methylsalicylate/menthol topical

Action and Spectrum

Actions and Spectrum: 

methylsalicylate and menthol are active ingredients in topical products, particularly in pain relief formulations such as creams, ointments, and gels. They have distinct actions and provide a combined spectrum of effects. 

• methylsalicylate: methylsalicylate is derived from salicylic acid and has analgesic (pain-relieving) and anti-inflammatory properties. It is often used topically to alleviate muscle and joint pain, including arthritis, strains, sprains, and minor sports injuries. methylsalicylate works by inhibiting the production of prostaglandins, which contribute to pain and inflammation. It is generally absorbed through the skin and acts locally on the affected area. 
• menthol: menthol is a naturally occurring compound derived from mint oils. It produces a cooling and numbing sensation when applied topically. menthol acts as a counterirritant, temporarily relieving attention from underlying pain. It stimulates the skin’s cold receptors, producing a cooling sensation that helps mask pain and provide a soothing effect. menthol is commonly used in topical products for conditions such as muscle aches, sprains, and insect bites. 

Combining methylsalicylate and menthol: When methylsalicylate and menthol are used in topical formulations, they can synergize. The cooling sensation of menthol helps alleviate discomfort, while methylsalicylate targets pain and inflammation at a deeper level. This combination can provide a broader spectrum of relief for various musculoskeletal conditions. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Tingling 

Burning 

Stinging 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

methylsalicylate/menthol topical products may have contraindications in certain situations. Here are some potential contraindications to consider: 

• Allergy or hypersensitivity: Individuals allergic or hypersensitive to methylsalicylate, menthol, or any other ingredients present in the topical product should avoid its use. 
• Broken or damaged skin: Using methylsalicylate/menthol topical products is generally contraindicated on broken or damaged skin, such as open wounds, cuts, abrasions, or burns. Applying these products to compromised skin can lead to irritation, increased absorption, or adverse reactions. 
• Asthma or respiratory conditions: People with a history of asthma or other respiratory conditions may be more susceptible to respiratory irritation or bronchospasm triggered by methylsalicylate or menthol vapors. These individuals should exercise caution or avoid using topical products containing these ingredients. 
• Children and infants: methylsalicylate/menthol topical products may only suit young children or infants, especially with proper medical guidance. The skin of young children may be more sensitive, and systemic absorption of these ingredients can be higher in this population. 
• Pregnancy and breast-feeding: There is lesser information on the safety of methylsalicylate/menthol topical products during pregnancy and breastfeeding.  
• Sensitivity to salicylates or aspirin: Individuals with known sensitivities or allergies to salicylates or aspirin should exercise caution when using methylsalicylate/menthol topical products, as they contain methylsalicylate, a salicylate derivative. 

Caution 

When using methylsalicylate/menthol topical products, it is crucial to consider specific cautions. While these products are generally safe when used as directed, here are some cautions to keep in mind: 

• Avoid contact with sensitive areas: Avoid contact with sensitive areas like eyes, nose, mouth, and genital area. These products are intended for external use and should not be ingested/applied to mucous membranes. 
• Do not apply to damaged/irritated skin: Avoid applying methylsalicylate/menthol topical products to broken, damaged, or irritated skin. Doing so may enhance the risk of adverse reactions or discomfort. 
• Patch test for skin sensitivity: Before applying the product to a large area, especially if you have sensitive skin, it is generally advisable to perform a patch test. Apply a minute amount of the product near the area of the skin and wait for any signs of irritation/allergic reaction, such as redness, itching, or swelling. If any adverse reactions occur, discontinue use. 
• Do not bandage tightly: Do not cover the application area with tight bandages or occlusive dressings unless specifically instructed by a healthcare professional. This can increase the absorption of the active ingredients and may lead to systemic effects. 
• Use as directed: Follow the instructions which is provided with the specific product regarding the recommended frequency and duration. Stay within the recommended dosage or apply the product more frequently than instructed. 
• Consult a healthcare professional for any underlying medical conditions, are taking other medications, or have concerns about using methylsalicylate/menthol topical products; it is advisable to meet with a healthcare professional/pharmacist for personalized advice. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Yes 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

methylsalicylate and menthol are active ingredients in topical products that exert their effects through different pharmacological mechanisms. Here’s an overview of their pharmacology: 

• methylsalicylate: methylsalicylate is derived from salicylic acid and belongs to the nonsteroidal anti-inflammatory drugs (NSAIDs) class. When applied topically, methyl salicylate exhibits analgesic (pain-relieving) and anti-inflammatory properties. Its mechanism of action involves inhibiting the synthesis of prostaglandins, which are chemical mediators involved in pain and inflammation. Methyl salicylate helps alleviate pain and reduce localized inflammation in the applied area by reducing prostaglandin production. 
• menthol: menthol is a naturally occurring compound derived from mint oils. It acts as a topical analgesic and counterirritant. menthol generally produces a cooling sensation by stimulating the skin’s cold receptors (TRPM8 receptors), leading to a temporary numbing effect and relief. This cooling sensation helps distract from underlying pain and also provides soothing effect on the skin. menthol also has mild local anesthetic properties, contributing to its pain-relieving effects. 

