Ibuprofen
Producer: JSC Borisovsky Plant of Medical Supplies Republic of Belarus
Code of automatic telephone exchange: M01AE01
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 200 mg of an ibuprofen in 1 tablet.
Excipients: potato starch, magnesium stearate, calcium stearate, povidone (polyvinylpirrolidone), опадрай ΙΙ (the polyvinyl alcohol which is partially hydrolyzed, talc, a macrogoal 3350, lecithin, titanium dioxide (E 171)).
Pharmacological properties:
Pharmacodynamics. The means of nonsteroid structure rendering the expressed antiinflammatory, analgeziruyushchy, febrifugal and antiagregantny action.
The mechanism of action is connected with inhibition of activity of cyclooxygenase I and II of types (an index of selectivity TsOG-I: TsOG-II = 5,0-10,0: 1). Reactions of the arachidonic cascade of synthesis of eicosanoids are as a result blocked and formation of prostaglandins PgE2, PgF22, TxA2 thromboxane, PgI2 prostacyclin is broken.
The ibuprofen reduces a hyperemia, exudation and permeability of capillaries in the inflammation center. Brakes activity of hyaluronidase, oppresses products of ATP, limiting power ensuring inflammatory process.
At rheumatic diseases has antiinflammatory and analgeziruyushchy effect. Weakens a rest pain and at the movement, reduces morning constraint and a swelling of joints, improves their function. Full antiinflammatory action develops for 5-7 day of regular use.
At posttraumatic and postoperative inflammatory processes quickly stops both spontaneous pain, and the pain arising at the movement. Reduces inflammatory hypostasis in the field of a wound.
The ibuprofen has soothing effect, raises an excitation threshold of the painful centers of a thalamus. Interferes with carrying out painful impulses from extra-and proprioceptive receptors on Gaulle and Burdakh's bunches. Reduces algogenny effect of bradikinin. In kernels of anti-nociceptive system the ibuprofen strengthens release of kinureninovy acid which slows down carrying out painful impulses (due to influence on AMPA-and NMDA receptors), and also endogenous opiopeptid. Eliminates the pains of weak and average intensity having, as a rule, somatic character: muscle, joints, sinews pains, nervous trunks, head and tooth hurt.
Reduces the increased body temperature, but does not influence normal body temperature. It is connected with ability of an ibuprofen to reduce activity of the thermoadjusting center of a hypothalamus, to reduce influence on it of endogenous pyrogens, to strengthen a thermolysis. The febrifugal effect develops in smaller doses, than antiinflammatory and arises in 30 min. after use of an ibuprofen, remaining for 6 h.
The ibuprofen breaks reaction of pasting (aggregation) of thrombocytes and leads to some lengthening of a bleeding time.
Pharmacokinetics. After intramuscular introduction it is well absorbed. Bioavailability makes 80%. The maximum concentration in a blood plasma after intake is on an empty stomach reached in 0,45-1 h, at reception after food – in 2,0-2,5 h. The maximum concentration in synovial fluid – in 3 h. Therapeutic concentration in plasma makes 10 – 50 mkg/ml, toxic – 100 – 700 mkg/ml. Biological activity of an ibuprofen is connected with S-enantiomerom. After absorption about 60% pharmacological of an inactive R-form are slowly transformed to an active S-form.
In blood reversibly contacts proteins of plasma (about 90-99%). Slowly gets into a cavity of joints, is late in synovial fluid, creating in it concentration big, than in plasma. The volume of distribution makes 0,1 l/kg.
It is metabolized in a liver with formation of 3 inactive metabolites. 60-90% of the entered dose are removed by kidneys with urine in the form of metabolites, to a lesser extent removed with bile. Excretion of not changed ibuprofen makes less than 1%. The period of semi-elimination of an ibuprofen makes 2-2,5 h, the general clearance 0,75 ± 0,20 ml/min.
At elderly patients the pharmacokinetics of an ibuprofen does not change.
Indications to use:
* inflammatory diseases of a musculoskeletal system: a pseudorheumatism (including a juvenile pseudorheumatism), the rheumatism ankylosing a spondylitis, chronic gouty arthritis, spondylarthrites, an osteoarthritis;
* degenerative diseases of a musculoskeletal system: the deforming osteoarthrosis;
* diseases of extraarticular fabrics: tendovaginitis, bursitis;
* rheumatic defeats of soft tissues;
* the posttraumatic and postoperative pain syndromes which are followed by an inflammation and hypostasis;
* a pain syndrome of weak and average intensity (including a headache, migraine, a dentagra, pains at an osteoarthrosis, arthritis, a panniculitis, a menalgiya, альгодисменорея);
* syndrome to Bara-Lyeu (cervical migraine, syndrome of a vertebral artery);
* a feverish syndrome at acute infectious, infectious and inflammatory diseases;
* symptomatic treatment of a SARS, flu and other catarrhal diseases;
* postural hypotension at reception of antihypertensives;
* a glomerulonephritis and a nephrotic syndrome (for reduction of expressiveness of a proteinuria);
* as an additional tool at a serious infectious and inflammatory illness of the ENT organs, pneumonia, perikardita and pleurisy proceeding with the expressed pain syndrome.
