Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspTablets, covered with enteric coating.
    Composition:
    1 tablet contains:

    Active substance:

    diclofenac sodium 25.0 or 50.0 mg.

    Excipients:

    lactose monohydrate 15.0 or 30.0 mg; calcium hydrophosphate dihydrate 20.0 or 40.0 mg; microcrystalline cellulose 24.5 or 49.0 mg; cornstarch 10.0 or 20.0 mg; sodium carboxymethyl starch 4.0 or 8.0 mg; magnesium stearate 1.0 or 2.0 mg; silicon dioxide colloid 0.5 or 1.0 mg.

    Sheath:

    methacrylic acid and ethyl acrylate copolymer [1: 1] [contains sodium lauryl sulfate 0.7%, polysorbate-80 2.3%] 6.42'or 11.32 mg; triethyl citrate 0.64 or 1.13 mg; talc 2.57 or 4.52 mg; titanium dioxide (EL 71) 0.19 or 0.33 mg; ferric oxide yellow (E 172) 0.54 or 0.95 mg.
    Description:
    Tablets 25 mg:

    Round biconvex tablets, covered with a film coat of brownish-yellow color, on a broken white color.

    Tablets 50 mg:

    Round biconvex tablets with a facet on both sides, covered with a film coat of a brownish-yellow color, on a broken white color.
    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 derivative of phenylacetic acid, has an anti-inflammatory, analgesic and antipyretic effect. 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. Like all non-steroidal anti-inflammatory drugs, diclofenac has antiaggregant activity.
    Pharmacokinetics:

    Quickly and almost completely absorbed from the gastrointestinal tract. The time to reach the maximum concentration of the drug in the blood serum is 2-3 hours. Eating slows the absorption rate by 1:2 hours and reduces the maximum concentration of diclofenac in plasma by half.Value removals linearly dose dependent.

    Diclofenac does not cumulate - with the recommended interval between applications of the drug. Penetrates into breast milk, through blood-brain and placental barriers.

    The connection with plasma proteins is more than 99.7% (mainly with albumins - 99.4%). The volume of distribution is 0.12-0.17 l / kg. Bioavailability - 50%.

    Metabolized as a result of multiple or single hydroxylation and conjugation with glucuronic acid. In the metabolism of the drug takes part isoenzyme CYP2C9. The pharmacological activity of metabolites is lower than that of diclofenac. No age differences in the absorption, metabolism and elimination of the drug have been found. Systemic clearance is 263 ± 56 ml / min. The half-life of plasma is 1-2 hours. More than 60% 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 concentration of metabolites in the blood increases approximately 4-fold, and their excretion with bile increases.

    In patients with chronic hepatitis or compensated cirrhosis, the pharmacokinetic parameters of diclofenac do not change.

