Pharmacodynamics
Dose response with inhibition of plasma prolactin, onset of maximal effect, and duration of effect has been documented following single Cabergoline doses to healthy volunteers (0.05 to 1.5 mg) and hyperprolactinemic patients (0.3 to 1 mg). In volunteers,
prolactin inhibition was evident at doses >0.2 mg, while doses ≥0.5 mg caused maximal suppression in most subjects.
Higher doses produce prolactin suppression in a greater proportion of subjects and with an earlier onset and longer duration of action. In 12 healthy volunteers, 0.5, 1 and 1.5 mg doses resulted in complete prolactin inhibition, with a maximum effect within 3 hours in 92% to 100% of subjects after the 1 and 1.5 mg doses compared with 50% of subjects after the 0.5 mg dose.
In hyperprolactinemic patients (n=51),
the maximal prolactin decrease after a 0.6 mg single dose of Cabergoline was comparable to 2.5 mg bromocriptine; however,
the duration of effect was markedly longer (14 days vs 24 hours). The time to maximal effect was shorter for bromocriptine than Cabergoline (6 hours vs 48 hours).
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