Diclofenac retard Obolensky tab prolong.p / v kish.rastv. 100mg 20 pieces

Description

Composition
Active substance:
1 tablet contains: Sodium diclofenac 100 mg ;.
Excipients:
[Hypromellose (hydroxypropylmethylcellulose), gietelloza (hydroxyethylcellulose), Kollidon SR [80% polyvinyl acetate, 19% povidone, 0.8% sodium lauryl sulfate, silica, 0.2%], sodium alginate, microcrystalline cellulose, magnesium stearate].
Excipients for the shell: [methacrylic acid and ethyl acrylate copolymer (kollikut MAE 100 P), propylene glycol, talc, povidone, titanium dioxide, iron oxide red, iron oxide yellow].
Description:
Coated tablets reddish-brown color, round, biconvex shape. The cross section shows two layers, the inner layer of white or almost white color.
Product form:
Prolonged action tablets, enteric-coated tablets, 100 mg.
10 tablets in blisters of PVC film and aluminum foil printed patent.
1, 2, 3, 5 or 10 contour of cellular packages with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity to active or auxiliary components (including other NSAIDs);
Full or partial combination of asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history);
Erosive and ulcerative lesions of the gastric mucosa and 12 duodenal ulcer, active bleeding of the gastrointestinal tract (GIT);
Inflammatory bowel disease (ulcerative colitis, Crohn’s disease);
Since the aortocoronary bypass surgery; III trimester of pregnancy, lactation;
Severe heart failure;
Cerebrovascular bleeding or other bleeding disorders and hemostasis;
Severe hepatic insufficiency or active liver disease;
Renal failure (creatinine clearance less than 30 mL / min), progressive renal disease, including confirmed by hyperkalemia;
Children up to age 18 years.
Hereditary galactose intolerance, malabsorption of glucose-galactose, severe lactase deficiency
Precautions: anemia, bronchial asthma, cerebrovascular diseases, coronary artery disease (CAD), congestive heart failure, hypertension (AH), peripheral artery disease, edema syndrome, hepatic or renal failure, history of liver disease, dyslipidemia / hyperlipidemia, diabetes diabetes, smoking, inflammatory bowel disease, a significant reduction in circulating blood volume (CBV), including after major surgery, porphyria, old age, including among patients receiving diuretics, debilitated patients with low body weight, diverticular disease, systemic connective tissue disease, pregnancy I-II trimester CC less than 60 ml / min.
Peptic ulcer and 12 duodenal ulcer, ulcerative colitis, Crohn’s disease, medical 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 anticoagulation therapy (e.g. warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), oral corticosteroids (e.g., dexamethazone), selective serotonin reuptake inhibitors (e.g., citalopram, fluoxetine, paroxetine, sertraline).
Indications
Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (ankylosing spondylitis), gouty arthritis, rheumatic soft tissue osteoarthritis of peripheral joints and spine, including radicular syndrome, tenosynovitis, bursitis).
Pain syndrome weak or moderate severity: neuralgia, myalgia, sciatica, post-traumatic pain, accompanied by inflammation, postoperative pain, headache, migraine, tuberculosis, adnexitis, proctitis, toothache.
In the combined therapy of infectious and inflammatory diseases of the ear, nose and throat with severe pain (pharyngitis, tonsillitis, otitis media).
The drug is intended for the symptomatic treatment by reducing pain and inflammation at the time of use, does not affect the progression of the disease.
Interaction with other drugs
Increasing the concentration of digoxin in plasma of methotrexate drugs lithium and cyclosporine.
Reduces the effect of diuretics, potassium-sparing diuretics in the background increases the risk of hyperkalemia; against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) – The risk of bleeding (usually from the gastrointestinal tract).
Reduces the effects of antihypertensive drugs and sleeping pills.
Increases the likelihood of side effects and other NSAIDs glucocorticosteroid means (digestive tract bleeding), the toxicity of methotrexate and cyclosporine nephrotoxicity.
