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Daytime pharmacodynamic and pharmacokinetic evaluation of low-dose sublingual transmucosal zolpidem hemitartrate.

Author(s): Roth T, Mayleben D, Corser BC, Singh NN

Affiliation(s): Henry Ford Hospital, Sleep Disorders and Research Center, Detroit, MI 48202, USA. troth1@hfhs.org

Publication date & source: 2008-01, Hum Psychopharmacol., 23(1):13-20.

Publication type: Evaluation Studies; Randomized Controlled Trial

OBJECTIVES: Buffered low-dose sublingual transmucosal zolpidem lozenge hemitartrate (ST zolpidem) is being developed for the treatment of middle-of-the-night insomnia. The objective of this double-blind placebo-controlled cross-over study (n = 24) was to evaluate the pharmacokinetics (PK) and daytime-sedative profile of 1.0, 1.75, and 3.5 mg dose of the formulation. METHODS: Daytime sedation was measured pre-dose and up to 5 h post-dose objectively by the Digit Symbol Substitution Test (DSST) and subjectively using the Visual Analog Scale (VAS). Blood samples for PK assessment was collected pre-dose and up to 12 h post-dose. RESULTS: The 1.75 and 3.5 mg, but not the 1 mg, ST zolpidem produced significant sedation versus placebo within 20 min of dosing which lasted for up to 3 h. Zolpidem from the formulation was rapidly absorbed and reached maximum plasma concentrations within 38 min of dosing, however the half-life was independent of the dose and side effects were consistent with the known pharmacology of the drug. CONCLUSIONS: ST zolpidem produced rapid, short duration of sedation and the effect was consistent with its PK profile. This novel low-dose formulation of zolpidem may provide clinicians and patients with a prn option for the management of sleep maintenance insomnia. (c) 2007 John Wiley & Sons, Ltd.

Page last updated: 2008-03-26

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