Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsp
    Solution for intramuscular injection.

    Composition:
    active substance: diclofenac sodium - 25 mg / ml

    auxiliary substances: propylene glycol, mannitol (manitol), benzyl alcohol, sodium metabisulphite (sodium disulfite), sodium hydroxide (1M sodium hydroxide solution), water for injection.

    Description:
    Transparent or slightly opalescent, slightly colored liquid with a faint smell of benzine 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 promotes a significant reduction in 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 and 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 compensated cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.
    Indications:
    For short-term treatment of pain of different genesis, 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 other NSAIDs or ancillary components), erosive and ulcerative lesions of the gastrointestinal tract (in the exacerbation phase), bleeding from the gastrointestinal tract, inflammatory bowel disease, severe hepatic insufficiency, liver disease in the acute period ,expressed renal insufficiency (creatinine clearance less than 30 ml / min), hyperkalemia, complete or incomplete acetylsalicylic acid intolerance syndrome (rhinosinusitis, urticaria, nasal mucosa polyps, bronchial asthma arising from the intake of acetylsalicylic acid or other NSAIDs), hematopoiesis disorders ( including hemophilia), pregnancy, children's age (under 18 years), lactation period, period after aortocoronary bypass surgery.
    Carefully:Coronary heart disease, cerebrovascular diseases, congestive heart failure, arterial hypertension, edematous syndrome, peripheral arterial disease, dyslipidemia, diabetes mellitus, anemia, bronchial asthma, renal failure (creatinine clearance less than 60 ml / min), alcoholism, erosive-ulcerative diseases gastrointestinal intestinal tract without exacerbation, diverticulitis, condition after extensive surgical interventions, induced porphyria, elderly age, smoking, severe somatic diseases, syst mnye connective tissue disease, long-term use of nonsteroidal anti-inflammatory drugs.
    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, further pass to oral, or rectal administration of diclofenac.
    Side effects:

    To reduce the risk of developing adverse events, use a minimally effective dose with a short course.

    Gastrointestinal tract:

    more often 1% - abdominal pain, sensation of bloating, diarrhea, digestive disorders, nausea, constipation, flatulence, increased level of "liver" enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;

    less often% vomiting, jaundice, melena, the appearance of blood in the stool, esophagus damage, aphthous stomatitis, dry mouth and mucous membranes, hepatitis (possibly fulminant), liver necrosis, cirrhosis, hepatorenal syndrome, appetite change, pancreatitis, cholecystopancreatitis, colitis.

    Nervous system:

    more often 1% - headache, dizziness;

    less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic

    meningitis (usually in patients with systemic lupus erythematosus and other systemic

    connective tissue diseases), convulsions, weakness, disorientation, nightmares

    dreams, a sense of fear.

    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 covers.

    more often 1% - skin itch, skin rash;

    less than 1% - alopecia, urticaria, eczema, toxic dermatitis, multiforme exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's 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, pneumonitis.

    The cardiovascular system:

    less than 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain.

    Allergic reactions:

    less often% - 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, dizziness, headache, dyspnea, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

    Treatment: symptomatic therapy, forced diuresis. Hemodialysis is ineffective.
    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; on the background of anticoagulants, 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 glucocorticosteroid agents (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 preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract.

    Diclofenac 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.
    Special instructions:Patients using the drug should refrain from activities that require increased attention and rapid mental and motor reactions, alcohol consumption.
    Form release / dosage:solution for intramuscular injection 25 mg / ml.
    Packaging:3 ml into ampoules of neutral glass. 10 ampoules per box of cardboard with corrugated paper inserts. The box contains instructions for medical use, ampoule knife or scarifier (when packing ampoules with notches, rings and dots of knives and scarifiers do not invest).
    Storage conditions:List B. In a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C.
    Shelf life:2 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000086
    Date of registration:31.05.2007
    The owner of the registration certificate:PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC PHARMSTANDART-UFIM VITAMIN FACTORY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp10.03.2016
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