de Vries M H, Raghoebar M, Mathlener I S, van Harten J
Department of Clinical Pharmacology, Solvay Duphar, B.V., Weesp, The Netherlands.
Ther Drug Monit. 1992 Dec;14(6):493-8. doi: 10.1097/00007691-199212000-00010.
The pharmacokinetics of fluvoxamine maleate was studied in two separate studies in healthy young and elderly subjects. In a single and multiple oral dose administration study, six healthy young subjects received an initial 50 mg oral dose followed by 50 mg tablets every 12 h for 28 days. In a second study, 13 elderly subjects received 50 mg tablets every 12 h for 28 days. Fluvoxamine peak plasma concentrations were reached in approximately 5-6 h following oral administration of single and multiple 50 mg doses to healthy young and elderly volunteers. The area under the curve (AUC) of fluvoxamine tended to be larger following multiple (873 ng.h/ml) as compared to single-dose administration (652 ng.h/ml). Also the terminal half-life after chronic dosing (22 +/- 6 h) tended to be longer than after single dosing. Steady-state plasma levels were obtained within 10 days' administration. The pharmacokinetics of fluvoxamine in elderly healthy subjects were no different from those recorded in young subjects. These results suggest that it is not necessary to adjust the dosage of fluvoxamine in elderly depressed patients, on the basis of pharmacokinetic arguments. Independent of the age group, approximately 3% of a dose was recovered as unchanged drug in the urine.
在两项分别针对健康年轻受试者和老年受试者的研究中，对马来酸氟伏沙明的药代动力学进行了研究。在一项单剂量和多剂量口服给药研究中，6名健康年轻受试者最初口服50毫克剂量，随后每12小时服用50毫克片剂，持续28天。在第二项研究中，13名老年受试者每12小时服用50毫克片剂，持续28天。对健康年轻和老年志愿者单次和多次口服50毫克剂量后，氟伏沙明在大约5 - 6小时达到血浆峰值浓度。与单剂量给药（652纳克·小时/毫升）相比，多次给药后（873纳克·小时/毫升）氟伏沙明的曲线下面积（AUC）往往更大。而且长期给药后的终末半衰期（22±6小时）往往比单次给药后更长。在给药10天内达到稳态血浆水平。老年健康受试者中氟伏沙明的药代动力学与年轻受试者记录的情况没有差异。这些结果表明，基于药代动力学依据，在老年抑郁症患者中没有必要调整氟伏沙明的剂量。无论年龄组如何，约3%的剂量以原形药物形式在尿液中回收。
