Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspModified-release tablets.
    Composition:

    1 tablet with modified

    liberation contains active ingredient: for granules of enteric-soluble - diclofenac sodium 25 mg, for enteric-dissolution granules with sustained release - Diclofenac sodium 50 mg;

    Excipients: for

    granules of enteric-soluble corn starch 45,000 mg, lactose monohydrate 43,125 mg, sodium carboxymethyl starch 20,000 mg, acrylic from white (methacry) lactic acid and methyl methacrylate copolymer [1: 1], talc, titanium dioxide, triethyl citrate, silicon dioxide colloid, sodium bicarbonate, sodium lauryl sulfate) - 15,000 mg; simethicone [emulsion 30%] - 0.075 mg, magnesium stearate - 1,000 mg, silicon colloidal dioxide - 0,800 mg; for enteric-dissolution granules with sustained release corn starch - 40,000 mg, lactose monohydrate 37.370 mg, sodium carboxymethyl starch 20,000 mg, acrylic from white (methacrylic acid and methyl methacrylate copolymer [1: 1], talc, titanium dioxide, triethyl citrate, silicon dioxide colloid, sodium hydrogen carbonate ,sodium lauryl sulfate) - 20,000 mg; Simethicone [emulsion 30%] - 0.100 mg, hypromellose 30,000 mg, magnesium stearate 1,200 mg, silicon colloidal dioxide 1,000 mg, aluminum dye-based lacquer sunset yellow [E110] 0.330 mg.

    Description:Round, biconcave, two-layer tablets, one layer of orange, the second - from white to yellowish white, with small impregnations of white and orange on orange and white layers of tablets, respectively.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:
    Non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid. Diclofenac has anti-inflammatory, analgesic, antiplatelet and antipyretic effect. By indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain.

    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.
    Pharmacokinetics:
    The drug Rapten Duo is a form of diclofenac (sodium salt) in the form of two-layer tablets.

    After oral administration diclofenac quickly and completely absorbed from the gastrointestinal tract. After taking a single dose - the maximum concentration in the plasma is achieved in 20-60 minutes due to 25 mg of diclofenac from the first acid-resistant layer. From the second layer slowly released 50 mg of diclofenac for 6 or more hours, which provides a lasting effect (12-24 hours). 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. With plasma proteins, 99% of the applied dose binds, the drug is well distributed in tissues and tissue fluids. Penetrates into the synovial fluid; The joints in the synovial fluid are observed 2-4 hours later than in the plasma. The half-life (T [L]) of the synovial fluid is 3-6 h (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 h).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. Systemic clearance is about 260 ± 50 ml / min, the volume of distribution is 550 ml / kg. T1 / 2 from the plasma averages about 2.5 hours. 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% excreted unchanged in the rest of the dose (less than 35%) is excreted as metabolites in the bile.

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

    The drug passes through the blood-brain and the placental barrier, and a small amount excreted in the milk.
    Indications:
    - Symptomatic treatment of diseases of the musculoskeletal system (incl.rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Bekhterev's disease); gouty arthritis, osteoarthrosis of peripheral joints and spine, including with radicular syndrome, tendovaginitis, bursitis;

    The drug removes or reduces pain and inflammation during the treatment period, without affecting the progression of the disease;

    - Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumbago, sciatica, ossalgia, post-traumatic and postoperative pain syndrome, accompanied by inflammation, pain in cancer, headache, migraine, algodismenorea, adnexitis, toothache;

    - In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).
    Contraindications:
    - Hypersensitivity to the active substance (including other NSAIDs) or ancillary components.

    - Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in the anamnesis).

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

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

    - The period after aortocoronary bypass surgery.

    - III trimester of pregnancy, the period of breastfeeding.

    - Decompensated heart failure.

    - Violations of hematopoiesis, hemostasis disorders (including hemophilia).

    - Severe hepatic impairment or active liver disease.

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

    - Children under 18 years.

    - Patients with rare hereditary diseases, such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption, should not take the drug.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency (KC 30-60 ml / min),a history of liver disease, dyslipidemia / hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease, a significant decrease in the volume of circulating blood (including after extensive surgery), hepatic porphyria, diverticulitis, systemic connective tissue diseases, pregnancy I-II trimester .

    Stomach ulcer and duodenal ulcer (including history), presence of Helicobacter pylori infection, elderly patients (including those receiving diuretics, weakened patients and low-body weight), 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).
    Dosing and Administration:
    Inside, without chewing, during or after a meal, with enough liquid.

    The daily dose for adults is 75 mg (1 tablet of the drug).

    The maximum daily dose is 150 mg (1 tablet 2 times a day - preferably the first

    tablet before breakfast, and second after 12 hours).

    To reduce the risk of developing adverse events from the gastrointestinal tract (GIT), a minimum effective dose should be used with the minimum possible short course.
    Side effects:Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.001%, 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 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, 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, night "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.

    On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, 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 - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction. From the respiratory system: rarely - exacerbation of bronchial asthma, dyspnea; very rarely - pneumonitis.

    From the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, erythema including. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

    Other: rarely - swelling.

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

    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 (due to the significant connection 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 agents (alteplase, streptokinase, urokinase) - risk of bleeding (more often from the gastrointestinal tract).Reduces the effects 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, selective serotonin reuptake inhibitors and St. John's wort increases the risk of bleeding in the gastrointestinal 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 diclofenac take 30 minutes before meals. In other cases, take before, during or after eating, without chewing, squeezed with enough water.

    Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful when administered to patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, decrease in circulating blood volume is observed (eg , 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), the 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.

    If the increase in the activity of "liver" transaminases persists or increases during the administration of the drug, if clinical symptoms of hepatotoxicity (including nausea, fatigue, drowsiness, diarrhea, pruritus, jaundice) are noted, treatment should be discontinued.

    Diclofenac (like other NSAIDs) can cause hyperkalemia. 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.

    Patients taking the drug should refrain from drinking alcohol.
    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 driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Modified release tablets 75 mg.
    Packaging:
    For 10 tablets in a blister of PVC / AJT. For 3 blisters, together with instructions for use, put in a pack of cardboard.
    Storage conditions:
    For 10 tablets in a blister of PVC / AJT. For 3 blisters, together with instructions for use, put in a pack of cardboard.
    Shelf life:
    3 years.

    Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-003038/10
    Date of registration:09.04.2010
    The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia
    Manufacturer: & nbsp
    Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia
    Information update date: & nbsp17.02.2016
    Illustrated instructions
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