Journal article
Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders.
- Muehlan C Department of Clinical Pharmacology, Idorsia Pharmaceuticals Ltd , Allschwil, Switzerland.
- Vaillant C Department of Clinical Pharmacology, Idorsia Pharmaceuticals Ltd , Allschwil, Switzerland.
- Zenklusen I Department of Clinical Pharmacology, Idorsia Pharmaceuticals Ltd , Allschwil, Switzerland.
- Kraehenbuehl S Department of Clinical Pharmacology and Toxicology, University Hospital Basel , Basel, Switzerland.
- Dingemanse J Department of Clinical Pharmacology, Idorsia Pharmaceuticals Ltd , Allschwil, Switzerland.
- 2020-09-09
Published in:
- Expert opinion on drug metabolism & toxicology. - 2020
Efficacy
orexin
performance
pharmacodynamics
pharmacokinetics
receptor
review
safety
selectivity
sleep
English
INTRODUCTION
The last two decades have witnessed a rapid increase in the knowledge about the role of the orexin system, particularly in the regulation of wakefulness and arousal. Dual orexin receptor antagonists (DORAs) have been approved for the treatment of insomnia disorders (suvorexant, lemborexant) and drugs with a distinctive profile (daridorexant) or orexin-2 receptor selectivity (seltorexant) are in development.
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.
The last two decades have witnessed a rapid increase in the knowledge about the role of the orexin system, particularly in the regulation of wakefulness and arousal. Dual orexin receptor antagonists (DORAs) have been approved for the treatment of insomnia disorders (suvorexant, lemborexant) and drugs with a distinctive profile (daridorexant) or orexin-2 receptor selectivity (seltorexant) are in development.
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.
- Language
-
- English
- Open access status
- closed
- Identifiers
-
- DOI 10.1080/17425255.2020.1817380
- PMID 32901578
- Persistent URL
- https://folia.unifr.ch/global/documents/51071
Statistics
Document views: 51
File downloads: