chloroxylenol

Action and Spectrum

Actions and Spectrum: 

Actions: 

Para-chloro-meta-xylenol (PCMX), often known as chloroxylenol, is an antiseptic and disinfectant used to clean surgical tools and skin. It can be found in household antiseptics, antibacterial soaps, and products for cleaning wounds. Because halophenol is phenolic, it has been demonstrated to work best against Gram-positive bacteria by disrupting their cell walls. 

Spectrum: 

Chloroxylenol, a substituted phenol, has been extensively utilized for an extended period as a component in antiseptic and disinfectant products designed for external application. It is recognized for its bactericidal properties at low concentrations against a broad spectrum of both Gram-positive and Gram-negative bacteria. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Angioedema 

Breathing difficulty 

Hives 

Itching 

Fever 

Dryness 

Irritation 

Rash 

Thinning of skin 

Black Box Warning

Black Box Warning: 

Exercise caution when using chloroxylenol in patients with any allergies, particularly drug allergies, infections, or chronic and prolonged ear infections (e.g., chronic otitis media).

This medication should be employed only when deemed necessary during pregnancy or lactation. Prolonged use of this drug over months may necessitate temporary supplementation with corticosteroids (e.g., hydrocortisone) during periods of severe stress, such as major surgery, serious injury, or critical infections. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 

Cautions 

• Ear infection 
• Meningitis 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

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: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

Chloroxylenol is a chemical compound renowned for its antimicrobial properties, employed to control algae, bacteria, and fungi in emulsions, adhesives, wash tanks, and paints. The disruption of cell membrane potentials is responsible for its antibacterial effect. 

Pharmacodynamics: 

Functioning as a phenol antiseptic, chloroxylenol is thought to operate by binding its hydroxyl (-OH) groups to specific proteins on the bacterial cell membrane, causing disruption and subsequent leakage of the cell contents. This initial breach enables chloroxylenol to penetrate the bacterial cell, where it further binds with proteins and enzymes, incapacitating the cell’s normal functioning. At elevated concentrations of chloroxylenol, the targeted bacterial cells experience coagulation of proteins and nucleic acids, resulting in a cessation of function and ultimately leading to swift cell death. 

Pharmacokinetics: 

Absorption 

No measurable concentrations of chloroxylenol were detected in the bloodstream after the dermal application of 2 g of p-chloroxylenol in an ethanol/olive oil vehicle in human subjects. At a 5 g dose, only minimal traces were discerned. Following an 8 g dose, 1 mg % (1 mg/dL) was evident in the blood after 3 hours and 4 mg % (4 mg/dL) after 24 hours. With a 20 g dose, 4 mg % (4 mg/dL) was recorded after half an hour, and 1 mg % (1 mg/dL) persisted at 72 hours. 

Concerning its application for antiseptic purposes, chloroxylenol is acknowledged to be effectively absorbed when administered to the skin. 

Distribution 

The sole available data on the volume of distribution for chloroxylenol pertains to the mean Vss of 22.45 L, which was established after administering a 200 mg intravenous single dose of chloroxylenol to healthy mongrel dog subjects. 

Regarding protein binding, a study indicated that chloroxylenol exhibits approximately 85.2% +/- 2.32% binding to serum albumin and 89.8% +/- 2.99% binding to whole human serum. 

Metabolism  

Certain studies in animals have indicated that after the dermal application of chloroxylenol, absorption occurs rapidly, reaching a Cmax within 1-2 hours. The administered substance is then predominantly excreted via the kidneys, with nearly complete elimination observed within 24 hours.

The primary metabolites identified in the excreted urine include glucuronides and sulfates. Some chloroxylenol monographs draw parallels between its pharmacokinetic profile and that of another antiseptic, triclosan, which is also rapidly excreted in the urine, primarily as a glucuronide metabolite, as observed in human models. 

Furthermore, in a single human subject administered 5 mg intragluteally, approximately 14% was excreted with glucuronic acid and 17% with sulfuric acid at the 3-day mark. 

Any chloroxylenol that enters the body is likely extensively metabolized by the liver and promptly excreted, primarily in the urine, in the form of sulfate and glucuronide conjugates. 

Elimination and Excretion 

The primary route of excretion is anticipated to be through urine, although there may be detectable amounts of bile and traces in exhaled air. Regarding half-life, one study approximated the mean terminal half-life and mean residence time after administering a 200 mg intravenous single dose of chloroxylenol to healthy mongrel dog subjects to be 1.7 and 1.69 hours, respectively.

Conversely, certain product monographs draw a comparison between chloroxylenol and a similar liquid antiseptic, triclosan, with the calculated urinary excretion half-life in humans estimated to be approximately 10 hours. 

Adminstartion

Administration: 

Chloroxylenol can be administered through diverse routes depending on its intended application and formulation. The following are standard methods of administration: 

1. Topical Application: Chloroxylenol is frequently featured as an active component in topical products like soaps, hand washes, and skin cleansers, directly applied to the skin for its antiseptic properties. 
2. Dermal Application: In specific scenarios, chloroxylenol may be directly applied to the skin or affected areas for targeted dermatological purposes. 
3. Intravenous Administration: In research or medical contexts, chloroxylenol can be delivered intravenously, entering directly into the bloodstream. 
4. Inhalation: Some formulations incorporate chloroxylenol into products designed for inhalation, such as vaporized or aerosolized solutions. 
5. Ingestion: In particular formulations, chloroxylenol may be employed in products intended for oral use, such as mouthwashes or oral antiseptic solutions. 

It’s paramount to recognize that the chosen mode of administration is contingent on the product’s intended function and formulation. Always adhere to the recommended guidelines and instructions provided by healthcare professionals or product labels to ensure secure and practical usage. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: chloroxylenol 

Pronounced: klaw-roh-zai-luh-nawl 

Why do we use chloroxylenol? 

Chloroxylenol is valued for its antimicrobial attributes and finds widespread use as an antiseptic and disinfectant in various products like soaps, hand washes, and household cleaning agents.  As an antibacterial and antiseptic hand cleaner, chloroxylenol is used to treat cuts, bites, stings, and abrasions. 

The primary rationales for utilizing chloroxylenol encompass the following: 

Antimicrobial Action: Demonstrating potent antimicrobial properties, chloroxylenol is particularly effective against bacteria and fungi. Its role in eliminating or controlling the growth of these microorganisms makes it well-suited for incorporation into hygiene and sanitation products. 

Skin Disinfection: Found in personal care items such as soaps and hand washes, chloroxylenol serves to disinfect the skin. This contribution aids in diminishing the risk of infections by impeding the proliferation of bacteria. 

Wound Care: In certain wound care products, chloroxylenol is included to thwart infections in minor cuts, scrapes, and wounds. Its antiseptic characteristics play a role in maintaining cleanliness in the affected area. 

Surface Disinfection: In household and industrial cleaning formulations, chloroxylenol is integrated for its disinfecting prowess. It proves effective in eradicating bacteria and other microbes on surfaces, fostering a hygienic environment. 

Infection Prevention: Chloroxylenol is enlisted in healthcare settings for disinfecting surfaces and equipment, playing a crucial role in averting the spread of infections in hospitals and clinics.