A pilot study assessing pharmacokinetics and tolerability of oral and intravenous baclofen in healthy adult volunteers

Suresh K. Agarwal, Robert L. Kriel, James C Cloyd, Lisa D Coles, Lisa A. Scherkenbach, Michael H. Tobin, Linda E. Krach

Research output: Contribution to journalArticle

9 Citations (Scopus)

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 languageEnglish (US)
Pages (from-to)37-41
Number of pages5
JournalJournal of Child Neurology
Volume30
Issue number1
DOIs
StatePublished - Jan 1 2014

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Baclofen
Healthy Volunteers
Pharmacokinetics
Biological Availability
Area Under Curve
Ataxia
Cross-Over Studies
Safety
Pharmaceutical Preparations

Keywords

  • Baclofen
  • Baclofen withdrawal
  • Intravenous therapy
  • Muscle spasticity
  • Pharmacokinetics

Cite this

A pilot study assessing pharmacokinetics and tolerability of oral and intravenous baclofen in healthy adult volunteers. / Agarwal, Suresh K.; Kriel, Robert L.; Cloyd, James C; Coles, Lisa D; Scherkenbach, Lisa A.; Tobin, Michael H.; Krach, Linda E.

In: Journal of Child Neurology, Vol. 30, No. 1, 01.01.2014, p. 37-41.

Research output: Contribution to journalArticle

Agarwal, Suresh K. ; Kriel, Robert L. ; Cloyd, James C ; Coles, Lisa D ; Scherkenbach, Lisa A. ; Tobin, Michael H. ; Krach, Linda E. / A pilot study assessing pharmacokinetics and tolerability of oral and intravenous baclofen in healthy adult volunteers. In: Journal of Child Neurology. 2014 ; Vol. 30, No. 1. pp. 37-41.
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