Products
Lemborexant was approved in the United States in 2019 in film-coated tablet form (Dayvigo). This as the second agent in the orexin receptor antagonist group.
Structure and properties
Lemborexant (C22H20F2N4O2, Mr = 410.42 g/mol) is a pyrimidine and pyridine derivative. It exists as a white powder and is practically insoluble in water.
Effects
Lemborexant has sleep-inducing and depressant properties. The effects are due to competitive antagonism at the orexin receptors OX1R and OX2R (GPCR). Because Lemborexant interacts with both receptors, the drug is also referred to as (DORA). The neuropeptides orexin A and orexin B are produced by neurons in the hypothalamus. They are involved in promoting wakefulness. The active metabolite M10 binds to the receptors with comparable affinity. Lemborexant has a long half-life of 17 to 19 hours.
Indications
For the treatment of sleep onset and sleep maintenance disorders.
Dosage
According to the professional information. The tablets are taken just before going to bed. They may be administered only once per night. When taken with a meal, the onset of action is delayed.
Abuse
Lemborexant, similar to other sleep aids, can be abused as a depressant intoxicant.
Contraindications
- Hypersensitivity
- Narcolepsy
Full precautions can be found in the drug label.
Interactions
Central depressant drugs and alcohol may potentiate adverse effects. Lemborexant is metabolized primarily by CYP3A4 and to a lesser extent by CYP3A5. The major metabolite is M10.
Adverse effects
The most common potential adverse effect is drowsiness the following day. Withdrawal symptoms were not observed in the studies conducted.