Route of administration and doses:
Apply inside, it is more preferable between meals.
The adult appoint 400 – 600 mg (2 – 3 tablets) 3 – 4 times a day. At a pseudorheumatism – on 800 mg (4 tablets) 3 times a day. At algodismenory appoint 400 – 600 mg (2 – 3 tablets) with an interval of 4 - 6 hours. The maximum single dose makes 800 mg (4 tablets), a daily dose – 2400 mg (12 tablets).
To children appoint in a dose 5 – 10 mg/kg/days in 3 – 4 receptions. The maximum daily dose of an ibuprofen of 20 mg/kg, at a juvenile pseudorheumatism – to 40 mg/kg. To children at the age of 3 – 6 years (body weight of 16 - 20 kg) on 100 mg (½ tablets) 3 times a day, the maximum daily dose of 300 mg. To children of 6 - 9 years (21 – 30 kg) on 100 mg (½ tablets) 4 times a day, the maximum daily dose of 400 mg. To children of 9 - 12 years (31 – 41 kg) on 200 mg (1 tablet) 3 times a day, the maximum daily dose of 600 mg. To children 12 years (more than 41 kg) on 200 mg (1 tablet) 4 times a day, the maximum daily dose – 800 mg are more senior.
As febrifugal appoint at body temperature more than 38,5 °C (patients with febrile spasms in the anamnesis – at a temperature have more than 37,5 °C). If body temperature exceeds 39,2 °C appoint at the rate of 10 mg/kg, at a temperature below 39,2 °C – in a dose of 5 mg/kg.
Features of use:
Pregnancy. Use of an ibuprofen during pregnancy is possible only when the expected advantage for mother exceeds potential risk for a fruit. It is necessary to appoint drug in a minimal effective dose. Use of an ibuprofen in the III trimester of pregnancy in connection with possible oppression of sokratitelny ability of a uterus and premature closing of an arterial channel at a fruit is not recommended.
Lactation period. The ibuprofen gets into breast milk therefore at its use in the period of a lactation it is necessary to provide the termination of breastfeeding for the entire period of treatment.
Persons with GIT pathology. During use of an ibuprofen careful medical observation of patients who have complaints from bodies of a GIT, a GIT canker in the anamnesis, and also nonspecific ulcer colitis or a disease Krone is necessary. Against the background of use of an ibuprofen for this group of patients there can be (for the first time or repeatedly) gastrointestinal bleeding or ulceration/perforation of a GIT which can not be followed by symptoms harbingers. In all such cases drug has to be cancelled.
Persons with pathology of system of blood. The ibuprofen temporarily inhibits aggregation of thrombocytes therefore at patients with disturbances of a hemostasis careful control of the corresponding laboratory indicators is necessary. At prolonged use of an ibuprofen systematic control of peripheral blood is shown.
Persons with liver diseases. During use of an ibuprofen perhaps tranzitorny increase in activity of liver enzymes. At long therapy the ibuprofen as a precautionary measure showed laboratory control of function of a liver. If disturbances from functional indicators remain or amplify, and also if there are clinical manifestations of other damages of a liver, the ibuprofen should be cancelled. It is necessary to remember that hepatitis against the background of use of an ibuprofen can arise without prodromal manifestations.
Persons with pathology of cardiovascular system. As prostaglandins play an important role in maintenance of a normal renal krovtok, extra care is required when using an ibuprofen from the patients suffering from renal failures and chronic congestive heart failure at the persons receiving diuretic means and also at patients with considerable reduction of volume of the circulating plasma (for example, during the period before and after massive surgical interventions). In all these cases control of function of kidneys is recommended as a precautionary measure. Drug phase-out usually leads to recovery of function of kidneys to initial level.
Influence on laboratory indicators. In need of definition of 17 ketosteroids in urine, reception of an ibuprofen has to be stopped for 48 h before carrying out the analysis.
Influence on ability to driving of motor transport and control of mechanisms. During use of an ibuprofen it is necessary to abstain from all types of activity requiring special attention, bystry mental and motor reaction.
During treatment ethanol reception is not recommended.
