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

    Tablet core composition:

    Active substance: diclofenac sodium - 50 mg

    Excipients: lactose 56.89 mg, calcium hydrophosphate 53.80 mg, povidone 6.28 mg, corn starch 23.90 mg,
    sodium carboxymethyl starch 11.1 mg, stearate 1.25 mg, talc purified 2.51 mg.

    The composition of the enteric film coating:

    Fell yellow:
    dye sunset sunset yellow (dye yellow No. 6) 11.5 mg
    dye iron oxide red 0.20 mg
    dye iron oxide yellow 0.20 mg titanium dioxide 2.5 mg
    Description:Round biconvex tablets with beveled edges from brown to light brown, covered with enteric film membrane.
    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, a derivative of phenylacetic acid.Has anti-inflammatory, analgesic 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 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 NSAIDs, the drug has antiaggregant activity.
    Pharmacokinetics:
    Absorption is fast and complete, food slows down the absorption rate. After oral administration of 50 mg the 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 administered dose. 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.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.

    Systemic clearance is about 260 +/- 50 ml / min, the volume of distribution is about 550 ml / kg. The half-life from the plasma averages about 2.5 hours. 65% 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 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, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.


    Indications:
    Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthritis of peripheral joints and spine, including 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, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache.

    With the composition of complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).
    Contraindications:
    - Period after aortocoronary bypass surgery;

    - III trimester of pregnancy, the period of breastfeeding;

    - Decompensated heart failure;

    - Hypersensitivity to the active substance or auxiliaries;

    - Anamnestic data on an attack of bronchial obstruction, rhinitis, hives after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);

    -Erosively ulcerous changes in the mucous membrane of the stomach or duodenum, active gastrointestinal hemorrhage;

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

    - Severe hepatic impairment or active liver disease;

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

    - Children's age (up to 15 years);

    - Hereditary lactose intolerance, impaired lactose absorption, severe lactase deficiency.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal failure, dyslipidemia / hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease, condition after extensive surgical interventions, induced porphyria, advanced age, diverticulitis, systemic connective tissue diseases, creatinine clearance less than 60 ml / min.

    Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illnesses.

    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). Pregnancy I-II trimester.
    Dosing and Administration:Inside, not liquid, during or after a meal, adults and adolescents over 15 years - 25-50 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 50 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 0.001%, 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, 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 side of 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 and shock; very rarely - angioedema (including face).

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

    On the part of the respiratory system, rarely - bronchial asthma (including dyspnea); very rarely - pneumonitis.

    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, seizures, increased blood pressure, respiratory depression, 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 (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 - anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract). Reduces the effects of hypotensive and hypnotics. Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (gastrointestinal bleeding), 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 agents.

    Cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin increase the frequency of hypoprothrombinemia. Cyclosporin 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, serotonin reuptake inhibitors and St. John's wort increases the risk of bleeding in the gastrointestinal tract. Diclofenac enhances the effect of drugs that cause photosensitivity.

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

    Effect on the results of laboratory tests: diclofenac may affect serum transaminase levels (if this effect is long-lasting or if complications occur, treatment should be discontinued), and may cause an increase in potassium concentration.
    Special instructions:
    In order to quickly achieve the desired therapeutic effect taken for 30 minutes. before meals. In other cases, take before, during or after eating, without chewing, squeezed with enough water.

    Because of the important role of Pg in maintaining renal blood flow, care should be taken when assigning to patients with cardiac or renal insufficiency, as well as in the treatment of elderly patients taking diuretics, and patients who for any reason have a decrease in BCC (incl. h after extensive surgery).

    If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

    In patients with renal insufficiency with CC less than 10 ml / min Css metabolites in plasma should theoretically be significantly higher than in patients with normal renal function, however this is not really observed, since in this situation the excretion of metabolites with bile is enhanced.

    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. 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.

    Care must be taken when combined with ACE inhibitors, beta-blockers; digoxin; when treating nephrotoxic drugs, zidovudine.

    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 other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions. To reduce the risk of developing adverse events on the part of the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

    Patients taking the drug should refrain from drinking alcohol.
    Form release / dosage:Tablets coated with enteric film coating 50 mg.
    Packaging:For 10 tablets in a blister of AL / PVC.1, 2 or 5 blisters together with instructions for use in a cardboard pack.
    Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° 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:P N013706 / 03-2002
    Date of registration:12.12.2008
    The owner of the registration certificate:Agio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspAgio Pharmaceuticals Ltd.Agio Pharmaceuticals Ltd.
    Information update date: & nbsp25.02.2016
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