Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsptablets, coated with enteric film coating
    Composition:

    1 tablet contains:

    CORE:

    Active substance:

    Diclofenac sodium 50.00 mg

    Excipients:

    Lactose Monohydrate 40.00 mg

    Corn starch 57.00 mg

    Microcrystalline cellulose 40.00 mg

    Povidone 4.00 mg

    Silicon dioxide colloidal, anhydrous 2.00 mg

    Magnesium stearate 2.00 mg

    Intestinal Shell:

    Hypromellose 2.00 mg

    Iron colorant oxide red, E172 0.02 mg

    Iron coloring agent yellow, E172 0.43 mg

    Titanium dioxide 0.23 mg

    Methacrylic acid - ethyl acrylate

    copolymer 20.00 mg *

    Propylene glycol 0.60 mg

    Talc 1.90 mg

    * corresponds to 6.00 mg of dry matter

    Description:
    Round, slightly biconcave, smooth tablets covered with enteric-curable film coat of brownish-yellow color.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:

    Diclofenac sodium is a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects.

    The main mechanism of its action and associated side effects are indiscriminate inhibition of the activity of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2), which leads to a disruption of the metabolism of arachidonic acid, a decrease in the synthesis of prostaglandins, prostacyclin and thromboxane. The level of various prostaglandins in urine, gastric mucosa and synovial fluid decreases. The most effective for inflammatory pain. 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 (NSAIDs), diclofenac has antiaggregant activity. In therapeutic doses diclofenac sodium has virtually no effect on bleeding time. With prolonged treatment, the analgesic effect of diclofenac sodium does not decrease.

    Pharmacokinetics:

    Absorption - fast and complete, the food slows the absorption rate for 1 to 4 hours and reduces the maximum concentration by 40%. After oral administration, 50 mg maximum concentration (Cmax) - 1.5 μg / ml is achieved after -2-3 hours. The concentration in the plasma is linear depending on the amount of the dose taken. 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 the 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 remains higher for another 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug has not been elucidated.

    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 P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac. The systemic clearance is 260 ml / min, the volume of distribution is 550 ml / kg. The half-life of plasma is 2 hours. About 70% of the administered dose is excreted as pharmacologically inactive 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 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, as well as elderly patients, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.

    Indications:

    - Inflammatory and degenerative diseases of the musculoskeletal system:rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis, arthritis in Reiter's disease, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine, including with radicular syndrome, tendosygonitis, periarthritis, bursitis, myositis, synovitis).

    - Pain syndrome weak or moderate severity: neuralgia, myalgia, sciatica, post-traumatic pain, accompanied by inflammation, postoperative pain, headache, migraine, tuberculosis, adnexitis, proctitis, toothache, renal and biliary colic.

    - In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).

    - Feverish syndrome.

    Diclofenac is intended for symptomatic therapy and does not affect the progression of the disease.

    Contraindications:

    - Hypersensitivity to diclofenac; with anamnestic data fit bronchial, rhinitis, urticaria, after receiving aspirin or other nonsteroidal anti-inflammatory drug (NSAID) (complete or incompletesyndrome intolerance of acetylsalicylic acid - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma).

    - The period after aortocoronary bypass surgery.

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

    - Inflammatory bowel disease, in the phase of exacerbation (Nonspecific ulcerative colitis (NJC), Crohn's disease).

    - 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), including confirmed hyperkalemia, progressive kidney disease.

    - Decompensated heart failure.

    - Inhibition of bone marrow hematopoiesis.

    - III trimester of pregnancy, the period of breastfeeding.

    - This dosage form is contraindicated in children weighing less than 45 kg (or under 15 years of age).

    Carefully:Ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking,creatinine clearance less than 60 ml / min; medical history of the development of ulcerative lesions of the gastrointestinal tract, the presence of infection Helicobacter pylori, old age, long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs), frequent alcohol consumption, severe somatic diseases induced porphyria, epilepsy, elderly, diverticular disease, systemic connective tissue disease , a significant reduction in circulating blood volume (CBV) (including after massive surgery), elderly patients (including receiving iuretiki weakened patients with low body weight), concomitant therapy following drugs: anticoagulant (e.g., warfarin), antiplatelet agents (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticoids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline). To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as little as possible.
    Pregnancy and lactation:The use of diclofenac in pregnant women is possible only when the expected benefit exceeds the potential risk to the fetus. Diclofenac it is not recommended to use during the last trimester of pregnancy. Although diclofenac is found in breast milk in small amounts, its use during breastfeeding is not recommended.
    Dosing and Administration:Inside, without chewing, during or after a meal, with a small amount of water. Adults and adolescents with 15 years (and weighing more than 45 kg) - 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 100 mg / day. The maximum daily dose is 150 mg.
    Side effects:

    Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.01%, including individual cases.

    From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely - gastritis, proctitis, bleeding from the gastrointestinal tract (gastrointestinal tract) (vomiting with blood, melena, diarrhea with an admixture of blood),Gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rarely - stomatitis, glossitis, dryness of the mucous membranes (including the mouth), damage to the esophagus, diaphragm-like bowel strains (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis.

    From the nervous system: often - headache, dizziness; rarely - 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: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

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

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

    From the cardiovascular system: very rarely - palpitation, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

    From the respiratory system: rarely - cough, bronchial asthma (including dyspnea); very rarely - pneumonitis, laryngeal edema.

    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.

    Overdose:
    Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, convulsions, with a significant overdose - acute renal failure, hepatotoxic effect.

    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 (significant association with proteins and intensive metabolism).
    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 (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often the gastrointestinal tract).

    Reduces the effect of hypotensive and hypnotic drugs. Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (bleeding from 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 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.

    Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation. Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

    Antibacterial drugs from the quinolone group - the risk of seizures.

    Special instructions:

    In order to quickly achieve the desired therapeutic effect, take the drug for 30 minutes. before meals. In other cases, take before, during or after a meal wholly, with plenty of water.

    To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

    Caution should be used for ulcerative colitis and Crohn's disease because of a possible exacerbation of the disease.

    With long-term use of diclofenac, it is possible, although in rare cases, the development of serious hepatotoxic reactions, and therefore it is recommended to regularly examine the function of the liver.

    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, as well as in the treatment of elderly people taking diuretics and patients who for any reason have a decrease in circulating blood volume (for example , after a major surgical intervention). If in such cases appoint diclofenac, it is recommended as a precaution to monitor kidney function.

    Caution should be given diclofenac in patients with disorders of blood coagulation, porphyria, epilepsy, as well as in patients receiving anticoagulants or fibrinolytics.

    When carrying out long-term therapy, it is necessary to monitor the picture of peripheral blood, to conduct a fecal occult blood test.In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended. In patients with infertility (including undergoing examination) it is recommended to cancel the drug. Patients taking the drug should refrain from drinking alcohol.

    In infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac sodium can mask the symptoms of these diseases.

    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 engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Tablets coated with enteric film coating, 50 mg.
    Packaging:10 tablets in a blister pack. 2 blisters per cardboard pack together with instructions for use.
    Storage conditions:
    Store in a dry place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:

    5 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013166 / 03
    Date of registration:14.03.2008 / 28.10.2013
    Expiration Date:Unlimited
    Date of cancellation:2017-08-29
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    KRKA, d.d. Slovenia
    Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Information update date: & nbsp28.05.2018
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