Pharmacological properties

Pharmacodynamics. diklosafe/diklosafe forte with active ingredient diclofenac is npvp for external use.

Diclofenac — NPVP which renders the antirheumatic, anesthetizing, anti-inflammatory and febrifugal action expressed. The main mechanism of action is suppression of biosynthesis of prostaglandins.

At the inflammation caused by injuries or rheumatic diseases, gel with diclofenac leads to reduction of severity of pain, hypostasis of fabrics and reductions of the period of updating of functions of the injured joints, ligaments, sinews and muscles. By clinical data it is proved that gel with diclofenac reduces an acute pain already in 1 h after initial drawing. Drug reduces an oxycinesia by 75% within two days. 94% of patients had affirmative answer on gel with diclofenac in 2 days of treatment in comparison with 8% of the patients who had affirmative answer on placebo. Overcoming pain and functional violations was reached after 4 days of treatment by gel with diclofenac. Thanks to an aqueous-alcoholic basis, medicine renders also mestnoanesteziruyushchy and cooling effect.

Pharmacokinetics. The amount of diclofenac which is soaked up through skin in proportion to the area of its drawing and depends both on the general dose of medicine, and on extent of hydration of skin. After local drawing 2.5 g of gel with diclofenac on the surface of skin of 500 cm ² extent of absorption of diclofenac makes about 6%. Use of an occlusive bandage during 10 h leads to increase in absorption of diclofenac three times.

After putting gel on diclofenac in blood plasma (where its C _max is about 100 times lower, than after oral administration of the same amount of diclofenac), in a synovial membrane and synovial fluid. Linking of diclofenac with proteins makes 99.7%.

Diclofenac collects in skin which serves as a vessel from where there is a gradual release of substance in nearby fabrics. From there diclofenac mainly comes to deeper inflamed fabrics, such as joints where continues to work and is defined in concentration up to 20 times higher, than in blood plasma.

by hydroxylation with formation of several phenolic derivatives, two of which are pharmacological active, but in much smaller degree, than diclofenac.

mainly with urine. The general system clearance of diclofenac is 263±56 ml/min., and final T _½ — on average 1–3 h

In a renal or liver failure the metabolism and removal from an organism of diclofenac do not change.

Indication

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

Diklosafe forte. Treatment of pain, inflammation and hypostasis at:

• damage of soft tissues: injuries of sinews, ligaments, muscles and joints (for example owing to dislocation, stretching, bruises) and dorsodynias (sports injuries);
• localized forms of rheumatism of soft tissues: tendinitis (including "tennis elbow"), bursitis, humeral syndrome and periartropatiya.

Symptomatic treatment of an osteoarthritis of the small and average joints located superficially such as joints of fingers or knee joints.

Use

Diklosafe

Adults and children are aged more senior than 14 years: it is necessary to apply Diklosafe gel 3–4 times a day, slightly rubbing in skin. The amount of medicament which is used depends on the size of the struck zone (so, 2–4 g, by the size corresponding to 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.

Patients of advanced age: medicine dose adjustment is not required.

If to apply the Diklosafe's gel on big parts of the body, system absorption of diclofenac will be more and the risk of emergence of side reactions, especially will increase if therapy is performed often.

forte

Adults and children are aged more senior than 14 years: to apply Diklosafe Forte gel 2 times a day (in the morning and in the evening), slightly rubbing in skin in the place of localization of pain. The amount of the used medicament depends on the size of the struck zone (so, 2–4 g, by the size corresponding to cherry or walnut, are enough for drawing on the site of 400-800 cm ² ).

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

If to apply the Diklosafe's gel forte on big parts of the body, system absorption of diclofenac will be more and the risk of emergence of side reactions, especially will increase if therapy is performed often.

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

more than 14 days in a row at damages or rheumatism of soft tissues longer than 21 days at a joint pain at arthritises if other is not recommended the doctor.

needs to see behind consultation a doctor if the expressiveness of symptoms of a disease does not decrease or manifestations amplify after 7 days of treatment.

Children. As there are no sufficient data on efficiency and safety of gel with diclofenac for children aged up to 14 years, medicine is contraindicated to children of this age group (see CONTRAINDICATIONS). 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.

Contraindication

• hypersensitivity to diclofenac or other components of medicine;
• existence in the anamnesis of attacks OH, a small tortoiseshell or the sharp rhinitis caused by intake of acetylsalicylic acid or other NPVP;
• last trimester of pregnancy;
• children's age up to 14 years.

forte

• hypersensitivity to diclofenac, acetylsalicylic acid, other NPVP or other components of medicine;
• existence in the anamnesis of attacks OH, a small tortoiseshell or the sharp rhinitis caused by intake of acetylsalicylic acid or other NPVP;
• combined application with other medicines containing diclofenac;
• combined application with other NPVP;
• last trimester of pregnancy.

Gel with diclofenac is usually well transferred by

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

Infection and invasion: pustulous rashes.

from the immune system: hypersensitivity reactions (including small tortoiseshell), Quincke's disease.

from the respiratory system, bodies of a thorax and mediastinum: OH.

from skin and hypodermic cellulose: rash, itch, eczema, erythema, dermatitis, including contact dermatitis, bullous dermatitis, reactions of photosensitivity, skin burning.

