Daridorexant (nemorexant) is a newer class of sedative-hypnotic drugs under non-benzodiazepine category. it is used to treat insomnia in adults. daridorexant blocks binding of wake promoting neuropeptides (orexin A and orexin B) to its receptors OX-1 and OX-2. It should be avoided in patients with depression.
Drug class
Orexin receptor antagonist, hypnotics
Available preparation
Daridorexant hydrochloride (also known as nemorexant hydrochloride)
Tablet: 25 mg, 50 mg
Dosage
- Adult: 25 – 50 mg (30 min before bedtime)
- Children: not recommended
Common use
Insomnia (sleep initiation and maintenance disorder)
Side effects
- Worsening of depression, suicidal thoughts
- Hypnogogic/hypnopompic hallucination
- Daytime sleepiness, so avoided in pts requiring continuous attention like driving
- Cataplexy like symptoms, so avoided with alcohol
- Abuse potential/ physical dependence develops on long term use
Contraindicated in pts with narcolepsy (sleep paralysis) and compromised respiratory function.
Overdose causes muscle weakness, sleep paralysis, catalepsy, headache, constipation.
Pharmacological characteristics
- Onset of action: 30 min with peak plasma concentration in 1-2 hours.
- Half-life (t1/2): 8 hours
- Duration of action: 7-10 hours
- MOA: blocking the binding of wake promoting neuropeptides (orexin A and orexin B) to its receptors OX-1 and OX-2
- Oral bioavailability: 62%
- No QT-interval prolongation (at a dose of 4 times the max recommended dose)
- Metabolized by CYP 3A4 enzyme, so avoided concomitant use of strong CYP enzyme inducers and inhibitors.
- Inactive metabolites are excreted in feces (57%) and urine (28%)
- Safety and effectiveness have not been established during pregnancy and lactation.
- No fetal toxicity/malformation observed on animal study.