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

    Diclofenac sodium - 0.05 g

    Excipients:

    propylene glycol - 0.05 g

    silicon dioxide colloid (aerosil) - 0.018 g

    hard fat - - 1.382 g
    Description:
    Suppositories white or white with a yellowish hue of color, torpedo-shaped.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.
    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 (COX-1 and COX-2), it breaks the metabolism of arachidonic acid, reduces the amount of prostaglandin (Pg) in the inflammatory focus. The most effective for inflammatory pain. Like all NSAIDs, the drug has antiplatelet activity.
    Pharmacokinetics:
    With rectal administration, the time to reach the maximum plasma concentration in the plasma (TCmax) is 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. Bioavailability - 50%. The connection with plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into breast milk, synovial fluid; the maximum concentration of the drug (C max) in the synovial fluid is observed 24 hours later than in the plasma. The half-life of the drug (T1 / 2) from the synovial fluid is 3-6 hours (the concentration of the drug in the synovial fluid 4-6 hours after its administration is higher than in the plasma, and remain higher for another 12 hours).

    50% of the drug 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 isozyme CYP2C9 also participates in the metabolism of the drug. Pharmacological activity of metabolites is less than diclofenac. Systemic clearance is 260 ml / min. Half-life 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, incl. rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), osteoarthritis, gouty arthritis (in case of an acute attack of gout, quick-acting dosage forms are preferred), bursitis, tenosynovitis.

    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.Infectious and inflammatory diseases of JIOP organs with severe pain syndrome (as part of complex therapy); pharyngitis, tonsillitis, otitis media.
    Contraindications:Hypersensitivity (including to other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other non-steroidal anti-inflammatory drugs (including in the history), erosive-ulcerative lesions of the gastrointestinal tract (GIT) and duodenum, active gastrointestinal bleeding, inflammatory bowel disease, severe hepatic and heart failure; period after aortocoronary shunting; severe renal failure (QC less than 30 ml / min), progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (III trimester), lactation period, children's age (under 14 years); proctitis.
    Carefully:Stomach ulcer and duodenal ulcer (in the anamnesis), ulcerative colitis, Crohn's disease without exacerbation; liver disease in history, hepatic porphyria, chronic heart failure (CHF), arterial hypertension, a significant decrease in the volume of circulating blood (bcc) (incl.after extensive surgical intervention), elderly patients (including those receiving diuretics, weakened patients and with low body weight), bronchial asthma, simultaneous reception of glucocorticosteroids (including PKN) (including prednisolone), anticoagulants (including (including ASC, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic heart disease (IHD), cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, diseases ne ifericheskih arteries, smoking, chronic renal failure (CRF) (CC 30-60 ml / min), the presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe somatic disorders, pregnancy (I and II trimesters).
    Pregnancy and lactation:
    The drug should not be used in the III trimester of pregnancy.
    Use in I and II trimesters is possible only after consultation with a doctor. Experience in using the drug during lactation is not available.
    Dosing and Administration:
    Rectally, the adults receive an initial dose of 100-150 mg / day, divided into 2-3 doses; in mild cases and with prolonged therapy - 75-100 mg / day; in addition to oral intake, the daily dose (rectally) 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 in the following days, the daily dose should not exceed 150 mg in several administrations. Children over 14 years - 1 suppository with a dosage of 50 mg to 2 times a day.
    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 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, exacerbation of hemorrhoids.

    From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity (including 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 marked reduction in blood pressure (BP) and shock; very rarely - angioedema (including face).

    From the side of the cardiovascular system (SSS): very rarely - a feeling of palpitation, chest pain, increased blood pressure, vasculitis, heart failure (CH), 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, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitization, 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 (BP), acute renal failure, hepatotoxic effect, respiratory depression, coma.

    Treatment: symptomatic therapy aimed at eliminating the increase in blood pressure, violations of kidney function, seizures, irritation of the gastrointestinal tract, respiratory depression; in case of erroneous oral administration of suppositories, gastric lavage is recommended, and activated charcoal is taken. Forced diuresis, hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
    Interaction:
    Increases the concentration in the plasma digoxin, lithium preparations.

    Reduces the effect of diuretics, against the background of potassium-sparing diuretics, the risk of developinghyperkalemia; on the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often the gastrointestinal tract). Reduces the effect of hypotensive and hypnotic drugs. Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroids (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine (due to an increase in their concentration in the plasma).

    ASA reduces the concentration of diclofenac in the blood. Reduces the effect of hypoglycemic drugs.

    Paracetamol increases the risk of developing nephrotoxic effects of diclofenac. 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 Pg in the kidneys, which is manifested by increased nephrotoxicity.

    Selective serotonin reuptake inhibitors increase the risk of bleeding from the gastrointestinal tract.

    Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract.

    Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.

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

    If during the reception of the drug the increase in the activity of the liver transaminases persists or increases, if clinical symptoms of hepatotoxicity (including nausea, fatigue, drowsiness, diarrhea, pruritus, jaundice) are noted, treatment should be stopped.

    Diclofenac (as well as other non-steroidal anti-inflammatory drugs) can cause hyperkalemia.

    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 are planning 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 ability to drive transp. cf. and fur:During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving transport and 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 are placed in a contour mesh package made of a polyvinyl chloride film.

    Two contour mesh packages 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 20 ° C. Keep out of the reach of children.
    Shelf life:
    2 years.

    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-001439
    Date of registration:15.06.2011
    The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp14.02.2016
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