Pharmacological properties

Pharmacodynamics. diclofenac — npvp for external use of group of derivatives of phenylacetic acid. diclofenac has the significant local antirheumatic, analgeziruyushchy and anti-inflammatory properties caused by oppression of synthesis of prostaglandins — mediators of pain and inflammation.

At the inflammation caused by injuries or rheumatic diseases, medicine leads to reduction of severity of pain, hypostasis of fabrics and reduction of the period of restoration of functions of the injured joints, ligaments, sinews and muscles.

Pharmacokinetics. The amount of the diclofenac absorbed through skin in proportion to the area of its drawing also depends both on the general dose of medicine, and on extent of hydration of skin. Extent of absorption of diclofenac makes about 6% of a dose after topical administration of 2.5 g of gel of diclofenac on 500 cm ² skin which are defined in relation to the general kidney elimination in comparison with diclofenac tablets. Occlusion for 10 h leads to 3-fold increase in amount of diclofenac.

After topical administration of gel in hands and knee joints concentration of diclofenac can be measured by

in blood plasma, synovial fabric and synovial fluid. The C _max in diclofenac blood plasma after topical administration is about 100 times lower, than after reception of tablets. 99.7% of diclofenac contact proteins of blood plasma, mainly albumine (99.4%). Diclofenac collects in skin which serves as a vessel from which there is a gradual release of substance in nearby fabrics. From there diclofenac mainly comes to the deep inflamed fabrics, such as joints where continues to work and is defined in concentration up to 20 times higher, than in blood plasma.

Metabolism of diclofenac includes a partial glyukuronirovaniye of intact molecules, but mainly hydroxylation with formation of several phenolic metabolites. 2 of these phenolic metabolites are biologically active, but in much smaller degree, than diclofenac. The general system clearance of diclofenac is 263±56 ml/min. (average value ± SD). The t _½ makes 1–2 h 4 metabolites, including 2 active, also have short T _½ — 1–3 h. One metabolite, 3 '-hydroxies-4 '-metoksi-diclofenac, has longer T _½ from blood plasma, but is practically not active. Diclofenac and its metabolites are removed generally with urine.

Indication

Topical treatment of pain and inflammation of joints, muscles, ligaments and sinews of rheumatic or traumatic origin.

Use

At adults and children is aged more senior than 14 years диклак® lipogel apply 3–4 times a day. the amount of medicine which is used depends on the size of the struck zone (for example 2–4 g of gel which on volume are similar to the size of cherry or walnut, are enough for drawing on the site of 400-800 cm2). to apply gel with a thin layer and to rub slightly in skin. it is not necessary to put under an air-tight occlusive bandage.

After applique of medicine needs to wash up hands, except those cases when this site is subject to treatment.

Duration of therapy depends on indications and efficiency of treatment.

should not use Drug longer than 14 days in a row at damages or rheumatism of soft tissues and 21 days at a joint pain of artritny origin if it is not recommended by the doctor.

needs to address for consultation of the doctor if expressiveness of symptoms of a disease do not decrease or amplifies after 7 days of treatment.

Diklak ^® Gel are applied by 3–4 times a day, slightly rubbing in skin. The amount of medicine which is used depends on the size of the struck zone (for example 2–4 g of gel which on volume are similar to the size of cherry or walnut, are enough for drawing on the site of 400-800 cm ² ).

After applique of medicine needs to wash up hands, except those cases when this site is subject to treatment.

Duration of therapy depends on the nature of a disease and efficiency of treatment.

should not use Drug longer than 14 days in a row.

in case of use of medicine not on doctor's orders needs to address it for consultation if after 7 days of treatment the condition of the patient did not improve or worsened.

Patients of advanced age (65 years are more senior). There are no bases to consider that patients of advanced age need special selection of a dose or they can have side reactions other than other patients.

Patients with a renal failure. There are no bases to consider that patients with a renal failure need special selection of a dose.

Patients with a liver failure. There are no bases to consider that patients with a liver failure need special selection of a dose.

Contraindication

Hypersensitivity to diclofenac or others npvp, to isopropyl alcohol or other components of medicine. existence in the anamnesis of attacks oh, small tortoiseshells, sharp rhinitis, nasal polyps, the angioedema caused by use of acetylsalicylic acid or others npvp. infectious damages of skin, open wounds, eczema. not to apply on mucous membranes. iii pregnancy trimester.

