Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbsprectal suppositories
    Composition:

    1 suppository contains:

    active substance: ketoprofen 0.1 g;

    bases for suppositories: Distilled monoglycerides, Tween-80 (polysorbate-80), solid fat or Witepsol H-15, Vitessol W-35.

    Description:

    Suppositories white with a yellowish or creamy hue of color, torpedo-shaped.

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

    M.02.A.A.10   Ketoprofen

    Pharmacodynamics:

    Non-steroidal anti-inflammatory drug (NSAID), a derivative of propionic acid. Has anti-inflammatory, analgesic and antipyretic, anti-aggregation 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:

    Absorption - fast, bioavailability - 90%. Up to 99% of absorbed ketoprofen binds to plasma proteins, mainly with albumin. Ketoprofen well penetrates into the synovial fluid and connective tissue.The maximum concentration in the synovial fluid is 30% of the concentration in the serum, and after 4-6 hours after ingestion it exceeds it. Ketoprofen penetrates the blood-brain barrier.

    It is excreted by the kidneys (mainly) and the intestines (1-8%). The half-life of ketoprofen (T1/2) - 1,6-1,9 hours. In the elderly, the elimination half-life increases to 3-5 hours, in patients with renal insufficiency (creatinine clearance 20-60 ml / min) is about 3.5 hours. It does not cumulate.

    Indications:

    Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic arthritis, Bechterew's disease (ankylosing spondylitis), gouty arthritis (in case of an acute attack of gout, 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.

    Contraindications:

    - Hypersensitivity to ketoprofen or to any component of the drug;

    - bronchial asthma in history caused by ketoprofen, other non-steroidal anti-inflammatory drugs or acetylsalicylic acid;

    - recurrent gastric ulcer and duodenal ulcer;

    - peptic ulcer;

    - severe hepatic impairment;

    - severe renal failure;

    - insufficiency of the circulatory system;

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

    - pregnancy and the period of breastfeeding;

    - childhood;

    - hemophilia and other disorders of blood clotting;

    - ulcerative colitis, Crohn's disease, diverticulitis.

    - rectal bleeding, hemorrhoids, trauma or inflammation of the rectum.

    Carefully:

    Anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic liver cirrhosis, hyperbilirubinemia, hepatic and renal (because the drug is mainly excreted by the kidneys), insufficiency, diabetes mellitus, dehydration, sepsis, chronic heart failure, arterial hypertension, coronary heart disease, diseases of the blood (including leucopenia), stomatitis, elderly age.

    Pregnancy and lactation:

    The use of ketoprofen is contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Enter deep into the rectum. 1 suppository in the morning and evening.

    Side effects:

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

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

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

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

    From the skin: skin rash, alopecia and 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, rhinitis, angioedema, exfoliative dermatitis, anaphylactic shock.

    Other: increased sweating, myalgia, muscle twitching, thirst, vaginal bleeding, irritation of the rectal mucosa, pain during defecation.

    Overdose:

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

    Treatment: symptomatic.

    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 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, thrombolytic agents, antiaggregants, 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, 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 or 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 the most sensitive indicator of NSAID-induced liver dysfunction), 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.

    Like the rest of the drugs in this group, it 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 practicing other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Suppositories rectal 100 mg.

    Packaging:

    Suppositories of 5 pieces are placed in a contour mesh package made of a polyvinyl chloride film.

    1, 2 contoured cell packs together with instructions for use are placed 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:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-009317/08
    Date of registration:25.11.2008
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia
    Manufacturer: & nbsp
    Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia
    Information update date: & nbsp14.09.2017
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