Nurofen Express, 200 mg capsules 8 pcs

Indications

Nurofen® Express is used for headaches, migraines, toothaches, painful menstruation, neuralgia, back pain, muscle and rheumatic pain; for feverish conditions such as influenza and colds.

Pharmacological effect

The mechanism of action of ibuprofen, a derivative of propionic acid from the group of non-steroidal
anti-inflammatory drugs (NSAIDs) are caused by inhibition of the synthesis of prostaglandins, mediators of pain, inflammation and hyperthermic reaction. Indiscriminately blocks cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), as a result of which it inhibits the synthesis of prostaglandins. It has a rapid, targeted effect against pain (analgesic), antipyretic and anti-inflammatory effects. In addition, ibuprofen reversibly inhibits platelet aggregation.

Pharmacokinetics

Absorption is high, quickly and almost completely absorbed from the gastrointestinal tract (GIT). After taking 2 capsules of the drug on an empty stomach, ibuprofen is detected in the blood plasma after 10 minutes, the maximum concentration (Cmax) of ibuprofen in the blood plasma is achieved after 30-40 minutes, which is two times faster than after taking an equivalent dose of Nurofen, in the dosage form of 200 mg film-coated tablets.

Taking the drug with food may increase the time to reach maximum concentration (TCmax). Communication with blood plasma proteins is more than 90%, half-life (T1/2) 2 hours. Slowly penetrates into the joint cavity, lingers in the synovial fluid, creating higher concentrations in it than in the blood plasma. After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into the active S-form. Metabolized in the liver. Excreted by the kidneys (no more than 1% unchanged) and, to a lesser extent, with bile.

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

In limited studies, ibuprofen has been found in breast milk at very low concentrations.

Special instructions

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

During long-term treatment, monitoring of the peripheral blood picture and the functional state of the liver and kidneys is necessary. When symptoms of gastropathy appear, careful monitoring is indicated, including esophagogastroduodenoscopy, a complete blood count (hemoglobin determination), and a stool test for occult blood. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study. During the treatment period, ethanol intake is not recommended.

Patients with renal failure should consult a doctor before using the drug, as there is a risk of deterioration in the functional state of the kidneys.

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.

In patients with uncontrolled hypertension, NYHA class II-III congestive heart failure, coronary artery disease, peripheral arterial disease, and/or cerebrovascular disease, ibuprofen should be prescribed only after a 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 developing severe purulent complications of infectious and inflammatory diseases of the skin and subcutaneous fat (for example, necrotizing fasciitis). In this regard, it is recommended to avoid using the drug for chickenpox.

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

Impact on the ability to drive vehicles and machinery

Patients who experience dizziness, drowsiness, lethargy, or blurred vision while taking ibuprofen should avoid driving or operating machinery.

Active ingredient

Ibuprofen

Composition

One capsule contains

active ingredient – ​​ibuprofen 200 mg,

excipients:

Macrogol-600 218.33 mg,

potassium hydroxide 25.6 mg,

water 17.07 mg;

capsule shell:

gelatin 119.8 mg, sorbitol 76% solution 58.19 mg, crimson dye [Ponceau 4R] (E124) 0.485 mg, water 15.02 mg, white ink [Opacode WB NS-78-18011] (water 48%, titanium dioxide (E171) 29%, propylene glycol 10%, isopropanol 8%, hypromellose 5%).

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 non-steroidal anti-inflammatory drugs (including a history).

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

History of bleeding or perforation of a gastrointestinal ulcer caused by the use of NSAIDs.

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

Severe liver failure or active liver disease.

Severe renal failure (creatinine clearance 30 ml/min), confirmed hyperkalemia.

Decompensated heart failure; period after coronary artery bypass surgery.

Cerebrovascular or other bleeding.

Hemophilia and other bleeding disorders (including hypocoagulation), hemorrhagic diathesis.

Fructose intolerance.

Pregnancy (III trimester).

Children’s age up to 12 years.

Side Effects

The risk of side effects can be minimized if the drug is taken in a short course, at the minimum effective dose required to eliminate symptoms.

Side effects are predominantly dose dependent.

The following adverse reactions were observed 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 frequency of adverse reactions was assessed based on the following criteria: very common (1/10), common (1/100 to 1/10), uncommon (1/1000 to 1/100), rare (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 ulcers in the mouth, 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, reactions from the respiratory tract (bronchial asthma, including its exacerbation, bronchospasm, shortness of breath, dyspnea), skin reactions (itching, urticaria, purpura, Quincke’s edema, 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, 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.

Disorders of the liver and biliary tract

Very rare: liver dysfunction (especially with long-term use), hepatitis and jaundice.

