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

Excipients: corn starch - 62.875 mg; pregelatinized starch - 18,625 mg; sodium carboxymethyl starch (type C) - 9,000 mg; stearic acid - 4,000 mg; talc - 4.0 mg; silicon dioxide colloid - 1,500 mg.

Film sheath: hypromellose - 5,750 mg; Macrogol-6000 - 1,100 mg; talc - 3.185 mg; titanium dioxide (E171) - 2.420 mg; simethicone emulsion SE4 (water - 67.4%, dimethicone - 30.0%; methyl cellulose - 2.5%; sorbic acid 0.1%) 0.045 mg.

One 400 mg tablet contains:

The core of the tablet:

active substance: ibuprofen 400.00 mg;

Excipients: corn starch - 125,750 mg; pregelatinized starch - 37.250 mg; sodium carboxymethyl starch (type C) - 18,000 mg; stearic acid - 8.0 mg; talcum - 8,000 mg; silicon dioxide colloid - 3,000 mg.

Film sheath: hypromellose - 11,500 mg; Macrogol-6000 - 2,200 mg; talc - 6,370 mg; titanium dioxide (E171) - 4.840 mg; simethicone emulsion SE4 (water - 67.4%, dimethicone - 30.0%; methyl cellulose - 2.5%; sorbic acid 0.1%) 0.090 mg.

Description:

Round, biconvex tablets, covered with a film coat from white or almost white to yellowish color.

Pharmacotherapeutic group:NSAIDs

ATX: & nbsp

M.01.A.E.01 Ibuprofen

Pharmacodynamics:

Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID), a derivative of propionic acid. The therapeutic effect of ibuprofen is associated with the indiscriminate inhibition of the effects of cyclooxygenase 1 (COX1) and cyclooxygenase 2 (COX2) enzymes, leading to the inhibition of the synthesis of prostaglandin mediators of pain,inflammation and hyperthermia.

Ibuprofen has analgesic, antipyretic and anti-inflammatory effects. The analgesic effect occurs in 30 minutes and lasts 4-6 hours, the antipyretic effect occurs after 2-4 hours and lasts 4-8 hours.

Pharmacokinetics:

Suction

After oral administration ibuprofen well absorbed.

Distribution

The maximum concentration (C_mOh) in blood plasma when taking the drug on an empty stomach is reached after 45 minutes, with the reception during meals - after 1-3 hours. Food intake has little effect on the bioavailability of ibuprofen.

Connection with blood plasma proteins - 90%. Slowly penetrates into the joint cavity, lingers in the synovial tissue, creating in it greater concentrations than in the plasma.

Metabolism

After absorption about 60% of pharmacologically inactive Rform is slowly transformed into an active S-form.

It is metabolized in the liver.

Excretion

It is excreted by the kidneys, mainly in the form of metabolites and their conjugates (unchanged not more than 1%), less excreted with bile and excreted through the intestine. T_1/2(half-life) - 2 hours After ingestion ibuprofen withdrawal ends after 24 hours.

Ibuprofen penetrates the placental barrier and is excreted in breast milk in amounts less than 1 μg / ml.

There are no specific differences in the pharmacokinetic profile in the elderly.

Indications:

- Headache (including tension headache and migraine);

- toothache, pain after tooth extraction (including surgical removal of the retinas tooth);

- pain with dysmenorrhea (painful menstruation);

- backache;

- muscular and rheumatic pain;

- neuralgia;

- feverish conditions with influenza and colds.

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:

- Erosion-ulcerative lesions of the gastrointestinal tract, peptic ulcer of the stomach and duodenum, peptic ulcer in the exacerbation or in the anamnesis (2 or more confirmed episodes of ulceration or bleeding), Crohn's disease, ulcerative colitis;

- hypersensitivity to ibuprofen or to the components of the drug;

- hypersensitivity to acetylsalicylic acid or other NSAIDs in history,complete or incomplete acetylsalicylic acid intolerance syndrome (bronchial asthma, urticaria, rhinitis, nasal mucosa polyps, triggered by the use of acetylsalicylic acid (salicylates) or other NSAIDs);

