Active substanceKetoprofenKetoprofen
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  • Dosage form: & nbspsolution for infusion and intramuscular injection
    Composition:

    1 ml of the solution contains:

    active ingredient: ketoprofen 50 mg;

    auxiliary components: propylene glycol 400 mg, ethanol (ethyl alcohol) 95% 100 mg, benzyl alcohol 20 mg, sodium hydroxide to pH 6.5-7.5, water for injection up to 1 ml.

    Description:

    Pcolorless or slightly colored liquid.

    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, a derivative of propionic acid. Has analgesic and antipyretic effect. Severity of anti-inflammatory action - is insignificant. 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 the condition of the articular cartilage.

    Pharmacokinetics:

    ATsating. MThe maximum concentration (Cmah) of the drug in plasma is achieved with intramuscular (IM) administration after 20 minutes (10-45 minutes). Ketoprofen penetrates into the synovial fluid.

    The area under the "active substance concentration-time" (AUC) curve for parenteral administration is proportional to the dose. The connection with plasma proteins is 99%.

    RAllocation. ATThe distribution time is 0.35 h, the volume of distribution is 0.25 l / kg.

    Mmetabolism. MIt is metabolized in the liver by conjugation with hyaluronic acid.

    ATIntroduction. ATIt is mainly metabolized by the kidneys.

    The half-life (T1/2) of the drug from the blood plasma is 1.65 h (1-2.7 h), in the elderly T1/2 lengthened by 48%.

    Indications:

    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 diseases;

    - algodismenorea.

    Contraindications:

    - Hypersensitivity to the active substance or ancillary components;

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses, and intolerance of acetylsalicylic acid and other non-steroidal anti-inflammatory drugs (including in history);

    - erosive-ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding;

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

    - hemophilia and other disorders of blood coagulability; Decompensated heart failure;

    - liver failure;

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

    - period after aortocoronary shunting;

    - pregnancy, lactation period;

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

    Carefully:

    Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min.

    Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract (GIT), the presence of infection Helicobacter pyroli, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe somatic diseases, concomitant therapy with the following drugs:

    - anticoagulants (for example, warfarin);

    - antiaggregants (eg, acetylsalicylic acid, clopidogrel);

    - oral glucocorticosteroids (for example, prednisolone);

    - selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

    Dosing and Administration:

    Intravenously (intravenously) in the form of infusions, intramuscularly.

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

    In / in the infusion of ketoprofen should be carried out only in a hospital.

    For a short-term intravenous infusion, 100-200 mg (1-2 ampoules) of ketoprofen is dissolved in 100 ml of a 0.9% solution of sodium chloride (saline) and injected for 0.5-1 hour; it is possible to re-introduce after 8 h.

    For a continuous IV infusion, 100-200 mg (1-2 ampoules) of ketoprofen is dissolved in 500 ml of the infusion solution (saline solution, Ringer's solution, glucose solution) and injected for 8 hours; After 8 h infusion can be repeated.

    Ketoprofen can be used in combination with central action analgesics. For combined use ketoprofen mixed with morphine and dissolved in physiological saline or Ringer's solution and injected every 8 hours.

    Because of the photosensitivity, the vials with the infusion solution of ketoprofen should be stored wrapped in dark paper or foil.

    In the form of IM injections of 100 mg (1 ampoule) 1-2 times a day. The daily dose should not exceed 200 mg. Injections should be done deeply. Treatment should not exceed 2 days. If necessary, the continuation of therapy goes to taking oral forms or suppositories.

    Side effects:

    The incidence of side effects is characterized as very common (> 10%), common (1-10%), non-common (0.1-1%), rare (0.01-0.1%) and very rare (<0.01%).

    Allergic reactions: common - skin reactions (itching, hives), unrequited - rhinitis, dyspnea, bronchospasm, angioedema, anaphylactoid reactions.

