Usage
This topical medication is prescribed for the relief of pain and inflammation associated with musculoskeletal conditions such as:
- Sprains
- Strains
- Bruises
- Soft tissue rheumatism
- Arthritis
- Backaches
- Fibrositis
- Lumbago
- Sciatica
- Stiff neck
- Tennis elbow
- Rheumatic pain
- Chilblains
Pharmacological Classification:
- Nonsteroidal anti-inflammatory drug (NSAID)
- Analgesic (pain reliever)
- Counterirritant
Alternate Names
While the combination itself doesn’t have a specific international nonproprietary name (INN), the individual components do: Diclofenac diethylamine, Menthol, Methyl salicylate, and Oleum lini (linseed oil).
Brand Names:
Brand names vary regionally. Some examples include:
- KRISHAT RELIEF GEL
- FIXACHE GEL
- Muscoleve
- Relaxo Gel
- Diclogesic Gel
- Lini-Gel
- Dfo 4x Gel
- Diclofen Gel
How It Works
Pharmacodynamics:
Diclofenac diethylamine, a non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase (COX) enzymes, primarily COX-2. This action reduces the production of prostaglandins, which are key mediators of pain and inflammation. Menthol acts as a counterirritant, producing a cooling sensation that can override pain signals. Methyl salicylate, also a counterirritant, produces a warming sensation by dilating blood vessels. Oleum lini (linseed oil), rich in omega-3 and omega-6 fatty acids, has emollient and anti-inflammatory properties, improving diclofenac penetration.
Pharmacokinetics:
Topical application results in limited systemic absorption of diclofenac. Methyl salicylate and menthol are absorbed through the skin to a greater extent. Diclofenac is metabolized primarily in the liver. Approximately 60% of the administered diclofenac dose is eliminated in the urine as metabolites, and the remainder is excreted in bile and feces. Menthol and methyl salicylate are also metabolized in the liver and excreted via the kidneys.
Dosage
Standard Dosage
Adults:
Apply a 2-4 g (approximately a 2.0-2.5 cm diameter circle or a 4-8 cm strand, equivalent to approximately 1 inch of gel) to the affected area 3-4 times daily. Gently rub into the skin until the gel disappears.
Children:
This combination product is typically not recommended for children under 14 years of age. Consult a pediatrician before use in children. Some sources specifically contraindicate the use in children under 14 years of age.
Special Cases:
- Elderly Patients: Use with caution. Closely monitor for adverse effects.
- Patients with Renal Impairment: Use with caution. Although systemic absorption is minimal, monitoring is recommended. Some sources contraindicate usage.
- Patients with Hepatic Dysfunction: Use with caution as liver metabolism is the primary route of elimination for diclofenac, menthol, and methyl salicylate. Monitor for adverse effects.
- Patients with Comorbid Conditions: Evaluate on a case-by-case basis, considering potential drug interactions and existing medical conditions, such as cardiovascular disease, recent heart surgery, stomach ulcers, or bleeding problems.
Clinical Use Cases
This topical medication is not typically indicated for clinical use cases such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. It is primarily intended for localized musculoskeletal pain and inflammation.
Dosage Adjustments
Adjustments may be needed based on individual patient response and tolerance. Consult a physician if symptoms continue for more than 7 days or worsen.
Side Effects
Common Side Effects
- Redness at the application site
- Mild itching or irritation
- Burning or warming sensation
- Dry skin
- Rash or hives
Rare but Serious Side Effects
- Allergic reactions
- Increased cardiovascular risk (heart attack, stroke) - primarily with prolonged use or at higher doses than recommended.
Long-Term Effects
With prolonged use, increased risk of cardiovascular events and gastrointestinal complications can occur, particularly if large amounts are used over a wide area of skin.
Adverse Drug Reactions (ADR)
Severe skin reactions such as blistering, peeling, or swelling require immediate discontinuation and medical assessment. Any signs of allergic reaction like difficulty breathing or hives warrant immediate medical attention.
Contraindications
- Hypersensitivity to any component of the formulation.
