Диклоген®

General characteristics. Structure:

Active ingredient: 75 mg of diclofenac in 3 ml of solution.

Excipients: water for injections, benzyl alcohol, Mannitolum, sodium sulfite, propylene glycol, hydrochloric acid.

Pharmacological properties:

Pharmacodynamics. Diklogen is a non-steroidal anti-inflammatory drug (NPVS) from group of derivatives of phenylacetic acid. Drug has considerable antiinflammatory, analgetic and moderate febrifugal effects. The main role in the mechanism of effect of drug is played by braking of biosynthesis of prostaglandins which matters important in a pathogeny an inflammation, pains and fevers.

At rhematoid diseases antiinflammatory and analgetic effect of drug Diklogen before considerable decrease in pain (both at rest, and at the movement), morning constraint, a swelling of joints, and by that, before improvement of a functional condition of the patient. At nonspecific an inflammation that arises after injuries or operations, Diklogen reduces feeling of pain and inflammatory hypostasis. Injection the form of drug is especially shown for appointment in initial stages of therapy of inflammatory and degenerative rheumatological diseases and at pain syndromes of other etiology.

Pharmacokinetics. Drug Diklogen - the tablets covered with a film enterosoluble cover are quickly and completely absorbed in digestive tract. Food slows down the absorption speed, however amount of substance which is soaked up, does not change. The maximum concentration of drug in a blood plasma at reception of tablets Diklogen in a single dose of 50 mg is reached in 2 hours after reception and makes 1,5 mkg / a pier. Concentration of drug in plasma is in linear dependence on size of the accepted dose.

Owing to slow release of active ingredient from drug tablets-retard Diklogen concentration in plasma a little lower, than concentration when using of not prolonged drug form Diklogen of tablets on 50 mg, and removal of active ingredient is slowed down at several o'clock.

After intake of the prolonged drug form Diklogen system bioavailability of active ingredient makes 82% of a corresponding indicator after reception of tablets of 50 mg. At a single dose of drug Diklogen of a tablet-retard on 100 mg the maximum concentration is reached in 4-5 hour and makes 0,45 mkg / a pier.

After intramuscular administration of drug Diklogen, the area under a curve concentration time approximately twice big from corresponding size that is observed at intake.

After reusable administration of drug its pharmacokinetics does not change. Cumulation of drug is noted.

99,7% of active ingredient of drug contact serum proteins, generally albumine - 99,4%.

Active agents of drug Diklogen gets into synovial fluid: here the maximum concentration of drug is noted 2-4 hours later, than in plasma. Time of semi-removal of drug from synovial fluid 3-6 hour. Thus, its concentration in a cavity of a joint exceeds concentration of drug in plasma only in 4-6 hour after its reception inside and remains to higher during the 12th hour.

About 50% of active ingredient of drug Diklogen is metabolized in a liver at the "first" passing.

The elimination half-life makes 1-2 hours. About 60% of a dose of drug are removed in the form of metabolites by kidneys; less than 1% are excreted with urine in an invariable look. Another a part of drug is removed in the form of metabolites with bile. Serious distinctions of pharmacokinetic parameters of drug Diklogen depending on age are not revealed. The system clearance of active agent makes about 263 ml/minutes.

At patients with the expressed renal failures (clearance of creatinine less than 10 ml/minutes.) specific weight removal of metabolites from bile therefore increase in their concentration in blood is not observed increases. Patients with a liver failure have pharmacokinetic parameters of drug such most, as well as in the absence of abnormal liver functions.

Indications to use:

- general and degenerative diseases of joints and backbone:

- a pseudorheumatism, semi-removal from synovial, an ankylosing spondylitis, an osteoarthrosis, a spondylarthrosis;

- rheumatic diseases of circumarticular soft tissues;

- acute gouty arthritis;

- pain syndromes from a backbone;

- posttraumatic and postoperative pain and inflammation;

- primary dysmenorrhea.

Route of administration and doses:

Injections appoint, as a rule, in a dose 75 mg (one ampoule of 3 ml.) in days. Drug solution Diklogen enter deeply into a muscle in upper an external square of buttocks. For this purpose use a standard needle for intramuscular injections. In hard cases (for example, gripes of various origin) as the exception, is allowed uses of two ampoules for days. In such cases it is necessary to remember about what the interval between injections has to make several hours and the following injection it is necessary to do in other buttock.

It is also possible to combine purpose of drug Diklogen of an injection (1 ampoule 75mg/3ml in days) with drug Diklogen of a tablet. The general daily dose of these two dosage forms has to make 150 mg. Diklogen is recommended to enter injections no more than 2 days in a row then to pass tablets to Diklogen.

Features of use:

Diklogen, injections 75mg/3ml should not be mixed in one syringe with solutions of other medicines.

It is necessary to adhere to care at purpose of drug Diklogen to patients who have in the anamnesis of the instruction on gastrointestinal diseases, a round ulcer, ulcer colitis, a disease Krone, and also the patient with the expressed abnormal liver functions. When decrease in volume of blood is possible that circulates (including, at reception of diuretics; to or after large operations), and also at patients with a renal failure, chronic heart failure, arterial hypertension.

Diklogen it is worth applying with care through danger decrease in a renal blood-groove. Special attention it is necessary at treatment of patients of advanced age (the weakened faces and persons with a body underweight) because ulcerations, perforation and bleeding from a GIT brings into them to more serious effects and can arise during any period of therapy, without harbingers or the complicated anamnesis.

