Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSuppositories rectal.
    Composition:
    1 suppository contains:

    active substance: diclofenac sodium - 50 mg or 100 mg;

    excipients: solid fat - 1098.5 mg or 1030.0 mg.
    Description:White or white with a yellowish hue, torpedo-shaped suppositories with a smooth surface. The longitudinal section is homogeneous, there are no inclusions.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Diclofenac, a derivative of phenylacetic acid, has an anti-inflammatory, analgesic and antipyretic effect. 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, and also improves the functional state of the joint. With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling. Diclofenac also has antiaggregant activity.
    Pharmacokinetics:With rectal administration of 50 mg, the maximum concentration in the blood plasma is 1.0 μg / ml, reached after 30-40 min and is linear depending on the dose used. Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted, do not accumulate. Bioavailability - 50%. The connection with blood plasma proteins is more than 99.7% (mainly with albumins). The volume of distribution is 0.12-0.17 l / kg. Penetrates into synovial fluid (the maximum concentration in the synovial fluid is reached 2 to 4 hours later than in the blood plasma, and remains higher, even for 12 hours). Metabolized as a result of multiple or single hydroxylation and conjugation with glucuronic acid. The isozyme CYP2C9 is involved in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.
    Systemic clearance is 263 ± 56 ml / min. The half-life of plasma is 1 to 2 hours, of synovial fluid 3 to 6 hours. More than 60% 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 concentration of metabolites in the blood increases approximately 4-fold, and their excretion increases with
    bile.
    In patients with chronic hepatitis or compensated cirrhosis, the pharmacokinetic parameters of diclofenac do not change.
    Indications:
    - inflammatory and degenerative diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis;
    gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine, including radicular syndrome, tendovaginitis, bursitis);
    - neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome, accompanied by
    inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis;
    - Infectious and inflammatory diseases of ENT organs with severe pain syndrome
    (as part of complex therapy): pharyngitis, tonsillitis, otitis media.
    The drug is intended for symptomatic therapy, reducing pain and inflammation,
    the progression of the disease is not affected.
    Contraindications:
    - hypersensitivity to diclofenac (including other NSAIDs) and other components of the drug;
    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in the anamnesis);
    - erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding;
    - Inflammatory bowel diseases (Crohn's disease, ulcerative colitis in the acute stage) in the phase of exacerbation;
    - disorders of hematopoiesis, hemostasis disorders (including hemophilia);
    - severe renal failure (CC less than 30 ml / min);
    - liver failure;
    Decompensated heart failure;
    - cardiac ischemia;
    - Chronic heart failure (grade II-IV according to the NYHA classification (New York classification of the functional state of patients with chronic heart failure);
    - cerebrovascular diseases;
    - diseases of peripheral arteries;
    - increased risk of arterial thrombosis and thromboembolism;
    - early postoperative period after aortocoronary shunting;
    - proctitis, hemorrhoids;
    - pregnancy (III trimester);
    - Children's age (for 50 mg to 14 years, for 100 mg to 18 years);
    - confirmed hyperkalemia;
    lactation period.
    Carefully:- patients with arterial hypertension, dyslipidemia, hyperlipidemia, inflammatory bowel disease outside the acute phase, liver diseases in history, liver porphyria, renal insufficiency (CK 30-60 ml / min), seasonal allergic rhinitis, chronic obstructive pulmonary disease, chronic respiratory tract infections, edema
    Quincke, edema of the nasal mucosa (including those with nasal polyps), bronchial asthma, diabetes mellitus, systemic connective tissue diseases;
    - elderly patients with anemia and data on the development of ulcerative gastrointestinal lesions in history, perforation;
    - for infections caused by Helicobacter pylori;
    - with prolonged use of non-steroidal anti-inflammatory drugs, frequent use of alcohol;
    - with concomitant therapy with anticoagulants (warfarin), antiplatelet agents (acetylsalicylic acid, clopidogrel), oral glucocorticosteroids, and (prednisolone), selective
    inhibitors of serotonin reuptake (citalopram, fluoxetine, paroxetine, sertraline);
    - in patients receiving diuretics and other drugs that affect the function of the kidneys, as well as patients with a significant decrease in the volume of circulating blood of any etiology, for example, before and after massive surgical interventions;
    - in elderly patients (including weakened patients, with low body weight), patients with
    severe somatic diseases, smoking patients.
    Pregnancy and lactation:
    The use of diclofenac in pregnant women has not been investigated. Therefore, it is not recommended to use the drug in pregnant women during the first and second trimester, unless the intended benefit to the mother exceeds the potential risk to the fetus. Contraindicated in the use of diclofenac in pregnant women during the third trimester because of the possibility of developing weakness in labor activity of the uterus and / or premature closing
    arterial duct.
    Studies in animals showed no harmful effects on fetal / fetal and postnatal development. Diclofenac at small amounts penetrates into breast milk, so during the lactation period, the drug should not be used, or it is necessary to resolve the issue of cessation breastfeeding.
    Dosing and Administration:

    It is administered rectally.