- History of asthma, urticaria, or acute rhinitis precipitated by aspirin or other NSAIDs.
- Third trimester of pregnancy.
- Open wounds or damaged skin.
Drug Interactions
- Oral NSAIDs: Increased risk of systemic side effects.
- Anticoagulants (e.g., warfarin): Methyl salicylate may potentiate effects.
- Immunosuppressants (e.g., cyclosporine): Increased risk of renal toxicity.
- Methotrexate: Increased risk of methotrexate toxicity.
- ACE inhibitors or ARBs: Interactions with diclofenac leading to decreased antihypertensive effect and increased risk of renal impairment, particularly with prolonged topical use over large areas.
Pregnancy and Breastfeeding
Use during pregnancy (especially the third trimester) should be avoided unless clearly needed. Limited systemic absorption occurs, but safety has not been conclusively established. Consult a doctor before using during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Diclofenac inhibits COX enzymes, reducing inflammation and pain. Methyl salicylate and menthol act as counterirritants and analgesics. Linseed oil enhances absorption and adds emolliency.
- Side Effects: Local skin reactions (itching, redness, burning). Rare: allergic reactions, increased cardiovascular risk.
- Contraindications: Hypersensitivity, aspirin/NSAID-induced asthma/urticaria/rhinitis, third trimester of pregnancy, open wounds.
- Drug Interactions: Oral NSAIDs, anticoagulants, immunosuppressants, methotrexate, ACE inhibitors, ARBs.
- Pregnancy & Breastfeeding: Avoid unless benefits outweigh risks. Consult a doctor before use.
- Dosage: Adults/adolescents (over 14): 2-4 g applied 3-4 times daily. Children (under 14): Not generally recommended/contraindicated.
- Monitoring Parameters: Local skin reactions, systemic side effects (especially with prolonged use).
Popular Combinations
While this is already a combination product, it may be prescribed alongside oral analgesics if pain is severe. However, concomitant use with oral NSAIDs should be avoided due to increased risk of side effects.
Precautions
- Apply only to intact skin.
- Avoid contact with eyes, mucous membranes, and open wounds.
- Wash hands thoroughly after application (unless hands are the treated area).
- Do not use with occlusive dressings.
- Monitor for allergic reactions.
- Use cautiously in patients with asthma or aspirin sensitivity.
- Avoid prolonged sun exposure as the medication might increase photosensitivity.
- Discontinue use if severe skin irritation occurs.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac diethylamine + Menthol + Methyl Salicylate + Oleum Lini?
A: Adults and adolescents (over 14 years): 2-4 g applied 3-4 times daily. Children (under 14 years): Not recommended.
Q2: Can this gel be used on open wounds?
A: No, it should only be applied to intact skin. Avoid contact with open wounds, cuts or damaged skin.
Q3: Can I use this gel if I am pregnant or breastfeeding?
A: Consult a doctor before using if pregnant or breastfeeding. Use during the third trimester of pregnancy is contraindicated.
Q4: I have a history of asthma triggered by aspirin. Can I use this gel?
A: No, it is contraindicated in individuals with aspirin- or NSAID-induced asthma, urticaria, or rhinitis.
Q5: Can I use a heating pad after applying this gel?
A: No, avoid applying heat to the treated area.
Q6: I forgot to apply the gel. What should I do?
A: Apply it as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not apply extra to make up for a missed dose.
Q7: How long can I use this gel?
A: Do not use for more than 7 days without consulting a physician.
Q8: Can I use this gel with other pain relievers?
A: Consult a doctor before using this gel in combination with oral NSAIDs or other pain medications, particularly oral anticoagulants or immunosuppressants, as there might be interactions.
Q9: What should I do if I experience side effects?
A: If you experience mild skin irritation, discontinue use and consult a doctor. For severe reactions such as swelling or difficulty breathing, seek medical attention immediately.
Q10: Can I use this gel if I have kidney problems?
A: Consult your physician. Some sources indicate caution while some contraindicate the usage of this medication in individuals with renal impairment.