Acetylsalicylic acid reduces the concentration of diclofenac in the blood.
Simultaneous use of paracetamol with increased risk of nephrotoxic effects of diclofenac.
Reduces the effect of hypoglycemic agents.
Cefamandole, cefoperazone, cefotetan, valproic acid and increase the incidence plicamycin hypoprothrombinemia.
Cyclosporine and preparations of gold increases the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases the nephrotoxicity.
Simultaneous with the appointment ethanol, colchicine, corticotropin and drugs St. John’s wort increases the risk of gastrointestinal bleeding.
Diclofenac enhances the action of drugs that cause photosensitization.
Drugs that block tubular secretion, increase the concentration of diclofenac in plasma, thereby increasing its toxicity.
Antibacterial drug of the quinolone group increase the risk of seizures.
Selective serotonin reuptake inhibitors increase the risk of bleeding from the gastrointestinal tract.
Drugs that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.
Drugs that block tubular secretion, increase the concentration of diclofenac in plasma, thereby enhancing its efficacy and toxicity.
Overdose
Symptoms: dizziness, headache, hyperventilation, dizziness, vomiting, bleeding from the gastrointestinal tract, diarrhea, tinnitus, convulsions, with significant overdose – acute renal failure, hepatotoxicity.
Treatment: gastric lavage, administration of activated charcoal. Symptomatic treatment is aimed at eliminating the increase in blood pressure, renal failure, convulsions, gastrointestinal irritation, respiratory depression. Forced diuresis, hemodialysis ineffective (due to significant bond and intense protein metabolism).
pharmachologic effect
Pharmacological group:
NSAIDs.
Pharmacodynamics:
Nonsteroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid; anti-inflammatory, analgesic and antipyretic effect.
Non-selectively inhibiting cyclooxygenase 1 and 2 (and TSOG1 TSOG2) gives the metabolism of arachidonic acid, reduces the amount of prostaglandins in inflammation. Most effective for pain of inflammatory nature. Like all NSAIDs, the drug has antiplatelet effect. In rheumatic diseases inflammatory and analgesic effect of diclofenac contributes to a significant reduction in the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. When trauma, postoperative diclofenac reduces pain and inflammatory edema.
Pharmacokinetics:
Absorption is fast and complete. The food slows the rate of absorption for 1-4 hours and reduces the maximum concentration (Cmax) is 40%.
As a result, sustained release of drug in plasma Cmax lower than that created by the administration of pharmaceuticals (drugs) short-acting; however, it remains high for a long time after administration. Cmax – 0,5-1,0 g / ml, the time to reach maximum plasma concentration (TCmax) – 5 hours after administration of 100 mg tablets of prolonged action.
Changes in the pharmacokinetics of diclofenac on the background of multiple doses is not marked. Not accumulates at the recommended interval between meals.
Bioavailability – 50%. Relationship to plasma proteins – more than 99% (most associated with albumin). It passes into breast milk, synovial fluid; Cmax observed in the synovial fluid for 2-4 hours later than in plasma. The half-life (T1 / 2) of the synovial fluid – 3-6 h (the drug concentration in the synovial fluid after 4-6 h after administration is higher than in the plasma, and remains higher for a further 12 hours). 50% of the active substance is metabolised during the “first pass” through the liver. Metabolism occurs as a result of single or multiple hydroxylation and conjugation with glucuronic acid. The metabolism of the drug participates enzyme system cytochrome P450 CYP2C9. The pharmacological activity of the metabolites is less than diclofenac.
Systemic clearance is 206 ml / min. . T1 / 2 of plasma – 1-2 h 60% of the administered dose is excreted through the kidneys as metabolites; less than 1% is excreted in unaltered form, the remainder of the dose excreted in bile as metabolites.
In patients with severe renal failure (creatinine clearance (CC) of less than 10 ml / min) increases the excretion of metabolites in the bile, thus increasing their concentration in the blood is not observed.
In patients with chronic hepatitis or compensated cirrhosis pharmacokinetic parameters are not changed.
