Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbsp
    Tablets, coated with enteric coating, solution for injection.
    Composition:
    pills: each tablet contains 25 mg or 50 mg of diclofenac active ingredient, as well as excipients: lactose, corn starch, disodium EDTA, sodium metabisulphite, magnesium stearate, methacrylic acid copolymer, diethyl phthalate, titanium dioxide, red iron oxide, yellow iron oxide.

    injection: Each ml of the injection contains 25 mg of diclofenac and auxiliary substances: benzyl alcohol, propylene glycol, sodium metabisulphite, sodium hydroxide, water for injection.
    Description:
    Tablets: round, biconvex tablets, covered with a membrane; 50 mg tablets are brownish-yellow, tablets of 25 mg are reddish-yellow.

    Solution for injection: a clear, colorless or slightly yellowish solution with a faint 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:Pharmacological action - anti-inflammatory, analgesic, antipyretic, antiaggregational. It inhibits cyclooxygenases 1 and 2, as a result of which the reactions of the arachidonic cascade are blocked and the synthesis of prostaglandins, thromboxane A2, prostacyclin, leukotrienes and release of lysosomal enzymes is disrupted; suppresses platelet aggregation; with long-term use has a desensitizing effect.
    Pharmacokinetics:
    Absorption is fast and complete, food slows down the absorption rate. After oral administration of 50 mg, the maximum concentration is achieved after 2-3 hours and is 1.5 μg / ml, bioavailability is 50%. 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. Do not cumulate while observing the recommended interval between meals.

    The connection with plasma proteins is 95-98% (most of it is associated with albumins). Penetrates into the synovial fluid; The maximum concentration in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life of the synovial fluid is 3-6 hours (concentration of the active substancein the synovial fluid 4-6 hours after the administration of the drug is higher than in the plasma, and remain higher for another 12 hours).

    Metabolism: 50% of the active substance undergoes metabolism during the "first pass" through the liver; The area under the pharmacokinetic 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 pharmacological activity of metabolites is less than that of diclofenac.

    Systemic clearance is 260 ml / min. Half-life 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 dysfunction (the clearance of cratinin is less than 10 ml / min), the excretion of metabolites with bile is increased, while the increase in their concentration in the blood is not observed.

    In patients with chronic hepatitis or compensated cirrhosis, the pharmacokinetic parameters of diclofenac are the same as in patients without liver disease.

    Indications:Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis), acute gouty arthritis. Degenerative diseases of the musculoskeletal system (deforming osteoarthritis, osteochondrosis). Lumbago, sciatica, neuralgia, myalgia.

    Diseases of extraarticular tissues (tendovaginitis, bursitis, rheumatic soft tissue damage).

    Post-traumatic pain syndromes accompanied by inflammation, post-operative pain, migraine, renal or biliary colic; primary algodismenorea, adnexitis, proctitis.

    Infectious-inflammatory diseases of LOP organs with severe pain syndrome (pharyngitis, tonsillitis, otitis), residual pneumonia. Feverish syndrome.
    Contraindications:Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), "aspirin" asthma, hematopoietic disorders, pregnancy, younger children, lactation.
    Carefully:Induced acute liver porphyria, severe impairment of liver and kidney function, heart failure.
    Dosing and Administration:
    Inside, not liquid, during or after a meal, adults - 25-50 mg 2-3 times a day. When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 50 mg / day. The maximum daily dose is 150 mg. For children older than 6 years and adolescents, only tablets of usual duration of action of 25 mg are used; daily dose of 2 mg / kg of the child's body weight. With juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg. Tablets should be taken whole, not liquid, fasting, with a small amount of liquid.

    In / in the drip. The maximum daily dose is 150 mg. Immediately before IV introduction diclofenac (the contents of 1 ampoule - 75 mg) should be diluted in 100-500 ml of 0.9% solution of sodium chloride or 5% glucose solution (previously adding sodium bicarbonate solution to infusion solutions - 0.5 ml 8.4% or 1 ml 4.2% solution). Depending on the severity of the pain syndrome, the infusion is performed within 30-180 minutes.

