Brustan - instructions for use, dose, side effects, contraindications

Excipients: methylparahydroxybenzoate 10 mg, propylparahydroxenbenzoate 1 mg, disodium edetate 15 mg, sucrose 3000 mg, carmellose sodium 12.5 mg, xanthan gum 10 mg, glycerol 250 mg, sodium hydrosulfite 7.5 mg, citric acid monohydrate - 5 mg, sodium citrate - 25 mg, silicon colloidal dioxide - 15 mg, polysorbate 80 - 10 mg, dye quinoline yellow - 0.415 mg, orange flavor (521-00014-11) - 15 mg, peach flavor (ST 5977/01) - 1.5 mg, purified water - q.s. up to 5 ml.

Description:Suspension yellow, with a characteristic odor.

Pharmacotherapeutic group:Analgesic combined (NSAID + analgesic non-narcotic)

ATX: & nbsp

M.01.A.E.51 Ibuprofen in combination with other drugs

Pharmacodynamics:

Pharmacological properties

Brustan - a combined preparation, has anti-inflammatory, analgesic and antipyretic effect.

Ibuprofen is characterized by a peripheral anti-inflammatory effect, whereas paracetamol has a central analgesic effect.

Pharmacodynamics

Ibuprofen

The mechanism of action of ibuprofen, a derivative of propionic acid from the group of nonsteroidal anti-inflammatory drugs (NSAIDs), is due to inhibition of the synthesis of prostaglandins - mediators of pain, inflammation and hyperthermia. Non-selectively blocks cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), which inhibits the synthesis of prostaglandins. Has a quick directional action against pain (analgesic), antipyretic and anti-inflammatory action. Ibuprofen reversibly inhibits platelet aggregation.

Paracetamol

Non-selectively blocks COX, mainly in the central nervous system, affecting the centers of pain and thermoregulation.In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on COX, which explains the almost complete absence of significant anti-inflammatory effect. The absence of influence on the synthesis of prostaglandins in peripheral tissues causes the absence of a negative effect on the water-salt exchange and mucous membrane of the gastrointestinal tract (GIT).

Pharmacokinetics:

Ibuprofen

Quickly absorbed from the digestive tract after oral administration. Time to reach the maximum concentration (Tc_mOh) after oral administration - about 1-2 hours. The half-life (T_1/2) - 2 ± 0.5 h. Ibuprofen is characterized by active binding to plasma proteins (90-99%). There is no evidence of accumulation with multiple admission. Slowly penetrates into the joint cavity, accumulates in the synovial fluid, creating higher concentrations in it than in the blood plasma. After absorption about 60% of pharmacologically inactive Rform is slowly transformed into an active S-form. Metabolism of ibuprofen is carried out in the liver with the formation of two inactive metabolites (hydroxylated and carboxylated compounds).More than 90% is excreted by the kidneys (unchanged not more than 1%) and to a lesser extent with bile, in the form of metabolites and their conjugates.

Paracetamol

Rapidly absorbed from the gastrointestinal tract, reaching the maximum concentration of Tc_mOhoccurs within 10-60 minutes. The value of C_mOh 5-20 μg / ml. The connection with plasma proteins is less than 10% and slightly increases with an overdose. Sulfate and glucuronide metabolites do not bind to plasma proteins even at relatively high concentrations. It is evenly distributed in the liquid medium of the body. Penetrates through the blood-brain barrier.

About 90-95% of paracetamol is metabolized in the liver with the formation of inactive conjugates with glucuronic acid (60%), taurine (35%) and cysteine (3%), as well as a small amount of hydroxylated and deacetylated metabolites. A small part of paracetamol is hydroxylated by microsomal enzymes with the formation of highly active N-acetyl-nbenzoquinonimine, which is rendered harmless by binding to the sulfhydryl groups of glutathione in the liver. After an overdose of paracetamol, N-acetyl-n-benzoquinonimine can accumulate and lead to liver damage.

