Usage
This topical medication is prescribed for the relief of pain and inflammation associated with musculoskeletal and joint disorders such as:
- Sprains
- Strains
- Bruises
- Soft tissue rheumatism
- Arthritis
- Backache
- Fibrositis
- Lumbago
- Sciatica
- Stiff neck
- Tennis elbow
- Rheumatic pain
Pharmacological Classification:
- Non-steroidal anti-inflammatory drug (NSAID)
- Topical analgesic
- Counterirritant
Mechanism of Action: This combination product works through multiple pathways:
- Diclofenac diethylamine and Methyl salicylate: Inhibit cyclooxygenase (COX) enzymes, reducing prostaglandin production, which are responsible for pain and inflammation.
- Linseed oil: Softens and moisturizes the skin, facilitating the penetration of other ingredients. Also contains alpha-linolenic acid with anti-inflammatory properties.
- Menthol: Creates a cooling sensation by activating TRPM8 receptors, distracting from pain and improving blood flow through vasodilation.
- Methyl salicylate (wintergreen oil): Inhibits prostaglandin synthesis. Warms the skin.
Alternate Names
This combination does not have a universally recognized international non-proprietary name (INN). Names often reflect the specific combination and concentrations of ingredients.
Brand Names: Numerous brand names exist depending on the manufacturer and region. Examples include:
- Krishat Relief Gel
- Muscoleve
- Muscodac Gel
- Lofnac Gel
- Qtgesic Gel
- Diclotal+ Gel
- Diclotal-Forte Gel (with added Capsaicin)
How It Works
Pharmacodynamics:
- Diclofenac diethylamine and Methyl salicylate: Reduce pain and inflammation by inhibiting COX-1 and COX-2 enzymes, decreasing prostaglandin synthesis.
- Menthol: Activates TRPM8 receptors, causing a cooling sensation and vasodilation.
- Linseed oil: Emollient and moisturizing effects. Alpha-linolenic acid contributes to anti-inflammatory action.
Pharmacokinetics:
- Diclofenac diethylamine: After topical application, systemic absorption is low (around 100 times lower than oral administration). Diclofenac is metabolized primarily in the liver, with metabolites excreted in urine and bile/feces.
- Methyl salicylate: Absorbed through the skin, metabolized to salicylic acid, and excreted in urine. Absorption is enhanced by heat, exercise, or skin damage.
- Menthol and Linseed oil: Limited systemic absorption after topical use.
Mode of Action: The components of this combination act synergistically:
- COX inhibition: Diclofenac and methyl salicylate inhibit COX enzymes, decreasing prostaglandin synthesis, which reduces pain and inflammation.
- TRP channel modulation: Menthol activates TRPM8 (cold-sensitive) receptors, creating a cooling sensation, while capsaicin (in some formulations) activates TRPV1 (heat-sensitive) receptors, initially causing a burning sensation followed by desensitization.
- Enhanced penetration: Linseed oil facilitates the absorption of other active ingredients into the skin.
Elimination pathways: Primarily renal and hepatic.
Dosage
Standard Dosage
Adults and Children over 14 years:
- Apply a 2-4 g (approximately 4-8 cm strip or a circular mass of 2.0-2.5 cm diameter) to the affected area 3-4 times daily.
- Gently rub until absorbed.
- Wash hands after application, unless treating hands.
- Do not exceed 32g total daily dose of Diclofenac, or 8g per joint when applied to the upper body.
- Duration of treatment: Typically, up to 7 days without medical consultation. For osteoarthritis, review treatment after 4 weeks. Other indications, review after 2 weeks.
Children: Not recommended for children under 14 years.
Special Cases:
- Elderly Patients: The usual adult dose can be used but monitor for adverse events.
- Patients with Renal Impairment: Use with caution. Monitor renal function. Contraindicated in advanced renal disease.
- Patients with Hepatic Dysfunction: Use with caution. Monitor liver function.
- Patients with Comorbid Conditions: Use cautiously in those with asthma, cardiovascular diseases, gastrointestinal problems, or bleeding/clotting disorders.
Clinical Use Cases
The medication is primarily used for musculoskeletal pain relief. It’s not typically used in settings such as intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Adjust dosage for renal/hepatic impairment. Monitor for adverse events and adjust accordingly.
Side Effects
Common Side Effects
- Application site reactions: itching, irritation, redness, burning sensation, dryness
Rare but Serious Side Effects
- Allergic reactions (skin rash, hives, difficulty breathing, swelling of face, lips, tongue, or throat).