    In order to prevent postoperative pain, infusion is performed with a "shock" dose of the drug (25-50 mg for 15-60 min). Further infusion is continued at a rate of 5 mg / h (until the maximum daily dose of 150 mg).For the treatment of acute or chronic disease exacerbation cupping it is also possible to / m (one-time) introduction of further treatment continued oral administration of diclofenac with the maximum daily dose - 150 mg (including the day of injection). The injection solution is injected deep in the / m for no more than 2 days.
    Side effects:
    From the digestive system: gastralgia, nausea, vomiting, diarrhea, stomach cramps, dyspepsia, flatulence, anorexia, increased activity of "liver" transaminases, gastrointestinal bleeding (hematemesis, melena), hepatitis with jaundice or without jaundice, fulminant hepatitis, pancreatitis , nonspecific colitis haemorrhage, exacerbation of ulcerative colitis or Crohn's disease, aphthous stomatitis, glossitis, erosive esophagitis, constipation.

    From the nervous system: headache, dizziness, fatigue, disorders of perception, paresthesia, memory loss, loss of sense of direction, reduced visual acuity, diplopia, hearing loss, tinnitus, insomnia, irritability, convulsions, depression, anxiety, "nightmarish "dreams, tremor psychotic reactions, dysgeusia.

    From the skin: rashes on the skin, bullous eruptions, eczema, polymorphic erythema, erythroderma (exfoliative dermatitis), alopecia, photosensitivity, purpura.

    From the urinary system: acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

    On the part of the hemopoiesis: thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia, aplastic anemia.

    Allergic reactions: bronchospasm, urticaria, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), allergic purpura, systemic anaphylactic reactions (including shock).

    Other: swelling, impotence, palpitation, chest pain, increased blood pressure. In the place of / m introduction - burning; infiltration, aseptic abscess, necrosis of adipose tissue.
    Overdose:
    Symptoms: dizziness, headache, hyperventilation, confusion, in children - myoclonic cramps, gastrointestinal disorders (nausea, vomiting, abdominal pain, bleeding), disorders of liver and kidney function.

    Treatment: gastric lavage, the introduction of activated charcoal, 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.
    Interaction:
    Increases plasma concentrations of digoxin, lithium and cyclosporine. Against the background of potassium-sparing diuretics, the risk of hyperkalemia increases, against the background of anticoagulants - the risk of bleeding.

    Reduces the effects of diuretic, hypotensive and hypnotics. Increases the likelihood of side effects of non-steroidal anti-inflammatory drugs, glucocorticosteroids (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine. Acetylsalicylic acid reduces the concentration of diclofenac in the blood. With simultaneous use with oral hypoglycemic drugs, it is possible to develop both hypo- and hyperglycemia.
    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 for the treatment of elderly people taking diuretics,which for some reason has a decrease in the volume of circulating blood (for example, after extensive surgical intervention). 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.
    During the treatment period, the speed of mental and motor reactions may decrease.
    Form release / dosage:
    Tablets of 25 mg, 50 mg.
    Packaging:For 10 tablets in blisters of aluminum foil and polyvinyl chloride film. For 2.3 or 5 blisters in a cardboard bundle. Solution for injection 25 in ampoules of 3 ml.
    Storage conditions:List B. In a dry, the dark place at a temperature below 30 ° C. Keep out of the reach of children. In the dark place at a temperature below 30 C (for solution).
    Shelf life:Tablets - 4 years, injection for 3 years.Do not use the product after the date shown on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N014940 / 01-2003
    Date of registration:23.07.2008
    The owner of the registration certificate:M. J. Biofarm Pvt. Ltd.M. J. Biofarm Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspM.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group M.J. BIOFARM Pvt. Ltd. division of the corporation MJ Group India
    Information update date: & nbsp28.02.2016
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