Диклофенак-Акри® ретард

General characteristics. Structure:

Active ingredient: 100 mg of diclofenac of sodium.

Excipients: лудипресс, oksipropilmetiltsellyuloza, magnesium stearate, aerosil, stearic acid, polyethyleneglycol, glycerin, titanium dioxide, gland oxide.

The drug rendering antiinflammatory, analgetic, febrifugal and anti-aggregation action.

Pharmacological properties:

Pharmacodynamics. Not selectively oppressing a tsikloksigenaza 1 and 2, breaks 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.

Pharmacokinetics. Absorption — bystry and full, food slows down absorption speed. 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.

As a result of the slowed-down release of active agent peak concentration in plasma is lower than that which is formed at administration of drug of short action; however it remains high after reception for a long time. The maximum concentration of 0,5-1 mkg/ml, time of achievement of the maximum concentration — 5 hours after reception of 100 mg of a tablet of the prolonged action.

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 — 3-6 h (concentration of active agent in synovial fluid in 4-6 h after administration of drug are 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. Metabolism results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. Pharmacological activity of metabolites is lower, than diclofenac.

The system clearance makes 260 ml/min. of 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 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 same, as well as at patients without liver diseases.

Indications to use:

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

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

Lumbago, sciatica, neuralgia, mialgiya.

Diseases of circumarticular fabrics (tendovaginitis, bursitis).

The posttraumatic pain syndromes which are followed by an inflammation, postoperative pains, migraine, renal colic; primary альгодисменорея, adnexitis, proctitis.

Infectious and inflammatory diseases of ENT organs with the expressed pain syndrome (pharyngitis, tonsillitis, otitis), the residual phenomena of pneumonia.

Feverish syndrome.

Route of administration and doses:

Inside, without chewing, to, in time or after food, washing down with a small amount of water. The adult — on 100 mg of 1 times a day.

At a dysmenorrhea and attacks of migraine - to 200 mg/days. At reception of 100 mg ретард in need of increase in a daily dose up to 150 mg/days it is possible to accept in addition on 1 usual tablet (50 mg). Maximum daily dose of 150 mg.

Features of use:

For bystry achievement of desirable therapeutic effect accept in 30 min. prior to 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.

Use at pregnancy and a lactation. Contraindicated.

Side effects:

Frequent side effects develop more than in 1%, infrequent — less than 1%, more than 0,1%, rare — less than 0,1%.

From the alimentary system: frequent — the NPVP-gastropathy (a gastralgia, nausea, vomiting, diarrhea, abdominal pains, a meteorism), erosive cankers of the digestive tract (DT), bleeding GIT, nonspecific colitis, dryness in a mouth, a lock. Infrequent — pancreatitis, aphthous stomatitis, a glossitis, increase in activity of "hepatic" transaminases, toxic hepatitis, fulminantny hepatitis.

From a nervous system: frequent — a headache, dizziness, increased fatigue, sleeplessness, uneasiness, "dreadful" dreams, disturbance of flavoring feelings. Infrequent — paresthesias, decrease in memory, a disorientation, irritability, a depression, psychotic reactions, anorexia. Rare — spasms, a tremor, aseptic meningitis.

From sense bodys: infrequent — decrease in visual acuity, a diplopia, scotoma, decrease in hearing, a sonitus.

From integuments: frequent — a skin itch, skin rash (preferential erythematic, urti-karny), a Quincke's disease. Infrequent — eczema, a photosensitization, an allergic purpura, much формная an exudative erythema (including Stephens-Johnson's syndrome). Seldom — an erythrosis, an alopecia, a toxic epidermal necrolysis (scalded skin syndrome).

From an urinary system: frequent — a nephrotic syndrome (hypostases). Infrequent — an acute renal failure, a hamaturia, a proteinuria, an oliguria, intersticial nephrite, a papillary necrosis, cystitis.
From bodies of a hemopoiesis: infrequent — thrombocytopenia, a leukopenia, anemia. Rare — an agranulocytosis, hemolitic anemia.

From respiratory system: infrequent — a bronchospasm.

From cardiovascular system: frequent — heartbeat, a stethalgia, arrhythmias. Infrequent — increase in arterial pressure, system anaphylactic reactions, including shock.

Endocrine frustration: rare — impotence.

Interaction with other medicines:

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

Against the background of kaliysberegayushchy diuretics the risk 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 glucocorticoids (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.

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

Cyclosporine and drugs of gold increase influence of diclofenac on synthesis of prostaglandins in kidneys that is shown by increase in nephrotoxicity.

Simultaneous use with ethanol, colchicine, corticotropin and drugs of a St. John's Wort increases risk of development of bleedings in a GIT.

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, the lactation period.

With care. The induced acute hepatic porphyrias, heavy abnormal liver functions and kidneys, heart failure.

Overdose:

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

Treatment: a gastric lavage, administration of absorbent carbon, the symptomatic therapy directed to elimination of increase in the ABP, a renal failure, spasms, irritations of a GIT, respiratory depression. The artificial diuresis, a hemodialysis are ineffective.

Storage conditions:

List B. To store at a temperature not above 25 °C in the place protected from light. In the dry place. To store in the place, unavailable to children. Not to use after expiry date. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets ретард, coated, 0,1 g. Primary packaging: on 10 tablets in a blister strip packaging. Secondary packaging: on 1, 2 or 3 blister strip packagings with the application instruction in a cardboard pack.