Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses

✍ Scribed by F. Bressolle; P. Costa; R. Rouzier-Panis; C. Marquer

• Publisher: Springer
• Year: 1996
• Tongue: English
• Weight: 390 KB
• Volume: 49
• Category: Article
• ISSN: 0031-6970
• DOI: 10.1007/bf00203788

✦ Synopsis

Objective: The concentration-time profiles of specific metabolites of moxisylyte, an ~-adrenoceptor blocking agent, in the plasma and urine from 18 healthy volunteers were investigated after intracavernous (IC) administrations at three dose levels (10, 20 and 30 mg). Results: Four metabolites, unconjugated desacetylmoxisylyte (DAM), DAM glucuronide, and DAM and monodesmethylated DAM (MDAM) sulphates were found in plasma and urine. For all metabolites, tl/2 elimination was independent of the administered dose (1.19 h for unconjugated DAM; 1.51 h for DAM glucuronide; 1.51 h for DAM sulphate; and 2.17 h for MDAM sulphate). Cm~x and AUC increased in direct proportion to dose, except for the inactive DAM glucuronide. Any the differences detected were small and equivalence of the three doses can be accepted. Conchtsion: The pharmacokinetics of moxisylyte in humans following intracavernous administration were linear in the dos;e range 10 to 30 mg.