Products
Suvorexant was approved in the United States in 2014 as the first agent in the orexin receptor antagonist group in the form of film-coated tablets (Belsomra).
Structure and properties
Suvorexant (C23H23ClN6O2, Mr = 450.9 g/mol) exists as a white powder that is insoluble in water. It is a benzoxazole, diazepane and triazole derivative.
Effects
Suvorexant has sleep-inducing properties. It is a selective and dual antagonist at the orexin receptors OX1R and OX2R. It blocks the binding of the neuropeptides orexin A and orexin B, produced in the hypothalamus of neurons, to their receptors. This system is partly responsible for promoting wakefulness. Suvorexant has a medium-long half-life of about 12 hours. Unlike many other sleep aids, it does not interact with GABA receptors.
Indications
For the treatment of sleep onset and sleep maintenance disorders.
Dosage
According to the professional information. Tablets are taken before bedtime and no more than once per night. When taken with food, the onset of action is delayed.
Abuse
Suvorexant may be abused as an intoxicant due to its depressant effects.
Contraindications
- Hypersensitivity
- Narcolepsy
Full precautions can be found in the drug label.
Interactions
Suvorexant is a substrate of CYP3A and corresponding interactions with CYP inhibitors and CYP inducers are possible. CYP2C19 is involved in metabolism to a lesser extent. Combination with alcohol and centrally depressant drugs is not recommended because adverse effects may be increased.
Adverse effects
The most common potential adverse effect is drowsiness (during the day), which may adversely affect reaction time and impair participation in road traffic. The development of physical dependence was not observed in clinical trials. If this proves true in practice, it would represent an advantage over many other sleep aids.