Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbspmodified release tablets
    Composition:

    1 modified release tablet contains:

    active substance: ketoprofen 150 mg;

    Excipients: hypromellose (hydroxypropylmethylcellulose 15000), calcium hydrophosphate dihydrate, silicon dioxide colloid (aerosil), magnesium stearate.

    Description:

    Tablets are white, round, biconvex. Insignificant surface roughness is allowed.

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

    M.02.A.A.10   Ketoprofen

    Pharmacodynamics:

    Nonsteroidal anti-inflammatory drug, has anti-inflammatory, analgesic and antipyretic effects associated with inhibition of cyclooxygenases 1 and 2, regulating the synthesis of prostaglandins and bradykinin; stabilizes the lysosomal membranes.

    It does not adversely affect the condition of the articular cartilage.

    Pharmacokinetics:

    Absorption - fast, bioavailability - more than 90%. The connection with plasma proteins is 99%.The minimum effective concentration is determined after 45-60 minutes. When oral ketoprofen tablets are taken with a modified action, the maximum concentration of the drug in the plasma is reached after 4-6 hours. The therapeutic concentration in the synovial fluid is maintained for 6-8 hours. In significant amounts it does not penetrate the blood-brain barrier.

    Virtually completely metabolized in the liver by glucuronation, has the effect of "first passage" through the liver.

    It is excreted by the kidneys (mainly in the form of ketoprofen glucuronide) and intestine (1%). The half-life is 1.6-1.9 hours. It does not accumulate.

    Indications:

    Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic arthritis, Bechterew's disease (ankylosing spondylitis), gouty arthritis, osteoarthritis.

    The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

    Pain syndrome: myalgia, ossalgia, neuralgia, tendonitis, arthralgia, bursitis, sciatica, adnexitis, otitis media, headache and toothache, with oncological diseases; post-traumatic and postoperative pain syndrome, accompanied by inflammation, algodismenorea.

    Contraindications:

    Hypersensitivity to ketoprofen and other components of the drug, as well as to other non-steroidal anti-inflammatory drugs.

    Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including anamnesis).

    Stomach ulcer and / or duodenal ulcer (stage of exacerbation), ulcerative colitis (stage of exacerbation), Crohn's disease; hemophilia and other disorders of blood clotting; confirmed hyperkalemia; diverticulitis, peptic ulcer, active gastrointestinal bleeding, inflammatory bowel disease; decompensated heart failure, period after aortocoronary bypass surgery; severe hepatic impairment or active liver disease; severe renal failure (QC less than 30 ml / min), progressive kidney disease; children's age (up to 15 years); pregnancy (III trimester), the period of breastfeeding.

    Carefully:

    Anemia, bronchial asthma, ischemic heart disease, cerebrovascular disease and peripheral arterial disease,chronic heart failure, peptic ulcer disease, dyslipidemia / hyperlipidemia, hepatic insufficiency, hyperbilirubinemia, alcoholic liver cirrhosis, renal failure (CC less than 60 ml / min), arterial hypertension, edema, blood diseases (including leukopenia), stomatitis , dehydration, sepsis, diabetes mellitus, anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of infection Helicobacter pylori, tobacco smoking, alcoholism, concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, sertraline), prolonged use of NSAIDs, severe somatic diseases, advanced age, pregnancy (I, II trimester), the period of lactation.

    Pregnancy and lactation:

    In the third trimester of pregnancy, the use of ketoprofen is contraindicated.

    In the first and second trimesters of pregnancy, the prescription of the drug is only possible if the intended benefit to the mother exceeds the potential risk to the fetus.

    During the lactation period, when taking the drug, it is necessary to resolve the issue of stopping breastfeeding.

    Dosing and Administration:

    Inside, during or after a meal, 1 tablet (150 mg) 1 time per day. Tablets should be swallowed whole, without chewing, washed down with a large amount (at least 100 ml) of water or milk.

    A minimum effective dose should be used with the minimum possible short course.