Side effects

гель/диклак® lipogel are usually well transferred by

Diklak®. undesirable reactions include easy temporary reactions on skin in the site of application. in rare instances there can be allergic reactions.

Assessment of side reactions is given by

on the frequency of manifestations: very often (≥1/10), it is frequent (≥1/100, 1/10), infrequently (≥1/1000, 1/100), is rare (≥1/10,000, 1/1000), is very rare (1/10,000).

Infection and invasion: seldom — pustulous rashes.

from skin: infrequently — rash, an itch, reddening, eczema, a dieback, an erythema, burning, appearance of hypostases and vesicles, papules, pustules, peeling and xeroderma, dermatitis (including contact dermatitis); seldom — bullous dermatitis; very seldom — reactions of photosensitivity, generalized skin rashes, skin burning.

from the immune system: very seldom — hypersensitivity reactions (including a small tortoiseshell), a Quincke's disease of the person, short wind.

from a respiratory system: very seldom — OH.

from digestive system the side reactions arise very seldom after topical administration of the medicines containing diclofenac.

At use of gel in high doses or its drawing on big sites of skin cannot exclude possibility of system side reactions and also reactions of hypersensitivity in the form of an angioedema, dispnoe.

Special instructions

With care should use medicament with oral npvp.

Likelihood of development of system side effects at topical administration of diclofenac is insignificant

in comparison with application of its oral forms, but it is not excluded at use of medicine on rather big sites of skin for a long time.

Diklak ^® Gel / ® Lipogel is recommended to apply

to Diklak of ^{only on intact sites of skin, avoiding hit on the inflamed, wound surface or infected skin. It is necessary to avoid contact of medicine with a mucous membrane of eyes and other mucous membranes. Not to use medicament inside.}

At appearance of any skin rash medicament treatment should be stopped. Use of an air-tight occlusive bandage is not recommended, but use of medicine under not occlusive bandage is allowed. In case of sprain the affected area can be tied up bandage. Not to apply on open wounds or the infected skin and also on the sites of skin affected with eczema or on mucous membranes.

At the states which are followed by reddening or swelling of joints, an acute pain in the waist irradiating in the lower extremities and/or soprovozhdyushcheysya neurologic violations (feeling of numbness, pricking) should consult with the doctor.

Diklak ^® Gel contains isopropyl alcohol which can cause the slight localized irritation of skin.

Use during pregnancy and feeding by a breast. Clinical experience concerning use of medicine during pregnancy is limited therefore its application during pregnancy and feeding is not recommended by a breast. Drug is contraindicated in the III trimester of pregnancy in connection with a possibility of development of weakness of patrimonial activity and/or premature closing of an arterial channel. During the researches on animals the adverse effect of diclofenac on pregnancy or embryonic development, childbirth or post-natal development of the child is not revealed.

sodium Diclofenac in insignificant quantity gets into breast milk therefore in the presence of strong reasons for use of the medicine Diklak ^® Gel / to Diklak of ^® Lipogel during feeding by a breast when the expected advantage, according to the doctor, exceeds potential risk, it it is not necessary to apply on mammary glands or big sites of skin and it is not necessary to apply for a long time.

Fertility. There are no available data on influence of diclofenac at topical administration on fertility of the person.

Children. There are no recommendations concerning dosing and therapeutic indications for use of the medicine Diklak ^® Gel at children. Diklak ^® Lipogel do not apply at children aged up to 14 years. At use of medicine for children 14 years longer are aged more senior than 7 days or if symptoms of a disease amplify, it is necessary to see behind consultation a doctor.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Does not influence.

Interaction

As system absorption of diclofenac owing to topical administration of medicine very low, emergence of interactions is improbable.

Overdose

Overdose is improbable

in connection with low absorption of diclofenac in a system blood-groove at topical administration. in case of accidental ingestion it is necessary to consider that 1 tuba of medicine диклак® gel on 100 g contains an equivalent of 1 g of diclofenac of sodium, at the same time development of system side reactions is possible.

in case of accidental ingestion of medicine should empty a stomach at once and to apply adsorbent. Symptomatic treatment using the therapeutic actions which should be used at NPVP poisoning is shown.

Storage conditions

At a temperature not above 25 °C. to store out of children's reach.