Brustan, pills, 10pcs

Composition

Each tablet contains: Active ingredients: Ibuprofen 400 mgParacetamol 325 mgm Auxiliary substances: Calcium hydrophosphate 20,995 mg, corn starch 88,005 mg, povidone K 306,000 mg, purified talc 10,000 mg; Film-coated: Opadry orange (06G53189) (hypromellose 5 CP 29,500%, hypromellose 15 CP 29,500%, titanium dioxide 22,833%, dye sunset yellow 6,667%, macrogol 6000 5,500%, propylene glycol 5,500%, sodium lauryl 0,500%) 15,000 mg.

Pharmacological properties

Pharmacotherapeutic group

of non-steroidal anti-inflammatory drug (NSAID) non-narcotic and analgesic agent.

ATX code: M 01 AE 51.

Pharmacological properties

Combined drug. It has analgesic, anti-inflammatory and antipyretic effects. The mechanism of anti-inflammatory action of ibuprofen is due to the inhibition of cyclogenase activity (COX), followed by suppression of prostaglandin synthesis.

Paracetamol is a non-narcotic analgesic, blocks COX mainly in the central nervous system, affecting the centers of pain and thermoregulation, has analgesic and antipyretic effects.

Pharmacokinetics

Ibuprofen is well absorbed from the stomach. Tmax – about 1 hour. Absorption decreases slightly when the drug is taken after a meal. About 99% binds to plasma proteins. Ibuprofen is slowly distributed in the synovial fluid and is eliminated from it more slowly than from plasma. It is metabolized in the liver, mainly by hydroxylation and carboxylation of the isobutyl group. The isoenzyme CYP2C9 is involved in the metabolism of the drug. After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen is slowly converted to the active S-form. It has two-phase elimination kinetics. The plasma half-life (T ? ) is 2-3 hours. Up to 90% of the dose can be detected in the urine as metabolites and their conjugates. Less than 1% is excreted unchanged in the urine and, to a lesser extent, in the bile. Ibuprofen is completely eliminated in 24 hours.

Paracetamol is rapidly absorbed from the gastrointestinal tract. Time to reach C max in 0.5-2 hours. Evenly distributed in body fluids. The binding to plasma proteins is variable within 15%. Penetrates through the BBB. It is metabolized in the liver (90-95%): 80% enters into conjugation reactions with glucuronic acid and sulfates to form inactive metabolites; 17% undergoes hydroxylation to form 8 active metabolites, which, when conjugated with glutathione, form inactive metabolites. If there is a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. The isoenzyme CYP2E1 is involved in the metabolism of paracetamol. T 1/2 1-4 hours. It is excreted by the kidneys in the form of conjugates, and only 3% in unchanged form. In elderly patients, paracetamol clearance decreases and T 1/2 increases.

Indications

For adults:

• moderate pain syndrome in childbirth (bruises, sprains, dislocations, fractures);
• postoperative period;
• algodismenorrhea;
• toothache;
• neuralgia;
• myalgia;
• lumbago;
• fibrositis;
• tendovaginitis;
• rheumatoid arthritis;
• osteoarthritis;
• ankylosing spondylitis;
• sinusitis;
• tonsillitis;
• headache;
• fever.

For children (as an auxiliary tool):  tonsillitis; acute infectious and inflammatory diseases of the upper respiratory tract.

Contraindications

• Hypersensitivity to ibuprofen, paracetamol, acetylsalicylic acid or other NSAIDs, as well as to other components of the drug;wbr>Indication in the anamnesis of an attack of bronchial obstruction, urticaria, rhinitis, provoked by taking acetylsalicylic acid (salicylates) or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome: rhinosinusitis, urticaria, nasal mucosal polyps, bronchial asthma).
• Post-coronary artery bypass grafting period
• Erosive and ulcerative lesions of the gastrointestinal tract, active gastric bleeding
• Inflammatory bowel diseases
• Hypocoagulation condition, cerebrovascular bleeding
• Severe renal and / or hepatic insufficiency, confirmed hyperkalemia;
• Pregnancy of the third trimester, lactation period;
• Children under 12 years of age (this dosage form)
• With caution: congestive heart failure, arterial hypertension, coronary heart disease, cerebrovascular diseases, dyslipidemia, diabetes mellitus, peripheral arterial diseases, smoking, frequent alcohol consumption, hyperbilirubinemia, cirrhosis of the liver with portal hypertension, hepatic and/or renal failure, nephrotic syndrome, pregnancy I and II trimesters, old age, glucose-6-phosphate dehydrogenase deficiency, ulcerative colitis diseases of the stomach and duodenum 12 (in the anamnesis), gastritis, blood diseases of unclear etiology (leukopenia and anemia).