Half-life T_1/2 is 2-3 hours. In patients with liver cirrhosis T_1/2 slightly increases.In elderly patients, clearance of paracetamol decreases and T_1/2. It is excreted by the kidneys, mainly in the form of glucuronide and sulfate conjugates (less than 5% in unchanged form).

Breast milk penetrates less than 1% of the accepted dose of paracetamol.

In children, the ability to form conjugates with glucuronic acid is lower than in adults.

Indications:

Brustan is used in children from the age of 2 as an antipyretic agent for acute respiratory infections, influenza, childhood infections, post-vaccination reactions and other infectious and inflammatory diseases accompanied by fever.

Pain syndrome of mild or moderate intensity, including: headache and toothache, migraine, neuralgia, pain in the ears and throat, pain in stretching and other types of pain.

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

Contraindications:

- Hypersensitivity to the components of the drug, a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);

- hepatic and / or renal failure with creatinine clearance less than 30 ml / min;

- progressive kidney disease;

- active liver disease;

- severe heart failure (III-IV functional class according to the NYHA classification);

- ulcer of the stomach and duodenum (in the phase of exacerbation);

- bleeding or perforation of a gastrointestinal ulcer in an anamnesis, provoked by the use of NSAIDs;

- hemophilia and other disorders of blood clotting (including hypocoagulation), hemorrhagic diathesis;

- bleeding of any etiology;

- intracranial hemorrhage;

- hypersensitivity reactions (bronchospasm, angioedema, asthma, rhinitis, urticaria) associated with aspirin (acetylsalicylic acid) or other non-steroidal anti-inflammatory drugs;

- period after aortocoronary shunting;

- inflammatory bowel disease;

- confirmed hyperkalemia;

- diseases of the optic nerve;

- deficiency of glucose-6-phosphate dehydrogenase;

- deficiency of sugar / isomaltase;

- intolerance to fructose;

- glucose-galactose malabsorption

- pregnancy, lactation;

- children under 2 years;

- simultaneous administration of other drugs containing non-steroidal anti-inflammatory drugs, including specific inhibitors cyclooxygenase 2 and doses of acetylsalicylic acid over 75 mg per day;

- simultaneous reception of other drugs containing paracetamol in connection with an increased risk of serious adverse reactions.

Carefully:

- Elderly age;

- chronic heart failure (NYHA I-II functional class);

- cardiac ischemia;

- arterial hypertension;

- cerebrovascular diseases;

- diseases of peripheral arteries;

- dyslipidemia / hyperlipidemia;

- cirrhosis of the liver with portal hypertension;

- Viral hepatitis;

- nephrotic syndrome;

- renal failure with creatinine clearance of 30-60 ml / min;

- benign hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson and Rotor syndrome);

- systemic lupus erythematosus and other systemic diseases of connective tissue;

- An ulcer of the stomach or duodenum (in the anamnesis);

- gastritis, enteritis, colitis;

- infection Helicobacter pylori;

- blood diseases of unclear etiology (leukopenia, anemia);

- bronchial asthma;

- diabetes;

- prolonged use of NSAIDs;

- Smoking;

- Alcoholism;

- severe physical illnesses;

- simultaneous administration of oral glucocorticosteroids (including prednisolone);

- simultaneous reception of anticoagulants (including warfarin);

- simultaneous administration of antiplatelet agents (including clopidogrel);

- simultaneous reception of serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Pregnancy and lactation:

The drug is contraindicated in pregnancy.

If it is necessary to apply in the period should stop breastfeeding.

In the experimental, embryotoxic, teratogenic and mutagenic effects of the components of the Brustant preparation have not been established.

Dosing and Administration:

The drug is taken orally.

Shake the bottle thoroughly before use.

5 ml of the drug contain 100 mg of ibuprofen and 125 mg of paracetamol.

The dose of the drug depends on the age and body weight of the child.

