Gel for external application of a uniform, creamy, white to white with a yellowish tinge.
diclofenac diethylamine 2.32 g,
that corresponds to the content of diclofenac sodium 2 g
Excipients: carbomers * - 1.1-1.7 g, tsetostearomakrogol - 2 g, Coco kaprilokaprat - 2.5 g diethylamine * 0.89-1.37 g isopropanol - 17.5 g paraffin liquid - 2.5 g oleyl alcohol - 0.75 g, eucalyptus flavor - 0.1 g, propylene glycol - 5 g, BHT - 0.02 g purified water * - 64.22-65.32 Mr.
* When using different manufacturing equipment of different sizes and series (1000 kg and 2500 kg) quantity of carbomers, dietilenamina purified water and may be slightly adjusted within these figures.
The active ingredient diclofenac - a non-steroidal anti-inflammatory drug, has expressed analyeziruyuschimi, anti-inflammatory and antipyretic properties. Non-selectively inhibiting the COX-1 and type 2, violates the metabolism of arachidonic acid.
Voltaren® Emulgel® used to eliminate pain and inflammation in the joints, muscles and ligaments of traumatic or rheumatic origin, helping to reduce pain and swelling associated with inflammation, increasing joint mobility.
The amount of diclofenac absorbed through the skin, proportional to the surface area being treated and depends on the total dose of drug applied and the degree of skin hydration. After application to a skin surface area of 400 cm2 Voltaren® Emulgel® gel for topical application 2% (two per day application), the concentration of active substance in plasma corresponds to its concentration by using 1% diclofenac gel (4 in deposition day). On the 7th day, the relative bioavailability (AUC ratio) is 4.5% (for an equivalent dose of diclofenac sodium salt). When equipped with the liquid pervious dressings absorption did not change.
We measured the concentration of diclofenac in plasma, synovial membrane and synovial fluid when applying the drug to the area of the affected joint. Cmax in the plasma was about 100 times lower than after oral administration of the same amount of diclofenac. 99.7% diclofenac associated plasma proteins, mainly albumin (99.4%). Diclofenac advantageously distributed and retained in deep tissues prone to inflammation, such as joints, where its concentration is 20 times higher than in plasma.
diclofenac metabolism is achieved partly by glucuronidation unmodified molecule, but mainly by single and multiple hydroxylation which leads to the formation of several phenolic metabolites, most of which is converted to glucuronide conjugates. Two phenolic metabolites biologically active, but to a much lesser extent than diclofenac.
Total plasma clearance of diclofenac system is 263 ± 56 mL / min. The final T1 / 2 1-2 h. T1 / 2 metabolites, including the pharmacologically active 2, and also of short duration is 1-3 hours. One of the metabolites (3'-hydroxy-4'-metoksidiklofenak) has a longer T1 / 2 however, this metabolite is completely inactive. Most of diclofenac and its metabolites are excreted in the urine.
Adverse reactions are mainly characterized by moderately severe skin manifestations and passing the site of application of the gel. In very rare cases may develop allergic reactions.
Classification of the incidence of adverse reactions: very often - more appointments 1/10 (> 10%); often - more than 1/100 and less than 1/10 of appointments (> 1% but <10%); infrequently - 1/1000 more, but less than 1/100 of appointments (> 0.1% and <1%); rarely - more than 1/10000 and less than 1/1000 of appointments (> 0.01% and <0.1%); very rare - less than one ten thousandth of appointments (<0.01%).
Infectious and parasitic diseases: very rare - pustular rash.
Immune system: very rarely - a generalized skin rash, allergic reactions (urticaria, hypersensitivity: angioedema).
With the respiratory system and organs of thoracic and mediastinal disorders: very rare - asthma attacks, bronchospastic reactions.
For the skin: often - erythema, dermatitis, including contact dermatitis (symptoms: eczema, itching, swelling of the treated area of the skin, rash, papules, vesicles, scaling); rare - bullous dermatitis; very rarely - photosensitivity reactions.
Voltaren® Emulgel® should only be applied to intact skin, avoiding contact with open wounds. Do not allow contact with the drug in the mouth, eyes and mucous membranes. After application of the drug allowed the imposition of bandage, but it should not impose an airtight occlusive dressings. In the case of skin rash after application of the preparation of its use should be discontinued.
The product contains propylene glycol, which in some people can cause mild local irritation. It also contains BHT that can cause local skin reactions (eg contact dermatitis) or irritation of the eyes and mucous membranes.
Effects on ability to drive and use machines
Does not affect.
Due to the low systemic absorption when applied to the gel, overdose is unlikely. In case of accidental ingestion may develop systemic side effects. Treatment of overdose Accidental ingestion: gastric lavage, induction of vomiting, activated charcoal, symptomatic therapy. Dialysis and diuresis are not effective since diclofenac high binding to plasma proteins (about 99%).
- Back pain in inflammatory and degenerative diseases of the spine (sciatica, osteoarthritis, lumbago, sciatica);
- Pain in the joints (joints of the fingers, knees, etc.) In rheumatoid arthritis, osteoarthritis;
- Muscle pain (due to stretching, overvoltage, bruises, injuries);
- Inflammation and swelling of the soft tissues and joints due to injuries and rheumatic diseases (tendonitis, bursitis, defeat periarticular tissues, CTS).
- Hypersensitivity to diclofenac or other ingredients;
- The tendency to occurrence of asthma attacks, skin rashes or acute rhinitis when using aspirin or other NSAIDs;
- Pregnancy (III trimester)
- Children's age (12 years);
- Violation of the integrity of the skin in the proposed site of application.
Be wary of hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe liver and kidney function, blood clotting disorders (including hemophilia, prolongation of bleeding time, the propensity to bleeding), chronic heart failure, asthma bronhialnaoy, in old age, pregnancy (I and II trimester).
Pregnancy and breast-feeding
In the absence of data on the use of Voltaren® Emulgel® in pregnant women, the use of the drug during the I and II trimester of pregnancy is recommended only on prescription by comparing the benefits to the mother and the risk to the fetus. The drug is contraindicated in the III trimester of pregnancy due to the possibility of lowering the tone of the uterus and / or premature closure of the fetal blood flow.
In the absence of data on the penetration Voltaren® Emulgel® into breast milk drug is not recommended for use during breastfeeding. If it is necessary the use of the drug, it should not be applied to the breasts or to a large surface of skin and does not use long.