Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspLong-acting tablets.
    Composition:
    one tablet contains:

    active substance: diclofenac sodium - 75 mg or 150 mg
    auxiliary substances: lactose monohydrate, methylhydroxypropylcellulose, microcrystalline cellulose, calcium hydrogen phosphate dihydrate, corn starch, sodium starch glycolate, silicon dioxide colloid, magnesium stearate, iron oxide red.

    Description:Round flat cylindrical tablets of white color, one surface of which is pink in color with white impregnations, with a facet on both sides. On the cross-section of the tablet are visible two layers: white and pink with white impregnations.
    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:
    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.

    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. In the metabolism of the drug takes participation enzyme system P450 CYP2C9.

    The pharmacological activity of metabolites is lower than that of diclofenac.

    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 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, osteoarthritis of peripheral joints and spine, including with 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 to the active substance and / or other constituents of the drug;
    - intolerance of other NSAIDs in history;
    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including
    anamnesis);
    - erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding;
    - inflammatory bowel disease (Crohn's disease, ulcerative colitis, proctitis) in the phase of exacerbation;
    - hemophilia and other bleeding disorders;
    - severe renal failure (CC less than 30 ml / min);
    - liver failure;
    - cardiac ischemia;
    - chronic heart failure (II-IV functional class according to NYHA (New York classification of the functional state of patients with chronic heart failure));
    - cerebrovascular diseases;
    - diseases of peripheral arteries;
    - increased risk of arterial thrombosis and thromboembolism;
    - early postoperative period after aortocoronary shunting;
    - lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;
    - confirmed hyperkalemia;
    - pregnancy (III trimester);
    - the period of breastfeeding;
    - children's age (under 18 years).

    Carefully:
    - patients with arterial hypertension, dyslipidemia, hyperlipidemia, inflammatory
    diseases of the intestine outside the acute phase, liver disease in the history, hepatic
    porphyria, seasonal allergic rhinitis, chronic obstructive pulmonary disease,
    chronic infections of the respiratory tract, Quinck's edema, edema of the nasal mucosa (including those with nasal polyps), bronchial asthma, diabetes mellitus,
    systemic connective tissue diseases;
    - elderly patients with anemia and data on the development of ulcerative gastrointestinal lesions in history, perforation;
    - patients with arterial hypertension, dyslipidemia, hyperlipidemia, inflammatory
    diseases of the intestine outside the acute phase, liver disease in the history, hepatic
    porphyria, seasonal allergic rhinitis, chronic obstructive pulmonary disease, chronic infections of the respiratory tract, Quinck's edema, edema of the nasal mucosa (including nasal polyps), bronchial asthma, diabetes, systemic connective tissue diseases;
    - elderly patients with anemia and data on the development of ulcerative gastrointestinal lesions in history, perforation; patients with low body weight), patients with severe medical conditions, smokers;
    - with renal failure (KK 30-60 ml / min).
    Pregnancy and lactation:The use of diclofenac in pregnant women has not been investigated. Therefore, it is not recommended to use the drug in pregnant women during the first and second trimester. Contraindicated in the use of diclofenac in pregnant women during the third trimester because of the possibility of developing weakness in the uterine labor activity and / or premature closure of the arterial duct. Studies in animals have shown no harmful effects on fetal / fetal and postnatal development. Diclofenac in small quantities penetrates into breast milk, so if you need to prescribe Diclac® during breastfeeding, you should decide whether to stop breastfeeding.
    Dosing and Administration:
    Inside, not liquid, squeezed a little water, usually during or after a meal.

    Tablets of 75 mg: 1 tablet 1-2 times a day.

    Tablets 150 mg 1 tablet per day.

    The maximum daily dose of the drug is 150 mg.
    Side effects:According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very often (>1/10), often (>1/100, <1/10), infrequently (>1/1000, <1/100), rarely (>1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

    From the gastrointestinal tract

    often: nausea, vomiting, diarrhea, indigestion, abdominal pain, bloating, anorexia; rarely: gastritis, vomiting with an admixture of blood, gastrointestinal

    bleeding, melena, gastric or intestinal ulcers, possibly with complications (bleeding, perforation), frequent stools with a trace of blood, proctitis;

    rarely: esophagitis, esophageal motility disorder, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, stomatitis, glossitis, pancreatitis, exacerbation of hemorrhoids, intestinal adhesions.

    From the nervous system

    often: headache, dizziness;

    rarely: drowsiness;

    rarely: depression, anxiety, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, weakness, disorientation, nightmarish dreams, memory impairment, tremor, cerebrovascular disorders, sensitivity disorders (including paresthesia )

    From the senses often: vertigo;

    rarely: noise in the ears, hearing impairment, blurred vision, diplopia, a violation of taste sensations.

    From the urinary system

    rarely: acute renal failure, hematuria, proteinuria, nephrotic syndrome, interstitial nephritis, papillary necrosis.

    On the part of the organs of hematopoiesis and lymphatic system

    rarely: anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia

    (thrombocytopenic purpura), eosinophilia, agranulocytosis.

    From the immune system

    rarely: anaphylactic reactions (including lowering of arterial pressure and shock);

    rarely: angioedema edema (including Quincke's edema).

    From the respiratory system

    rarely: cough, bronchospasm, swelling larynx;

    rarely: pneumonitis.

    From the side of cardiovascular systems

    infrequently: myocardial infarction, chronic heart failure;

    rarely: rise arterial pressure, vasculitis, a feeling of palpitations, extrasystole, chest pain cell.

    From the skin

    often: skin itching, skin rash;

    rarely: hives;

    rarely: Bullous rash, toxic dermatitis, eczema, polymorphic erythema, toxic epidermal necrolysis (syndrome Lyell, Stevens- Johnson), photosensitization.

    From the side are baked and bile ducts

    often: increased activity of "liver" transaminases;

    rarely: jaundice, liver damage;

    rarely: hepatitis (possibly fulminant course), necrosis liver, cirrhosis, hepatorenal

    syndrome, hepatic failure.

    Other

    rarely: edema.

    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:
    Tablets of prolonged action 75 or 150 mg.
    Packaging:
    For a dosage of 75 mg:
    Primary packaging
    For 10 tablets in a blister of PVC / PVDC / A1 or PP / A1.
    Secondary packaging
    For 1, 2, 5 or 10 blisters together with instructions for use in a pack of cardboard.
    For a dosage of 150 mg:
    Primary packaging
    For 10 tablets in a blister from PP / A1.
    Secondary packaging
    For 1, 2, 5 or 10 blisters together with instructions for use in a pack of cardboard.
    Storage conditions:
    List B

    At a temperature of no higher than 25 ° C. In a place inaccessible to children.

    Shelf life:
    3 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011215 / 03
    Date of registration:04.08.2010
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    HEXAL, AG Germany
    Representation: & nbspHEXAL AG HEXAL AG Germany
    Information update date: & nbsp16.02.2016
    Illustrated instructions
      Instructions
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