Main physical and chemical characteristics: light blue color, round, oboyevypukly tablets, film coated;
Structure. 1 tablet contains 100 mg of ketoprofen;
other components: magnesium stearate, silicon dioxide colloid anhydrous, povidone, starch corn, talc, lactoses monohydrate, hydroxypropyl cellulose, polyethyleneglycol 400, dye blue E 132 indigotin, titan dioxide, wax of karnaubskiya.
Form of release of medicine. Tablets, film coated.
Farmakoterapevtichesky group. Nonsteroid anti-inflammatory and antirheumatic drugs. Code of automatic telephone exchange M01A E03.
Effect of the medicine. Pharmacodynamics. Ketoprofen is non-steroidal anti-inflammatory drug which has analgeziruyushchy, antiinflammatory and febrifugal action.
At an inflammation ketoprofen inhibits synthesis of prostaglandins and leukotrienes, braking activity of cyclooxygenase and partially – lipoxygenases, also it inhibits synthesis of bradikinin and stabilizes lizosomalny membranes.
Renders analgesic effect and eliminates manifestations of symptoms of inflammatory and degenerative diseases of a musculoskeletal system.
Pharmacokinetics. Absorption. After oral administration it is quickly soaked up in a digestive tract. After reception of a dose of 100 mg the maximum concentration of ketoprofen in a blood plasma (10, 4 mkg/ml) is formed approximately in 1, 5 hours. Bioavailability of ketoprofen in tablets makes 90% and in direct ratio to a dose, applied.
Distribution. Extent of linkng with proteins – 99%. Volume distribution – 0, 1 - 0, 2 l/kg. Ketoprofen gets into synovial fluid. Stable concentration of ketoprofen in a blood plasma is reached within 24 hours after reception of peroral forms. The ketoprofen pharmacokinetics significantly does not differ depending on age of patients. Cumulation of ketoprofen in fabrics is not observed.
Metabolism and removal. Ketoprofen is intensively metabolized in a liver by means of reaction of a microsomal oxidation. Out of an organism it is brought in the form of a conjugate with glucuronic acid. The elimination half-life makes 2 hours. To 80% of the entered dose of ketoprofen about 10% – with excrements are brought with urine, as a rule (more than 90%) in the form of a glucuronide.
Patients with a renal failure have a ketoprofen removal in a slowed-up way, the elimination half-life increases for an hour. At patients with a liver failure ketoprofen can collect in fabrics. Patients of advanced age have a metabolism and removal of ketoprofen are slowed down, however it has clinical value only at a renal failure.
extra articulate rheumatism (tendinitis, bursitis, shoulder capsulitis);
pain syndrome (posttraumatic pains; postoperative pains; pains at metastasises of tumors);
Way of use and dose.
Doses are selected individually, depending on a condition of the patient and his reaction to treatments.
The usual daily dose of ketoprofen makes 100 – 300 mg.
The maximum daily dose of ketoprofen makes 300 mg.
The ketocash is accepted forte on 1 tablet by 2–3 times for days.
Pill is taken during food, washing down with water or milk (not less than 100 ml).
For prevention of negative effect of ketoprofen on mucous membranes of bodies of a digestive tract it is possible to accept antiacid means at the same time.
Side effect. The dispepsichesky phenomena, nausea, a meteorism, pain in an abdominal cavity, diarrhea, a lock, digestion disturbances, loss of appetite, vomiting, stomatitis are most often observed.
The headache, dizziness, drowsiness, depression, sleeplessness, nervousness is seldom noted.
Abnormal liver function and kidneys, vision disorders and a sonitus were very seldom noted.
At less than 1% of patients gastritis, the emptying of black color, bleeding from a rectum hidden blood in Calais, perforation of stomach ulcer, gastrointestinal breaks, a hematemesis were observed.
Frequency of development of stomach ulcer in patients is defined by risk factors which include to become, age, smoking, alcohol intake, a stress, a concomitant use of such drugs as acetylsalicylic acid, corticosteroids, and also a dose of ketoprofen and duration of its reception.
Ketoprofen can worsen the course of hypertensia and increase risk of development of peripheral hypostases.
