menthol topical

Action and Spectrum

Actions and Spectrum: 

Mechanism of Action: 

• Activation of Cold Receptors: menthol activates specific receptors called transient receptor potential cation channel subfamily M member 8 (TRPM8) receptors, primarily responsible for sensing cold temperatures. By stimulating these receptors, menthol produces a cooling sensation on the skin or mucous membranes. 
• Desensitization of Pain Receptors: menthol can also desensitize pain receptors, such as the nociceptors, which are involved in sensing and transmitting pain signals. This desensitization effect may help alleviate pain and provide temporary relief. 

Spectrum of Activity: 

• Analgesic Effect: menthol has analgesic properties and is commonly used to relieve minor aches, pains, and muscle soreness temporarily. It can help alleviate discomfort associated with muscle strains, sprains, arthritis, and bruises. 
• Cooling Sensation: menthol produces a cooling sensation on the skin or mucous membranes, providing relief and freshness. This cooling effect is often used in topical products such as creams, gels, lotions, and ointments. 
• Itching and Irritation Relief: menthol can help relieve itching and minor skin irritations. Its cooling properties can soothe the skin and temporarily relieve itching caused by insect bites, poison ivy, or other irritants. 
• Respiratory relief: menthol is sometimes used in topical preparations for its decongestant properties. When applied near the nasal passages, it can help open the airways and provide relief in cases of nasal congestion or minor respiratory discomfort. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Stinging sensation on skin 

Hypersensitivity reaction 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity or Allergy: Individuals with known hypersensitivity or allergy to menthol or other components of the topical product should avoid its use. Allergic reactions can range from mild skin irritation to more severe reactions, such as rash, itching, swelling, or difficulty breathing. 
• Broken or Damaged Skin: menthol topical preparations should not be applied to open wounds, cuts, burns, or areas of broken or damaged skin. menthol can cause further irritation or increase the risk of absorption into the bloodstream, leading to systemic effects. 
• Asthma or Respiratory Conditions: menthol inhalation or application near the face may trigger respiratory symptoms, particularly in individuals with asthma or other respiratory conditions. It is advisable to avoid applying menthol topical preparations near the nose, mouth, or eyes of individuals with respiratory sensitivities. 
• Children: menthol topical products should be cautiously used in children, particularly infants under two. The cooling sensation of menthol may cause discomfort or skin irritation in young children. It is recommended to consult a healthcare professional before using menthol topical on children. 
• Sensitivity to Cold: Individuals with cold hypersensitivity or disorders such as Raynaud’s disease may be more sensitive to the cooling effects of menthol. menthol can potentially exacerbate symptoms in these individuals and should be used cautiously or avoided. 

Caution: 

• Avoiding Eye Contact: menthol topical products should not encounter the eyes. If accidental eye contact occurs, rinse thoroughly with water and seek medical attention if irritation persists. 
• Sensitive Skin: Individuals with sensitive skin may experience irritation or allergic reactions to menthol topical preparations. To check for any adverse reactions, it is advisable to perform a patch test on a small skin area before widespread use. If skin irritation, redness, itching, or swelling occurs, discontinue use, and consult a healthcare professional. 
• Sensitivity to Cooling Sensation: Some individuals may find the cooling sensation produced by menthol topical preparations uncomfortable or intolerable. If the cooling sensation becomes overwhelming or causes discomfort, it is advisable to discontinue use or consult a healthcare professional. 
• Interaction with Other Topical Preparations: menthol topical preparations may interact with or affect the absorption of other topically applied medications. It is recommended to wait sufficient time between applying different topical products or consult a healthcare professional for guidance on concurrent use. 
• Pregnancy and Breastfeeding: While there is limited research on topical menthol products during pregnancy and breastfeeding, it is generally advisable to consult a healthcare professional before using them to assess the potential risks and benefits. 
• Age Considerations: In young children and infants, menthol topical products should be used with caution and under the guidance of a healthcare professional. menthol can cause discomfort or skin irritation in young children, and their skin may be more sensitive. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

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: 

The key pharmacological aspects of menthol topical: 

• Activation of TRPM8 Receptors: menthol activates the transient receptor potential cation channel subfamily M member 8 (TRPM8) receptors primarily responsible for sensing cold temperatures. By stimulating these receptors, menthol produces a cooling and soothing sensation on the skin or mucous membranes. 
• Modulation of Sensory Perception: menthol can modulate the perception of sensations, including pain, itchiness, and temperature. It can temporarily reduce pain perception by stimulating the TRPM8 receptors and desensitizing the nerve endings responsible for transmitting pain signals. 
• Counterirritant Effect: menthol acts as a counterirritant, providing a cooling or tingling sensation that can distract from underlying pain or discomfort. This counterirritant effect can help alleviate minor aches, muscle soreness, and irritation. 
• Local Vasodilation: menthol can cause local vasodilation, which widens the blood vessels in the application area. This increased blood flow can help reduce inflammation, aid the delivery of nutrients, and remove waste products from the tissues. 
• Antipruritic (Anti-Itching) Effect: menthol has mild antipruritic properties, which can help alleviate itching and relieve minor skin irritations. The menthol’s cooling sensation can help soothe itchiness and reduce the urge to scratch. 

