How daridorexant works?

Daridorexant is an exciting new sleep medication that provides an alternative solution to the current highly addictive Z drugs. Why are we so excited about Quviviq or daridorexant? Well, because it’s a classic example of out-of-the-box thinking when it comes to helping you drift off to the land of nod. This is why we decided to write a blog about how daridorexant works.

What is daridorexant

Daridorexant, known by the brand name Quviviq, is the new kid on the block when it comes to sleep medicines. It belongs to a class of drugs known as DORAs. No, they are not named after an intrepid explorer (if you have kids, you know who I am referring to), but rather, they stand for dual orexin receptor antagonist.

Daridorexant is the result of a highly tailored research program that sought an optimised sleep-promoting molecule that could last the whole night without having any lingering residual effects in the morning.

Before we go into more detail, let’s have a quick review of insomnia and the older sleeping pills and how they work.

Insomnia

We have all had that occasional night when we couldn’t sleep. It may be that you couldn’t get to sleep, that is, you had difficulties with sleep onset, or that you couldn’t stay asleep because you had a problem with sleep maintenance.

Insomnia is characterised by difficulties with sleep onset and/or sleep maintenance and impairment of daytime functioning. [1]

It is thought that chronic insomnia affects approximately 5-20% of the adult population. [2]

Insomnia can seriously impact the quality of life, causing daytime tiredness, altered mood and can impair memory. [3]

In addition to making you feel lousy, insomnia can have severe impacts on your long-term health and is associated with hypertension, diabetes and depression. [4]

Zopiclone and zolpidem

Zopiclone and zolpidem, known as the “Z drugs”, were popular choices for treating insomnia until they were found to be highly addictive and of limited benefit. They are classed as hypnotics and work by suppressing brain activity by increasing the effects of the neurotransmitter gamma-aminobutyric acid (GABA). [5]

So, the general idea was to knock you out with these drugs by turning off brain activity by enhancing the effects of GABA. Sure, they worked, but they also disrupted your normal sleep rhythm and had several side effects.

Zopiclone and zolpidem side effects

Zopiclone and zolpidem are associated with several side effects and can cause problems with movement and balance, leading to clumsiness or falls. They can also affect memory and thinking, making remembering or staying focused harder.

There’s also risk that people might misuse these  Z-drugs, becoming dependent on them, or need higher doses over time for the same effect. These issues limit how much and how long these medications can be safely used. [6]

How daridorexant works

Daridorexant is an example of left-of-field thinking. Rather than stick with the prevailing idea of suppressing brain activity, a sledgehammer-to-crack-a-nut approach, the researchers behind the daridorexant tried a more nuanced approach.

They thought, rather than turning the brain off, why don’t we turn off the switch that keeps us awake? This is a subtle but very important difference.

Daridorexant decreases wakefulness and thereby promotes sleep while not interfering with the natural sleep cycle. [7]

Orexin and wakefulness

DORAs such as daridorexant act through an entirely different mechanism of action than the classical sleeping tablets. Daridorexant targets two orexin receptors (OX1R and OX2R), blocking the effects of the orexin neuropeptides.

Orexin neurons are most active during periods of wakefulness and are virtually silent during sleep. [8] So, by stabilising the wake-promoting areas of the brain, the orexins keep us awake. This is fine during the day, but if we are wired but tired, we need something to switch off the wakefulness switch, and this is precisely what daridorexant or Quviviq does.

Selective targeting of daridorexant

Daridorexant or Quviviq selectively targets the activity of the wake-promoting neurons in the brain. It avoids the widespread inhibition of large areas of the brain that comes when you modulate the effects of GABA, such as occurs with the Z-drugs.

This means that daridorexant can help you drift off by switching off the lights in the wake-inducing areas of the brain without affecting other areas. It also means that it has fewer side effects than the older sleeping tablets.

Can I buy daridorexant in the UK?

Yes, daridorexant is available in the UK under the brand name Quviviq. You can now purchase daridorexant online from medicalmojo.co.uk after completing a short health questionnaire.

More help sleeping

Having trouble catching those Zs? Unsure about the right solution? Medical Mojo is here to support you with a FREE sleep consultation. We’ll guide you on the best methods to improve your sleep, whether it’s with melatonin, Quviviq, or personalised sleep coaching. Let us help you find the perfect sleep solution.

Disclaimer: This information is for educational purposes only and is not a replacement for professional medical advice.

References

1. American Academy of Sleep Medicine (2014) International Classification of Sleep Disorders – Third Edition (ICSD-3). American Academy of Sleep Medicine, Darien, IL
2. Roth, T., Coulouvrat, C., Hajak, G., Lakoma, M.D., Sampson, N.A., Shahly, V., Shillington, A.C., Stephenson, J.J., Walsh, J.K. and Kessler, R.C., 2011. Prevalence and perceived health associated with insomnia based on DSM-IV-TR; international statistical classification of diseases and related health problems, tenth revision; and research diagnostic criteria/international classification of sleep disorders, criteria: results from the America insomnia survey. Biological psychiatry, 69(6), pp.592-600.
3. Carey, T.J., Moul, D.E., Pilkonis, P., Germain, A. and Buysse, D.J., 2005. Focusing on the experience of insomnia. Behavioral sleep medicine, 3(2), pp.73-86.
4. https://www.ncbi.nlm.nih.gov/books/NBK19961/
5. Atkin, T., Comai, S., Gobbi, G. and Barker, E.L., 2018. Drugs for insomnia beyond benzodiazepines: pharmacology, clinical applications, and discovery. Pharmacological reviews, 70(2), pp.197-245.
6. Gunja, N., 2013. In the Zzz zone: the effects of Z-drugs on human performance and driving. Journal of Medical Toxicology, 9, pp.163-171.
7. Boss, C., Gatfield, J., Brotschi, C., Heidmann, B., Sifferlen, T., von Raumer, M., Schmidt, G., Williams, J.T., Treiber, A. and Roch, C., 2020. The quest for the best dual orexin receptor antagonist (daridorexant) for the treatment of insomnia disorders. ChemMedChem, 15(23), pp.2286-2305.
8. Azeez, I.A., Del Gallo, F., Cristino, L. and Bentivoglio, M., 2018. Daily fluctuation of orexin neuron activity and wiring: The challenge of “chronoconnectivity”. Frontiers in pharmacology, 9, p.1061.

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