Lemborexant
Other hypnotics (melatonin agonists and orexin antagonists)
Other hypnotics (melatonin agonists and orexin antagonists)
A dual orexin receptor antagonist for insomnia. It switches off the brain's wake signal; next-day drowsiness and sleep paralysis can occur.
Quick facts
- Group
- Other hypnotics (melatonin agonists and orexin antagonists)
- Target
- Orexin receptors OX1 and OX2
- Used for
- Insomnia with trouble falling
- Key effects
- Somnolence and tiredness · Headache
- Monitor
- Next-day alertness
- ATC
- N05CJ02
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows lemborexant itself bound to the human OX2 orexin receptor; it also blocks OX1.
Lemborexant blocks orexin 1 and orexin 2 receptors, so the orexin neuropeptides that keep the brain awake cannot act. Unlike benzodiazepines and Z-drugs it does not act on GABA-A receptors and does not cause anterograde amnesia.
- Blocks OX1 and OX2 orexin receptors
- The orexin wake signal is switched off
- Sleep begins and is maintained
Indications
- Insomnia with trouble falling or staying asleep Insomnia disorder →
Adverse effects
Common
- Somnolence and tiredness
- Headache
- Vivid dreams or nightmares
Contraindications
- Narcolepsy
Key interactions
- Alcohol
- Worse side effects
- Other sleep medicines and sedatives
- Added sedation and next-day impairment
- St John's wort
- May change how well it works
What is monitored
- Next-day alertness, driving and falls
- Mood and unusual night-time behaviour
Administration and safety
- Given by mouth right before bedtime, at most once a night
- Controlled medicine (Schedule IV in the United States)
Nursing care
- Ask about narcolepsy, sleep apnoea, lung disease, liver disease and depression
- Teach to avoid alcohol and other sedatives
- Teach to report sleep paralysis, leg weakness or actions done while asleep
Pharmacokinetics
- Half-life
- Long, about 17 to 19 hours
Test yourself
Think of the answer, then tap the question to see it.
Which receptors does lemborexant block?
Orexin 1 and orexin 2 receptors.
Why is it avoided in narcolepsy?
Narcolepsy is caused by loss of orexin; blocking orexin further makes sense to avoid.
Does lemborexant cause anterograde amnesia like benzodiazepines?
No; it does not act on GABA-A receptors.
Connections
← Back to the class: Other hypnotics (melatonin agonists and orexin antagonists)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Lemborexant: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); 7XRR: Crystal structure of the human OX2R bound to the insomnia drug lemborexant. (RCSB Protein Data Bank, 2022); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.