Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbspRAsterol for intravenous and intramuscular administration
    Composition:

    Per 1 ml of the preparation:

    active substance: ketoprofen - 50 mg;

    Excipients: propylene glycol 400 mg, ethanol 96% - 100 mg, benzyl alcohol - 20 mg, sodium hydroxide - to adjust the pH 7.0 ± 0.5, water for injection - up to 1 ml.

    Description:

    A clear, colorless or light yellow solution.

    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. Due to the inhibition of cyclooxygenases 1 and 2 and, in part, lipoxygenase, ketoprofen suppresses the synthesis of prostaglandins and bradykinin, stabilizes the lysosomal membranes.

    Ketoprofen does not adversely affect compound state cartilage.
    Pharmacokinetics:

    Suction

    Ketoprofen is easily absorbed from the gastrointestinal tract when ingested. After oral administration of ketoprofen capsules prolonged action 200 mg maximum concentrations in blood plasma CmOh from 3.1 to 3.4 ± 1.2 mg / l are achieved within 5 hours.

    Bioavailability of the drug is 90%. Eating does not affect the overall bioavailability of ketoprofen, but decreases the rate of absorption.

    Distribution

    Ketoprofen is 99% bound to blood plasma proteins, mainly with the albumin fraction. The volume of distribution is 0.1 l / kg. Ketoprofen penetrates into the synovial fluid and reaches there a concentration equal to 50% of the concentration in the blood plasma. Plasma clearance of ketoprofen is approximately 0.08 l / kg / h. Effective concentrations of ketoprofen are determined in the blood even after 24 hours after its administration.

    Metabolism and excretion

    Ketoprofen undergoes intensive metabolism under the action of microsomal liver enzymes, the half-life is less than 2 hours. Ketoprofen binds to glucuronic acid and is excreted from the body in the form of glucuronide. There are no active metabolites of ketoprofen. Up to 80% of ketoprofen is excreted by the kidneys within 24 hours, mainly in the form of ketoprofen glucuronide. In patients with severe renal insufficiency, most of the drug is secreted through the intestine. When taking high doses, the liver clearance also increases. Through the intestines, up to 40% preparation.

    In patients with hepatic insufficiency the plasma concentration of ketoprofen is doubled (probably due to hypoalbuminemia, and as a result of this high the level of unbound active ketoprofen), such patients need to prescribe the drug in the minimum therapeutic dose.

    In patients with renal insufficiency clearance of ketoprofen is reduced, but correction of doses is required only in the case of severe renal failure.

    In elderly patients metabolism and excretion of ketoprofen proceed more slowly, which is of clinical importance only for patients with severe renal insufficiency.

    Indications:

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

    Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, seronegative arthritis (ankylosing spondylitis - Bechterew's disease, psoriatic arthritis, reactive arthritis (Reiter's syndrome)), gout, pseudogout, osteoarthritis.

    Pain syndrome: tendonitis, bursitis, myalgia, neuralgia, sciatica; headache; post-traumatic and postoperative pain syndrome; pain syndrome in cancer; algodismenorea.

    Contraindications:

    - Hypersensitivity to ketoprofen or other components of the drug, as well as salicylates or other NSAIDs;

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

    - erosive and ulcerative lesions of the gastrointestinal tract and duodenum;

    - inflammatory bowel disease (ulcerative colitis (exacerbation), Crohn's disease (exacerbation));

    - hemophilia and other bleeding disorders;

    - Decompensated heart failure;

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

    - renal failure of severe degree (creatinine clearance less than 30 ml / min), progressive kidney disease;

    - hepatic insufficiency of severe degree (10-15 points on the Child-Pugh scale) or active liver disease;

    - condition after aortocoronary bypass surgery;

    - confirmed hyperkalemia;

    - children's age (up to 18 years);

    - chronic dyspepsia;

    - pregnancy III trimester;

    - the period of breastfeeding.

