Cabergoline (brand names Dostinex and Cabaser), an ergot-derivative,
\nis a potent dopamine receptor agonist on D2-Receptors. It also acts on
\ndopamine-receptors in lactophilic hypothalamus cells and causes thereby a
\nsuppression of the prolactin-production in pituitary gland.<\/p>\n
Cabergoline has a very long half life, so it can be taken once or twice a week. <\/p>\n
Pharmacokinetics<\/span> Carcinogenity<\/span> Off-Label\/Recreational Uses<\/span> Side effects<\/span> GI-Tract: Side effects were extremly frequent. Fiftythree Per Cent of Psychiatric Disturbances and CNS: Altogether 51% of patients were Cardiovascular: Approximately 30% of patients experienced side effects. In a combination study with 2,000 patients also treated with levodopa As with other ergot-derivatives pleuritis, exsudative pleura disease, The reported incidence and severity of side effects in hyperprolactinemic patients was comparable.<\/p>\n","protected":false},"excerpt":{"rendered":"
\nFollowing an oral single dose the drug is resorbed within 0.5 to 4
\nhours from the GI-Tract with considerable interindividual differences.
\nMeals do not alter the absorption characteristic. Human bioavailibility
\nwas not determined, because the drug is intended for oral use only. In
\nmice and rats the absolute bioavailability was 30 and 63%, respectively.
\nCabergoline is rapidly and to a great extend metabolized in the liver
\nand excreted in bile and far less in urine. All metabolites are less
\nactive than the parental drug or inactive. The human elimination
\nhalflife is estimated to be 63 to 68 hours in patients with M. Parkinson
\nand 79 to 115 hours in patients with pituitary tumors.<\/p>\n
\nIn rodents a dose dependent increase in malignant tumors has been
\nfound. They are thought to be species-specific. No clinical data exists
\non carcinogenity in humans.<\/p>\n
\nIt has at times been used as an adjunct to SSRI antidepressants as
\nthere is some evidence that it counteracts certain side effects of those
\ndrugs such as reduced libido and anorgasmia. It also has been suggested
\nonline that it has a possible recreational use in reducing or
\neliminating the male refractory period.<\/p>\n
\nApproximately 200 patients with newly diagnostizised M. Parkinson
\nparticipated in a clinical study regarding the monotherapy with
\ncabergoline. Seventynine (79) % reported at least one side effect. These
\nside effects were chiefly mild or moderate:<\/p>\n
\npatients reported side effects. Nausea (30%), obstipation (22%), and dry
\nmouth (10%) were very frequent. Frequent were gastric irritation (7%),
\nvomiting (5%), and dyspepsia (2%).<\/p>\n
\naffected. Very frequent were disturbances of sleep (somnolence 18%,
\ninsomnia 11%), vertigo (27%), and depression (13%). Frequent were
\ndyskinesia (4%) and hallucinations (4%).<\/p>\n
\nMost frequent were hypotension (10%), peripheral edema (14%) and
\nnon-specific edema (2%). Arrhythmias were encountered in 4.8%,
\npalpitations in 4.3%, and angina pectoris in 1.4%.<\/p>\n
\nthe incidence and severity of side effects was comparable to
\nmonotherapy. Encountered side effects required a termination of
\ncabergoline treatment in 15% of patients. Additional side effects were
\ninfrequent cases of hematological side effects, and an occasional
\nincrease in liver enzymes or serum creatinine without signs or symptoms.<\/p>\n
\npleura fibrosis, lung fibrosis, and pericarditis are seen. These side
\neffects are noted in less than 2% of patients. They require immediate
\ntermination of treatment. Clinical improvement and normalization of
\nX-Ray findings are normally seen soon after cabergoline withdrawal.<\/p>\n