Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspenteric coated tablets
    Composition:

    1 tablet contains:

    Active substance: diclofenac sodium (diclofenac) - 25.0 mg.

    Excipients: lactose monohydrate - 58.4 mg, sucrose - 6.2 mg, potato starch - 4.6 mg, povidone (low molecular weight polyvinylpyrrolidone, plasdon K-17) 4.8 mg, calcium stearate 1.0 mg.

    Shell accessories: acetylphthalylcellulose - 3,051 mg, titanium dioxide - 0,657 mg, castor oil - 0,576 mg, vaseline oil - 0,616 mg, tropeolin 0 - 0,100 mg.

    Description:
    Tablets, covered with enteric-coated shell, orange-yellow or orange, round, biconvex. Two layers are visible on the cross-section.
    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, antiplatelet and antipyretic effect. 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:
    Absorption - Fast and complete, the food slows the absorption rate by 1-4 hours and reduces the maximum concentration by 40%. After oral administration, 25 mg maximum concentration (Cmax) - 1.0 μg / ml is achieved after 2 to 3 hours. The concentration in the plasma is linear depending on the amount of the administered dose.
    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 for 2-4 hours later than in the plasma. The half-life of the synovial fluid is 3-6 hours (the concentration of the 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 systemic 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 insufficiency (creatinine clearance less than 10 ml / min) increases the excretion of metabolites with bile, and there is no increase in their concentration in the blood.
    In patients with chronic hepatitis or compensated cirrhosis of the liver 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). Feverish syndrome.
    Contraindications:Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, bronchial asthma, urticaria or acute rhinitis triggered by the use of acetylsalicylic acid or other NSAIDs ; severe renal / hepatic and congestive heart failure; disorders of hematopoiesis, hemostasis disorders (incl.hemophilia); hereditary intolerance to galactose, impaired absorption of glucose-galactose, severe lactose deficiency; pregnancy, children's age (up to 6 years), lactation.
    Carefully:Anemia, asthma, congestive heart failure, arterial hypertension, edema 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, elderly age, diverticulitis, systemic connective tissue diseases, simultaneous administration of glucocorticosteroids, anticoagulants, antiaggregants, selective inhibition serotonin reuptake inhibitors.
    Dosing and Administration:Inside, not liquid, during and after meals, with a small amount of water. Adults and adolescents from 15 years - 25-50 mg 2-3 times a day. When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 50 mg / day. The maximum daily dose is 150 mg.For children (over 6 years of age) a daily dose of up to 2 mg / kg of body weight, divided into 2-3 doses. With juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg body weight.

    The approximate mode of application is shown in the table:

    Age (body weight, kg)

    Single dose (number of tablets, [mg])

    Daily dose (number of tablets, [mg])

    6-7 lay down (20-24)

    1[25]

    1[25]

    8-11 years old (25-37)

    1[25]

    2-3[50-75]

    12-14 years old (38-50)

    1-2[25-50]

    3-4[75-100]

    Older than 15 and adults

    1-2[25-50]

    2-6[50-150]

    Side effects:

    From the gastrointestinal tract:

    more often 1% - abdominal pain, sensation of bloating, diarrhea, nausea, constipation, flatulence, increased level of "liver" enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding; vomiting, jaundice, melena, the appearance of blood in the stool, the defeat of the esophagus, aphthous stomatitis, dryness of the mucous membranes (including the mouth), hepatitis (possibly lightning), liver necrosis, cirrhosis, hepatorenal syndrome, changes in appetite - Anorexia, pancreatitis, cholecystopancreatitis, colitis;

    very rarely - glossitis, diaphragm-like intestinal textures (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease).

    From the central 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, general weakness, disorientation, nightmares, fear;

    very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremors, anxiety, cerebrovascular disorders, mental disorders.

    From the cardiovascular system:

    less than 1% - increased blood pressure; congestive heart failure,

    extrasystole, chest pain;

    very rarely - palpitations, myocardial infarction.

    From the hemopoietic system 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 (including the development of necrotizing fasciitis).

    From the respiratory system:

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

    From the urinary system:

    more often 1% - fluid retention;

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

    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 often 1% - alopecia, urticaria, eczema, toxic dermatitis, multi-form exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, small-spot hemorrhages.

    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 nephrotic diclofenac effects.

    Reduces the effect of hypoglycemic agents.

    Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increases the frequency 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 actions of drugs that cause photosensitivity. Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

    Selective serotonin reuptake inhibitors increase the risk of bleeding from the gastrointestinal tract.

    Antibacterial drugs from the quinolone group - the risk of seizures.
    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.
    Effect on the ability to drive transp. cf. and fur:Patients taking the drug should refrain from activities that require increased attention and rapid mental and motor reactions, alcohol consumption.
    Form release / dosage:Tablets coated with enteric coating 25 mg.
    Packaging:For 10 or 15 tablets in a contour mesh package. 2, 3, 4, 5, 6 contour cell packs of 10 tablets or 2, 3, 4 contour packs of 15 tablets together with instructions for use are placed in a pack of cardboard.
    Storage conditions:In the dark place at a temperature of no higher than 25 ° C.
    Shelf life:
    3 years. Do not use after the time specified on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-002352/08
    Date of registration:02.04.2008 / 10.01.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.06.2017
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