DICLOTROY (Diclofenac Diethylamine Topical Solution 4.64% w/v) is clear, colourless to yellow coloured solution filled in 30 ml frosted cobalt blue moulded vial USP type-I and sealed with spray pump crimp on covered with pump ring and actuator.
Each pump strokes contains 0.1 ml which is equivalent to 4 mg of diclofenac sodium.
Composition: Diclofenac Diethylamine BP 4.64% w/v equivalent to Diclofenac Sodium BP 4.00% w/v, Absolute Alcohol BP in topical solution base 10.00% v/v.
Pharmacology: Pharmacodynamics: Diclofenac inhibits the cyclo-oxygenase (COX) enzyme, an early component of the arachidonic acid cascade, resulting in the reduced formation of prostaglandins, thromboxanes and prostacyclin. Diclofenac, the active component has anti-inflammatory, anti-nociceptive and antipyretic effects.
Pharmacokinetics: Absorption: A study was conducted in 18 healthy male volunteers to evaluate pharmacokinetic parameters. 5 ml DICLOTROY (200 mg of diclofenac) was applied over the back of volunteers. The maximum plasma concentration of diclofenac was 175.93 ± 89.49 ng/ml while time to reach maximum plasma concentration was 5.24 ± 2.59 hours. AUC0-t was found to be 1224.19 ± 445.69 hr.ng/ml while AUC0-inf was 1718.21 ± 740.58 hr.ng/ml.
Distribution: Diclofenac is more than 99% bound to human serum proteins, primarily to albumin. Diclofenac diffuses into and out of the synovial fluid.
Metabolism: The major diclofenac metabolite, 4'hydroxy-diclofenac, has very weak pharmacological action. The formation of 4'-hydroxy-diclofenac is primarily mediated by CPY2C9. Both diclofenac and its metabolites undergo glucuronidation or sulfation followed by biliary excretion. CYP3A4 is responsible for the formation of minor metabolites, 5-hydroxy and 3'-hydroxy-diclofenac.
Elimination: Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged diclofenac is excreted in the urine.
DICLOTROY is indicated for the symptomatic relief of mild to moderate pain and inflammation associated with: Low backache, sprain and strain; blunt trauma of the tendons, ligaments, muscles and joints.
DICLOTROY is for external use only and not to be administered orally. It should not be applied on any mucosa, open wound, cut or diseased skin.
Patients should be advised to ensure that the site of application is clean and dry before applying DICLOTROY. Before using DICLOTROY for the first time, prime the pump by spraying it into the air 2-3 times. On the affected area, 4 pump strokes (0.4 ml equivalent to 16 mg of diclofenac sodium) should be applied 4 times a day at regular intervals. Number of the pump strokes to be applied may be higher or lower depending on the area to be treated. The maximum single dose of 7 pump strokes and the maximum daily dose of 30 pump strokes (120 mg of diclofenac sodium) should not be exceeded. It should be sprayed from a distance of 6-8 inches from the site of application.
DICLOTROY is a non-aqueous solution, hence the spray pattern will not be like the spray pattern of aqueous solutions or aerosol sprays. The prime purpose of the spray system is to ensure accurate dosing with each metered dose spray, which delivers 0.1 ml of solution. After applying the required number of sprays, spread the solution gently with your fingertip. Patients should be instructed not to massage the treated area after application. Avoid wearing clothing over the Diclotroy treated area until the treated area is dry. It is recommended that lowest effective dose for shortest duration should be used.
The treatment may be discontinued when the symptoms (pain and/or swelling) have subsided.
Patients should be instructed to consult a doctor if the pain and/or swelling do not improve or if they get worse within 7 days. When it is required for more than 7 days patients should be advised to use it as per recommended by doctor.
Special Population: Pediatric Use: Use in pediatric population is not recommended as data related to safety and efficacy is not available.
Geriatric Use: No overall difference in effectiveness or safety is expected between elderly and younger patients, but greater sensitivity to the effect of NSAIDs in some older individuals cannot be ruled out. Because elderly patients are more likely to have decreased renal function, care should be taken when using DICLOTROY in the elderly and it may be useful to monitor renal function.
