Colao A, Di Sarno A, Sarnacchiaro F, Ferone D, Di Renzo G, Merola B, Annunziato L, Lombardi G
Department of Molecular and Clinical Endocrinology, University Federico II, Naples, Italy.
J Clin Endocrinol Metab. 1997 Mar;82(3):876-83. doi: 10.1210/jcem.82.3.3822.
Cabergoline (CAB), a new, potent, and long-lasting PRL-lowering agent, was shown to be effective in tumoral hyperprolactinemia. The aim of this study was to investigate the effectiveness of CAB in patients with prolactinoma proven to be resistant to bromocriptine (BRC) and quinagolide (CV 205-502). Twenty-seven patients (19 macro- and 8 microprolactinomas) were treated with CAB at a weekly dose of 0.5-3 mg for 3-22 months. All patients were previously shown to be resistant to BRC, and 20 of them were resistant to CV 205-502 as well. Basal serum PRL levels before CAB treatment ranged from 108-3500 micrograms/L in macroprolactinomas and from 64-205 micrograms/L in microprolactinomas. Gonadal failure was present in all patients, whereas symptoms of tumor expansion, such as visual field defects and headache, were present in 10 of 27 patients. Eight macroprolactinomas had previously undergone surgery and/or radiotherapy. CAB treatment normalized serum PRL levels in 15 of 19 macroprolactinomas and in all 8 microprolactinomas. In 3 of the remaining 4 patients it caused a notable decrease in prolactinemia (89%, 80.5%, and 68.7% of the baseline). Only 1 patient was withdrawn from CAB therapy after 3 months at the weekly dose of 2 mg due to the absence of any significant clinical, hormonal, or radiological improvement. Gonadal function was restored in 18 of 27 patients, galactorrhea disappeared in 5 of 6 women, and headache improved in 7 of 8 patients. A significant tumor shrinkage was detected by computed tomography and/or magnetic resonance imaging in 9 macroprolactinomas and 4 microprolactinomas. CAB was well tolerated by all patients, except 6 who referred slight and short-lasting nausea, postural hypotension, abdominal pain, dizziness, and sleepiness at the beginning of treatment. In particular, CAB was well tolerated by 19 patients previously shown to be poorly tolerant to BRC and CV 205-502. In conclusion, CAB may represent, at the moment, the only successful therapy for prolactinoma-bearing patients resistant to BRC and CV 205-502, as it normalized PRL levels in 22 of 27 patients, reduced tumor size in 13 of 27 patients, and improved clinical symptoms in 25 of 27 patients in the present study.
卡麦角林（CAB）是一种新型、强效且作用持久的降低催乳素（PRL）的药物，已被证明对肿瘤性高催乳素血症有效。本研究的目的是调查卡麦角林对已证实对溴隐亭（BRC）和喹高利特（CV 205 - 502）耐药的催乳素瘤患者的有效性。27例患者（19例大催乳素瘤和8例微催乳素瘤）接受卡麦角林治疗，每周剂量为0.5 - 3毫克，疗程为3 - 22个月。所有患者先前均被证明对溴隐亭耐药，其中20例对喹高利特也耐药。卡麦角林治疗前，大催乳素瘤患者的基础血清PRL水平为108 - 3500微克/升，微催乳素瘤患者为64 - 205微克/升。所有患者均存在性腺功能减退，而27例患者中有10例出现肿瘤扩大的症状，如视野缺损和头痛。8例大催乳素瘤患者先前接受过手术和/或放疗。卡麦角林治疗使19例大催乳素瘤中的15例以及所有8例微催乳素瘤患者的血清PRL水平恢复正常。在其余4例患者中的3例，其催乳素血症显著降低（分别为基线水平的89%、80.5%和68.7%）。仅1例患者在每周剂量2毫克治疗3个月后因无任何显著的临床、激素或影像学改善而退出卡麦角林治疗。27例患者中有18例性腺功能恢复，6例女性中有5例溢乳消失，8例患者中有7例头痛改善。通过计算机断层扫描和/或磁共振成像检测到9例大催乳素瘤和4例微催乳素瘤有显著的肿瘤缩小。除6例患者在治疗开始时出现轻微且短暂的恶心、体位性低血压、腹痛、头晕和嗜睡外，所有患者对卡麦角林耐受性良好。特别是，19例先前对溴隐亭和喹高利特耐受性差的患者对卡麦角林耐受性良好。总之，在本研究中，卡麦角林目前可能是对溴隐亭和喹高利特耐药的催乳素瘤患者唯一成功的治疗方法，因为它使27例患者中的22例PRL水平恢复正常，27例患者中的13例肿瘤缩小，27例患者中的25例临床症状改善。
