1994
DOI: 10.1002/jps.2600831012
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Pharmacodynamics and Relative Bioavailability of Cabergoline Tablets vs Solution in Healthy Volunteers

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Cited by 24 publications
(9 citation statements)
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“…It is much more likely that levodopa as a metabolic precursor of DA enhances DA synthesis and turnover. [27][28][29][30] The absence of measurable effects on EDVR values with the longer acting compound cabergoline measured on a day without medication does not support that the pharmacokinetic differences between both drugs are responsible for their differential effects on putaminal DA turnover. In contrast, we did not detect significant effects by the long-acting dopamine D2 receptor agonist cabergoline on putaminal DA turnover.…”
Section: Figurementioning
confidence: 92%
“…It is much more likely that levodopa as a metabolic precursor of DA enhances DA synthesis and turnover. [27][28][29][30] The absence of measurable effects on EDVR values with the longer acting compound cabergoline measured on a day without medication does not support that the pharmacokinetic differences between both drugs are responsible for their differential effects on putaminal DA turnover. In contrast, we did not detect significant effects by the long-acting dopamine D2 receptor agonist cabergoline on putaminal DA turnover.…”
Section: Figurementioning
confidence: 92%
“…This could suggest that NS patients need higher chronic doses of BCR to induce a significant remission of the syndrome. On the other hand, the successful result obtained with CAB and not replicated by BCR may reside in the pharmacokinetic and pharmacodynamic properties of CAB; this drug is a long-lasting dopamine agonist with a prolonged half-life (62–68 h) and a low clearance rate (85% eliminated in 7 days after the administration of a single 1-mg dose) as per the studies performed in healthy women [24]. It has been calculated that in the treatment of hyperprolactinemia a single 1-mg dose of CAB corresponds to a treatment with a 2.5-mg dose of BCR given twice daily for 14 days [25].…”
Section: Discussionmentioning
confidence: 99%
“…These results clearly indicate that cabergoline is superior to bromocriptine in terms of both the normalization rate and the mean suppressibility of elevated prolactin. The fact that cabergoline was moreefficacious than bromocriptine in patients with idiopathic and micro-and macroprolactinoma-related hyperprolactinemia, suggests that in addition to having a more selective affinity to dopamineD2 than Dl receptors and a longer half-life, it may have another mechanism of action on prolactin as proposed by others (29)(30)(31). Thus if cabergoline is tried in patients who have an inadequate response and poor tolerance to bromocriptine, the proportion of patients whoundergo additional surgery or radiotherapy, and hence those who will develop pituitary failure, may be reduced.…”
Section: Discussionmentioning
confidence: 88%