Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspTablets, covered with enteric coating.
    Composition:
    Diclofenac sodium 50.00 mg or 100.00 mg.

    Excipients: microcrystalline cellulose, lactose, corn starch, sodium carboxymethyl starch, magnesium stearate,

    Ingredients of enteric coating: hypromellose phthalate, diethyl phthalate, dye sunset yellow E-110, titanium dioxide.
    Description:Tablets of 50 mg and 100 mg: Biconvex tablets of orange color, coated, on the one hand, NP engraving on the background of wood.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Non-steroidal anti-inflammatory drug, a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effect. Indiscriminately inhibiting cycloxygenase 1 and cycloxygenase 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus.The most effective for inflammatory pain. Like all non-steroidal anti-inflammatory drugs, the drug has antiaggregant activity.
    Pharmacokinetics:
    Absorption is fast and complete, food slows down the absorption rate. After oral administration, 50 mg maximum concentration is 1.5 μg / ml, the maximum concentration time is 2-3 hours.
    The drug in tablets of 100 mg does not have the properties of a prolonged dosage form.
    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.

    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. The half-life of the drug from the synovial fluid is 3-6 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 is 2 times lower 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:
    Diclofenac is used as an anti-inflammatory and analgesic for the musculoskeletal system (rheumatoid arthritis,psoriatic, ankylosing spondylitis; gouty arthritis, rheumatic soft tissue damage, osteoarthritis of peripheral joints and spine, including with radicular syndrome, tendovaginitis, bursitis). In the treatment of degenerative diseases of the musculoskeletal system, the drug is intended only for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

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

    In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).
    Contraindications:
    - Hypersensitivity to the active substance or ancillary components;

    - 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 changes in the gastric mucosa or duodenum, active gastrointestinal bleeding;

    - Inflammatory bowel disease (nonspecific ulcerative colitis, Crohn's disease);

    - Period after aortocoronary bypass surgery;

    - Hereditary intolerance to galactose, impaired glucose absorption-- III trimester of pregnancy, the period of breastfeeding;

    - Uncompensated heart failure;

    - Cerebrovascular bleeding or other bleeding and hemostasis disorders;

    - Severe hepatic impairment or active liver disease;

    - Severe renal insufficiency (creatinine clearance less than 30 ml / min); progressive kidney disease, incl. confirmed hyperkalemia;

    - The drug of 50 mg is contraindicated for children under 15 years, for 100 mg to 18 years.
    Carefully:
    Anemia, bronchial asthma, cerebrovascular disease, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal failure, dyslipidemia / hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease,state after major surgery, induced porphyria, advanced age, diverticular disease, systemic connective tissue disease, pregnancy I-II trimester, creatinine clearance less than 60 mL / min. 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 aptycoagulants (for example, warfarin), apyagregantami (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetype, paroxetine, sertraline).

    Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful when administered to patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, decrease in circulating blood volume is observed (eg , after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.
    Dosing and Administration:Adults: inside, not liquid, 50 mg 2 - 3 times a day during or after a meal. The maximum daily dose is 150 mg. If you take 100 mg tablets and, if necessary, increase the daily dose to 150 mg, you can additionally take 1 tablet of diclofenac 50 mg, but not earlier than 6-8 hours after taking the tablet 100 mg. Adolescents older than 15 years: 50 mg not more than 2 times a day. Tablets of 100 mg not more than 1 time per day. The maximum daily dose is 100 mg.
    Side effects:

    Often - 1-10%; sometimes 0.1-1%; rarely - 0,01-0,1%; very rarely - less than 0.001%, including individual cases.

    From the digestive system: often - eiigastric 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, impaired 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, 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, hemolytic and aplastic anemia, agripulocytosis.

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

    Other: rarely - swelling.

    Overdose:
    Symptoms: dizziness, headache, hyperventilation of the lungs, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

    Treatment: gastric lavage, Activated carbon, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are ineffective.
    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 CPAP and glucocorticoid 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.

    Cefamandol, cefoperazone, cefotetan, valproic acid and scrambling increase the frequency 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 UV irradiation.

    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:
    In order to quickly achieve the desired therapeutic effect take 30 minutes before meals. In other cases, take before, during or after eating, without chewing, squeezed with enough water. The drug removes or reduces pain and inflammation during the treatment period, without affecting the progression of the disease.

    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, 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.

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

    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.
    Form release / dosage:
    Tablets coated with enteric coating 50 mg and 100 mg.
    Packaging:
    For 10 tablets in a PVC / A1 blister. For 1, 2, 3, 4, 5 blisters in a cardboard box with instructions for use.
    Storage conditions:At a temperature of no higher than 25 ° C, in a dry, dark place. Keep out of the reach of children!
    Shelf life:
    3 years.

    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:П N014450 / 02
    Date of registration:07.10.2008
    Date of cancellation:2017-03-10
    The owner of the registration certificate:Natur Product Europe BVNatur Product Europe BV Netherlands
    Manufacturer: & nbsp
    Representation: & nbspNatur Product International Inc.Natur Product International Inc.Russia
    Information update date: & nbsp10.03.2017
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