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Clinical Pharmacokinetics of Cabergoline

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Abstract

Cabergoline is a synthetic ergoline dopamine agonist with a high affinity for D2 receptors indicated for use in both early and advanced Parkinsons’s disease and in hyperprolactinaemic disorders.

Following oral administration, peak plasma concentrations of cabergoline are reached within 2–3 hours. Over the 0.5–7mg dose range, cabergoline shows linear pharmacokinetics in healthy adult volunteers and parkinsonian patients. Cabergoline is moderately bound (around 40%) to human plasma proteins in a concentration-independent manner; concomitant administration of highly protein-bound drugs is unlikely to affect its disposition. The absolute bioavailability of cabergoline is unknown.

Cabergoline is extensively metabolised by the liver, predominantly via hydrolysis of the acylurea bond of the urea moiety. Cytochrome P450-mediated metabolism appears to be minimal. The major metabolites identified thus far do not contribute to the therapeutic effect of cabergoline. A significant fraction of the administered dose undergoes a first-pass effect. Less than 4% is excreted unchanged in the urine. The elimination half-life of cabergoline estimated from urinary data of healthy subjects ranges between 63 and 109 hours. Mild to moderate renal and hepatic impairment, administration of food and the use of concomitant antiparkinsonian medications, such as levodopa and Selegiline, have no effect on the pharmacokinetics of cabergoline.

The pharmacokinetic properties of cabergoline allow once daily administration in patients with Parkinsons’s disease and twice weekly administration in patients with hyperprolactinaemia, making this drug advantageous over other dopaminergic agents in term of both therapeutic compliance and better symptom control.

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The authors have provided no information on sources of funding or on conflicts of interest directly relevant to the content of this review.

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  1. Department of Neuroscience, Movement Disorders Unit, University of Pisa, Pisa, Italy

    Paolo Del Dotto & Ubaldo Bonuccelli

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  1. Paolo Del Dotto
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Correspondence to Paolo Del Dotto.

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Del Dotto, P., Bonuccelli, U. Clinical Pharmacokinetics of Cabergoline. Clin Pharmacokinet 42, 633–645 (2003). https://doi.org/10.2165/00003088-200342070-00003

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