At topical administration of diclofenac cannot exclude possibility of side reaction which are usually connected with its system application * (see. Special INSTRUCTIONS).

in case of side reactions should stop treatment and to see a doctor.

* Information on the side reactions connected with system use of diclofenac contains in the relevant sources.

Special instructions

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.

With care should use medicament along with oral NPVP as the frequency of undesirable, especially system, side effects can increase (see INTERACTIONS).

Diklosafe/Diklosafe Gel forte should not be applied along with other medicines containing diclofenac.

only on the intact, intact sites of skin, avoiding hit on the inflamed, wounded or infected skin. It is necessary to avoid contact of medicine with a mucous membrane of eyes and other mucous membranes. It is impossible to swallow of drug.

At appearance of any skin rashes medicament treatment should be stopped.

Diklosafe/Diklosafe Gel forte should not be applied under an air-tight occlusive bandage, but its application under not occlusive bandage is allowed. In case of sprain the affected area can be tied up bandage.

At topical administration of diclofenac some probability of gastrointestinal bleeding at those patients who transferred it in the past exists.

Diklosafe/Diklosafe Gel forte contains propylene glycol and butyl hydroxytoluene. Propylene glycol can cause irritation of skin. Butyl hydroxytoluene can cause local skin reactions (for example contact dermatitis) or irritation of a mucous membrane of an eye and other mucous membranes.

Use during pregnancy and feeding by a breast. Pregnancy. After topical administration of diclofenac its system concentration is lower in comparison with reception of oral forms. Considering experience of therapy by system NPVP, it is recommended to take the following into account.

Inhibition of synthesis of prostaglandins can negatively affect a course of pregnancy and/or development of an embryo/fruit. Data of epidemiological researches confirm the increased risk of an abortion and/or risk of development of warm defects and a gastroshizisa after use of inhibitor of synthesis of prostaglandins in the early stages of pregnancy. The absolute risk of cardiovascular defects was increased with less than 1 to 1.5%. It is considered that the risk increases with a dose and duration of treatment. It is shown that at animals the introduction of inhibitor of synthesis of prostaglandins leads to increase before - and post-implantation loss and lethality of an embryo/fruit.

Besides, at the animals receiving inhibitor of synthesis of prostaglandins in the period of an organogenesis registered the increased frequency of various malformations, including from a cardiovascular system. During I and II trimester of pregnancy it is not necessary to apply diclofenac if it is not necessary. If diclofenac is applied by the woman planning pregnancy or if medicament is used during I or II trimester of pregnancy the dose of medicine has to be as low as possible, and treatment duration — is as little as possible.

In the III trimester of pregnancy all inhibitors of synthesis of prostaglandins can influence a fruit as follows:

• cardiopulmonary toxicity (with premature closing of an arterial channel and pulmonary hypertensia);
• violation of functions of kidneys which can progress to a renal failure with oligogidramniony.

Use of inhibitors of synthesis of prostaglandins at the end of pregnancy can influence mother and the newborn as follows:

• possible lengthening of a bleeding time, antiagregantny effect which can be observed even at very low doses;
• slowing down of reductions of a uterus that leads to a delay or lengthening of childbirth.

So, diclofenac is contraindicated during the III trimester of pregnancy (see CONTRAINDICATIONS).

Feeding by a breast. As well as other NPVP, diclofenac in insignificant quantity gets into breast milk. However at application in therapeutic doses of Diklosafe/Diklosafe gel forte no influence on breastfeeding is expected. Due to the lack of controlled researches at the women nursing Diklosafe/Diklosafe gel forte during this period should be applied only on doctor's orders. During feeding by a breast medicine should not be applied on mammary glands or big sites of skin and not to apply for a long time (see. Special INSTRUCTIONS and USE).

Fertility. Data on influence of diclofenac on fertility of the person at his external use are absent.

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, the probability of emergence of interactions insignificant. for today there are no data on interaction of diclofenac in case of its topical administration. information on the known interactions of oral forms of diclofenac contains in the relevant sources.

Overdose

Symptoms. the overdose is improbable in connection with low absorption of diclofenac in a system blood-groove at topical administration. at the same time development of system side reactions can be observed in case of accidental ingestion of gel diklosafe/diklosafe forte (it is necessary to consider that 1 tuba of medicine on 30 g contains an equivalent of 0.3 g of diclofenac of sodium). at accidental ingestion of medicine and emergence of considerable system side reactions it is necessary to apply the general therapeutic actions which are used at treatment of poisoning npvp. gastric lavage and intake of activated carbon, especially is recommended when the ingestion of medicine took place recently.

Treatment. Treatment of overdose of NPVP consists in application of the supporting and symptomatic therapy. There is no typical clinical picture caused by overdose of gel with diclofenac. The supporting and symptomatic treatment is shown at such complications as arterial hypotension, a renal failure, spasms, violations from a GIT and respiratory depression. It is improbable that an artificial diuresis, the hemodialysis or hemoperfusion are useful to removal of NPVP as active agents of these medicines substantially contact proteins of blood plasma and are exposed to intensive metabolism.

Storage conditions

At a temperature not above 25 °C.