Ibuprofen 200 mg, 10 capsules

Instructions for Ibuprofen

Dosage form Ibuprofen:

hard gelatin capsules No. 1 of white color with green caps containing powder of white or white color with a yellowish tint.

Composition Ibuprofen:

1 capsule: active substance: ibuprofen 200 mg; excipients: croscarmellose sodium 28 mg; talcum powder 4.8 mg; magnesium stearate 2.4 mg; Aerosil (colloidal silicon dioxide) (A-380) 4.8 mg;

Pharmacodynamics Ibuprofen:

Nonsteroidal anti-inflammatory drug (NSAIDs); It has an analgesic, antipyretic and anti-inflammatory effect due to the indiscriminate blockade of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2).

The mechanism of action of ibuprofen is due to inhibition of the synthesis of prostaglandins (PG) - mediators of pain, inflammation and hyperthermia.

Analgesic effect is most pronounced for inflammatory pain. It has an inhibitory effect on platelet aggregation.

Pharmacokinetics Ibuprofen:

Absorption Well absorbed from the gastrointestinal tract (GIT). Absorption is slightly reduced when taking the drug after a meal.

The time to reach maximum concentration (Cmax) when taken on an empty stomach is 45 minutes, when taken after meals - 1.5-2.5 hours, in synovial fluid - 2-3 hours (where it creates higher concentrations than in plasma) . Distribution Communication with blood plasma proteins is about 90%.

Lower concentrations of ibuprofen are found in the cerebrospinal fluid compared to blood plasma. It penetrates slowly into the joint cavity, but lingers in the synovial tissue, creating higher concentrations in it than in the blood plasma. Metabolism Metabolized in the liver.

After absorption, about 60% of the pharmacologically inactive R-form of ibuprofen slowly transforms into the active S-form. In the metabolism of the drug, the isoenzyme CYP2C9 takes part. Excretion Has a two-phase elimination kinetics with a half-life of 2-2.5 hours. The half-life (T1 / 2) of blood plasma is 2-3 hours. Up to 90% of the dose can be detected in the urine in the form of metabolites and their conjugates.

Excreted by the kidneys (unchanged no more than 1%) and to a lesser extent - with bile. Ibuprofen is completely eliminated in 24 hours.

Elderly patients. Elderly patients showed no significant differences in the pharmacokinetic profile of the drug compared to younger patients. In limited studies, ibuprofen is not detected.

Side effects Ibuprofen:

The frequency of side effects was evaluated as follows: very often (> 1/10); cha-hundred (> 1/100, <1/10); infrequently (> 1/1000, <1/100); rarely (> 1/10000, <1/1000); very rarely (<1/10000), the frequency is unknown (the incidence of side effects cannot be estimated based on available data). Infectious and parasitic diseases: very rarely - worsening inflammation due to infectious lesions (for example, the development of necrotic fasciitis), symptoms of aseptic meningitis with stiff neck, headache, nausea, vomiting, fever or confusion, especially in patients with autoimmune diseases ( SLE, systemic diseases of the connective tissue).
Disorders from the blood and lymphatic system: very rarely - violation of blood-forming (anemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis). Immune system disorders:
infrequently - hypersensitivity reactions: non-specific allergic reactions and anaphylactic reactions, reactions from the respiratory tract (bronchial asthma, including its exacerbation, bronchospasm, shortness of breath, dyspnea),
skin reactions (pruritus, urticaria, purpura, Quincke's edema, exfoliative and bullous dermatoses, including toxic epidermal necrolysis (Lyell-la syndrome), Stevens-Johnson syndrome, erythema multiforme), allergic rhinitis, eosinophilia; very rarely - severe hypersensitivity reactions, manifested in the form of swelling of the face, tongue and larynx, shortness of breath, tachycardia, arterial hypotension (anaphylaxis, Quincke's edema or severe anaphylactic shock).

Mental disorders: infrequently - psychomotor agitation, irritability, very rarely - neurosis, depression.
Disorders from the nervous system: infrequently - headache, dizziness, insomnia. Violations of the organ of vision: infrequently - impaired vision. Hearing disorders and labyrinth disorders: rarely - “tinnitus”.
Disorders from the heart: very rarely - tachycardia, heart failure, myocardial infarction. Vascular disorders: arterial hypertension. Disorders from the gastrointestinal tract: often - heartburn, abdominal pain, nausea, vomiting, flatulence, diarrhea, constipation, minor gastrointestinal bleeding, which can lead to the development of anemia; infrequently - peptic ulcer with possible complications (bleeding, perforation), ulcerative stomatitis, exacerbation of colitis and Crohn's disease, gastritis; very rarely - esophagitis, pancreatitis, the development of membrane intestinal strictures.

Violations of the liver and biliary tract: very rarely - impaired liver function, hepatotoxicity (especially with prolonged use), hepatic insufficiency, acute hepatitis. Disorders from the kidneys and urinary tract: very rarely - the development of edema, especially in patients with arterial hypertension or renal failure, nephrotic syndrome, interstitial nephritis, which may be accompanied by acute renal failure, damage to the renal tissue (papillary necrosis). Ibuprofen

Laboratory and instrumental data: infrequently - a decrease in hemoglobin and hematocrit, an increase in bleeding time, a decrease in blood glucose levels, a decrease and increase in serum creatinine concentration, an increase in the activity of “liver” transaminases, and very rarely an increase in uric acid level in the blood . The risk of ulceration of the gastrointestinal mucosa, bleeding (gastrointestinal, gingival, uterine, hemorrhoidal), visual impairment (color vision impairment, scotoma, amblyopia) increases with prolonged use in large doses.

