Active substanceDiclofenacDiclofenac
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  • Dosage form: & nbspCapsules with modified release.
    Composition:
    One capsule contains:

    - Diclofenac pellets intestinal soluble 78.50 mg, equivalent to 25 mg of diclofenac sodium;

    - diclofenac pellets with a sustained release of 130.55 mg, equivalent to 50 mg of diclofenac sodium.

    Composition - Diclofenac pellets enteric-soluble:

    active substance: diclofenac sodium 25 mg;

    Excipients: microcrystalline cellulose 31.87 mg, povidone-K25 5 mg, silicon dioxide colloidal anhydrous 0.63 mg;

    shell pellets intestine soluble: methacrylic acid and ethyl acrylate copolymer [1: 1] 10 mg [sodium lauryl sulfate 0.7% and polysorbate 80% 2.3%], propylene glycol 1 mg, talc 5 mg.

    Composition - Diclofenac pellets with sustained release: active substance: diclofenac sodium 50 mg:

    Excipients: cellulose microcrystalline 63.75 mg, povidone-K25 10 mg, silicon dioxide colloidal anhydrous 1.25 mg;

    a pellet with prolonged release: methyl methacrylate, trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [1: 2: 0.1] (Eudragit Rs 100, type B) 2.49 mg, methyl methacrylate,

    trimethylammonioethyl methacrylate chloride and ethyl acrylate copolymer [1: 2: 0.2] (Eudragit RL 100, type A) 0.5 mg, triethyl citrate 0.3 mg, talc 2.26 mg.

    Capsule shell composition: lid: indigo carmine (E132) 0.05%, titanium dioxide (E171) 2%, gelatin to 100%; body: gelatin 100%; The capsule shell can contain up to 2000 rpm of sodium lauryl sulphate.

    Composition of white ink: shellac 25.803%. lecithin soybean 0,16%, defoamer DC1510 0.001%, titanium dioxide (E171) 38.499%.

    Description:Hard gelatin capsules. Size of the capsule is № 2. Capsule color: body - transparent, colorless; The lid is matte, light blue. On the case and the lid there is an inscription with white ink "D75M". The contents of the capsule are pellets from white to light yellow color.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.
    ATX: & nbsp

    S.01.B.C.03   Diclofenac

    M.01.A.B.05   Diclofenac

    Pharmacodynamics:Has anti-inflammatory, analgesic and antipyretic effect. By indiscriminately inhibiting cyclooxygenase 1 (COX1) and cyclooxygenase 2 (COX2), it breaks 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 (NSAIDs), the drug has antiplatelet activity.
    Pharmacokinetics:

    Suction: after oral administration diclofenac it is easily absorbed into the systemic circulation. Eating does not affect the degree suction of the drug, but slows the rate of absorption. Diclofenac prolonged action: as a result of sustained release of the drug, the maximum concentration in the blood plasma (Cmax) is lower than the one created when introducing JIC short action; however, it remains high for a long time after administration. FROMmah - 0.5-1 μg / ml, time to reach Cmah - 5 hours after taking 100 mg of prolonged action tablets. The concentration in the plasma is linear depending on the amount of the administered dose.

    Distribution: the connection with plasma proteins is more than 99% (most of it is associated with albumins). The apparent volume of distribution of diclofenac in the body is on average 0.12-0.55 l / kg. Penetrates into breast milk, synovial fluid; FROMmah in the synovial fluid is observed 2-4 hours later than in the plasma. T1 / 2 from the synovial fluid - 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).

    Metabolism: 50% of the drug is metabolized during the "first pass" through the liver. Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. In the metabolism of the drug is also involved isoenzyme CYP2C9. The main metabolite of the drug (4'-hydroxydiclofenac) has a slight anti-inflammatory activity.

    Excretion: 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, pharmacokinetic parameters do not change.