When methylsalicylate and menthol are combined in topical formulations, they can provide a synergistic effect. methylsalicylate targets pain and inflammation at a deeper level, while menthol provides a cooling and numbing sensation on the skin’s surface. This combined action helps provide a broader spectrum of relief for musculoskeletal conditions. 

Pharmacodynamics: 

Mechanism of action: The action of methylsalicylate and menthol in topical products involves their effects on sensory receptors and signaling pathways, leading to pain relief and a cooling sensation. 

Additionally, methylsalicylate may also affect sensory nerve endings by inhibiting the generation and conduction of nerve impulses. This can contribute to the localized analgesic effect observed with its use. 

Furthermore, menthol has been shown to modulate other sensory receptors, such as kappa-opioid receptors and voltage-gated sodium channels, which might contribute to its analgesic properties. These interactions can alter neuronal signaling and dampen pain transmission. 

When methylsalicylate and menthol are combined in topical formulations, they work synergistically to provide a broader spectrum of relief. methylsalicylate targets pain and inflammation at a deeper level, while menthol provides a cooling and numbing sensation on the skin’s surface. 

Pharmacokinetics: 

Absorption 

Both methylsalicylate and menthol can penetrate the skin and be absorbed into the underlying tissues. The absorption rate can be influenced by factors such as the concentration and formulation of the topical product, the surface area of application, the integrity of the skin (e.g., intact or damaged), and the duration of contact. Absorption of these compounds through the skin is generally considered relatively low. Still, it can be increased if the product is applied to maximum areas of the body, areas with thin skin, or areas with compromised skin. 

Distribution 

After absorption, methylsalicylate and menthol can distribute to various tissues in the body. However, their distribution is primarily localized to the site of application and the surrounding tissues. methylsalicylate may also exhibit some systemic distribution after absorption but at lower levels than oral administration of salicylates. 

Metabolism 

methylsalicylate is metabolized primarily in the liver through processes such as hydrolysis and conjugation. It undergoes ester hydrolysis to form salicylic acid, which is metabolized by conjugation with glycine or glucuronic acid to form water-soluble metabolites eliminated from the body. The metabolism of menthol, on the other hand, primarily occurs in the liver through oxidation and glucuronidation pathways. 

Elimination and Excretion 

The metabolites of methylsalicylate and menthol are excreted primarily in the urine. After metabolism, the water-soluble metabolites of methylsalicylate, such as salicylic acid conjugates, are eliminated through renal excretion. menthol and its metabolites, including glucuronide conjugates, are also excreted in the urine. 

Adminstartion

Administration: 

Topical administration 

When using methylsalicylate/menthol topical products, it is crucial to follow the specific instructions provided by the product manufacturer. Some general guidelines for the administration of these topical products: 

• Clean the affected area: Prior to applying the product, delicately cleanse it using mild soap and water, then pat it dry with clean towel. 
• Apply a thin layer: Take a small amount of the methylsalicylate/menthol topical product and apply it to the affected area. Use your fingertips or a clean applicator to spread the product evenly into thin layer. Avoid excessive application, as a little goes a long way. 
• Massage into the skin: Gently massage the product into the skin using circular motion till it is absorbed. This can help enhance the penetration of the active ingredients and promote better absorption. 
• Wash hands after application: After applying the product, wash your hands to remove any residue. This will prevent accidental contact with sensitive areas or transferring the product to other surfaces. 
• Follow recommended frequency and duration: Pay attention to the product instructions regarding the recommended frequency and duration of use. Some products may recommend applying it multiple times a day, while others may specify a maximum number of applications per day or a specific duration of use. Adhere to these guidelines to ensure safe and effective use. 
• Store properly: Store the methylsalicylate/menthol topical product according to the instructions, typically at room temperature and away from direct sunlight/excessive heat. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: methylsalicylate/menthol topical 

Why do we use methylsalicylate/menthol topical? 

methylsalicylate/menthol topical products are commonly used for various purposes due to their analgesic and soothing properties. Here are some common uses: 

• Pain relief: These topical products are often used to temporarily relieve muscle and joint pain, including arthritis, strains, sprains, and minor sports injuries. They can help alleviate discomfort and reduce localized pain. 
• Muscular aches and tension: methylsalicylate/menthol topicals can soothe muscular aches, stiffness, and tension. They are commonly applied to the back, neck, shoulders, and legs to provide a cooling and analgesic effect. 
• Sports-related injuries: These products are frequently used by athletes and individuals participating in physical activities to manage pain associated with sports-related injuries, such as muscle strains, ligament sprains, and bruises. 
• Overuse injuries: methylsalicylate/menthol topicals may benefit from overuse injuries, like repetitive strain injuries (RSI) or tendonitis. They can help diminish pain and inflammation in affected areas. 
• Post-workout recovery: These topicals can provide a soothing and cooling sensation to fatigued muscles after intense physical activity or exercise. They may aid in relieving muscle soreness and promoting recovery. 
• Minor cuts and insect bites: methylsalicylate/menthol topicals may help relieve itching and provide a soothing effect on minor cuts, scrapes, and insect bites. However, ensuring the skin is not broken or irritated before applying the product is crucial.