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

    active substance: diclofenac sodium - 100 mg;

    auxiliary substances: lactose monohydrate - 98.1 mg, hypromellose - 39.5 mg, magnesium stearate - 2.4 mg.
    Description:
    Round biconvex tablets white or almost white.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.
    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 promotes a significant reduction in 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:
    After taking long-acting tablets diclofenac completely absorbed from the intestine. Systemic bioavailability of diclofenac, released from prolonged-action tablets, averages 82% of the same value after taking the coated tablets at the same dose. After taking the prolonged-action tablet 100 mg, the maximum concentration of diclofenac in the blood plasma is achieved on average after 4 hours, the average value is 0.5 μg / ml (1.6 μmol / l). The intake of food does not have a clinically significant effect on the absorption of the active substance from the sustained-release tablets and its systemic bioavailability. Within 24 hours after taking the sustained-release tablet 100 mg, the concentration of diclofenac in the blood plasma is on average 13 ng / ml (40 nmol / l).The degree of absorption is directly related to the amount of the drug.

    Since the "first pass" through the liver metabolizes about half the amount of diclofenac, the maximum concentration after taking long-acting tablets is approximately 2 times less than in the case of parenteral administration of an equivalent dose of the drug.

    Do not cumulate while observing the recommended interval between doses of the drug. Penetrates into breast milk, through blood-brain and placental barriers.

    The connection with blood plasma proteins is more than 99.7% (mainly with albumin 99.4%). Metabolized as a result of multiple or single hydroxylation and conjugation with glucuronic acid. The enzyme system of cytochrome P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.

    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. After taking the drug inside the differences in absorption, metabolism or excretion of the drug, associated with the age of patients, is not noted.
    Indications:
    - inflammatory and degenerative diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthritis of the peripheral joints and spine, including radicular syndrome, tendovaginitis, bursitis);

    - neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine;

    - gynecological diseases accompanied by pain and inflammation, for example, primary algodismenorea, adnexitis;

    - in the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis). The main treatment of the disease is carried out in accordance with generally accepted principles, including,with the appointment of etiotropic therapy. Isolated fever is not an indication for the use of the drug.
    Contraindications:
    - hypersensitivity to the active substance and / or 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 (in t.ch. in the 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 (creatinine clearance (CK) less than 30 ml / min);
    - Decompensated heart failure;
    - early postoperative period after aortocoronary shunting;
    - active liver disease;
    - intolerance to galactose, lactase deficiency or glucose-galactose malabsorption syndrome;
    - confirmed hyperkalemia;
    - pregnancy (III trimester);
    - lactation period;
    - children's age (under 18 years).
    Carefully:
    With caution, the drug should be administered to patients:
    - with ulcerative lesions of the stomach or intestines, Helicobacter pylori infection, ulcerative colitis, Crohn's disease, liver function disorders in history, with complaints of gastrointestinal tract (GIT) diseases. The risk of developing 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, since the drug can provoke porphyria attacks;
    - with bronchial asthma, seasonal allergic rhinitis, edema of the nasal mucosa (including with nasal polyps), chronic obstructive pulmonary disease (COPD),chronic respiratory infections (particularly associated with allergic rhinitis-like symptoms);
    - with cardiovascular diseases (including ischemic heart disease, cerebrovascular diseases,
    compensated heart failure, peripheral vascular disease), impaired renal function including chronic renal failure (CK 30-60 mL / min), dyslipidemia / hyperlipidemia, diabetes mellitus, hypertension, treatment of smokers or alcohol abusers, 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, in periods 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 first and second trimester. Contraindicated in the use of diclofen in pregnant women during the III 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 diclofenac feeding mother, you should decide whether to stop breastfeeding.
    Dosing and Administration:
    The drug should be used in a minimally effective dose as little as possible. Take the inside of the pill completely, without chewing, squeezed with a small amount of water, during or after a meal. 1 tablet (100 mg) once a day. The maximum daily dose of the drug is 150 mg.

    To achieve a maximum daily dose of 150 mg, other forms of diclofenac sodium may be taken in a dose of 50 mg.

    With symptomatic treatment of dysmenorrhea, a single daily dose can be increased to 200 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 seemed possible.

    From the gastrointestinal side tract:

    often: nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, 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: stomatitis, glossitis, esophagitis, esophageal motility disorder, pancreatitis, intestinal stricture, nonspecific

    hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, exacerbation of hemorrhoids.

    From the nervous system:

    often: headache, dizziness;

    rarely: drowsiness;

    rarely: depression, irritability, aseptic meningitis (usually in patients with systemic lupus erythematosus and other systemic connective tissue diseases), weakness,disorientation, nightmarish dreams, a sense of fear, memory impairment, tremor, cerebrovascular disorders, impaired sensitivity (including paresthesia), seizures.

    From the senses: often: vertigo, coordination disorder;

    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.

    From the organs of hematopoiesis and the immune system:

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

    rarely: anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of the course of infectious processes (development of necrotizing fasciitis, pneumonia), angioedema (including Quincke's edema).

    From the respiratory system:

    rarely: cough, bronchospasm, laryngeal edema;

    rarely: pneumonitis.

    From the cardiovascular system:

    infrequently: myocardial infarction, chronic heart failure, palpitations and chest pain;

    rarely: increased blood pressure, vasculitis, extrasystole.

