchial asthma worsens, the use of bronchodilators is recommended.

Drug Interactions

Concomitant use of ibuprofen with the drugs listed below should be avoided.

Acetylsalicylic acid except for low doses of acetylsalicylic acid (not more than 75 mg/day) prescribed by a doctor, since concomitant use may increase the risk of side effects. When used concomitantly, Ibuprofen reduces the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (an increase in the frequency of acute coronary insufficiency is possible in patients receiving low doses of acetylsalicylic acid as an antiplatelet agent after starting ibuprofen).

Other NSAIDs, particularly selective COX-2 inhibitors: The concomitant use of two or more drugs from the NSAID group should be avoided due to a possible increased risk of side effects.

The drug should be used with caution when taken concomitantly with the medicines listed below.

Anticoagulants and thrombolytic drugs NSAIDs may enhance the effect of anticoagulants, in particular warfarin, and thrombolytic drugs.

Antihypertensive agents (ACE inhibitors and angiotensin II receptor antagonists) and diuretics NSAIDs may reduce the effectiveness of drugs in these groups. Diuretics and ACE inhibitors may increase the nephrotoxicity of NSAIDs.

Corticosteroids increased risk of gastrointestinal ulceration and gastrointestinal bleeding.

Antiaggregants and selective serotonin reuptake inhibitors increased risk of gastrointestinal bleeding.

Cardiac glycosides concomitant administration of NSAIDs and cardiac glycosides may lead to worsening of heart failure, decreased glomerular filtration rate, and increased plasma concentration of cardiac glycosides.

Lithium preparations there is evidence of a probable increase in plasma lithium concentration during the use of NSAIDs.

Methotrexate there is evidence of a probable increase in plasma methotrexate concentration during the use of NSAIDs.

Cyclosporine increased risk of nephrotoxicity with concomitant administration of NSAIDs and cyclosporine.

Mifepristone: NSAID use should be started no earlier than 8-12 days after taking mifepristone, as NSAIDs may reduce the effectiveness of mifepristone.

Tacrolimus: concomitant administration of NSAIDs and tacrolimus may increase the risk of nephrotoxicity.

Zidovudine concomitant use of NSAIDs and zidovudine may lead to increased hematotoxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive patients with hemophilia receiving combined treatment with zidovudine and ibuprofen.

Quinolone antibiotics in patients receiving combined treatment with NSAIDs and quinolone antibiotics, an increased risk of seizures is possible.

Cefamandole, cefoperazone, cefotetan, valproic acid, plicamycin increased incidence of hypoprothrombinemia.

Drugs that block tubular secretion: decreased excretion and increased plasma concentration of ibuprofen.

Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants): increased production of hydroxylated active metabolites, increased risk of severe intoxications.

Inhibitors of microsomal oxidation reduced risk of hepatotoxic effects.

Oral hypoglycemic drugs, sulfonylurea derivatives and insulin enhanced effect.

Antacids and cholestyramine reduced absorption.

Caffeine enhanced analgesic effect.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years. Do not use the drug after the expiration date.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.