Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSolution for intramuscular injection.
    Composition:
    Active substance: diclofenac sodium - 25 mg / ml

    Excipients: propylene glycol, mannitol (manitol), benzyl alcohol, sodium metabisulphite, sodium hydroxide (sodium hydroxide) 1 M solution, water for injection.
    Description:Transparent lightly colored liquid with a weak smell of benzyl alcohol.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Diclofenac has anti-inflammatory, analgesic and antipyretic effects. Indiscriminately inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. With injuries, in the postoperative period diclofenac reduces pain inflammatory swelling.
    Pharmacokinetics:The time to reach the maximum concentration with intramuscular application at a dose of 75 mg is 15-30 minutes, the maximum concentration is 1.9-4.8 (on average 2.7 μg / ml). After 3 hours after administration, the plasma concentration averages 10% of the maximum.
    The connection with plasma proteins is more than 99% (most of it is associated with albumins). Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The enzyme system P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.

    The system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. Half-life from the plasma -2 hours 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile.

    In patients with severe renal failure (creatinine clearance less than 10 ml / min), the excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood.

    In patients with chronic hepatitis or compressed liver cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.
    Indications:
    For short-term symptomatic treatment of pain of different genesis of moderate intensity:

    - diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of the peripheral joints and spine (including radicular syndrome);

    - lumbago, sciatica, neuralgia;

    - algodismenorea, inflammatory processes of the pelvic organs, incl. adnexitis;

    - post-traumatic pain syndrome, accompanied by inflammation;

    - postoperative pain.
    Contraindications:Hypersensitivity (including to other NSAIDs or ancillary components), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, inflammatory bowel disease in the phase of exacerbation (nonspecific ulcerative colitis, disease Crown),severe hepatic impairment; liver disease or in acute, severe renal impairment (creatinine clearance less than 30 mL / min), progressive kidney disease, hyperkalemia; bronchoobstruction, rhinitis, urticaria provoked by taking aspirin or other NSAIDs (including history).; violations of blood, hemostatic disorders (including hemophilia), pregnancy, children's age (18 years), lactation, period after coronary artery bypass grafting.
    Carefully:
    Anemia, asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, hypertension, peripheral artery disease, edema syndrome, liver or kidney failure, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, condition after major surgery, induced porphyria, advanced age, diverticulitis ^ systemic connective tissue disease, creatinine clearance less than 60 mL / min, erosive lang vascular diseases of the gastrointestinal tract without exacerbation.
    A history of the development of ulcerative diseases of the gastrointestinal tract, the presence of infection Helicobacter pylori, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases.
    Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:It is administered intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours later. Duration of use no more than 2 days, if necessary, then switch to oral, or rectal administration of diclofenac.
    Side effects:
    Gastrointestinal tract:
    more often 1% - abdominal pain, sensation of bloating, diarrhea, digestive disorders, nausea, constipation, flatulence, increased activity of "liver" enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;
    vomiting, jaundice, melena, the appearance of blood in the stool, esophagus damage, aphthous stomatitis, dry mouth and mucous membranes, hepatitis (possibly fulminant course), liver necrosis, cirrhosis, hepatorenal syndrome, anorexia, pancreatitis, cholecystopancreatitis, colitis, gastritis, proctitis, impaired hepatic function, glossitis, diaphragm-like intestinal textures (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease).

    Nervous system:
    more often 1% - headache, dizziness;
    less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, weakness, disorientation, nightmares, feelings of fear, sensitivity disorder, incl. paresthesia, memory disorders, tremors, anxiety, cerebrovascular disorders, mental disorders.

    Sense organs:
    more often 1% - noise in the ears;
    less than 1% - blurred vision, diplopia, a taste disorder, reversible or irreversible hearing loss, scotoma. Skin:
    more often 1% - skin itch, skin rash;
    less than 1% - alopecia, urticaria, eczema, toxic dermatitis, multiform exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome), increased photosensitivity, small-point hemorrhages.

    Genitourinary system:
    more often 1% - fluid retention;
    less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

    Hematopoiesis and the immune system:

    less than 1% - anemia (including hemolytic and aplastic anemia), leukopenia,; thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of the course of infectious processes (development of necrotizing fasciitis,

    pneumonia).

    Respiratory system:
    less than 1% - cough, bronchospasm, laryngeal edema, pneumonia.

    The cardiovascular system:
    less than 1% - increased blood pressure; congestive heart failure, extrasystole and I, chest pain, palpitations, myocardial infarction.

    Allergic reactions:
    less often 1% - anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.

    Local reactions with intramuscular injection:
    burning, infiltration, aseptic necrosis, necrosis of adipose tissue.
    Overdose:
    Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, headache, tinnitus, convulsions, dyspnea, turbidity, with a significant overdose - acute renal failure, hepatotoxic effect.

    Treatment: symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, irritation of the gastrointestinal tract, respiratory depression.

    Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
    Interaction:
    Increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.

    Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; against the background of anti-coagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract). Reduces the effects of hypotensive and hypnotics.

    Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroids (bleeding in the gastrointestinal tract),toxicity of methotrexate and nephrotoxicity) of cyclosporine.

    Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac. Reduces the effect of hypoglycemic agents.

    Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.

    Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.

    Simultaneous administration with ethanol, colchicine, corticotropin, selective serotonin reuptake inhibitors and St. John's wort increases the risk of bleeding in the gastrointestinal tract.

    Dikpofenac enhances the effect of drugs that cause photosensitivity. Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

    Antibacterial drugs from the quinolone group - the risk of developing seizures!
    Special instructions:
    Patients using the drug should refrain from activities,requiring increased attention and rapid mental and motor reactions, alcohol consumption.

    To reduce the risk of developing adverse events from the gastrointestinal tract, a minimally effective dose should be used with the minimum possible short course.
    Form release / dosage:
    Solution for intramuscular injection 25 mg / ml.
    Packaging:
    Solution for intramuscular injection 25 mg / ml in ampoules of 3 ml. For 10 ampoules with instructions for use and a knife ampoule or scarifier for! The need for a pack or box of cardboard.

    For 5 or 10 ampoules in a contour cell package. For 1 or 2 contour squares in a pack of cardboard with instructions for use, a knife or scarifier, ampoule if necessary.
    Storage conditions:In the dark place at a temperature of 18 to 20 ° 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:LSR-003655/09
    Date of registration:15.05.2009
    The owner of the registration certificate:MICROGEN FGUP Scientific and Production Association MICROGEN FGUP Scientific and Production Association Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.02.2016
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