Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSolution for intramuscular injection.
    Composition:
    1 ampoule (3 ml) contains as active ingredient: diclofenac sodium 75 mg.

    Excipients: propylene glycol 600.0 mg, mannitol 18.0 mg, sodium disulfite 9.0 mg. benzyl alcohol - 120.0 mg, sodium hydroxide solution 1M - up to pH 8.0-9.0, water for injection - up to 3 ml.
    Description:
    Colorless or with a yellowish tint transparent liquid.

    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Diclofenac non-steroidal anti-inflammatory drug (NSAID). It has a pronounced analgesic, antipyretic and anti-inflammatory properties. Non-selective inhibitor of cyclooxygenases 1 and 2 types. It disrupts the metabolism of arachidonic acid and the synthesis of prostaglandins, which are the main link in the development of inflammation. In rheumatic diseases, the drug contributes to a significant reduction in pain, morning stiffness, swelling of the joints,which contributes to the improvement of the functional state of the joint. With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling.
    Pharmacokinetics:The maximum concentration is achieved after a single intramuscular injection of 75 mg - after 15-30 minutes and averages 2.7 μg / ml. After 3 hours after administration, the plasma concentration is about 10% of the maximum. 99% of diclofenac binds to plasma proteins, namely albumins. 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 systemic clearance of the active substance is approximately 260 ml / min. The half-life is 1-2 hours. Approximately 60% is excreted by the kidneys in the form of metabolites, less than 1% is excreted unchanged in the urine, the rest 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:
    For short-term symptomatic treatment of pain of different genesis of moderate intensity:

    - inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis, rheumatic soft tissue damage, osteoarthritis of the peripheral joints and spine (including radicular syndrome);

    - lumbago, sciatica, neuralgia;

    - algodismenorea, inflammatory processes of the pelvic organs, incl. adnexitis;

    - post-traumatic pain syndrome, accompanied by inflammation;

    - postoperative pain.
    Contraindications:
    - hypersensitivity (including other non-steroidal anti-inflammatory drugs or ancillary components);

    - erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation);

    - bleeding from the gastrointestinal tract,inflammatory bowel disease in the phase of exacerbation (ulcerative colitis, Crohn's disease);

    - severe hepatic insufficiency or liver disease in an acute period;

    - severe renal failure (creatinine clearance less than 30 ml / min);

    - progressive kidney disease;

    - hyperkalemia;

    - bronhoobstruktsiya, rhinitis, urticaria, provoked by the reception of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including in the anamnesis);

    - violation of hematopoiesis, hemostasis disorders (including hemophilia);

    - pregnancy (III trimester);

    - lactation period;

    - children's age (up to 18 years);

    - period after aortocoronary bypass surgery.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency (creatinine clearance 30-60 ml / min), dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory bowel disease, a condition after extensive surgical interventions, induced porphyria, advanced age,diverticulitis, systemic connective tissue diseases, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation.
    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 anti coagulants and (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticoids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Pregnancy and lactation:The drug should not be used in the third trimester of pregnancy and during breastfeeding.
    Dosing and Administration:The solution is administered intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours later. Duration of use no more than 2 days, if necessary, further pass to oral, or rectal administration of diclofenac.
    Side effects:

    Gastrointestinal tract (GIT):

    more often 1% - abdominal pain, sensation of bloating, diarrhea, indigestion, nausea, constipation, flatulence, increased activity of "liver" enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;

    vomiting, jaundice, melena, the appearance of blood in the stool, the defeat of the esophagus, aphthous stomatitis, dry mouth, hepatitis (possibly fulminant), liver necrosis, cirrhosis, hepatorenal syndrome, anorexia, pancreatitis, cholecystopancreatitis, colitis, gastritis, proctitis, impaired liver function, glossitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease.

    Nervous system:

    more often 1% - headache, dizziness;

    less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, weakness, disorientation, nightmares, feelings of fear, sensitivity disorder, incl. , paresthesia, memory disorders, tremor, anxiety, cerebrovascular disorders, mental disorders.

    Sense organs: more often 1% - noise in the ears;

    less than 1% - blurred vision, diplopia, a taste disorder. Reversible or irreversible hearing loss, scotoma.

    Skin:

    more often 1% - skin itch, skin rash;

    less than 1% - alopecia, urticaria, eczema, toxic dermatitis, multiform exudative erythema, incl. Stevens-Johnson, toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, small-point hemorrhage.

    Genitourinary system: more often 1% - fluid retention;

    less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

    Hematopoiesis:

    less often I% - anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura.

    Respiratory system:

    less than 1% - cough, bronchospasm, laryngeal edema, pneumonia.

    The cardiovascular system:

    less than 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain, palpitations, myocardial infarction.

    Allergic reactions:

    less often 1% - anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.

    Local reactions:

    burning, infiltration, aseptic necrosis, necrosis of adipose tissue.

    Other:

    less than 1% - worsening of the course of infectious processes (development of necrotizing fasciitis, pneumonia).

    Overdose:
    Symptoms: nausea, vomiting, severe abdominal pain, bleeding from the gastrointestinal tract, diarrhea, dizziness, headache, tinnitus, convulsions, dyspnea, confusion. With a significant overdose - acute renal failure, hepatotoxic effect.

    Treatment: there is no specific antidote. Treatment - symptomatic, aimed at eliminating violations of kidney function, gastrointestinal irritation, respiratory depression, seizures. It is necessary to constantly monitor the patient's condition for several days, since there is a danger of later manifestation of some gastrointestinal lesions - ulceration or bleeding.

    Forced diuresis and hemodialysis are ineffective (due to significant binding to plasma proteins and intensive metabolism).
    Interaction:
    Increases the concentration in the plasma digoxin, methotrexate, lithium ions and cyclosporine.Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; on the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often from the gastrointestinal tract). Reduces the effect of hypotensive and hypnotic drugs. It increases the likelihood of side effects of other nonsteroidal anti-inflammatory drugs and corticosteroids (bleeding from the gastrointestinal tract), the toxicity of methotrexate and cyclosporine nephrotoxicity. Reduces the effect of hypoglycemic drugs. Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

    Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac,

    Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of pseudorothrombinemia.

    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, selective serotonin reuptake inhibitors and St. John's wort preparations: 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.
    Special instructions:With special care, the drug is prescribed for patients with cardiac or renal insufficiency, as well as for elderly people taking diuretics and patients who for any reason have a decrease in the volume of circulating blood. In these cases, it is recommended to monitor kidney function as a precautionary measure.

    In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism of diclofenac do not differ from those in patients with normal liver function. When carrying out the overcoat therapy it is necessary to monitor the function of the liver, the picture of peripheral blood,feces for blood.

    In connection with the negative impact on fertility, women planning to become pregnant, diclofenac 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 with diclofenac, the speed of mental and motor reactions may be reduced, so it is necessary to refrain from driving vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Solution for intramuscular injection 25 mg / ml.
    Packaging:To 3 ml in ampoules of colorless glass. 5 ampoules per contour cell pack. For 1 or 2 contour packs with instructions for use in a pack of cardboard.
    Storage conditions:
    In the dark place at a temperature of no higher than 25 ° C.
    Keep out of the reach of children.
    Shelf life:5 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N003996 / 01
    Date of registration:16.11.2009
    The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp20.02.2016
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