Usage
- Medical Conditions: This topical medication is prescribed for the relief of pain and inflammation associated with musculoskeletal and joint conditions such as sprains, strains, bruises, tendinitis, bursitis, backache, osteoarthritis, rheumatoid arthritis, and other soft tissue rheumatism.
- Pharmacological Classification: Topical non-steroidal anti-inflammatory drug (NSAID) combined with counterirritants and a skin soother.
- Mechanism of Action: Diclofenac reduces pain and inflammation by inhibiting cyclooxygenase (COX) enzymes, which are responsible for producing prostaglandins. Methyl salicylate and menthol act as counterirritants, creating warming and cooling sensations respectively, which distract from pain perception. Linseed oil, rich in omega-3 fatty acids, adds anti-inflammatory effects and facilitates drug penetration.
Alternate Names
- No officially recognized alternate names for this specific combination exist.
- Brand names vary depending on the manufacturer. Some examples include: Muscoleve, Krishat Relief Gel, Diclotal+ Gel, Lofnac Gel, Fixache Gel.
How It Works
- Pharmacodynamics: Diclofenac inhibits COX-1 and COX-2 enzymes, reducing prostaglandin synthesis, thus mitigating pain and inflammation. Methyl salicylate and menthol stimulate peripheral nerve endings, creating a sensation of warmth or coolness that masks pain signals. Linseed oil may provide additional anti-inflammatory effects through its omega-3 fatty acids.
- Pharmacokinetics: Topical application leads to minimal systemic absorption of diclofenac. The other components primarily exert local effects. Metabolism and elimination pathways for absorbed diclofenac are similar to oral forms (primarily hepatic metabolism and renal excretion).
- Mode of Action: Diclofenac primarily targets COX enzymes. Methyl salicylate and menthol act on TRP channels (TRPV1 and TRPM8 respectively), influencing sensory nerve signaling. Linseed oil’s action is related to the anti-inflammatory properties of omega-3 fatty acids.
Dosage
Standard Dosage
Adults: Apply a thin layer to the affected area 3-4 times daily. The amount of gel per application can range from 2-4 grams, depending on the size of the affected area. Do not exceed 32 grams of diclofenac-containing product per day across all treated areas.
Children: Not recommended for children under 14 years of age due to limited safety and efficacy data. For older children, consultation with a doctor is essential.
Special Cases:
- Elderly Patients: Use with caution due to potential increased risk of adverse effects, especially gastrointestinal issues and renal impairment.
- Patients with Renal Impairment: Use with caution and under close medical supervision.
- Patients with Hepatic Dysfunction: Use with caution and under close medical supervision.
- Patients with Comorbid Conditions: Caution is advised in patients with asthma, cardiovascular disease, bleeding disorders, peptic ulcers, and gastrointestinal problems.
Clinical Use Cases
The drug is primarily used for localized pain relief in outpatient settings and is not typically applied during intubation, surgical procedures, mechanical ventilation, or in the ICU or for emergency situations.
Dosage Adjustments
Dose adjustments may be necessary for elderly patients and those with renal or hepatic dysfunction. The lowest effective dose for the shortest duration should be used in these populations.
Side Effects
Common Side Effects
- Itching
- Irritation
- Redness
- Burning or stinging sensation at the application site
- Dry skin
- Contact dermatitis
Rare but Serious Side Effects
- Allergic reactions (rash, hives, itching, swelling, difficulty breathing)
- Severe skin reactions (blistering, peeling)
Long-Term Effects
Long-term use can potentially lead to skin thinning or other skin problems. Systemic effects are rare due to low absorption but could include gastrointestinal bleeding or renal issues with prolonged high doses.
Adverse Drug Reactions (ADR)
- Severe allergic reactions (anaphylaxis)
- Gastrointestinal bleeding or ulceration (rare with topical use)
Contraindications
- Hypersensitivity to diclofenac, aspirin, other NSAIDs, or any component of the formulation.
- Asthma, urticaria, or acute rhinitis precipitated by aspirin or other NSAIDs.
- Third trimester of pregnancy.
- Open wounds or broken skin.
- Children under 14 years of age.
- Recent heart surgery or history of heart attack, stroke, or gastrointestinal bleeding.
Drug Interactions
- Oral NSAIDs (increased risk of side effects)
- Anticoagulants (e.g., warfarin, increased bleeding risk)
- ACE inhibitors (potential reduced effectiveness of ACE inhibitors)
- Topical medications applied to the same area
Pregnancy and Breastfeeding
- Pregnancy: Contraindicated in the third trimester. Use with caution during the first and second trimesters only if clearly needed and under close medical supervision.
- Breastfeeding: Diclofenac is excreted in breast milk in small amounts. Consult a doctor before using while breastfeeding.
Drug Profile Summary
- Mechanism of Action: Inhibits COX enzymes, reducing pain and inflammation; counterirritant action.
- Side Effects: Itching, irritation, redness, burning sensation, skin reactions.
- Contraindications: Hypersensitivity, aspirin-induced asthma/urticaria, third-trimester pregnancy, open wounds, children <14 years.
- Drug Interactions: Oral NSAIDs, anticoagulants, ACE inhibitors.
- Pregnancy & Breastfeeding: Use with caution during pregnancy (contraindicated in third trimester); consult doctor while breastfeeding.
- Dosage: Apply thinly 3-4 times/day; 2-4 g/application; max 32 g/day.
- Monitoring Parameters: Observe for skin reactions and any signs of systemic effects.
Popular Combinations
- This formulation itself is a common combination. Additional combined therapy with oral analgesics is generally avoided unless deemed necessary by a physician due to potential increased risk of adverse effects.
Precautions
- Avoid contact with eyes, mucous membranes, and open wounds.
- Wash hands after application.
- Use the lowest effective dose for the shortest duration.
- Consult a doctor if symptoms worsen or persist for more than 7 days.
- Be cautious in patients with asthma, cardiovascular disease, bleeding disorders, peptic ulcers, and gastrointestinal issues.
- Avoid prolonged sun exposure.
- Limit alcohol intake.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Linseed Oil + Menthol + Methyl Salicylate?
A: Apply a thin layer 2-4 grams to the affected area 3-4 times daily. Do not exceed 32 grams of this product per day.
Q2: Can I use this gel on open wounds?
A: No, apply only to intact skin. Avoid contact with open wounds, mucous membranes, and eyes.
Q3: Can I use this with other pain relievers like ibuprofen?
A: Consult your doctor before combining with other NSAIDs like ibuprofen, as it may increase the risk of side effects.
Q4: I’m pregnant. Can I use this gel?
A: It’s contraindicated in the third trimester. Consult your doctor before use during the first and second trimesters.
Q5: I’m breastfeeding. Is it safe to use this gel?
A: Diclofenac passes into breast milk in small amounts. Discuss the risks and benefits with your doctor.
Q6: Can children use this gel?
A: Not recommended for children under 14 years old. Consult a doctor for older children.
Q7: How long can I use this gel?
A: Do not use for more than 14 days unless advised by a doctor. Consult if symptoms do not improve within 7 days or worsen.
Q8: What if I accidentally get the gel in my eyes?
A: Rinse thoroughly with water and consult a doctor if irritation persists.
Q9: What are the most common side effects?
A: Common side effects include itching, irritation, redness, and burning sensation at the application site.
Q10: What should I do if I develop a rash after using the gel?
A: Discontinue use and consult your doctor.
