Sodium diclofenac

General characteristics. Structure:

Active ingredient: 0,3 g of diclofenac of sodium in each tuba.

Excipients: dimethyl sulfoxide, propylene glycol, macrogoal 1500, macrogoal 400.

Pharmacological properties:

Pharmacodynamics. Renders antiinflammatory, antirheumatic, analgeziruyushchy and moderate febrifugal action. Eliminates a hyperthermia, pain, reduces hypostasis, an erythema in the place of use. At inflammatory damages of joints are promoted reduction of inflammatory hypostasis, a swelling and morning constraint, increase in volume of movements, simplification of pains when pressing by the Pharmacodynamics

The non-steroidal anti-inflammatory drug derivative of phenylacetic acid, has antiinflammatory and analgeziruyushchy effect. Not selectively oppressing cyclooxygenase 1 and cyclooxygenase 2, breaks metabolism of arachidonic acid, reduces amount of prostaglandins, including in the inflammation center.

Pharmacokinetics. Absorption. The amount of Diclofenac of sodium which is absorbed through skin in proportion to the size of the square on which apply medicine and depends both on the general applied dose, and on extent of hydration of skin. Extent of absorption makes about 6% of the applied dose after topical administration of 2,5 g of medicine on 500 cm2 of skin, defined taking into account full renal elimination, in comparison with Diclofenac tablets. 10-hour occlusion leads to triple increase in amount of the absorbed diclofenac.

Distribution. Concentration of Diclofenac of sodium were measured in plasma, synovial fabric and synovial fluid after local putting ointment on joints of hands and a knee. The maximum concentration in plasma is about 100 times lower, than concentration after peroral introduction of the same amount of Diclofenac of sodium. 99,7% of Diclofenac of sodium contact proteins of serum, are preferential with albumine (99,4%).

Metabolism. Sodium Diclofenac biotransformation partially includes a glyukuronidation of an invariable molecule, but preferential single or repeated hydroxylation leads to formation of several phenolic metabolites, the majority of which turn into glucuronic conjugates. Two phenolic metabolites are biologically active, but their activity is significantly lower than activity of Diclofenac of sodium.

Elimination. The general system clearance of Diclofenac of sodium makes of a blood plasma 263 ± 56 ml/min. Terminal plasma elimination half-life makes 1 - 2 h. Four of metabolites, including two active, also show short plasma elimination half-life which makes 1-3 h. One metabolite, 3-hydroxy - 4-метокси-diclofenac, shows longer elimination half-life, but actually is inactive. Diclofenac of sodium and its metabolites are removed preferential with urine.

Pharmacokinetics at separate groups of patients. Accumulation of Diclofenac of sodium and its metabolites at patients who have a renal failure is not supposed. At patients with chronic hepatitis or nedekompensirovanny cirrhosis kinetics and metabolism of Diclofenac of sodium same, as well as at patients who have no pecheni.a diseases the movement.

Indications to use:

Traumatic the caused inflammations of sinews, sheaves, muscles and joints (owing to stretchings, at loading and bruises).

The localized forms of rheumatism of soft tissues, such as syndrome "shoulder brush", a tendovaginitis, a bursitis, a periartropatiya.

The localized rheumatic diseases, for example, arthrosis of joints.

Route of administration and doses:

Outwardly, 2-4 g of ointment (that on volume also enough for processing of surface area of a body of 400-800 cm2 is comparable according to the size of cherry or walnut) put with a thin layer, slightly rubbing in skin over the inflammation center, 2-3 times a day. After putting ointment of a hand it is necessary to wash up if they are not area of treatment (at arthroses of fingers of hands). The maximum daily dose - 8 g.

Duration of treatment depends on indications and noted effect (ointment can be applied to strengthening of effect together with other dosage forms of diclofenac). It is necessary to consult with the doctor after 2 weeks of use of medicine.

Features of use:

Apply only on the unimpaired sites of skin. After imposing it is not necessary to apply an occlusive bandage.

At prolonged use and/or drawing on the extensive surfaces of skin the risk of development of system side effects increases, including increase in activity of liver enzymes can be observed. For minimization of possible risk of development of side reactions from a liver Diclofenac of sodium should be used in minimum effective dose during minimum short period.

It is necessary to avoid hit of ointment in eyes, on mucous membranes or open wounds. To apply only outwardly.

Use during pregnancy. There are no controlled clinical trials at pregnant women therefore Diclofenac of sodium should not will be applied during pregnancy. Use is especially dangerous in the III trimester of pregnancy because of possible early closing of a botallovy channel and probability of suppression of labor pains.

Use during breastfeeding. There are no data on penetration into breast milk of Diclofenac of the sodium applied locally. Therefore medicine should not be applied at the feeding women. At good reasons of appointment medicine should not be applied on area of a breast, they cannot process extensive sites of a surface and to use long time.

Side effects:

From integuments: eczema, a photosensitization, contact dermatitis (an itch, a hyperemia, puffiness of the processed site of skin, papular and vesicular rashes, a peeling).

Allergic reactions: (an itch and burning of skin, erythematic skin rash, a small tortoiseshell, a Quincke's disease, system anaphylactic reactions (including shock).

Interaction with other medicines:

Can strengthen effect of the medicines causing a photosensitization.

With care to use with other medicines possessing obviously known gepatoksichnost, for example, antibiotics, protiepileptichesky medicines.

Clinically significant interaction with other medicines is improbable, owing to insignificant system absorption.

Contraindications:

Hypersensitivity to Diclofenac of sodium or other components of medicine, acetylsalicylic acid or other NPVP, "aspirinovy" asthma, pregnancy (the III trimester), the lactation period, children's age (up to 12 years), disturbance of integrity of integuments.

With care. Hepatic porphyria (aggravation), digestive tract erosive cankers, heavy abnormal liver functions and kidneys, chronic heart failure, bronchial asthma, advanced age, pregnancy I and II trimesters.

Overdose:

In view of low system absorption at ointment application, the overdose is improbable.

Storage conditions:

At a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after the termination of a period of validity.

Issue conditions:

Without recipe

Packaging:

On 30 g in tubas in packaging No. 1.