- bleeding, incl. gastrointestinal bleeding and intracranial hemorrhage;

- disorders of blood clotting and hemopoiesis;

- confirmed hyperkalemia;

- severe heart failure, decompensated heart failure (functional class II-IV by classification NYHA);

- hepatic failure of severe severity or active liver disease;

- renal failure of severe severity (creatinine clearance less than 30 ml / min), progressive kidney disease;

- severe degree of dehydration associated with vomiting, diarrhea, or insufficient fluid intake;

- diseases of the optic nerve, violation of color vision, amblyopia, scotoma;

- third trimester of pregnancy;

- children under 12 years of age and weighing less than 40 kg (for tablets 400 mg) and children under 6 years of age and weighing less than 20 kg (for tablets of 200 mg);

- decreased hearing, pathology of the vestibular apparatus;

- period after aortocoronary bypass surgery.

Carefully:

- In elderly patients (increased risk of erosive-ulcerative lesions of the gastrointestinal tract);

- if there is: a peptic ulcer of the stomach and 12 duodenal ulcer in the anamnesis; gastritis; enteritis; colitis; bleeding from the gastrointestinal tract in anamnesis;

- with arterial hypertension; chronic heart failure; ischemic heart disease; atherosclerotic lesion of peripheral arteries and / or cerebrovascular diseases;

- with concomitant diseases of the liver and / or kidneys (creatinine clearance 30-60 ml / min); nephrotic syndrome; hyperbilirubinemia; cirrhosis of the liver with portal hypertension; dyslipidemia;

- with diabetes mellitus;

- with blood diseases of unclear etiology (leukopenia and anemia); systemic lupus erythematosus and other autoimmune diseases of connective tissue (risk of developing aseptic meningitis);

- when combined with other NSAIDs, including specific inhibitors of cyclooxygenase type 2; simultaneous ingestion of glucocorticosteroids (GCS) (including prednisolone), anticoagulants (incl.warfarin), selective serotonin reuptake inhibitors (see section "Interaction with other drugs");

- 1 and 2 trimesters of pregnancy;

- in the period of breastfeeding;

- at the use of alcohol and smoking;

- with prolonged use of NSAIDs.

Pregnancy and lactation:

Pregnancy

Contraindicated use of the drug in the III trimester of pregnancy; if necessary, the use of the drug in I-II trimester of pregnancy apply only if the potential benefit to the mother exceeds the potential risk to the fetus.

Breastfeeding period

Ibuprofen and its metabolites penetrate the breast milk of nursing mothers in extremely low concentrations (0.0008% of the dose). Due to the low content in breast milk, the short half-life of ibuprofen and the lack of documentary evidence to date of adverse effects on infants, ibuprofen can be used only briefly at recommended doses as an analgesic or antipyretic agent in nursing mothers.

Dosing and Administration:

Tablets should be taken orally, with water.

Adults and children over 12 years of age (with a body weight of more than 40 kg)

200 mg 3-4 times a day.

To achieve a more rapid effect in adults, a single dose can be increased to 400 mg three times a day.

The maximum daily dose is 1200 mg.

The maximum daily dose for adolescents aged 12-17 years is 1000 mg.

Children from 6 to 12 years old (with a body weight of more than 20 kg)

200 mg not more than 4 times a day. The interval between taking the tablets should be at least 6 hours.

The maximum daily dose of 20-35 mg / kg, divided into several doses, with juvenile rheumatoid arthritis can be increased to 40-50 mg / kg.

If symptoms persist for 2-3 days after taking the drug, stop treatment and consult a doctor.

Side effects:

When using the drug Ibuprofen during 2-3 days, side effects are practically not observed.

In the case of prolonged use of the drug Ibuprofen the appearance of the following side effects may occur, which are divided according to the system-organ classes in accordance with the classification of the Medical Dictionary for Regulatory Activities (MedDRA).The WHO classification was used to indicate the incidence of adverse events: very often (≥ 10%); often (≥ 1% and <10%); infrequently (≥ 0.1% and <1%); rarely (≥ 0.01% and <0.1%); very rarely (<0.01%); an unknown frequency (according to available data, it is not possible to determine the frequency of occurrence of a side effect).

