Diclofenac

General characteristics. Structure:

Active agent – diclofenac of sodium 0, 01 of.

Excipients: carbomer, a macrogoal (poly(ethylene oxide) 400), propylene glycol, oil mint, Natrium benzoicum, alcohol of ethyl 96%, the water purified.

Pharmacological properties:

Pharmacokinetics. The maximum concentration in plasma at chrezkozhny is 1% less than adsorption, than at parenteral use.

When putting gel diclofenac concentrates on skin of knee joints and joints of hands in synovial fluid and fabrics more than in plasma, 99,7% of diclofenac contact proteins of plasma.

Part of diclofenac biotransformirutsya by a glyukoronization of an intact molecule, but the most part biotransformirutsya by a hydroxylation with formation of several derivatives, two of these metabolites are biologically active, but in much smaller degree, than diclofenac.

Diclofenac and its metabolites, generally in the form of glyukoronid, are removed preferential with urine. The general system plasma clearance of diclofenac averages 263ml/mines, and the final period of removal of a 1-2chas.

Pharmacokinetics in special clinical cases. The plasma clearance of diclofenac does not depend on a liver or renal failure, but the clearance of metabolites in this case can be reduced.

 

Pharmacodynamics. Diclofenac – antiinflammatory drug with the expressed analgeziruyushchy action. The main active ingredient – sodium diclofenac – oppresses activity of cyclooxygenase which is the main enzyme of metabolism of arachidonic acid, reducing at the same time synthesis of prostaglandins (PG), kinin and other mediators of an inflammation. At rheumatic diseases reduces joint pains, and also morning constraint, promotes increase in volume of movements.

Indications to use:

- the pseudorheumatism ankylosing a spondylarthritis as a part of complex therapy;

- gouty, infectious, psoriasis arthritis as a part of complex therapy;

- osteoarthrosis;

- bursitis, tendovaginitis;

- miositis;

- neuralgia, mialgiya and other diseases of a musculoskeletal system which are followed by an inflammation and a pain syndrome;

- traumatic injuries of sinews, sheaves, muscles and joints (stretchings, dislocations, bruises) without disturbance of integrity of integuments.

Route of administration and doses:

Outwardly. 1,0-2,0g (1 cm of a column of gel) gel apply to adults on skin, easily rubbing throughout 1-2min 2-4 times a day.

The average daily dose is equal 4,0g gel.

Duration of treatment depends on indications and noted effect.

The average duration of a course of treatment – 10-14 days.

After 2 weeks of use of drug it is necessary to consult with the doctor.

After putting drug of a hand it is necessary to wash up.

Features of use:

Gel is intended only for external use.

Drug is recommended to be applied only on the unimpaired skin, avoiding hit of ointment on sites of damage and open wounds. It is not necessary to allow hits of drug on mucous membranes (a mouth, eyes and others).

Duration of a course of treatment should not exceed 14 days without consultation of the doctor.

At the expressed abnormal liver functions and kidneys, chronic heart failure and advanced age, use of drug is shown only after consultation of the doctor.

Use of drug can provoke an aggravation of a hepatic porphyria therefore its use for such group of patients has to be carried out with care.

It is necessary to avoid action of direct sunshine.

After imposing it is not necessary to apply an occlusive bandage.

When drawing on the big surfaces of skin the risk of development of system side effects increases for a long time.

Drug does not exert impact on driving and potentially dangerous mechanisms.

Side effects:

Local reactions:

- an itch, a hyperemia, feeling of heat, burning in a drug site of application;

- allergic rash.

System reactions are possible:

- a bronchospasm, system anaphylactic reactions, including shock;

- appetite loss, nausea, a meteorism, pains in epigastric area;

- formation of infiltrate, abscess, necrosis of fatty tissue;

- dizziness, headache, sonitus;

- excitement, sleeplessness or drowsiness, irritability, feeling of fatigue, mental disturbances, depression;

- paresthesias;

- vision disorder;

- spasms, tremor;

- anemia, leukopenia, thrombocytopenia, agranulocytosis;

- photosensitization.

Interaction with other medicines:

At use of drug in this dosage form interaction with other medicines is not established. However, especially proceeding from a possibility of simultaneous use of gel and tablets of sodium of diclofenac (at the same time the daily dose of the last should not exceed 50 mg), it is necessary to consider that the last can exponentiate specific effects and ulcerogenic action of corticosteroids, increase concentration of digoxin in blood, weaken effect of thiazide diuretics and furosemide.

The combined use with kaliysberegayushchy diuretics leads to a hyperpotassemia. The therapeutic effectiveness at use with salicylates decreases, at the same time ulcerogenic action increases by a mucous membrane of a stomach. When using along with anticoagulants it is necessary to control system of a blood coagulation.

Contraindications:

- hypersensitivity to drug components (including to other non-steroidal anti-inflammatory drugs);

- the bronchial asthma, a small tortoiseshell or rhinitis provoked by use of acetylsalicylic acid (salicylates);

- peptic ulcer of a stomach and 12-perstny gut;

- disturbances of a hemopoiesis of an unknown etiology;

- disturbance of integrity of integuments;

- children's and teenage age up to 18 years;

- pregnancy and period of a lactation.

Overdose:

Taking into account a route of administration and at observance of the mode of a dosage the overdose by gel is a little probable. The probability of development of overdose increases when using drug in high doses or when drawing on the big area of integuments.

Symptoms: dizziness, a headache, myoclonic spasms at children, anorexia, nausea, vomiting, pains and unpleasant feelings in epigastric area, bleedings from digestive tract.

Treatment: to remove or wash away the remained gel from the damaged site of skin or a joint. If necessary to carry out symptomatic therapy. The artificial diuresis and a hemodialysis are ineffective. There is no specific antidote.

Storage conditions:

To store in the dry, protected from light place, at a temperature not over 25 ºС.

To store in the place, unavailable to children!

Issue conditions:

Without recipe

Packaging:

On 30 g in tubas aluminum for medical ointments from bushona with an internal covering it is delicious.

On one tuba together with the instruction on a medical use in the state and Russian languages place in a pack from a cardboard.