Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspThe tablets are covered with an enteric membrane.
    Composition:

    Active substance: diclofenac sodium - 0.025 g;

    Tablet core aids:

    sugar milk (lactose) - 0.03 g; sugar-sugar (sucrose) - 0.03 g; potato starch, "Extra" variety - 0.0094 g; polyvinylpyrrolidone (povidone) 0.0046 g; stearic acid - 0, 001 g;

    Ingredients of enteric coating:

    tselanecefat - 0.003866 g, titanium dioxide - 0.000387 g, tropeolin dye - 0.000039 g, liquid paraffin - 0.000064 g, castor oil, medical - 0.000644 g.

    Description:The tablets are round biconvex, covered with an enteric-soluble orange-yellow or orange coating; two layers are visible on the cross-section. The color of the core without a shell is white or almost white.
    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, analgesic 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. Like all NSAIDs, the drug has anti-aggregative activity.
    Pharmacokinetics:

    Absorption is fast and complete, food slows the absorption rate by 1 to 4 hours and reduces the maximum concentration of diclofenac in plasma by 40%. After oral administration, 25 mg maximum concentration (CmOh) - 1.0 μg / ml is achieved after - 2-3 hours. The concentration in the plasma is in linear dependence on the amount of the administered dose.

    Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted, diclofenac Do not cumulate.

    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-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 diclofenac concentration in synovial fluid and its clinical efficacy is not clear. Metabolism: 50% of the active substance undergoes metabolism during the "first passage" through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid. In the metabolism of the drug takes part isoenzyme CYP2C9. 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), excretion of metabolites with bile is increased, while increasingtheir concentrations in the blood are not observed.

    In patients with chronic hepatitis or compensated cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.

    Indications:
    Inflammatory and degenerative diseases of the musculoskeletal system, including rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), osteoarthritis, gouty arthritis, bursitis, tenosynovitis. The drug is intended for symptomatic therapy, reducing pain and, inflammation at the time of use, the progression of the disease is not affected.

    Pain syndrome: headache (including migraine) and toothache, lumbago, sciatica, ossalgia, neuralgia; myalgia, arthralgia, radiculitis, with oncological diseases, post-traumatic and postoperative pain syndrome, accompanied by inflammation.

    Algodismenorea; inflammatory processes in the small pelvis, including adnexitis. Infectious and inflammatory diseases of the ENT - organs with severe pain syndrome (in the composition, complex therapy): pharyngitis, tonsillitis, otitis media.
    Contraindications:Hypersensitivity (including other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including those in the anamnesis),erosive and ulcerative lesions of the stomach and duodenum, active gastrointestinal bleeding, inflammatory bowel disease, severe hepatic and heart failure; period after aortocoronary shunting; severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (III trimester), lactation period, children's age (up to 6 years - for tablets coated with enteric membrane 25 mg). Hereditary lactose intolerance, impaired absorption of glucose-galactose, deficiency of lactase.
    Carefully:Stomach ulcer and duodenal ulcer, ulcerative colitis, Crohn's disease, liver disease in history, hepatic porphyria, chronic heart failure (CHF), arterial hypertension, a significant decrease in the volume of circulating blood (BCC) (including after extensive surgical intervention) , elderly patients (including those receiving diuretics, weakened patients and patients with low body weight), bronchial asthma,simultaneous reception of glucocorticosteroids (GCS) (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including ACK, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), coronary heart disease (CHD), cerebrovascular disease; dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, chronic renal failure (CRF) (CK 30-60 ml / min), presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe physical illnesses.
    Pregnancy and lactation:
    In I and II trimester of pregnancy should be used under strict indications and in the smallest dose.

    Diclofenac penetrates into breast milk. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.
    Dosing and Administration:To achieve the desired therapeutic effect rapid take 30 minutes before a meal. In other cases take before, during or after a meal in a nerazzhevannom, squeezed with sufficient water.Adults and adolescents from 15 years - 25-50 mg 2-3 times a day. Upon reaching the optimal therapeutic effect dose was gradually reduced, and pass on maintenance therapy at a dose of 50 mg / day. The maximum daily dose is 150 mg.
    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 (to

    Daily dose (to


    the number of tablets,

    the number of tablets,

    6-7 years (20-24)

    1 [25]

    1 [25]

    8-11 years old (25-37)

    1[25]

    2-3 [50-75]

    12-14 years (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 or spasm, sensation of bloating, diarrhea, nausea, constipation, flatulence, increased activity of "liver" tranaminaz; peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding without ulcers;

    less often 1% - vomiting, jaundice, melena, blood in the doghouse, esophageal lesion, aphthous stomatitis, dryness of mucous membranes (including the mouth), hepatitis (possibly fulminant course), hepatic necrosis, cirrhosis, hepatorenal syndrome, appetite change, pancreatitis (in including those with concomitant hepatitis), holetsistopankreatit colitis.

    From the 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, general weakness, disorientation, nightmares, fear.

    From the sense organs:

    more often 1% - noise in the ears;

    On the part of the skin :, more often 1% - skin itch, skin rash;

    less often 1% - alopecia, urticaria, eczema, toxic dermatitis, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), increased photosensitivity, small-point hemorrhages.

    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 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 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, shortness of breath, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, dysfunction of the liver and kidneys.
    Treatment: gastric lavage, the introduction of activated charcoal, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are 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 synthesis, prostaglandins in the kidneys, which increases nephrotoxicity. Simultaneous use 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: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.
    Effect on the ability to drive transp. cf. and fur:During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Tablets coated with enteric coating 25 mg.
    Packaging:

    For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 30 tablets in cans of glass type BTS.

    1 or 3 contour squeeze packs or a jar along with instructions for use are put in a pack of cardboard.
    Storage conditions:
    In dry, protected from light, out of reach of children at a temperature of no higher than 25 ° C.

    Shelf life:3 years. Do not use after the expiry date printed on the package
    Terms of leave from pharmacies:On prescription
    Registration number:PL-000214
    Date of registration:16.02.2011
    Date of cancellation:2016-02-16
    The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia
    Manufacturer: & nbsp
    Information update date: & nbsp14.02.2016
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