benzocaine/menthol oropharyngeal

Action and Spectrum

Actions and Spectrum 

Action benzocaine: benzocaine, a member of the ester local anesthetic class, exerts its action by reversibly binding to sodium channels in nerve membranes. This binding impedes the initiation and conduction of nerve impulses, leading to a temporary loss of sensation in the affected area. By blocking pain signals, benzocaine provides local anesthesia, thereby relieving or reducing discomfort in the oropharyngeal region. 

Action menthol:  acts as an analgesic by activating specific cold-sensitive receptors, particularly the transient receptor potential melastatin 8 (TRPM8) ion channels. This activation induces a cooling and numbing sensation on the mucous membranes, which helps alleviate pain and soothe irritation in the oropharyngeal area.

Spectrum: benzocaine/menthol oropharyngeal demonstrates a broad spectrum of activity, primarily targeting conditions affecting the oropharyngeal region, including but not limited  

Sore Throat: benzocaine/menthol oropharyngeal provides temporary relief from sore throat symptoms. The local anesthetic properties of benzocaine help numb the affected area, reducing pain and discomfort. Additionally, the cooling effect of menthol contributes to a soothing sensation. 

Canker Sores: The application of benzocaine/menthol oropharyngeal can assist in alleviating the pain associated with canker sores. By providing localized anesthesia, benzocaine reduces discomfort and facilitates the healing process. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Black Box Warning

Black Box Warning:  

None  

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: The drug should not be used in individuals with a known hypersensitivity or allergic reaction to benzocaine, menthol, or any inactive ingredients in the formulation. 

Methemoglobinemia: benzocaine has been reported to cause methemoglobinemia, a rare but potentially serious condition characterized by an abnormal increase in the level of methemoglobin in the blood.  

Children under 2 years of age: The use of this drug in children under 2 years is contraindicated due to the potential risk of developing methemoglobinemia, which can be life-threatening in this age group. 

Concurrent use of other local anesthetics: Simultaneous use of multiple local anesthetics may increase the risk of systemic toxicity. Caution should be exercised when using benzocaine/menthol oropharyngeal in conjunction with other local anesthetic products. 

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:  

benzocaine/menthol oropharyngeal solution is a pharmaceutical formulation used to temporarily relieve minor sore throat and mouth pain. It combines the local anesthetic benzocaine with the cooling agent menthol to provide a dual mechanism of action. 

Pharmacodynamics:  

benzocaine/menthol oropharyngeal solution exerts its analgesic effects through two distinct mechanisms. as a local anesthetic, benzocaine inhibits nerve impulses’ initiation and conduction by blocking voltage-gated sodium channels By doing so, it reduces the generation and transmission of pain signals from the oropharyngeal region to the central nervous system.   

Pharmacokinetics: 

Absorption  

The absorption of benzocaine is primarily influenced by factors such as concentration, surface area, and contact time. menthol, on the other hand, has limited systemic absorption due to its relatively high molecular weight and hydrophilic nature.  

Distribution 

benzocaine undergoes systemic distribution primarily through passive diffusion. The distribution of benzocaine throughout the body is limited due to its high degree of protein binding. menthol, being less systemically available, exhibits limited distribution beyond the site of application. 

Metabolism 

benzocaine is primarily metabolized in the liver through the process of ester hydrolysis by carboxylesterases, yielding the metabolites PABA (p-aminobenzoic acid) and PAG (p-aminobenzoic acid glucoside). menthol, being a naturally occurring compound, undergoes minimal metabolism and is primarily excreted unchanged. 

Excretion and Elimination 

benzocaine and its metabolites are primarily eliminated through renal excretion. The unchanged benzocaine accounts for a small proportion of the total elimination, with the majority being attributed to the excretion of its metabolites. menthol, due to its limited systemic absorption, undergoes primarily pulmonary elimination via exhalation. 

Adminstartion

Administration:  

benzocaine/menthol oropharyngeal solution is intended for local application within the oropharyngeal cavity. The solution is typically applied using a suitable applicator, spray, or gargle technique, ensuring that the affected area is adequately covered. It is essential to avoid swallowing or ingesting the solution. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: benzocaine/menthol oropharyngeal 

Why do we use benzocaine/menthol oropharyngeal? 

Sore throat: The combination of benzocaine and menthol provides local anesthesia and cooling effects, offering temporary relief from pain and discomfort associated with sore throat. 

Throat irritation: benzocaine’s local anesthetic properties help alleviate throat irritation, while menthol’s cooling sensation offers a soothing effect. 

Minor mouth or gum irritation: benzocaine’s topical numbing action can alleviate minor irritations in the mouth or gums, providing temporary relief from pain and discomfort. 

Swallowing difficulties: drug formulation may help reduce discomfort during swallowing by temporarily numbing the oropharyngeal region.