Institute of Endocrinology, Rabin Medical Centre, Beilinson Hospital, Petach Tikva, and School of Medicine, Tel-Aviv University, Israel.
Best Pract Res Clin Endocrinol Metab. 2024 Jul;38(4):101887. doi: 10.1016/j.beem.2024.101887. Epub 2024 Feb 28.
Cabergoline is an ergot derivative long-acting dopamine receptor 2 (DR2) selective agonist administered orally and widely used for the treatment of prolactin-secreting adenomas and Parkinson's disease. DR2 is expressed in most somatotroph adenomas. In acromegaly, cabergoline is used off-label and its role is limited by the relatively modest efficacy for achieving hormonal remission and thus, it is largely indicated in patients with mild elevation of GH/IGF-I postoperatively. It can be given as monotherapy, usually at a higher weekly dose than usually required to treat prolactinomas, but also as an add-on treatment in patients partially responding to the somatostatin receptor ligands octreotide or lanreotide. IGF-1 normalization with cabergoline can be achieved in about a third of the patients. Low baseline IGF-1 level (below 1.5 x ULN) before cabergoline initiation is a good predictor for remission. Combination treatment with the GH receptor antagonist pegvisomant can also be beneficial. The inexpensive, well-tolerated and convenient oral administration of cabergoline makes it an attractive medical therapy for active acromegaly.
卡麦角林是一种长效多巴胺受体 2(DR2)选择性激动剂,属于麦角生物碱衍生物,可口服给药,广泛用于治疗催乳素分泌腺瘤和帕金森病。DR2 在大多数生长激素腺瘤中表达。在肢端肥大症中,卡麦角林是一种超适应证用药,其疗效相对有限,无法实现激素缓解,因此主要适用于术后 GH/IGF-I 轻度升高的患者。卡麦角林可单独使用,通常每周的剂量高于治疗催乳素腺瘤所需的剂量,但也可作为对生长抑素受体配体奥曲肽或兰瑞肽部分反应的患者的附加治疗。用卡麦角林可使大约三分之一的患者 IGF-1 恢复正常。卡麦角林治疗前 IGF-1 水平较低(低于 ULN 的 1.5 倍)是缓解的良好预测指标。与 GH 受体拮抗剂培维索孟联合治疗也可能有益。卡麦角林价格低廉、耐受性好且服用方便,是治疗活动期肢端肥大症的一种有吸引力的药物治疗选择。