Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSuppositories rectal.
    Composition:
    Active substance:

    sodium diclofenac - 50 mg

    Excipients:

    Macrogol 400 (polyethylene oxide 400) - 0.1 g, solid fat - a sufficient amount to obtain a suppository with a mass of 2.0 g.
    Description:Suppressor torpedo shape from white to white with a creamy shade of color.
    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. 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. Like all non-steroidal anti-inflammatory drugs, the drug has antiplatelet activity.
    Pharmacokinetics:
    The maximum concentration in the blood plasma is created after 30-40 minutes and is in linear dependence on the used dose. Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted, do not accumulate.

    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 occurs as a result of multiple or single

    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 system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. The half-life of plasma is 2 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:
    Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic arthritis, spondylitis; gouty arthritis, rheumatic damage, soft tissues, osteoarthrosis 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 syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic, pain syndrome accompanied by inflammation, postoperative pain, 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:
    - The period after aortocoronary shunting;

    - III trimester of pregnancy, the period of breastfeeding;

    - Uncompensated heart failure;

    - Hypersensitivity to the active substance or ancillary components (including other NSAIDs);

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

    - Erosive-ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal hemorrhage;

    - Inflammatory bowel disease in the stage of exacerbation (ulcerative colitis, 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), progressive kidney disease, including confirmed hyperkalemia;

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

    - Rectal bleeding, hemorrhoids, trauma or inflammation of the rectum.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure, hypertension; peripheral arterial disease, edematous syndrome, liver disease in history, hepatic or renal insufficiency (creatinine clearance 30-60 ml / min), dyslipidemia / hyperlipidemia, diabetes, smoking, a significant decrease in BCC (including after extensive surgery) , elderly patients (including, receiving diuretics, weakened patients and low body weight), induced porphyria, systemic connective tissue diseases, pregnancy (I-II trimester).

    Ulcerative colitis, Crohn's disease is beyond aggravation; anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, prolonged use of non-steroidal anti-inflammatory drugs, frequent alcohol consumption, severe somatic diseases.

    Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective inhibitors of reuptake, serotonin (for example, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:Rectally, adults and adolescents over 15 years of age receive a single dose of 50 mg, a daily dose of 100-150 mg; in mild cases and with prolonged therapy -50-100'mg / day; in addition to oral administration, the total daily dose (rectally and orally) should not exceed 150 mg. With algodismenosis (with the appearance of the first symptoms) the initial dose is 50-100 mg / day, which, if necessary, is increased for several menstrual cycles to 150 mg. A migraine attack is 100 mg at the first signs of an attack. If necessary, repeat 100 mg. If it is necessary to continue treatment, the following days the daily dose should not exceed 150 mg for several administrations.
    Side effects:

    Often - 1-10%; sometimes 0.1-1%; rarely 0.01-0.1%; very rarely - less, 0.001%, including individual cases.

    From the digestive side. 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 mixed with blood), gastrointestinal ulcers (with or without bleeding or perforation g), hepatitis, jaundice, liver dysfunction; very rarely - stomatitis, glossitis, -Damage esophagus, bowel strictures diafragmopodobnye (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis, exacerbation of hemorrhoids.

    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, personality disorders.

    From the sense organs: often - vertigo; very rarely - blurred vision (blurred vision, diplopia), impaired hearing, tinnitus, taste disturbance.

    From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

    On the part of the blood-forming organs: 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, the cardiovascular system: very rarely - palpitations, chest pain, increased blood pressure; vasculitis, heart failure, myocardial infarction.

    Co 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.

    Local reactions with rectal administration: irritation of the mucous membrane of the rectum, mucous discharge with an admixture of blood, pain during defecation, rectal bleeding.

    Overdose:
    Symptoms: dizziness, headache, hyperventilation of the lungs, and confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.
    Treatment: symptomatic therapy.Forced diuresis, hemodialysis are ineffective.
    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) - 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 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 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 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.
    Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.
    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.
    Antibacterial drugs from the quinolone group - the risk of seizures.
    Special instructions: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, is recommended as a precautionary measure to monitor kidney function.

    In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis of the liver), 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.

    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.

    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.
    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:Suppositories rectal 50 mg.
    Packaging:5 suppositories per contour cell package. Two contour packs together with the instruction for use are placed in a pack of cardboard.
    Storage conditions:In a dry, dark place at a temperature of no higher than 15 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use the product after the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-000928
    Date of registration:18.10.2011
    Date of cancellation:2016-10-18
    The owner of the registration certificate:ALTAYVITAMINS, CJSC ALTAYVITAMINS, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp10.02.2016
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