Usage
This combination medication is primarily prescribed for the local symptomatic relief of pain and inflammation associated with musculoskeletal disorders. These include:
- Mild to moderate muscle pain
- Contusions
- Post-traumatic pain
- Sprains and strains
- Knee pain/arthritis
- Low back pain
Pharmacological Classification:
This is a combination product with multiple classifications:
- Diclofenac: Non-steroidal anti-inflammatory drug (NSAID)
- Methyl Salicylate: NSAID, counterirritant
- Menthol: Counterirritant, topical analgesic
- Benzyl Alcohol: Topical anesthetic, antiseptic, preservative
- Linseed Oil: Anti-inflammatory, emollient
Mechanism of Action:
Diclofenac and Methyl Salicylate inhibit cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing pain and inflammation. Menthol and Benzyl Alcohol act as counterirritants, providing a cooling sensation and mild local anesthetic effect. Linseed oil enhances drug penetration through the skin due to its emollient properties and also contributes to anti-inflammatory action.
Alternate Names
This combination doesn’t have a specific international nonproprietary name (INN). It is often referred to by its component ingredients.
Brand Names:
Brand names vary depending on the manufacturer and region. Some examples include: Muscoleve, Volitra Plus Gel, DICLOTAL+ Gel, DICLOTAL-FORTE Gel. (Please note: Brand names are subject to regional availability and may change.)
How It Works
Pharmacodynamics:
Diclofenac and Methyl Salicylate exert their analgesic and anti-inflammatory effects by inhibiting COX-1 and COX-2 enzymes, which are responsible for the production of prostaglandins. Menthol and Benzyl Alcohol stimulate cold receptors in the skin, creating a cooling sensation that distracts from pain signals. Linseed oil, rich in alpha-linolenic acid (an omega-3 fatty acid), may have additional anti-inflammatory properties.
Pharmacokinetics:
- Absorption: Diclofenac is absorbed percutaneously, achieving higher concentrations in inflamed tissues compared to plasma. Methyl Salicylate is also absorbed through the skin. Menthol and Benzyl Alcohol are minimally absorbed systemically.
- Metabolism: Diclofenac is primarily metabolized in the liver. Methyl salicylate is metabolized to salicylic acid.
- Elimination: Diclofenac and its metabolites are mainly excreted in urine. Methyl salicylate and its metabolite (salicylic acid) are also excreted in urine.
Mode of Action:
The primary mode of action involves COX enzyme inhibition (Diclofenac and Methyl Salicylate), counterirritant action (Menthol and Benzyl Alcohol), and enhanced skin penetration (Linseed oil). These actions synergistically reduce pain and inflammation.
Elimination Pathways:
Primarily renal excretion for Diclofenac, Methyl Salicylate, and their metabolites.
Dosage
Standard Dosage
Adults:
Apply a thin layer to the affected area 3-4 times daily. A single dose is typically 2-4 grams (equivalent to a 4-8 cm strip from a standard tube). The maximum daily dose of diclofenac-containing topical preparations should not exceed 32 grams.
Children:
Use in children under 14 years of age is contraindicated due to limited safety and efficacy data. For children over 14, the dosage is usually the same as for adults.
Special Cases:
- Elderly Patients: Use with caution. Closely monitor for adverse events.
- Patients with Renal Impairment: Contraindicated in patients with moderate to severe renal impairment due to potential systemic accumulation of Diclofenac.
- Patients with Hepatic Dysfunction: Use with caution in patients with severe liver dysfunction.
- Patients with Comorbid Conditions: Use cautiously in patients with asthma, cardiovascular disease, or a history of peptic ulcers.
Clinical Use Cases
This medication is not typically used in clinical settings like intubation, surgical procedures, mechanical ventilation, or ICU use. Its application is primarily limited to topical pain relief in musculoskeletal conditions.
Dosage Adjustments
Dosage adjustments are typically not made for this topical formulation, except in cases of renal or hepatic impairment, where caution is advised.
Side Effects
Common Side Effects:
- Application site reactions (itching, irritation, redness, burning sensation, dryness)
- Skin rash
Rare but Serious Side Effects:
- Allergic reactions (urticaria, angioedema, bronchospasm)
- Severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis)
- Gastrointestinal bleeding (with prolonged use or in susceptible individuals)
- Cardiovascular events (increased risk with prolonged use or high doses)
Long-Term Effects:
Prolonged use can potentially increase the risk of gastrointestinal and cardiovascular events.