Side effects

When using the drug, side effects are rarely observed, but the following side effects may occur: :

Gastrointestinal tract: NSAID gastropathy (nausea, vomiting, heartburn, abdominal pain, constipation, flatulence, decreased appetite, rarely-ulceration of the gastrointestinal tract mucosa, in some cases complicated by bleeding and perforation), irritation or dryness of the oral mucosa, pain in the mouth, ulceration of the gum mucosa,

• Hepatobiliary system: hepatitis
• Allergic reactions: skin rash (usually erythematous or urticaria), pruritus, angioedema, anaphylactoid reactions, anaphylactic shock, bronchospasm or dyspnoea, fever, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), eosinophilia, allergic rhinitis.
• Cardiovascular system: heart failure, tachycardia, high blood pressure.
• Central and peripheral nervous system: headache, dizziness, insomnia, anxiety, nervousness and irritability, psychomotor agitation, drowsiness, depression confusion, hallucinations, rarely-aseptic meningitis (more often in patients with autoimmune diseases)
• Hematopoietic organs: anemia (including hemolytic, aplastic), thrombocytopenia and thrombocytopenic purpura, agranulocytosis, leukopenia.
• Respiratory system: shortness of breath, bronchospasm.
• Sensory organs: hearing impairment (ringing or tinnitus), visual impairment (toxic optic neuritis, blurred vision or diplopia, dry and irritated eyes, conjunctival and eyelid edema of allergic origin, scotoma)
• Urinary system: acute renal failure, allergic nephritis, nephrotic syndrome (edema), polyuria, cystitis
• Laboratory parameters: bleeding time, serum creatinine concentration, hepatic “transaminase” activity (may increase); serum glucose concentration, creatinine clearance, hemotokrit or hemoglobin (may decrease).
• Interaction

Inducers of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of severe hepatotoxic reactions. Microsomal oxidation inhibitors reduce the risk of hepatotoxic effects. Reduces the hypotensive activity of vasodilators (including slow calcium channel blockers and ACE inhibitors), natriuretic and diuretic – furosemide and hydrochlorothiazide.. Reduces the effectiveness of uricosuric drugs, enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics (increased risk of hemorrhagic complications), ulcerogenic effect with bleeding of glucocorticosteroids, colchicine, estrogens, ethanol; enhances the effect of oral hypoglycemic drugs and insulin. Antacids and colestyramine reduce the absorption of ibuprofen.. Increases the concentration in the blood of digoxin, lithium preparations and methotrexata Cofein increases the analgesic effect. When administered concomitantly, the active component of Brustan – ibuprofen reduces the anti-inflammatory and antiplatelet effects of acetylsalicylic acid (ASA) (after starting ibuprofen, the frequency of acute coronary insufficiency may increase in patients receiving small doses of ASA as an antiplatelet agent). When prescribed with anticoagulants and thrombolytic drugs (alteplase, streptokinase, urokinase), serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline), the risk of serious gastrointestinal bleeding increases. Cefamandol, cefaperazone, cefotetan, valproic acid, and plicamycin increase the incidence of hypoprothrombinemia. Myelotoxic drugs increase the manifestations of hematotoxicity of the drug. Cyclosporine and gold preparations enhance the effect of ibuprofen on prostaglandin synthesis in the kidneys, which is manifested by increased nephrotoxicity. Ibuprofen increases the plasma concentration of cyclosporine and the likelihood of developing its hepatotoxic effects.. Drugs that block tubular secretion reduce excretion and increase the plasma concentration of ibuprofen.

How to take it, course of administration and dosage

The drug is taken orally after a meal. Adults and children over 15 years of age: the drug is taken 1 tablet 3-4 times a day with an interval of 6-8 hours (no more than 4 times a day!). Children from 12 to 15 years (body weight more than 40 kg): 1 tablet 3 times a day. If the fever persists for more than 3 days, you should consult your doctor.

The duration of treatment is determined by the doctor depending on the therapeutic effect and the nature of the disease.

Overdose

Problems of overdose occur very rarely, however, in case of accidental overdose, you should immediately consult a doctor. Symptoms: abdominal pain, nausea, vomiting, headache, tinnitus, metabolic acidosis, coma, acute renal failure, low blood pressure, bradycardia, tachycardia. A hepatotoxic effect may occur with the development of hepatonecrosis associated with paracetamol. Treatment: gastric lavage (only within an hour after ingestion), activated charcoal, alkaline drinking, forced diuresis, use of SH-group donors and glutathione synthesis precursors-methionine and N-acetylcysteine. The need for additional therapeutic measures (further use of methionine, intravenous use of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after taking it. In addition, symptomatic therapy is indicated.

Special instructions

Treatment with the drug should be carried out in the minimum effective dose, the shortest possible course.

During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

When symptoms of gastropathy appear, careful monitoring is indicated, including esophagogastroduodenoscopy, a blood test with the determination of hemoglobin, hematocrit, and a fecal occult blood test.

. To prevent the development of NSAID gastropathy, it is recommended to combine with prostaglandin E preparations (misoprostol).. Patients should refrain from all activities that require increased attention, rapid mental and motor reactions. During the treatment period, alcohol (ethanol) is not recommended.

When administered concomitantly with indirect anticoagulants, it is necessary to monitor the blood coagulation system.

Form of production

Coated tablets.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

: Ibuprofen, Paracetamol

Dosage form

Tablets

Purpose

Pregnant women in the first and second trimester as prescribed by a doctor, Children over 12 years of age, Children as prescribed by a doctor, For adults

Indications

Sciatica, Sprains and Sprains, Migraines, Bursitis, Myositis, Tendon Inflammation, Flu, Neuritis, Lumbago, Osteoarthritis and Arthritis, Colds, Osteochondrosis