To this contingent of patients Diklogen appoint in smaller doses. In the course of treatment by drug necessary systematic control of function of a liver and kidneys, pictures of peripheral blood. If an abnormal liver function with firmness remain, it is necessary to stop Diklogen's reception. It is reasonable to stop administration of drug also in cases of emergence of skin rashes, an eosinophilia, at emergence of a canker of a GIT, bleeding from digestive tract. At drug use Diklogen at patients with a hepatic porphyria can develop porphyrinic crisis. Therefore at their treatment special care is necessary.

If during treatment by drug Diklogen the patient had a dizziness or others disturbance from the central nervous system, then he is recommended to abstain from driving by the car or works with mechanisms that need special attention. At drug use Diklogen it is worth abstaining from alcohol intake.

Side effects:

From the digestive tract (DT): possible pain in epigastriums, nausea, vomiting, diarrhea, abdominal spasms, dyspepsia, a meteorism, anorexia. In isolated cases emergence of the erosive and ulcer defects of a mucous membrane of a GIT complicated gastrointestinal by bleeding, vomiting is possible.

Are in some cases observed disturbance from lower parts intestines (for example, nonspecific hemorrhagic colitis, an exacerbation of ulcer colitis or a disease Krone), locks. Aphthous stomatitis, disturbance from a gullet can develop.

From the central and peripheral nervous system: the headache, dizziness are sometimes observed; seldom - fatigue. In separate isolated cases disturbance of memory, orientation, sight, hearing are possible; frustration of a dream, spasm, irritability, tremor, mental disturbances, depression, excitement, disturbance of flavoring feelings.

Dermatological: are possible an enanthesis; seldom – a small tortoiseshell. The described separate liquid cases of violent rashes, eczemas, a mnogomorfny erythema, Stephens-Johnson's syndrome, a scalded skin syndrome (a toxic epidermal necrosis), an erythrosis, a hair loss, a photosensitization, a purpura.

From kidneys: isolated cases of an acute renal failure, intersticial nephrite, a nephrotic syndrome, papillary to a necrosis are celebrated; hamaturia, proteinariya.

From a liver: tranzitorny increase in activity of hepatic transaminases in blood. Seldom hepatitis (with jaundice or without it).

From peripheral blood: separate cases of development of thrombocytopenia, a leukopenia, an agranulocytosis, hemolitic anemia, aplastic anemia are described.

Allergic reactions: seldom - attacks of bronchial asthma, system anaphylactic-anaphylactoid reactions (including arterial hypotension). Local: morbidity and consolidation in places of injections is seldom noted, and development of abscess and to a necrosis of soft tissues is in exceptional cases noted.

Others: seldom - hypostases. It is noted exceptional cases of developing of tachycardia, breast pain, arterial hypertension.

Interaction with other medicines:

Diklogen can increase concentration of lithium and digoxin in plasma at simultaneous use with drugs which contain these substances. Diklogen with kaliysberegayushchy diuretics can lead drug sharing to increase in level of potassium in blood.

Diklogen, as well as other NPVS, can reduce diuretic effect of "loopy" diuretics; and also to reduce hypotensive action of anti-hypertensive means. Simultaneous use of drug Diklogen with other NPVS, and also with glucocorticoids can increase risk of emergence of side effects.

The described separate cases of developing of bleedings at simultaneous use of drug Diklogen and anticoagulants.

There are separate messages about development of a hypoglycemia or hyperglycemia in patients with a diabetes mellitus who applied Diklogen together with antidiabetic drugs.

It is necessary to reveal care when using NPVS less, as in the 24th hour prior to use or after the end of therapy by a methotrexate because its level in blood (and, therefore, toxicity) can increase.

At drug co-administration Diklogen with cyclosporine increase in toxicity of the last is possible.

Contraindications:

- gastrointestinal diseases in an aggravation phase;

- hypersensitivity to diclofenac of sodium or any auxiliary ingredient which is a part of drug Diklogen is known in this patient (see the section "WAREHOUSE");

- anapsikhichesky certificates about the attacks of bronchial asthma, acute rhinitis connected using acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NPVS);

- disturbance hemopoiesis of the obscure genesis;

- children up to 12 years;

- pregnancy (III trimester).

Dosage forms of drug Diklogen: the tablets-retard covered with a film kishechnorastvorimy cover on 100 mg and solution to injections of 75 mg / 3 ml are not recommended to be applied to therapy at children up to 18 years.

Overdose:

The drug overdose Diklogen is not characterized by the expressed clinical picture. The specific antidote does not exist. At acute poisoning absorption of drug needs to avoid as soon as possible from digestive tract. To appoint a gastric lavage, reception of absorbent carbon and carrying out other symptomatic and maintenance therapy, especially in case of such complications as hypotension, a renal failure, spasms, irritations of a GIT or braking of breath. Use of an artificial diuresis, dialysis or hemotransfusion is inexpedient, that NPVS mostly contact proteins of serum and have extensive metabolism.

Storage conditions:

To store at a temperature that does not exceed 25 °C, in dark, protected from influence of liquid, dust and solar lighting, and the place, unavailable to children. At reception of the above-stated storage conditions the period of validity of drug makes 3 (three) years. It is not recommended to use drug after the termination of the period of validity specified on its packaging!

Issue conditions:

According to the recipe

Packaging:

On 3 ml of solution in ampoules, on 5 or 10 ampoules in planimetric packagings and cardboard packs.