Fate of the anthelmintic, phenothiazine, in man.

Abstract

1. Radiolabelled [(35)S]-phenothiazine has been administered orally to two healthy adult male volunteers (6 mg kg(-1) body weight). Faeces were the major route of excretion of radioactivity (68%), the remainder being eliminated via the urine (32%) with an estimated urinary half-life (biphasic) of 6-16 h. Over the 5 days of the study a complete recovery of radioactivity was achieved. 2. From urinary data, it was shown that metabolism occurred via ring carbon oxidation to form phenothiazone and thionol and via ring sulphur oxidation to form phenothiazine sulphoxide. The majority of urinary material (92%) was present in the form of conjugates of phenothiazine and phenothiazone. Only unchanged phenothiazine was detected in the faeces. Phenothiazine sulphoxide was reduced to phenothiazine during incubation with faecal homogenates.

• Authors: S C Mitchell, P Kestell, G B Steventon, R H Waring
• Journal: Xenobiotica; the fate of foreign compounds in biological systems (Xenobiotica) Vol. 32 Issue 9 Pg. 771-82 (Sep 2002) ISSN: 0049-8254 [Print] England
• PMID: 12396274 (Publication Type: Journal Article)

Chemical References

• Antiprotozoal Agents
• Phenothiazines
• Sulfur Radioisotopes
• phenothiazine

Topics

• Adult
• Antiprotozoal Agents (metabolism, pharmacokinetics)
• Chromatography, High Pressure Liquid
• Chromatography, Thin Layer
• Humans
• Male
• Models, Chemical
• Phenothiazines (metabolism, pharmacokinetics)
• Spectrophotometry
• Sulfur Radioisotopes
• Time Factors