Dolaren® (Dolaren® )

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDiclofenac + ParacetamolDiclofenac + Paracetamol
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  • Dolaren®
    pills inwards 
    Outline Pharma Pvt. Ltd.     India
    • Dosage form: & nbspPills.
    Composition:
    ONE TABLE CONTAINS:

    active substance: paracetamol 500 mg and diclofenac sodium - 50 mg; Excipients: starch, talc, magnesium stearate, sodium carboxymethyl starch (sodium starch glycolate), gelatin, colloidal silicon dioxide, sodium methyl parahydroxybenzoate, propyl parahydroxybenzoate sodium, microcrystalline cellulose, croscarmellose, yellow dye "sunset" (Sunset Yellow FCF) (E 110).
    Description:Round biconvex bilayer tablets on one side of white to almost white color, on the other hand orange interspersed with white and dark orange color.
    Pharmacotherapeutic group:Analgesic combined (NSAIDs + analgesic non-narcotic remedy).
    ATX: & nbsp

    M.01.A.B.55   Diclofenac in combination with other drugs

    Pharmacodynamics:The effect of the drug is due to the properties of its constituent components. Diclofenac has anti-inflammatory, analgesic, antiplatelet and antipyretic effect. Indiscriminately inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus.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. Paracetamol - non-narcotic analgesic, blocks cyclooxygenase 1 and 2 mainly in the central nervous system, affecting the centers of pain and thermoregulation. In inflamed tissues, cellular peroxidases neutralize the effect of paracetamol on cyclooxygenases, which explains the almost complete absence of anti-inflammatory effect.
    Pharmacokinetics:

    Absorption of active components (diclofenac and paracetamol) - fast and complete, food slows the absorption rate of diclofenac for 1-4 hours and reduces the maximum concentration by 40%. The concentration of active components in the plasma is linearly dependent on the amount of the administered dose, not cumulated.

    Link with plasma proteins diclofenac - more than 99% (most of it binds to albumins), paracetamol binds to blood proteins by 15%.Both components in a small amount penetrate into the mother's milk. Diclofenac 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 (the concentration of the active substance in the synovial fluid 4-6 hours after the administration of the drug is higher than in the plasma, and remains higher for another 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug has not been elucidated.

    Metabolism

    Diclofenac - 50% of the active substance 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, the enzymatic system of cytochrome P450 CYP2C9. The pharmacological activity of metabolites is lower than that of diclofenac.

    The system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. Half-life from the plasma -2 hours 65% of the administered dose is excreted as metabolites by 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, the pharmacokinetic parameters of diclofenac do not change.

    Paracetamol is metabolized in the liver (90-95%): 80% enters the conjugation reaction with glucuronic acid and sulfates with the formation of inactive metabolites; 17% undergoes hydroxylation with the formation of 8 active metabolites, which are conjugated with glutathione with the formation of already inactive metabolites. With a lack of glutathione, these metabolites can block enzymatic, hepatocyte systems and cause their necrosis. In the metabolism of the drug is also involved isoenzyme CYP2E1. T1 / 2 1-4 h. It is excreted by the kidneys in the form of metabolites, mainly conjugates, only 3% unchanged. In elderly patients, the clearance of the drug decreases and T1 / 2 increases.

    Indications:
    Short-term therapy of pain in rheumatic diseases (rheumatoid arthritis, osteoarthritis).Neuralgia, myalgia, lumboeishalgia, 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 and febrile syndrome (pharyngitis, tonsillitis, otitis).
    Contraindications:Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, anamnestic data on the attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, nasal mucosa polyps, bronchial asthma), post-coronary artery bypass grafting, inflammatory bowel disease in the exacerbation phase, severe hepatic insufficiency or active liver disease, marked renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, hematopoietic disorders, hemostasis disorders (incl.hemophilia), pregnancy, children's age, lactation.
    Carefully:
    Ischemic heart disease, cerebrovascular disease, anemia, bronchial asthma, stagnant cardiac failure,

    dyslipidemia / hyperlipidemia, arterial hypertension, edematous syndrome, hepatic or renal failure, benign hyperbilirubinemia (including Gilbert's syndrome), alcoholism, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes mellitus, peripheral arterial disease, post-extensive condition surgical interventions, induced porphyria, advanced age, systemic connective tissue diseases.
    Pregnancy and lactation:

    Dosing and Administration:

    Inside, without chewing, during or after a meal, with a small amount of water. Adults take 1 tablet 2-3 times a day. Duration of therapy up to 7 days.

