dyclonine/menthol

Action and Spectrum

Actions and Spectrum 

Action of dyclonine: 

Local Anesthetic: dyclonine works by inhibiting the conduction of nerve impulses in the affected area, thereby numbing the sensory nerves. It binds to and blocks the voltage-gated sodium channels in the nerve membranes, preventing the influx of sodium ions and subsequent generation of action potentials. This action helps to relieve pain and discomfort locally. 

Action of menthol: 

Cooling Sensation: menthol stimulates the cold-sensitive receptors in the skin and mucous membranes, producing a cooling sensation. It achieves this effect by activating the transient receptor potential (TRPM8) channels responsible for detecting cold temperatures. This cooling sensation can help relieve itching, burning, and discomfort. 

Spectrum: dyclonine and menthol are typically combined in various (OTC) products, such as throat lozenges, sprays, and mouthwashes, to provide temporary relief from throat soreness, irritation, and minor pain. The combination of dyclonine’s local anesthetic action and menthol’s cooling effect offers a dual approach to alleviate discomfort in the affected area. The numbing effect of dyclonine helps to reduce pain, while menthol’s cooling sensation provides a soothing feeling, offering relief to individuals with minor throat and mouth issues. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Black Box Warning

Black Box Warning:  

None  

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity or allergy: Individuals who have known hypersensitivity or allergic reactions to dyclonine, menthol, or any other ingredients in the formulation should avoid using products containing this drug. 

methemoglobinemia: dyclonine has the potential to cause methemoglobinemia, a rare condition where the oxygen-carrying capacity of the blood is reduced. It is recommended to avoid using this drug in individuals with a history of methemoglobinemia or those who are known to have a deficiency of methemoglobin reductase enzyme. 

Severe liver disease: The liver may be responsible for metabolizing some components of the medication, and impaired liver function can affect the clearance and safety of the drug. 

Pregnancy and breast-feeding: limited information on the safety of this drug use during pregnancy and breastfeeding is available. It is recommended to seek guidance from a healthcare provider before utilizing these drugs during pregnancy or while breastfeeding to evaluate the possible advantages and risks involved. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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: dyclonine and menthol are both commonly used as topical analgesics, typically found in over-the-counter products for relief of minor pain and irritation. 

Pharmacodynamics:  

dyclonine is a local anesthetic that blocks nerve signals in the area where it is applied. It acts by inhibiting the influx of sodium ions into nerve cells, preventing the generation and propagation of nerve impulses. This action numbs the area and provides temporary relief from pain and discomfort. 

Conversely, menthol is a naturally occurring compound derived from peppermint or other mint oils. The drug acts by activating certain receptors in the skin called TRPM8 receptors, which are responsible for detecting cold temperatures. Activation of these receptors leads to the sensation of cooling and analgesic effects, providing relief from pain and itching. 

Pharmacokinetics: 

Absorption 

When applied to the mucous membranes, dyclonine is readily absorbed and exerts its local anesthetic effects. menthol can be absorbed through various routes, including topical application, inhalation, and ingestion. When applied topically, it can be absorbed through the skin. When inhaled or ingested, it can be absorbed through the respiratory or gastrointestinal tract. 

Distribution 

menthol is a lipophilic compound, meaning it has an affinity for fat and can distribute into various tissues in the body. menthol’s distribution throughout the body depends on the route of administration and the specific formulation. 

After absorption, dyclonine may distribute throughout the local tissues, primarily targeting the nerves in the area of application. Systemic distribution is minimal due to limited absorption from topical use. 

Metabolism 

dyclonine undergoes minimal metabolism in the body. It is primarily eliminated unchanged, with only a small portion being metabolized by liver enzymes. The exact metabolic pathways and products are not well characterized. menthol is primarily metabolized in the liver by cytochrome P450 enzymes, specifically CYP2A6.  

Excretion and elimination 

The elimination of dyclonine occurs primarily through renal excretion. It is mainly excreted in the urine as unchanged drug or its metabolites. 

The metabolites of menthol are excreted primarily in urine.

Adminstartion

Administration:  

Apply a thin layer: If you use a gel formulation, squeeze a small amount onto your fingertip or a cotton swab. 

 If you are using a spray, hold the can about 6-12 inches away from the affected area and spray a thin layer evenly.  

Rub in gently: After applying the medication, gently rub it into the skin using a circular motion or by patting it in.  

This helps the medication to be absorbed and provide maximum effectiveness. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dyclonine/menthol 

Why do we use dyclonine/menthol?   

dyclonine: dyclonine is a local anesthetic that is commonly used to relieve pain and itching in the mouth and throat. It is often found in over-the-counter products such as lozenges, mouthwashes, and sprays designed to provide temporary relief from sore throat, canker sores, and minor mouth irritations. dyclonine works by blocking nerve signals in the affected area, thereby reducing pain and discomfort.  

menthol- 

Topical Analgesic: drug is a common ingredient in topical analgesic products such as creams, gels, and sprays. It provides a cooling effect and can help alleviate minor aches, muscle soreness, and joint pain.  

Respiratory Relief: drug is often used in cough drops, throat lozenges, and inhalers due to its ability to soothe and numb the throat, providing temporary relief from coughs, throat irritation, and congestion.  

Oral Care: drug is added to toothpaste, mouthwashes, and oral sprays for its refreshing flavor and cooling effect. It can help freshen breath and provide a mild numbing sensation for toothaches or oral discomfort.  

Skin Care: In some skin care products, drug is included for its cooling and soothing properties. It can be found in creams, lotions, and balms to relieve sunburns, insect bites, and minor skin irritations.