Ibuprofen Welfarm, 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 propionic acid derivative of the group of nonsteroidal anti-inflammatory drugs, is due to inhibition of the synthesis of prostatic glandins – mediators of pain, inflammation and hyperthermia. It indiscriminately blocks cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), thus inhibiting the synthesis of prostaglandins. It has a fast directed effect against pain (analgesic), antipyretic and anti-inflammatory effects. In addition, ibuprofen reversibly inhibits platelet aggregation. The analgesic effect of the drug lasts up to 8 hours.

Pharmacokinetics

Ibuprofen is quickly and almost completely absorbed from the gastrointestinal tract, its maximum plasma concentrations are reached 1-2 hours after oral administration, in synovial fluid – 3 hours, it is 99% bound to plasma proteins.

It penetrates slowly into the joint cavity, stays in the synovial tissue, creating higher concentrations in it than in plasma.

The metabolism of ibuprofen occurs mainly in the liver. The elimination half-life (T1/2) from plasma is 2-3 hours. It is excreted by kidneys as metabolites (not more than 1% is excreted unchanged), to a lesser degree – with bile. Ibuprofen is completely eliminated in 24 hours.

Indications

Ibuprofen is used for headache, migraine, toothache, painful menstruation, neuralgia, back pain, muscle pain, rheumatic pain and joint pain; and for fevers of the flu and colds.

Active ingredient

Composition

Per tablet:

The active ingredient: ibuprofen – 400.0 mg;

The excipients: povidone K90 (collidon 90 F), microcrystalline cellulose MS-101, talc, crosspovidone (collidon CL, collidon CL-M), calcium stearate, colloidal cream dioxide (aerosil), corn starch.

The composition of the shell: [dry film-coating mixture containing hypromellose, titanium dioxide, macrogol or hypromellose (oxypropyl methylcellulose), titanium dioxide, macrogol 6000 (polyethylene glycol 6000, polyethylene oxide 6000)].

How to take, the dosage

Adults, the elderly and children over 12 years: in tablets of 200 mg 3-4 times a day; in tablets of 400 mg 2-3 times a day. The daily dose is 1200 mg (do not take more than 6 tablets of 200 mg or 3 tablets of 400 mg) for 24 hours.

The tablets should be swallowed with water, preferably during or after a meal. Do not take more than 4 hours at a time.

Do not exceed the stated dose!

Treatment without medical advice should not exceed 5 days. If symptoms persist, talk to your doctor.

Do not use in children under 12 years of age without medical advice.

In children 6 to 12 years of age (body weight over 20 kg): 1 tablet 200 mg max. 4 times a day. The interval between the intake of tablets is at least 6 hours.

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 per day) prescribed by a physician, because co-administration may increase the risk of side effects. When concomitant use, ibuprofen reduces anti-inflammatory and antiaggregative effects of acetylsalicylic acid (increased incidence of acute coronary failure is possible in patients receiving low doses of acetylsalicylic acid as antiaggregative agents after starting ibuprofen);

– other NSAIDs, in particular selective COX-2 inhibitors: Single-temporal use of two or more drugs from the NSAID group should be avoided because of the possible increased risk of side effects;

Cautiously use concomitantly with the following medications:

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

– antihypertensive agents (ACE inhibitors and angiotensin II antagonists) and diuretics: NSAIDs may decrease 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), simultaneous administration of ACE inhibitors or angiotensin II antagonists and cyclooxygenase inhibitors may lead to worsening of renal function, including 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 GI bleeding.

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

Lithium preparations: there is data on the likelihood of increased plasma lithium concentrations with NSAIDs;

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

– cyclosporine: increased risk of nephrotoxicity with concomitant administration of NSAIDs and cyclosporine;

– mifepristone: NSAIDs should not be started until at least 8-12 days after mifepristone administration, 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 lead to increased hematotoxicity. There is evidence of an increased risk of hemarthrosis and hematoma in HIV-positive patients with hemophilia who received concomitant treatment with zidovudine and ibuprofen;

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

– 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;

– microsomal oxidation inducers (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: enhancement of drug action;

– antacids and colestyramine: decrease in absorption;

– uricosuric drugs: decrease in drug effectiveness;

– caffeine: increase in analgesic effect.

