Fate of the anthelmintic, phenothiazine, in man.
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.
Mitchell
S C
SC
Biological Chemistry, Division of Biomedical Sciences, Faculty of Medicine, Imperial College, South Kensington, London SW7 2AZ, UK. s.c.mitchell@ic.ac.uk
Kestell
P
P
Steventon
G B
GB
Waring
R H
RH
D000328:Adult; D000981:Antiprotozoal Agents / Q000378:metabolism / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D006801:Humans; D008297:Male; D008956:Models, Chemical; D010640:Phenothiazines / Q000378:metabolism / Q000493:pharmacokinetics*; D013053:Spectrophotometry; D013462:Sulfur Radioisotopes; D013997:Time Factors
D000981:Antiprotozoal Agents; D010640:Phenothiazines; D013462:Sulfur Radioisotopes; C031637:phenothiazine