Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspThe tablets covered with a film intestine-soluble membrane.
    Composition:

    1 tablet contains:

    The core of the tablet

    Active substance: diclofenac sodium (sodium diclofenac) - 25 mg Excipients: lactose monohydrate 30.5 mg, sugar 6.8 mg, povidone 12.6 thousand (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700) 1.4 mg, stearic acid 0.94 mg , potato starch - 35.36 mg

    Sheath: cellulose (castor oil) - 0.536 mg, titanium dioxide (titanium dioxide) 0.371 mg, tropeolin-O (tropeolin O) dye-0.124 mg, azorubin (acid red 2C) dye 0.002 mg.

    Description:Tablets are orange-yellow or orange, round, biconvex, covered with a film intestinal membrane. On the cross-section, the shell is visible, orange-yellow or orange, and: the core 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 - a non-steroidal anti-inflammatory drug (NSAID), a phenylacetic acid / acid derivative; has anti-inflammatory, analgesic and antipyretic effect. By indiscriminately inhibiting cyclooxygenase-1 and cyclooxygenase-2, it breaks the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain. Like all NSAIDs, 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 umenyvanet painful sensations and inflammatory edema.
    Pharmacokinetics:

    Absorption is fast and complete; food slows the absorption rate by 1-4 hours and reduces the maximum concentration (CmOh) by 40%. After oral administration of 25 mg CmOh - 1.0 μg / ml, 50 mg CmOh- 1.5 μg / ml, time to reach the maximum concentration (TCmOh) - 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; FROMmOh in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life (T1/2) from the synovial fluid - 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. In the metabolism of the drug involved enzyme system P 450 CYP2C9. 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 in the form of 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, mild or moderate: 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, nasal mucosa, asthma);

    - Erosive and ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding;

    - Inflammatory bowel disease, 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 insufficiency or active liver disease;

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

    - Children under 6 years.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome,hepatic or renal insufficiency, 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 (GI), presence of Helicobacter pylori infection, prolonged use of NSAIDs, frequent use of alcohol, severe somatic diseases.

    Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Pregnancy and lactation:
    The drug is contraindicated for use in the third trimester of pregnancy and during breastfeeding.

    In the first and second trimesters of pregnancy diclofenac should be taken only in cases of extreme necessity, at the minimum prescribed dose, if the expected effect of therapy exceeds the potential risk to the fetus.
    Dosing and Administration:
    Inside, not chewing, during or after a meal, with a small amount of water.

    Adults and adolescents with 15 years of age - 1-2 tablets (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 in a dose of 1 tablet (25 mg) twice a day (50 mg / day).

    The maximum daily dose is 150 mg.

    For children over 6 years. and adolescents - 1 tablet (25 mg) 2-3 times a day (the drug is prescribed from the calculation of the daily dose of 2 mg / kg of the child's mass, divided into 2-3 sessions). With juvenile "rheumatoid arthritis, the daily dose can be increased to 3 mg / kg." The tablets should be taken whole, not chewing, fasting, with a small amount of liquid.
    Side effects:

    When assessing the frequency of occurrence of various side effects, the following grades are used: often - 1-10%; sometimes -0.1-1.%; rarely - 0,01-0,1%; very rarely - less than 0.001%, including individual cases.

    Allergic reactions:

    rare- anaphylactic / anaphylactoid reactions, including marked lowering of blood pressure (BP) and shock;

    very rarely - angioedema (including facial).

    From the nervous system: often - headache, dizziness;

    rarely - sleep disturbance, drowsiness;

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

    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.

    From the urinary system:

    Often - fluid retention;

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

    From the digestive system:

    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,diaphragm-like intestinal strictures (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis.

    From the hematopoiesis:

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

    From the respiratory system:

    rarely - bronchial asthma (including dyspnea);

    very rarely - pneumonitis.

    From the sense organs:

    often - vertigo;

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

    From the cardiovascular system:

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

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, inform the doctor about it.

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

    Treatment: gastric lavage, Activated carbon, symptomatic therapy aimed at eliminating the increase in blood pressure; violations of kidney 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, antiplatelet agents and thrombolytic drugs (LS) (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 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 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 increases nephrotoxicity.

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

    Diclofenac enhances the action of LC, causing photosensitivity.

    LC, which 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.

    If you are taking other medications, you should consult your doctor.
    Special instructions:
    In order to quickly achieve the desired therapeutic effect, take 30 minutes before eating. In other cases, take before, during or after a meal without chewing, squeezed with enough water.

    Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when assigning to 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 the volume of circulating blood (for example, 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 of the liver), 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 from the gastrointestinal tract, the minimum effective dose should be used as little as possible with a 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,therefore 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:
    The tablets covered with a film intestine-soluble coating, 25 mg.
    Packaging:
    10 tablets in a planar cell package; 1, 2, 3, 5, contour cell packs with instructions for use are placed in packs of cardboard.
    Storage conditions:In the 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.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-000821
    Date of registration:13.08.2010
    The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp16.02.2016
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