    Side effects:

    From the digestive system: often - dyspepsia (nausea, diarrhea or constipation, flatulence, vomiting, heartburn, decreased appetite,) NSAID-gastropathy, abdominal pain, stomatitis, impaired liver function; rarely - perforation of the organs of the gastrointestinal tract, exacerbation of Crohn's disease, melena, gingival, gastrointestinal, hemorrhoidal bleeding.

    From the central nervous system: often - headache, dizziness, insomnia, drowsiness, fatigue, agitation, nervousness, depression, asthenia; rarely - confusion or loss of consciousness, forgetfulness, migraine, peripheral neuropathy; very rarely - hallucinations, disorientation and speech disorder.

    From the sense organs: rarely - noise or ringing in the ears, blurry vision, taste change, conjunctivitis, hearing loss, dry eye mucosa, eye pain, conjunctival hyperemia, vertigo.

    On the part of the CAS: rarely - tachycardia, arterial hypertension, peripheral edema.

    On the part of the organs of hematopoiesis: ketoprofen reduces platelet aggregation, transient increase in the level of liver enzymes, rarely - agranulocytosis, anemia, thrombocytopenia, purpura, hemolytic anemia, and leukopenia.

    From the urinary system: rarely - renal dysfunction, cystitis, urethritis, interstitial nephritis, nephrotic syndrome, hematuria (often develop in people taking NSAIDs and diuretics for a long time).

    Allergic reactions: often - skin reactions (itching, urticaria); rarely - rhinitis, dyspnea, bronchospasm, angioedema, anaphylactoid reactions, exfoliative dermatitis.

    Other: increased sweating, rarely - hemoptysis, epistaxis, menometrorrhagia, muscle twitching, thirst, photosensitization.
    Overdose:

    When an overdose of ketoprofen, as well as other non-steroidal anti-inflammatory drugs,nausea, vomiting, vomiting with blood, abdominal pain, melena, impaired consciousness, respiratory depression, convulsions, impaired renal function and renal insufficiency may occur.

    There is no specific antidote. Treatment is symptomatic. The effect of ketoprofen on the gastrointestinal tract can be weakened with the help of antagonists H2-receptors, proton pump inhibitors and prostaglandins. It shows gastric lavage and the use of activated charcoal.

    Interaction:

    Ketoprofen can weaken the action of diuretics and antihypertensives and increase the effect of oral hypoglycemic and some anticonvulsants (phenytoin).

    Joint reception with other NSAIDs, glucocorticosteroids, salicylates, ethanol, corticotropin increases the risk of developing adverse events from the gastrointestinal tract.

    Simultaneous administration with anticoagulants, thrombolytic agents, antiaggregants, as well as with cefoperazone, cefamandol, cefotetan and moxalactam increases the risk of bleeding.

    With the simultaneous administration of non-steroidal anti-inflammatory drugs with diuretics and ACE inhibitors, the risk of renal dysfunction increases.

    Increases the concentration in the plasma of cardiac glycosides, blockers of slow calcium channels, lithium preparations, cyclosporine, methotrexate. Non-steroidal anti-inflammatory drugs can reduce the effectiveness of mifepristone. Reception of NSAIDs should be started no earlier than 8-12 days after withdrawal mifepristone.

    Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites. Co-administration with sodium valproate causes disruption of platelet aggregation.

    Increases hypoglycemic effect of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    Ketoprofen can be drunk with milk or taken with antacids to reduce the incidence of gastrointestinal disorders; antacids and milk do not affect the absorption of the drug.

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

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

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

    Taking the drug may mask signs of an infectious disease. Do not use the drug simultaneously with other NSAIDs.

    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:

    Modified release tablets, 150 mg.

    Packaging:

    For 20 tablets in a bottle of dark glass, ukuporenny lid.

    1 bottle with instructions for use in a pack of cardboard.

    Storage conditions:

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

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008051/08
    Date of registration:10.10.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOKOM, CJSC BIOKOM, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp05.01.2018
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