Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSuppositories rectal.
    Composition:Active substance: diclofenac sodium-25 mg, 50 mg or 100 mg
    Excipient: Solid fat (fatty acid glycerides) - 0.975 g, 1.95 g or 1.9 g
    Description:Suppositories from white to white with a yellowish hue of color, torpedo shape without visible inclusions on the longitudinal section.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Diclofenac has anti-inflammatory, analgesic and antipyretic effects. Indiscriminately inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. 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.
    Pharmacokinetics:
    Absorption is fast and complete. The maximum concentration of the drug is reached after 30 minutes. 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 accumulate.

    Bioavailability - 50%. The connection with plasma proteins is 95-98% (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. 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 diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile and chronic arthritis, ankylosing spondylitis, gouty arthritis).

    Degenerative diseases of the musculoskeletal system (deforming osteoarthritis, osteochondrosis). Lumbago, sciatica, neuralgia, myalgia.

    Diseases of extraarticular tissues (tendovaginitis, bursitis, rheumatic soft tissue damage).

    Post-traumatic pain syndromes, accompanied by inflammation,postoperative pain, migraine, renal or biliary colic; primary algodismenorea, adnexitis, proctitis. Feverish syndrome.

    NSAIDs are intended for symptomatic therapy, reducing pain and inflammation at the time of use, and the progression of the disease is not affected.
    Contraindications:
    - period after aortocoronary shunting;

    - III trimester of pregnancy, the period of breastfeeding;

    - Children under 6 years of age (for suppositories of 50 mg to 15 years, suppositories of 100 mg for children do not use);

    - hypersensitivity to the active substance or ancillary component;

    - anamnestic data on an attack 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;

    - severe hepatic impairment or active liver disease;

    - severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease;

    - confirmed hyperkalemia;

    - hemorrhoids.
    Carefully:
    I-II trimester of pregnancy, ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min.

    Anamnestic data on the development of ulcerative lesions of the digestive tract, the presence of Helicobacter pylori infection, prolonged use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs:

    - anticoagulants (eg, warfarin)

    - antiaggregants (eg, acetylsalicylic acid, clopidogrel)

    - oral glucocorticosteroids (eg, prednisolone)

    - selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline)

    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.
    Dosing and Administration:
    The drug is used rectally (injected into the rectum). To remove the suppository from the cell package, one cell with the suppository must be broken off by notching and disconnecting the edges of the tape,pull for them in different directions. The suppository should be inserted into the anus with a pointed end, as deep as possible. For a more convenient introduction of the suppository, it is recommended to bend down, squat or lie on one side, with your legs tucked.

    Suppositories with a dosage of 100 mg adults once a day.

    Suppositories with a dosage of 50 mg adults 2 times a day, children over 15 years 1 time per day.

    Suppositories with a dosage of 25 mg adults 3-4 times a day, children over 12 years 2 times a day, children over 6 years 1 time per day.
    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 - nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely - gastritis, proctitis, gastrointestinal bleeding, gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rarely - stomatitis, glossitis, diaphragm-like intestinal sticures (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: often - fluid retention, very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis, oliguria, azotemia.

    From the hematopoiesis: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis, eosinophilia, thrombocytopenic purpura, worsening of the course of infectious processes (development of necrotizing fasciitis.

    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 - cough, bronchospasm, bronchial asthma (including dyspnea); very rarely - edema of the larynx, pneumonitis.

    From the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, toxic dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic, small-point hemorrhage.

    Overdose:
    Symptoms: vomiting, dizziness, headache, dyspnea, confusion, in children - myoclonic cramps, nausea, abdominal pain, bleeding, impaired liver and kidney function.

    Treatment: the introduction of activated charcoal, symptomatic therapy, forced diuresis.

    Hemodialysis is 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; on 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 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 agents.

    Cefamandol, cefoperazone, cefotetan, valproic acid th 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.

    Simultaneous administration with antibacterial drugs from the quinolone group increases the risk of seizures.
    Special instructions:During the treatment with the drug should be a systematic control of the picture of peripheral blood, liver function, kidneys, examination of feces for the presence of blood.
    Patients who use the drug should refrain from activities that require increased concentration of attention and rapid mental and motor reactions, alcohol consumption.
    Form release / dosage:Suppositories rectal 25 mg, 50 mg, 100 mg.
    Packaging:There are 5 suppositories in a contiguous cell package. 2 contour mesh packages together with instructions for use in a pack of cardboard.
    Storage conditions:List B. In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:2 years and 6 months. Do not use after expiry date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N002096 / 01
    Date of registration:23.07.2008
    The owner of the registration certificate:ALTFARM, LLC ALTFARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp26.02.2016
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