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) |
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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
Publisher Copyright:© The Author(s) 2014.
Keywords
- Baclofen
- Baclofen withdrawal
- Intravenous therapy
- Muscle spasticity
- Pharmacokinetics