Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSuppositories rectal.
    Composition:
    1 suppository contains
    Active ingredient: Diclofenac sodium - 100 mg
    Excipients: semi-synthetic glycerides

    Description:Suppositories white or almost white with a grayish or yellowish tint of torpedo shape with a smooth oily surface.
    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. By indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain.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. Like all NSAIDs, the drug has antiaggregant activity.
    Pharmacokinetics:When rectal administration, TCmax is 0.5-2 hours, the maximum concentration is about 1.5 mg / ml on average. 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, the drug does not cumulate under the recommended interval between doses food.

    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: 50% of the active substance 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 enzyme system P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac. Systemic clearance is about 350 ml / min, the volume of distribution is about 550 ml / kg. The half-life from the plasma averages about 2.5 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.

    In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters do not change.
    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). The drug removes or reduces pain and inflammation during the treatment period, without affecting the progression of the disease.

    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 an attack of bronchial obstruction, rhinitis, hives 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), progressive kidney disease, incl. confirmed hyperkalemia.

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

    - Rectal bleeding, hemorrhoids, trauma or inflammation of the rectum.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure, hypertension,peripheral artery disease, edema syndrome, hepatic or renal 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.

    Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illnesses.

    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. Adults before using the suppository are recommended to relieve the intestines.

    Usually, one suppository is used in the evening as a single daily dose. The maximum daily dose is 150 mg.

    It is advisable to share with oral forms of diclofenac as the last dose of daily treatment instead of oral administration. For example, if the daily dose is 150 mg, one tablet of 50 mg is administered orally throughout the day and one suppository rectally in the evening (overnight).

    At a migraine attack - one suppository of 100 mg at the first signs of an attack. The duration of use of the drug is not more than 7 days.
    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 side of 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, damages of the esophagus, diaphragmatic 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: 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 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: vomiting, dizziness, headache, shortness of breath, blurred vision, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function. Treatment: cleansing enema; with occasional oral administration: gastric lavage, administration of activated charcoal, symptomatic therapy, forced diuresis.

    Hemodialysis is ineffective.

    In case of overdose, it is necessary to consult a doctor immediately.
    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.

    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.

    Antibacterial drugs from the quinolone group - the risk of seizures.
    Special instructions:
    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. With prolonged treatment, it is necessary to monitor the functions of the liver and kidneys. Caution is necessary in surgical interventions, since there is a high risk of bleeding: diclofenac inhibits platelet aggregation. In cases of renal and hepatic insufficiency, only small doses should be used, since the level of excretion of the drug is lower.

    When using the drug, the risk of toxic gastrointestinal reactions increases.In patients with hypersensitivity to acetylsalicylic acid diclofenac can lead to bouts of bronchial asthma.

    Care must be taken when combined with ACE inhibitors, beta-blockers; digoxin; when treating nephrotoxic drugs, zidovudine.

    When using the drug, it is necessary to refrain from activities requiring increased attention and rapid mental and motor reactions, since the drug can affect the central nervous system. Patients taking the drug should refrain from drinking alcohol.

    In connection with the negative impact on fertility, women who want to become pregnant, the drug is not recommended.
    Form release / dosage:
    Suppositories rectal by 100 mg.
    Packaging:
    3 or 5 suppositories in a PVC blister. 2 blister along with instructions for use in a cardboard pack.
    Storage conditions:In dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children!
    Shelf life:
    3 of the year.

    Do not use after the expiry date printed on the package!
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-008646/08
    Date of registration:30.10.2008
    The owner of the registration certificate: Magister KiK Magister KiK Romania
    Manufacturer: & nbsp
    Representation: & nbspРомфарма ОООРомфарма ООО
    Information update date: & nbsp26.02.2016
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