    From the digestive system: common - dyspepsia (nausea, diarrhea or constipation, flatulence, company, decreased or increased appetite), abdominal pain, stomatitis, dry mouth, unrequited (with prolonged use in large doses) - ulceration of the mucosa of the gastrointestinal tract, exacerbation of Crohn's disease, melena, gastrointestinal bleeding.

    From the central nervous system: common - headache, dizziness, drowsiness, fatigue, nervousness, nightmarish dreams, rare - Migraine, peripheral polyneuropathy; very rare - hallucinations, disorientation and speech disorder.

    From the sense organs: rare - noise in the ears, change in taste, blurred vision, conjunctivitis.

    From the side of the cardiovascular system: Undistributed - tachycardia, arterial hypertension, peripheral edema.

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

    Local reactions: in the place of the / m introduction possible burning, in some cases - the formation of infiltrates, abscess, necrosis of adipose tissue.

    Other: rare hemoptysis, menometrorrhagia.

    Laboratory indicators: ketoprofen reduces platelet aggregation, a transient increase in the level of liver enzymes; rare - agranulocytosis, anemia, thrombocytopenia, purpura.

    Overdose:

    In case of an overdose of ketoprofen, nausea, vomiting, abdominal pain, vomiting with blood, melena, impaired consciousness, respiratory depression, convulsions, impaired liver function and renal failure may occur.

    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 antagonists H2 - receptors, proton pump inhibitors and prostaglandins.

    Interaction:

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

    Co-administration with other NSAIDs, glucocorticosteroids, ethanol, corticotropin can lead to the formation of ulcers and the development of gastrointestinal bleeding, an increased risk of developing impaired functions kidney.

    Simultaneous administration with oral anticoagulants, heparin, thrombolytic agents, antiaggregants increases the risk of bleeding. Increases hypoglycemic action of insulin and oral hypoglycemic drugs (dose recalculation is necessary).

    Increases the concentration in the plasma of cardiac glycosides, blockers of slow calcium channels, lithium preparations, cyclosporine, methotrexate.

    To avoid sediment, do not mix in one bottle ketoprofen and tramadol.
    Special instructions:

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

    If there are signs of liver damage (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of urine, increased level of "liver" transaminases), stop taking the drug and consult a doctor. If it is necessary to determine 17-ketosteroids, the drug should be discontinued 48 hours before the test.

    Reception of ketoprofen can mask signs of an infectious disease.

    Do not use ketoprofen concurrently with other NSAIDs.

    Ketoprofen can alter the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

    The use of ketoprofen can adversely affect female fertility and is not recommended for women planning a pregnancy.

    After 2 weeks of using the drug, it is necessary to monitor the indicators of liver function ("transaminase").

    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:

    Solution for infusion and intramuscular injection 50 mg / ml.

    Packaging:

    2 ml into the ampoules of the light-protective glass.

    For 10 ampoules, together with instructions for medical use and a scarifier, the ampullum is placed in a cardboard bundle with cardboard partitions, or 5 or 10 ampoules are placed in a contour cell box made of a polyvinyl chloride film.

    When using ampoules with a notch or a fracture ring, the scarifier is not inserted.

    For 1 or 2 contour squares, together with the instructions for use, are placed in a cardboard box.

    Marking. On the ampoule or label of the ampoule (primary packaging) indicate: trade and international non-proprietary name of the drug, concentration in mg / ml, volume in milliliters, serial number, expiration date.On the package (secondary consumer packaging) indicate: the name of the manufacturer, its trademark, address, telephone, fax, trade and international non-proprietary name of the drug, dosage form, concentration in mg / ml, volume in milliliters, composition, "Sterile", "Store in a place inaccessible to children "," Methods of application are indicated in the instructions for medical use of the drug "," Use as directed by a doctor ", storage conditions, leave conditions, number of ampoules per pack, registration certificate number, bar code, but EP series, the expiration date.

    Storage conditions:

    AT protected from light 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 printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000291
    Date of registration:17.02.2011
    The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp17.02.2011
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