Sulindac sulphone

Protein Binding. In plasma, sulindac, sulphone, and sulphide, about 95%. 

Sulforal, 992 Sulforidazine, 980 (metabolite), 738, 1020 Sulformethoxine, 978 Sulforthomidine, 978 Sulfotrimin, 988 Sulfuno, 991 Sulginum, 986 Sulindac, 981 Sulindac sulphide, 981 Sulindac sulphone, 981 Sulla, 989 Sulmycin, 637 Sulpha..., see also under Sulphacalyre, 981 Sulphacarbamide, 995 Sulphacetamide, 981 Sulphacetamide sodium, 981 Sulphacetamide, soluble, 981 Sulphachlorpyridazine, 982 Sulphadiazine, 982 Sulphadiazine sodium, 983 Sulphadiazine, soluble, 983 Sulphadimethoxine, 983 Sulphadimethyloxazole, 991 Sulphadimethylpyrimidine, 984... 

While all NSAIDs have the potential for inducing renal failure, there has been speculation of quantitative differences among the individual NSAIDs. Sulindac was thought to be renal sparing, possibly because of its unusual metabolic pathway [29, 77-79]. The parent compound, sulindac sulphoxide, is an inactive prodrug, which undergoes hepatic metabolism to sulindac sulphide, the metabolite responsible for its anti-inflammatory activity. Sulindac sulphoxide is also metabolized to a much lesser extent to an inactive metabolite, sulindac sulphone. It was hypothesized that, within the human kidney, sulindac sulphide was reversibly oxidized to the inactive parent compound, sulindac sulphoxide, with the result that renal prostaglandin production was not perturbed [29, 78]. 

The combined RIA-technique and isotope dilution has been successfully developed to estimate SULINDAC along with its two prominent metabolites, namely its sulphone and its sulphide present in the plasma-level as shown in the following chemical structures X and Y. 

Quantification. High Pressure Liquid Chromatography. In plasma or urine sulindac and its sulphide and sulphone metabolites, sensitivity 100 ng/ml in plasma, UV detection—B. 

Following daily oral doses of 200 mg, twice a day to 12 subjects, mean maximum steady-state plasma concentrations were sulindac S.Opg/ml, sulphide 6.9 ig/ml, sulphone 2.6pg/ml a diurnal variation in plasma concentrations was reported with lower concentrations being attained after the evening dose. After oral administration of 400 mg once daily to 12 subjects, maximum steady-state plasma concentrations were sulindac 8.7 ig/ml, sulphide 8.8 pg/ml, sulphone 3.9 ig/ml (B. N. Swanson et al., Clin. Pharmac. Ther., 1982, 32, 397-403). 

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