Bouchot O, Soret J Y, Jacqmin D, Lahlou N, Roger M, Blumberg J
Clinique Urologique, Hôtel-Dieu, CHU de Nantes, France.
Horm Res. 1998;50(2):89-93. doi: 10.1159/000023241.
The pharmacodynamics and the pharmacokinetic characteristics of a new longer-acting formulation containing 11.25 mg of triptorelin (Decapeptyl) to be administered every 3 months were evaluated in 14 patients with advanced prostate carcinoma. After one single injection, the mean time to reach the surgical castration testosterone range is 22 days, and this effective testosterone suppression is maintained for the 3-month therapy. After a first plasma surge (35.70 ng/ml) occurring 2.5 h after injection and a rise between day 17 and day 31 (maximum on day 24: 0.32 ng/ml), the mean triptorelin plasma level is stable (0.06 +/- 0.05 ng/ml) and maintained until day 91. This new formulation was well tolerated both locally and systemically.
对14例晚期前列腺癌患者评估了一种新的长效制剂(每3个月注射一次,含11.25 mg曲普瑞林(德普凯肽))的药效学和药代动力学特征。单次注射后,达到手术去势睾酮范围的平均时间为22天,这种有效的睾酮抑制在3个月的治疗期间得以维持。注射后2.5小时出现首次血浆峰值(35.70 ng/ml),第17天至第31天出现升高(第24天最高:0.32 ng/ml),之后曲普瑞林的平均血浆水平稳定(0.06±0.05 ng/ml)并维持至第91天。这种新制剂在局部和全身均具有良好的耐受性。