Renal and urinary tract disorders

Very rare: acute renal failure (compensated and decompensated), especially with long-term use, in combination with an increase in the concentration of urea in the blood plasma 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.

Cardiovascular system disorders

Frequency unknown: heart failure, peripheral edema, with long-term use increased risk of thrombotic complications (for example, myocardial infarction), increased blood pressure.

Disorders of the respiratory system and mediastinal organs

Frequency unknown: bronchial asthma, bronchospasm, shortness of breath.

Other

Very rare: edema, including peripheral edema.

Laboratory indicators

hematocrit or hemoglobin (may decrease)
bleeding time (may increase)
plasma glucose concentration (may decrease)
creatinine clearance (may decrease)
plasma creatinine concentration (may increase)
liver transaminase activity (may increase)

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

Interaction

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

Acetylsalicylic acid: with the exception of low doses of acetylsalicylic acid (no more than 75 mg per day) prescribed by a doctor, since combined use may increase the risk of side effects. With simultaneous use, ibuprofen reduces the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (an increase in the incidence of acute coronary insufficiency in patients receiving small doses of acetylsalicylic acid as an antiplatelet agent is possible after starting ibuprofen).
Other NSAIDs, including selective COX-2 inhibitors: The simultaneous use of two or more NSAIDs should be avoided due to a possible increased risk of side effects.

Use with caution simultaneously with the following medications:

Anticoagulants and thrombolytic drugs: NSAIDs may enhance the effect of anticoagulants, in particular warfarin and thrombolytic drugs.
Antihypertensives (ACE inhibitors and angiotensin II antagonists) and diuretics: NSAIDs may reduce the effectiveness of drugs in these groups. Diuretics and ACE inhibitors may increase the nephrotoxicity of NSAIDs.
Glucocorticosteroids: increased risk of gastrointestinal ulceration and gastrointestinal bleeding.
Antiplatelet agents and selective serotonin reuptake inhibitors: increased risk of gastrointestinal bleeding.
Cardiac glycosides: simultaneous administration of NSAIDs and cardiac glycosides can lead to worsening heart failure, a decrease in glomerular filtration rate and an increase in the concentration of cardiac glycosides in the blood plasma.
Lithium preparations: there is evidence of the likelihood of an increase in the concentration of lithium in the blood plasma during the use of NSAIDs.
Methotrexate: there is evidence of the likelihood of an increase in the concentration of methotrexate in the blood plasma during the use of NSAIDs.
Cyclosporine: increased risk of nephrotoxicity when NSAIDs are administered concomitantly with cyclosporine.
Mifepristone: NSAIDs should be started no earlier than 8 to 12 days after taking mifepristone, as NSAIDs may reduce the effectiveness of mifepristone.
Tacrolimus: When NSAIDs are co-administered with tacrolimus, the risk of nephrotoxicity may increase.
Zidovudine: Concomitant use of NSAIDs and zidovudine may result in increased hematotoxicity. There is evidence of an increased risk of hemarthrosis and hematomas in HIV-positive patients with hemophilia who received concomitant treatment with zidovudine and ibuprofen.
Quinolone antibiotics: In patients receiving concomitant treatment with NSAIDs and quinolone antibiotics, the risk of seizures may be increased.
Cefamandole, cefoperazone, cefotetan, valproic acid, plicamycin: increased incidence of hypoprothrombinemia.
Drugs that block tubular secretion: decreased excretion and increased plasma concentrations of ibuprofen.
Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants): increased production of hydroxylated active metabolites, increased risk of developing severe intoxications.
Microsomal oxidation inhibitors: reducing the risk of hepatotoxicity.
Oral hypoglycemic drugs and insulin, sulfonylurea derivatives: increased effect.
Antacids and cholestyramine: decreased absorption.
Caffeine: increased analgesic effect.

Overdose

In children, overdose symptoms may occur after taking a dose exceeding 400 mg/kg body weight. In adults, the dose-dependent effect of overdose is less pronounced. The half-life of the drug in case of 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: symptomatic, with mandatory maintenance of airway patency, monitoring of ECG and vital signs until the patient’s condition is normalized.

Oral use of activated charcoal or gastric lavage is recommended within 1 hour after taking a potentially toxic dose of ibuprofen. If ibuprofen has already been absorbed, an alkaline drink may be prescribed in order to eliminate the acidic derivative of ibuprofen by the kidneys, forced diuresis. Frequent or prolonged seizures should be treated with intravenous diazepam or lorazepam. If bronchial asthma worsens, the use of bronchodilators is recommended.

Storage conditions

Store in a dry place at a temperature not exceeding 25 °C.

Shelf life

2 years

Manufacturer

Patheon Softgels B.V., The Netherlands