Effect of clarithromycin on the pharmacokinetics of cabergoline in healthy controls and in patients with Parkinson's disease.

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Nakatsuka A, Nagai M, Yabe H, Nishikawa N, Nomura T, Moritoyo H, Moritoyo T, Nomoto M

Effect of clarithromycin on the pharmacokinetics of cabergoline in healthy controls and in patients with Parkinson's disease.

J Pharmacol Sci. 2006 Jan;100(1):59-64. doi: 10.1254/jphs.fp0050711. Epub 2006 Jan 13.

PubMed ID

16410677 [ View in PubMed

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Abstract

Cabergoline is used in the treatment of Parkinson's disease (PD). Clarithromycin is a potent inhibitor of CYP3A4 and P-glycoprotein and is often co-administered with cabergoline in usual clinical practice. We studied the effect of clarithromycin co-administration on the blood concentration of cabergoline in healthy male volunteers and in PD patients. Study 1: Ten healthy male volunteers were enrolled and were randomized to take a single oral dose of cabergoline (1 mg/day) for 6 days or a single oral dose of cabergoline plus clarithromycin (400 mg/day) for 6 days. Study 2: Seven PD patients receiving stable cabergoline doses were enrolled. They were evaluated for the plasma cabergoline concentration before and after the addition of clarithromycin 400 mg/day for 6 days, and again 1 month after discontinuation of clarithromycin. The dose and duration of clarithromycin were decided according to usual clinical practice. In healthy male volunteers, mean Cmax and AUC(0-10 h) of cabergoline increased to a similar degree during co-administration of clarithromycin. Mean plasma cabergoline concentration over 10 h post-dosing increased 2.6-fold with clarithromycin co-administration. In PD patients, plasma cabergoline concentration increased 1.7-fold during clarithromycin co-administration. Co-administration with clarithromycin may increase the blood concentration of cabergoline in healthy volunteers and in PD patients.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Cabergoline	Cytochrome P450 3A4	Protein	Humans	Unknown	Substrate	Details

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
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Food Interactions

Drug	Interaction
Cabergoline	Exercise caution with grapefruit products. Cabergoline is partially metabolized through the CYP3A4 pathway. Therefore coadministration with grapefruit, a CYP3A4 inhibitor, may increase its serum concentration.
Cabergoline	Exercise caution with St. John's Wort. Cabergoline is partially metabolized through the CYP3A4 pathway. Therefore coadministration with St. John's Wort, a CYP3A4 inducer, may reduce its serum concentration.