Disorders from the gastrointestinal tract

Often: nausea, vomiting, heartburn, diarrhea, flatulence, constipation.

Often: pain in epigastrium.

Rarely: gastritis, gastric ulcer, ulcer of 12-типерстной intestines, complicated by a gastrointestinal bleeding or perforation; bloody vomiting, bleeding gums, melena, hemorrhoidal bleeding (with prolonged use in large doses).

Rarely: dryness of the oral mucosa or pain in the mouth, aphthous stomatitis, exacerbation of Crohn's disease, exacerbation of ulcerative colitis.

Unknown frequency: anorexia, pancreatitis.

Disturbances from the liver and bile ducts

Rarely: violations of the liver (usually reversible).

Unknown frequency: hepatitis.

Violations of the blood and lymphatic system

Rarely: neutropenia, agranulocytosis, aplastic or hemolytic anemia, thrombocytopenia.

Unknown frequency: leukopenia.

Heart Disease

Rarely: heart failure.

Rarely: tachycardia.

Disorders from the metabolism and nutrition

Rarely: sodium and water retention.

Vascular disorders

Rarely: lowering blood pressure, increasing blood pressure.

Disturbances from the nervous system

Infrequently: headache, dizziness.

Rarely: aseptic meningitis (usually in patients with systemic lupus erythematosus and other autoimmune connective tissue diseases).

Unknown frequency: agitation, drowsiness, confusion.

Hearing disorders

Unknown frequency: hearing loss, ringing or noise in the ears.

Disorders of the psyche

Rarely: insomnia, depression, emotional lability.

Unknown frequency: hallucinations.

Disorders from the kidneys and urinary tract

Rarely: cystitis, hematuria, renal dysfunction, including interstitial nephritis or nephrotic syndrome (edema).

Unknown frequency: polyuria.

Disturbances on the part of the organ of sight

Rarely: visual impairment, including blurred vision and diplopia, scotoma, impaired color vision, toxic amblyopia.

Unknown frequency: dryness and irritation of the eyes, edema of the conjunctiva and eyelids.

Disturbances from the respiratory system, chest and mediastinal organs

Rarely: bronchospasm, shortness of breath.

Disturbances from the skin and subcutaneous tissues

Rarely: bullous reactions, including multiforme exudative erythema, Stevens-Johnson syndrome and toxic epidermal necrolysis.

Immune system disorders

Rarely: hypersensitivity reactions (fever, rash, hepatotoxicity).

Unknown frequency: itching, urticaria, Quincke's edema, anaphylactoid reactions, anaphylactic shock, eosinophilia, allergic rhinitis.

Common violations

Rarely: edema.

If side effects occur, stop taking the medication and consult a doctor.

From the laboratory indicators

Increased serum creatinine concentration, decreased creatinine clearance, increased bleeding time, reduced serum glucose concentration, increased activity of "hepatic" transaminases, decreased hematocrit, decreased hemoglobin concentration.

Overdose:

Symptoms

Ibuprofen at a dose of 100 mg / kg body weight is non-toxic, doses above 400 mg / kg body weight can cause severe intoxication.

From the nervous system: headache, dizziness, drowsiness, drowsiness, depression, tinnitus, nystagmus, convulsions, up to coma.

There may be abdominal pain, nausea, vomiting, diarrhea.

In severe cases, an overdose can cause acute renal and hepatic insufficiency, metabolic acidosis, lowering of arterial pressure, bradycardia, tachycardia, atrial fibrillation, respiratory arrest.

Treatment of acute overdose

As soon as possible, you should rinse the stomach or induce a vomiting reflex with the subsequent intake of activated charcoal (only within an hour after intake), appoint an alkaline drink.

Symptomatic treatment aimed at maintaining the vital vital functions of the body.

Control and the necessary correction of the water-electrolyte balance.

In the case of frequent or prolonged seizures, anticonvulsants should be used (diazepam and lorazepam).

