Cabergoline

What cabergoline is

Cabergoline is a dopamine agonist from the group of ergoline derivatives and is prescription-only. In Germany it has been approved as Dostinex since 1995: for primary suppression of lactation after childbirth and for disorders caused by an elevated prolactin level, such as absent menstruation, absent ovulation or milk flow outside breastfeeding, including in small prolactin-producing pituitary tumors.

What is rated is the state of knowledge. For the approved use it is good, with a large randomized trial and decades of experience. For lifestyle use in healthy people, that is, more desire or a shorter recovery phase after orgasm, it is thin.

How it works

Cabergoline stimulates the dopamine D2 receptors on the prolactin-producing cells of the pituitary gland. There, dopamine is the natural braking signal; the prolactin level falls, and does so for a long time. Above the dose needed for this, cabergoline also has central dopaminergic effects, according to the prescribing information.

As an ergoline derivative, it additionally activates the serotonin 5-HT2B receptor. This property is shared by the active substances with which fibrosis and heart valve changes occur after prolonged use. The idea behind lifestyle use: prolactin rises markedly after orgasm and could dampen desire and the recovery phase. In humans, this pathway has only been tested in one short-term experiment.

What the studies show

Webster 1994: cabergoline versus bromocriptine

Webster 1994 (NEJM) treated 459 women with hyperprolactinemic amenorrhea, double-blind for 8 weeks, then open-label for 16 weeks with dose adjustment. A stably normal prolactin level was reached by 186 of 223 women under cabergoline (83 percent) and 138 of 236 under bromocriptine (59 percent), p<0.001. Amenorrhea persisted in 7 versus 16 percent. Side effects occurred in 68 versus 78 percent.

Krüger 2003: ten healthy men

Krüger 2003 (J Endocrinol) studied 10 healthy men in a single-blind, placebo-controlled crossover design. A single dose of 0.5 mg cabergoline lowered the prolactin level; arousal and orgasm were then induced with an erotic film and masturbation. Sexual desire (p<0.05), sexual function (p<0.01) and the positive experience of the recovery phase (p<0.01) increased. When protirelin, which raises prolactin, was given in addition, the effects disappeared. This is the central study behind lifestyle use: 10 men, a single dose, single-blind.

Krüger 2018: the same in women, without effect

Using a double-blind, placebo-controlled crossover design, the same research group found no change in objective or subjective sexual parameters in 13 healthy women. The authors suspect a sex difference in the role of the dopamine system.

Hollander 2016: orgasm disorder without a control group

In an andrology practice, 131 men with delayed or absent orgasm were treated with 0.5 mg cabergoline twice a week. 87 (66.4 percent) reported subjective improvement, 44 no change. Longer treatment and concurrent testosterone therapy were associated with a better response. The analysis was retrospective and without a control group; the authors call for randomized trials.

Heart valves: high versus low doses

Schade 2007 (NEJM) found, in a British cohort of 11,417 people prescribed Parkinson’s medications, a 4.9-fold higher rate of newly diagnosed valvular regurgitation under cabergoline (95 percent confidence interval 1.5 to 15.6). At the low doses used against prolactin, the finding is weaker: a meta-analysis of 13 studies found tricuspid regurgitation on ultrasound more often (OR 3.74; 1.79 to 7.8), but no increase in other valve changes and no symptoms from it in any patient (Stiles 2018). In a cohort of 646 prolactinoma patients, with a median weekly dose of 2.1 mg, 2.8 percent reached valve surgery or heart failure, compared with 2.33 percent of controls; relative risk 0.78 (0.41 to 1.48), no significant difference (Stiles 2021).

Where the data stop

• Libido in healthy people. What is established is a single dose in 10 men in the laboratory. There are no controlled data on repeated use or on effects in everyday life; in 13 women no effect was found.
• Prolactin during hormone treatments. No controlled studies were found during research on lowering prolactin in testosterone or anabolic steroid use without proven hyperprolactinemia.
• Whether prolactin is the key. The 2003 study does not show with certainty that the effect runs via prolactin; the authors themselves point out that the substances used act at different sites.
• Low doses over many years. Whether the tricuspid regurgitation seen more often on ultrasound at low doses becomes clinically significant is open; the authors of the meta-analysis describe its significance as unclear.

Status, approval and legal

Cabergoline has been approved in Germany as Dostinex since February 24, 1995, and is prescription-only, for primary suppression of lactation and for disorders caused by hyperprolactinemia. According to the prescribing information, the therapeutic dose for hyperprolactinemia is usually 1 mg per week, and the maximum dose is 3 mg per day. Use for libido, orgasm or prolactin lowering in healthy people is not approved.

In June 2008, the Committee for Medicinal Products for Human Use of the European Medicines Agency concluded a review procedure on fibrosis under ergot-derived dopamine agonists. For cabergoline, it recommended echocardiography before and during treatment, lowering the maximum dose to 3 mg per day, and listing cardiac fibrosis as a very common side effect. The approval remained in place.

Cabergoline is not listed in the annex of the German Anti-Doping Act.

Safety

The best-known risk is fibrosis of the lungs, the pericardium and the retroperitoneal space, as well as changes to the aortic, mitral and tricuspid valves. According to the prescribing information, long-term treatment requires an echocardiogram before starting, the first check after 3 to 6 months, and thereafter at least every 6 to 12 months. Heart valve disease before long-term treatment and a history of fibrosis are contraindications.

The second risk concerns behavior. Dopamine agonists, including cabergoline, can trigger impulse control disorders: pathological gambling, increased libido, hypersexuality, compulsive shopping, binge eating. A meta-analysis of 8 studies with 858 prolactinoma patients found impulse control disorders more often under dopamine agonists (relative risk 1.71), especially hypersexuality (2.61). If you are considering cabergoline for desire, this point is part of the picture.

Common side effects are nausea, headache, dizziness and a drop in blood pressure; sudden onset of sleep has also been described. Cabergoline should not be given together with antipsychotics.

Sources

• Webster J et al., N Engl J Med 1994 – cabergoline versus bromocriptine in hyperprolactinemic amenorrhea, RCT with 459 women
• Krüger TH et al., J Endocrinol 2003 – acute prolactin lowering and sexual experience, crossover with 10 healthy men
• Krüger THC et al., J Sex Marital Ther 2018 – no effect on sexual experience in 13 healthy women
• Hollander AB et al., Sex Med 2016 – cabergoline in male orgasmic disorder, retrospective, 131 men
• Schade R et al., N Engl J Med 2007 – dopamine agonists and valvular heart regurgitation, case-control study
• Stiles CE et al., J Clin Endocrinol Metab 2018 – meta-analysis of heart valves under cabergoline in hyperprolactinemia
• Stiles CE et al., J Clin Endocrinol Metab 2021 – hard cardiac endpoints in 646 prolactinoma patients
• Penchev P et al., J Clin Neurosci 2025 – meta-analysis of impulse control disorders under dopamine agonists in prolactinoma
• EMA, press release of June 26, 2008 – new warnings and contraindications for ergot-derived dopamine agonists
• Dostinex prescribing information (as of March 2024, German)