Effects of the orexin receptor antagonist suvorexant on respiration during sleep in healthy subjects

J Clin Pharmacol. 2015 Oct;55(10):1093-100. doi: 10.1002/jcph.523. Epub 2015 Jun 3.

Abstract

Suvorexant is an orexin receptor antagonist for treating insomnia. The maximum approved dose in the United States and Japan is 20 mg. We evaluated suvorexant effects on respiration during sleep in a randomized, double-blind, 3-period crossover study of healthy adult men (n = 8) and women (n = 4) ≤ 50 years old who received single-dose suvorexant 40 mg, 150 mg, and placebo. Respiration during sleep was measured by oxygen saturation (SpO2 , primary end point) and the Apnea Hypopnea Index (AHI). The study was powered to detect a reduction greater than 5% in SpO2 . There was no effect of suvorexant on mean SpO2 during sleep. The mean (90%CI) treatment differences versus placebo were -0.3 (-1.2-0.6) for 40 mg and 0.0 (-0.9-0.9) for 150 mg. There were no dose-related trends in individual SpO2 values. Mean SpO2 was >96% for all treatments during total sleep time and during both non-REM and REM sleep. There was no effect of either suvorexant dose on AHI. The mean (90%CI) treatment differences versus placebo were 0.8 (-0.7-2.3) for 40 mg and -0.2 (-1.7-1.3) for 150 mg. Suvorexant was generally well tolerated; there were no serious adverse experiences or discontinuations. These data from healthy subjects suggest that suvorexant lacks clinically important respiratory effects during sleep at doses greater than the maximum recommended dose for treating insomnia.

Keywords: MK-4305; healthy subjects; orexin; randomized trial; respiration; suvorexant.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Azepines / adverse effects
  • Azepines / blood
  • Azepines / pharmacokinetics
  • Azepines / pharmacology*
  • Cross-Over Studies
  • Double-Blind Method
  • Female
  • Healthy Volunteers
  • Humans
  • Male
  • Middle Aged
  • Orexin Receptor Antagonists / adverse effects
  • Orexin Receptor Antagonists / blood
  • Orexin Receptor Antagonists / pharmacokinetics
  • Orexin Receptor Antagonists / pharmacology*
  • Oximetry
  • Oxygen / metabolism
  • Polysomnography
  • Respiration / drug effects*
  • Sleep Aids, Pharmaceutical / adverse effects
  • Sleep Aids, Pharmaceutical / blood
  • Sleep Aids, Pharmaceutical / pharmacokinetics
  • Sleep Aids, Pharmaceutical / pharmacology*
  • Triazoles / adverse effects
  • Triazoles / blood
  • Triazoles / pharmacokinetics
  • Triazoles / pharmacology*

Substances

  • Azepines
  • Orexin Receptor Antagonists
  • Sleep Aids, Pharmaceutical
  • Triazoles
  • suvorexant
  • Oxygen