Диклоген®

General characteristics. Structure:

Active ingredient: 50 mg of diclofenac of sodium.

Excipients: lactose, calcium dihydrophosphate, povidone, starch corn, starch glikolit sodium, magnesium stearate, talc the purified, isopropyl alcohol, a methylene chloride, dye yellow (Opadry Yellow mix/OY-P-5290).

Pharmacological properties:

Pharmacodynamics. Has antiinflammatory, analgetic and febrifugal effect. Oppresses to a tsikloksigenaz 1 and 2, breaking metabolism of arachidonic acid, reduces amount of prostaglandins (Pg) both in the inflammation center, and in healthy fabrics, suppresses exudative and proliferative phases of an inflammation. Has antiagregantny effect.

Pharmacokinetics. Absorption - bystry and full, food slows down absorption speed. After oral administration of 50 mg the maximum concentration (Cmax) - 1.5 mkg/ml are reached through - 2-3 h. Concentration in plasma is in linear dependence on size of the entered dose. Change of pharmacokinetics of diclofenac against the background of repeated introduction is not noted. Does not kumulirut at observance of the recommended interval between meals.

Bioavailability - 50%. Communication with proteins of plasma - 95-98% (the most part contacts albumine). Gets into synovial fluid; The Maximum concentration in synovial fluid is observed on 2-4 h later, than in plasma. Time of semi-removal from synovial fluid in 4-6 h after administration of drug is higher, than in plasma, and remain higher during 12 h).

Metabolism: 50% of active agent are exposed to metabolism during "the first passing" through a liver; The Area under a curve of concentration is twice less after peroral administration of drug, than after parenteral administration of the same dose.

Metabolism results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. Pharmacological activity of metabolites - below, than diclofenac.

The system clearance makes 260 ml/min. Plasma semi-removal time - 1-2 h 60% of the entered dose is removed in the form of metabolites through kidneys; less than 1% are removed in not changed look, other part of a dose is removed in the form of metabolites with bile.

At patients with the expressed renal failures (clearance of creatinine less than 10 ml/min.) removal of metabolites with bile increases, at the same time increase in their concentration in blood is not observed.

At patients with chronic hepatitis or the compensated cirrhosis pharmacokinetic parameters of diclofenac same, as well as at patients without liver diseases.

Indications to use:

Inflammatory diseases of a musculoskeletal system (a pseudorheumatism, the psoriasis, juvenile chronic arthritis ankylosing a spondylitis; gouty arthritis).

Degenerative diseases of a musculoskeletal system (the deforming osteoarthrosis, osteochondrosis).

Lumbago, sciatica, neuralgia, mialgiya, tendovaginitis, bursitis.

The posttraumatic pain syndrome which is followed by an inflammation, postoperative pain, migraine, renal colic; primary альгодисменорея, adnexitis, proctitis.

As a part of complex therapy of infectious and inflammatory diseases of ENT organs with the expressed pain syndrome (pharyngitis, tonsillitis, otitis).

Route of administration and doses:

Inside, without chewing, in time or after food, washing down with a small amount of water. The adult - on 50 mg 2-3 times a day. At achievement of optimum therapeutic effect the dose is gradually reduced and pass to the supporting treatment in a dose 50 mg/days. The maximum daily dose - 150 mg.

For children over 12 years a daily dose to 2 mg/kg of the child. At a juvenile pseudorheumatism the daily dose can be increased to 3 mg/kg.

Features of use:

For bystry achievement of desirable therapeutic effect accept in 30 min. Before meal. In other cases accept to, in time or after food in not chewed look, washing down with enough water.

Because of an important role of prostaglandins in maintenance of a renal blood-groove patients should show extra care at appointment with a heart or renal failure, and also at therapy of the elderly people accepting diuretics and patients at whom for any reason decrease in volume of the circulating liquid is observed (for example, after large surgical intervention). If in such cases appoint diclofenac, recommend to control function of kidneys as a precautionary measure.

At patients with a liver failure (chronic hepatitis, the compensated cirrhosis) the kinetics and metabolism do not differ from similar processes at patients with normal function of a liver. When performing long therapy it is necessary to control function of a liver, a picture of peripheral blood, the analysis a calla on the occult blood.

