Capsaicin + Diclofenac + Linseed Oil + Menthol + Methyl Salicylate

Usage

This topical medication is prescribed for the local symptomatic relief of mild to moderate musculoskeletal pain and inflammation. This includes:

• Muscle pain
• Sprains
• Strains
• Bruises
• Joint pain associated with osteoarthritis
• Back pain

Pharmacological Classification:

• Topical Analgesic
• Non-Steroidal Anti-Inflammatory Drug (NSAID) - Diclofenac component
• Counterirritant - Capsaicin, Menthol, and Methyl Salicylate components

Mechanism of Action: This combination product works through multiple pathways to reduce pain and inflammation. Diclofenac inhibits cyclooxygenase (COX) enzymes, reducing prostaglandin synthesis, thereby decreasing pain and inflammation. Capsaicin acts on TRPV1 receptors, initially causing a burning sensation, but subsequently desensitizing nociceptors and reducing pain transmission. Methyl salicylate and menthol act as counterirritants, producing cooling and warming sensations that distract from pain perception. Methyl salicylate also converts to salicylic acid, contributing to anti-inflammatory effects. Linseed oil, rich in alpha-linolenic acid, aids in skin penetration and has some anti-inflammatory properties.

Alternate Names

There are no officially recognized alternate names for this specific combination. However, individual components have other names:

• Diclofenac: Diclofenac sodium, Diclofenac potassium, Diclofenac diethylamine
• Methyl Salicylate: Wintergreen oil
• Linseed Oil: Flaxseed oil

Brand Names: Brand names vary regionally. Examples from the sources include Muscoleve, Diclosal Plus, Krishat Relief Gel, Orthofec Plus, Diclotal-Forte, and Speedo Strong.

How It Works

Pharmacodynamics: Diclofenac, a non-selective NSAID, inhibits both COX-1 and COX-2 enzymes, reducing prostaglandin synthesis, which mediates pain and inflammation. Capsaicin, menthol, and methyl salicylate primarily act as counterirritants, stimulating peripheral nerve endings and creating sensations of warmth, coolness, or burning that distract from deeper pain. Capsaicin also depletes substance P, a neurotransmitter involved in pain transmission. Linseed oil enhances the penetration of other active ingredients into the skin due to its emollient properties.

Pharmacokinetics: Following topical application, diclofenac is absorbed through the skin and reaches therapeutic levels in underlying tissues and joints, with minimal systemic absorption. Methyl salicylate is also absorbed through the skin and metabolized to salicylic acid. Menthol and capsaicin exert their effects locally, with limited systemic absorption. The pharmacokinetics of linseed oil, applied topically, are not well-established.

Receptor Binding/Enzyme Inhibition/Neurotransmitter Modulation: Diclofenac inhibits COX-1 and COX-2 enzymes. Capsaicin activates and then desensitizes TRPV1 receptors. Menthol activates TRPM8 receptors. Methyl salicylate, upon conversion to salicylic acid, may also inhibit COX enzymes.

Elimination Pathways: Diclofenac is primarily metabolized in the liver and excreted through the kidneys. Salicylic acid (metabolite of methyl salicylate) is also conjugated in the liver and eliminated renally. Menthol and capsaicin are primarily metabolized locally and systemically by the cytochrome P450 system.

Dosage

Standard Dosage

Adults (over 14 years): Apply a thin layer of the gel/cream to the affected area 3-4 times daily. Gently rub until absorbed. The amount required depends on the size of the affected area. Typically, a 2-4 g (4-8 cm strip) dose is recommended. Do not exceed 32 grams of diclofenac-containing product in 24 hours.

Children: Use in children below 14 years is not recommended due to insufficient safety and efficacy data. Some sources suggest use in children above 12 years under strict medical supervision with similar dosing as adults, but this is not widely accepted.

Special Cases:

• Elderly Patients: Generally, no dosage adjustment is needed, but monitor for systemic side effects due to potentially increased skin permeability.
• Patients with Renal Impairment: Use cautiously as systemic absorption, though minimal, can affect renal function. Monitor renal function.
• Patients with Hepatic Dysfunction: Use cautiously as diclofenac and methyl salicylate are metabolized in the liver. Monitor liver function.
• Patients with Comorbid Conditions: Use cautiously in patients with cardiovascular disease, asthma, gastrointestinal bleeding history, or recent heart surgery due to increased risk of adverse effects.

Clinical Use Cases

The medication is intended for topical use and not recommended for systemic administration in the following cases:

• Intubation: Not applicable.
• Surgical Procedures: Not applicable.
• Mechanical Ventilation: Not applicable.
• Intensive Care Unit (ICU) Use: Not applicable.
• Emergency Situations: Not applicable.