Body weight (age)	Single dose, ml
10-15 (2-3 years)	5
16-21 (4-6 years)	7,5
22-26 (7-9 years)	10
27-32 (10-11 years old)	12,5
33-43 (12-14 years)	15

The drug is taken 3-4 times a day at intervals of 6-8 hours (no more than 4 times a day!). If the fever persists, talk to your doctor.

Duration of treatment should not exceed 5 days with the appointment as an anesthetic and more than 3 days - as an antipyretic.

Continuation of treatment with the drug is possible only after consulting a doctor.

If there is no effect on the recommended dose, consult a doctor.

Side effects:

To reduce the risk of adverse reactions, use the lowest effective dose as little as possible with a short course.

To assess the frequency of side effects, the following criteria were used: "very often" (≥1 / 10), "often" (≥1 / 100, <1/10), "infrequently" (≥1 / 1000, <1/100), "rarely" (≥1 / 10000, <1/1000), "very rarely" (<1/10000), "frequency is unknown" (the incidence of side effects can not be estimated).

From the central and peripheral nervous system: infrequently - headache, dizziness; very rarely - paresthesia, optic neuritis, drowsiness; frequency unknown - insomnia, anxiety, nervousness and irritability, psychomotor excitation, aseptic meningitis (more often in patients with autoimmune diseases), stroke.

Mental disorders: very rarely - confusion, depression, hallucinations.

From the side of cardiovascular system: very rarely - swelling, increased blood pressure, heart failure; frequency unknown - tachycardia, angina pectoris, myocardial infarction, peripheral edema.

From the respiratory system: very rarely - asthma, exacerbation of asthma, shortness of breath, bronchospasm.

From the gastrointestinal side tract: often - NSAIDs-gastropathy (abdominal pain, nausea, vomiting, heartburn, decreased appetite, diarrhea); infrequently - flatulence, constipation, ulceration of the gastrointestinal mucosa, which in some cases is complicated by perforation and bleeding; frequency unknown - irritation or dryness of the oral mucosa, mouth pain, ulceration of the gingival mucosa, aphthous stomatitis, gastritis, melena, pancreatitis, Crohn's disease, exacerbation of colitis.

From the hepatobiliary system: very rarely - hepatitis, jaundice, liver necrosis, violations of the liver, leading to the development of hepatic insufficiency, hepatic encephalopathy.

From the urinary system: very rarely - nephrotic syndrome; frequency unknown - acute renal failure, polyuria, cystitis, acute tubular necrosis, medullary nephronecrosis, interstitial nephritis.

From the organ of hearing: very rarely - ringing or tingling in the ears; frequency unknown - hearing impairment, hearing loss.

From the side of the organ of vision: very rarely - a vision disorder; frequency unknown - blurred vision or dilation, scotoma, dry and irritated eyes, conjunctival edema and eyelids (allergic genesis).

Allergic reactions: infrequently - angioedema; frequency unknown - anaphylaxis, anaphylactoid reactions, anaphylactic shock, fever, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), eosinophilia, allergic rhinitis.

From the skin: infrequent - skin rash (usually erythematous or urticaria), maculopapular rash, itchy skin; very rarely - hyperhidrosis, purpura, photosensitivity; frequency unknown - exfoliative dermatitis.

From the hematopoiesis: very rarely - anemia (including hemolytic, aplastic), thrombocytopenia and thrombocytopenic purpura, agranulocytosis, and leukopenia.

The risk of ulceration of the gastrointestinal mucosa, bleeding (gastrointestinal, gum, uterine, hemorrhoidal),visual impairment (color vision, scotoma, optic nerve damage) increases with prolonged use of the drug in large doses.

Laboratory indicators: often - an increase in the activity of "liver" transaminases, an increase in serum creatinine and urea concentration; frequency unknown - prolongation of bleeding time, decrease in serum glucose concentration, decrease in hematocrit, decrease in hemoglobin concentration, pancytopenia.

