Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsp
    Solution for intramuscular injection.
    Composition:
    1 ampoule (3 ml of the drug) contains:
    Active substance:
    Diclofenac sodium 75.00 mg
    Excipients:
    benzyl alcohol 120.00 mg, propylene glycol 630.00 mg, sodium disulfite 3.00 mg, sodium hydroxide q.s. up to pH = 8.5, water for injection q.s. up to 3.00 ml.
    Description:Transparent, colorless or slightly yellowish solution, with no visible mechanical 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 is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic effects.

    The main mechanism of its action consists in indiscriminate inhibition of the activity of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2), which leads to a disruption of the metabolism of arachidonic acid, a decrease in the synthesis of prostaglandins, prostacyclin and thromboxam.

    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, diclofenac has antiaggregant activity. In therapeutic doses diclofenac practically does not affect the time of bleeding. With prolonged treatment, the analgesic effect of diclofenac does not decrease.
    Pharmacokinetics:
    Time to reach the maximum concentration with intramuscular (IM) administration of 75 mg -15-30 minutes. Connection with plasma proteins, mainly with albumins - 99%. Diclofenac actively penetrates into the synovial fluid, where it reaches 60 to 70% of serum concentrations. After 3-6 hours after IM, the concentration of the active substance and metabolites in the synovial fluid is higher than in the serum. Diclofenac from the synovial fluid is excreted faster than from the serum. 50% of the drug is metabolized during the "first pass" through the liver.It is almost completely metabolized in the liver, mainly by hydroxylation, followed by conjugation with glucuronic acid and sulfation.

    The half-life (T1 / 2) is 1-2 hours. With mild violations of the liver or kidney T1 / 2 remains unchanged. 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.

    Approximately 70% of diclofenac is excreted by the kidneys in the form of pharmacologically inactive metabolites. Only 1% of the drug is excreted unchanged, the rest of the metabolites through the intestine.

    In elderly patients, pharmacokinetic parameters without significant changes.
    Indications:
    Diseases that require the achievement of a rapid anti-inflammatory or analgesic effect:

    - Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis,ankylosing spondylitis (Bechterew's disease), gouty arthritis, arthritis with Reiter's disease, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine, including with radicular syndrome, tendovaginitis, periarthritis, bursitis, myositis, synovitis.

    - Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache, renal and biliary colic.

    Diclofenac is intended for symptomatic therapy and does not affect the progression of the disease.
    Contraindications:
    - Hypersensitivity (including other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis).

    - The period after aortocoronary bypass surgery.

    - Erosive-ulcerous changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding.

    - Inflammatory bowel diseases (incl.nonspecific ulcerative colitis (NNC), Crohn's disease) in the phase of exacerbation.

    - Cerebrovascular bleeding or other haemorrhage and hemostasis disorders.

    - Severe hepatic impairment or active liver disease.

    - Severe renal insufficiency (CC less than 30 ml / min),

    including confirmed hyperkalemia, progressive kidney disease.

    - Decompensated heart failure.

    - Inhibition of bone marrow hematopoiesis.

    - III trimester of pregnancy, the period of breastfeeding.

    - Children's age (up to 18 years).
    Carefully:
    ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance 30-60 ml / min; anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, prolonged use of NSAIDs, frequent alcohol use, severe physical illnesses, induced porphyria, epilepsy, diverticulitis, systemic connective tissue diseases, a significant decrease in circulating blood volume (bcc) (in including after extensive surgery),elderly patients (including those receiving diuretics, weakened patients and low body weight), pregnancy (I-II trimester), concomitant therapy with the following drugs: anticoagulants (for example, warfarin), antiplatelet agents (e.g., acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).

    To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as little as possible.
    Pregnancy and lactation:The use of diclofenac in the I-II trimesters of pregnancy is possible only if the expected benefit exceeds the potential risk to the fetus. In the III trimester and during breastfeeding, Naklofen is contraindicated.
    Dosing and Administration:Intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours (patients with renal colic can be re-injected after 30 minutes).When using other dosage forms diclofenac should not exceed the maximum daily dose of -150 mg. Duration of use no more than 2 days, if necessary, further pass to oral, or rectal administration of diclofenac. Do not mix Naklofen with other drugs in the same syringe.
    Side effects:
    Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.01%, including individual cases.

    From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, dysfunction of the liver; very rarely - stomatitis, glossitis, dryness of the mucous membranes (including oral cavity), erosive-ulcerative lesions of the esophagus, diaphragm-like intestinal strictures, 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, 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.

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

    Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure (BP) and shock; very rarely - angioedema (including face).

    From the cardiovascular system: very rarely - palpitation, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

    From the respiratory system: rarely - cough, bronchial asthma (including dyspnea); very rarely - pneumonitis, laryngeal edema.

    From the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

    Other: at the site of the / m introduction of possible irritation, pain, swelling and redness of the skin.

    Overdose:
    Symptoms: for parenteral administration, an overdose is unlikely. Clinical symptoms of an overdose with parenteral administration are similar to those that can occur when using other medicinal forms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure, respiratory depression; with a significant overdose - acute renal failure, hepatotoxic effect.

    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 (significant association with proteins and intensive metabolism).
    Interaction:

    Increases plasma concentration digoxin, methotrexate, lithium preparations and cyclosporine.

    Reduces the effect diuretics, on the background of non-diuretics increased risk of hyperkalemia: against the background of anticoagulants, antiaggregant and thrombolytic drugs (alteplase, streptokinase, urokinase) the risk of developing bleeding increases (more often the gastrointestinal tract). Reduces the effect hypotensive and hypnotic drugs. Increases the likelihood of side effects, etc. NSAIDs and glucocorticosteroids (bleeding from the gastrointestinal tract), toxicity methotrexate and nephrotoxicity 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 hypoglycemic drugs.

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

    Cyclosporine and preparations of gold 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 appointment with ethanol, colchicine, corticotropin and preparations of St. John's wort perfumed 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 canal secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity. Antibacterial drugs from the quinolone group - risk of seizures.

    Do not mix Naklofen with other drugs in the same syringe. Patients should inform doctors about the development of side effects.

    Special instructions:
    To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

    With long-term use of diclofenac, it is possible, although in rare cases, the development of serious hepatotoxic reactions, and therefore it is recommended to regularly examine the function of the liver.

    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, as well as in the treatment of elderly people taking diuretics and patients who for any reason have a decrease in circulating blood volume (for example , after extensive surgical intervention). If in such cases appoint diclofenac, it is recommended as a precaution to monitor kidney function.

    Caution should be given diclofenac in patients with disorders of blood coagulation, porphyria, epilepsy, as well as in patients receiving anticoagulants or fibrinolytics.

    When carrying out long-term therapy, it is necessary to monitor the picture of peripheral blood, to conduct a fecal occult blood test.

    In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended. In patients with infertility (including undergoing examination) it is recommended to cancel the drug.

    Patients taking the drug should refrain from drinking alcohol.

    In infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac sodium can mask the symptoms of these diseases.

    It is not recommended to mix the Naklofen solution with other medicines in the same syringe.
    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 engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Solution for intramuscular injection 75 mg / 3ml.
    Packaging:For 3 ml in a vial of neutral glass. The ampoule contains a colored dot indicating the line of the broken ampoule, and a color coding ring. 5 ampoules per blister or 5 ampoules in a plastic pallet. 1 blister / pallet in a pack of cardboard along with instructions for use.
    Storage conditions:
    Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
    Shelf life:
    5 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N013166 / 04
    Date of registration:03.11.2009
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    KRKA, d.d. Slovenia
    Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Information update date: & nbsp20.02.2016
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