Instructions Diclosafe emulsion gel for external use 1.16% tube 100 g
Composition
active ingredient: diclofenac diethylamine;
1 g of gel contains 11.6 mg of diclofenac diethylamine, equivalent to 10 mg of diclofenac sodium;
Excipients: propylene glycol, isopropyl alcohol, carbomer, diethylamine, cocoyl caprylocaprate, oleyl alcohol, polyethylene glycol cetostearyl ether, light mineral oil, butylhydroxytoluene (E 321), purified water.
Dosage form
Emulsion gel for external use.
Main physicochemical properties: white or almost white soft homogeneous gel.
Pharmacotherapeutic group
Topical agents for joint and muscle pain. Nonsteroidal anti-inflammatory drugs for topical use. Diclofenac. ATC code M02A A15.
Pharmacological properties
Pharmacodynamics.
Diclosafe® with the active ingredient diclofenac is a highly effective non-steroidal anti-inflammatory drug (NSAID) for external use.
Diclofenac is an NSAID that has a pronounced antirheumatic, analgesic, anti-inflammatory and antipyretic effect. The main mechanism of therapeutic action of diclofenac is the inhibition of prostaglandin biosynthesis by cyclooxygenase 2 (COX-2).
In case of inflammation and pain of traumatic or rheumatic origin, diclofenac gel reduces pain, tissue swelling and shortens the recovery period of damaged joints, ligaments, tendons and muscles. Clinical data have shown that diclofenac gel reduces acute pain within 1 hour of initial application. The drug reduces pain during movement by 75% within two days. 94% of patients had a positive response to diclofenac gel after 2 days of treatment compared to 8% of patients who had a positive response to placebo. Overcoming pain and functional disorders was achieved after 4 days of treatment with diclofenac gel. Due to the water-alcohol base, the drug also exhibits a local anesthetic and cooling effect.
Pharmacokinetics.
The amount of diclofenac absorbed through the skin is proportional to the area of application and depends on both the total dose of the drug applied and the degree of skin hydration. After topical application of 2.5 g of diclofenac gel to a skin surface area of 500 cm2, the degree of absorption of diclofenac is approximately 6%. The use of an occlusive dressing for 10 hours leads to a threefold increase in diclofenac absorption.
After application of diclofenac gel to the skin of the hand and knee joints, diclofenac is found in the blood plasma (where its maximum concentration is approximately 100 times lower than after oral administration), in the synovial membrane and synovial fluid. The binding of diclofenac to proteins is 99.7%.
Diclofenac accumulates in the skin, which serves as a reservoir from which the substance is gradually released into the surrounding tissues. From there, diclofenac mainly enters deeper inflamed tissues, such as joints, rather than into the blood plasma. There it continues to act and is detected in concentrations up to 20 times higher than in the blood plasma.
Diclofenac is metabolized mainly by single- or multi-step hydroxylation and subsequent glucuronidation or glucuronidation of the entire molecule.
Diclofenac and its metabolites are excreted mainly in the urine. The total systemic plasma clearance of diclofenac is 263 ± 56 ml/min, and the terminal plasma half-life is on average 1-2 hours. Four metabolites, including two active ones, have a short half-life (1-3 hours), and one has a slightly longer half-life, but is practically inactive.
In renal or hepatic insufficiency, the metabolism and excretion of diclofenac are not altered.
Indication
Local treatment of pain and inflammation of joints, muscles, ligaments and tendons of rheumatic or traumatic origin.
Contraindication
Hypersensitivity to diclofenac or to other components of the drug.
History of attacks of bronchial asthma, angioedema, urticaria or acute rhinitis caused by taking acetylsalicylic acid or other NSAIDs.
The last trimester of pregnancy.
Children under 14 years old.
Interaction with other medicinal products and other types of interactions
Since systemic absorption of diclofenac following topical administration is very low, the likelihood of interactions is very low. There are currently no data on interactions with diclofenac when applied topically. Information on known interactions with oral forms of diclofenac can be found in the relevant sources.
Application features
The drug should be used with caution simultaneously with oral NSAIDs.
The drug should be used with caution simultaneously with oral NSAIDs, as the frequency of undesirable, especially systemic, side effects may increase (see section "Interaction with other medicinal products and other types of interactions").
Like other drugs that inhibit prostaglandin synthetase, diclofenac and other NSAIDs may cause bronchospasm when used in patients with or a history of bronchial asthma.
Diclosafe® gel should be applied only to intact, undamaged skin, avoiding contact with inflamed, injured or infected skin. Avoid contact with eyes and mucous membranes. Do not swallow.
If any skin rashes appear, treatment with the drug should be discontinued.
Diclosafe® gel should not be used under an airtight occlusive dressing, but it can be used under a non-occlusive dressing.
With topical use of diclofenac, there is some possibility of gastrointestinal bleeding in those patients who have had it in the past.
Due to the possibility of photosensitivity, direct sunlight and visits to the solarium should be avoided during treatment and for 2 weeks after discontinuation of treatment.
The patient should be advised not to smoke or go near open flames as this can lead to serious burns. Fabrics (clothing, bedding, dressings) that have come into contact with the product can easily catch fire and pose a serious fire hazard. Washing clothing and bedding may reduce the build-up of the gel but will not remove it completely.
Excipients
Diclosafe® gel contains propylene glycol and butylhydroxytoluene. Propylene glycol may cause skin irritation. Butylhydroxytoluene may cause local skin reactions (e.g. contact dermatitis) or irritation of the eyes and mucous membranes.
