阿夫唑嗪在良性前列腺增生患者重复口服给药后的前列腺组织分布情况。
Prostatic tissual distribution of alfuzosin in patients with benign prostatic hyperplasia following repeated oral administration.
作者信息
Mottet Nicolas, Bressolle Françoise, Delmas Vincent, Robert Michèle, Costa Pierre
机构信息
Urology Department, Central Hospital Gaston Doumergue, 5 Rue Hoche, 30029 Nimes Cedex 9, France.
出版信息
Eur Urol. 2003 Jul;44(1):101-5. doi: 10.1016/s0302-2838(03)00154-4.
OBJECTIVES
The blood and prostatic concentrations of alfuzosin were determined in patients with benign prostatic hyperplasia (BPH).
METHODS
12 patients scheduled for BPH surgery were treated with alfuzosin 5 mg twice daily prior to surgery in an open trial. Seven doses were given over a 4-day period. Blood samples were drawn before the first and the last intake (day 3). On day 4 (surgery day), a blood and prostate tissue sample were taken simultaneously 12 hours after the last drug intake.
RESULTS
Mean trough blood levels were 6.0+/-4.6 ng/ml and 5.8+/-3.7 ng/ml on day 3 and day 4, respectively, indicating a stable alfuzosin concentration. The mean prostate concentration on day 4 was 12.3+/-5.6 ng/g. Alfuzosin prostate and blood concentrations at 12 hours post dosing on day 4 were significantly correlated (r=0.804, p=0.0016); the prostate-blood ratio was 2.4+/-0.7.
CONCLUSIONS
Oral administration of alfuzosin leads to a high diffusion of the drug into the prostate of BPH patients.
目的
测定良性前列腺增生（BPH）患者中阿夫唑嗪的血液和前列腺浓度。
方法
在一项开放性试验中，12例计划接受BPH手术的患者在手术前每天两次服用5毫克阿夫唑嗪。在4天内给予7剂。在第一次和最后一次服药前（第3天）采集血样。在第4天（手术日），在最后一次服药12小时后同时采集血液和前列腺组织样本。
结果
第3天和第4天的平均谷血水平分别为6.0±4.6纳克/毫升和5.8±3.7纳克/毫升，表明阿夫唑嗪浓度稳定。第4天的平均前列腺浓度为12.3±5.6纳克/克。第4天给药12小时后阿夫唑嗪的前列腺和血液浓度显著相关（r = 0.804，p = 0.0016）；前列腺与血液的比率为2.4±0.7。
结论
口服阿夫唑嗪可使药物大量扩散至BPH患者的前列腺中。
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