international and chemical name: ketoprofen; 3 - benzoyl - alpha metilbenzoluksusnaya acid or in the form of lizinovy salt of ketoprofen-D, the L-lysine, 2-(3-benzoilfenit) propionate;
Main physical and chemical characteristics: the capsule has a transparent body and a blue cover; capsule contents – white and yellow spherical granules;
Structure. 1 capsule includes ketoprofen 150 mg;
other components: kernel of a spherical granule: cellulose microcrystallic, lactoses monohydrate, povidone, sodium of a kroskarmeloz, polysorbate 80;
cover of a kernel of a spherical granule: eudrazhit RS 30D, yellow (E172), silicon dioxide colloid anhydrous eudrazhit RL 30D, triethyl citrate, polysorbate 80, talc, ferrous oxide.
Form of release of medicine. Solid capsules.
Farmakoterapevtichesky group. Nonsteroid anti-inflammatory and antirheumatic drugs.
Code of automatic telephone exchange M01A E03.
Effect of the medicine. Pharmacodynamics. Ketoprofen inhibits synthesis of prostaglandins and leukotrienes, braking activity of enzyme of cyclooxygenase and thus suppresses synthesis of prostaglandins from arachidonic acid, also it inhibits synthesis of bradikinin and stabilizes lizosomalny membranes.
Absorption. Ketoprofen in the form of capsules Ketonal Duo is well soaked up after oral administration. Ketonal Duo represents a new dosage form which differs from ordinary capsules in way release of active ingredient. Capsules contain two types of pellets: white and yellow. Ketoprofen is released quickly from one type of pellets, and slowly – from another that causes the prolonged effect of drug. Bioavailability of capsules with the modified release makes 90%. Reception of food does not influence the general bioavailability of ketoprofen, but reduces absorption speed. The food is fat increases time of achievement of the maximum concentration, but does not reduce bioavailability and the maximum concentration of ketoprofen in plasma. The concomitant use of antiacid or other drugs that reduce acidity of a gastric juice, does not influence the speed and volume ketoprofen absorption. After oral administration of capsules Ketonal Duo with the modified release the maximum plasma concentration 9036, 64 ng/ml are reached within 1, 76 hour.
Distribution. Ketoprofen in 99% contacts proteins of a blood plasma, mainly albuminous fraction. Volume distribution makes 0, 1 l/kg. Ketoprofen gets into synovial fluid and reaches there concentration which is equal to 30% of plazmovy.
Metabolism and removal. Ketoprofen is subject a metabolism in a liver where it conjugates with glucuronic acid and creates unstable connection ketoprofenglyukuronid which is the reservoir of active ingredient. At patients with a renal failure can happen accumulation of a conjugate in a blood plasma and splitting to release of active ingredient. The konjyugovanny form of ketoprofen is found in healthy adults in a blood plasma only in small quantities. At people of advanced age above contents of a conjugate can be caused by lower values of renal clearance. About 60 - 75% of ketoprofen are removed with urine, mainly in the form of a conjugate with glucuronic acid. Less than 10% are brought in an invariable view with a stake. There are no active metabolites of ketoprofen. The hydroxyl a metabolite is also not active. The plasma clearance of ketoprofen makes about 0, 08 l/kg/h.
Indications for use. Diseases of joints: pseudorheumatism; seronegative spondylarthrites (ankylosing spondylarthritis, psoriartrichny arthritis, reactive arthritis); gout, pseudogout; arthrosis; extra articulate rheumatism (tendinitis, bursitis, capsulitis of a shoulder joint).
Pain syndrome: posttraumatic; algodismenoreya; postoperative; pain at metastasises in a bone of patients with oncological diseases.
Way of use and dose. The standard dose for adults and children is more senior than 15 years 1 capsule of Ketonal Duo (150 mg) a day makes. At incontinuous use the maximum daily dose makes 300 mg – on 1 capsule each 12 hours. Capsules should be accepted with food, swallowing of whole and washing down with a full glass of water. Capsules can also be washed down with milk or to accept together with antiacid drugs for the purpose of decrease in frequency of gastrointestinal disturbances; milk and antiacid drugs do not influence drug adsorption.
Duration of treatment depends on a current and disease severity.