Overdose:

Symptoms: gastrointestinal disorders (diarrhea, nausea, vomiting, anorexia, epigastric pain), retardation, drowsiness, depression, headache, tinnitus, impaired consciousness, convulsions, heart rhythm disturbance, lowering of blood pressure, acute pancreatitis, bleeding through 12-48 hours (vomiting of blood, hematuria), hypoglycemia and anomalies of glucose metabolism, an increase in prothrombin time, an increase in the international normalized ratio (INR).

Overdose of paracetamol leads to toxic kidney damage with the development of nephronecrosis, acute renal failure and impaired liver function,sometimes leading to necrosis of the liver, with the possible development of hepatic insufficiency, encephalopathy, cerebral edema. Hepatotoxic effect in adults is manifested by taking 10 g of paracetamol and more.

An overdose of ibuprofen leads to disorders of the central nervous system - drowsiness, sometimes arousal, convulsions, disorientation or coma.

If you suspect an overdose, seek medical help immediately.

Treatment: gastric lavage (only for an hour after ingestion), Activated carbon, alkaline drink, forced diuresis, administration of SH-group donors and glutathione-methionine synthesis precursors 8-9 hours after an overdose and N acetylcysteine inside or intravenously after 12 hours, antacids, hemodialysis, symptomatic therapy (acid-base correction , blood pressure).

The need for additional therapeutic measures (further introduction of methionine, intravenous administration of N-acetylcysteine is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration.With frequent or prolonged seizures caused by an overdose of ibuprofen, diazepam or lorazepam is given intravenously.

Interaction:

Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, flumecinol, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication during an overdose.

Inhibitors of microsomal oxidation (incl. cimetidine) reduce the risk of hepatotoxic effects.

With simultaneous application ibuprofen reduces the effectiveness of uricosuric drugs.

The efficacy of furosemide and thiazide diuretics can be reduced due to a delay in sodium associated with inhibition of prostaglandin synthesis in the kidneys.

Ibuprofen enhances the effect of direct (heparin) and indirect (coumarin and indanedione derivatives) anticoagulants, thrombolytic drugs (alteplase, anestreplase, streptokinase, urokinase), antiplatelet agents, colchicine - the risk of hemorrhagic complications increases.

Simultaneous administration of ibuprofen with serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline) increases the risk of developing serious gastrointestinal bleeding.

With simultaneous use with acetylsalicylic acid ibuprofen reduces its antiaggregant effect (it is possible to increase the incidence of acute coronary insufficiency in patients receiving small doses of acetylsalicylic acid as antiplatelet agents).

Ibuprofen may reduce the effectiveness of antihypertensive drugs.

Ibuprofen increases the concentration in the blood plasma of digoxin, phenytoin and lithium.

Ibuprofen (like other non-steroidal anti-inflammatory drugs) should be used with caution in combination with acetylsalicylic acid or other non-steroidal anti-inflammatory drugs and glucocorticosteroids due to an increased risk of developing adverse effects of the drug on the gastrointestinal tract.

Like other non-steroidal anti-inflammatory drugs, ibuprofen when used simultaneously with cardiac glycosides, can lead to an increase in the content of cardiac glycosides.

Non-steroidal anti-inflammatory drugs should not be used within 8-12 days after the administration of mifepristone, as the effect of mifepristone decreases.

With the simultaneous use of ibuprofen (as well as other non-steroidal anti-inflammatory drugs) and tacrolimus, the risk of nephrotoxicity of ibuprofen increases.

Ibuprofen may increase the concentration of methotrexate in the plasma.

With the simultaneous use of lithium and ibuprofen drugs, lithium release is reduced.

Caffeine increases the analgesic effect of ibuprofen.

Combined treatment with zidovudine and ibuprofen may increase the risk of hemarthrosis and hematoma in HIV-infected patients with hemophilia.

Ibuprofen enhances the hypoglycemic effect of oral hypoglycemic agents and insulin; it may be necessary to adjust the dose.

