Contraindications
Hypersensitivity to ergot derivatives
Pediatric patients (no clinical experience)
Severely impaired liver function or cholestasis
Concomitant use with drugs metabolized mainly by CYP450 enzymes such as erythromycin and ketoconazole, because increased plasma levels of cabergoline may result (although cabergoline undergoes minimal CYP450 metabolism). Cautions: severe cardiovascular disease, Raynauds disease, gastroduodenal ulcers, active gastrointestinal bleeding, hypotension. Side effects
Side effects are mostly dose dependent. Much more severe side effects are reported for treatment of Parkinsons disease and (off-label treatment) for restless leg syndrome which both typically require very high doses. The side effects are considered mild when used for treatment of hyperprolactinemia and other endocrine disorders or gynecologic indications where the typical dose is one hundredth to one tenth that for Parkinsons disease.Cabergoline requires slow dose titration (2–4 weeks for hyperprolactinemia, often much longer for other conditions) to minimise side effects. The extremely long bioavailability of the medication may complicate dosing regimens during titration and require particular precautions. Cabergoline is considered the best tolerable option for hyperprolactinemia treatment although the newer and less tested quinagolide may offer similarly favourable side effect profile with quicker titration times. Approximately 200 patients with newly diagnosed Parkinsons disease participated in a clinical study of cabergoline monotherapy. Seventy-six (76) percent reported at least one side effect. These side effects were chiefly mild or moderate:

GI tract: Side effects were extremely frequent. Fifty-three percent of patients reported side effects. Very frequent: Nausea (30%), constipation (22%), and dry mouth (10%). Frequent:  Gastric irritation (7%), vomiting (5%), and dyspepsia (2%).
Human bioavailability has not been determined since the drug is intended for oral use only. In mice and rats the absolute bioavailability has been determined to be 30 and 63 percent, respectively. Cabergoline is rapidly and extensively metabolized in the liver and excreted in bile and to a lesser extent in urine. All metabolites are less active than the parental drug or inactive altogether. The human elimination half-life is estimated to be 63 to 68 hours in patients with Parkinsons disease and 79 to 115 hours in patients with pituitary tumors. Average elimination half-life is 80 hours. The therapeutic effect in treatment of hyperprolactinemia will typically persist for at least 4 weeks after cessation of treatment. History
Cabergoline was first synthesized by scientists working for the Italian drug company Farmitalia-Carlo Erba in Milan who were experimenting with semisynthetic derivatives of the ergot alkaloids, and a patent application was filed in 1980. The first publication was a scientific abstract at the Society for Neuroscience meeting in 1991.Farmitalia-Carlo Erba was acquired by Pharmacia in 1993, which in turn was acquired by Pfizer in 2003.Cabergoline was first marketed in The Netherlands as Dostinex in 1992. The drug was approved by the FDA on December 23, 1996. It went generic in late 2005 following US patent expiration. Society and culture
Brand names
Brand names of cabergoline include Cabaser, Dostinex, Galastop (veterinary), and Kelactin (veterinary), among others. Research
Cabergoline was studied in one person with Cushings disease, to lower adrenocorticotropic hormone (ACTH) levels and cause regression of ACTH-producing pituitary adenomas. References
External links
Cabergoline, Mayo Clinic