Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspThe tablets of the prolonged action covered with a cover.
    Composition:
    Active substance
    Diclofenac sodium 0.100 g
    (Henan Dongtai Farm Co..
    Ltd., China)
    Excipients
    Hypromellose (Methocel K4M) 0.05 g
    (USP / NF, EP)
    Cellulose 0.09 g
    microcrystalline
    (NF, EP, JP)
    Magnesium stearate 0.0075 grams
    (EP, USP, JP)
    Silicon dioxide
    colloidal 0.0025 grams
    (EP, USP / NF, JP)

    Weight of a tablet
    without shell 0.250 g

    Sheath Opadrai II yellow
    (manufacturer specification):
    Talc
    (USP, FCC, EP, JP) 0.00104 g
    Titanium dioxide 0.00121 g
    (USP, FCC, EP, JP)
    Macrogall 3350 (NF, EP) 0.00141 g

    Polyvinyl alcohol 0.00280 grams
    (USP, FCC, EP, JPE)

    Quinoline dye
    yellow aluminum lacquer
    (USP / NF, FDA) 0.00054 g

    Shell weight 0,0070 g

    Weight of the tablet with a coating of 0.2570 g
    Description:Round biconvex tablets, coated with a yellow coating.
    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 type 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:
    Absorption - fast and complete, food slows the absorption rate by 1 -2 hours and reduces the maximum concentration by 2 times. In the case of taking the drug with food, the maximum concentrations are observed on average 5-6 hours.

    Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted, do not accumulate.

    Bioavailability - 50%. The connection with plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into the synovial fluid; The maximum concentration in the synovial fluid is observed 2-4 hours later than in the plasma. The half-time of elimination from the synovial fluid is 3-6 hours (the concentration of active substance in the synovial fluid 4-6 hours after the administration of the drug is higher than in the plasma, and remains higher for another 12 hours).The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug has not been elucidated.

    Metabolism: 50% of the active substance is metabolized during the "first pass" through the liver. 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:
    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, tendovaginitis, bursitis).

    Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache.

    In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).
    Contraindications:Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, "aspirin" asthma, hematopoiesis disorders, hemostasis disorders (incl. hemophilia), pregnancy, children's age (under 18 years), lactation.
    Carefully:Anemia, bronchial asthma, congestive heart failure, hypertension,edematous syndrome, liver or kidney failure, alcoholism, inflammatory bowel disease, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes, a condition after major surgery, induced porphyria, old age, diverticular disease, systemic connective tissue diseases.
    Dosing and Administration:Inside, not liquid, squeezed a little water, usually during or after a meal. 1 tablet once a day.
    Side effects:

    Gastrointestinal tract:

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

    less than 1% - vomiting, jaundice, melena, blood in stool, esophageal lesion, aphthous stomatitis, dryness of the mouth and the mucous membranes, hepatitis (possibly fulminant), hepatic necrosis, cirrhosis, hepatorenal syndrome, appetite change, pancreatitis, holetsistopankreatit, colitis .

    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, 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:

    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,deterioration of the course of infectious processes (development of necrotizing fasciitis).

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

    Overdose:
    Symptoms: vomiting, dizziness, headache, dyspnea, confusion, in children - myoclonic cramps, nausea, abdominal pain, bleeding, impaired liver and kidney function.
    Treatment: gastric lavage, administration of activated charcoal, 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 NSAIDs 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.
    Special instructions:
    During the treatment with the drug should be a systematic control of the picture of peripheral blood, liver function, kidneys, examination of feces for the presence of blood.

    Patients taking the drug should refrain from activities that require increased concentration of attention and rapid mental and motor reactions, alcohol consumption.
    Form release / dosage:
    The tablets of the prolonged action covered with a cover, 100 mg.
    Packaging:
    For 10 tablets in a planar cell packaging made of polyvinyl chloride film and aluminum foil printed lacquered.

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

    Packing for hospitals.

    100, 200, 300, 400 or 500 contour-cell packs with instructions for use are placed in cardboard boxes.

    For 500, 1000 or 2000 tablets are packed in polymer cans with lids made of polymer materials. For 1, 2, 3, 4, 5 or 6 cans with instructions for use are put in boxes of cardboard.

    Storage conditions:In dry, the dark place at a temperature of no higher than 25 "C. Keep out of reach of children.
    Shelf life:
    3 years. Do not take the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:P N004025 / 01
    Date of registration:26.01.2010
    The owner of the registration certificate:ZIO-HEALTH, JSC ZIO-HEALTH, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp19.02.2016
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