Interaction:

When the drug is prescribed Ibuprofen it is necessary to take into account its interaction with the following preparations:

- Acetylsalicylic acid or other NSAIDs: increased risk of ulcerative lesions of the gastrointestinal tract and gastrointestinal bleeding. Ibuprofen can inhibit the anti-inflammatory and antiplatelet effect of acetylsalicylic acid (aspirin) in small doses during their simultaneous administration.

- Glucocorticosteroids and mineralocorticosteroids: increased risk of ulcerative lesions of the gastrointestinal tract or development of gastrointestinal bleeding.

- Hypotensive drugs and diuretics: NSAIDs may reduce effects diuretics and antihypertensive drugs. In some patients with impaired renal function (eg, in patients with dehydration, or in elderly patients with impaired renal function), simultaneous use of ACE inhibitors, beta-blockers and angiotensin II receptor inhibitors with cyclooxygenase inhibiting drugs can lead to further impairment of function kidney, including the possibility of developing acute renal failure, which is usually reversible. Therefore, this combination should be used with caution, especially in elderly patients.Patients should be sufficiently hydrated, and after the initiation of combination therapy and periodically thereafter they should monitor renal function.

- Potassium-sparing diuretics: simultaneous use of ibuprofen and potassium-sparing diuretics can lead to hyperkalemia (it is recommended to monitor the potassium content in the blood).

- Indirect anticoagulants, antiaggregants, fibrinolytics: NSAIDs can enhance the effects of indirect anticoagulants, such as warfarin.

- Thrombolytics: with simultaneous use with thrombolytic drugs (alteplase, streptokinase, urokinase), the risk of bleeding increases.

- Selective serotonin reuptake inhibitors: increased risk of gastrointestinal bleeding.

- Preparations of lithium, digoxin, phenytoin: Combined therapy with ibuprofen with lithium preparations, digoxin or phenytoin may increase the serum concentrations of these drugs.

- Methotrexate: the use of ibuprofen at a dose of 200 mg within 24 hours before or after the administration of methotrexate may lead to an increase in the concentrations in the blood of methotrexate and an increase in its toxic effects.

- Baclofen: There are clinical data indicating that NSAIDs can increase plasma concentrations of baclofen.

- Zidovudine: there is evidence that the risk of hemarthrosis and hematoma increases in HIV-infected patients with hemophilia receiving concomitantly zidovudine and ibuprofen.

- Quinolones: data from animals indicate that NSAIDs may increase the risk of seizures associated with the use of quinolones. Patients taking both quinolones and ibuprofen, have an increased risk of seizures.

- Cyclosporine, tacrolimus, preparations of gold: may increase the risk nephrotoxicity due to decreased synthesis of prostaglandins in the kidneys. During combined therapy, renal function should be carefully monitored, especially in elderly patients. Ibuprofen increases the plasma concentration of cyclosporine and the likelihood of its hepatotoxic effects.

- Mifepristone: since NSAIDs can reduce the effectiveness of mifepristone, NSAIDs should be started no earlier than 8-12 days after the withdrawal of mifepristone.

- Drugs that block tubular secretion: can increase the plasma concentration of ibuprofen.

- Hypoglycemic drugs for oral administration, derivatives of sulfonylureas: as a precautionary measure, it is recommended to control the concentration of glucose in the blood when they are used together.

- Sulfinpyrazone, probenecid: when combined with ibuprofen, the inhibition of ibuprofen excretion is possible.

- Aminoglycosides: ibuprofen can reduce the clearance of aminoglycosides, which can increase the nephrotoxicity and hepatotoxicity of these drugs.

- Cefamandol, cefaperazone, cefotetan, valproic acid, plikamycin: may increase the incidence of hypoprothrombinemia in a joint appointment with ibuprofen.

- Inductors of microsomal oxidation (phenytoin, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants): when combined, they increase the production of hydroxylated active metabolites, increasing the risk of severe intoxication.

- Urikozuric preparations: ibuprofen reduces the effectiveness of uricosuric drugs.

- Estrogens, ethanol: with the simultaneous use of ibuprofen may increase the side effects of estrogens, ethanol.

