Instructions Diclosafe forte emulsion gel for external use 2.32% tube 100 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
Diclosafe® Forte with the active ingredient diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) for external use.
Diclofenac is a nonsteroidal anti-inflammatory drug that has a pronounced antirheumatic, analgesic, anti-inflammatory and antipyretic effect. The main mechanism of action is the inhibition of prostaglandin biosynthesis.
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 applied dose of the drug and the degree of skin hydration. After topical application to a skin surface area of 400 cm2, the degree of systemic absorption of diclofenac gel, defined as the concentration of the active substance in the blood plasma, is equivalent to applying diclofenac at a concentration of 1.16% 4 times a day. The relative systemic bioavailability of diclofenac when using diclofenac gel on the 7th day is 4.5% compared to 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 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. 99.7% of diclofenac binds to plasma proteins, mainly 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, joints, where it continues to act and is detected in concentrations up to 20 times higher than in 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 total systemic plasma clearance of diclofenac is 263 ± 56 ml/min, and the terminal half-life is on average 1-2 hours. Four metabolites, including two active ones, also have short half-lives 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: tendonitis (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 to other components of the drug. History of attacks of bronchial asthma, urticaria or acute rhinitis caused by taking acetylsalicylic acid or other NSAIDs. Concomitant use with other drugs containing diclofenac. Concomitant use with other NSAIDs. Last trimester of pregnancy.
Interaction with other medicinal products and other types of interactions
Since systemic absorption of diclofenac following topical application is very low, the likelihood of interactions is very low. There are currently no data on interactions of diclofenac following topical application*. Concomitant use of Diclosafe® Forte with steroids may increase the incidence of side effects. Concomitant use of Diclosafe® Forte with other systemic NSAIDs is contraindicated (see section “Contraindications”).
*Information on known interactions associated with systemic use of diclofenac is contained in the relevant sources.
Application features
The likelihood of developing systemic side effects with topical application of diclofenac is insignificant compared to the use of its oral forms, but it cannot be ruled out when the drug is used on relatively large areas of skin for a long time.
Diclosafe® Forte gel is recommended to be applied only to intact, undamaged areas of the skin, avoiding contact with inflamed, injured 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 may be used under a non-occlusive dressing. In the case of a sprain, the affected area can be bandaged.
When diclofenac is used topically in patients with peptic ulcer disease (current or past), there is a slight 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.
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.
Ability to influence reaction speed when driving vehicles or other mechanisms
Does not affect.
Use during pregnancy or breastfeeding
Pregnancy.
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 is contraindicated during the third trimester of pregnancy (see section "Contraindications").
Breast-feeding.
Like other NSAIDs, diclofenac passes into breast milk in small amounts. However, when using therapeutic doses of Diclosafe® Forte gel, no effect on breastfeeding is expected. Due to the lack of controlled studies in breastfeeding women, Diclosafe® Forte 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 for use” and “Method of administration and dosage”).
Fertility.
There are no data on the effect of diclofenac on human fertility when applied topically.
Method of administration and doses
Adults and children over 14 years of age: 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 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 days 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.
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 therapy is used frequently.
Children
Since there is insufficient data on the efficacy and safety of diclofenac gel in children under 14 years of age, the drug is contraindicated for use in children under 14 years of age (see section "Contraindications"). When using the drug in children over 14 years of age for more than 7 days or if the symptoms of the disease worsen, a doctor should be consulted.
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 borne in mind that 1 tube of the drug of 30 g contains the equivalent of 0.6 g of diclofenac sodium). In case of accidental ingestion of the drug and the occurrence of significant systemic adverse reactions, general therapeutic measures used in the treatment of NSAID poisoning should be applied. Gastric lavage and administration of activated charcoal are recommended, especially in cases where the drug was ingested recently.
Treatment.
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. Adverse reactions include mild, transient skin reactions at the application site. In rare cases, allergic reactions may occur.
Infections and infestations: pustular eruptions.
Immune system disorders: hypersensitivity reactions (including urticaria), angioedema.
Respiratory, thoracic and mediastinal disorders: bronchial asthma.
Skin and subcutaneous tissue disorders: rash, itching, eczema, erythema, dermatitis, including contact dermatitis, bullous dermatitis, photosensitivity reactions, burning sensation of the skin.
When using diclofenac topically, the possibility of adverse reactions that are usually associated with its systemic use* cannot be excluded (see section "Special warnings and precautions for use").
If adverse reactions occur, treatment should be discontinued and a doctor should be consulted.
*Information on adverse reactions associated with systemic use of diclofenac is contained in the relevant sources.
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
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 its business address
SP-289 (A), RIICO Industrial area, Chopanki, Bhiwadi, Dist. Alwar (Rajasthan), India.
