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Abstract
1. Sensitive methods were developed for identification of the antihypertensive agent guanoxan (2-guanidinomethyl-1,4-benzodioxan) and some possible metabolites, and for the quantitative determination of guanoxan and 6- or 7-hydroxyguanoxan extracted from biological media.
2. Urine from a number of hypertensive patients and from a normal human subject receiving oral guanoxan (20 to 200 mg daily) contained non-conjugated 6- or 7-hydroxyguanoxan in amounts ranging from 11.7% to over 50% of the daily amount taken. This represented the main mode of clearance of the drug.
3. Faeces from these patients and the normal human subject contained only low levels of both guanoxan and 6- or 7-hydroxyguanoxan.
4. No metabolite of guanoxan other than 6- or 7-hydroxyguanoxan and no conjugate of either compound was detected in human excreta.
5. Following oral administration, guanoxan was rapidly and extensively absorbed and subject to aromatic hydroxylation in man.