Side effect. Most of people transfer ketoprofen well and do not test side effects. But nausea, gripes and an abdominal pain, locks, diarrhea, appetite loss, a headache, dizziness, drowsiness or a sleep disorder can spoterigatisya; breath disturbance; stethalgia; disturbance of a heart rhythm; rash, small tortoiseshell; photosensitivity; hypostasis of a shin, legs, persons; bleeding or tendency to formation of hematomas is increased; jaundice (yellow coloring of skin and scleras); decrease urination; an acute pain in a stomach, vomiting blood or amount of black color; black bloody sticky kcal; diarrhea of the obscure etiology or pharyngalgia; increase of arterial pressure.
Contraindications. Hypersensitivity to ketoprofen or other components of medicine, salicylic acid, other nonsteroid antirheumatic means; aggravation of a peptic ulcer of a stomach or duodenum; if there was an ulcer a stomach or gastrointestinal bleeding earlier; chronic dyspepsia (discomfort and pain in upper part of a stomach); heavy renal failure; tendency to bleedings; bronchial asthma and rhinitis; pregnancy and lactation; children till 15 years.
Symptoms: nausea, vomiting, abdominal pain, vomiting blood, kcal of black color, dizziness, braking of breath, spasm, disturbance of renal and hepatic function.
Treatment: symptomatic; gastric lavage, reception of absorbent carbon, use of antagonists histamine H2 receptors, inhibitors of the proton pump, prostaglandins.
Features of use. With care patients should appoint from gastrointestinal diseases in the anamnesis. Bleeding and perforation can develop without the previous symptoms at once. The special attention is required by use of drug for patients with disturbance of a hemostasis, hemophilia, an angiohemophilia, heavy thrombocytopenia, a renal and liver failure, and also at patients who accept anticoagulants (coumarin and derivatives of heparin, basically low-molecular heparins).
Also with care people of advanced age, people who abuse alcohol and to smokers should appoint Ketonal Duo. The risk of emergence of side effects is higher at people of advanced age.
As well as all non-steroidal anti-inflammatory drugs, ketoprofen can mask symptoms of infectious diseases.
Patients who are ill on arterial hypertension and with heart diseases, the liquids which are followed by a delay in an organism should appoint ketoprofen with care. At reception of non-steroidal anti-inflammatory drugs monitoring of arterial pressure, especially at patients with cardiovascular diseases is recommended.
Long-term courses of therapy by ketoprofen, as well as other non-steroidal anti-inflammatory drugs, need monitoring of hematologic indicators, indicators of function of a liver and kidneys, especially at patients of advanced age. At levels of clearance of creatinine more than 0, 33 ml/sec. (20 ml/minutes) it is necessary to change a ketoprofen dose. Before carrying out a surgery it is necessary to stop ketoprofen reception.
Laboratory analyses. Ketoprofen reduces aggregation of thrombocytes and increases a bleeding time. Very often (to 15% of patients) at reception of ketoprofen insignificant increase of level of liver enzymes is observed. Significant increase in ALT or nuclear heating plant is observed in less as 1% of patients who accept non-steroidal anti-inflammatory drugs.
Use during pregnancy and a lactation. Safety of use of ketoprofen during pregnancy and feeding by a breast is not revealed. In І - ІІ drug use trimesters perhaps only when the expected advantage for mother exceeds potential risk for a fruit or the child.
Purpose of non-steroidal anti-inflammatory drugs in ІІІ a trimester of pregnancy can cause premature closing botalovy channels and pulmonary hypertensia at newborns, and also late childbirth.
Chest feedings need to be stopped for treatment by ketoprofen.
Influence on psychophysical abilities. In isolated cases at people who have hypersensitivity to non-steroidal anti-inflammatory drugs, possible development dizziness, vertigo and drowsiness. Such patients should not steer the car or work with difficult mechanisms.
Interaction with other medicines. It is not necessary to accept ketoprofen along with other nonsteroid antirheumatic means or salicylates (acetylsalicylic acid). At a concomitant use of ketoprofen with hypotensive drugs and diuretics decrease hypotensive and diuretic actions is possible. Ketoprofen strengthens effect of antiunconscious and antidiabetic drugs. At a concomitant use of diuretics, APF inhibitors and ketoprofen the risk of nephrotoxicity increases. Reception of ketoprofen along with anti-coagulates and corticosteroid hormones increases risk of bleedings. Ketoprofen can reduce excretion of cardiac glycosides, lithium, cyclosporine and a methotrexate and by that to increase their toxicity. The concomitant use of non-steroidal anti-inflammatory drugs reduces effect of mifepristone. It is necessary to accept non-steroidal anti-inflammatory drugs not earlier, as in 8 - 12 days after mifepristone cancellation.
Conditions and periods of storage. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C. A period of validity – 2 years.