Usage
This combination medication is prescribed for topical relief of pain and inflammation associated with musculoskeletal conditions like sprains, strains, bruises, back pain, and arthritis. It falls under the pharmacological classifications of:
- Nonsteroidal anti-inflammatory drug (NSAID): (Diclofenac)
- Local anesthetic: (Lidocaine)
- Muscle relaxant: (Mephenesin)
- Counterirritants: (Menthol and Methyl Salicylate)
- Emollient: (Linseed Oil)
The mechanism of action involves a multifaceted approach: Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and inflammation. Lidocaine blocks nerve signals, reducing pain sensation. Mephenesin acts centrally to relax muscles. Methyl salicylate and menthol act as counterirritants, creating warming and cooling sensations that distract from pain. Linseed oil enhances penetration of active ingredients.
Alternate Names
This specific combination doesn’t have a single generic name. It is sometimes referred to by brand names such as Lignogesic gel.
How It Works
Pharmacodynamics: Diclofenac reduces pain and inflammation by inhibiting COX enzymes, decreasing prostaglandin synthesis. Lidocaine blocks sodium channels, inhibiting nerve impulse transmission and producing local anesthesia. Mephenesin acts on the central nervous system to relax skeletal muscles. Methyl salicylate and menthol cause vasodilation, creating warming and cooling sensations that distract from pain perception.
Pharmacokinetics: When applied topically, diclofenac is absorbed through the skin, reaching therapeutic levels in underlying tissues and joints. Lidocaine absorption is limited, primarily exerting a local effect. Systemic absorption of other components is minimal. Diclofenac is primarily metabolized in the liver and excreted by the kidneys. Lidocaine is metabolized in the liver and excreted in urine.
Mode of Action: Diclofenac’s mode of action is COX enzyme inhibition, specifically COX-1 and COX-2, reducing prostaglandin production. Lidocaine blocks voltage-gated sodium channels in nerve axons, inhibiting action potential propagation. Mephenesin’s mode of action is not fully understood but it is believed to act on the central nervous system, possibly as a central muscle relaxant. Methyl Salicylate and Menthol stimulate TRP channels in the skin to produce cooling and warming sensations.
Elimination Pathways: Diclofenac is primarily excreted by the kidneys, with some biliary excretion. Lidocaine is metabolized by the liver and excreted in urine.
Dosage
Standard Dosage
Adults: Apply a thin layer to the affected area 3-4 times daily. The amount applied depends on the size of the affected area, usually 2-4 grams of gel (a circular mass approximately 2-2.5 cm in diameter).
Special Cases:
- Elderly Patients: No specific dosage adjustments are typically needed, but start with a lower dose and monitor closely for adverse events.
- Patients with Renal Impairment: Use with caution. Monitor renal function.
- Patients with Hepatic Dysfunction: Use with caution and at lower doses. Monitor liver function.
- Patients with Comorbid Conditions: Use with caution in patients with asthma, a history of gastrointestinal bleeding, or cardiovascular diseases.
Clinical Use Cases
This topical formulation is not intended for clinical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations.
Dosage Adjustments
Dosage adjustments are generally not required except in special cases as mentioned above.
Side Effects
Common Side Effects
Application site reactions (burning, irritation, itching, redness, rash, dryness).
Rare but Serious Side Effects
Allergic reactions (urticaria, angioedema, anaphylaxis). Systemic side effects like gastrointestinal issues or kidney problems are rare with topical use.
Long-Term Effects
Prolonged topical use may cause skin thinning or irritation. Systemic side effects are rare with topical application.
Adverse Drug Reactions (ADR)
Severe allergic reactions requiring immediate discontinuation and medical attention.
Contraindications
Hypersensitivity to any component. History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Third trimester of pregnancy. Open wounds or broken skin. Age below 6 or 14 years, depending on the formulation.
Drug Interactions
May interact with oral NSAIDs, anticoagulants (warfarin), diuretics, and some antihypertensives. Concomitant use of other topical medications on the same area should be avoided unless specifically prescribed by a doctor.
Pregnancy and Breastfeeding
Avoid use during the third trimester. Use during the first and second trimesters only if the potential benefit justifies the potential risk to the fetus. Consult a doctor before use during pregnancy or breastfeeding. Excretion in breast milk is minimal with topical diclofenac, but avoid application on the nipple area to minimize infant exposure.
Drug Profile Summary
- Mechanism of Action: Multimodal – NSAID (diclofenac), local anesthetic (lidocaine), muscle relaxant (mephenesin), counterirritants (menthol, methyl salicylate), emollient (linseed oil).
- Side Effects: Application site reactions (burning, itching, redness), rarely allergic reactions.
- Contraindications: Hypersensitivity, aspirin-sensitive asthma, third trimester of pregnancy.
- Drug Interactions: Oral NSAIDs, anticoagulants, diuretics, antihypertensives.
- Pregnancy & Breastfeeding: Avoid in the third trimester. Consult a doctor before use during pregnancy or breastfeeding.
- Dosage: Apply topically 3-4 times daily, 2-4 grams per application.
- Monitoring Parameters: Monitor for local skin reactions and any systemic side effects. Renal and liver function tests may be warranted for prolonged use or in patients with pre-existing conditions.
Popular Combinations
This is already a combination product. Combining it with other topical analgesics is generally not recommended unless specifically prescribed.
Precautions
Avoid application to broken skin or open wounds. Avoid contact with eyes, mucous membranes, and sensitive areas. Wash hands after use. Use with caution in patients with liver or kidney disease, asthma, or a history of gastrointestinal bleeding. Avoid prolonged or excessive use. Don’t bandage tightly. Protect treated area from sunlight.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Diclofenac + Lidocaine + Linseed Oil + Menthol + Mephenesin + Methyl Salicylate?
A: Apply a thin layer to the affected area 3-4 times per day. The amount to be applied depends on the size of the area, usually 2-4 grams per application for adults. Consult product-specific guidelines for children, if applicable.
Q2: Can this combination be used during pregnancy?
A: Avoid using during the third trimester. Consult a doctor before using during the first and second trimesters.
Q3: What are the common side effects?
A: Common side effects include application site reactions like burning, itching, redness, and rash.
Q4: Are there any drug interactions I should be aware of?
A: Yes, it may interact with oral NSAIDs, anticoagulants, diuretics, and some antihypertensives. Inform your doctor about all medications you are taking.
Q5: Can I use this on broken skin?
A: No, avoid applying to broken skin, open wounds, or infected areas.
Q6: How long can I use this medication?
A: Do not use for prolonged periods without consulting a doctor. If symptoms persist after a few days, seek medical advice.
Q7: What should I do if I accidentally get it in my eyes?
A: Immediately rinse your eyes with plenty of water. If irritation persists, seek medical attention.
Q8: Can I use a heating pad after applying this medication?
A: No, do not apply heat to the treated area.
Q9: Is it safe to use this with other topical pain relievers?
A: Do not combine with other topical pain relievers unless specifically advised by your doctor.
Q10: What happens if I use too much?
A: Using excessive amounts can increase the risk of systemic side effects, though they are rare with topical application. Always follow the recommended dosage. If you experience any unusual symptoms, contact your doctor.