Long-term combined use with paracetamol, cyclosporine, and gold preparations increases the risk of developing nephrotoxic effects.

Cefamandol, cefaperazone, cefotetan, valproic acid, plikamycin increase the frequency of hypoprothrombinemia.

With prolonged treatment with carbamazepine and paracetamol, the risk of developing acute tubular nephronecrosis is increased.

The combination of paracetamol with ethanol, glucocorticosteroids, corticotropin increases the risk of erosive and ulcerative lesions of the gastrointestinal tract.

With prolonged use of paracetamol, the anticoagulant effect of warfarin and other coumarins increases, which leads to an increased risk of bleeding.

Antacids and colestramine reduce the absorption of the drug.

Myelotoxic drugs promote the manifestation of hematotoxicity of the drug.

With the simultaneous administration of chloramphenicol and paracetamol, the concentration of chloramphenicol in the blood plasma increases.

Absorption of paracetamol increases with simultaneous administration with metoclopramide and domperidone. Nevertheless, there is no need to avoid concurrent administration of paracetamol with metoclopramide and domperidone.

Paracetamol enhances the action of monoamine oxidase (MAO) inhibitors with simultaneous application. When using paracetamol together during treatment with MAO inhibitors and within 2 weeks after the end of treatment, there is a risk of developing arousal andfever.

Special instructions:

When there are signs of bleeding from the gastrointestinal tract ibuprofen should be canceled.

At simultaneous application of anticoagulants of indirect action it is necessary to supervise parameters of a coagulating system of blood.

When used simultaneously with serotonin reuptake inhibitors (SSRIs), the risk of developing gastrointestinal bleeding increases. Care should be taken when simultaneous use of ibuprofen with SSRIs is required.

Ibuprofen can mask objective and subjective signs of infection, so ibuprofen therapy in patients with infection should be administered with caution.

Data from clinical and epidemiological studies show that the use of ibuprofen, especially at high doses (2,400 mg / day) for a long time, may be associated with a slightly increased risk of arterial thrombotic events (myocardial infarction or stroke).

To reduce the risk of developing adverse reactions, the minimum effective dose should be used as short a course as possible.With prolonged use of analgesics, there is a risk of developing analgesic nephropathy.

Anorexia and malnutrition increase the risk of side effects of paracetamol.

Due to ibuprofen can affect proglandin-dependent processes of oocyte maturation, the drug is not recommended for women during pregnancy silt fattening.

Patients who report visual impairment with ibuprofen therapy should stop treatment and undergo ophthalmic examination.

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

When the symptoms of gastropathy shows careful monitoring, including bringing esophagogastroduodenoscopy, a blood test with the hemoglobin, hematocrit, fecal occult blood.

To prevent the development of NSAIDs, gastropathy is recommended to be combined with preparations of prostaglandin E (misoprostol).

If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

It is necessary to avoid the joint administration of Brustan with other NSAIDs.

During the period of treatment, ethanol is not recommended.

Effect on the ability to drive transp. cf.and fur:

It should refrain from driving and other potentially hazardous activities requiring increased attention and speed of psychomotor reactions, as the drug may cause dizziness and other side effects that may affect these abilities.

Form release / dosage:

Suspension for oral administration, 100 mg + 125 mg / 5 ml

Packaging:

For 60 ml or 100 ml of the drug in a bottle of dark glass with a screw cap.

1 bottle with instructions for use and a measuring cup in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-000112

Date of registration:27.12.2010 / 27.05.2016

Expiration Date:Unlimited

The owner of the registration certificate:San Pharmaceutical Industries Co., Ltd.San Pharmaceutical Industries Co., Ltd. India

Manufacturer: & nbsp

Madras Pharmaceuticals India

Representation: & nbspSAN PHARMACEUTICAL INDUSTRIES LTD. SAN PHARMACEUTICAL INDUSTRIES LTD. India

Information update date: & nbsp19.04.2017

Illustrated instructions

Instructions

Brustan (Brustan)