Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSolution for intramuscular injection.
    Composition:
    1 ml of the solution contains:

    Active Ingredient: diclofenac sodium - 25 mg

    Auxiliary ingredients: mannitol 6 mg, sodium sulfite 3 mg, benzyl alcohol 0.04 mg, propylene glycol 0.1 mg, hydrochloric acid concentrated to pH 8.5, water for injection up to 1 ml.
    Description:Transparent solution from colorless to colorless with a yellowish hue.
    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 and inflammatory swelling.
    Pharmacokinetics:
    Time to reach the maximum concentration with intramuscular application at a dose of 75 mg - 15-30 minutes, the maximum concentration

    - 1.9 - 4.8 (mean 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, osteoarthritis 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 to the active substance or ancillary components;

    - Anamnestic data on an attack of bronchial obstruction, rhinitis, hives after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);

    - Erosive-ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal hemorrhage;

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

    - Severe hepatic impairment or active liver disease;

    - Severe renal insufficiency (creatinine clearance less than 30 ml / min), progressive kidney disease, incl. confirmed hyperkalemia.

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

    - Violation of hemostasis (including hemophilia);

    - Period after aortocoronary bypass surgery;

    - III trimester of pregnancy, the period of breastfeeding;

    - Decompensated heart failure.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, heart failure (in the compensation stage), arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, condition after extensive surgical interventions, induced porphyria, advanced age, diverticulitis, systemic connective tissue diseases, creatinine clearance less than 60 ml / min.
    Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illnesses.
    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).
    Diseases of the liver in the anamnesis, a significant decrease in the volume of circulating blood. Pregnancy I-II trimester.
    Pregnancy and lactation:
    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.

    From the digestive system:

    more than 1% - abdominal pain, feeling bloated, indigestion, diarrhea, nausea, constipation, flatulence, increased levels of "liver" enzymes, peptic ulcer with possible complications;

    less than 1% - dry mouth and mucous membranes, changes in appetite, gastritis, glossitis, esophageal damage, aphthous stomatitis, vomiting, jaundice, proctitis, digestive disorders, non-specific haemorrhagic colitis, gastro-intestinal bleeding, exacerbation of ulcerative colitis or

    Crohn's disease, hepatitis (fulminant possible), hepatic necrosis, cirrhosis, hepatorenal syndrome, pancreatitis, holetsistopankreatit, colitis.

    From the nervous system:

    more often 1% - headache, dizziness;

    less than 1% - insomnia, drowsiness, depression, irritability, aseptic meningitis (usually in patients with systemic lupus erythematosus and other connective tissue diseases), cramps, weakness, disorientation, nightmares, feeling of fear; very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremor, cerebrovascular disorders, insomnia, mental disorders.

    From the sense organs:

    more often 1% - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disorders;

    From the 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's syndrome), increased photosensitivity melkotochechnye hemorrhage;

    very rare - bullous rash, exfoliative dermatitis.

    From the genitourinary system:

    more often 1% - fluid retention;

    less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

    From the organs of hematopoiesis and the immune system:

    less than 1% - anemia (including haemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of infectious processes (development of necrotizing fasciitis, pneumonia).

    From the respiratory system:

    less than 1% - cough, bronchospasm, laryngeal edema, pneumonitis, bronchial

    asthma (including dyspnea).

    From the cardiovascular system:

    less than 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain; very rarely - palpitations, vasculitis, myocardial infarction.

    Allergic reactions:

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

    Other:

    more often 1% - irritation at the injection site; very rarely - an abscess at the injection site.

    Overdose:Symptoms: vomiting, dizziness, headache, shortness of breath, blurred vision, diarrhea, tinnitus, 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. Decreasing 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.

    Antibacterial drugs from the quinolone group - the risk of seizures.

    Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.
    Special instructions:
    Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful in the appointment of diclofenac in patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, a decrease in blood volume is observed (for example, after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

    In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism do not differ from similar processes in patients with normal liver function. When performing long-term therapy, it is necessary to monitor liver function, the picture of peripheral blood, the analysis of feces for latent blood. During the treatment period, the speed of mental and motor reactions may decrease.

    In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended.
    Form release / dosage:Solution for intramuscular injection 25 mg / ml.
    Packaging:For 3 ml of the drug in a vial of colorless glass. 5 ampoules are placed in a plastic outline package. 1 or 2 plastic contour packs with instructions for use - put in a cardboard box. 10 1 ampoules are placed in a plastic outline package. 1 plastic outline packaging with instructions for use is placed in a cardboard box. 5 ampoules are placed in an AL / PVC blister. 1 AL / PVC blister with instructions for use are placed in a cardboard box.
    Storage conditions:
    List B. Store in a dry, protected from light place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.
    Shelf life:
    3 years.

    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013706 / 02
    Date of registration:11.12.2008
    The owner of the registration certificate:Agio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspAgio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd.
    Information update date: & nbsp26.02.2016
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