Abstract
Objective: The concentration-time profiles of specific metabolites of moxisylyte, an α-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 desacetyl-moxisylyte (DAM), DAM glucuronide, and DAM and monodesmethylated DAM (MDAM) sulphates were found in plasma and urine. For all metabolites, t1/2 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). Cmax 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.
Conclusion: The pharmacokinetics of moxisylyte in humans following intracavernous administration were linear in the dose range 10 to 30 mg.
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References
Krane RJ, Goldstein I, Saenz de Tejada I (1989) Medical progress. Impotence. N Engl J Med 321:1649–1659
Feldman HA, Goldstein I, Hatzichristou DG, Krane RJ, McKinlay JB (1994) Impotence and its medical and psychosocial correlates: results of the Massachusetts male aging study. J Urol 151:54–61
Costa P, Soulie-Vassal ML, Sarrazin B, Rebillard X, Navratil H, Bali JP (1993) Adrenergic receptors on smooth muscle cells isolated from human penile corpus cavernosum. J Urol 150:859–863
Buvat J, Lemaire A, Buvat-Herbaut M, Marcolin G (1989) Safety of intracavernous injections using an alpha-blocking agent J Urol 141:1364–1367
Buvat J, Buvat-Herbaut M, Lemaire A, Marcolin G (1991) Reduced rate of fibrotic nodules of the cavernous bodies following auto-intracavernous injection of moxisylyte compared to papaverine. Int J Impotence Res 3:123–128
Costa P, Sarrazin B, Bressolle F, Colson MH, Bondil P, Saudubray F (1993) Efficiency and side-effects of intracavernous injections of moxisylyte in impotent patients: a dose-finding study versus placebo. J Urol 149:301–305
Costa P, Bressolle F, Bromet-Petit M, Mosser J, Sarrazin B (1992) Pharmacokinetics of moxisylyte in healthy volunteers after intravenous and oral administration. J Pharm Sci 81:1223–1225
Costa P, Bressolle F, Sarrazin B, Mosser J, Galtier M (1993) Pharmacokinetics of moxisylyte in healthy volunteers after intravenous and intracavernous administration. J Pharm Sci 82:729–733
Costa P, Bressolle F, Sarrazin B, Mottet N, Rouzier-Panis R, Navratil H, Marquer C (1996) Pharmacokinetics of moxisylyte after intravenous and intracavernous administration. Interest to place a tourniquet. Ther Drug Monit (in press)
Costa P, Bressolle F, Sarrazin B, Mosser J, Navratil H, Galtier M (1992) Moxisylyte plasma kinetics in humans after intracavernous administration. Biopharm Drug Disposit 13:671–679
Costa P, Bressolle F, Jarroux E, Sarrazin B, Mosser J, Navratil H, Galtier M (1993) Multiple-dose pharmacokinetics of moxisylyte after oral administration to healthy volunteers. J Pharm Sci 82:968–971
Marquer C, Trouvin JH, Lacolle JY, Dupont Ch, Jacquot C (1991) Pharmacokinetics of a prodrug thymoxamine: dose-dependence of the metabolite ratio in healthy subjects. Eur J Drug Metab Pharmacokinet 16:183–188
Vollmer KO, Poisson A (1985) Metabolism of thymoxamine. I: Studies with 14C-thymoxamine in man. Eur J Drug Metab Pharmacokinet 10:71–76
Duchene P, Bernouillet C, Bromet-Petit M, Mosser J, Feniou C, Gaudin D, Virelizier H (1988) Metabolism of 14C-thymoxamine in rat and man. Xenobiotica 18:919–928
Gomeni C, Gomeni R (1987) SIPHAR: An integrated computer system for statistical and pharmacokinetic data analysis. In: Serio A, O'Moore R, Tardini A, Roger FH, eds. Proceedings of the 7th International Congress of Medical Informatics. Rome: European Federation for Medical Informatics, pp 507–516
Taburet AM, Steimer JL, Doucet D, Singlas E (1986) Le temps de présence moyen dans l'organisme: un nouveau paramètre pharmacocinétique. Thérapie 41:1–10
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Bressolle, F., Costa, P., Rouzier-Panis, R. et al. Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses. Eur J Clin Pharmacol 49, 411–415 (1996). https://doi.org/10.1007/BF00203788
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DOI: https://doi.org/10.1007/BF00203788