Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspTablets of prolonged action, covered with enteric coating.
    Composition:

    1 tablet contains:

    Core:

    Active substance: Diclofenac sodium - 100.0 mg

    Excipients Guar gum - 20,00 mg, hypromellose - 10,00 mg, povidone - 15,00 mg, magnesium stearate - 2,00 mg, microcrystalline cellulose - 3,33 mg, talc - 3, 33 mg.

    Sheath: ethyl cellulose 1.66 mg, hypromellose 7.66 mg, iron (III) oxide red 0.10 mg, titanium dioxide 1.50 mg, talc 7.00 mg, propylene glycol 0.001 mg.

    Description:Round biconvex with slightly slanted edges of the tablet, covered with a film enteric coating from pink to light brown, on the cross section the nucleus 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 and antipyretic effects.Indiscriminately inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation. 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 is 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-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 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:
    Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthritis of peripheral joints and spine, including radicular syndrome, tendovaginitis, bursitis). The drug removes or reduces pain and inflammation during the treatment period, without affecting the progression of the disease. Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache.

    With the composition of complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).

    Children

    Retard form of diclofenac in pediatrics is not applied.
    Contraindications:
    - Period after aortocoronary bypass surgery;

    - III trimester of pregnancy, the period of breastfeeding;

    - Decompensated heart failure;

    - 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 mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;

    - Inflammatory bowel disease (ulcerative colitis, Crohn's disease) in the phase of exacerbation;

    - 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);
    Carefully:Anemia, bronchial asthma, congestive heart failure, arterial hypertension, edematous syndrome, hepatic or renal insufficiency, alcoholism, inflammatory bowel disease, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes, state after extensive surgical interventions, porphyria induced, elderly age, diverticulitis, systemic connective tissue diseases.
    Pregnancy and lactation:It is not recommended to use Diklogen® in the III trimester of pregnancy. If it is necessary to prescribe the Diklogen® preparation of a nursing mother, the question of stopping breastfeeding should be addressed.
    Dosing and Administration:
    Undesirable effects can be minimized by using the lowest effective dose and the shortest course, sufficient to manage the symptoms.

    The recommended dose is 1 tablet 100 mg once a day. Tablets should be taken

    wholly with liquid, preferably during meals.

    Children

    Diclogen® is not recommended for children because of the high content of active ingredient in the tablet.

    Elderly patients

    For elderly patients or for patients with a certain physical ailment (patients with pronounced weakness) it is recommended to prescribe the minimum effective dose. At the same time, it should be noted that the pharmacokinetic properties of diclofenac sodium do not deteriorate in any clinically significant degree when using this drug in elderly patients.
    Side effects:

    Gastrointestinal tract:

    Often 1-10%: abdominal pain, sensations of bloating, diarrhea, nausea, constipation, flatulence, increased activity of "liver" enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;

    Uncommon 0.1 - 1%: vomiting, jaundice, melena, the appearance of blood in the feces, the defeat of the esophagus, aphthous stomatitis, dry mouth and mucous membranes, hepatitis (possibly fulminant flow),

    Rarely 0.01 - 0.1%: liver necrosis, cirrhosis, hepatorenal syndrome, appetite change, pancreatitis, cholecystopancreatitis, colitis.

    Nervous system:

    Often 1-10%: headache, dizziness;

    Uncommon 0.1 - 1%: sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic diseases of connective tissue);

    Rarely 0.01 -0.1%: convulsions, weakness, disorientation,

    Very rarely - less than 0.001%: including individual cases - nightmarish dreams,

    feeling of fear.

    Sense organs:

    Often 1-10%: noise in ears;

    Not infrequently 0.1-1%: blurred vision, diplopia, a taste disorder,

    Rarely 0.01 -0.1%: reversible or irreversible hearing loss, scotoma. Skin:

    Often 1-10%- skin itching, skin rash;

    Uncommon 0.1 - 1%: areata, urticaria, eczema, chronic dermatitis, erythema multiforme, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell syndrome),

    Rarely 0.01 - 0.1%: increased photosensitivity, small-point hemorrhage.

    Genitourinary system:

    Often 1-10%: fluid retention;

    Uncommon 0.1 - 1%: nephrotic syndrome, proteinkriya, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal insufficiency, azotemia.

    Hematopoiesis and the immune system:

    Often 1 to 10%: Anemia (including haemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of infectious processes (development of necrotising fasciitis).

    Respiratory system:

    Not infrequently 0.1-1%: cough, bronchospasm, laryngeal edema, pneumonitis. The cardiovascular system:

    Uncommon 0.1 - 1%: increased blood pressure; congestive heart failure, extrasystole, chest pain.

    Allergic reactions:

    Rarely 0.01 - 0.1%: 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, 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.

    Cefomandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.

    Cyclosporine and gold medications increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.

    Simultaneous administration with ethanol, colchicine, corticopropine and St. John's wort increases the risk of bleeding in the gastrointestinal tract.

    Diclofenac enhances the effect of drugs that cause photosensitivity. Preparations blocking tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.
    Special instructions:
    During Diclogen® treatment, gastrointestinal bleeding may occur at any time, or a gastrointestinal ulcer may develop, sometimes complicated by perforation; and not always there are symptoms-precursors of these complications or the presence of anamnestic information about ulcerative lesions. More serious consequences of these complications can be observed in elderly patients. In this case the drug should be canceled.
    In a patient who has not previously taken Diclogen®, during the treatment with the drug, allergic reactions, including anaphylactic and anaphylactoid reactions, can rarely develop.

    Diklogen® due to its pharmacodynamic properties, can mask the complaints and symptoms characteristic of infectious and inflammatory diseases. During the application of Diklogena®, careful medical supervision of those patients who have complaints indicating gastrointestinal tract diseases is necessary; who have anamnestic information about ulcerative lesions of the stomach or intestines; suffering from ulcerative colitis or Crohn's disease, as well as those with impaired liver function. During the application of Diclogen®, the level of one or more hepatic enzymes may increase. Therefore, with prolonged use of the drug, as a precautionary measure, a regular study of liver function is indicated.

    It is not recommended to prescribe the drug to patients with hepatic porphyria (due to the danger of porphyria attacks).

    Since prostaglandins play an important role in maintaining renal blood flow,special caution is required in the treatment of patients with impaired cardiac or renal function, elderly patients, patients receiving diuretics.

    With prolonged use of the drug, a systematic control of the pattern of peripheral blood is shown.

    Diclogen® can temporarily inhibit platelet aggregation. Therefore, patients with hemostasis disorders need careful monitoring of relevant laboratory parameters.

    Caution when using Diclogen® is also necessary in elderly patients. This is especially true in weakened or low-weight elderly people. They are recommended to prescribe the drug in the minimum effective dose.
    Impact on fertility

    In connection with the negative effect on fertility, women who want to become pregnant, the drug 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 period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving transport and practicing other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:
    Tablets of prolonged action, covered with enteric coating 100 mg.
    Packaging:
    For 10 tablets per strips of Al / Al or a blister from Al / PVC. 1 or 2 strip or 1 or 2 blisters with instructions for use packed in a cardboard box.

    Storage conditions:In a dry 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 printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011100
    Date of registration:30.12.2011
    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: & nbsp08.02.2016
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