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, and chilblains.
Pharmacological Classification:
- Nonsteroidal anti-inflammatory drug (NSAID)
- Analgesic (pain reliever)
- Counterirritant
- Emollient
Mechanism of Action:
Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing the production of prostaglandins, which are key mediators of pain and inflammation. Menthol and methyl salicylate act as counterirritants, producing cooling and warming sensations, respectively, that distract from pain. Oleum lini (linseed oil) provides emollient properties and may contribute to reducing inflammation.
Alternate Names
Diclofenac Diethylamine + Linseed Oil + Methyl Salicylate + Menthol Gel; KRISHAT RELIEF GEL (in some regions). Several brand names exist depending on the manufacturer and region.
How It Works
Pharmacodynamics:
Diclofenac inhibits COX-1 and COX-2 enzymes, reducing prostaglandin synthesis. Menthol and methyl salicylate act as counterirritants, stimulating peripheral nerve endings to produce cooling and warming sensations that mask pain signals. Oleum lini provides emollient and moisturizing effects to the skin.
Pharmacokinetics:
Topical application results in minimal systemic absorption. Diclofenac that is absorbed is primarily metabolized in the liver via conjugation and oxidation and excreted by the kidneys. Small amounts are also eliminated through the bile.
Mode of Action:
Diclofenac’s primary mechanism involves the non-selective inhibition of COX enzymes. Methyl salicylate, after skin absorption, is hydrolyzed to salicylic acid which also inhibits COX enzymes and exerts anti-inflammatory effects. Menthol and Methyl Salicylate activate TRPM8 receptors, causing a cooling sensation. Oleum Lini or linseed oil, rich in alpha-linolenic acid, softens the skin and possibly inhibits inflammatory mediators.
Dosage
Standard Dosage
Adults:
Apply an approximately one-inch band (around 3cm) of gel to the affected area three to four times daily, rubbing gently until the gel disappears. Do not apply more than 32 grams per day over all affected joints. For single joints in the upper body do not exceed 8 grams per day and for single joints of the lower body do not exceed 16 grams per day. The quantity may vary based on the size of the affected area.
Children:
This combination product is typically not recommended for children under 12 years of age. Consult a pediatrician for guidance if considering use in younger patients.
Special Cases:
- Elderly Patients: No specific dosage adjustments are typically required, but close monitoring for adverse effects is essential.
- Patients with Renal Impairment: Caution is advised; systemic absorption is minimal, but monitoring is recommended.
- Patients with Hepatic Dysfunction: Caution is advised. Systemic absorption is minimal, but monitoring is recommended.
- Patients with Comorbid Conditions: Evaluate on a case-by-case basis, considering potential drug interactions.
Clinical Use Cases
This topical medication is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, ICU, or emergency situations. It is primarily intended for outpatient musculoskeletal pain management.
Dosage Adjustments
Dose modifications may be needed for patients with renal or hepatic impairment, though systemic absorption is minimal. Always consider individual patient factors and potential drug interactions when determining the appropriate dosage.
Side Effects
Common Side Effects:
- Application site reactions (itching, irritation, redness, burning sensation)
- Dry skin
Rare but Serious Side Effects:
- Allergic reactions (rash, hives, difficulty breathing, swelling of the face, lips, tongue, or throat)
- Severe skin reactions (Stevens-Johnson syndrome)
Long-Term Effects:
With topical application, long-term systemic side effects are rare due to limited absorption. However, prolonged use may increase the risk of local skin reactions.
Adverse Drug Reactions (ADR):
Serious skin reactions or allergic reactions require immediate medical attention.
Contraindications
- Hypersensitivity to any component of the gel
- History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs, especially aspirin-sensitive asthma.
- Third trimester of pregnancy
Drug Interactions
Clinically significant interactions with topical application are rare due to limited systemic absorption. However, concomitant use of oral NSAIDs may increase the risk of systemic side effects. Caution should be exercised with:
- Oral NSAIDs (e.g., ibuprofen, naproxen)
- Anticoagulants/antiplatelet medications (e.g., warfarin, heparin)
- Immunosuppressants (e.g., cyclosporine)
- Topical salicylates may potentiate the anticoagulant effect of warfarin.
- Menthol (when taken orally) might reduce warfarin’s effectiveness.
Pregnancy and Breastfeeding
Use during pregnancy and breastfeeding should be under the guidance of a physician. While systemic absorption is minimal, the benefits should outweigh the potential risks to the fetus or neonate. Avoid use during the third trimester of pregnancy. It is not known whether this drug is excreted in human milk.
Drug Profile Summary
- Mechanism of Action: Diclofenac: COX inhibitor; Menthol/Methyl Salicylate: Counterirritants; Oleum Lini: Emollient.
- Side Effects: Local irritation, redness, itching. Rarely: allergic reaction, serious skin reactions.
- Contraindications: Hypersensitivity to ingredients, history of aspirin/NSAID sensitivity, third trimester of pregnancy.
- Drug Interactions: Minimal with topical use; caution with oral NSAIDs and anticoagulants.
- Pregnancy & Breastfeeding: Use with caution under physician guidance. Avoid use during the third trimester of pregnancy.
- Dosage: Apply 3-4 times daily to the affected area. Do not exceed maximum daily limits.
- Monitoring Parameters: Observe for local skin reactions and any signs of allergic reaction.
Popular Combinations
This is already a combination product and it is not generally combined with other topical agents.
Precautions
- General Precautions: Screen for allergies, relevant medical history (heart, liver, or kidney conditions), and current medications.
- Specific Populations:
- Pregnant Women: Consult physician; avoid use in the third trimester.
- Breastfeeding Mothers: Consult physician.
- Children & Elderly: Use with caution in children under 12 and elderly patients, monitoring for adverse effects.
- Lifestyle Considerations: Avoid activities requiring alertness until effects are known. Avoid exposure to direct sunlight or solariums during treatment.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Menthol + Methyl Salicylate + Oleum Lini?
A: Adults: Apply approximately 1 inch (3 cm) of gel to the affected area 3-4 times daily. Do not exceed 32 g/day total, 8 g/day per upper extremity joint, or 16 g/day per lower extremity joint. Not generally recommended for children under 12.
Q2: Can this gel be used during pregnancy?
A: Consult a physician before use during pregnancy. Avoid use during the third trimester.
Q3: Are there any drug interactions I should be aware of?
A: While systemic absorption is low, inform your doctor about all medications you are taking, especially oral NSAIDs, anticoagulants, and immunosuppressants.
Q4: What should I do if I experience side effects?
A: Mild skin reactions are common. If you experience any severe or persistent side effects, such as allergic reactions or severe skin irritation, discontinue use and consult your doctor immediately.
Q5: Can I use a heating pad on the treated area?
A: No, avoid applying heat to the treated area.
Q6: How does this gel actually reduce pain?
A: Diclofenac works by reducing inflammation, while menthol and methyl salicylate provide counterirritant effects that create competing sensations to distract from pain.
Q7: Can this gel be used on open wounds?
A: No, do not apply the gel to open wounds, broken skin, or areas with infections or rashes.
Q8: What if I miss a dose?
A: Apply the missed dose as soon as you remember, unless it is close to your next scheduled dose. Do not apply extra to make up for missed doses.
Q9: Is this a steroid cream?
A: No, this is an NSAID-based topical analgesic with counterirritant and emollient properties. It does not contain steroids.
Q10: Can I use this gel with other topical pain relievers?
A: Consult with your physician before using this gel with other topical medications, especially other pain relievers.