    From the skin:

    often: skin itching, skin rash; rarely: hives; rarely: erythema, bullous rashes, chronic dermatitis, eczema, polymorphic erythema, toxic epidermal necrolysis (Lyell's syndrome, Stevens-Johnson syndrome), photosensitivity, purpura, Henoch-Schönlein purpura, exfoliative dermatitis, alopecia, photosensitivity.

    From the hepatobiliary system:

    often: increased activity of "liver" transaminases;

    rarely: hepatitis, jaundice, dysfunction of the liver;

    rarely: hepatitis (fulminant possible), hepatic necrosis, cirrhosis, hepatorenal syndrome, hepatic failure.

    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: symptomatic therapy. Hemodialysis, forced diuresis and hemoperfusion are ineffective.When an overdose of the drug recommended gastric lavage and intake of adsorbents (Activated carbon).
    Interaction:

    Increases the concentration in the blood plasma digoxin, methotrexate, lithium and cyclosporine. When used simultaneously with diruetics and antihypertensive drugs (beta-adrenoblockers, ACE inhibitors) diclofenac can reduce their antihypertensive effect. Therefore, in patients, especially the elderly, with simultaneous application

    diclofenac and diuretics or antihypertensives should regularly monitor blood pressure, monitor kidney function and the degree of hydration (especially with a combination of diuretics and ACE inhibitors due to an increased risk of nephrotoxicity).

    Simultaneous application potassium-sparing diuretics increases the risk of hyperkalemia.

    On the background anticoagulants and thrombolytic agents the risk of bleeding increases (more often from the gastrointestinal tract).

    Increases toxicity methotrexate and nephrotoxicity cyclosporine and preparations of gold.

    Reduces effects hypotensive and hypnotics.

    Increases the likelihood of side effects of others NSAIDs (including selective COX inhibitors2) and glucocorticosteroids (in particular, from 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 effect. In some cases, it may affect the effectiveness of oral hypoglycemic agents, therefore it is recommended to control glucose sweating in the blood.

    Cefamandol, cefoperazone, cefotetan, valproic acid, and plikamycin increase the frequency of hypoprothrombinemia. The effect of diclofenac on the synthesis of prostaglandin in the kidneys can enhance toxic effects preparations of gold. Simultaneous application with ethanol, colchicine, corticotropin and preparations of St. John's wort perfumed increases the risk of bleeding in the gastrointestinal tract. Diclofenac enhances the effect of drugs that cause photosensitivity.

    Drugs that block canal secretion, increase the concentration of diclofenac in the blood plasma, thereby increasing its toxicity.

    With the simultaneous use of diclofenac and antibacterial drugs from the quinolone group the risk of seizures increases.

    When used simultaneously with inhibitors of isoenzyme CYP2C9 it is possible to increase the concentration of the drug in the blood plasma. When used simultaneously with derivatives phenytoin it is possible to enhance the effect of the drug.

    Special instructions:To reduce the risk of developing adverse events, a minimally effective dose of diclofenac should be used as short as possible course.

    Gastrointestinal tract (GIT) 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 those receiving low-dose acetylsalicylic acid therapy or other drugs that can increase the risk of gastrointestinal damage, should take gastroprotectors (for example, proton pump inhibitors or misoprostol). Patients with a history of gastrointestinal disease, especially the elderly, should be informed of the appearance of undesirable phenomena on the part 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 or renal insufficiency, and when treating elderly patients,

    taking diuretics, and patients who for some cause there is a decrease volume of circulating blood (for example, after surgery interventions). If in such cases appoint diclofenac, is recommended as a measure precautions, control kidney function.

    Impact on the system hematopoiesis

    Diclofenac temporarily inhibits aggregation of platelets, so patients with impaired blood coagulability is recommended regularly monitor relevant laboratory indicators.

    Patients with bronchial asthma

    In patients suffering from allergic rhinitis, nasal polyps, chronic obstructive pulmonary disease or

    chronic infectious respiratory diseases (especially those related to allergic rhino-like

    symptoms) most often noted intolerance of NSAIDs, A bronchial asthma, a quincke edema and hives. In this group patients, as well as in patients with allergy to other drugs (rash, itching, urticaria) with administration of the drug should be observe special care. Diclofenac affects the female fertility, therefore in patients with infertility (including passing examination) is recommended cancel the drug. Long-term therapy with diclofenac and therapy using high Doses can lead to an increase in risk of developing serious cardio- vascular thrombotic

    complications (including myocardial infarction myocardium and stroke). Diclofenac can mask symptoms of infectious- inflammatory diseases.

    Effect on the ability to drive transp. cf. and fur:Patients who have dizziness or other unpleasant sensations on the part of the nervous system, including visual impairment, should refrain from driving vehicles and practicing potentially dangerous activities that require increased attention and speed of psychomotor reactions.
    Form release / dosage:
    Long-acting tablets 100 mg.
    Packaging:
    For 10 tablets in a blister of PVC / aluminum or polypropylene / aluminum.

    By 1; 2; 3; 5 or 10 blisters together with instructions for use in a cardboard box.
    Storage conditions:
    At a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. 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 / 02
    Date of registration:01.02.2013
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp07.02.2016
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