Special conditions Ibuprofen:

During 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 indicated, including esophagogastroduodenoscopy, a blood test with hemoglobin, hematocrit, and occult blood feces.

To prevent the development of NSAIDs, gastropathy is recommended to be combined with PGE1 (misoprostol) preparations. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the study. During treatment, ethanol is not recommended. To reduce the risk of adverse events from the gastrointestinal tract, the minimum effective dose should be used with the minimum possible short course. During treatment, in very rare cases, a violation of blood formation is possible.

The first signs of hematopoiesis can be fever, sore throat, superficial ulcerations of the oral cavity, flu-like symptoms, severe weakness, nose bleeding, hemorrhagic skin rashes. If these symptoms occur, you must stop taking the drug and consult a doctor.

If there is severe pain in the epigastric region, melena or vomiting with blood, it is necessary to stop taking the drug and consult a doctor immediately. Influence on the ability to drive vehicles and work with mechanisms During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions (with the appearance of dizziness and other side effects that may affect to specified abilities).

Indications Ibuprofen:

Symptomatic treatment: - mild to moderate pain syndrome of various etiologies (headache, migraine, toothache, neuralgia, postoperative pain, post-traumatic pain, painful menstruation, myalgia, rheumatic pains of the joints and spine (rheumatoid arthritis, ankylosing spondylitis, osteoarthritis , gouty arthritis); - febrile conditions with flu and colds.

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

Drug Interactions Ibuprofen:

When used with ibuprofen, microsomal oxidation inducers (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites, increasing the risk of developing severe hepatotoxic reactions.

With the simultaneous use of ibuprofen, microsomal oxidation inhibitors reduce the risk of hepatotoxicity. With the simultaneous use of ibuprofen, it reduces: - hypotensive activity of vasodilators (including blockers of "slow" calcium channels and angiotensin converting enzyme (ACE) inhibitors), - natriuretic and diuretic activity of furosemide and hydrochlorothiazide, - the effectiveness of uricosuric drugs (C) - anti-inflammatory and antiplatelet effect of ASA (it is possible to increase the incidence of acute coronary insufficiency in patients receiving small doses of AS as an antiplatelet agent After the beginning of reception of ibuprofen).

With the simultaneous use of ibuprofen, it enhances: - the effect of indirect anticoagulants, antiplatelet agents, fibrinolytics and thrombolytic drugs (alteplases, streptokinases, urokinases) (increased risk of hemorrhagic complications); - ulcerogenic effect with bleeding of mineralocorticosteroid and glucocorticosteroid drugs, colchicine, estrogen, ethanol; - the effect of oral hypoglycemic drugs and insulin. Antacids and colestyramine reduce the absorption of ibuprofen. Ibuprofen increases the concentration in the blood of digoxin, lithium preparations and meto-traxate. Ibuprofen

With the simultaneous use of caffeine enhances the analgesic effect of ibuprofen. The simultaneous use of ibuprofen with drugs: cefamandol, cefaperazone, cefotetan, valproic acid, plicamycin increases the incidence of hypoprothrombinemia.

Myelotoxic drugs increase the manifestation of hematotoxicity of ibuprofen. Cyclosporin and gold preparations enhance the effect of ibuprofen on the synthesis of PG 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. Mifepristone: NSAIDs, including acetylsalicylic acid, should not be used for 8-12 days after the use of mifepristone, because NSAIDs may affect the effectiveness of mifepristone treatment.

Dosage Ibuprofen:

Adults, elderly and children over 12 years of age: 200 mg 3 times a day. Capsules should be swallowed with water, preferably during or after meals. To achieve a quick therapeutic effect, the dose can be increased to 400 mg (2 capsules) 3 times a day.

When the therapeutic effect is achieved, the daily dose of the drug is reduced to 600-800 mg. The maximum daily dose of the drug is not more than 1200 mg (do not take more than 6 capsules within 24 hours). Take a repeated dose no more than 4 hours later. If complaints persist for more than 4 days, a doctor’s consultation is required.

Do not use in children under 12 years of age without medical advice. Children from 6 to 12 years: 1 capsule no more than 4 times a day; the drug can be used only if the body weight of the child is more than 20 kg.

The interval between taking the drug Ibuprofen for at least 6 hours (daily dose of not more than 30 mg / kg).

Overdose Ibuprofen:

Symptoms: headache, dizziness, drowsiness, loss of consciousness (children also have myoclonic seizures), abdominal pain, nausea and vomiting. Perhaps the development of bleeding from the gastrointestinal tract, as well as liver and kidney failure.
Hypotension, respiratory depression and cyanosis can also be observed.

Treatment: gastric lavage (only within an hour after ingestion), activated charcoal, alkaline drink, forced diuresis, symptomatic therapy. In the case of the development of frequent or prolonged convulsions, anticonvulsants (diazepam or lorazepam intravenously) must be used. There is no specific antidote. Ibuprofen