Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbspsustained-release capsules
    Composition:

    1 capsule contains:

    active substance: ketoprofen 200 mg;

    Excipients: Macrogol 4000, ethylcellulose, stearic acid, ammonium methacrylate copolymer, talc, neutral granules (sugar and corn starch [3: 1]);

    capsule shell: gelatin, titanium dioxide.

    Description:

    Hard gelatin capsules No. 1, containing white or almost white pellets.

    The capsule case is transparent, the lid is white or white with a creamy shade of color.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)
    ATX: & nbsp

    M.02.A.A.10   Ketoprofen

    Pharmacodynamics:

    Ketoprofen is a non-steroidal anti-inflammatory drug from the group of propionic acid derivatives.

    It has the following properties:

    - has analgesic effect;

    - has antipyretic effect;

    - exhibits anti-inflammatory action;

    - inhibits the aggregation of platelets.

    All of the above properties are a consequence of the reduction of prostaglandin synthesis, by a non-selective inhibition of cyclooxygenase 1 and type 2 activity.

    Pharmacokinetics:

    Capsules BYSTRUMKPS 200 mg contain granules with controlled release of active substance, which are intended for reception once a day.

    The release of ketoprofen from the granules occurs gradually in the intestinal tract.

    Suction. After oral administration, ketoprofen almost completely absorbed from the intestinal tract, has the effect of "first passage" through the liver. The maximum concentration in the blood plasma is achieved 6-8 hours after oral administration of a dose of 200 mg. Do not cum in the body. Food does not affect the overall bioavailability of ketoprofen.

    Distribution. Ketoprofen binds to plasma proteins by 99%. Ketoprofen penetrates into the synovial fluid, where it reaches a higher concentration than in the plasma.

    In a small amount, it penetrates the placental barrier.

    Metabolism. Biotransformation of ketoprofen proceeds in two main ways: by hydroxylation, as well as compounds with glucuronic acid; the latter is the main pathway of metabolism.

    Less than 1% of the received dose of ketoprofen is found unchanged in urine, the rest are metabolites, of which 65-75% are metabolites of glucuronic acid.

    Excretion. It is excreted by the kidneys. The half-life (T1/2) is about 8 hours.Within 5 days after taking 70-90% of the dose is excreted in the urine and 1-8% with feces.

    In elderly people, the elimination of ketoprofen decreases, and T1/2 increases, and in persons with impaired renal function T1/2 increases depending on the degree of impaired renal function.

    Indications:

    Diseases of the musculoskeletal system and pain syndrome of different genesis:

    - symptomatic treatment of inflammatory-degenerative diseases of the musculoskeletal system (bursitis, synovitis, capsulitis, tendinitis, periarthritis);

    - articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis), is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected;

    - Pain in the lower back and spine (neuralgia, myalgia, sciatica, lumbago);

    - Post-traumatic pains (uncomplicated injuries, in particular sports, damage to ligaments and tendons, bruises);

    - Postoperative pain;

    - pain with dysmenorrhea.

    Contraindications:

    - Hypersensitivity to ketoprofen or to any component of the drug (including other NSAIDs);

    - bronchial asthma, rhinitis or urticaria in history caused by ketoprofen, acetylsalicylic acid or other NSAIDs;

    - stomach ulcer and duodenal ulcer (exacerbation);

    - ulcerative colitis (exacerbation);

    - Crohn's disease;

    - diverticulitis;

    - peptic ulcer;

    - hemophilia and other disorders of blood clotting;

    - active gastrointestinal, cerebrovascular and other bleeding (or suspicion of bleeding);

    - severe renal failure (creatinine clearance less than 30 ml / min);

    - progressive kidney disease;

    - severe hepatic impairment or active liver disease;

    - condition after aortocoronary bypass surgery;

    - confirmed hyperkalemia;

    - inflammatory bowel disease;

    - children's age till 15 years;

    - pregnancy (III trimester), the period of lactation.

    Carefully:

    Anemia, bronchial asthma, alcoholism, smoking, alcoholic cirrhosis, hyperbilirubinemia, hepatic failure, dehydration, sepsis, chronic heart failure, edema, hypertension, blood diseases (including leukopenia), stomatitis, coronary heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, creatinine clearance less than 60 mL / min, ulcerative lesions of the gastrointestinal tract (GIT) in history, presence of infection Helicobacter pylori, long-term use of NSAIDs, severe somatic diseases, simultaneous administration of oral glucocorticosteroids (including SCP) (including prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective serotonin reuptake inhibitors (including number, citalopram, fluoxetine, paroxetine, sertraline), advanced age, pregnancy (I, II trimester).

    Dosing and Administration:

    Orally.

    Adults and teens over 15 years of age: one capsule 200 mg once a day with meals.

    Side effects:

    From the digestive system: NSAIDs-gastropathy, heartburn, nausea, vomiting, diarrhea, constipation, flatulence, decreased appetite, stomatitis, abdominal pain and epigastric region; rarely - a change in taste. With prolonged use in large doses - ulceration of the mucous membrane of the gastrointestinal tract, gingival, hemorrhoidal bleeding, intestinal perforation.

