Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbsprectal suppositories
    Composition:

    1 suppository contains:

    active substance: ketoprofen 100 mg;

    Excipients: solid fat (Vitessol H-15) 1850 mg, glyceryl caprylcaprate (Miglyol 812) 200 mg.

    Description:Suppositories white or almost white, torpedo-shaped.
    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 with anti-inflammatory, analgesic and antipyretic effects. Suppresses the activity of cyclooxygenases I and II, regulating the synthesis of prostaglandins. The analgesic effect is due to both central and peripheral mechanisms. It has anti-bradykinin activity, stabilizes lysosomal membranes, and delays the release of enzymes that promote tissue destruction in chronic inflammation.

    Pharmacokinetics:

    Ketoprofen is well absorbed from the gastrointestinal tract, bioavailability is 90%. Connection with blood plasma proteins - 99%. Time to reach the maximum concentration (TCmOh) with rectal administration - 1.4-4 h.

    Ketoprofen penetrates into the synovial fluid and reaches therapeutic concentrations there. The therapeutic concentration in the synovial fluid is maintained for 6-8 hours.

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

    Up to 80% of ketoprofen is excreted by the kidneys, and approximately 10% by the intestine. In connection with rapid metabolism, the half-life (T1/2) is less than 2 hours.

    In elderly patients, metabolism and elimination of ketoprofen is slower, but this is clinically important only for patients with impaired renal function.

    Indications:

    Symptomatic therapy of painful and inflammatory processes of various origin, including:

    - inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic arthritis, Bechterew's disease (ankylosing spondylitis), gouty arthritis (in case of an acute gout attack quick-acting dosage forms are preferred), osteoarthritis;

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

    - algodismenorea.

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

    Contraindications:

    - Hypersensitivity to ketoprofen or other components of the drug;

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in history);

    - peptic ulcer of the stomach and duodenum in the phase of exacerbation;

    - ulcerative colitis (exacerbation), Crohn's disease in the phase of exacerbation;

    - peptic ulcer;

    - hemophilia and other bleeding disorders;

    - confirmed hyperkalemia;

    - severe hepatic impairment;

    - active liver disease;

    - severe renal failure (creatinine clearance <30 mL / min);

    - progressive kidney disease;

    - Decompensated heart failure;

    - Postoperative period after coronary artery bypass grafting;

    - chronic dyspepsia;

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

    - inflammatory bowel disease, including proctitis, diverticulitis;

    - children's age till 15 years;

    - pregnancy (III trimester) and the period of breastfeeding.

    Carefully:

    Anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic liver cirrhosis, hyperbilirubinemia, chronic hepatic insufficiency, chronic renal failure (creatinine clearance 30-60 ml / min), ulcerative lesions of the gastrointestinal tract in an anamnesis, inflammatory bowel diseases (including ulcerative colitis, Crohn's disease) without exacerbation, the presence of infection Helicobacter pylori, severe somatic diseases, diabetes mellitus, peripheral arterial diseases, dehydration, sepsis, chronic heart failure, coronary heart disease, edema, arterial hypertension, blood diseases (including leukopenia), stomatitis, cerebrovascular diseases, dyslipidemia / hyperlipidemia, prolonged use of NSAIDs , simultaneous administration of oral glucocorticosteroids (including prednisolone),anticoagulants (including warfarin), antiplatelet agents (including clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), advanced age, pregnancy (I, II trimester).

    In case of deterioration of the patient should stop treatment with the drug.

    Pregnancy and lactation:The use of Ketoprofen in the III trimester of pregnancy is contraindicated. In the first and second trimesters of pregnancy, the prescription of the drug is only possible in cases where the intended use for the mother exceeds the potential risk to the fetus.

    When taking the drug in the period of breastfeeding, you should decide whether to stop breastfeeding.

    Dosing and Administration:

    Rectally.

    Suppositories are injected deep into the rectum. Patients assigned to 1 suppository 100 mg 1-2 times a day. The maximum daily dose of the drug Ketoprofen should not exceed 200 mg.

    Side effects:

    From the digestive system: NSAIDs-gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, decreased appetite, diarrhea), stomatitis, impaired liver function, change in taste.

    With prolonged use in large doses - ulceration of the mucous membrane of the gastrointestinal tract, gingival, gastrointestinal, hemorrhoidal bleeding.

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

    From the sense organs: noise or ringing in the ears, blurred vision, conjunctivitis, congestion hyperemia, dry eye, eye pain, hearing loss, vertigo.

    From the side of the cardiovascular system: increased blood pressure, tachycardia.

    On the part of the organs of hematopoiesis: agranulocytosis, anemia, hemolytic anemia, leukopenia, thrombocytopenia.

    On the part of the respiratory system: dyspnea, bronchospasm, rhinitis, laryngeal edema, epistaxis, hemoptysis, dyspnea.

    From the urinary system: edematous syndrome, cystitis, urethritis, renal dysfunction, interstitial nephritis, nephrotic syndrome, hematuria.

    From the skin: alopecia, eczema, multi-form exudative erythema, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), photodermatitis.

    Allergic reactions: skin rash, including erythematous, urticaria, itching, angioedema, exfoliative dermatitis, anaphylactic shock.

    Other: increased sweating, myalgia, muscle twitching, thirst, with prolonged use in large doses - vaginal bleeding.

    Overdose:

    Symptoms: there may be drowsiness, nausea, vomiting, abdominal pain, bleeding, liver and kidney dysfunction.

    Treatment: symptomatic therapy. In case of accidental ingestion, gastric lavage and / or Activated carbon and / or other sorbents.

    Interaction:

    Reduces the effectiveness of uricosuric medicines, enhances the effect of anticoagulants, antiaggregants, fibrinolytics, ethanol, side effects of glucocorticosteroids and mineralocorticosteroids, estrogens; reduces the effectiveness of antihypertensive drugs and diuretics.

    Ketoprofen is pharmaceutically incompatible with tramadol solution.

    Antacids and colestramine reduce absorption.

    Joint administration with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, an increased risk of kidney dysfunction. Simultaneous administration with oral anticoagulants, heparin, antiaggregants, thrombolytic agents, cefoperazone, cefamandol and cefotetan increases the risk of bleeding.

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

    Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, phenylbutazone, rifampicin, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

    Co-administration with valproic acid causes disruption of platelet aggregation.

    Increases the concentration in the plasma of verapamil and nifedipine, lithium preparations, methotrexate.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

    During treatment with a drug Ketoprofen it is necessary to control the picture of peripheral blood and the functional state of the liver and kidneys. If the kidney and liver function is impaired, a dose reduction and careful monitoring is necessary.

    Care should be taken when prescribing the drug to patients with ulcerative gastrointestinal diseases in the anamnesis.

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

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

    With the simultaneous use of ketoprofen and warfarin, as well as coumarin anticoagulants or lithium salts, patients should be under strict medical supervision.

    Drug administration Ketoprofen can mask the signs of an infectious disease.

    With the development of violations from the eyes, consultation of the ophthalmologist is necessary.

    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,requiring increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Suppositories rectal 100 mg.

    Packaging:For 5 or 6 suppositories in the outline of a polyvinylchloride laminated polyethylene film, two contour squares, together with instructions for use, are placed in a pack of cardboard.
    Storage conditions:AT protected from light 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 expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002765
    Date of registration:17.12.2014 / 17.10.2016
    Expiration Date:17.12.2019
    The owner of the registration certificate:FARMPROJECT, CJSC FARMPROJECT, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspFARM PROJECT CJSC FARM PROJECT CJSC Russia
    Information update date: & nbsp05.01.2018
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