    Carefully:

    Anemia, bronchial asthma, alcoholism, tobacco smoking, alcoholic liver cirrhosis, hyperbilirubinemia, liver failure, dehydration, sepsis, chronic heart failure (CHF), edema, arterial hypertension, blood diseases (including leukopenia), stomatitis, ischemic heart disease (IHD), cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, chronic renal failure (CRF) (KK 30-60 ml / min), ulcerative lesions of the gastrointestinal tract (gastrointestinal tract) in an ana Veronese, the presence of infection Helicobacter pylori, long-term use of NSAIDs, severe somatic diseases, simultaneous use of oral glucocorticosteroid agents (including Prednisolone), anticoagulants (including warfarin), antiaggregants (including clopidogrel), selective inhibitors of re-uptake serotonin (including citalopram, fluoxetine, paroxetine, sertraline), elderly age.

    Pregnancy and lactation:

    Ketoprofen is contraindicated in III trimgestation of pregnancy. AT I and II trimesters of pregnancy, the use of Ketoprofen is possible in cases where the potential benefit to the mother exceeds the potential risk to the fetus, to be used only under the supervision of a physician.

    If it is necessary to use Ketoprofen during lactation, breastfeeding should be discontinued.

    Dosing and Administration:

    Intravenous, intramuscular.

    Intramuscular administration: on 100 mg (1 ampoule) 1-2 times a day.

    Intravenous infusion introduction ketoprofen should be administered only in a hospital setting.

    Short intravenous infusion: 100-200 mg (1-2 ampoules) of ketoprofen diluted in 100 ml of a 0.9% solution of sodium chloride is injected for 0.5-1 hours; it is possible to re-introduce after 8 hours.

    Continuous intravenous infusion: 100-200 mg (1-2 ampoules) of ketoprofen diluted in 500 ml of an infusion solution (0.9% sodium chloride solution, lactate-containing Ringer's solution, 5% dextrose solution) is introduced for 8 hours; it is possible to re-introduce after 8 hours.

    Ketoprofen can be combined with analgesics of central action; it can be mixed with opioids (for example, morphine) in one bottle, it is impossible to mix in one bottle with tramadol because of precipitation.

    Parenteral administration of the drug can be combined with the use of oral forms (tablets, capsules) or rectal suppositories.

    Duration of therapy 48 hours (2 days).

    The maximum dose of ketoprofen is 200 mg / day.

    Side effects:

    According to the World Health Organization (WHO), undesirable effects are classified according to their frequency of development as follows: very often (≥1/10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, < 1/100), rarely (≥1 / 10000, <1/1000), very rarely (<10000) the frequency is unknown (the frequency of occurrence of phenomena can not be determined from the available data).

    On the part of the hematopoiesis and lymphatic system:

    Rarely: hemorrhagic anemia, leukopenia;

    Frequency unknown: agranulocytosis, thrombocytopenia, impaired bone marrow function.

    From the immune system:

    Frequency unknown: anaphylactic reactions (including anaphylactic shock).

    From the nervous system:

    Infrequently: headache, dizziness, drowsiness;

    Rarely: paresthesia;

    Frequency unknown: convulsions, a violation of taste.

    From the sense organs:

    Rarely: blurred vision, tinnitus.

    From the side of the cardiovascular system:

    Frequency unknown: heart failure, hypertension, vasodilation.

    From the respiratory system:

    Rarely: asthma, nosebleeds, laryngeal edema;

    Frequency unknown: bronchospasm (in particular, in patients with hypersensitivity to NSAIDs), rhinitis.

    From the gastrointestinal tract:

    Often: nausea, vomiting, indigestion, pain in the abdomen;

    Infrequently: constipation, diarrhea, bloating, gastritis;

    Rarely: peptic ulcer, stomatitis;

    Rarely: exacerbation of ulcerative colitis or Crohn's disease, gastrointestinal bleeding, perforation.

    From the liver and biliary tract:

    Rarely: hepatitis, an increase in the level of "hepatic" enzymes and bilirubin.