    Indications:- inflammatory and degenerative diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine, including radicular syndrome, tendovaginitis, bursitis );
    - in the treatment of pain syndrome and / or inflammation in gynecology (dysmenorrhea, adnexitis);
    - neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine;
    - 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, on
    the progression of the disease is not affected.
    Contraindications:
    -hypersensitivity to diclofenac (including other NSAIDs) and other components of the drug;
    -complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in anamnesis);
    -rotozionno-ulcerous changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding;
    -inflammatory bowel diseases (Crohn's disease, ulcerative colitis, proctitis) in the phase of exacerbation;
    hemophilia and other bleeding disorders;
    - severe renal failure (creatinine clearance (CK) less than 30 ml / min);
    -decompensated heart failure;
    early postoperative period after aortocoronary bypass surgery;
    - intolerance of galactose, lactase deficiency or glucose-galactose malabsorption syndrome;
    - confirmed hyperkalemia;
    -Birth (III trimester);
    -period of lactation;
    -baby age (for tablets 25 mg - up to 6 years, for tablets 50 mg - up to 14 years)
    Carefully:
    - with ulcerative lesions of the stomach or intestines, Helicobacter pylori infection, ulcerative colitis, Crohn's disease,
    violations of liver function in history, with complaints of diseases of the gastrointestinal tract (GIT). Risk
    the development of gastrointestinal bleeding increases with increasing doses of non-steroidal anti-inflammatory
    drugs (NSAIDs) or in the presence of ulcerative anamnesis, especially bleeding and perforation of the ulcer and in the elderly;
    - receiving drugs that increase the risk of gastrointestinal bleeding: systemic glucocorticosteroids,
    antiaggregants (including clopidogrel, acetylsalicylic acid), anticoagulants (including warfarin) or
    selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline);
    - with mild and moderate impairment of liver function, as well as with hepatic porphyria, as the drug may
    provoke porphyria attacks;
    - with bronchial asthma, seasonal allergic rhinitis, edema of the nasal mucosa (including with nasal polyps), chronic obstructive pulmonary disease (COPD), chronic infectious diseases
    respiratory tract (especially associated with allergic rhinitis-like symptoms);
    - with cardiovascular diseases (including ischemic heart disease, cerebrovascular diseases
    diseases, compensated heart failure, peripheral vascular disease), impaired function
    kidney, including chronic renal failure (CK 30 - 60 ml / min), dyslipidemia / hyperlipidemia, sugar
    diabetes, hypertensive disease, in the treatment of smokers or patients who abuse alcohol,
    patients receiving diuretics or other drugs that affect the function of the kidneys, as well as patients with significant
    a decrease in the volume of circulating blood (BCC) of any etiology, for example, before and after massive
    surgical interventions;
    - with defects in the hemostatic system, with a risk of developing cardiovascular thrombosis (including myocardial infarction and
    strokes);
    - elderly, in particular, having a low body weight.
    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 I and II trimester, unless the intended benefit for
    the mother exceeds the potential risk to the fetus. Contraindicated in the use of diclofenac in pregnant women during
    III trimester because of the possibility of developing weakness in the uterine labor activity and / or premature
    Closure of the arterial duct in the fetus.
    Diclofenac penetrates into breast milk in small amounts, so when using the drug during lactation it is necessary to resolve the issue of stopping breastfeeding.
    Dosing and Administration:
    The drug should be used in a minimally effective dose as little as possible.
    Inside, not liquid, squeezed a small amount of water, before eating.
    Adults prescribe in the initial daily dose of 100-150 mg in 2-3 divided doses. Tablets 25 mg: 1-2 tablets 2-3 times a day.
    Tablets of 50 mg: 1 tablet 2-3 times a day.
    The maximum daily dose of the drug is 150 mg.
    With symptomatic treatment of dysmenorrhea, a single daily dose can be increased to 200 mg.
    Children over 6 years the drug is prescribed in a daily dose of 1-2 mg / kg body weight; this. The dose is divided into 2-3 doses depending on the severity of the symptoms. In the treatment of juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg, which is the maximum daily dose.
    Recommended dosage regimen Diclofenac Sandoz® in children over 6 years old

    Age (body weight, kg)

    Single dose (number of tablets, (mg))

    Daily dose (number of tablets, (mg))

    6-7 years (20-24)

    1 (25)

    1(25)

    8-11 years old (25-37)

    1(25)

    2-3 (50-75)

    12-14 years old (38-50)

    1-2(25-50)'

    3-4 (75-100)

    Older than 14

    1-2(25-50)

    2-6(50-150)


    Side effects:

    According to the World Health Organization (WHO)

    unwanted 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, flatulence, anorexia, decreased appetite;

    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: memory impairment, convulsions, anxiety, tremor, aseptic meningitis (usually in patients with systemic lupus erythematosus and other systemic diseases connective tissue), cerebrovascular disorders, disorientation, depression, insomnia, nightmares, irritability, weakness, impaired sensitivity (including paresthesia).

    From the sense organs:

    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 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 blood pressure (BP) and anaphylactic shock);

    rarely: angioedema (including Quincke's edema).

    From the respiratory system:

    rarely: cough, bronchospasm, swelling larynx;

    rarely: pneumonitis.

    From the side of cardiovascular system:

    infrequently: myocardial infarction, chronic heart insufficiency heart palpitations and pain in the chest;

    rarely: increased blood pressure, vasculitis, extrasystole.

    From the skin:

    often: skin itching, skin rash;

    rarely: hives;

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

    From the liver and bile excretory ways:

    often: increased activity "hepatic" transaminases;

    rarely: hepatitis, jaundice, violation liver function;

    rarely: hepatitis (possibly fulminant course), necrosis liver, cirrhosis, hepatorenal syndrome, hepatic insufficiency.

    Other:

    rarely: edema.

    Overdose:Symptoms: vomiting, bleeding from the gastrointestinal tract, dizziness, headache, diarrhea, tinnitus, dyspnea, myoclonic cramps, respiratory depression, impaired liver and kidney function, coma.
    Treatment: gastric lavage, the introduction of activated charcoal, 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 blood plasma digoxin, methotrexate, lithium and cyclosporine preparations.
    Increases toxicity methotrexate and nephrotoxicity цiklospirin and preparations of gold.
    Reduces efficiency diuretics, on the background potassium-sparing diuretics increased risk of hyperkalemia; on the background
    anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) and selective serotonin reuptake inhibitors increase the risk bleeding (more often from the gastrointestinal tract). When used simultaneously with diuretics and antihypertensive drugs (beta- adrenoblockers, inhibitors angiotensin-converting enzyme (ACE)) diclofenac can reduce their hypotensive effect. Therefore, in patients, especially the elderly, with the simultaneous administration of diclofenac and diuretics or antihypertensive agents, blood pressure should be measured regularly,control kidney function and the degree of hydration (especially with a combination of diuretics and ACE inhibitors due to increased risk of nephrotoxicity). Reduces effects hypnotics.

