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 of migraine, is currently available as subcutaneous injection and oral tablets. Rectal or intranasal formulations may offer advantages over those marketed. This study compared the pharmacokinetics of sumatriptan via all four routes. Usual absorption parameters were described and the rate of absorption was assessed using deconvolution technics. There were no statistical differences between the non-parenteral routes for tmax or Cmax/AUCinfinity. However, Cmax and AUCtmax were statistically greater with the suppository than with the tablet, but there was no difference between intranasal and oral routes. The highest rate of absorption occurred earlier with the intranasal than with the oral route. Relative to the subcutaneous route, the bioavailability for the 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.
Duquesnoy
C
C
Department of Clinical Pharmacology, Laboratoire Glaxo Wellcome, 20, rue Rouget de Lisle, 92442 Issy les Moulineaux Cedex, France.
Mamet
J P
JP
Sumner
D
D
Fuseau
E
E
D000281:Administration, Intranasal; D000284:Administration, Oral; D000285:Administration, Rectal; D000328:Adult; D019540:Area Under Curve; D018592:Cross-Over Studies; D004333:Drug Administration Routes; D006207:Half-Life; D006801:Humans; D007279:Injections, Subcutaneous; D008657:Metabolic Clearance Rate; D008875:Middle Aged; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D018170:Sumatriptan / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014662:Vasoconstrictor Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*
D017366:Serotonin Receptor Agonists; D014662:Vasoconstrictor Agents; D018170:Sumatriptan