Use during pregnancy or breastfeeding
Pregnancy.
Clinical experience with the use of Diclosafe® in pregnant women is limited.
After topical application of diclofenac, its systemic concentration is lower compared to oral administration. Based on experience with systemic NSAIDs, the following should be considered.
Inhibition of prostaglandin synthesis may adversely affect the course of pregnancy and/or embryo/foetal development. Epidemiological studies have shown an increased risk of miscarriage and/or cardiac malformations and gastroschisis following the use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk of cardiovascular malformations was increased from less than 1% to approximately 1.5%. The risk is thought to increase with dose and duration of treatment. In animals, administration of a prostaglandin synthesis inhibitor has been shown to result in increased pre- and post-implantation loss and embryo/foetal lethality.
In addition, an increased incidence of various malformations, including cardiovascular malformations, has been reported in animals treated with a prostaglandin synthesis inhibitor during organogenesis. Diclofenac should not be used during the first and second trimesters of pregnancy unless clearly necessary. If diclofenac is used by a woman attempting to conceive, or if the drug is used during the first or second trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may affect the fetus in the following ways:
cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);
renal dysfunction, which may progress to renal failure with oligohydramnios.
The use of prostaglandin synthesis inhibitors in late pregnancy may affect the mother and newborn in the following ways:
possible prolongation of bleeding time, antiplatelet effect, which can be observed even at very low doses;
inhibition of uterine contractions, leading to delayed or prolonged labor.
Therefore, diclofenac, like other NSAIDs, is contraindicated during the third trimester of pregnancy (see section "Contraindications").
Breastfeeding period.
Like other NSAIDs, diclofenac passes into breast milk in small amounts. However, when using therapeutic doses of Diclosafe® gel, no effect on breastfeeding is expected. Due to the lack of controlled studies in breastfeeding women, Diclosafe® gel should be used during this period only as prescribed by a doctor. During breastfeeding, the drug should not be applied to the mammary glands or large areas of skin and should not be used for a long time (see sections “Special instructions” and “Dosage and administration”).
Fertility.
There are no data on the effect of diclofenac on human fertility when applied topically.
Ability to influence reaction speed when driving vehicles or other mechanisms
The effect of diclofenac is absent when applied externally.
Method of administration and doses
The drug is intended for external use only.
Diclosafe® gel should be applied 3-4 times a day, gently rubbing into the skin at the site of pain. The amount of the drug used depends on the size of the affected area (for example, 2-4 g, which is the size of a cherry or walnut, is enough to cover an area of 400-800 cm2).
After applying the drug, hands should be washed, except when this is the area to be treated.
The duration of therapy depends on the nature of the disease and the effectiveness of the treatment.
The drug should not be used for longer than 14 consecutive days for soft tissue injuries or rheumatism and for longer than 21 days for joint pain of arthritic origin, unless otherwise recommended by a doctor.
You should seek medical advice if the symptoms of the disease do not improve or worsen after 7 days of treatment.
Elderly patients
You can use the usual adult doses of the drug.
If Diclosafe® gel is applied to large areas of the body, systemic absorption of diclofenac will be greater and the risk of adverse reactions will increase, especially if the drug is used frequently.
Children.
There is insufficient data on the efficacy and safety of Diclosafe® in children under 14 years of age (see section "Contraindications").
When using the medicine in children aged 14 years and over for longer than 7 days or if the symptoms of the disease worsen, it is necessary to seek medical advice.
Overdose
Symptoms
Overdose is unlikely due to the low absorption of diclofenac into the systemic bloodstream when applied topically. At the same time, the development of systemic adverse reactions may occur in case of accidental ingestion of Diclosafe® gel (it should be noted that 1 tube of the drug of 30 g contains the equivalent of 0.3 g of diclofenac sodium).
Treatment
In case of accidental ingestion and significant systemic adverse reactions, general therapeutic measures for the treatment of NSAID poisoning should be used. Gastric lavage and administration of activated charcoal are recommended, especially in cases where ingestion has occurred recently.
Treatment of NSAID overdose consists of supportive and symptomatic therapy. There is no typical clinical picture caused by an overdose of diclofenac gel. Supportive and symptomatic treatment is indicated for complications such as hypotension, renal failure, convulsions, gastrointestinal disorders and respiratory depression. Forced diuresis, hemodialysis or hemoperfusion are unlikely to be useful for the removal of NSAIDs, since the active substances of these drugs are highly bound to plasma proteins and undergo extensive metabolism.
Adverse reactions
The frequency category of adverse reactions is defined as follows: very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100); rare (≥ 1/10000, < 1/1000); very rare (< 1/10000); frequency unknown (cannot be estimated from the available data).
Infections and infestations: very rare – pustular eruptions.
On the part of the immune system: very rarely - hypersensitivity reactions (including urticaria), angioedema.
Respiratory, thoracic and mediastinal disorders: very rarely - bronchial asthma.
Skin and subcutaneous tissue disorders: common: rash, pruritus, eczema, erythema, dermatitis, including contact dermatitis; rare: bullous dermatitis; very rare: photosensitivity reactions; frequency unknown: desquamation, skin discoloration, burning sensation of the skin.
If adverse reactions occur, treatment should be discontinued and a doctor should be consulted.
Reporting of suspected adverse reactions
Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
30 g, 50 g or 100 g in a tube. 1 tube in a cardboard box.
Vacation category
Without a prescription.
Producer
Kusum Healthcare Pvt Ltd.
Location of the manufacturer and address of its place of business.
SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India/SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India.
Address
SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India/SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India.
