Nurofast Forte, 400 mg 20 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drug (NSAID).

The ATC code: M01AE01

Pharmacological properties

Pharmacodynamics

The mechanism of action of ibuprofen, a derivative of propionic acid from the group of non-steroidal anti-inflammatory drugs (NSAIDs), is due to the inhibition of the synthesis of prostaglandins – mediators of pain, inflammation and hyperthermia.

Inhibits cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2) indiscriminately, thereby inhibiting the synthesis of prostaglandins. It has a fast directed action against pain (analgesic), antipyretic and anti-inflammatory effect. In addition, ibuprofen reversibly inhibits platelet aggregation. The analgesic effect of the drug lasts up to 8 hours.

Pharmacokinetics

Absorption is high and is quickly and almost completely absorbed from the gastrointestinal tract (GIT). After taking the drug on an empty stomach the maximum concentration (C_max) of ibuprofen in blood plasma is reached after 45 minutes. Taking the drug with food can increase the time to reach maximum concentration (TC_max) up to 1-2 hours. The binding to plasma proteins is 90%.

Slowly penetrates into the joint cavity, stays in synovial fluid, creating higher concentrations in it than in blood plasma. In cerebrospinal fluid lower concentrations of ibuprofen are found compared to blood plasma. After absorption about 60% of pharmacologically inactive R-form is slowly transformed into active S-form. It is metabolized in the liver. The half-life (T_1/2) is 2 hours. It is excreted by kidneys (not more than 1% unchanged) and, to a lesser extent, with bile.

In limited studies ibuprofen was detected in breast milk in very low concentrations.

Indications

Active ingredient

Composition

1 film-coated tablet contains:

the active substance: ibuprofen – 400 mg;

excipients: croscarmellose sodium, sodium citrate dihydrate, sodium lauryl sulfate, colloidal silicon dioxide (aerosil), magnesium stearate, stearic acid;

coating aids: Opadray II 85F48105 white (polyvinyl alcohol, macrogol, talc, titanium dioxide).

How to take, the dosage

For oral administration. Patients with hypersensitivity of the stomach are recommended to take the drug with meals.

For short-term use only. Read the instructions carefully before you take this medicine.

Adults and children over 12 years of age, 1 tablet (400 mg) up to 3 times daily.

In children from 6 to 12 years old 1/2 tablet (200 mg) up to 3 to 4 times a day; the drug can only be taken if the body weight of the child is more than 20 kg.
Tablets should be taken with water.

The interval between taking the pills should be at least 4 hours.

The maximum daily dose for adults is 1200 mg (3 tablets).

The maximum daily dose for children from 6 to 18 years is 800 mg (2 tablets).

If symptoms persist or worsen when taking the drug for 2-3 days, you should stop treatment and see a doctor.

Interaction

The concomitant use of ibuprofen with the following drugs should be avoided:

– Acetylsalicylic acid: except in low doses of acetylsalicylic acid (no more than 75 mg daily) prescribed by a physician, because concomitant use may increase the risk of side effects. Co-administration of ibuprofen reduces anti-inflammatory and antiplatelet effects of acetylsalicylic acid (the incidence of acute coronary failure may increase in patients receiving low doses of acetylsalicylic acid as antiplatelet agents after starting ibuprofen administration).

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

Cautiously use concomitantly with the following drugs:

– Anticoagulants and thrombolytics: NSAIDs may increase the effect of anticoagulants, particularly warfarin and thrombolytics.

– Antihypertensives (ACE inhibitors and angiotensin antagonists
II) and diuretics: NSAIDs may reduce the effectiveness of drugs in these groups. In some patients with impaired renal function (e.g., in patients with dehydration or elderly patients with impaired renal function), the simultaneous administration of ACE inhibitors or angiotensin II antagonists and cyclooxygenase 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 concomitantly with ACE inhibitors or angiotensin II antagonists. In this regard, the combined use of the above drugs should be administered with caution, especially in the elderly. It is necessary to prevent dehydration in patients, and to consider monitoring renal function after initiation of such combined treatment and periodically thereafter.

Diuretics and ACE inhibitors may increase nephrotoxicity of NSAIDs.

– Glucocorticosteroids: increased risk of GI ulcers and gastrointestinal bleeding.

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

– Cardiac glycosides: concomitant administration of NSAIDs and cardiac glycosides may worsen heart failure, decrease glomerular filtration rate, and increase plasma concentrations of cardiac glycosides.