- Gastrointestinal bleeding or ulceration (especially with prolonged use or in high doses).
- Increased risk of heart attack or stroke.
- Renal or hepatic dysfunction.
Long-Term Effects
Chronic complications from prolonged topical use are rare due to limited systemic absorption, but include:
- Skin thinning or discoloration.
- Gastrointestinal issues.
- Renal or hepatic dysfunction.
Adverse Drug Reactions (ADR)
- Anaphylaxis
- Angioedema
- Stevens-Johnson syndrome
- Toxic epidermal necrolysis
Contraindications
- Hypersensitivity to diclofenac, methyl salicylate, menthol, linseed oil, or any other ingredients.
- Aspirin-sensitive asthma.
- History of allergic reaction to NSAIDs.
- Third trimester of pregnancy.
- Advanced renal disease.
- Open wounds or broken skin.
Drug Interactions
- Oral NSAIDs (increased risk of gastrointestinal side effects).
- Anticoagulants (increased risk of bleeding).
- ACE inhibitors (potential for renal dysfunction).
- Other topical medications applied to the same area (potential for interactions).
- Corticosteroids (increased risk of GI side effects)
- Methotrexate (increased toxicity)
- Lithium (increased serum levels)
Pregnancy and Breastfeeding
- Pregnancy: Contraindicated during the third trimester. Use with caution during the first and second trimesters only if essential and no safer alternatives exist. Potential for premature closure of fetal ductus arteriosus.
- Breastfeeding: Diclofenac passes into breast milk in small amounts. At therapeutic doses, effects on the nursing infant are unlikely, but use with caution and only if clearly needed.
Drug Profile Summary
- Mechanism of Action: Diclofenac and methyl salicylate inhibit COX enzymes, reducing pain and inflammation. Menthol creates a cooling sensation. Linseed oil enhances penetration.
- Side Effects: Application site reactions (itching, redness, burning), rarely allergic reactions or systemic side effects.
- Contraindications: Hypersensitivity, aspirin-sensitive asthma, third trimester of pregnancy, advanced renal disease.
- Drug Interactions: Oral NSAIDs, anticoagulants, ACE inhibitors.
- Pregnancy & Breastfeeding: Use with caution; contraindicated in third trimester.
- Dosage: 2-4 g applied 3-4 times daily to affected area. Max 32g/day.
- Monitoring Parameters: Renal and hepatic function, signs of gastrointestinal bleeding, allergic reactions.
Popular Combinations
This product itself represents a common combination. Adding other ingredients like thiocolchicoside (muscle relaxant) or capsaicin (counterirritant) can further enhance pain relief in certain cases. However, the potential for drug interactions and side effects increases with complex combinations.
Precautions
- Apply only to intact skin.
- Avoid contact with eyes, mucous membranes, and open wounds.
- Do not use occlusive dressings.
- Use cautiously in patients with liver or kidney disease, asthma, and during pregnancy/breastfeeding.
- Avoid prolonged sun exposure on treated areas.
- Monitor for signs of allergic reactions, gastrointestinal bleeding, or other adverse events.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac diethylamine + Linseed Oil + Menthol + Methyl Salicylate?
A: Adults and children over 14 years: apply 2-4 grams to the affected area 3-4 times daily. Do not exceed 32g total daily dose, and do not exceed 8g per joint when applied to upper body.
Q2: Can I use this gel if I am pregnant?
A: It’s contraindicated during the third trimester. Consult your doctor if you are pregnant or planning to become pregnant as it should only be used if essential.
Q3: Can I use this gel if I am breastfeeding?
A: While the medication can pass into breast milk, effects on the infant are usually minimal at therapeutic doses. Consult your doctor before using.
Q4: Can I use this gel on open wounds?
A: No, apply only to intact, healthy skin.
Q5: What should I do if I experience a burning sensation after applying the gel?
A: A mild burning sensation can be normal, especially with formulations containing capsaicin. If it’s severe or unbearable, wash the area with cool water and consult your doctor.
Q6: Can I use this gel along with oral pain relievers like ibuprofen?
A: Generally, combining topical and oral NSAIDs is not recommended due to the increased risk of side effects. Consult your doctor before combining any medications.
Q7: Can I use this gel for a headache?
A: No, this medication is for localized musculoskeletal and joint pain. It’s not effective for headaches.
Q8: How long can I use this gel without consulting a doctor?
A: Do not use for more than 7 days without seeking medical advice.
Q9: Are there any specific precautions for elderly patients?
A: The usual adult dosage can be used, but elderly patients should be carefully monitored for any adverse events.
