Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSolution for intramuscular injection.
    Composition:Composition 1 ml of the drug: active ingredient: diclofenac sodium 25 mg; auxiliary substances: benzyl alcohol - 35.0 mg, sodium disulfite - 0.8 mg, mannitol - 10.0 mg, sodium hydroxide - 0.4 mg, propylene glycol-200.0 mg, water for injection - up to 1 ml.
    Description:Transparent from colorless to slightly yellow color solution with a weak characteristic smell of petrol 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 pronounced analgesic, antipyretic and anti-inflammatory properties. 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, plasma concentrations averaged 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 symptomatic treatment of pain of different genesis of moderate intensity :.

    Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bekhterev's disease); gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of 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 of the gastrointestinal tract (in the phase of exacerbation), bleeding from the digestive tract, inflammatory bowel disease in the phase of exacerbation (ulcerative colitis, Crohn's disease),severe hepatic insufficiency or liver disease in acute period, severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, hyperkalemia; bronhoobstruktsiya, rhinitis, urticaria, provoked by the use of acetylsalicylic acid or other NSAIDs (including in the anamnesis); violation of hematopoiesis, hemostasis disorders (including hemophilia), pregnancy, children's age (under 18 years), lactation period, period after aortocoronary shunting.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular disease, coronary heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal failure, dyslipidemia / hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease, condition after extensive surgery, induced porphyria, elderly age, diverticulitis, systemic connective tissue diseases, creatinine clearance less than 60 ml / min, erosive-ulcer Gastrointestinal diseases without exacerbation.

    Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, prolonged use of NSAIDs, frequent use of alcohol, severe somatic diseases.

    Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticoids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:The injection solution is injected deeply 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:

    Gastrointestinal tract:

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

    less than 1% 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, anorexia, pancreatitis, cholecystopancreatitis, colitis, gastritis, proctitis , a dysfunction of the liver, glossitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease.

    Nervous system:

    more often 1% - headache, dizziness;

    less often 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, impaired sensation, incl. paresthesia, memory disorders, tremors, anxiety, cerebrovascular disorders, mental disorders.

    Sense organs:

    more often 1% - noise in ears;

    less than 1% - blurred vision, diplopia, a taste disorder, reversible or irreversible hearing loss, scotoma.

    Skin:

    more often 1% - skin itching, skin rash;

    less than 1% - Alopecia, hives, eczema, toxic dermatitis, multiforme

    exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal

    necrolysis (Lyell syndrome), increased photosensitivity, small-scale

    hemorrhage.

    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, palpitations, myocardial infarction.

    Allergic reactions:

    less than 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, cramps, shortness of breath, blurred consciousness. With a significant overdose - acute renal failure, hepatotoxic effect.

    Treatment:

    There is no specific antidote. Treatment - symptomatic, aimed at eliminating the increase in blood pressure, violations of kidney function, seizures, irritation of the gastrointestinal tract, respiratory depression.

    Forced diuresis and hemodialysis are ineffective (due to significant binding to 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; 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 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 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.

    Antibacterial drugs from the quinolone group - the risk of seizures.
    Special instructions:With special caution appoint the drug to patients with cardiac or renal insufficiency, as well as elderly people taking diuretics and patients,which for any reason has a decrease in the volume of circulating blood. In these cases, it is recommended to monitor kidney function as a precautionary measure.
    In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism of diclofenac do not differ from those in patients with normal liver function. When performing long-term therapy, it is necessary to monitor the function of the liver, the picture of peripheral blood, the study of feces for the presence of blood.

    In connection with the negative impact on fertility, women who want to become pregnant, diclofenac is not recommended.

    In patients with infertility (including those undergoing examination) it is recommended to cancel the drug.
    Effect on the ability to drive transp. cf. and fur:During the treatment with diclofenac, the speed of mental and motor reactions may be reduced, so it is necessary to refrain from driving vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Solution for intramuscular injection 25 mg / ml.
    Packaging:To 3 ml of the drug in the ampoule of colorless glass I hydrolytic class. The ampoule is painted with a brown paint with a dot and a ring. 5 ampoules in a contour mesh PVC-package with aluminum coating. Contour pack together with instructions for use in a pack of cardboard.
    Storage conditions:
    Store at temperatures between 15 ° C and 25 ° C.

    Keep out of the reach of children!
    Shelf life:
    3 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011648 / 03
    Date of registration:06.11.2009
    The owner of the registration certificate:Hanmi Farm. Co., LtdHanmi Farm. Co., Ltd The Republic of Korea
    Manufacturer: & nbsp
    Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia
    Information update date: & nbsp20.02.2016
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