Composition, form of production and packaging
Tablets, covered with enteric coating 1 tab.
diclofenac sodium 25 mg
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
10 pieces. - packings cellular planimetric (3) - packs cardboard.
30 pcs. - banks of dark glass (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Diclofenac has anti-inflammatory, analgesic, analgesic and antipyretic effects. 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. In injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema. Like all NSAIDs, the drug has anti-aggregative activity.
Absorption is fast and complete, food slows the absorption rate by 1-4 h and reduces C max of diclofenac in plasma by 40%. After oral administration, 25 mg C max - 1.0 Ојg / ml is achieved after - 2-3 hours. The concentration in the plasma is linear depending on the amount of the administered dose.
Changes in the pharmacokinetics of diclofenac against a background of repeated administration are not noted, diclofenac does not accumulate.
Bioavailability - 50%. The connection with plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into the synovial fluid; C max in synovial fluid is observed 2-4 hours later than in plasma. T 1/2 from the synovial fluid 3-6 hours (the concentration of 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 diclofenac concentration in synovial fluid and its clinical efficacy has not been elucidated.
Metabolism : 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. The isozyme CYP2C9 is involved in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac. The system clearance is 350 ml / min, V d - 550 ml / kg. T 1/2 from the plasma - 2 h. 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. Diclofenac penetrates into breast milk.
Inflammatory and degenerative diseases of the musculoskeletal system , including rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), osteoarthritis, gouty arthritis, bursitis, tenosynovitis. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.
Pain syndrome: headache (including migraine) and toothache, lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis, with oncological diseases, post-traumatic and postoperative pain syndrome, accompanied by inflammation.
Algodismenorea: inflammatory processes in the small pelvis, including adnexitis.
Infectious and inflammatory diseases of the ENT - organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media.
To achieve a quick desired therapeutic effect take 30 minutes before meals. In other cases, take before, during or after a meal, in an undigested form, with plenty of water. Adults and adolescents with 15 years of age - 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.
With juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg body weight.
The approximate mode of application is shown in the table:
Age (body weight, kg) Single dose (number of tablets) Daily dose (number of tablets)
6-7 years (20-24) 1  1 
8-11 years old (25-37) 1  2-3 [50-75]
12-14 years old (38-50) 1-2 [25-50] 3-4 [75-100]
Older than 15 and adults 1-2 [25-50] 2-6 [50-150]
On the part of the gastrointestinal tract: more often 1% - abdominal pain or spasm, sensation of bloating, diarrhea, nausea, constipation, flatulence, increased activity of "hepatic" trannaminases, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding without ulcers; vomiting, jaundice, melena, the appearance of blood in the stool, the defeat of the esophagus, aphthous stomatitis, dryness of the mucous membranes (including the oral cavity), hepatitis (possibly lightning), liver necrosis, cirrhosis, hepatorenal syndrome, appetite change, pancreatitis (including concomitant hepatitis), cholecystopancreatitis, colitis.
From the 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.
From the sense organs: more often 1% - noise in the ears; less than 1% - blurred vision, diplopia, a taste disorder, reversible or irreversible hearing loss, scotoma.
From the skin: more often 1% - skin itching, 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.
On the part of the genitourinary system: more often 1% - fluid retention; less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia.
From the hemopoiesis and 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).
On the part of the respiratory system: less than 1% - cough, bronchospasm, laryngeal edema, pneumonitis.
From the cardiovascular system: less than 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain.
Allergic reactions: less than 1% - anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.
Hypersensitivity (including other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in anamnesis), erosive and ulcerative lesions of the stomach and 12-finger intestines, active gastrointestinal bleeding, inflammatory bowel disease, severe hepatic and heart failure; period after aortocoronary shunting; severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, active liver disease, confirmed hyperkalemia, pregnancy (III trimester), lactation period, children's age (up to 6 years - for tablets coated with enteric membrane 25 mg).
Hereditary lactose intolerance, impaired absorption of glucose-galactose, deficiency of lactase.
Carefully. Stomach ulcer and duodenal ulcer, ulcerative colitis, Crohn's disease, liver disease in history, hepatic porphyria, chronic heart failure, arterial hypertension, a significant decrease in the volume of circulating blood (BCC) (including after extensive surgery), elderly patients (including those receiving diuretics, weakened patients and patients with low body weight), bronchial asthma, simultaneous reception of GCS (including prednisolone), anticoagulants (including warfarin), antiplatelet agents ( clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), ischemic heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, chronic renal failure (QC 30- 60 ml / min), the presence of Helicobacter pylori infection, prolonged use of NSAIDs, alcoholism, severe physical illness.
PREGNANCY AND LACTATION
Contraindicated in the III trimester of pregnancy. In the I and II trimester of pregnancy should be used according to strict indications and in the lowest dosage.
Diclofenac penetrates into breast milk. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated: severe renal failure (creatinine clearance (CK) less than 30 ml / min), progressive kidney disease.
With caution: chronic renal failure (KK 30-60 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated: severe hepatic impairment, active liver disease.
With caution: liver disease in the anamnesis, hepatic porphyria.
APPLICATION FOR CHILDREN
Contraindicated in childhood (up to 6 years - for tablets, coated with enteric-coated 25 mg).
APPLICATION IN ELDERLY PATIENTS
With caution: elderly patients (including those receiving diuretics, weakened patients and patients with low body weight).
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.
Symptoms: vomiting, dizziness, headache, shortness of breath, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, dysfunction of the liver and kidneys.
Treatment: gastric lavage, the introduction of activated charcoal, 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.
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; against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract).
Reduces the effects of hypotensive and hypnotics.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (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 agents.
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 increases nephrotoxicity.
Simultaneous use with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract.
Diclofenac enhances the effect of drugs that cause photosensitivity. Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.
Antibacterial drugs from the quinolone group - the risk of seizures.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The preparation should be stored in a dry place, protected from light, inaccessible to children, at a temperature not exceeding 25 В° РЎ.
Shelf life - 3 years. Do not use after the expiry date printed on the package