Dosage Adjustments

Dose adjustments based on patient-specific factors are discussed above under “Special Cases.”

Side Effects

Common Side Effects:

• Application site reactions: Itching, burning, stinging, redness, dryness, rash.

Rare but Serious Side Effects:

• Allergic reactions: Hives, difficulty breathing, swelling of the face, lips, tongue, or throat.
• Systemic effects (with overuse or prolonged use on large skin areas): Gastrointestinal bleeding or ulceration, increased risk of cardiovascular events (heart attack, stroke), renal dysfunction.

Long-Term Effects:

Potential long-term complications include skin thinning, discoloration, or photosensitivity with prolonged use, especially at high doses.

Adverse Drug Reactions (ADR):

Severe allergic reactions, significant gastrointestinal bleeding, acute renal failure, and cardiovascular events.

Contraindications

• Hypersensitivity to any components, including diclofenac, capsaicin, methyl salicylate, linseed oil, or menthol.
• History of asthma, urticaria, or acute rhinitis precipitated by aspirin or other NSAIDs.
• Third trimester of pregnancy.
• Recent coronary artery bypass graft (CABG) surgery.
• Open wounds or broken skin.

Drug Interactions

• Oral NSAIDs: Increased risk of systemic side effects.
• Anticoagulants (e.g., warfarin): Methyl salicylate may potentiate anticoagulant effects.
• ACE inhibitors: May reduce antihypertensive efficacy.
• Topical medications: Interactions with other topical products applied to the same area.

Pregnancy and Breastfeeding

• Pregnancy: Contraindicated in the third trimester. Use with caution in the first and second trimesters only if potential benefits outweigh the risks.
• Breastfeeding: Diclofenac is excreted in breast milk in small amounts. While adverse effects on the infant are unlikely at therapeutic doses, use with caution and avoid applying to the breasts.

Drug Profile Summary

• Mechanism of Action: Multimodal analgesic: Diclofenac (NSAID), capsaicin (TRPV1 agonist and substance P depleter), methyl salicylate (counterirritant, converted to salicylic acid), menthol (counterirritant), linseed oil (enhances absorption).
• Side Effects: Application site reactions (itching, burning, redness), rarely allergic reactions or systemic effects with excessive use.
• Contraindications: Hypersensitivity, aspirin/NSAID-induced asthma/urticaria/rhinitis, third trimester of pregnancy, recent CABG surgery, open wounds.
• Drug Interactions: Oral NSAIDs, anticoagulants, ACE inhibitors.
• Pregnancy & Breastfeeding: Use with caution. Contraindicated in third-trimester pregnancy.
• Dosage: Adults: 2-4g, 3-4 times/day topically. Children under 14: Not recommended.
• Monitoring Parameters: If used long-term or excessively: Monitor for systemic side effects, including renal and liver function, gastrointestinal symptoms, and cardiovascular events.

Popular Combinations

Not applicable, this is already a combination product.

Precautions

• Apply only to intact skin. Avoid contact with eyes and mucous membranes.
• Wash hands after application (unless treating hands).
• Do not use occlusive dressings.
• Avoid sun exposure on treated areas.
• Patients with hepatic/renal dysfunction, cardiovascular disease, or asthma should use cautiously.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Capsaicin + Diclofenac + Linseed Oil + Menthol + Methyl Salicylate?

A: Adults: Apply 2-4g (4-8 cm strip) to the affected area 3-4 times daily. Do not exceed 32g total diclofenac-containing product in 24 hours. Children below 14 years: Not recommended.

Q2: Can I use this cream if I am pregnant or breastfeeding?

A: It is contraindicated in the third trimester of pregnancy. Consult a doctor before use during pregnancy or while breastfeeding.

Q3: Can I use this cream on broken skin or open wounds?

A: No, apply only to intact skin.

Q4: I have asthma. Can I use this product?

A: If you have asthma triggered by aspirin or other NSAIDs, this product is contraindicated.

Q5: Can I use a heating pad after applying this cream?

A: No, avoid applying heat to the treated area.

Q6: I am taking warfarin. Can I use this cream?

A: Consult your physician. Methyl salicylate may interact with warfarin and increase bleeding risk. Close monitoring may be required.

Q7: What should I do if I experience a burning sensation after application?

A: A mild burning sensation can be normal initially, but if it is severe, wash the area with cool water and consult your doctor.

Q8: Can I use this cream together with oral ibuprofen?

A: Avoid concomitant use of oral NSAIDs with this cream to minimize the risk of systemic adverse events. Consult your doctor.

Q9: How long can I use this cream?

A: You should use this medication for the duration recommended by your healthcare provider. For osteoarthritis, therapy should be reviewed after 4 weeks. For other indications, review treatment after 2 weeks.