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

    Composition for one tablet:

    Active substance: diclofenac sodium - 25 mg;

    Excipients (core): Stearic acid 0.531 mg, talc 0.469 mg, potato starch 9.406 mg, lactose monohydrate 30 mg, sucrose 30 mg, povidone (low molecular weight polyvinylpyrrolidone or Plasdon K-17) 4,594 mg; Film sheath AdvantiaPrime 190100BA01 (hypromellose 0.9375 mg, titanium dioxide 0.375 mg, macrogol (polyethylene glycol) 0.1875 mg) 1.5 mg; The enteric membrane AdvantiaPerformance 345061AM49 (copolymer of methacrylic acid with ethyl acrylate - 6.08 mg, talc 1.52 mg, triethyl citrate - 1.064 mg, silicon dioxide colloid - 0.12 mg, titanium dioxide 0.723 mg, riboflavin 0.468 mg, iron dye red oxide - 0.003 mg, iron-oxide oxide yellow-0.022 mg) -10 mg.

    Description:The tablets covered with an enteric-coated membrane are round, biconvex, orange-yellow or orange. On the cross-section, two layers are visible: the first is orange-yellow or orange, the second-white. A slight unevenness of the coating is allowed.
    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 (NSAID), a derivative of phenylacetic acid. Has anti-inflammatory, analgesic and antipyretic effect. By indiscriminately inhibiting cyclooxygenase-1 and cyclooxygenase-2, it breaks the metabolism of arachidonic acid and reduces the amount of prostaglandins in the inflammatory focus. Effective for inflammatory pain. Has antiaggregant activity.
    Pharmacokinetics:
    Absorbed quickly and completely, the absorption rate slows down when eating. After taking 50 mg, the maximum concentration is 1.5 μg / ml, the time to reach the maximum concentration is 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%. It binds to plasma proteins by 99% (mainly with albumins). Penetrates into breast milk, 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 remain higher for another 12 hours). The relationship between the concentration of the drug and synovial fluid and the clinical efficacy of the drug has not been revealed.

    50% of the drug is metabolized at the "first pass" through the liver. Metabolism occurs as a result of single or multiple hydroxylation and conjugation with glucuronic acid. The enzyme system CYP2C9 also participates in the metabolism of the drug. The pharmacological activity of metabolites is less than that of diclofenac.

    Systemic clearance is 260 ml / min. Half-life 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, pharmacokinetic parameters do not change.
    Indications:
    Symptomatic treatment of diseases of the musculoskeletal system: rheumatoid arthritis, gouty arthritis, psoriatic, ankylosing spondylitis, 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, toothache, headache, migraine, algodismenorea, adnexitis, proctitis. In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome: pharyngitis, tonsillitis, otitis media.

    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, urticaria 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 (ulcerative colitis, Crohn's disease);

    - uncompensated heart failure;

    - period after aortocoronary shunting;

    - marked renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia;

    - severe hepatic impairment or active liver disease;

    - cerebrovascular bleeding or other bleeding and hemostasis disorders;

    - III trimester of pregnancy;

    - the period of breastfeeding;

    - Children under 6 years.
    Carefully:
    Bronchial asthma, anemia, congestive heart failure, hypertension, ischemic heart disease, edematous syndrome, cerebrovascular diseases, peripheral arterial disease,hepatic or renal failure, dyslipidemia / hyperlipidemia, diabetes, smoking, diverticular disease, inflammatory bowel disease, advanced age, condition after major surgery, systemic connective tissue disease induced porphyria, pregnancy I-II trimester, creatinine clearance of 30-60 ml / min.
    A history of the development of ulcerative diseases of the gastrointestinal tract, the presence of infection Helicobacter pylori, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases.
    Simultaneous therapy with oral glucocorticosteroids (for example, prednisolone), anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
    Pregnancy and lactation:The use of the drug in the third trimester of pregnancy and during lactation is contraindicated. Use the drug in the I-II trimesters of pregnancy with caution.
    Dosing and Administration:
    Inside, without chewing, during or after a meal, with a small amount of water. Adults and adolescents with 15 years of age - 25-50 mg (1-2 tablets) 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, the daily dose is 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.

    The approximate mode of application is shown in the table:

    Age

    Single dose

    Daily dose

    (mass m

    (number of tablets

    (number of tablets,

    la, kg)

    current (mg))

    (mg))

    6-7 years

    1 [25]

    1 [25]

    (20-24)

    8-11 years old

    1 [25]

    2-3 [50-75]

    (25-37)

    12-14 years old

    1-2 [25-50]

    3-4 [75-100]

    (38-50)

    Older than 15

    1-2 [25-50]

    2-6 [50-150]

    and adults

    Side effects:

    Often - 1-10%; sometimes 0.1-1%; rarely - 0,01-0,1%; very rarely - less than 0.001%, including individual cases.

    From the gastrointestinal tract (GIT): often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases;

    rarely - gastritis, proctitis, bleeding from the digestive tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function;

    very rarely - stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis. From the nervous system: often - headache, dizziness; rarely - drowsiness, sleep disturbances;

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

    From the hematopoiesis: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

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

    From the side of 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 - bullous eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

    Other: rarely - swelling.

    Overdose:
    Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, headache, hyperventilation of the lungs, turbidity, tinnitus, convulsions, with a significant overdose - acute renal failure, hepatotoxic effect; 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 and hemodialysis are ineffective.
    Interaction:
    Increases the concentration in the plasma digoxin, lithium preparations.

    Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; on the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often the gastrointestinal tract).

    Reduces the effect of hypotensive and hypnotic drugs (LS). Increases the likelihood of side effects caused by other NSAIDs and glucocorticosteroids (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine (due to an increase in their plasma concentrations).

    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 drugs.

    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 is manifested by increased nephrotoxicity.

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

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

    LC, which cause photosensitivity, increase the sensitizing effect of diclofenac to UV irradiation.

    LC, which block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its effectiveness and toxicity. Antibacterial drugs from the quinolone group - 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 eating, without chewing, squeezed with enough water.

    Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised in appointing patients with cardiac or renal insufficiency, and also in the treatment of elderly patients taking diuretics and patients who for any reason have a decrease in circulating blood volume (in t.ch.after extensive surgical intervention). If in such cases appoint diclofenac, recommended as a precautionary measure to monitor kidney function. In patients with renal insufficiency with creatinine clearance less than 10 ml / min, the equilibrium concentration of metabolites in plasma should theoretically be significantly higher than in patients with normal renal function, but this is not really observed, because in This situation increases the excretion of metabolites with bile.

    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.

    To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.
    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 other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Tablets coated with enteric film coating 25 mg.
    Packaging:For 10 tablets in a contour mesh box made of PVC film and aluminum foil. 2, 3, 4, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.
    Storage conditions:Store in a dry, dark 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:LS-001733
    Date of registration:19.09.2011
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.02.2016
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