Adverse Drug Reactions (ADR):
Clinically significant ADRs are rare but include severe allergic reactions, severe skin reactions, and gastrointestinal bleeding.
Contraindications
- Hypersensitivity to any component of the formulation (Diclofenac, Methyl Salicylate, Menthol, Benzyl Alcohol, Linseed oil, or any excipients)
- Asthma, urticaria, or acute rhinitis precipitated by aspirin or other NSAIDs
- Third trimester of pregnancy
- Patients with renal impairment
- Recent coronary artery bypass graft (CABG) surgery
Drug Interactions
- Oral NSAIDs: Increased risk of gastrointestinal side effects
- Anticoagulants (e.g., warfarin): Increased risk of bleeding
- Methotrexate: Increased risk of methotrexate toxicity
- Cyclosporine: Increased risk of nephrotoxicity
- Other topical medications containing salicylates or diclofenac: May increase the risk of local and systemic adverse effects
Pregnancy and Breastfeeding
- Pregnancy: Contraindicated in the third trimester. Use with caution during the first and second trimesters only if the potential benefits outweigh the risks.
- Breastfeeding: Limited information is available. Use with caution.
Drug Profile Summary
- Mechanism of Action: Inhibition of COX enzymes, counterirritant, and mild local anesthetic effects
- Side Effects: Application site reactions (itching, burning, redness); rarely, allergic reactions, severe skin reactions, GI bleeding.
- Contraindications: Hypersensitivity; asthma/urticaria/rhinitis induced by NSAIDs; third-trimester pregnancy; renal impairment; recent CABG surgery; children <14 years.
- Drug Interactions: Oral NSAIDs, anticoagulants, methotrexate, cyclosporine.
- Pregnancy & Breastfeeding: Contraindicated in the third trimester; caution during breastfeeding.
- Dosage: Apply thinly 3-4 times daily, not exceeding recommended limits.
- Monitoring Parameters: Local skin reactions and systemic side effects.
Popular Combinations
This product already contains multiple active ingredients. Additional combinations are generally not recommended unless specifically prescribed by a physician.
Precautions
- Apply only to intact skin, avoid open wounds, mucous membranes, and eyes.
- Do not use occlusive dressings.
- Wash hands after application.
- Monitor for local skin reactions and systemic side effects.
- Pre-existing medical conditions: Use cautiously in patients with liver or kidney dysfunction, asthma, or cardiovascular disease.
- Avoid excessive sun exposure.
- Use with caution in elderly patients.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Benzyl Alcohol + Diclofenac + Linseed Oil + Menthol + Methyl Salicylate?
A: Apply 2-4 grams to the affected area 3-4 times daily. Do not exceed 32 grams of diclofenac-containing topical product daily.
Q2: Can this gel be used during pregnancy?
A: It’s contraindicated during the third trimester. Use with caution during the first and second trimesters only if clearly needed.
Q3: What are the common side effects?
A: Common side effects include application site reactions like itching, redness, burning, and dryness.
Q4: Are there any drug interactions I should be aware of?
A: Yes. It can interact with oral NSAIDs, anticoagulants like warfarin, methotrexate, and cyclosporine.
Q5: Can I use this gel if I have asthma?
A: This gel is contraindicated in individuals with asthma, urticaria, or acute rhinitis triggered by aspirin or other NSAIDs.
A: Linseed oil helps with drug penetration and has anti-inflammatory properties.
Q7: Can this be used on open wounds?
A: No. Apply only to intact skin. Avoid open wounds, mucous membranes, and eyes.
Q8: Can I use a heating pad or tight bandage over the applied gel?
A: No. Occlusive dressings are not recommended.
Q9: What should I do if I accidentally ingest this gel?
A: Seek immediate medical attention. While systemic absorption is low, significant ingestion could lead to systemic side effects.
Q10: Can I use this with other topical pain relievers?
A: Consult a physician before using with other topical pain medications, particularly those containing salicylates or diclofenac. Concurrent use may increase the risk of adverse effects.