Lithium drugs: there is data on the likelihood of increased plasma lithium concentrations with NSAIDs.

– Methotrexate: there is data on the likelihood of increased plasma concentrations of methotrexate with NSAIDs.

Cyclosporine: there is an increased risk of nephrotoxicity with concomitant administration of NSAIDs and cyclosporine.

– Mifepristone: NSAIDs should not be administered earlier than
8-12 days after taking mifepristone because 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 increase hematotoxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive patients with hemophilia co-treated with zidovudine and ibuprofen.

– Quinolone antibiotics: patients co-treated with NSAIDs and quinolone antibiotics may have an increased risk of seizures.

– Myelotoxic drugs: increase in hematotoxicity.

– Cefamandole, cefoperazone, cefotetan, valproic acid, plikamycin: 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 intoxication.

– Microsomal oxidation inhibitors: decreased risk of hepatotoxic effects.

– Oral hypoglycemic drugs and insulin, sulfonylurea derivatives: increasing the effect of the drugs.

– Antacids and colestyramine: decrease absorption.

– Uricosuric drugs: decrease in the effectiveness of the drugs.

– Estrogens, ethanol: increased risk of side effects.

– Caffeine: increased analgesic effect.

Special Instructions

It is recommended that the drug be taken for as short a course as possible and in the minimum effective dose necessary to eliminate symptoms. If it is necessary to take the drug for more than 10 days, a physician should be consulted.

In patients with bronchial asthma or 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 aseptic meningitis.

When using during long-term treatment it is necessary to monitor peripheral blood count and functional state of liver and kidneys. In case of gastropathy symptoms a thorough control is indicated, including esophagogastroduodenoscopy, general blood test (hemoglobin determination), fecal occult blood test. If it is necessary to determine 17-ketosteroids, the drug should be cancelled 48 hours before the study. During the treatment period it is not recommended to take ethanol.

Patients with renal insufficiency should consult a physician before using the drug, since there is a risk of impairment of renal function.

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

Patients with uncontrolled arterial hypertension, NYHA class II-III congestive heart failure, coronary heart disease, peripheral artery disease and/or cerebrovascular disease should only be prescribed ibuprofen after careful benefit-risk assessment, and 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 suppurative complications of infectious and inflammatory skin and subcutaneous fat diseases (e.g., necrotizing fasciitis). In this regard, it is recommended to avoid using the drug in case of chicken pox.

Information for women planning pregnancy: The drug suppresses cyclooxygenase and prostaglandin synthesis, affects ovulation, disrupting female reproductive function (reversible after treatment withdrawal).

Impact on driving and operating machinery

Patients who have dizziness, drowsiness, lethargy or visual disturbances while taking ibuprofen should avoid driving or operating machinery.

Synopsis

Double convex oblong-shaped tablets with rounded ends, film-coated in white or almost white with a ridge. On cross section the core is white or almost white.

Contraindications

– Hypersensitivity to ibuprofen or any of the ingredients in the drug.

– Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including a history).

– Erosive-ulcer disease of the gastrointestinal tract (including gastric and duodenal ulcer, Crohn’s disease, ulcerative colitis) or ulcer bleeding in the active phase or in the anamnesis (two or more confirmed episodes of ulcer disease or ulcer bleeding).

– Bleeding or gastrointestinal ulcer perforation in a history triggered by the use of NSAIDs.

– Severe heart failure (NYHA class IV – New York Heart Association classification).

– Severe hepatic insufficiency or active liver disease.

– Severe renal insufficiency (creatinine clearance
< 30 ml/min), confirmed hyperkalemia.

– Decompensated heart failure; period after coronary artery bypass grafting.

– Cerebrovascular or other bleeding.

– Hemophilia and other blood clotting disorders (including hypocoagulation), hemorrhagic diathesis.

– Pregnancy (III trimester).

– Children under 6 years of age.

Cautions

If you have any of the conditions listed in this section, you should see your doctor before using the drug.

Concomitant use of other NSAIDs; history of a single episode of gastric or duodenal ulcer or GI ulcer bleeding; gastritis, enteritis, colitis, Helicobacter pylori infection, ulcerative colitis; bronchial asthma or allergic diseases in the acute stage or in the history – possible development of bronchospasm; systemic lupus erythematosus or mixed connective tissue disease (Sharp syndrome) – increased risk of aseptic meningitis; varicella renal failure, including dehydration (creatinine clearance less than 30-60 ml/min), nephrotic syndrome, liver failure, 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, peripheral arterial disease, smoking, frequent alcohol consumption, concomitant use of medications that may increase the risk of ulceration or bleeding, particularly oral glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline) or antiaggregants (including acetylsalicylic acid, clopidogrel), pregnancy I-II trimester, breastfeeding period, old age.

