

Pharmacotherapeutic group non-steroidal anti-inflammatory drug (NSAIDs) and analgesic non-narcotic agent.
ATH code: M01AE51.
Pharmacological properties
Combined drug. It has analgesic, anti-inflammatory and antipyretic effect. The mechanism of the anti-inflammatory effect of ibuprofen is due to the inhibition of the activity of cyclogenases (COX) with the subsequent suppression of the synthesis of prostaglandins.
Paracetamol is a non-narcotic analgesic that blocks COX mainly in the central nervous system, acting on the pain and thermoregulation centers, and has an analgesic and antipyretic effect.
Pharmacokinetics
Ibuprofen is well absorbed from the stomach. Тmax - about 1 hour. Absorption is slightly reduced when taking the drug after a meal. About 99% binds to plasma proteins. Ibuprofen is slowly distributed in the synovial fluid and is removed from it more slowly than from plasma. Metabolized in the liver, mainly by hydroxylation and carboxylation of the isobutyl group. CYP2C9 isoenzyme is involved in the metabolism of the drug. After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen slowly transforms into the active S-form. It has a biphasic elimination kinetics. The half-life (T?) Of plasma 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 excreted in 24 hours.
Paracetamol is rapidly absorbed from the gastrointestinal tract. The time to reach C max in 0.5-2 hours. Evenly distributed in body fluids. Communication with plasma proteins is variable within 15%. Gets through the BBB. Metabolized in the liver (90-95%): 80% reacts conjugation with glucuronic acid and sulfates with the formation of inactive metabolites; 17% is hydroxylated to form 8 active metabolites, which, when conjugated to glutathione, form inactive metabolites. With a lack of glutathione, these metabolites can block the enzyme systems of hepatocytes and cause their necrosis. CYP2E1 isoenzyme is involved in paracetamol metabolism. T 1/2 1-4 hours. Excreted by the kidneys as conjugates, and only 3% unchanged. In elderly patients, paracetamol clearance decreases and T1 / 2 increases.
The febrile reaction in acute respiratory diseases, influenza, post-vaccination reactions and other infectious and inflammatory diseases.
Each tablet contains:
Active ingredients:
Ibuprofen 400 mg
Paracetamol 325 mg
Excipients:
Calcium hydrogen phosphate 20.995 mg, corn starch 88.005 mg, povidone K306,000 mg, talc purified 10,000 mg;
Film coating: Opied orange (06G53189) (hypromellose 5 cP 29.500%, hypromellose 15 cP 29.500%, titanium dioxide 22.833%, sunset sunflower yellow 6.667%, macrogol 6000 5,500%, propylene glycol 5.500%, sodium lauryl sulfate 0.500%) 15,000 mg.
Ibuprofen, paracetamol is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Brustan | Ranbaxy Laboratories Ltd | India | pills |
capsules | |||
Nurofen Long | Reckitt Benckiser | UK | pills |
Next | Pharmstandard | Russia | pills |
Ibuclin | Dr. Reddy`s | India | pills |
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The drug is taken orally after a meal.
Precautions: congestive heart failure, hypertension, coronary heart disease, cerebrovascular disease, dyslipidemia, diabetes mellitus, peripheral vascular disease, smoking, frequent alcohol use, hyperbilirubinemia, liver cirrhosis with portal hypertension, liver and / or renal failure, nephrotic syndrome, pregnancy I and II trimesters, advanced age, deficiency of glucose-6-phosphate dehydrogenase, gastric ulcer and 12 duodenal ulcer (in history), gastritis, diseases of the cr Ovi of unknown etiology (leukopenia and anemia).
Inductors of microsomal oxidation (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of developing severe hepatotoxic reactions.
Inhibitors of microsomal oxidation reduce the risk of hepatotoxic action.
Reduces the hypotensive activity of vasodilators (including blockers of "slow" calcium channels and inhibitors of ace inhibitors), natriuric and diuretic - furosemide and hydrochlorothiazide. , ulcerogenic effect with bleeding glucocorticosteroids, colchicine, estrogen, ethanol; enhances the effect of oral hypoglycemic drugs and insulin.
Antacids and colestyramine reduce the absorption of ibuprofen .. Increases blood concentration of digoxin, lithium preparations and methotrexate
Caffeine enhances the analgesic effect.
With the simultaneous appointment of the active component of Brustan - ibuprofen reduces the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (ASK) (after starting ibuprofen, it is possible to increase the incidence of acute coronary insufficiency in patients who receive small doses of ASA as an antiplatelet agent).
When administered with anticoagulants and thrombolytic drugs (alteplase, streptokinase, urokinase), serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline) increases the risk of serious gastrointestinal bleeding.
Cefamendol, cefaperazon, cefotetan, valproic acid, plicamycin increase the incidence of hypoprothrombinemia.
Myelotoxic drugs increase the hematotoxicity of the drug.
Cyclosporine and gold preparations enhance the effect of ibuprofen on the synthesis of prostaglandins in the kidneys, which is manifested by increased nephrotoxicity.Ibuprofen increases the plasma concentration of cyclosporine and the likelihood of its hepatotoxic effects. Drugs that block tubular secretion, reduce excretion and increase the plasma concentration of ibuprofen.
The drug is contraindicated in the III trimester of pregnancy. Use in the I and II trimester, the lactation period should be discussed with your doctor.
Treatment with the drug should be carried out in the minimum effective dose, the shortest possible course.
During treatment, control of the pattern of peripheral blood and the functional state of the liver and kidneys is necessary. When symptoms of gastropathy appear, careful monitoring is shown, including esophagogastroduodenoscopy, a blood test with hemoglobin, hematocrit, fecal occult blood analysis. activities requiring increased attention, quick mental and motor responses. During the period of treatment is not recommended alcohol intake (ethanol).
When taken simultaneously with indirect anticoagulants, it is necessary to control the blood coagulation system.
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.
Hepatotoxic effect may occur with the development of hepatonecrosis associated with paracetamol.
Treatment: gastric lavage (only within an hour after ingestion), Activated charcoal, alkaline drink, forced diuresis, the introduction of SH-group donators and precursors of the synthesis of glutathione - methionine and N-acetylcysteine. The need for additional therapeutic measures (the further introduction of methionine, IV the introduction of N-acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as the time elapsed after taking it. In addition, symptomatic therapy is indicated.