Abstract | INTRODUCTION: AREAS COVERED: This review discusses pharmacokinetics (PK), pharmacodynamics (PD), efficacy, and safety properties of orexin receptor antagonists (ORAs). EXPERT OPINION: In general, the drugs described have a similar effect on sleep characteristics although their pharmacokinetic variables differ. ORAs have the potential to revolutionize the pharmacological treatment of insomnia because they not only improve sleep, but, in addition, appear to have no dependence - and tolerance-inducing effects, which makes them suitable for long-term-treatment. The safety and tolerability profile of ORAs clearly differ from those of more traditional sleep-promoting drugs. Further research is needed to demonstrate benefits to patients suffering from insomnia disorder, e.g., with respect to improving not only sleep but also daytime functioning. In addition, ongoing and future research will show whether ORAs may have beneficial effects in patients with various psychiatric and neurodegenerative disorders, including Alzheimer's disease.
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Authors | Clemens Muehlan, Cedric Vaillant, Isabelle Zenklusen, Stephan Kraehenbuehl, Jasper Dingemanse |
Journal | Expert opinion on drug metabolism & toxicology
(Expert Opin Drug Metab Toxicol)
Vol. 16
Issue 11
Pg. 1063-1078
(Nov 2020)
ISSN: 1744-7607 [Electronic] England |
PMID | 32901578
(Publication Type: Journal Article, Review)
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Chemical References |
- Orexin Receptor Antagonists
- Orexins
- Sleep Aids, Pharmaceutical
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Topics |
- Animals
- Humans
- Orexin Receptor Antagonists
(administration & dosage, adverse effects, pharmacology)
- Orexins
(metabolism)
- Sleep Aids, Pharmaceutical
(administration & dosage, adverse effects, pharmacology)
- Sleep Initiation and Maintenance Disorders
(drug therapy, physiopathology)
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