Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsp
    Tablets, covered with enteric coating.
    Composition:
    Active substance: diclofenac sodium - 25 mg or 50 mg.

    Excipients: silicon colloidal dioxide (aerosil), potato starch, crospovidone, calcium stearate, microcrystalline cellulose.

    Auxiliary substances for the shell: methacrylic acid and ethyl acrylate copolymer (Collicut MAE P100), povidone (Kollidon 30), iron oxide brown, propylene glycol, talc, titanium dioxide, hydroxypropylmethylcellulose (hypromellose).
    Description:The tablets covered with a cover of brown color, round, biconcave form. On the cross-section, two layers are visible, the inner layer is almost white.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Non-steroidal anti-inflammatory drug, a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effect.Indiscriminately inhibiting cycloxygenase 1 and cycloxygenase 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain. Like all non-steroidal anti-inflammatory drugs, the drug has an antiaggregant effect. 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, the food slows the absorption rate by 1-4 hours and reduces the maximum concentration (C max) by 40%. After oral administration, 25 mg of Cmax -1.0 μg / ml; 50 mg of Cmax - 1.5 μg / ml, Tmax - 2-3 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 cumulate while observing the recommended interval between meals. Bioavailability - 50%.The connection with plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into breast milk, synovial fluid; Stax in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life (T1 / 2) of the synovial fluid is 3-6 hours (the concentration of the drug in the synovial fluid 4-6 hours after its administration is higher than in the plasma, and remain higher for another 12 hours). 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 P 450 CYP2C9 takes part in the metabolism of the drug. Pharmacological activity of metabolites is less than diclofenac. Systemic clearance is 260 ml / min. T1 / 2 from the plasma - 1-2 hours 60% of the administered dose is excreted as metabolites through 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 of the liver, the pharmacokinetic parameters do not change. Diclofenac penetrates into breast milk.
    Indications:
    Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of 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).

    The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.
    Contraindications:
    - 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 and ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding;

    - Inflammatory bowel disease (nonspecific ulcerative colitis, Crohn's disease);

    - Period after aortocoronary bypass surgery;

    - III trimester of pregnancy, the period of breastfeeding;

    - Uncompensated heart failure;

    - Cerebrovascular bleeding or other bleeding and hemostasis disorders;

    - Severe hepatic impairment or active liver disease;

    - Severe renal insufficiency (creatinine clearance less than 30 ml / min), progressive kidney disease, incl. confirmed hyperkalemia;

    - Children under 6 years old for tablets of 25 mg, tablets of 50 mg are contraindicated in children under 15 years of age.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure,hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal failure, dyslipidemia / hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease, condition after extensive surgical interventions, induced porphyria, advanced age, diverticulitis, systemic connective tissue diseases, pregnancy I- II trimester, creatinine clearance less than 60 ml / min.

    Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illnesses.

    Simultaneous therapy with anticoagulants and (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (eg, prednisalone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:
    Inside, without chewing, during or after a meal, 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 and adolescents, 25 mg tablets are used; daily dose of 2 mg / kg of the body weight of the child, divided into 2-3 doses. With juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg body weight. Tablets should be taken whole, not liquid, fasting, with a small amount of liquid.
    Side effects:

    Often - 1-10%; sometimes 0.1-1%; rarely - 0,01-0,1%; very rarely - less than 0,001%, including

    isolated cases.

    On the part of the digestive system:

    often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases;

    rarely - gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with a trace of blood), ulcers of the gastrointestinal tract (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rarely - stomatitis, glossitis, esophagitis, diaphragm-like bowel patterns (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis.

    From the nervous system:

    often - headache, dizziness; rarely - sleep disturbance, drowsiness;

    very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

    From the sense organs:

    often - vertigo;

    very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.

    From the urinary system: often - fluid retention;

    very rarely - acute renal failure, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

    From the organs of hematopoiesis and the immune system:

    very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

    Allergic reactions:

    rarely anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock; very rarely - angioedema (including face).

    From the cardiovascular system:

    very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

    From the respiratory system:

    rarely - bronchial asthma (including dyspnea); very rarely - pneumonitis.

    From the skin:

    often - skin rash; rarely - hives;

    very rarely - painful rashes, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

    Overdose:
    Symptoms: dizziness, headache, hyperventilation of the lungs, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

    Treatment: gastric lavage, Activated carbon, 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; against the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often from the gastrointestinal tract).

    Reduces the effect of hypotensive and hypnotic drugs. Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroid agents (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, serotonin reuptake inhibitors and 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 increase the risk of seizures.
    Special instructions:
    In order to quickly achieve the desired therapeutic effect take 30 minutes before meals. In other cases, take before, during or after a meal without chewing, drinking with a sufficient amount of water.

    Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful when administered to patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, decrease in circulating blood volume is observed (eg , after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

    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.

    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 motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Tablets, covered with enteric coating, 25 mg and 50 mg.
    Packaging:
    For 10 or 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 1, 2, 3, 10 (for a dosage of 25 mg) or 2, 3, 5, 10 (for a dosage of 50 mg) of contiguous cell packs with instructions for use in a pack of cardboard.
    Storage conditions:List B. In a dry, the dark place at a temperature of no higher than 25 ° C.Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001467 / 01
    Date of registration:13.10.2008
    The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.02.2016
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