Pharmacodynamics
The drug belongs to non-steroidal anti-inflammatory drugs (NSAIDs). It has analgesic, antipyretic and anti-inflammatory effects. Blocks COG1 and COG2 indiscriminately.
The mechanism of action of ibuprofen is due to inhibition of the synthesis of prostaglandins - mediators of pain, inflammation and hyperthermic reaction.
Pharmacokinetics
Absorption - high, quickly and almost completely absorbed from the gastrointestinal tract. Cmax of ibuprofen in plasma is achieved 1-2 hours after taking the drug. Communication with plasma proteins is more than 90%, T1 / 2 - 2 hours. Slowly penetrates into the joint cavity, lingers in the synovial tissue, creating higher concentrations in it than in plasma. After absorption, about 60% of the pharmacologically inactive R-form is slowly transformed into the active S-form. Metabolized. It is excreted by the kidneys (not more than 1% unchanged) and, to a lesser extent, with bile.
Contraindications
hypersensitivity to any of the ingredients that make up the drug. Hypersensitivity to acetylsalicylic acid or other NSAIDs, incl. anamnestic data about an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or another NSAID; complete or incomplete syndrome of intolerance to acetylsalicylic acid (rhinosinusitis, urticaria, nasal mucosa polyps, bronchial asthma);
erosive and ulcerative diseases of the gastrointestinal tract in the stage of exacerbation (including peptic ulcer of the stomach and duodenum, Crohn's disease, ulcerative colitis);
inflammatory bowel disease;
hemophilia and other blood clotting disorders (including hypocoagulation), hemorrhagic diathesis;
period after coronary artery bypass grafting;
gastrointestinal bleeding and intracranial hemorrhage;
severe liver failure or active liver disease;
progressive kidney disease;
severe renal failure with creatinine clearance less than 30 ml / min, confirmed hyperkalemia;
pregnancy;
children under 6 years of age.
Carefully. Elderly age, heart failure, arterial hypertension, ischemic heart disease, cerebrovascular disease, dyslipidemia, diabetes mellitus, peripheral arterial disease, smoking, frequent alcohol consumption, liver cirrhosis with portal hypertension, hepatic and / or renal failure with creatinine clearance less than 60 ml / min, nephrotic syndrome, hyperbilirubinemia, gastric ulcer and duodenal ulcer (history), presence of H. pylori infection, gastritis, enteritis, colitis, blood diseases of unknown etiology (leukopenia and anemia), lactation period, prolonged use of NSAIDs, severe somatic diseases, simultaneous administration of oral corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine , paroxetine, sertraline).
Pregnancy and lactation
Contraindicated in pregnancy. Use with caution during lactation.
Side effects
Gastrointestinal tract (GIT): NSAID-gastropathy (abdominal pain, nausea, vomiting, heartburn, loss of appetite, diarrhea, flatulence, constipation; rarely - ulceration of the gastrointestinal mucosa, which in some cases is complicated by perforation and bleeding); irritation or dryness of the oral mucosa, pain in the mouth, ulceration of the gingival mucosa, aphthous stomatitis, pancreatitis. Hepato-biliary system: hepatitis.
Respiratory system: shortness of breath, bronchospasm.
Sense organs: hearing impairment: hearing loss, ringing or tinnitus; visual impairment: toxic damage to the optic nerve, blurred vision or double vision, scotoma, dry and irritated eyes, edema of the conjunctiva and eyelids (allergic genesis). 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).Cardiovascular system: heart failure, tachycardia, increased blood pressure. Urinary system: acute renal failure, allergic nephritis, nephrotic syndrome (edema), polyuria, cystitis. Allergic reactions: skin rash (usually erythematous or urticaria), pruritus, Quincke's edema, anaphylactoid reactions, anaphylactic shock, bronchospasm or dyspnea, fever, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal syndrome , eosinophilia, allergic rhinitis. Hematopoietic organs: anemia (including hemolytic, aplastic), thrombocytopenia and thrombocytopenic purpura, agranulocytosis, leukopenia.
Others: increased sweating.
The risk of ulceration of the mucous membrane of the gastrointestinal tract, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), visual impairment (color vision disorders, scotoma, amblyopia) increases with prolonged use in large doses.
Laboratory indicators:
bleeding time (may increase);
serum glucose concentration (may decrease);
creatinine clearance (may decrease);
hematocrit or hemoglobin (may decrease);
serum creatinine concentration (may increase);
activity of "hepatic" transaminases (may increase).
If side effects occur, you should stop taking the drug and consult a doctor.
Interaction
Simultaneous administration of acetylsalicylic acid and other NSAIDs is not recommended. With the simultaneous administration of ibuprofen, it reduces the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (it is possible to increase the incidence of acute coronary insufficiency in patients receiving small doses of acetylsalicylic acid as an antiplatelet agent after starting ibuprofen).When administered with anticoagulant and thrombolytic drugs (alteplase, streptokinase, urokinase), the risk of bleeding increases at the same time. Concomitant use with serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline) increases the risk of serious gastrointestinal bleeding. Cefamandol, cephaperazone, cefotetan, valproic acid, plicamycin, increase the incidence of hypoprothrombinemia. Cyclosporine and gold preparations increase the effect of ibuprofen on the synthesis of prostaglandins in the kidneys, which is manifested by an increase in 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. Microsomal oxidation inducers (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of severe intoxication. Microsomal oxidation inhibitors - reduce the risk of hepatotoxic effects. Reduces the hypotensive activity of vasodilators, natriuretic and diuretic activity in furosemide and hydrochlorothiazide. Reduces the effectiveness of uricosuric drugs, enhances the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics (increasing the risk of hemorrhagic disorders), enhances the ulcerogenic effect with bleeding of mineralocorticosteroids, glucocorticosteroids, colchicine, estrogens, ethanol. Enhances the effect of oral hypoglycemic drugs and insulin, sulfonylurea derivatives. Antacids and cholestyramine reduce absorption. Increases the concentration in the blood of digoxin, lithium preparations, methotrexate. Caffeine enhances the analgesic effect.
Dosage and administration
Ibuprofen is prescribed for adults and children over 12 years old by mouth, in tablets of 200 mg 3-4 times a day. To achieve a quick therapeutic effect, the dose can be increased to 400 mg (2 tablets) 3 times a day. When the therapeutic effect is achieved, the daily dose of the drug is reduced to 600-800 mg. The morning dose is taken before meals with plenty of water (for faster absorption of the drug). The remaining doses are taken throughout the day after meals. The maximum daily dose is 1200 mg (do not exceed 6 tablets in 24 hours). The repeated dose should be taken no more than 4 hours later. The duration of the drug use without consulting a doctor is not more than 5 days. Do not use in children under 12 years of age without consulting a doctor.
Children from 6 to 12 years old: 1 tablet no more than 4 times a day; the drug can be used only if the child's body weight is more than 20 kg. The interval between taking the tablets is at least 6 hours (daily dose is not more than 30 mg / kg).
Overdose
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.
Special instructions
Treatment with the drug should be carried out in the minimum effective dose, the minimum possible short course. During long-term treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys. When symptoms of gastropathy appear, careful monitoring is shown, including esophagogastroduodenoscopy, a general blood test (determination of hemoglobin), and fecal occult blood test. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study. Patients should refrain from all types of activities that require increased attention, quick mental and motor reactions. It is not recommended to take ethanol during the treatment period.
