Peringatan Keamanan

An oral dose of 100-400 mg/kg or a parenteral dose of 5-15 mg/kg is believed to be fatal in humans L1816.

A potential concern for larger concentrations of benzalkonium chloride to possibly cause corneal damage when implemented as an excipient ingredient in aqueous eye products is an issue that should be discussed between potential patents and their health care providers L1816. Since decreased regular blinking and tear generation in patients experiencing dry eyes due to any number of eye conditions can result in reduced dilution of applied eye drops containing the benzalkonium chloride preservative L1816, alternative options including benzalkonium chloride-free products should be considered.

Additionally, benzalkonium chloride has been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy. In addition, benzalkonium chloride may cause eye irritation and is known to discolour soft contact lenses L1816. There may also be the possibility of benzalkonium chloride containing eye drops to cause some stinging and pain L1816.

There is the possibility of ototoxicity occurring when benzalkonium chloride containing ear drops are applied to the ear L1816.

Benzalkonium chloride used as a preservative in nebulised solutions of anti-asthma drugs has been reported to cause dose-related bronchoconstriction especially in asthmatic patients and has been associated with the precipitation of respiratory arrest L1816.

Despite the fairly widespread cutaneous use of benzalkonium chloride, only limited human evidence of sensitization in relatively small populations of individuals have been reported L1816. Nevertheless, the main adverse effect for topical formulations of benzalkonium chloride is usually the warning 'may cause local irritation' L1816.

Benzalkonium

DB11105

small molecule approved investigational

Deskripsi

Benzalkonium is a quaternary ammonium compound used as a biocide, a cationic surfactant, and as a phase transfer agent FDA Label. Benzalkonium is more commonly contained in consumer products in its salt form, benzalkonium chloride FDA Label. This salt is used in a great variety of international pharmaceutical products such as eye, ear, and nasal drops or sprays as an excipient ingredient serving as an antimicrobial preservative FDA Label. When used as an ingredient in antiseptic and disinfectant products however, it is an active antimicrobial agent L1806.

Struktur Molekul 2D

Struktur tidak tersedia

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi When applied as a topical antibacterial, antiseptic, disinfectant, or sanitizer it is believed that molecules of benzalkonium chloride are poorly absorbed (perhaps due to their large, positively charged nature [L1816]), especially considering expectations for such topical applications to keep their biocidal agents available for action at the topical level and to not be absorbed significantly beyond it. When benzalkonium chloride is implemented as an excipient preservative ingredient in various eye, nose, and ear aqueous products, such products will always have other active pharmacological agents whose volume of distribution will be of greater importance. In these cases the excipients will only ever be present at the minimal levels necessary to maintain the integrity of the product substance. Moreover, Benzalkonium chloride is currently listed as a Category III ingredient by the United States Food and Drug Administration [L1826]. Ingredients are listed in the FDA Category III when the data available about them are insufficient to classify as safe and effective, requiring further testing to determine more formal details about elements like human pharmacokinetic studies, and studies on the ingredients' absorption, distribution, metabolism, and excretion.
Klirens (Clearance) -

Absorpsi

Percutaneous absorption is considered to be insignificant L1814. In one study, benzalkonium chloride absorption was evaluated in women using tampons containing the agent. Venous blood samples were drawn 15 minutes before the tampon application and then again at 15 min, 1 h, 3 h, and 24 h after application. Benzalkonium chloride was not detected in any of the blood samples at any time tested. L1814 Similarly, in another study, benzalkonium chloride absorption was tested in women using tampons containing the agent. Venous blood and breast milk samples were taken 15 minutes before application and 3 h and 24 h after tampon administration. Benzalkonium chloride was not found in any of the subjects' samples. L1814. Moreover, in a study where benzalkonium chloride solution was placed on the corneal surface of rabbit subjects, at various intervals after administration, the rabbits' eyes would be washed with 1 mL saline and the following tissues and fluids were removed: bulbar and palpebral conjunctiva, aqueous humour, corneal epithelium, endothelium and stroma, iris-ciliary body, lens, vitreous, retina, and choroid. Plasma samples were obtained with direct cardiac punctures. After administration of one drop, benzalkonium chloride was found in the corneal epithelium, endothelium, and stroma, and in the bulbar and palpebral conjunctivae. Benzalkonium chloride loss from ocular tissues was such that about one-third to two thirds of its concentration (depending on the tissue) at 30 min remained after 24 hr; measurable values existed for as long as 120 hr. The administration of multiple drops led to continued accumulation of benzalkonium chloride. L1814.

Metabolisme

Since benzalkonium chloride is structurally a large, positively charged molecule it is likely poorly absorbed and eliminated largely in faeces, similar to other quaternary ammonium compounds L1816.

Rute Eliminasi

Administered benzalkonium chloride is likely eliminated largely in faeces, similar to other quaternary ammonium compounds L1816.

Interaksi Obat

0 Data
Tidak ada data.

Referensi & Sumber

Artikel (PubMed)
  • PMID: 14999632
    Pankey GA, Sabath LD: Clinical relevance of bacteriostatic versus bactericidal mechanisms of action in the treatment of Gram-positive bacterial infections. Clin Infect Dis. 2004 Mar 15;38(6):864-70. doi: 10.1086/381972. Epub 2004 Mar 1.

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