    Increases the likelihood of side effects of other NSAIDs (including selective inhibitors of cyclooxygenase-2 (COX2)) and glucocorticosteroids (bleeding in the gastrointestinal tract).

    Acetylsalicylic acid reduces the concentration of diclofenac in the blood. The simultaneous use of diclofenac and paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

    Clinical studies have shown that diclofenac can be assigned together with hypoglycemic drugs for oral administration, and it does not affect their clinical effect. However, there are separate reports of a decrease or intensification of the effect hypoglycemic agents: it is recommended to monitor the concentration of glucose in the blood.

    Cefamandol, cefoperazone, cefotetan, valproic acid, and plikamycin increase the frequency of hypoprothrombinemia. Simultaneous application with ethanol, colchicine, corticotropin and preparations of St. John's wort perfumed increases the risk of bleeding in the digestive tract.

    Diklofenac enhances action drugs that cause photosensitization.

    Preparations blocking tubular secretion, increase the diclofenac concentration in plasma blood, thereby increasing it toxicity.

    With simultaneous application diclofenac and antibacterial medicines from the group quinolone increased risk of developing seizures.

    When used simultaneously with inhibitors of cytochrome CYP2C9 an increase in concentration is possible

    drug in the blood plasma.

    When used simultaneously with derivatives phenytoin perhaps intensification of the action of phenytoin.

    Special instructions:To reduce the risk of developing The use of undesired phenomena should be a minimally effective dose of diclofenac minimally possible short course.

    Gastrointestinal tract

    When using diclofenac, there were such phenomena as bleeding or ulceration / perforation of the gastrointestinal tract, in some cases with a fatal outcome. Patients with an increased risk of developing gastrointestinal complications, as well as receiving therapy with low doses of acetylsalicylic acid or other drugs,Gastroprotective agents (for example, proton pump inhibitors or misoprostol). Patients with a history of gastrointestinal disease, especially the elderly, should be told the doctor about the symptoms of the digestive system.

    Skin Reactions

    In rare cases with diclofenac treatment, such serious dermatological reactions as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, in some cases fatal cases have been noted. When developing in patients receiving diclofenac sodium, the first signs of skin rash, lesions of the mucous membranes or other symptoms of hypersensitivity drug should be canceled.

    Effects on the liver

    In the presence of symptoms of hepatotoxicity (including nausea, diarrhea, pruritus, jaundice), diclofenac treatment should be discontinued. When conducting therapy, it is necessary to monitor liver function, a clinical blood test, a fecal occult blood test.

    Effects on the kidneys

    Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when administering the drug to patients with cardiac orrenal insufficiency, as well as 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 surgery). If in such cases appoint diclofenac, it is recommended, as a precaution, to monitor kidney function.

    Impact on the system hematopoiesis

    Diclofenac temporarily inhibits platelet aggregation, so patients with bleeding disorders should be monitored regularly

    relevant laboratory indicators.

    Patients with bronchial asthma

    In patients with allergic rhinitis, nasal polyps, chronic obstructive pulmonary disease, or chronic respiratory infections (especially those associated with allergic rhinopod symptoms), NSAID intolerance, bronchial asthma, Quincke's edema and urticaria are most often noted. In this group of patients, as well as in patients with allergies to other drugs (rash, itching, urticaria), special care should be taken when prescribing the drug.

    Diclofenac affects female fertility, so patients with infertility (including undergoing examination) are recommended to cancel the drug.

    Long-term diclofenac therapy and high-dose therapy may lead to an increased risk of developing serious cardiovascular thrombotic complications (including myocardial infarction and stroke). Diclofenac can mask the symptoms of infectious and inflammatory diseases.

    Form release / dosage:
    Tablets, coated with enteric coating, 25 mg, 50 mg.
    Packaging:
    Primary packaging
    For 10 tablets per blister of PP / Al.
    Secondary packaging
    By 1; 2; 3; 5 or 10 blisters together with instructions for use 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:
    18 months.
    Do not use at the end of the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N008475 / 01
    Date of registration:15.11.2011
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp02.03.2016
    Illustrated instructions
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