Instructions Diclosafe forte emulsion gel for external use 2.32% tube 50 g
Composition
active ingredient: diclofenac diethylamine;
1 g of gel contains 23.2 mg of diclofenac diethylamine, equivalent to 20 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.
Dicloceif Forte with the active ingredient diclofenac is a nonsteroidal 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 period of restoration of functions of damaged joints, ligaments, tendons, and muscles.
Clinical data have shown that in ankle sprains, diclofenac gel significantly reduced pain on movement compared to placebo within three days of treatment, including in a subgroup of patients with severe pain. In addition, treatment with this drug also significantly improved ankle function within three days of treatment.
Due to its water-alcohol base, diclofenac gel also has 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 (2 times a day) to a skin surface area of 400 cm2, the degree of systemic absorption of the drug, defined as the concentration of the active substance in the blood plasma, is equivalent to applying diclofenac diethylamine with a concentration of 1.16% 4 times a day.
The relative systemic bioavailability of diclofenac when using diclofenac gel on day 7 is 4.5% compared to 50 mg tablets (at the same dose of diclofenac sodium). Absorption is independent of the use of a moisture-permeable and vapor-permeable dressing.
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 of the same amount of diclofenac), in the synovial membrane and synovial fluid. The binding of diclofenac to proteins is 99.7%, mainly to albumin (99.4%).
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 and ligaments, where it continues to act and is detected in concentrations up to 20 times higher than in blood plasma.
Diclofenac is metabolized partly by glucuronidation and mainly by hydroxylation to form several phenolic derivatives, two of which are pharmacologically active, but to a much lesser extent than diclofenac.
Diclofenac and its metabolites are excreted mainly in the urine. The terminal half-life of diclofenac from blood plasma is on average 1-2 hours. Four metabolites, including two active ones, also have a short half-life of 1-3 hours. One of the metabolites - 3´-hydroxy-4´-methoxydiclofenac - has a longer half-life, but is almost inactive.
In renal failure, accumulation of diclofenac and its metabolites in the body is not observed. In chronic hepatitis or non-decompensated cirrhosis of the liver, the kinetics and metabolism of diclofenac are not changed.
Indication
Treatment of pain, inflammation and swelling in:
soft tissue injuries: injuries to tendons, ligaments, muscles and joints (e.g. due to dislocation, sprain, contusion) and back pain (sports injuries);
localized forms of soft tissue rheumatism: tendinitis (including "tennis elbow"), bursitis, shoulder syndrome and periarthropathy.
Symptomatic treatment of osteoarthritis of small and medium-sized superficial joints, such as finger joints or knee joints.
Contraindication
Hypersensitivity to diclofenac, acetylsalicylic acid, other NSAIDs or 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 the systemic absorption of diclofenac following topical administration is very low, the likelihood of interactions is very low. To date, there are no data on interactions of diclofenac following topical administration. However, the possible interactions known for oral forms of diclofenac should be taken into account. Concomitant use of Diclosafe Forte with other systemic NSAIDs and steroids may increase the incidence of side effects.
Application features
Use Diclosafe Forte with oral NSAIDs with caution.
The possibility of developing systemic side effects (which occur with topical application of systemic forms of diclofenac) should be considered when using the drug on larger areas of skin or for a longer period of time than recommended.
Diclosafe Forte gel is recommended to be applied only to intact, undamaged areas of the skin, preventing contact with damaged (wounded or infected) skin. Contact of the drug with eyes and mucous membranes should be avoided. The drug should not be swallowed.
If any skin rashes appear, treatment with the drug should be discontinued.
Diclosafe Forte gel should not be used under an airtight occlusive dressing, but it can be used under a non-occlusive dressing.
When diclofenac is used topically in patients with peptic ulcer (current or history), there is some possibility of gastrointestinal bleeding.
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.
Due to the possibility of photosensitivity, direct sunlight should be avoided.
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 Forte 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 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.
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 drug has no or negligible influence on the ability to drive and use machines.
Method of administration and doses
The drug is intended for external use only.
Adults and children aged 14 and over
Diclosafe Forte gel should be applied twice a day (morning and evening), 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 apply to an area of 400-800 cm2). The analgesic effect lasts up to 12 hours.
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
Do not require dose adjustment.
If Diclosafe Forte 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 efficacy and safety in children under 14 years of age (see 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 Forte gel (it should be noted that 1 tube of the drug of 30 g contains the equivalent of 0.6 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
Diclofenac gel is usually well tolerated. Side effects include mild, temporary skin reactions at the application site. In rare cases, allergic reactions may occur.
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
2 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.
