Diclofenac + Linseed Oil + Menthol + Methyl Salicylate + Thiocolchicoside

Usage

• This combination medication is primarily prescribed for the topical relief of musculoskeletal pain and inflammation associated with conditions like osteoarthritis, sprains, strains, back pain, frozen shoulder, and soft tissue rheumatism.
• Pharmacological Classification: Topical non-steroidal anti-inflammatory drug (NSAID) combined with a muscle relaxant, counterirritants, and an anti-inflammatory agent.
• Mechanism of Action: Diclofenac and methyl salicylate inhibit cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis and thereby mitigating pain and inflammation. Thiocolchicoside acts as a muscle relaxant by activating GABA inhibitory pathways in the spinal cord, alleviating muscle spasms and stiffness. Linseed oil, rich in omega-3 fatty acids, contributes to the anti-inflammatory effect. Menthol provides a cooling sensation and acts as a counterirritant, further reducing pain perception.

Alternate Names

• No internationally recognized non-proprietary name exists for this specific combination. It is generally referred to by the names of its constituent drugs.
• Brand Names: Numerous brand names exist depending on the manufacturer and region, including Nifoxide-Plus, Reledol, Thiox Gel, Spafast Gel, ThioQuest Gel, Krishat Relief Gel, and Muscoleve.

How It Works

• Pharmacodynamics: Diclofenac and Methyl Salicylate, both NSAIDs, inhibit COX-1 and COX-2 enzymes, reducing the production of prostaglandins that mediate pain and inflammation. Thiocolchicoside, a muscle relaxant, acts centrally by activating GABAergic inhibitory pathways in the spinal cord, thus alleviating muscle spasms. Linseed oil contains alpha-linolenic acid (ALA), an omega-3 fatty acid with anti-inflammatory properties. Menthol activates TRPM8 receptors, producing a cooling sensation and acting as a counterirritant to reduce pain perception.
• Pharmacokinetics: The gel is applied topically, and the active ingredients are absorbed through the skin. Diclofenac’s systemic absorption is limited. Hepatic metabolism and renal excretion are likely involved in the elimination of absorbed components. The pharmacokinetics of the other ingredients in this topical formulation are less well-defined, but they are also likely metabolized in the liver and excreted via the kidneys.

Dosage

Standard Dosage

Adults: Apply a thin layer to the affected area 2-4 times daily. The maximum daily dose of diclofenac should not exceed 32g, including from all sources.

Children: Not recommended for use in children below 12 or 15 years of age, depending on the specific product formulation, as safety and efficacy have not been established.

Special Cases:

• Elderly Patients: Use with caution. Monitor for systemic adverse effects. Dose adjustments may be necessary based on individual patient response and tolerability.
• Patients with Renal Impairment: Use with caution. Monitor renal function. Dose adjustment may be necessary.
• Patients with Hepatic Dysfunction: Use with caution. Monitor liver function. Dose adjustment may be necessary.
• Patients with Comorbid Conditions: Use with caution in patients with a history of peptic ulcer disease, gastrointestinal bleeding, asthma, or allergic reactions to NSAIDs.

Clinical Use Cases

The medication is intended for topical use only and is not indicated for the following clinical settings:

• Intubation
• Surgical Procedures
• Mechanical Ventilation
• Intensive Care Unit (ICU) Use
• Emergency Situations

Dosage Adjustments: Dosage adjustments are generally not required except in cases of renal or hepatic impairment, or in elderly patients. Start with the lowest effective dose and titrate upwards based on patient response and tolerance.

Side Effects

Common Side Effects:

• Application site reactions (burning, itching, redness, dryness, rash).

Rare but Serious Side Effects:

• Allergic reactions (e.g., hives, difficulty breathing, swelling of the face, lips, tongue, or throat).
• Systemic effects of Diclofenac (e.g., gastrointestinal bleeding, kidney problems).

Long-Term Effects:

• Potential for skin thinning or other skin changes with prolonged use.

Adverse Drug Reactions (ADR):

• Severe skin reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis).

Contraindications

• Hypersensitivity to any component of the gel.
• History of asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.
• Active peptic ulcer or gastrointestinal bleeding.
• Open wounds, cuts, or infected skin.
• Third trimester of pregnancy.

Drug Interactions

• Oral anticoagulants (e.g., warfarin): Increased risk of bleeding.
• Antiplatelet agents (e.g., clopidogrel): Increased risk of bleeding.
• Other NSAIDs (e.g., ibuprofen, aspirin, naproxen): Increased risk of gastrointestinal and renal adverse effects.
• Methotrexate: Increased risk of methotrexate toxicity.
• Cyclosporine: Increased risk of nephrotoxicity.
• Diuretics and Antihypertensive drugs: May reduce the effectiveness of these medications.
• Alcohol: Although no specific interaction has been established, it is prudent to avoid or limit alcohol consumption during treatment.

Pregnancy and Breastfeeding

• Pregnancy: Consult a doctor before use, especially during the third trimester. Use only if clearly needed and no safer alternative is available.
• Breastfeeding: Consult a doctor before use. Limited data suggest that small amounts may be excreted in breast milk.

Drug Profile Summary (See dedicated sections above for detailed information).

Popular Combinations

This product is already a combination of several active ingredients. Additional combinations are usually not necessary and should be avoided unless specifically prescribed by a physician.

Precautions (See dedicated sections above for detailed information).

FAQs (Frequently Asked Questions)

(See dedicated sections above for answers)

• Q1: What is the recommended dosage?
• Q2: What are the common side effects?
• Q3: Can I use this gel if I am pregnant or breastfeeding?
• Q4: What should I do if I miss a dose?
• Q5: Can I use this gel on open wounds or broken skin?
• Q6: What are the potential drug interactions?
• Q7: How should I store this medication?
• Q8: Can this gel be used with other pain relievers?
• Q9: Are there any long-term effects of using this gel?