Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspSolution for intramuscular injection.
    Composition:1 ml of the solution contains: active substance: diclofenac sodium - 25 mg; auxiliary substances: propylene glycol-200 mg, benzyl alcohol-40 mg, mannitol-6 mg, sodium disulfite (sodium metabisulphite) -3 mg, sodium hydroxide, 1 M solution to pH 8.4, water for injection- up to 1 ml.
    Description:
    Transparent or slightly opalescent, slightly colored liquid with a characteristic odor.

    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. Not selectively inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation. The most effective for inflammatory pain. It has antiplatelet activity.
    Pharmacokinetics:
    Quickly absorbed after intramuscular injection. The time to reach the maximum concentration when administered at a dose of 75 mg is 15-30 minutes, the maximum concentration (Cmax) is 1.9-4.8 (mean 2.7) μg / ml. After 3 hours after administration, plasma concentrations averaged 10% of the maximum.

    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; Stax in the synovial fluid is observed 2-4 hours later than in the plasma. T1 / 2 from the synovial fluid -3 to 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; the area under the concentration-time curve (AUC) is 2 times less after oral administration of the drug than after parenteral administration of the same dose. 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. T1 / 2 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: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), osteoarthritis, gouty arthritis, arthritis with Reiter's disease. 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 syndrome: headache (incl.migraine) and toothache, bursitis, tendonitis, lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis, with oncological diseases, post-traumatic and postoperative pain syndrome accompanied by inflammation.

    Algodismenorea; inflammatory processes in the small pelvis, incl. adnexitis. Infectious and inflammatory diseases of the ENT organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media.
    Contraindications:Hypersensitivity (including other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis), erosive and ulcerative lesions of the gastrointestinal tract (GIT) and duodenal ulcers, active gastrointestinal bleeding, inflammatory bowel disease (in the acute stage), 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 hyperkalaemia, pregnancy (III trimester), lactation period, children's age.
    Carefully:Stomach and duodenal ulcer, ulcerative colitis, Crohn's disease, diverticulitis, liver disease in history, edematous syndrome, hepatic porphyria, chronic renal failure, chronic heart failure, arterial hypertension, significant decrease in the volume of circulating blood (including after massive surgical intervention), elderly patients (including those receiving diuretics, weakened patients and low body weight), bronchial asthma (risk of exacerbation), simultaneous reception of glucocorticoid (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic heart disease, cerebrovascular diseases, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, KC 30-60 ml / min, presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe physical illness.
    Pregnancy and lactation:The use of the drug in the third trimester of pregnancy and during lactation is contraindicated.The use of the drug in the I and II trimesters of pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
    Dosing and Administration:It is administered intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours later. The duration of intramuscular injection of the drug should not exceed 2 days, then switch to oral administration with a maximum daily dose of -150 mg (including and on the day of injection).
    Side effects:

    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 digestive system: often epigastric pain, nausea, vomiting. diarrhea, dyspepsia, flatulence, anor- sia. increased activity of aminotransferase; rarely gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting from the larynx, melanoma diarrhea, blood sores), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice. abnormal liver function; very rarely - stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease,constipation, pancreatitis, fulminant hepatitis.

    From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremor, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), disorientation, depression. insomnia, nightmares. irritability. mental disorders.

    From the sense organs: often - the vertical; 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.

    From the hematopoiesis: very rarely - thrombocytopenia. leukopenia, anemia (including hemolytic and aplastic), agranulocytosis.

    Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and anaphylactic 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, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell syndrome, exfoliative dermatitis, itching. loss of hair, photosensitivity. purpura, incl. allergic.

    Other: often - irritation at the injection site; very rarely - an abscess at the injection site; rarely - swelling.

    Long-term therapy with diclofenac for systemic use, especially in high doses (150 mg / day), may increase the risk of developing thrombotic lesions of arterial vessels (eg, myocardial infarction or stroke).

    Overdose:Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, lethargy, convulsions, rarely - increased blood pressure, acute renal failure, hepatotoxic effect, respiratory depression, coma.Treatment: symptomatic therapy; careful monitoring of the patient's condition. The specific antidote is not known. Forced diuresis, hemodialysis are ineffective (due to the 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 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 NSAIDs and glucocorticosteroids (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.

    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 is manifested by increased nephrotoxicity.

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

    Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the digestive 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:Because of the important role of prostaglandins 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,which for any reason has a decrease in the volume of circulating blood (including after extensive surgery). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function. In patients with hepatic insufficiency (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism do not differ from similar processes in patients with normal liver function. 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 want to become pregnant, the drug is not recommended. In patients with infertility (including those undergoing examination) it is recommended to cancel the drug.

    Diclofenac (like other NSAIDs) can cause hyperkalemia. 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.

    If during the reception of the drug an increase in the activity of the "liver" transaminases is maintained or increased,if there are clinical signs of hepatotoxicity (including nausea, fatigue, drowsiness, diarrhea, itching, jaundice), treatment should be discontinued.
    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 motor 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:
    3 ml in neutral glass ampoules.

    5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

    1 or 2 contour mesh packages together with the instruction for use and the ampoule scarifier are put in a pack of cardboard.

    When using ampoules with a notch, dot or ring fracture, the ampoule scaper is not inserted.
    Storage conditions:Store in a dark place at a temperature of 0 to 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:P N001127 / 01
    Date of registration:09.02.2009
    The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.02.2016
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