Side effects

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

The elderly have an increased incidence of adverse reactions with NSAIDs, especially gastrointestinal bleeding and perforations, in some cases fatal.

The side effects are predominantly dose-dependent.

The following adverse reactions have been reported with short-term administration of ibuprofen in doses not exceeding 1200 mg/day (3 tablets). When treating chronic conditions and with long-term use, other adverse reactions may occur.

The frequency of adverse reactions was evaluated based on the following criteria: very frequent (≥ 1/10), frequent (≥ 1/100 to < 1/10), infrequent (≥ 1/1000 to < 1/100), rare (≥ 1/10 000 to < 1/1000), very rare (1/10 000), frequency unknown (data to estimate frequency are not sufficient).

Disorders of the blood and lymphatic system

– Very rare: disorders of hematopoiesis (anemia, leukopenia, aplastic anemia, hemolytic anemia, thrombocytopenia, pancytopenia, agranulocytosis). The first symptoms of these disorders are fever, sore throat, superficial mouth ulcers, flu-like symptoms, marked weakness, nosebleeds and subcutaneous hemorrhages, bleeding and bruising of unknown etiology.

Immune system disorders

– Infrequent: hypersensitivity reactions – non-specific allergic reactions and anaphylactic reactions, respiratory reactions (bronchial asthma, including its exacerbation, bronchospasm, dyspnea), skin reactions (itching, urticaria, purpura, Quincke’s edema, exfoliative and bullous dermatoses, including toxic epidermal necrolysis (Lyell syndrome), Stevens-Johnson syndrome, erythema multiforme), allergic rhinitis, eosinophilia.

– Very rare: severe hypersensitivity reactions, including swelling of the face, tongue and throat, shortness of breath, tachycardia, arterial hypotension (anaphylaxis, Quincke’s edema or severe anaphylactic shock).

Gastrointestinal disorders

– Infrequent: abdominal pain, nausea, dyspepsia (including heartburn, bloating).

– Rare: diarrhea, flatulence, constipation, vomiting.

– Very rare: peptic ulcer, perforation or gastrointestinal bleeding, melena, bloody vomiting, in some cases fatal, especially in elderly patients, ulcerative stomatitis, gastritis.

– Frequency unknown: exacerbation of colitis and Crohn’s disease.

Liver and biliary tract disorders

– Very rare: liver dysfunction, increased activity of “hepatic” transaminases, hepatitis and jaundice.

Relary and urinary tract disorders

– Very rare: Acute renal failure (compensated and decompensated) especially with long-term use, combined 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

– Infrequent: headache.

– Very rare: aseptic meningitis.

Cardiovascular system disorders

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

Respiratory and mediastinal disorders

– Frequency unknown: bronchial asthma, bronchospasm, dyspnea.

Laboratory measures

– Hematocrit or hemoglobin (may decrease)

– Bleeding time (may increase)

/p>

– plasma glucose concentration (may decrease)

– creatinine clearance (may decrease)

/p>

– plasma creatinine concentration (may increase)

– “hepatic” transaminase activity (may increase)

If side effects occur, discontinue the drug and seek medical attention.

Overdose

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

Symptoms: nausea, vomiting, epigastric pain or, less frequently, diarrhea, tinnitus, headache and gastrointestinal bleeding. In more severe cases, manifestations of 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.

The treatment: symptomatic, with mandatory provision of airway patency, ECG monitoring 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 is already absorbed, alkaline drinking may be prescribed in order to excrete the acidic derivative of ibuprofen by the kidneys, forced diuresis. Frequent or prolonged seizures should be controlled with intravenous diazepam or lorazepam. In worsening bronchial asthma the use of bronchodilators is recommended.

Pregnancy use

The drug is contraindicated in the third trimester of pregnancy. Administration of the drug in I-II trimesters of pregnancy should be avoided, if it is necessary to take the drug should be consulted with a physician.

There is evidence that ibuprofen may pass into the breast milk in small amounts without any adverse effect on the health of the infant, therefore usually with short-term use there is no need to stop breast-feeding.

If prolonged use of the drug is necessary, a physician should be consulted to decide whether to stop breastfeeding for the period of use.

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