    Suppositories 50 mg.


    Adults and children over 14 years of age: 1 suppository up to two times a day.

    Suppositories 100 mg.

    Adults: 1 suppository once a day.

    The maximum daily dose is 150 mg. When applied simultaneously with oral forms of diclofenac, it is rational to apply a single dose of 50-100 mg per night (in this case, oral administration of oral forms of diclofenac is excluded). When algodismenore (with the appearance of the first symptoms) the initial dose is 50,100 mg / day, which if necessary is increased to 150 mg during several menstrual cycles.

    A migraine attack is 100 mg. If ineffectiveness - repeat in the same dosage, then if necessary continue treatment in the following days, the daily dose should not exceed 150 mg in several administrations.

    Side effects:
    According to the World Health Organization (WHO) adverse reactions are classified according to their frequency of development as follows: very often (>1/10), often (>1/100, <1/10), infrequently (>1/1000, <1/100), rarely (>1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.
    From the gastrointestinal tract:
    often: nausea, vomiting, diarrhea, dyspepsia, abdominal pain, bloating, decreased appetite; rarely: gastritis, vomiting with an admixture of blood, gastrointestinal bleeding, melena, stomach or bowel ulcers, possibly with complications (bleeding, perforation), frequent stools with a trace of blood, proctitis;

    rarely: esophageal motility disorder, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, stomatitis, glossitis, pancreatitis, exacerbation of hemorrhoids, adhesions intestines.

    From the nervous system:

    often: headache, dizziness;

    rarely: drowsiness;

    rarely: memory impairment, convulsions, anxiety, tremor, aseptic meningitis (more often patients with systemic red lupus and other systemic connective diseases tissue), cerebrovascular violations, disorientation, depression, insomnia, nightmares dreams, irritability, weakness sensitivity (including

    paresthesia).

    From the sense organs:

    often: vertigo;

    rarely: tinnitus, violation hearing, blurred vision, diplopia, a violation of taste sensations.

    From the urinary system:

    very rarely: acute renal insufficiency, hematuria, proteinuria, nephrotic syndrome, interstitial nephritis, papillary necrosis.

    From the organs of hematopoiesis and lymphatic system:

    rarely: anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia (thrombocytopenic purpura), agranulocytosis.

    From the immune system:

    rarely: anaphylactic reactions (including hypotension and shock);

    rarely: angioedema (including Quincke's edema).

    From the respiratory system:

    rarely: cough, bronchospasm, laryngeal edema;

    rarely: pneumonitis.

    From the cardiovascular system:

    infrequently: myocardial infarction, chronic heart failure;

    rarely: increased blood pressure, vasculitis, palpitations, extrasystole, pain in the chest cell.

    From the skin:

    often: skin rash;

    rarely: hives;

    rarely: bullous rash, toxic dermatitis, eczema, polymorphic erythema, toxic

    epidermal necrolysis (syndrome Lyell, Stevens-Johnson), photosensitization.

    From the side of the liver and bile ducts:

    often: increased activity "hepatic" transaminases

    rarely: jaundice, liver damage;

    rarely: hepatitis (possibly fulminant course), necrosis liver, cirrhosis, hepatorenal

    syndrome, hepatic failure.

    Other:

    rarely: edema.

    General disorders and disorders in place of administration:

    often: irritation in place introduction.

    Overdose:

    Symptoms: vomiting, bleeding from the gastrointestinal tract,

    dizziness, headache, diarrhea, nausea, tinnitus, dyspnea, myoclonic cramps, respiratory depression, dysfunction of the liver and kidneys, coma.

    Treatment: symptomatic therapy. Forced diuresis, hemodialysis are ineffective (since most of the drug binds to plasma proteins and is extensively metabolized).

