COMPARATIVE CLINICAL PHARMACOKINETICS OF SINGLE DOSES OF SUMATRIPTAN FOLLOWING SUBCUTANEOUS, ORAL, RECTAL AND INTRANASAL ADMINISTRATION

Sumatriptan, a 5-HT1 receptor agonist active for the acute treatment o f migraine, is currently available as subcutaneous injection and oral tablets. Rectal or intranasal formulations may offer advantages over t hose marketed. This study compared the pharmacokinetics of sumatriptan via all four routes. Usual absorption parameters were described and t he rate of absorption was assessed using deconvolution technics. There were no statistical differences between the non-parenteral routes for t(max) or C-max/AUC(infinity). However, C-max and AUC(tmax) were stat istically greater with the suppository than with the tablet, but there was no difference between intranasal and oral routes. The highest rat e of absorption occurred earlier with the intranasal than with the ora l route. Relative to the subcutaneous route, the bioavailability for t he suppository was greater than for intranasal spray and oral tablet. The amount of sumatriptan excreted in the urine unchanged was similar for all routes. Sumatriptan in this study was well tolerated. (C) 1998 Elsevier Science BV.