Abstract
Our objective was to characterize baclofen pharmacokinetics and safety given orally and intravenously. Twelve healthy subjects were enrolled in a randomized, open-label, crossover study and received single doses of baclofen: 3 or 5 mg given intravenously and 5 or 10 mg taken orally with a 48-hour washout. Blood samples for baclofen analysis were collected pre-dose and at regular intervals up to 24 hours post-dose. Clinical response was assessed by sedation scores, ataxia, and nystagmus. Mean absolute bioavailability of oral baclofen was 74%. Dose-adjusted areas under the curve between the oral and intravenous arms were statistically different (P = .0024), whereas area under the curve variability was similar (coefficient of variation: 18%-24%). Adverse effects were mild in severity and not related to either dose or route of administration. Three- and 5-mg intravenous doses of baclofen were well tolerated. Seventy-four percent oral bioavailability indicates that smaller doses of intravenous baclofen are needed to attain comparable total drug exposures.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 37-41 |
| Number of pages | 5 |
| Journal | Journal of Child Neurology |
| Volume | 30 |
| Issue number | 1 |
| DOIs | |
| State | Published - Jan 2014 |
Bibliographical note
Funding Information:The authors disclosed receipt of the following financial support for the research, authorship, and/or publication of this article: We would like to acknowledge Paralyzed Veterans of America Research Foundation for providing the initial funding for this study (grant no. 2866). Medtronic Inc provided financial support toward this study as well as the study drug.
Publisher Copyright:
© The Author(s) 2014.
Copyright:
Copyright 2021 Elsevier B.V., All rights reserved.
Keywords
- Baclofen
- Baclofen withdrawal
- Intravenous therapy
- Muscle spasticity
- Pharmacokinetics