Cherry and currant juice, sugar syrup increase the speed of absorption of an ibuprofen.
For decrease in risk of development of the undesirable phenomena from a GIT it is necessary to use a minimal effective dose minimum possible short course.
Side effects:
* heartburn, abdominal pains, nausea, vomiting, diarrhea, meteorism, anorexia, NPVS-gastropathy, gastrointestinal bleedings.
* headache, dizziness, sleeplessness or drowsiness, excitement, depression, sonitus, disturbances of auditory acuity, sight (disturbance of color sight, scotoma, amblyopia).
* skin allergic reactions, small tortoiseshell, Quincke's disease, multiformny exudative erythema (Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease), aseptic meningitis, bronchospasm.
* heart failure, tachycardia, increase in the ABP.
* edematous syndrome, renal failure, allergic nephrite.
* anemia, thrombocytopenia, agranulocytosis, leukopenia.
* sweating strengthening.
Interaction with other medicines:
The ibuprofen can increase concentration of a methotrexate, lithium and digoxin in plasma at simultaneous use with these drugs.
The ibuprofen, as well as other non-steroidal anti-inflammatory drugs (NPVP) can reduce effect of diuretics, blockers of calcium channels, APF inhibitors and other hypotensive drugs that is connected with disturbance of synthesis of prostaglandins in kidneys. Simultaneous use with kaliysberegayushchy diuretics can lead to increase in level of potassium in blood (in case of need such combination of medicines it is necessary to monitorirovat potassium level in plasma).
There are messages on increase in risk of bleeding in case of combined use of an ibuprofen and anticoagulants, fibrinolitic drugs.
At combined use with antidepressants, barbiturates, ziksoriny, rifampicin, phenylbutazone, Phenytoinum the risk of development of heavy intoxications due to increase in products of hydroxylated active metabolites of an ibuprofen increases.
The ibuprofen increases sugar-lowering efficiency of peroral gipoglikemiziruyushchy means that demands dose adjustment of these drugs against the background of use of an ibuprofen.
Glucocorticoid and mineralkortikoidny hormones, colchicine strengthen antiinflammatory action of an ibuprofen and increase risk of development of a gastrointestinal tract disease.
At combined use with tsefamandoly, tsefoperazony, tsefotetany, valproic acid and plikamitsiny the risk of development of a gipoprotrombinmiya increases.
Cyclosporine and drugs of gold strengthen nephrotoxic action of an ibuprofen.
The ibuprofen strengthens undesirable effect of estrogen at combined use.
The ibuprofen weakens efficiency of uricosuric action of antigouty means.
Colestyraminum slows down absorption of an ibuprofen.
Caffeine strengthens analgetic effect of an ibuprofen.
The ibuprofen increases toxicity of ethanol.
At combined use acetylsalicylic acid weakens effect of an ibuprofen and increases its toxicity, it is connected with replacement of an ibuprofen from communication with proteins and his metabolism with formation of toxic hydroxylated metabolites.
Contraindications:
* deficit glyukozo-6-fosfatdegidrogenazy;
* hypersensitivity to an ibuprofen;
* GIT erosive cankers in an aggravation phase;
* "aspirinovy" asthma and "aspirinovy" triad;
* hemorrhagic diathesis (angiohemophilia, Werlhof's disease, telangiectasias), prothrombinopenia, hemophilia;
* the stratifying aortic aneurysm;
* deficit of vitamin K;
* pregnancy in the III trimester and a lactation;
* diseases of an optic nerve, scotoma, amblyopia, disturbance of color sight;
* arterial hypertension, heart failure of the III-IV stage on NYHA;
* pathology of a vestibular mechanism, decrease in hearing;
* children's age up to 3 years.
Overdose:
Symptoms: the typical clinical picture at overdose of an ibuprofen does not develop. Emergence of abdominal pains, nausea, vomitings, dizzinesses, block, drowsiness, a depression, a headache, hypotonia, spasms, disturbance of a cordial rhythm, an acute renal failure, respiratory depression is possible.
Treatment: measures of the help include the drug withdrawal supporting and the symptomatic therapy directed to elimination of the arisen disturbances, correction of an acid-base state. Carrying out an artificial diuresis with co-administration of alkaline drink, absorbent carbon, for reduction of a reabsorption of an ibuprofen is possible. The specific antidote does not exist. The gastric lavage is effective only within an hour after administration of drug.
Storage conditions:
In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 3 years. Not to apply after the termination of a period of validity.
Issue conditions:
Without recipe
Packaging:
On 10 tablets in a blister strip packaging, in packaging No. 10 x 3, No. 10 x 5.