    Indications:
    - Arthritis (including rheumatoid arthritis), osteoarthritis, gouty arthritis;

    - periarthritis, tendonitis, tenosynovitis, bursitis;

    - post-traumatic and postoperative pain syndrome, accompanied by inflammation.
    Contraindications:
    - Hypersensitivity to diclofenac, to any other component of the drug or to soy;

    - erosive-ulcerous lesions of the gastrointestinal tract (GIT), active gastrointestinal bleeding, aggravation of inflammatory bowel disease;

    - cerebrovascular bleeding or existing bleeding disorders;

    - acute heart failure;

    - full or partial combination of recurrent asthma polyposis, nasal mucous membrane and paranasal capsules and intolerance of acetylsalicylic acid;

    - progressive kidney disease;

    - confirmed hyperkalemia;

    - the last trimester of pregnancy;

    - children's age (under 18 years).
    Carefully:Peptic ulcer and 12 duodenal ulcer, ulcerative colitis, Crohn's disease, a history of liver disease, hepatic porphyria, chronic liver failure, chronic heart failure, arterial hypertension, a significant reduction in circulating blood volume (including after extensive surgery),elderly patients (including those who receive diuretics, weakened patients and with low body weight), bronchial asthma, simultaneous reception of glucocorticosteroids (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 diseases (creatinine clearance 30-60 ml / min), the presence of Helicobacter pylori infection, the long-term use of non-steroidal anti-inflammatory drugs (NSAIDs), alcoholism, and severe physical illnesses.
    Pregnancy and lactation:
    Complete data on the use of diclofenac during pregnancy are absent. Experiments on animals showed reproductive toxicity. The potential risk to humans is unknown. If possible, avoid the use of diclofenac in the first and second trimesters of pregnancy. In cases of emergency diclofenac should be taken at minimal therapeutic doses for a short period of time.
    Diclofenac is contraindicated in the third trimester of pregnancy. In connection with its mechanism of action, it is possible to suppress the ability of the myometrium to contract, prolong the period of pregnancy and childbirth, cardiovascular and renal toxicity of the fetus, and the appearance of a tendency for bleeding in the mother and child.
    Diclofenac and its derivatives penetrate breast milk in small amounts, and therefore a short-term drug intake without interruption of feeding is possible. In cases where longer dosing is required, as well as taking high doses, it is recommended to stop breastfeeding for a while.
    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.
    Dosing and Administration:
    Inside, entirely, without chewing and washing down with the necessary amount of liquid.

    Dosage depends on the severity of clinical manifestations. The recommended adult dose is 75 mg to 150 mg diclofenac per day in one or two doses.The maximum single dose is 75 mg (one capsule). The maximum daily dose is 150 mg (two capsules).
    Side effects:

    Often - 1-10%; infrequently - 0.1-1%, rarely - 0.01-0.1%, very rarely - less than 0.001%, 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 digestive 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 (including 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, 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 - 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, including multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, including allergic.

    Other: rarely - swelling.

    Overdose:
    Symptoms: headache, dizziness, blurred vision, hyperventilation, gastrointestinal disorders (nausea, vomiting, abdominal pain, bleeding), impaired liver and kidney function.

    Treatment: Gastric lavage, activated charcoal, symptomatic therapy. Hemodialysis is ineffective. There is no special antidote.
    Interaction:
    The intake of diclofenac increases the concentration in the plasma of digoxin, lithium preparations.

    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 in the gastrointestinal tract).

    Reduces the effect of hypotensive and hypnotic drugs. Increases the likelihood of side effects (bleeding in the gastrointestinal tract) of other nonsteroidal anti-inflammatory drugs and glucocorticosteroids, toxicity of methotrexate and nephrotoxicity of cyclosporine due to an increase in their plasma concentrations. 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.

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

    Simultaneous use with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal 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 increase 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, and also in the treatment of elderly patients taking diuretics,and patients who for any reason have a decrease in the volume of circulating blood (including after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

    In patients with renal insufficiency with a creatinine clearance of less than 10 ml / min, the equilibrium concentration of metabolites in plasma should theoretically be significantly higher than in patients with normal renal function, but this is not really observed, since the excretion of metabolites with bile is enhanced. 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.
    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 speciesactivities that require increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:
    Capsules with modified release 75 mg.
    Packaging:
    10 capsules per blister, made of PVC / PVDC film and aluminum foil.

    For 1, 3 or 5 blisters together with the instructions for use are placed in a cardboard box.
    Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    4 years.

    Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:PL-000639
    Date of registration:28.09.2011
    Date of cancellation:2016-09-28
    The owner of the registration certificate:Delta Medikel Promotions AGDelta Medikel Promotions AG Switzerland
    Manufacturer: & nbsp
    Representation: & nbspRepresentation Delta Medikel Promotions AGRepresentation Delta Medikel Promotions AG
    Information update date: & nbsp12.02.2016
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