Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSolution for intramuscular injection.
    Composition:
    Active substance: diclofenac sodium-25.0 mg.

    Excipients: benzyl alcohol - 40.0 mg; sodium disulfite 3.0 mg; mannitol 6.0 mg; 1 M sodium hydroxide solution to pH 8.4; propylene glycol -200.0 mg; water for injection - up to 1.0 ml.
    Description:Colorless or slightly yellowish tinge transparent liquid with a weak characteristic smell of benzyl alcohol:
    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. By indiscriminately inhibiting cyclooxygenase 1 and 2, it disrupts the metabolism of arsenic acid, reduces the amount of prostaglandins in the inflammatory focus. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac promotes a significant reduction in 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:The time to reach the maximum concentration with intramuscular application at a dose of 75 mg is 15-30 minutes, the maximum concentration is -1.9-4.8 (mean 2.7) μg / ml. After 3 hours after administration, plasma concentrations are on average. 10% of the maximum. The connection with plasma proteins is more than 99% (most of it is associated with 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 system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. Half-life from the plasma -2 hours 65% of the administered dose is excreted as metabolites by the kidneys; less than I% is excreted 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:
    For short-term treatment of pain of different genesis of moderate intensity:

    - inflammatory and degenerative diseases of the porno-motor apparatus:

    - rheumatoid arthritis,

    - seronegative arthritis: ankylosing spondylitis - Bechterew's disease, psori-atric arthritis, reactive arthritis (Reiter's syndrome)

    - gout, pseudogout,

    - osteoarthritis,

    - pain syndrome:

    - tendonitis, bursitis, myalgia, neuralgia, sciatica,

    - headache,

    - post-traumatic and postoperative pain syndrome,

    - pain syndrome in cancer

    - algodismenorea
    Contraindications:
    - hypersensitivity to diclofenac (including other NSAIDs) or other components of the drug,

    - complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses, and intolerance to acetylsalicylic acid and other PNVP (including in the anamnesis),

    - erosive and ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding,

    - inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation

    - Hemophilia and other disorders of blood clotting

    - Decompensated heart failure

    - liver failure

    - active liver disease

    - expressed renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia

    - period after aortocoronary shunting

    - pregnancy, the period of breastfeeding

    - children's age (under 18)
    Carefully:
    Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min.
    Liver disease in history, hepatic porphyria, chronic renal failure, chronic heart failure, arterial hypertension; a significant decrease in the volume of circulating blood (including after massive surgical intervention), elderly patients (including those receiving diuretics, weakened patients and with low body weight), bronchial asthma.
    Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract (GI tract), the presence of Helicobacter pyroli infection, advanced age, prolonged use of NSAIDs, frequent alcohol use, severe somatic diseases, concomitant therapy with the following drugs:. - anticoagulants (for example, warfarin)
    - antiaggregants (eg, acetylsalicylic acid, clopidogrel)
    - oral glucocorticosteroids (for example, prednisolone)
    - selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
    Dosing and Administration:
    It is administered intramuscularly.

    A minimum effective dose should be used with the minimum possible short course.

    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, rectal administration of diclofenac.

    The maximum daily dose is 150 mg.
    Side effects:

    From the gastrointestinal tract (GIT):

    - more often 1% - abdominal pain, flatulence (sensation of bloating), diarrhea, digestive disorders,nausea, constipation, dyspepsia, anorexia, impaired hepatic function, increased "liver" enzymes, peptic ulcer with possible complications (perforation, bleeding), gastro-intestinal bleeding;

    - less than 1% - vomiting, jaundice, melena, blood in stool, esophageal lesion, aphthous stomatitis, dry mouth, mucosal, hepatitis (possibly fulminant), hepatic necrosis, cirrhosis, hepatorenal syndrome, pancreatitis, holetsistopankreatit, colitis, hemorrhagic colitis , exacerbation of ulcerative colitis or Crohn's disease, fulminant hepatitis.

    From the nervous system:

    - more often 1% - headache, dizziness;

    - less than 1% - insomnia, drowsiness, depression, irritability, aseptiche sky meningitis (usually in patients with systemic lupus erythematosus and other connective tissue diseases), cramps, weakness, disorientation, nightmares, feelings of fear, violation of sensitivity, including . paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, mental disorders.

    From the sense organs:

    - more often 1% - noise in the ears;

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

    From the skin:

    g more often 1% - skin rash;

    less than 1% - urticaria, bullous eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, toxic dermatitis, pruritus, hair loss, photosensitivity, purpura, incl. allergic.

    From the genitourinary system:

    - more often 1% - fluid retention;

    - less than 1% .- nephrotic syndrome, protein ria, ol and huria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

    From the organs of hematopoiesis and the immune system:

    - less often I% - anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of the course of infectious processes (development of necrotizing fasciitis, pneumonia):

    From the respiratory system:

    - less than 1% - cough, bronchospasm, laryngeal edema, pneumonitis, bronchial asthma (including dyspnea).

    From the cardiovascular system:

    - less than 1% - increased blood pressure (BP), congestive heart failure, extrasystole, chest pain, palpitations, vasculitis, myocardial infarction.

    Allergic reactions:

    - less than 1% - anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock (usually develops rapidly), swelling of the lips and. language, allergic vasculitis.

    Local reactions with intramuscular injection:

    - burning, infiltration, aseptic necrosis, necrosis of fatty taknia

    Overdose:
    Symptoms: vomiting, bleeding from the digestive tract, diarrhea, dizziness, headache, dyspnea, turbidity, tinnitus, convulsions, with a significant overdose-acute renal failure, hepatotoxic effect; in children - myoclonic cramps, nausea, vomiting, abdominal pain, impaired liver and kidney function.

    Treatment: symptomatic therapy aimed at eliminating the increase in blood pressure, violations of kidney function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are ineffective due to a significant connection with proteins and intensive metabolism).
    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, antiplatelet agents and thrombolytic agents (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often from 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 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 drugs. Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract. Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia. Cyclosporin and gold preparations increase the effect of diclofenac on the synthesis of prostaglandin in the kidneys, which is manifested by increased nephrotoxicity. Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract. Antibacterial drugs from the quinolone group - the risk of seizures. 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.
    Special instructions:Patients using the drug should refrain from activities that require increased attention and rapid mental and motor reactions, alcohol consumption. In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended. In patients with infertility (including those undergoing examination) it is recommended to cancel the drug.
    Form release / dosage:
    Solution for intramuscular injection 25 mg / ml.
    Packaging:
    3 ml of the drug into neutral glass ampoules.

    5 or 10 ampoules in contour cell packs from a polyvinylchloride film.

    For 1 or 2 outline carton packs along with instructions for use in a cardboard pack.
    Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-004690/09
    Date of registration:10.06.2009
    The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp23.02.2016
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