Peringatan Keamanan

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 L1992. In the event of accidental eye contact, was with Luke warm water L1992.

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 L1999.

Chloroxylenol

DB11121

small molecule approved

Deskripsi

Chloroxylenol, or para-chloro-meta-xylenol (PCMX), is an antiseptic and disinfectant agent used for skin disinfection and surgical instruments. It is found in antibacterial soaps, wound-cleansing applications, and household antiseptics. The halophenol is shown to be most effective against Gram positive bacteria where it disrupts the cell wall due to its phenolic nature A1351. Chloroxylenol is on the World Health Organization's List of Essential Medicines.

Struktur Molekul 2D

Berat 156.61
Wujud liquid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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 [L1989, L1993]. Alternatively, some product monographs liken chloroxylenol to a similar liquid antiseptic, triclosan, whose calculated urinary excretion half-life in man is approximately 10 hours [L1992].
Volume Distribusi 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 [L1989, L1993].
Klirens (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 [L1989, L1993]. 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 [A32350].

Absorpsi

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 A32349. 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 A32349. 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 A32349. For antiseptic purposes, chloroxylenol is considered to be well-absorbed when applied to the skin L1999.

Metabolisme

Certain animal studies have shown that following dermal application of chloroxylenol, that the absorption was rapid with a Cmax = 1-2 hours, and that the administered substance was excreted via the kidney with almost complete elimination within 24 hours L1992. The primary metabolites discovered in the excreted urine were glucuronides and sulfates L1992. Some chloroxylenol monographs liken its pharmacokinetic profile to that of another antiseptic - triclosan - which is rapidly excreted in the urine also as a glucuronide metabolite, as observed in the human model L1992. Moreover, In one human subject administered 5 mg intragluteally, 14% was excreted with glucuronic acid and 17% with sulfuric acid at 3 days A32350. Any chloroxylenol absorbed into the body is likely extensively metabolized by the liver and rapidly excreted, mainly in the urine, as sulphate and glucuronide conjugates L1999.

Rute Eliminasi

The major route of excretion is likely in urine L1993, L1992, although some amounts may be found in bile and traces in exhaled air L1989.

Interaksi Obat

1 Data
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Chloroxylenol.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9880479
    McDonnell G, Russell AD: Antiseptics and disinfectants: activity, action, and resistance. Clin Microbiol Rev. 1999 Jan;12(1):147-79.
  • PMID: 7143213
    Judis J: Binding of selected phenol derivatives to human serum proteins. J Pharm Sci. 1982 Oct;71(10):1145-7.
  • PMID: 21017619
    ZONDEK B, FINKELSTEIN M: Blood concentration of P-chloro-xylenol in man following parenteral, percutaneous and rectal application. Proc Soc Exp Biol Med. 1946 Feb;61:200-2.
  • PMID: 16747702
    Zondek B, Shapiro B: Fate of halogenated phenols in the organism. Biochem J. 1943;37(5):592-5.

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