Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspTablets of prolonged action, covered with enteric coating.
    Composition:

    Active substance: diclofenac sodium - 100.0 mg.

    Excipients (core): lactose monohydrate (milk sugar) 50.0 mg, hypromellose 95.0 mg, microcrystalline cellulose 53.0 mg, povidone (polyvinylpyrrolidone) 7.0 mg, talc 2.0 mg, magnesium stearate 3.0 mg.

    Auxiliary substances (shell): cellulose 8.0 mg, polysorbate 80 mg 3.0 mg, titanium dioxide 4.0 mg.

    Description:The tablets are round biconvex, covered with an enteric coating of white or almost white color. Surface roughness is allowed.
    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, antiplatelet and antipyretic effect.Indiscriminately inhibiting cycloxygenase 1 and cycloxygenase 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain.
    Pharmacokinetics:
    As a result of delayed release of the drug, Cmax (maximum concentration) in the plasma is lower than that produced by the administration of a short-acting drug; however, it remains high for a long time after administration. Сmах - 0.5-1 μg / ml, ТСmах (time of reaching the maximum concentration) -5 h after taking 100 mg of prolonged action tablets.

    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.

    Bioavailability - 50%. The connection with plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into breast milk, synovial fluid; Stax in the synovial fluid is observed 2-4 hours later than in the plasma. T1 / 2 (half-life) from synovial fluid - 3-6 hours (the concentration of the drug in the synovial fluid 4-6 hours after its administration is higher than in plasma, and remain higher for another 12 hours).

    50% of the drug is metabolized during the "first pass" through the liver; AUC (area under the concentration-time curve) is 2 times less after oral administration of the drug than after parenteral administration of the same dose. Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The isozyme CYP2C9 also participates in the metabolism of the drug. Pharmacological activity of metabolites is less than diclofenac.

    Systemic clearance is 260 ml / min. T1 / 2 from the plasma - 1-2 hours 60% of the administered dose is excreted as metabolites through 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, the pharmacokinetic parameters do not change.
    Indications:- Inflammatory and degenerative diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis,ankylosing spondylitis (Bekhterev's disease); gouty arthritis, osteochondrosis, deforming osteoarthritis of peripheral joints and spine, including with radicular syndrome, tendovaginitis, bursitis).

    The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

    - Pain: headache (including migraine headache) and dental pain, lumbago, sciatica, ossalgiya, neuralgia, myalgia, arthralgia, lumbago, in oncology, posttraumatic and postoperative pain, accompanied by inflammation.

    - Algodismenorea; inflammatory processes in the small pelvis, incl. adnexitis.

    - 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, auxiliary components and other non-steroidal anti-inflammatory drugs.

    - Complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or another non-steroidal anti-inflammatory drug (including in the anamnesis).

    - Erosive-ulcerative lesions of the gastrointestinal tract and duodenum.

    - Active gastrointestinal bleeding.

    - Inflammatory bowel disease (nonspecific ulcerative colitis, Crohn's disease).

    - Severe hepatic impairment; active liver disease.

    - Severe heart failure.

    - Conditions after aortocoronary bypass surgery.

    - Severe renal insufficiency (creatinine clearance less than 30 ml / min); progressive kidney disease.

    - Confirmed hyperkalemia.

    - Third trimester of pregnancy.

    - Children's age (up to 18 years).

    - Hereditary lactose intolerance, impaired absorption of glucose-galactose, deficiency of lactase.
    Carefully:
    Bronchial asthma, cerebrovascular disease, ischemic heart disease, chronic heart failure, hypertension, peripheral arterial disease, chronic renal failure (creatinine clearance of 30-60 ml / min), a history of liver disease, hepatic porphyria, dyslipidemia / hyperlipidemia, diabetes, a significant decrease in the volume of circulating blood (including after extensive surgical intervention).Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, prolonged use of non-steroidal anti-inflammatory drugs, alcoholism, smoking, severe physical illnesses.
    Elderly patients (including those receiving diuretics, weakened patients and with low body weight).
    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).
    In the I-II trimesters of pregnancy, the drug is used with caution.
    Pregnancy and lactation:
    Care should be taken when using the drug in the I-II trimesters of pregnancy.
    The use of the drug in the third trimester of pregnancy is contraindicated.
    If you need to use the drug during lactation, you should decide whether to stop breastfeeding.
    Dosing and Administration:
    Inside. Take during or after meals, without chewing, squeezed with enough water. Diclofenac prolonged action appoint 100 mg once 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.

    If you take 100 mg of prolonged-action tablets, if you need to increase the daily dose to 150 mg, you can additionally take 1 regular tablet (50 mg) of diclofenac.
    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 (vomiting with blood, melena, diarrhea with a trace of blood), ulcers of the gastrointestinal tract (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 urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

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

    From 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.

    Other: rarely - swelling.

    Overdose:

    Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, lethargy, convulsions, rarely - increased blood pressure, 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; against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) increases the 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 non-steroidal anti-inflammatory drugs and glucocorticosteroid agents (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, serotonin reuptake inhibitors and St. John's wort preparations increases the risk of bleeding in the gastrointestinal tract.

    Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to UV irradiation.

    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:
    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.

    Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised in appointing patients with cardiac or renal insufficiency, and also in the treatment of elderly patients taking diuretics and patients who for any reason have a decrease in circulating blood volume (in including 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.

    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.

    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. In case of an acute attack of gout, rapid-acting dosage forms are preferred.
    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,therefore 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:
    Tablets of prolonged action, covered with enteric coating 100 mg.
    Packaging:For 10, 20 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered. By 10, 20, 30, 40, 50 or 100 tablets into a polymer container for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 contour mesh packages together with the instruction for use are placed in a pack of cardboard.
    Storage conditions:3 years. Do not use the drug after the expiration date.
    Shelf life:Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-001592
    Date of registration:16.03.2012
    Date of cancellation:2017-03-16
    The owner of the registration certificate:OZONE, LLC OZONE, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp08.02.2016
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