Orexin Antagonists for Insomnia

Last updated: March 26, 2019

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With sleep disorders getting more and more attention, we also see more sleep aids getting released in the market. Aside from memory foam pillows and white noise machines, medications are also taking the spotlight in our search for that elusive perfect sleep. Orexin receptor antagonists belong to this growing list of sleep aids.

These sleep aids target orexin action. This means that they work by blocking the signal of the chemical orexin in the human brain. Orexin is a chemical that plays a role in keeping you awake. When you take a medication that blocks its action, there is a great potential that it can promote sleep.

What are orexins?

Orexins are also called hypocretins. They are neurotransmitters produced in small neuronal populations. These are sparsely distributed in the lateral hypothalamic area. Orexin came from the Greek word for appetite, orexis. This is a fitting name since Orexin peptides regulate arousal, wakefulness, and food intake.

Because of orexin’s role in regulating food intake, researchers are also exploring its potential in helping those who suffer from eating disorders. There is also research looking into the possibility of using orexin to help people with weight problems.

People who suffer from a deficiency in orexin-producing neurons often suffer from narcolepsy as well. Narcolepsy is a sleep disorder that causes chronic sleepiness. Those who have narcolepsy can fall asleep anytime, at any place, whatever they are doing. They can be driving a car or washing the dishes, and the next thing you know, they’ve fallen asleep.

Scientists identified orexins in 1998. From that point on, scientists have spent a considerable amount of time and research in orexins. The aim is to get more insight into their role in regulating sleep and arousal. The end goal, of course, is to use orexins as a treatment for sleep disorders such as narcolepsy and insomnia.

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In 2014, the first orexin antagonist got approved. The drug company Merck developed Suvorexant as a treatment for insomnia. It became available in the market as a prescription drug in 2015. As of this time, this is still the only orexin antagonist approved by the FDA.

Is Suvorexant safe to take?

In theory, any drug approved by the Food and Drug Administration is safe as long you take them exactly as prescribed. Suvorexant comes in tablet form and taken by mouth. Patients usually take them once a day. The medication is taken no earlier than 30 minutes before bedtime. This is the usually prescribed taking time for sleep aids because taking it earlier may affect your mobility and alertness.

You can take Suvorexant with or without food. However, as with most sleep medications, this drug will work faster if taken on an empty stomach. It is also important not to take more than one dose per day even if you are still unable to sleep or stay asleep. If you feel that a single dose is not enough for you, consult your doctor. Your doctor might prescribe a different medication for you, one that may work better.

Do I need to follow any special precautions?

Yes, there are special precautions that you need to follow before taking Suvorexant. You need to inform your physician if you are allergic to Suvorexant. Of course, you won’t be able to tell if you’re allergic to it without taking it so the safest way to go about this is to take a careful look at its ingredients. You can ask your pharmacist for a medication guide. The guide lists all of the ingredients in a Suvorexant tablet so you can make an informed decision.

You should also inform your doctor if you suffer from narcolepsy. Most of the time, we assume that sleep disorders are relieved by the same types of medication. That is not the case. Different sleep disorders require different medications. This is why you need to inform your doctor if you have two different sleep disorders. Your doctor can then decide what medication or medications to prescribe to you.

Are there any side effects associated with Suvorexant?

Yes, Suvorexant may cause side effects. Side effects are normal and should not be a cause of concern. Experiencing side effects also doesn’t mean that the medication is not working. However, you need to inform your doctor if any of these symptoms won’t go away or if they become severe. Common side effects include:

  • Dizziness
  • Drowsiness
  • Headache
  • Unusual dreams
  • Dry mouth
  • Diarrhea
  • Coughs

Orexin antagonists are some of the newest types of drugs that can potentially help those with sleep disorders. Right now, there is only one approved orexin antagonist, Suvorexant. Almorexant is another such drug but its manufacturers, GlaxoSmithKline and Actelion, concluded that it would not receive approval.

This doesn’t mean that orexin antagonists are not effective. There are just so many things left that we need to discover about them. Given enough time, we can harness orexin antagonists’ full potential in relieving us from sleep disorders.

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