    From the urinary system: rarely - cystitis, urethritis, renal dysfunction, acute renal failure, interstitial nephritis, nephrotic syndrome, hematuria, edema (especially in patients with arterial hypertension).

    From the side of the liver: changes in transaminase activity may be noted; rarely - hepatitis.

    From the nervous system: agitation, nervousness, drowsiness, depression, asthenia, headache, dizziness, sleep disturbance, insomnia, tinnitus; rarely - confusion or loss of consciousness, forgetfulness, migraine, peripheral neuropathy.

    From the side of the cardiovascular system: heart failure, increased blood pressure; rarely - tachycardia.

    Hypersensitivity reactions: rhinitis, angioedema, anaphylactic shock, rash, itching, urticaria, asthmatic attack, especially in patients with hypersensitivity to acetylsalicylic acid, as well as to other drugs from the NSAID group.

    Skin reactions: photosensitivity, alopecia, polymorphic erythema, multi-form exudative erythema, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

    On the part of the organs of hematopoiesis: anemia, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia; rarely - hemolytic anemia.

    From the sense organs: reversible toxic amblyopia,unclear vision or double vision; rarely - conjunctivitis, dry eye mucosa, eye pain, conjunctival hyperemia, decreased hearing.

    Other: increased sweating; rarely - hemoptysis, epistaxis, myalgia, muscle twitching, shortness of breath, thirst, with prolonged use in large doses - vaginal bleeding.

    If any side effects occur, stop taking the medication immediately.

    Overdose:

    When an overdose of ketoprofen may appear symptoms acute poisoning, such as: headache, dizziness, drowsiness, nausea, vomiting, diarrhea, epigastric pain, lowering of blood pressure, bronchospasm, bleeding from the digestive tract.

    In case of suspected overdose, you should immediately contact your doctor.

    Treatment for overdose: immediate discontinuation of the drug. If an overdose of the drug has passed no more than 1 hour, gastric lavage with activated charcoal in a dose of 60-100 g in adults, 1-2 g / kg of body weight in children. Symptomatic treatment.

    Interaction:

    Avoid simultaneous use with:

    - other NSAIDs (including salicylates in high doses), oral anticoagulants, heparin, ticlopidine - increases the risk of bleeding. If ketoprofen is needed, careful monitoring of the patient's condition should be carried out;

    - Lithium - the risk of increasing the toxic level of lithium in plasma. If necessary, during simultaneous use of lithium and ketoprofen preparations, and also after its termination, careful monitoring of lithium concentration in plasma should be made;

    - methotrexate (at a dose of more than 15 mg / week) - increases the risk of hematotoxicity. Intervals before and after taking methotrexate should be at least 12 hours from taking ketoprofen.

    Strengthens the effect of anticoagulants, antiaggregants, fibrinolytics, ethanol, side effects of GCS and ISS, estrogens.

    Increases the concentration in the plasma of verapamil and nifedipine.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Reduces the hypotensive effect of beta-blockers.

    Increases the risk of nephrotoxic effect of beta-blockers.

    Increases the risk of nephrotoxic effects of cyclosporine and tacrolimus, especially in elderly patients.

    Reduces the contraceptive effectiveness of intrauterine spirals.

    Increases the risk of bleeding with thrombolytics.

    Care must be taken when using with:

    - diuretics and inhibitors of angiotensin-converting enzyme - weakening of diuretic and hypotensive effects and the risk of developing renal failure, in patients with circulating blood volume deficiency;

    - pentoxifylline - increased risk of bleeding;

    - zidovudine - increases the risk of anemia (affects reticulocytes with the development of anemia).

    As with other NSAIDs, it is possible:

    - decrease in the effectiveness of uricosuric medicines;

    - increased risk of ulceration and development of gastrointestinal hemorrhages and development of renal dysfunction in joint admission with GCS, ethanol, corticotropin;

    - increased risk of bleeding with concomitant administration with cefoperazone, cefamandole and cefotetan;

    - increased hypoglycemic action of insulin and oral hypoglycemic drugs (dose recalculation is necessary);

    - increase in the production of hydroxylated active metabolites by inducers of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants);

    - disturbance of platelet aggregation when co-administered with sodium valproate;

    - antacids and colestramine reduce absorption.

    Special instructions:

    During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys.

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

    Reception of ketoprofen can mask signs of an infectious disease.

    If the kidney and liver function is impaired, a dose reduction and careful monitoring is necessary.

    To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as short a course as possible.

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

    During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:

    Capsules of prolonged action 200 mg.

    Packaging:

    For 10 capsules in a blister of PVC and aluminum foil.

    2 blisters together with instructions for use in a cardboard box.

    Storage conditions:

    In a dry, the dark place at a temperature of 15 ° C to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-007920/09
    Date of registration:06.10.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:Medan Pharma, Joint Stock CompanyMedan Pharma, Joint Stock Company Poland
    Manufacturer: & nbsp
    Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia
    Information update date: & nbsp14.03.2017
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