Ferrari C, Mattei A, Melis G B, Paracchi A, Muratori M, Faglia G, Sghedoni D, Crosignani P G
Second Department of Medicine, Fatebenefratelli Hospital, Milan, Italy.
J Clin Endocrinol Metab. 1989 Jun;68(6):1201-6. doi: 10.1210/jcem-68-6-1201.
Cabergoline, a new orally active dopaminergic drug with an extremely long-lasting PRL-lowering effect, was given to 48 hyperprolactinemic women for 3-18 months (median, 8 months) at doses varying between 0.2-3 mg/week administered one to three times weekly. Serum PRL levels declined to normal in 41 women, 30 of whom received 0.2-1 mg cabergoline once weekly, 8 received 0.2-0.5 mg twice weekly, and 3 received 0.4-0.6 mg 3 times weekly. Five women had slightly supranormal serum PRL levels while receiving 0.3-0.6 mg once weekly, but the dose was not increased because the lower dose had produced the desired clinical benefit. Two women had 50% reductions in their serum PRL levels, but remained hyperprolactinemic while receiving 2-3 mg cabergoline weekly. Among 30 amenorrheic women, 28 had resumption of menses, the exceptions being 2 hypopituitary women, presumptive evidence of ovulation was available in 21. Marked tumor shrinkage occurred after 3-month treatment in 5 of the 6 women who had macroprolactinomas. Only 4 women had side-effects during the first weeks of treatment, and these vanished despite continued cabergoline administration at the same or reduced, but still effective, doses. In a short term, double blind study, cabergoline at 3 different schedules (0.4 mg twice weekly, 0.2 mg 4 times weekly, and 0.4 mg 3 times weekly for 3 weeks, followed by 0.4 mg twice weekly) or placebo was given to a total of 24 hyperprolactinemic women (6 in each subgroup) for 8 weeks, with weekly evaluation of serum PRL levels and side-effects. All 3 cabergoline schedules, but not placebo, induced significant reductions in serum PRL concentrations during the 8-week treatment period. Mild transient side-effects occurred in 7 drug-treated patients (nausea in 5; dizziness in 3). We conclude that cabergoline is effective treatment for hyperprolactinemia. Its efficacy, tolerability, and long duration of action may make it the drug of choice for patients with hyperprolactinemia.
卡麦角林是一种新型口服活性多巴胺能药物，具有极其持久的降低催乳素（PRL）作用。对48名高催乳素血症女性给予卡麦角林治疗3 - 18个月（中位数为8个月），每周给药剂量为0.2 - 3毫克，每周给药1 - 3次。41名女性的血清PRL水平降至正常，其中30名女性每周一次接受0.2 - 1毫克卡麦角林治疗，8名女性每周两次接受0.2 - 0.5毫克治疗，3名女性每周三次接受0.4 - 0.6毫克治疗。5名女性在每周一次接受0.3 - 0.6毫克治疗时血清PRL水平略高于正常，但由于较低剂量已产生预期的临床益处，故未增加剂量。2名女性血清PRL水平降低了50%，但在每周接受2 - 3毫克卡麦角林治疗时仍为高催乳素血症。在30名闭经女性中，28名恢复了月经，2名垂体功能减退女性除外，21名有排卵的推定证据。6名患有大催乳素瘤的女性中有5名在治疗3个月后肿瘤明显缩小。只有4名女性在治疗的最初几周出现副作用，尽管继续以相同或降低但仍有效的剂量服用卡麦角林，这些副作用仍消失了。在一项短期双盲研究中，对总共24名高催乳素血症女性（每个亚组6名）给予3种不同给药方案的卡麦角林（每周两次0.4毫克、每周4次0.2毫克、每周3次0.4毫克，共3周，然后每周两次0.4毫克）或安慰剂，治疗8周，每周评估血清PRL水平和副作用。在8周治疗期内，所有3种卡麦角林给药方案均能显著降低血清PRL浓度，但安慰剂无此效果。7名接受药物治疗的患者出现轻度短暂副作用（5名恶心；3名头晕）。我们得出结论，卡麦角林是治疗高催乳素血症的有效药物。其疗效、耐受性和长效作用可能使其成为高催乳素血症患者的首选药物。