Special Instructions

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 long-term treatment it is necessary to control peripheral blood picture 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 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.

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

Impact on ability to drive vehicles, machinery Patients who have dizziness, drowsiness, lethargy or visual disturbances while taking ibuprofen should avoid driving or operating machinery.

Synopsis

Double convex oval tablets, white or almost white, coated with a film coating.

A single layer of white or almost white color is visible on the cross section.

Contraindications

– hypersensitivity to ibuprofen or any of the ingredients of 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 history);

– gastrointestinal erosive-ulcer disease (including gastric and duodenal ulcer, Crohn’s disease, ulcerative colitis) or active or history of peptic ulcer bleeding (two or more confirmed episodes of peptic ulcer disease or ulcer bleeding);

– Bleeding or gastrointestinal ulcer perforation with a history of NSAID use;

– severe hepatic impairment or active liver disease;

– severe renal insufficiency (creatinine clearance < 30 ml/min), confirmed hyperkalemia;

– decompensated heart failure – decompensated heart failure; period after coronary artery bypass grafting;

– cerebrovascular or other bleeding;

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

– pregnancy (3rd trimester);

– children: up to 6 years old – for 200 mg tablets; up to 12 years old – for 400 mg tablets.

Cautions

With the conditions listed in this section, consult a physician 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; 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 disease, blood diseases of unclear etiology (leukopenia and anemia), severe somatic diseases, dyslipidemia/hyperlipidemia, peripheral artery disease, smoking frequent alcohol consumption, phenylketonuria or phenylalanine intolerance, 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 acetylsalicylic acid, clopidogrel), I-II trimester pregnancy, breastfeeding, advanced age.

Side effects

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

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

The side effects are mostly dose-dependent. In particular, the risk of gastrointestinal bleeding depends on the dose range and the duration of treatment.

The following adverse reactions have been reported with short-term administration of ibuprofen in doses not exceeding 1200 mg/day (6 tablets, 200 mg; 3 tablets, 400 mg). When treating chronic conditions and with long-term use, other adverse reactions may occur.

The incidence of adverse reactions has been evaluated on the basis of the following criteria: Very frequent (≥ 1/10), Frequent (≥ 1/100 to < 1/10), Infrequent (≥ 1/1000 to < 1/100), Rare (≥ 1/10000 to < 1/1000), Very rare (< 1/10000), Frequency unknown (no frequency assessment data available).

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 – nonspecific 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’s 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.

Prevalence unknown: exacerbation of colitis and Crohn’s disease.

Liver and biliary tract disorders

Very rare: liver function abnormalities, increased liver transaminases activity, hepatitis and jaundice.

Rare: disorders of the kidneys and urinary tract

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, with long-term use, increased risk of thrombotic complications (e.g., myocardial infarction), increased blood pressure.

Respiratory and mediastinal disorders

Frequency unknown: bronchial asthma, bronchospasm, dyspnea.

Laboratory measures

-hematocrit or hemoglobin (may decrease);

– bleeding time (may increase);

– plasma glucose concentration (may decrease);

– creatinine clearance (may decrease);

– plasma creatinine concentration (may increase);

– “hepatic” transaminase activity (may increase).

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

Overdose

Do not exceed the specified dose. If you exceed the dose, see your doctor or the nearest medical facility immediately. Take a packet of the medicine with you.

Symptoms: abdominal pain, nausea, vomiting, lethargy, drowsiness, depression, headache, tinnitus, metabolic acidosis, coma, acute renal failure, decreased blood pressure, bradycardia, tachycardia, atrial fibrillation, respiratory arrest.

Treatment: gastric lavage (only within 1 hour after ingestion), activated charcoal, alkaline drinking, forced diuresis, symptomatic therapy (correction of acid-base status, blood pressure).

Similarities