Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsp
    Capsules with modified release.

    Composition:

    1 capsule contains:

    - Intestinal soluble pellets:

    Active substance: diclofenac sodium 25 mg

    Excipients: sugar spheres (sugar content not more than 92%), giprolase (hydroxypropylcellulose), hypromellose, magnesium carbonate, heavy, methacrylic acid and ethyl acrylate copolymer (1: 1) 30% dispersion, triethyl citrate, talc, titanium dioxide, sodium carboxymethylcellulose, macrogol, sodium hydroxide.

    - Pellets with prolonged release:

    - Active substance:

    diclofenac sodium 50 mg

    Excipients: sugar spheres (sugar content not more than 92%), giprolose (hydroxypropyl cellulose), ammonium methacrylate copolymer, Type B, ammonium methacrylate copolymer, Type A, triethyl citrate, talc.

    - Composition of the contents of the capsule:

    water-soluble pellets,pellets with prolonged release, talc (0.2% talc mixed with pellets before filling into capsules, talc prevents the appearance of electrostatic charge of pellets during the filling of capsules).

    - Capsule shell composition:

    BODY Capsule: gelatin EP, titanium dioxide (E171);

    Lid capsules: gelatin EP, titanium dioxide (E171), dye indigo carmine FD&C Blue2 (E132).

    Description:Capsules number 2, filled with pellets from white to yellowish color. The body of the capsule is white, the cap of the capsule is blue.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    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 is fast and complete. Diclofenac is contained in capsules of Naklofen Duo in the form of enteric-soluble pellets and pellets with prolonged release, therefore Naklofen Duo capsules have an immediate and prolonged effect. The maximum concentration in plasma is noted 30-60 minutes after administration. The therapeutic concentration is maintained twice as long as when using tablets,coated with an enteric film coating. 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. Diclofenac It is more slowly excreted from the synovial fluid than from the plasma.

    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 radicular syndrome , tendovaginitis, periarthritis, bursitis, myositis, synovitis).

    - Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, 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; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis).

    - 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.

    - Children's age (up to 18 years).
    Carefully:Ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min; anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, the elderly, the long-term use of non-steroidal anti-inflammatory drugs (NSAIDs), frequent alcohol use, severe physical illnesses, induced porphyria, epilepsy, advanced age, diverticulitis, systemic connective tissue diseases , a significant decrease in the volume of circulating blood (BCC) (including after massive surgical intervention), elderly patients (appointed to a lower doses) (including those receiving diuretics, weakened patients and low body weight), pregnancy I-II trimester, concomitant therapy with the following drugs: anticoagulants (for example, 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, the capsule should be swallowed whole, washed down with water at the end or after eating, usually in the mornings. Assigned individually, taking into account the severity of the disease. Adults usually appoint 1 capsule 75 mg 1 -2 times a 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, abdominal cramps, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity aminotransferase; rarely - gastritis, bleeding from the gastrointestinal tract (GIT) (vomiting blood, melena, bloody diarrhea), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, liver dysfunction; very rarely - stomatitis, glossitis, dryness of mucous membranes (including the mouth), oesophageal damage diafragmopodobnye bowel strictures (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 disturbances, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, confusion, depression, insomnia, night "nightmares", irritability, agitation, 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 side of the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis, edema.

    On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, eosinophilia, hemolytic and aplastic anemia, agranulocytosis.

    Allergic reactions: anaphylactic / anaphylactoid reactions, including marked reduction in blood pressure (BP) and shock; very rarely - angioedema (including face). The drug contains methyl parahydroxybenzoate and propyl parahydroxybenzoate, which can cause allergic reactions.

    From the side of the cardiovascular system: very rarely - palpitation, tachycardia, 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, skin itching, hair loss, photosensitivity, purpura, incl. allergic.

    Overdose:
    Symptoms: vomiting, nausea, abdominal pain, bleeding from the gastrointestinal tract, diarrhea, headache, dizziness, tinnitus, increased excitability, hyperventilation with W increased convulsive readiness, convulsions, with a significant overdose acute renal failure, hepatotoxic act.
    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, etc.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.

    Hypoglycemic agents - hypo- or hyperglycemia can be observed. With this combination of funds, blood sugar levels need to be monitored;

    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 W 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.

    The amount of sucrose contained in the preparation does not affect patients with the following conditions: lactase enzyme deficiency, galactosemia, and glucose / galactose uptake syndrome.
    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:Capsules with a modified release of 75 mg.
    Packaging:10 capsules in a five-layer film blister. Two blisters are placed in a pack of cardboard together with instructions for use.
    Storage conditions:
    Store at a temperature not exceeding 30 ° C. Keep out of the reach of children.

    Shelf life:
    3 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N014288 / 01
    Date of registration:17.06.2008
    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: & nbsp04.03.2016
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