    From the skin:

    Infrequently: skin rash, itchy skin;

    Frequency unknown: photosensitization, alopecia, urticaria, angioedema, erythema, bullous rash, toxic epidermal necrolysis.

    From the urinary system:

    Rarely: acute renal failure, interstitial nephritis, nephrotic syndrome, abnormal values ​​of renal function indicators.

    Other:

    Infrequently: swelling, fatigue;

    Rarely: increase in body weight.

    Overdose:

    In case of an overdose of ketoprofen, nausea, vomiting,pain in the abdomen, vomiting with blood, impaired consciousness, respiratory depression, convulsions, impaired renal function and renal failure.

    In case of overdosage, gastric lavage and the use of activated charcoal are indicated. Treatment is symptomatic; the effect of ketoprofen on the gastrointestinal tract can be weakened with the help of proton pump inhibitors and prostaglandins. In case of development of renal failure, hemodialysis is recommended.

    Interaction:

    Ketoprofen can weaken the action diuretics and antihypertensive drugs and strengthen action oral hypoglycemic and some anticonvulsants (phenytoin).

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

    Simultaneous appointment with anticoagulants (heparin, warfarin), thrombolytics, antiaggregants (ticlopidine, clopidogrel) increases the risk of bleeding.

    Simultaneous application with potassium-sparing diuretics, ACE inhibitors, NSAIDs, low molecular weight heparins, cyclosporine,tacrolimus and trimethoprim increases the risk of hyperkalemia.

    Increases the concentration in the blood plasma cardiac glycosides, slow calcium channel blockers, lithium preparations, cyclosporine, methotrexate and digoxin.

    Increases toxicity methotrexate and nephrotoxicity cyclosporine.

    Simultaneous use with probenecid significantly reduces the clearance of ketoprofen in the blood plasma.

    Combination with glucocorticoids and other NSAIDs (including selective inhibitors COX2) increases the likelihood of side effects (in particular, from the gastrointestinal tract).

    Nonsteroidal anti-inflammatory drugs can reduce the effectiveness of mifepristone. The intake of NSAIDs should be started no earlier than 8-12 days after the withdrawal of mifepristone.

    Special instructions:

    With prolonged use of NSAIDs, it is necessary to periodically evaluate the clinical analysis of the blood, and also monitor the liver and kidney function, especially in elderly patients (over 65 years old), to conduct a feces occult blood test.

    Care must be taken to control blood pressure more often when using ketoprofen for treatmentpatients with arterial hypertension, cardiovascular diseases, which lead to fluid retention in the body.

    If abnormalities occur on the part of the visual organs, treatment should be stopped immediately.

    Like other NSAIDs, ketoprofen can mask the symptoms of infectious and inflammatory diseases. In case of signs of infection or deterioration of well-being on the background of the use of the drug, you should immediately consult a doctor.

    If there is a history of contraindications from the gastrointestinal tract (bleeding, perforation, peptic ulcer disease), prolonged therapy and high doses of ketoprofen, the patient should be carefully monitored by the doctor.

    Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised in prescribing ketoprofen to patients with cardiac or renal insufficiency, and also in the treatment of elderly patients taking diuretics and patients who, for whatever reason, blood (for example, after surgery).

    The use of ketoprofen can affect women's fertility, so patients with infertility (including undergoing examination) are not recommended to use the drug.

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

    During the treatment with ketoprofen, the speed of mental and motor reactions may be reduced, so it is necessary to refrain from driving and doing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:

    Solution for intravenous and intramuscular injection, 50 mg / ml.

    Packaging:2 ml of solution in a dark glass ampoule I type; 5 or 10 ampoules per blister; 1 blister together with instructions for use are placed in a cardboard box.
    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 of the year.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003686
    Date of registration:16.06.2016
    Expiration Date:16.06.2021
    The owner of the registration certificate:VetProm ADVetProm AD Bulgaria
    Manufacturer: & nbsp
    VETPROM, AD Bulgaria
    Representation: & nbspVETPROM ADVETPROM ADBulgaria
    Information update date: & nbsp05.01.2018
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