Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Controlled Clinical Trial
. 2008 Mar;64(3):267-73.
doi: 10.1007/s00228-007-0414-1. Epub 2007 Dec 21.

Pharmacokinetics of eslicarbazepine acetate in patients with moderate hepatic impairment

Affiliations
Controlled Clinical Trial

Pharmacokinetics of eslicarbazepine acetate in patients with moderate hepatic impairment

Luis Almeida et al. Eur J Clin Pharmacol. 2008 Mar.

Abstract

Objective: To evaluate the effect of moderate liver impairment on the pharmacokinetics of eslicarbazepine acetate (BIA 2-093, ESL), a novel voltage-gated sodium channel blocker currently in clinical development.

Methods: The pharmacokinetics of ESL following an administration regimen of 800 mg once-daily for 8 days was characterized in patients with moderate liver impairment (n = 8) and in subjects with normal liver function (n = 8, control group).

Results: Eslicarbazepine acetate was rapidly and extensively metabolized by first-pass metabolism to its main active metabolite, eslicarbazepine (S-licarbazepine). There were more subjects with measurable plasma concentrations of the parent drug (ESL) in the hepatic impairment group than in the control group, suggesting that first-pass metabolism was slightly decreased by liver impairment. However, ESL plasma concentrations remained very low, representing only about 0.01% of total systemic exposure. No differences in the pharmacokinetics of eslicarbazepine or its metabolites were found between the hepatic impairment and control groups. Urinary excretion of eslicarbazepine and its glucuronide form was similar in the liver impaired and control subjects. The sum of drug moieties recovered in the urine corresponded to 91% of the administered dose in the control group and to 84% of the administered dose in the liver impairment group.

Conclusion: The pharmacokinetics of ESL was not affected by moderate hepatic impairment. Therefore, patients with mild to moderate liver impairment treated with ESL do not require dosage adjustment.

PubMed Disclaimer

References

    1. Drugs R D. 2003;4(5):269-84 - PubMed
    1. J Clin Pharmacol. 2004 Aug;44(8):906-18 - PubMed
    1. J Clin Pharmacol. 2005 Sep;45(9):1062-6 - PubMed
    1. Neurotherapeutics. 2007 Jan;4(1):88-96 - PubMed
    1. J Med Chem. 1999 Jul 15;42(14):2582-7 - PubMed

Publication types

LinkOut - more resources