- Antacids and colestramine: drugs reduce the absorption of ibuprofen.

- Caffeine: Caffeine enhances the analgesic effect of ibuprofen.

Special instructions:

Side effects can be minimized by applying the lowest effective doses with the shortest duration of their intake necessary to eliminate symptoms.

The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing NSAID doses, in patients with a history of instructions on peptic ulcer complicated by bleeding or perforation (see. Section "Contraindications") and in elderly patients. Such patients should begin treatment with the least effective doses.

In patients with an increased risk of side effects, and patients are constantly receiving aspirin in antiplatelet doses or other drugs that increase the risk of developing ulcerative erosive lesions of the gastrointestinal tract (see. Section "Interaction with other medicinal products"), should be considered the question of preventive intake of misoprostol or proton pump inhibitors.

When symptoms of gastrointestinal tract damage appear, careful monitoring is performed, including esophagogastroduodenoscopy, a general blood test (determination of hemoglobin), and analysis of feces for latent blood.

Patients with uncontrolled arterial hypertension, chronic heart failure, coronary heart disease, atherosclerotic lesions of peripheral arteries and / or cerebrovascular disease should take ibuprofen only if necessary. The same applies to patients with risk factors for developing cardiovascular diseases (such as hypertension, hyperlipidemia, diabetes mellitus).

Care should be taken when taking the drug for renal and hepatic insufficiency. Monitoring of renal function is recommended for patients with combined cardiac and renal insufficiency, taking diuretics, or when dehydrating the body. With prolonged treatment, it is recommended to monitor the parameters of the functional state of the liver and kidneys.

It is necessary to stop treatment with a decrease in the function of the liver and / or kidney due to taking the drug.

In patients with impaired glucose tolerance, glucose monitoring in the blood should be monitored.

Care should be taken when prescribing the drug Ibuprofen patients:

- with congenital disorders of porphyrin exchange (acute intermittent porphyria);

- receiving treatment with indirect anticoagulants;

- with systemic lupus erythematosus and other autoimmune diseases of connective tissue (risk of aseptic meningitis).

With prolonged treatment it is recommended to monitor the parameters of peripheral blood.

Very rarely reported serious skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis associated with the administration of NSAIDs (see section "Side effect"). Patients have the highest risk of these reactions in the early treatment of NSAIDs: the initial manifestations of these reactions usually appear during the first month of treatment. Reception of the drug Ibuprofen should be discontinued immediately after the first appearance of skin rash, damage to the mucous membranes or any other manifestations of hypersensitivity.

Ibuprofen, due to its pharmacological action, can reduce the diagnostic significance of such symptoms as fever, pain, and swelling.

The use of drugs that inhibit cyclooxygenase / prostaglandin synthesis can adversely affect fertility in women due to their effect on ovulation. This effect of ibuprofen is reversible and disappears after discontinuation of treatment.

During the treatment, alcohol (ethanol) is not recommended.

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

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

A drug Ibuprofen does not affect the ability to drive vehicles and use equipment, as well as engage in other potentially hazardous activities. However, if patients experience side effects from the nervous system, in particular dizziness, visual disorders (see "Side effect"), they should refrain from all activities requiring increased attention and rapid psychomotor reactions (including driving).

Form release / dosage:The film-coated tablets are 200 mg and 400 mg.

Packaging:

For 12 tablets in a blister (PVC / aluminum).

For the dosage of 200 mg: 1 or 2 blisters together with instructions for use in a cardboard bundle.

For a dosage of 400 mg: 1, 2 or 3 blisters together with instructions for use in a cardboard pack.

Storage conditions:

In a dry place, at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003431

Date of registration:02.02.2016

Expiration Date:02.02.2021

The owner of the registration certificate:Zentiva c.s.Zentiva c.s. Czech Republic

Manufacturer: & nbsp

ZENTIVA, k.s. Czech Republic

Representation: & nbspZENTIVA PHARMA, LLCZENTIVA PHARMA, LLC

Information update date: & nbsp19.10.2017

Illustrated instructions

Instructions

Ibuprofen (Ibuprofen )