Symptoms: The low systemic availability of diclofenac from DICLOTROY makes overdose very unlikely. However, undesirable effects, similar to those observed following overdose of diclofenac tablets, can be expected if DICLOTROY is inadvertently ingested.
Treatment: In the event of accidental ingestion, resulting in significant systemic adverse effects, general therapeutic measures, normally adopted to treat poisoning with non-steroidal anti-inflammatory medicines should be used. Management of overdosage with NSAIDs essentially consists of supportive and symptomatic measures. Gastric decontamination and the use of activated charcoal should be considered. Supportive and symptomatic treatment should be given for complications such as hypotension, renal failure, convulsions, gastrointestinal irritation, and respiratory depression; specific therapies such as forced diuresis, dialysis or haemoperfusion are probably of no help in eliminating NSAIDs due to their high rate of protein binding and extensive metabolism.
Hypersensitivity to diclofenac, acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (NSAIDs).
Patient with asthma or in patient when attacks of asthma, urticaria or acute rhinitis are precipitated by acetylsalicylic acid or other NSAIDs.
Children and adolescents less than 14 years.
During the last trimester of pregnancy.
DICLOTROY should be applied only to intact, non-diseased skin and not to skin wounds or open injuries. It should not be allowed to come into contact with the eyes or mucous membranes, and should not be ingested.
DICLOTROY is not recommended for use with occlusive dressing.
Photosensitivity reactions have been reported with topical use of diclofenac. Patients should be warned against excessive exposure to sunlight in order to reduce the incidence of photosensitivity.
Discontinue the treatment if a skin rash develops after application.
DICLOTROY should be used cautiously with oral NSAIDs as the incidence of undesirable systemic effects may increase.
DICLOTROY should be used with caution in patients with a history of peptic ulcer, hepatic or renal insufficiency, bleeding diathesis or inflammatory bowel disease as isolated incidences of such cases with topical diclofenac have been reported.
Pregnancy: No data is available for use of DICLOTROY in pregnant women. Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/foetal development. Data from epidemiological studies suggest an increased risk of miscarriage, cardiac malformation and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation increased from less than 1% to approximately 1.5%. The risk increases with dose and duration of therapy. In animals, administration of a prostaglandin synthesis inhibitor has been found to increase pre- and post-implantation loss and embryo/foetal lethality. In addition, increased incidence of various malformations including cardiovascular have been reported in animals administered with prostaglandin synthesis inhibitor during organogenesis.
During the first and second trimester of pregnancy, DICLOTROY should not be given unless the benefit outweighs the risk. If DICLOTROY is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept low and duration of treatment as short as possible.
DICLOTROY is contraindicated during the third trimester of pregnancy.
Lactation: Like other NSAIDs, diclofenac passes into breast milk in small amounts. However, at therapeutic doses of DICLOTROY no effects on the suckling child are anticipated. Because of a lack of controlled studies in lactating women, the product should only be used during lactation under advice from a healthcare professional. Under this circumstance, DICLOTROY should not be applied on the breasts of nursing mothers, nor elsewhere on large areas of skin or for a prolonged period of time.
Adverse reactions are ranked under the heading of frequency, the most frequent first, using the following convention: very common: (>1/10); common (≥1/100, <1/10); uncommon (≥1/1,000, <1/100); rare (≥1/10,000, <1/1000); very rare (<1/10,000); not known: cannot be estimated from available data.
Immune system disorders: Very rare: Hypersensitivity (including urticaria), angioneurotic oedema.
Infections and infestations: Very rare: Rash pustular.
Respiratory, thoracic and mediastinal disorders: Very rare: Asthma.
Skin and subcutaneous tissue disorders: Common: Rash, eczema, erythema, dermatitis (including dermatitis contact), pruritus. Rare: Dermatitis bullous.
Although less likely with the topical administration, some side effects normally associated with systemically administered diclofenac may also occur.
When used as per recommended dosage, the systemic availability of diclofenac from DICLOTROY is very low as compared to oral formulation of diclofenac. Hence the risk of drug interactions with other oral medicinal products is reduced. Concurrent acetylsalicylic acid or other NSAIDs may result in an increased incidence of adverse reaction.
Store below 30°C.
Keep the bottle in upright position.
M02AA15 - diclofenac ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.
Diclotroy topical spray 4.64% w/v
30 mL x 1's
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