Chloroxylenol + Triclosan

Uses

Chloroxylenol & Triclosan is used for Insect bites, Sunburn, Cuts, Scratches, Abrasions, Disinfection of the skin, Minor burns, Sore lips, Minor skin infections, Chapped roughened hands, Cracked itchy skin

Chloroxylenol + Triclosan is also used to associated treatment for these conditions: Skin Infections, Oral Hygiene, Skin disinfectionAcne, Dental Cavity, Dermabrasion, Gingivitis, Oral Infection, Plaque, Dental, Skin Infections, Bacterial, Abrasions, Minor burns, Antibacterial therapy, Antibiotic pre-surgical prophylaxis

How Chloroxylenol + Triclosan works

As a phenol antiseptic, it is believed that the hydroxyl -OH groups of the chloroxylenol molecule binds to certain proteins on the cell membrane of bacteria, and disrupts the membrane so as to allow the contents of the bacterial cell to leak out . This allows chloroxylenol to enter the bacterial cell to bind further with more proteins and enzymes to disable the cell's functioning . At particularly high concentrations of chloroxylenol, the protein and nucleic acid content of targeted bacterial cells become coagulated and cease to function, leading to rapid cell death .

Triclosan is a biocidal compound with multiple targets in the cytoplasm and membrane. At lower concentrations, however, triclosan appears bacteriostatic and is seen to target bacteria mainly by inhibiting fatty acid synthesis. Triclosan binds to enoyl-acyl carrier protein reductase enzyme (ENR). This complex has increased affinity for NAD+ and forms a ternary complex. This complex is unable to participate in fatty acid synthesis, weakening the cell membrane and causing cell death. Humans do not have an ENR enzyme, and thus are not affected.

Dosage

Chloroxylenol + Triclosan dosage

Adults and children 2 years of age and older: apply to the affected area no more than 3 to 4 times daily.

children under 2 years of age: consult a doctor

Side Effects

Skin sensitivity; irritation of conjunctiva, mucosal irritation; reversible brown staining of the teeth; tongue discoloration and burning sensation; transient taste disturbance; parotid gland swelling.

Toxicity

As chloroxylenol is predominantly employed as an active ingredient in various liquids or creams as cleaners, disinfectants, or antiseptics that are generally designed to be used topically, it is widely accepted that the use of such liquids - when used appropriately - is unlikely to present a sufficient volume that could be ingested to cause any medical problems . In the event of accidental eye contact, was with Luke warm water .

Chloroxylenol is known to have a low systemic toxicity, even at dosage levels many times higher that those likely to be absorbed during normal usage of the agent .

Oral LD50, Rat: 3700 mg/kg; Dermal LD50, Rabbit: 9300 mg/kg

Precaution

Condition worsens or symptoms persist for more than 7 days or clear up and occur again within a few days

Interaction

There are no known drug interactions and none well documented.

Volume of Distribution

The only data available regarding the volume of distribution of chloroxylenol is the mean Vss of 22.45 L determined after 200 mg intravenous single dose of chloroxylenol was administered to healthy mongrel dog subjects .

Elimination Route

No chloroxylenol was detected in the blood following the dermal administration of 2 g of p-chloroxylenol in an ethanol/olive oil vehicle in human subjects . After a dose of 5 g, only traces were found, after 8 g, 1 mg % (1 mg/dL) was found in the blood after 3 hours, and 4 mg % (4 mg/dL) after 24 hours . After a dose of 20 g, 4 mg % (4 mg/dL) was measured after half an hour, and 1 mg % (1 mg/dL) was present at 72 hours .

For antiseptic purposes, chloroxylenol is considered to be well-absorbed when applied to the skin .

A study conducted in 2000 demonstrated that low amounts of triclosan can be absorbed through skin and can enter the bloodstream. [PMID: 10722890] Triclosan is rapidly absorbed and distributed in the human body (Sandborgh-Englund et al., 2006). Maximum concentrations are reached within three hours after oral intake. However, the metabolism and excretion of the compound is fast.

Half Life

One study estimated the mean terminal half-life and mean residence time after a 200 mg intravenous single dose of chloroxylenol in healthy mongrel dog subjects to be 1.7 and 1.69 hours, respectively . Alternatively, some product monographs liken chloroxylenol to a similar liquid antiseptic, triclosan, whose calculated urinary excretion half-life in man is approximately 10 hours .

The terminal plasma half life of triclosan is 21 h (Sandborgh-Englund et al., 2006).

Clearance

The only data available regarding the clearance of chloroxylenol is the mean clearance rate of 13.76 L/hr following a 200 mg intravenous single dose of the substance into healthy mongrel dog subjects .

Moreover, in another study, when 8 g of chloroxylenol was administered dermal on a human subject in an alcohol/glycerin vehicle, 11% was excreted in 48 hours .

Elimination Route

The major route of excretion is likely in urine , although some amounts may be found in bile and traces in exhaled air .

In one study, after in vivo topical application of a 64.5mM alcoholic solution of [(3)H]triclosan to rat skin, 12% radioactivity was recovered in the faeces, 8% in the carcass 1% in the urine, 30% in the stratum corneum and 26% was rinsed from the skin surface at 24 hours after application. [PMID: 10722890]

Pregnancy & Breastfeeding use

Pregnancy Category: Not Classified

FDA has not yet classified the drug into a specified pregnancy category.

Contraindication

Hypersensitivity

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