Diclofenac passes into breast milk.
Pregnancy and breast-feeding
Diclofenac retard drug is contraindicated for use in the III trimester of pregnancy and during breastfeeding. Application in I-II trimester of pregnancy is possible with caution is justified, if the benefit to the mother outweighs the potential risk to the fetus.
Conditions of supply of pharmacies
Prescription.
side effects
The frequency of side effects emerged when taking carvedilol, classified according to World Health Organization recommendations: very often – at least 10%; often – at least 1% but less than 10%; infrequently – at least 0.1% but less than 1%; rarely – at least 0.01% but less than 0.1%; very rarely – less than 0.01%, including isolated reports.
On the part of the digestive system: often – epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased transaminases; rarely – gastritis, proctitis, bleeding from the gastrointestinal (vomiting blood, melena, bloody diarrhea), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, liver dysfunction; very rarely – stomatitis, glossitis, esophagitis, non-specific haemorrhagic colitis, exacerbation of ulcerative colitis or Crohn’s disease, constipation, pancreatitis, fulminant hepatitis.
From the nervous system: often – headache, dizziness; rarely – sleep disturbance, drowsiness; very rarely – a violation of the sensitivity, including paresthesia, memory disturbances, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, confusion, depression, insomnia, night “nightmares”, irritability, personality disorders.
From the senses: common – vertigo; very rarely – blurred vision (blurred vision, diplopia), impaired hearing, tinnitus, taste disturbance.
From the urinary system: often – fluid retention; very rarely – acute renal failure, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.
From the side of hematopoiesis and immune system: very rarely – thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.
Allergic reactions: seldom – anaphylactic / anaphylactoid reactions including marked reduction of blood pressure (BP) and shock; very rarely – angioneurotic edema (including face).
With the cardiovascular system: very rarely – palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
The respiratory system: rarely – bronchial asthma (including shortness of breath); very rarely – pneumonitis.
For the skin: often – skin rash; rarely – urticaria; very rarely – a painful rash, eczema, including multiforme and Stevens-Johnson syndrome, Lyell syndrome, exfoliative dermatitis, itching, loss of hair, photosensitivity, purpura, including allergic.
Other: rarely – swelling.
special instructions
In order to quickly achieve the desired therapeutic effect, taking for 30 minutes before a meal. In other cases take before, during or after a meal with liquid, squeezed with sufficient water.
Due to the importance of prostaglandins in maintaining renal blood flow, should exercise extreme caution 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, there is a decrease in the bcc (for example, after extensive surgery). If in such cases, prescribe diclofenac, is recommended as a precautionary measure to monitor renal function.
In patients with renal insufficiency with CC less than 10 ml / min equilibrium concentration of metabolites in the plasma should theoretically be significantly higher than in patients with normal renal function, but it really does not occur because in this situation increases the excretion of metabolites in the bile.
In patients with hepatic impairment (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism did not differ from similar processes in patients with normal liver function. During long-term therapy is necessary to monitor liver function, peripheral blood picture, analysis of fecal occult blood.
Due to the adverse effect on fertility, women wishing to become pregnant, the drug is not recommended. At infertile patients (including undergoing examination) it is recommended to cancel the drug.
To reduce the risk of adverse effects on the gastrointestinal tract should use the lowest effective dose of the lowest possible short course.
Effects on ability to drive vehicles and management mechanisms
The treatment period may reduce the rate of mental and motor reactions, so you must refrain from driving vehicles and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
Storage conditions
In a dry, dark place at a temperature not higher than 25 C. Keep out of reach of children.
Dosing and Administration
The inside is not liquid, squeezed small amounts of water, as a rule, during and after meals.
Diclofenac depot designate 100 mg 1 time per day (with migraine attacks and dysmenorrhea – 200 mg / day). When receiving the 100 mg sustained-release tablets with increasing daily dose necessary, up to 150 mg may further receive a conventional 1 tablet (50 mg) diclofenac.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist