Nurofast^® (Tablets, Capsules) 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 action against pain (analgesic), antipyretic, and anti-inflammatory effects. Furthermore, Ibuprofen reversibly inhibits platelet aggregation. The analgesic effect of the drug lasts up to 8 hours.

Pharmacokinetics

Absorption and Distribution

Absorption is high; it is rapidly and almost completely absorbed from the gastrointestinal tract. After taking the drug on an empty stomach, C_max of ibuprofen in blood plasma is reached within 45 minutes. Taking the drug with food may increase T_max to 1-2 hours. Plasma protein binding is 90%.

It slowly penetrates into the joint cavity, is retained in the synovial fluid, creating higher concentrations there than in the blood plasma. Lower concentrations of ibuprofen are detected in the cerebrospinal fluid compared to 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 is slowly transformed into the active S-form. It undergoes metabolism in the liver. T_1/2 is 2 hours. It is excreted by the kidneys (unchanged, not more than 1%) and, to a lesser extent, with bile.

Indications

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

ICD codes

Dosage Regimen

Tablets, Capsules

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

A single dose for adults and children over 6 years of age 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.

Adverse Reactions

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

Elderly people have an increased frequency of adverse reactions against the background of NSAID use, especially gastrointestinal bleeding and perforations, in some cases with fatal outcomes.

Side effects are predominantly dose-dependent.

The adverse reactions listed below were noted with short-term use of ibuprofen in doses not exceeding 1200 mg/day (6 tablets).

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 ≥1/10000 to <1/1000), very rare (<1/10000), frequency unknown (data to assess frequency is insufficient).

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 swelling of the face, tongue and larynx, 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 with fatal outcome, especially in elderly patients, ulcerative stomatitis, gastritis; frequency unknown – exacerbation of colitis and Crohn’s disease.

Hepatobiliary disorders very rare – liver function disorders, increased activity of liver transaminases, hepatitis and jaundice.

Renal and urinary disorders very rare – acute renal failure (compensated and decompensated) especially with long-term use, combined with an increase in 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.

Laboratory parameters decrease in hematocrit or hemoglobin; increased bleeding time; decrease in plasma glucose concentration; decrease in CC; increase in plasma creatinine concentration; increase in activity of liver transaminases.

If side effects occur, the patient should stop taking the drug and consult a doctor.

Contraindications

• Hypersensitivity to ibuprofen or any of the components included in 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);
• Bleeding or perforation of a gastrointestinal ulcer in history, provoked by the use of NSAIDs;
• Severe heart failure (NYHA class IV);
• Severe hepatic failure or active liver disease;
• Severe renal failure (CC <30 ml/min), confirmed hyperkalemia;
• Decompensated heart failure;
• Period after coronary artery bypass surgery;
• Cerebrovascular or other bleeding;
• Hemophilia and other blood clotting disorders (including hypocoagulation);
• Hemorrhagic diathesis;
• III trimester of pregnancy;
• Children under 6 years of age.

With caution

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

Concomitant use of other NSAIDs, history of a single episode of gastric and duodenal ulcer or gastrointestinal ulcer bleeding; gastritis, enteritis, colitis, presence of Helicobacter pylori infection, ulcerative colitis; bronchial asthma or allergic diseases in the acute stage 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 (CC 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 artery 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), I and II trimesters of pregnancy, breastfeeding period, elderly age, age under 12 years.

Use in Pregnancy and Lactation

The use of the drug is contraindicated in the III trimester of pregnancy. The use of the drug in the I and II trimesters of pregnancy should be avoided; if it is necessary to take the drug, you should 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, you should consult a doctor to decide on stopping breastfeeding during the period of drug use.

Use in Hepatic Impairment

Contraindicated in severe hepatic failure or active liver disease.

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

Use in Renal Impairment

Contraindicated in severe renal failure (CC <30 ml/min).

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

Pediatric Use

Contraindicated in children under 6 years of age.

The drug should be prescribed with caution to children under 12 years of age.

Geriatric Use

The drug should be prescribed 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. If it is necessary to take the drug for more than 10 days, you should consult a doctor.

In patients with bronchial asthma or an allergic disease in the acute stage, as well as in patients with a history of bronchial asthma/allergic disease, the drug may provoke bronchospasm.

The use of the drug in patients with systemic lupus erythematosus or mixed connective tissue disease is associated with an increased risk of developing aseptic meningitis.

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, it is not recommended to take ethanol.

Patients with renal failure should consult a doctor before using the drug, as there is a risk of deterioration in 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 artery diseases and/or cerebrovascular diseases, Ibuprofen should be prescribed only after a thorough 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 developing severe purulent complications of infectious and inflammatory diseases of the skin and subcutaneous fat (e.g., necrotizing fasciitis). In this regard, it is recommended to avoid using the drug for chickenpox.

Information for women planning pregnancy: the drug suppresses COX and prostaglandin synthesis, affects ovulation, disrupting female reproductive function (reversible after discontinuation of treatment).

Effect on ability to drive vehicles and machinery

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

Overdose

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

Symptoms nausea, vomiting, pain in the epigastric region 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, an exacerbation of this disease is possible.

Treatment 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 stopped by intravenous administration of diazepam or lorazepam. If bronchial asthma worsens, the use of bronchodilators is recommended.

Drug Interactions

Combinations to 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, in particular, selective COX-2 inhibitors the simultaneous use of two or more drugs from the NSAID group should be avoided due to the possible increase in the risk of side effects.

Combinations to be used with caution

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

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

In some patients with impaired renal function (for example, in patients with dehydration or in elderly patients with impaired renal function), the simultaneous administration of ACE inhibitors or angiotensin II antagonists and COX-inhibiting agents may lead to worsening of renal function, including the development of acute renal failure (usually reversible).

These interactions should be considered in patients taking coxibs concurrently with ACE inhibitors or angiotensin II antagonists.

In this regard, the combined use of the above agents should be prescribed with caution, especially in elderly persons.

Dehydration in patients should be prevented, and the possibility of monitoring renal function after initiation of such combined treatment and periodically thereafter should be considered.

Diuretics and ACE inhibitors may increase the nephrotoxicity of NSAIDs.

Corticosteroids increased risk of GI ulcers and gastrointestinal bleeding.

Antiplatelet agents and selective serotonin reuptake inhibitors: increased risk of gastrointestinal bleeding.

Cardiac glycosides simultaneous administration of NSAIDs and cardiac glycosides may lead to worsening of heart failure, decreased GFR, and increased plasma concentration of cardiac glycosides.

Lithium preparations there is evidence of the likelihood of increased plasma lithium concentration during the use of NSAIDs.

Methotrexate there is evidence of the likelihood of increased plasma methotrexate concentration during the use of NSAIDs.

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

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

Tacrolimus with simultaneous administration of NSAIDs and tacrolimus, an increased risk of nephrotoxicity is possible.

Zidovudine simultaneous use of NSAIDs and zidovudine may lead to increased hematotoxicity.

There is evidence of an increased risk of hemarthrosis and hematoma 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.

Myelotoxic drugs: increased hematotoxicity.

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 action.

Oral hypoglycemic drugs and insulin, sulfonylurea derivatives enhanced effect of the drugs.

Antacids and cholestyramine reduced absorption.

Uricosuric drugs reduced effectiveness of the drugs.

Estrogens, ethanol increased risk of side effects.

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

The shelf life is 3 years. Do not use 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.