Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSuppositories rectal.
    Composition:
    Active component
    Diclofenac sodium - 50 mg

    Auxiliary component
    Solid fat (suppository base) - until a suppository with a mass of 1.50 g
    Description:
    Suppositories white or white with a slightly yellowish hue of color, odorless, torpedo-shaped; On the cut, an air rod or a funnel-shaped depression 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 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 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 system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. Half-life from the plasma - 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:
    Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthritis of peripheral joints and spine, including radicular syndrome, tendovaginitis, bursitis). Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache.

    In the 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;

    - Uncompensated heart failure;

    - Hypersensitivity to the active substance or ancillary components;

    - Anamnestic data on the seizure of bronchial obstruction, rhinitis,

    urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);

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

    - Inflammatory bowel disease (nonspecific 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),
    Carefully:
    Anemia, asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, hypertension, peripheral artery disease, edema syndrome, liver or kidney failure, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, condition after major surgery, induced porphyria, advanced age, diverticular disease, systemic connective tissue disease, creatinine clearance less than 60 mL / min, beremennos s (I-II trimester). A history of the development of ulcerative diseases of the gastrointestinal tract, the presence of infection Helicobacter pylori, long-term use of NSAIDs, 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 serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:Rectally, the adult initial dose of 100 mg / day, divided into 2 doses; in mild cases and with prolonged therapy - 50 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 -repeatedly 100 mg. If it is necessary to continue treatment in the following days, the daily dose should not exceed 150 mg for several administrations. In adolescents over 15 years - no more than 1 suppository.
    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, damage to the esophagus,diaphragm-like intestinal textures (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, 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 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.

    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.

    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, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

    Treatment: Activated carbon, 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 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 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 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. 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:
    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 (for example , after a major 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.

    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:Diclofenac-MFF suppositories rectal 50 mg.
    Packaging:By 5 suppositories in a contour mesh package made of PVC film. Two contoured cell packs, along with instructions for medical use, are placed in a pack of cardboard.
    Storage conditions:
    Store at a temperature not exceeding +20 ° C.

    Keep out of the reach of children.
    Shelf life:2 years. Do not use the drug after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N000061 / 01
    Date of registration:18.04.2008
    The owner of the registration certificate:MOSCOW PHARMACEUTICAL FACTORY, CJSC MOSCOW PHARMACEUTICAL FACTORY, CJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp05.03.2016
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