Peringatan Keamanan

Data regarding the overdosage and toxicity of anethole trithione (ATT) is not readily accessible. Nevertheless, some common side effects associated with taking ATT include softening of stool and/or discoloration of the urine to a bright yellow L2377.

Anethole trithione

DB13853

small molecule approved experimental

Deskripsi

Anethole trithione (ATT) appears to have a broad range of unique functions, from increasing salivary secretion to help treat xerostomia A27165, A32618, A32620, A32621, to demonstrating an ability to inhibit carcinogenesis by increasing the activity of electrophile detoxification enzymes A32619, and even being used as an adjunctive therapy for cholecystitis, gallstone, indigestion, and acute/chronic hepatitis L2388 and is marketed in certain countries like France, Germany, and China A32614.

Unfortunately, many of the specific mechanisms of action to these activities have yet to be formally elucidated, which means that while studies are ongoing, ATT itself is not necessarily formally indicated for many of these aforementioned functions at this time and is only used in limited regions around the world.

Struktur Molekul 2D

Berat 240.35
Wujud -

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Despite the medication being studied and discussed as early as the 1980s, detailed pharmacokinetic information about it is not readily accessible and limited new pharmacokinetic data has only been determined for the drug for the first time only very recently (as recently as 2007) [A32615]. Consequently, after anethole trithione was administered to twenty-two healthy Chinese volunteers, the half-life observed was about 3.78 +/- 2.12 hours [A32615].
Volume Distribusi Despite the medication being studied and discussed as early as the 1980s, detailed pharmacokinetic information about it is not readily accessible and limited new pharmacokinetic data has only been determined for the drug for the first time only very recently (as recently as 2007) [A32615]. Nevertheless, the poor absorption and bioavailability of anethole trithione suggests any kind of volume of distribution measurement may not be entirely accurate.
Klirens (Clearance) Despite the medication being studied and discussed as early as the 1980s, detailed pharmacokinetic information about it is not readily accessible and limited new pharmacokinetic data has only been determined for the drug for the first time only very recently (as recently as 2007) [A32615]. Regardless, data about the estimated clearance of anethole trithione in the rat model after administration of anethole trithione oral aqueous suspension was observed to be approximately 113.20 +/- 52.37 L/h/kg [A32614].

Absorpsi

Although anethole trithione (ATT) has a high lipophilicity (log P = 3.8) and a high intestinal permeability, it has an extremely low water solubility (0.38 ug/ml). This low solubility limits ATT dissolution and bioavailability A32614, A32616. Regardless, after ATT was administered to twenty-two healthy Chinese volunteers, the Cmax observed was about 0.98 +/- 0.49 ng/mL and the recorded Tmax was 2.2 +/- 1.9 h A32615.

Metabolisme

Anethole trithione (ATT) is metabolized rapidly into 4-hydroxy-anethole trithione via O-demethylation A32614, A32616. This metabolite demonstrates similar pharmacological activities to its parent, ATT A32614, A32616. It is proposed that such metabolism occurs in liver microsomes, although neither this proposal or by what specific hepatic cytochrome P450 isoform(s) are involved in such metabolism has been formally elucidated A32614.

Rute Eliminasi

Despite the medication being studied and discussed as early as the 1980s, detailed pharmacokinetic information about it is not readily accessible and limited new pharmacokinetic data has only been determined for the drug for the first time only very recently (as recently as 2007) A32615.

Interaksi Makanan

1 Data
  • 1. Take before a meal.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Protein-glutamine gamma-glutamyltransferase 2 TGM2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10487404
    Hamada T, Nakane T, Kimura T, Arisawa K, Yoneda K, Yamamoto T, Osaki T: Treatment of xerostomia with the bile secretion-stimulating drug anethole trithione: a clinical trial. Am J Med Sci. 1999 Sep;318(3):146-51.
  • PMID: 21766311
    Yu HZ, Han SF, Li P, Zhu CL, Zhang XX, Gan L, Gan Y: An examination of the potential effect of lipids on the first-pass metabolism of the lipophilic drug anethol trithione. J Pharm Sci. 2011 Nov;100(11):5048-58. doi: 10.1002/jps.22702. Epub 2011 Jul 15.
  • PMID: 17586125
    Li T, Zhang Z, Jiao H, Zhang L, Tian Y, Chen Y, Pang X, Zhuang J: Determination of anethole trithione in human plasma using high performance liquid chromatography coupled with tandem mass spectrometric detection. Anal Chim Acta. 2007 Jul 2;594(2):274-8. doi: 10.1016/j.aca.2007.05.038. Epub 2007 May 26.
  • PMID: 19508887
    Han SF, Yao TT, Zhang XX, Gan L, Zhu C, Yu HZ, Gan Y: Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: effects of lipid composition and formulation. Int J Pharm. 2009 Sep 8;379(1):18-24. doi: 10.1016/j.ijpharm.2009.06.001. Epub 2009 Jun 7.
  • PMID: 11804400
    Nagano T, Takeyama M: Enhancement of salivary secretion and neuropeptide (substance P, alpha-calcitonin gene-related peptide) levels in saliva by chronic anethole trithione treatment. J Pharm Pharmacol. 2001 Dec;53(12):1697-702.
  • PMID: 15153695
    Fox PC: Salivary enhancement therapies. Caries Res. 2004 May-Jun;38(3):241-6. doi: 10.1159/000077761.
  • PMID: 8339252
    Reddy BS, Rao CV, Rivenson A, Kelloff G: Chemoprevention of colon carcinogenesis by organosulfur compounds. Cancer Res. 1993 Aug 1;53(15):3493-8.
  • PMID: 25175324
    Anil S, Vellappally S, Hashem M, Preethanath RS, Patil S, Samaranayake LP: Xerostomia in geriatric patients: a burgeoning global concern. J Investig Clin Dent. 2016 Feb;7(1):5-12. doi: 10.1111/jicd.12120. Epub 2014 Sep 1.
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Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Sialor
    Tablet • 25.0 mg • Oral • Canada • Approved
  • Sialor Tab 25mg
    Tablet • 25 mg / tab • Oral • Canada • Approved
  • Sulfarlem Tab 12.5mg
    Tablet • 12.5 mg / tab • Oral • Canada • OTC • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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