Diclofenac

General characteristics. Structure:

Active ingredient: 10 mg of diclofenac of sodium in the form of diethyl amine diclofenac in 1 g of gel.

Excipients: propylene glycol, a makrogolglitserin hydroxystearate, a macrogoal cetostearyl ether, cetostearyl alcohol, liquid paraffin, carbomer, isopropyl alcohol, a dimethyl sulfoxide, diethanol amide, a peppermint oil, the water purified.

The non-steroidal anti-inflammatory drug for topical administration having the antiinflammatory and anesthetizing effect.

Pharmacological properties:

Pharmacodynamics. Oppressing cyclooxygenase 1 and 2, breaks metabolism of arachidonic acid, reduces amount of prostaglandins in the inflammation center. Inhibits synthesis of proteoglycan in cartilages. Weakens or eliminates pains in a site of application, a joint pain at rest and at the movement, reduces morning constraint and a swelling of joints. Reduces posttraumatic and postoperative pains, and also inflammatory hypostasis. Promotes increase in volume of movements in the affected joints.

Thanks to an aqueous-alcoholic basis drug has also mestnoanesteziruyushchy and cooling effect.

Pharmacokinetics. Absorption. The amount of diclofenac which is soaked up through skin depends on time of contact of drug, the area of its drawing, extent of hydration of skin. Extent of absorption of diclofenac is insignificant and makes no more than 6% of the equivalent dosage of diclofenac accepted inside. Use of an occlusive bandage during 10 h leads to 3-fold increase in a resorption of diclofenac.

Distribution. The maximum concentration of diclofenac in plasma is about 100 times lower, than its concentration after peroral introduction in an equivalent dosage. Linkng of diclofenac with proteins (preferential albumine) makes about 99%.

Metabolism. Diclofenac biotransformation partially includes a glyukuronidation of not changed molecule, and also preferential single or repeated hydroxylation leading to formation of several phenolic metabolites, the majority of which turn into glucuronic conjugates. Two phenolic metabolites have pharmacological activity, but in much smaller degree, than diclofenac.

Removal. Diclofenac and its metabolites, generally in the form of glyukoronid, are removed preferential with urine. The general system plasma clearance of diclofenac averages 263 ml/min. (fluctuations from 207 ml/min. to 319 ml/min.). Final Т½ makes 1-2 h of plasma.

Pharmacokinetics in special clinical cases. Patients with diseases of kidneys have a cumulation of diclofenac and its metabolites it is not noted. At patients with chronic hepatitis or the compensated cirrhosis indicators of pharmacokinetics and metabolism of diclofenac do not change.

Indications to use:

For a topical symptomatic treatment of pain and an inflammation at:
- Injuries of sinews, sheaves, muscles and joints, for example, owing to sprain, retension and bruises;
- The localized forms of rheumatic diseases of soft tissues.

In 14 days of use of Diklofenak-emulgel, gel according to these indications it is necessary to reconsider its further appointment.

For treatment of an osteoarthritis of superficial joints, such, as knee.

In 4 weeks of use of medicine according to this indication it is necessary to reconsider its further appointment.

Route of administration and doses:

It is applied outwardly. To adults and children 14 years gel are more senior apply on skin of 3-4 times/days, slightly rub. The quantity of the applied means depends on the size of a painful zone. The single dose of medicine makes from 2 to 4 g that on volume also enough for processing of surface area of a body of 400-800 cm2 is comparable to the size of cherry or walnut.

After application of medicine of a hand it is necessary to wash up if they are not object of treatment (at arthroses of fingers of hands).

Duration of treatment depends on indications and efficiency of therapy. For strengthening of effect gel can be combined also with other dosage forms of diclofenac. Indications for continuation of treatment are recommended to be revised in 2 weeks.

Use at children's age. There are no sufficient data about efficiency and safety for children and teenagers 14 years are younger. At use of medicine for children 14 years more than 7 days are more senior or at deterioration in symptomatology it is recommended to see a doctor.

Features of use:

Medicine should be applied only on the unimpaired sites of skin, avoiding hit on open wounds. After putting gel it is not necessary to apply an occlusive bandage.

To avoid hit of gel in eyes and on mucous membranes.

When putting drug on extensive sites of skin and/or at its prolonged use it is impossible to exclude completely a possibility of manifestation of systemic side effects of diclofenac.

At long therapy by this medicine increase in activity of liver enzymes is possible.

At emergence of any side effects it is necessary to stop use of gel and to see a doctor.

It is necessary to consult with the doctor before use of gel at reception of other non-steroidal anti-inflammatory drugs.

Use in time pregnancy and feeding by a breast. In I and II pregnancy trimesters medicine is appointed as a last resort when the expected advantage for mother is higher, than potential risks for a fruit. In the III trimester use of gel is contraindicated as diclofenac well gets through a placental barrier and can cause disturbances in development of cardiovascular system in a fruit with the big term of a gestation. Medicine is not recommended to be applied in the period of a lactation.

Side effects:

Side reactions are ranged on frequency, using the following gradation: often (1/100 <1/10); infrequently (1/1,000 <1/100); seldom (1/10,000 <1/1,000); very seldom (<1/10,000), including separate messages.

Infections and invasions. Very seldom: pustular rash.

From immune system. Very exceptional cases: hypersensitivity, Quincke's disease.

From respiratory organs, a thorax and mediastinum. Very seldom: asthma.

From skin and hypodermic cellulose. Often: rash, eczema, erythema, dermatitis (including contact dermatitis). Seldom: violent dermatitis. Very exceptional cases: photosensitivity reactions (patients have to be warned about undesirability of excessive influence of sunshine for the purpose of decrease in probability of development of reactions of photosensitivity).

Interaction with other medicines:

So far it was not reported about any interaction of medicine with other medicines. Strengthening of effect of the medicines causing a photosensitization is possible.

Contraindications:

- hypersensitivity to diclofenac, acetylsalicylic acid and other non-steroidal anti-inflammatory drugs;
-  hypersensitivity to other components of a dosage form;
-  "aspirinovy" asthma;
-  disturbance of integrity of integuments;
-  lactation period;
-  pregnancy (III trimester)
-  children's age up to 14 years.

With care appoint: at a hepatic porphyria (aggravation), digestive tract erosive cankers, heavy abnormal liver functions and kidneys, chronic heart failure, bronchial asthma, advanced age, in I and in the II pregnancy trimesters.

Overdose:

The overdose is improbable since absorption of diclofenac in a system blood stream at topical administration is small.

Storage conditions:

To store at a temperature not above +25 °C. To store in the places unavailable to children. Period of validity 2 years.

Issue conditions:

Without recipe

Packaging:

Gel on 30,0 g, 40,0 g and 50,0 g in the tubas placed together with a leaf insert in packs from a cardboard.