Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbsp
    rectal suppositories
    Composition:

    1 suppository contains:

    active substance: ketoprofen 100 mg;

    Excipients: semi-synthetic solid glycerides 1850 mg, silicon dioxide colloid 50 mg.

    Description:

    Torpedo-shaped uniform from white to creamy white suppository, greasy to the touch.

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

    M.02.A.A.10   Ketoprofen

    Pharmacodynamics:

    FLEKSEN provides anti-inflammatory, analgesic and antipyretic, antiaggregatory actions. Suppresses the activity of cyclooxygenases 1 and 2, regulating the synthesis of prostaglandins. The analgesic effect is due to both the central and peripheral mechanisms. It has anti-bradykinin activity, stabilizes lysosomal membranes.

    Pharmacokinetics:

    When rectal administration is absorbed quickly, bioavailability is up to 90%. It binds to blood plasma proteins by 99%. Time to reach the maximum concentration in blood plasma - 0,5-2 hours.The therapeutic concentration in the synovial fluid is maintained for 6-8 hours.

    Metabolized in the liver by glucuronation.

    It is excreted mainly by the kidneys and 1% by the intestine. The half-life is 1.6-1.9 hours.

    Do not cumulate.

    Indications:

    Symptomatic treatment of acute pain syndrome in inflammatory processes of various origins: osteoarthritis, ankylosing spondylitis, gouty arthritis (in case of an acute gout attack quick-acting dosage forms are preferred), rheumatoid arthritis, psoriatic arthritis; bursitis, tendosinovitis; ishialgia, myalgia, neuralgia, dorsalgia, radiculitis; bruises and stretching of the muscles; adnexitis, otitis media; headache and toothache; pain syndrome in cancer; post-traumatic and postoperative pain syndrome; algodismenorea.

    Contraindications:

    - Individual hypersensitivity to ketoprofen, acetylsalicylic acid or other NSAIDs (including anamnesis for bronchospasm, urticaria, or rhinitis caused by acetylsalicylic acid);

    - Diseases of the gastrointestinal tract in the acute phase;

    - gastrointestinal bleeding and perforation in the anamnesis;

    - pronounced impairment of kidney and liver function;

    - Violations from the blood (leukopenia, thrombocytopenia, hemocoagulation disorders, hemophilia);

    - hemorrhoids and / or proctitis;

    - relief of pain syndrome immediately before or immediately after surgical treatment of the cardiovascular system;

    - severe heart failure;

    - Pregnancy and lactation;

    - Children's age (up to 18 years).

    Carefully:

    It should be used with caution in patients: with violations of the liver and / or kidney function, gastrointestinal diseases in history; bronchial asthma, rhinitis, urticaria, polyps of the nasal mucosa; hypertension and / or with cardiovascular diseases, cerebrovascular diseases; blood diseases, anemia; alcoholism, alcoholic cirrhosis of the liver, hyperbilirubinemia, diabetes, dehydration, smoking, sepsis and in elderly patients.

    Dosing and Administration:

    Suppositories are injected deep into the rectum.

    Adults appoint 1 suppository, 100 mg 1-2 times a day.

    The maximum daily dose of the drug should not exceed 300 mg.

    Side effects:

    From the digestive system: NSAIDs-gastropathy, abdominal pain, dyspepsia (nausea, vomiting, heartburn, flatulence, decreased appetite, diarrhea), stomatitis; change in taste, ulceration and perforation of the gastrointestinal mucosa, gingival, gastrointestinal, hemorrhoidal bleeding; increased activity of "hepatic" transaminases in the blood serum, hepatitis.

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

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

    From the cardiovascular system: increased blood pressure, tachycardia.

    From the hematopoiesis: rarely - agranulocytosis, anemia, hemolytic anemia, thrombocytopenia, leukopenia.

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

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

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

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

    Other: increased sweating, myalgia, muscle twitching, thirst, vaginal bleeding.

    The use of suppositories may cause local disorders, burning sensation, tenesmus and loose stools, irritation of mucous membranes.

    Overdose:

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

    Treatment symptomatic: there is no specific antidote. 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.

    Joint reception 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,

    thrombolytics, antiplatelet agents, cefoperazone, cefamandole and cefotetan increase 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, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites.

    Co-administration with sodium valproate causes disruption of platelet aggregation.

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

    Antacids and colestramine reduce absorption.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Special instructions:

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

    Care should be taken when prescribing the drug to patients with gastrointestinal ulcer diseases in history, renal and hepatic insufficiency. During treatment, it is necessary to monitor the picture of peripheral blood and the functional state of the liver and kidneys. If the kidney and liver function is impaired (increased ALT activity is an indicator of NSAID-induced liver dysfunction), a dose reduction and careful follow-up of the doctor are necessary.

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

    Avoid taking alcohol.

    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 should be taken when driving vehicles and practicing other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:

    Suppositories rectal 100 mg.

    Packaging:

    6 suppositories per contour polyvinyl chloride / polyethylene packaging.

    2 contour polyvinyl chloride / polyethylene packaging units together with instructions for use in a cardboard bundle.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    The drug should not be used after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011313 / 02
    Date of registration:27.11.2007
    The owner of the registration certificate:Italfarmaco SpAItalfarmaco SpA Italy
    Manufacturer: & nbsp
    Representation: & nbspITALFARMAKO SpA ITALFARMAKO SpA Italy
    Information update date: & nbsp11.09.2012
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