It is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: a gastralgia, nausea, vomiting, diarrhea, a meteorism, anorexia, increase in activity of "hepatic" transaminases, gastrointestinal bleeding (a hematemesis, a melena), hepatitis with jaundice or without jaundice, fulminant hepatitis, pancreatitis, nonspecific colitis with bleeding, GIT erosive cankers, aphthous stomatitis, a glossitis, a lock, abdominal pain, dryness in a mouth.

From a nervous system: headache, dizziness, increased fatigue, disturbance of perception, paresthesia, decrease in memory, orientation loss, decrease in visual acuity, diplopia, decrease in hearing, sonitus, sleeplessness, irritability, spasms, depression, uneasiness, "dreadful" dreams, tremor, psychotic reactions, disturbance of flavoring feelings, aseptic meningitis, scotoma.

From skin: skin itch, skin rash (preferential erythematic and urtikarny), Quincke's disease, eczema, allergic purpura, mnogoformny exudative erythema (century of h Stephens-Johnson's syndrome), erythrosis, toxic epidermal necrolysis (Lyell's disease), alopecia, photosensitization.

From an urinary system: acute renal failure, hamaturia, proteinuria, intersticial nephrite, nephrotic syndrome, papillary necrosis, oliguria, cystitis.

From bodies of a hemopoiesis: thrombocytopenia, leukopenia, agranulocytosis, hemolitic anemia, aplastic anemia.

From cardiovascular system: heartbeat, stethalgia, arrhythmias, increase in the ABP.

Others: impotence, hypostases, a bronchospasm, system anaphylactic reactions (including shock).

Interaction with other medicines:

Increases concentration in plasma of digoxin, drugs of lithium and cyclosporine.

Against the background of kaliysberegayushchy diuretics the risk of development of a hyperpotassemia, against the background of anticoagulants - risk of bleedings amplifies.

Reduces effects diuretic, hypotensive and hypnagogues. Increases probability of emergence of side effects of NPVP and glucocorticosteroids (gastrointestinal bleedings), toxicity of a methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces concentration of diclofenac in blood.

At simultaneous use with peroral antidiabetic drugs are possible both hypo - and a hyperglycemia.

Against the background of thrombolytic means (an alteplaza, Streptokinasa, an urokinase) – risk of bleedings (the GIT is more often).

Tsefamandol, цефаперазон, цефотетан, valproic acid, пликамицин increases the frequency of development of a prothrombinopenia.

Cyclosporine and drugs of gold potentsiirut influence of diclofenac on synthesis of prostaglandins in kidneys that increases nephrotoxicity ДИКЛОГЕНА®.

Simultaneous use with paracetamol increases risk of development of nephrotoxic effects ДИКЛОГЕНА®.

Simultaneous use with alcohol, glucocorticosteroids, colchicine, corticotropin and drugs of a St. John's Wort increases risk of development of the gastrointestinal complications accompanied with bleedings. Reduces hypotensive activity of vazodilatator.

Contraindications:

Hypersensitivity (including to other NPVP), erosive cankers of the digestive tract (DT) (in an aggravation phase), "aspirinovy" asthma, hemopoiesis disturbances, pregnancy, younger children's age (up to 6 years), the lactation period. With care - the induced acute hepatic porphyria, heavy abnormal liver functions and kidneys, heart failure, advanced age.

Overdose:

Symptoms: dizziness, a headache, a hyperventilation of lungs, consciousness opacification, children have myoclonic spasms, nausea, vomiting, abdominal pain, bleedings, an abnormal liver function and kidneys.

Treatment: a gastric lavage, administration of absorbent carbon, the symptomatic therapy directed to elimination of increase in arterial pressure, a renal failure, spasms, irritations of a GIT, respiratory depression.

The artificial diuresis, hemodialysis are ineffective.

Storage conditions:

List B. At a temperature which is not exceeding 25 °C in the dry and dark place unavailable to children. A period of validity - 3 years. Not to use until expiry date.

Issue conditions:

According to the recipe

Packaging:

5 blisters on 10 tablets with the instruction are packed into a cardboard box.