The enanthesis and other reactions of hypersensitivity, such as an acute anaphylaxis, a bronchospasm, an attack of bronchial asthma were seldom noted.
Contraindications. Hypersensitivity to ketoprofen or excipients, salicylates and other non-steroidal anti-inflammatory drugs;
digestive tract erosive cankers in an aggravation stage;
chronic dyspepsia in the anamnesis;
heavy abnormal liver functions and/or kidneys;
tendency to bleedings;
asthmatic attacks and rhinitis in the anamnesis after use of non-steroidal anti-inflammatory drugs;
pregnancy (III trimester) and chest feedings;
children till 14 flyings.
Overdose. At overdose of ketoprofen there can be nausea, vomiting, pain in epigastriums, is very rare – a hematemesis, emptying of black color, disturbance of consciousness, braking of breath, a spasm, a renal failure, an abnormal liver function and a renal failure.
At overdose the gastric lavage and reception of absorbent carbon is recommended. Treatment - symptomatic; antagonists histamine H2 receptors, inhibitors of the proton pump, prostaglandins apply.
Features of use. It is necessary to apply with care to treatment of patients with digestive tract diseases, disturbances of turning of blood, patients with hemophilia, Villibrand's diseases, thrombocytopenia, with a renal and liver failure, and also at co-administration of peroral anticoagulants and heparin, especially low-molecular.
As well as all other non-steroidal anti-inflammatory drugs, ketoprofen can mask symptoms and symptoms of infectious diseases.
It is necessary to adhere to care at purpose of ketoprofen to patients with hypertensia and cardiovascular diseases of which the liquid delay in an organism is characteristic. It is regularly necessary to control arterial pressure in all patients who accept ketoprofen, especially at patients with cardiovascular diseases.
At prolonged treatment by ketoprofen, especially patients of advanced age, it is necessary to control a blood count, and also functions of a liver and kidneys. At clearance of creatinine it is lower than 0, 33 ml / with (20 ml/minutes) it is necessary to modify a ketoprofen dose.
Laboratory analyses. Ketoprofen reduces aggregation of thrombocytes and increases a bleeding time. In 15% of patients indicators of functional hepatic tests raise. Sometimes (less than at 1% of patients) substantial increase of ALT or nuclear heating plant is noted.
Use during the periods of pregnancy and a lactation. Appointment in the third trimester of pregnancy is contraindicated, in the first and to another trimesters use of drug is possible only in this case when the potential advantage justifies possible risk of negative action on a fruit.
Purpose of non-steroidal anti-inflammatory drugs in the third trimester of pregnancy can cause premature closing of Botalova channels and pulmonary hypertensia at newborns, and also late childbirth.
Chest feedings need to be stopped for treatment by ketoprofen.
Influence on psychophysical abilities. Seldom nonsteroid antirheumatic means can cause dizziness, drowsiness. At these symptoms it is not necessary to steer the car or to work with mechanisms, work with which demands exact mental reactions.
Ketonal's interaction with other medicines. Ketoprofen can reduce effect of diuretics and anti-hypertensive drugs, increases efficiency of peroral gipoglikemiziruyushchy drugs – sulfanylurea derivatives, and also some antiunconscious means (Phenytoinum). Simultaneous use of ketoprofen and diuretics or inhibitors of an angiotenzinkonvertaza increases risk a renal failure.
Due to the increase of risk of bleeding at a concomitant use of ketoprofen and peroral anticoagulants or corticosteroids the patient has to is under constant medical control.
At a concomitant use of ketoprofen and cardiac glycosides, drugs of lithium, cyclosporine and a methotrexate their toxicity increases owing to decrease in excretion.
Ketoprofen can reduce effect of mifepristone therefore between a course of treatment mifepristone and the beginning of therapy by ketoprofen there have to pass not less than 8 days.
It is not necessary to appoint ketoprofen along with other non-steroidal anti-inflammatory drugs and salicylates.
Conditions and periods of storage. To store at a temperature not above 25 °C in the place, unavailable to children.
Period of validity – 5 years.
Not to use drug after the termination of a period of validity.