    Interaction:

    Increases the concentration in the blood plasma digoxin, methotrexate, lithium preparations and cyclosporine. Increases toxicity

    methotrexate and nephrotoxicity cyclosporine and preparations of gold. Reduces efficiency diuretics, on the background potassium-sparing diuretics increased risk of hyperkalemia; anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase)and selective serotonin reuptake inhibitors increases the risk of bleeding (more often from the gastrointestinal tract). When used simultaneously with diuretics and antihypertensive drugs (beta- adrenoblockers, ACE inhibitors) diclofenac can reduce their antihypertensive effect.

    Therefore, patients, especially the elderly, with the simultaneous administration of diclofenac and diuretics or antihypertensive agents, should regularly monitor blood pressure, monitor kidney function and the degree of hydration (especially with a combination of diuretics and ACE inhibitors due to an increased risk of nephrotoxicity). Reduces effects hypotensive (beta-adrenoblockers, angiotensin-converting enzyme inhibitors) and hypnotics.

    Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs (including selective inhibitors of cyclooxygenase-2) and glucocorticosteroids (bleeding in the gastrointestinal tract).

    Acetylsalicylic acid reduces the concentration of diclofenac in the blood. The simultaneous use of diclofenac and paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

    Clinical studies have shown that diclofenac can be used in conjunction with oral hypoglycemic agents, and it does not affect their clinical effect. However, there are separate reports of a decrease or intensification of the effect hypoglycemic agents: monitoring of blood glucose concentration is recommended.

    Cefamandol, cefoperazone, cefotetan, valproic acid and fuscamycin increase the frequency of hypoprothrombinemia.

    Simultaneous appointment with ethanol, colchicine, corticotropin and preparations of St. John's wort perfumed increases the risk of bleeding in the gastrointestinal tract. Diclofenac strengthens the action drugs that cause photosensitization.

    Preparations blocking tubular secretion, increase the concentration of diclofenac in the blood plasma, thereby increasing its toxicity.

    With the simultaneous use of diclofenac and antibacterial drugs from the quinolone group the risk of seizures increases.

    When used simultaneously with inhibitors of isoenzyme CYP2C9 it is possible to increase the concentration of the drug in the blood plasma. When combined with derivatives phenytoin it is possible to enhance the action of phenytoin.

    Special instructions:
    To reduce the risk of adverse events, use minimally
    The effective dose of diclofenac is minimally possible short course.
    Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when administering the drug to 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 surgery). If in such cases appoint diclofenac, recommend, as a precaution, to monitor kidney function.Patients with an increased risk of developing gastrointestinal complications, as well as receiving therapy low doses
    acetylsalicylic acid or other drugs that can increase the risk of GI loss, should take gastroprotectors (for example, proton pump inhibitors or misoprostol). Patients with a history of gastrointestinal disease, especially the elderly, should be informed of the side effects of the digestive system. In rare cases with diclofenac treatment, such serious dermatological reactions like exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, in some cases fatal. When developing in patients receiving diclofenac sodium, the first signs of skin rashes, lesions of mucous membranes or other symptoms
    hypersensitivity drug should be canceled.
    When availability symptoms of hepatotoxicity (including nausea, diarrhea, pruritus, jaundice), treatment with diclofenac should be discontinued. When conducting therapy, it is necessary to monitor liver function, a clinical blood test, a fecal occult blood test. Diclofenac affects women's fertility, therefore, in patients with infertility (including those undergoing examination) it is recommended to cancel the drug. Diclofenac temporarily inhibits platelet aggregation, so patients from a bleeding disorder is recommended regularly monitor appropriate laboratory indications. With prolonged use it is recommended that regular clinical analyzes
    peripheral blood. Long-term therapy with diclofenac and high-dose therapy can lead to an increased risk of developing serious cardiovascular thrombotic
    complications (including myocardial infarction and stroke). To reduce the risk of these complications,
    especially in patients with cardiovascular diseases, should be used diclofenac at the lowest effective dose with the minimum possible duration of treatment.
    Diclofenac can mask the symptoms of infectious and inflammatory diseases.
    Effect on the ability to drive transp. cf. and fur:Patients who, with the use of Diclac®, experience dizziness or other unpleasant sensations from the nervous system, including visual impairment,should refrain from driving vehicles and practicing potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:
    Suppositories rectal 50 mg, 100 mg.
    Packaging:
    For 5 suppositories in a contour non-cellular package made of PVC / PE.

    By 2, 6 or 10 contour non-jawed packages together with instructions for use in cardboard pack.
    Storage conditions:
    At a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiration date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N011215 / 02
    Date of registration:03.08.2010
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    HEXAL, AG Germany
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp16.02.2016
    Illustrated instructions
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