What are Sedative Hypnotics?

Sedative-hypnotics are sleep medications and they are used for treating insomnia. Several groups of medications fall into this class and they are prescribed based on the type of insomnia a person is experiencing. Behavioral and lifestyle modifications can be adequate in treating insomnia in many cases, therefore it is important to consult your doctor for proper treatment of insomnia.

Insomnia is a sleep disorder where a person has trouble falling or staying asleep. If a person consistently experiences insomnia, it may affect their mood, energy levels, health, and work performance. There are several causes of insomnia, including stress, a traumatic event, depression, anxiety, or even medications. That is why it is important to identify and treat the underlying problem before treating insomnia.

Classification of Sedative-Hypnotic Drugs

• Non-Benzodiazepines
• Benzodiazepines
• Melatonin Receptor Agonist
• Orexin Receptor Antagonist
• Antidepressants

List and Examples of Sedative Hypnotics

Benzodiazepines

• Temazepam (Restoril)
• Triazolam (Halcion)
• Flurazepam (Dalmane)
• Quazepam (Doral)
• Estazolam (Prosom)

Non-Benzodiazepine Benzodiazepine Receptor Agonists

• Zolpidem (Ambien, Ambien CR, Intermezzo, Zolpimist, Edluar)
• Zaleplon (Sonata)
• Eszopiclone (Lunesta)

Melatonin Receptor Antagonist

• Ramelteon (Rozerem)

Orexin Receptor Antagonist

• Suvorexant (Belsomra)

Antidepressants

• Doxepin (Selinor)
• Trazodone (Oleptra)
• Mirtazapine (Remeron)

How do Sedative Hypnotics Work?

Benzodiazepines

Benzodiazepines bind to gamma-aminobutyric acid (GABA) type A receptors. Gamma-aminobutyric acid is a neurotransmitter that slows the activity of nerves. Benzodiazepines reduce brain activity and cause sleep by increasing the effect of GABA. Benzodiazepines shorten the time it takes to fall asleep and they increase total sleep time.

Non-Benzodiazepine benzodiazepine receptor agonists

Zolpidem (Ambien) – Zolpidem exerts its sedative effects by binding to one type of GABA type A  receptor. Zolpidem induces sleep and helps maintain deep sleep for patients that might have awakenings in the middle of the night.

Zaleplon (Sonata) – Zaleplon binds to the same GABA type A receptor as zolpidem and in clinical studies, both drugs showed a similar decrease in time to sleep. However, using zolpidem resulted in fewer night awakenings when compared to zaleplon in a head-to-head study. Zaleplon is less likely to cause hangover sleepiness because it does remain in the body as long as zolpidem. 

Eszopiclone (Lunesta) –  Eszopiclone also stimulates GABA receptors. Eszopiclone shortens the time it takes to fall asleep and increases total sleep time. Its effects last longer than zaleplon and zolpidem. 

Melatonin Receptor Agonist

Melatonin is a hormone produced by the pineal gland in the brain and it controls sleep and wake cycles. Melatonin receptor agonists like ramelteon (Rozerem) are melatonin analogs that bind to melatonin receptors to induce the effect of melatonin.  Ramelteon is used for the treatment of insomnia that involves difficulty falling asleep.

Orexin Receptor Antagonist

Orexin is a chemical that plays a role in alertness and wakefulness. By blocking orexin from binding to receptors, suvorexant (Belsomra) can potentially help induce sleep.

Antidepressants

Doxepin and trazodone are antidepressants with sedative effects. They are primarily used when the underlying cause of insomnia is depression. Due to their sedating side effects, they help treat both depression and insomnia.

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