Pharmacodynamics: 

The pharmacodynamic effects of menthol topical are primarily localized to the application site and do not have significant systemic effects. The duration and intensity of the effects may vary depending on the concentration and formulation of the menthol topical product. 

Pharmacokinetics: 

Absorption 

menthol is primarily absorbed through the skin or mucous membranes upon topical application. It has relatively good penetration properties and can readily enter the underlying tissues. However, the extent of absorption can vary depending on factors such as the concentration and formulation of the menthol topical product, the condition of the skin, and the area of application. 

Distribution 

After absorption, menthol is distributed locally in the tissues near the application site. Its distribution is primarily limited to the area where it is applied, and systemic distribution is generally minimal. menthol does not tend to accumulate in specific organs or tissues. 

Metabolism 

menthol undergoes hepatic metabolism in the body. The primary pathway for menthol metabolism is through cytochrome P450 enzymes, specifically CYP2A6. menthol is primarily metabolized to menthol glucuronide and other metabolites. The metabolites are then eliminated from the body through urine and feces. 

Elimination and Excretion 

menthol and its metabolites are eliminated from the body mainly through urine and feces. The elimination half-life of menthol varies depending on various factors, including the dose, route of administration, and individual metabolic differences. 

Adminstartion

Administration: 

• Read the Product Instructions: Carefully read the product label and accompanying instructions provided by the manufacturer. Follow the recommended guidelines and any specific instructions for the menthol topical product you are using. 
• Clean and Dry the Area: Before applying menthol topical, ensure that the application area is clean and dry. Gently wash the area with mild soap and water, and pat it dry with a clean towel. 
• Apply a Thin Layer: Take enough of the menthol topical product and apply it to the affected area. A thin, even layer covering the desired area is generally recommended. Avoid excessive application, as it may not enhance efficacy and can increase the risk of skin irritation. 
• Massage or Rub In: After applying the menthol topical product, gently massage or rub it into the skin in a circular motion until it is absorbed. This can help facilitate its penetration and promote even distribution. 
• Wash Hands: After application, wash your hands thoroughly with soap and water to remove residual products. This will prevent accidental contact with sensitive areas, such as the eyes or mucous membranes. 
• Follow Frequency and Duration: Follow the recommended frequency of application as indicated on the product label or as directed by your healthcare professional. Also, adhere to the recommended duration of use, as prolonged or excessive use may increase the risk of skin irritation. 
• Avoid Covered or Occluded Areas: Some topical menthol products may have occlusive dressings or patches that enhance absorption. If using such products, follow the specific instructions for application and duration. Avoid applying menthol topical to covered or occluded areas unless specifically directed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: menthol topical 

Why do we use menthol topical? 

menthol topical products have a variety of uses and are commonly employed for their cooling and soothing effects on the skin. Here are some common uses of menthol topical: 

• Temporary Relief of Minor Muscle and Joint Pain: menthol topical products are often used to temporarily relieve minor muscle aches, joint pain, and stiffness. The cooling sensation of menthol can help soothe the affected area and alleviate discomfort. 
• Relief of Minor Headaches: when applied to the temples or forehead, menthol topical preparations may temporarily relieve minor headaches. The cooling effect can help ease tension and promote a sense of relaxation. 
• Relief of Sunburn: When applied to sunburned skin, topical menthol products can offer a cooling and soothing sensation. They can help alleviate the discomfort associated with sunburn, such as redness, inflammation, and heat sensation. 
• Relief of Itching and Irritation: menthol topical preparations can relieve itching and minor skin irritations caused by insect bites, poison ivy, rashes, or allergic reactions. The cooling effect can provide temporary relief from itchiness and soothe irritated skin. 
• Relief of Cough and Congestion: topical menthol products, such as chest rubs or inhalation balms, are commonly used to alleviate cough and congestion symptoms. The inhalation of menthol vapors can help provide a sensation of improved airflow and a soothing effect on the respiratory passages. 
• Massage Therapy: menthol topical products are often incorporated into massage oils, lotions, or creams for their cooling and relaxing properties. They can enhance the massage experience and provide a refreshing sensation on the skin.