    Side effects:

    Gastrointestinal tract:

    more often 1% - abdominal pain, sensation of bloating, diarrhea, nausea, constipation, flatulence, increased level of "liver" enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;

    vomiting, jaundice, melena, the appearance of blood in the stool, the defeat of the esophagus, aphthous stomatitis, dry mucous membranes (including the mouth), hepatitis (possibly lightning), liver necrosis, cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis , cholecystopancreatitis, colitis ..

    Nervous system:

    more often 1% - headache, dizziness;

    less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, general weakness, disorientation, nightmares, fear.

    Sense organs:

    more often 1% - noise in the ears;

    less than 1% - blurred vision, diplopia, a taste disorder, reversible or irreversible hearing loss, scotoma.

    Skin:

    more often 1% - skin itch, skin rash;

    less often 1% - alopecia, urticaria, eczema, toxic dermatitis, multi-form exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, small-spot hemorrhages.

    Genitourinary system:

    more often 1% - fluid retention;

    less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.

    Hematopoiesis and the immune system:

    less than 1% - anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of the course of infectious processes (including the development of necrotizing fasciitis).

    Respiratory system:

    less than 1% - cough, bronchospasm, laryngeal edema, pneumonitis.

    The cardiovascular system:

    less than 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain.

    Allergic reactions:

    less often 1% - anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.

    Overdose:
    The severity of an overdose, first of all, is due to the presence of paracetamol in the preparation.

    Symptoms: during the first 24 hours after administration - pallor of the skin, nausea, vomiting, anorexia, abdominal pain; disturbance of glucose metabolism, metabolic acidosis.Symptoms of liver dysfunction may appear 12-48 hours after an overdose. In severe overdose - liver failure with progressive encephalopathy, coma, death; acute renal failure with tubular necrosis (including in the absence of severe liver damage); arrhythmia, pancreatitis. Hepatotoxic effect in adults is manifested when taking 10 g or more. Treatment: the introduction of donors of SH-groups and precursors of glutathione -methionine synthesis 8-9 hours after overdose and acetylcysteine ​​after 12 hours. The need for additional therapeutic measures (further introduction of methionine, iv injection of acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as from the time that passed after his admission.
    Interaction:
    The interaction is due to the active ingredients included in the preparation: diclofenac and paracetamol.

    Diclofenac:

    - Increases the concentration in the plasma 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) the risk of bleeding increases (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 (due to an increase in their concentration in the plasma);

    - Acetylsalicylic acid reduces the concentration of diclofenac in the blood;

    - 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 gastrointestinal tract;

    - Simultaneous administration 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.

    Paracetamol:

    - Reduces the effectiveness of uricosuric medicines;

    - The concomitant use of paracetamol in high doses increases the effect of anticoagulant drugs (a decrease in the synthesis of procoagulant factors in the liver);

    - Inductors of microsomal oxidation in the liver (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants), ethanol and hepatotoxic drugs increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication even with a slight overdose;

    - Long-term use of barbiturates reduces the effectiveness of paracetamol;

    - Ethanol promotes the development of acute pancreatitis and liver damage;

    - Inhibitors of microsomal oxidation (incl. cimetidine) reduce the risk of hepatotoxic action;

    - Simultaneous long-term administration of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer;

    - Diflunisal increases the plasma concentration of paracetamol by 50% - the risk of developing hepatotoxicity;

    - Myelotoxic drugs enhance the manifestation of hematotoxicity of paracetamol.
    Special instructions:
    During the treatment, the drug should monitor the pattern of peripheral blood, liver, kidney function, examination of feces for the presence of blood.

    Patients taking the drug should refrain from activities that require increased attention and rapid mental and motor reactions, alcohol consumption.

    Do not simultaneously take additional NSAIDs, due to the increased risk of unwanted reactions.

    When using the drug, the laboratory parameters may be distorted in the quantitative determination of glucose and uric acid in the plasma.
    Form release / dosage:Tablets 50 mg + 500 mg.
    Packaging:For 10 tablets in a blister of PVC / aluminum. For 1 or 10 blisters together with instructions for use in a pack of cardboard.
    Storage conditions:In a dry, protected from light place at a temperature of no higher than 25 ° C.Keep out of the reach of children.
    Shelf life:4 years. Do not use at the end of the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005212/10
    Date of registration:07.06.2010
    The owner of the registration certificate:Outline Pharma Pvt. Ltd.Outline Pharma Pvt. Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia
    Information update date: & nbsp17.02.2016
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