Gaboxadol

Last updated: March 26, 2019

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Sleep disorders are extremely common and affect up to 40 percent of the general population. Sleep disorders can range from simple snoring issues to potentially life-threatening ones like sleep apnea. This is why we also have a wide range of treatments available. Some use non-pharmaceutical preparations while others rely on prescription medications. Some of these medication include benzodiazepines, antihistamines, and antidepressants.

More recently, we have seen the use of hypnotics as medications of choice for sleep disorders. New drugs are being developed to deal with the growing issue of sleep disorders. One such drug is Gaboxadol.

What is Gaboxadol?

Gaboxadol is a direct GABA receptor agonist. It is also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol or THIP. Gaboxadol was first synthesized by the Danish chemist Povl Krogsgaard-Larsen in 1977. This drug was the subject of a series of pilot studies conducted in the early 1980s. The aim of the said studies is to test the efficacy of Gaboxadol as an analgesic and anxiolytic. The also tested if the drug can become a treatment for tardive dyskinesia, spasticity, Alzheimer’s disease, and Huntington’s disease.

However, it was only in 1996 that researchers attempted to use Gaboxadol’s sedative effects as a treatment for insomnia. This was done through a series of clinical trials sponsored by Lundbeck and Merck. Unfortunately, Merck and Lundbeck canceled Gaboxadol research in 2007. Some of the reasons they cited were safety concerns and the failure of an efficacy trial.

Based on an article that appeared at in the New York Times, they claimed that the drug had unusual side effects. These include:

  • hallucinations
  • disorientation

In 2015, Lundbeck sold its rights to Gaboxadol to Ovid Therapeutics. Ovid Therapeutics plans to develop it for FXS and Angelman syndrome.

Is this the first time that medication for sleep disorder caused controversy?

No, Gaboxadol is not the first sleep disorder medication that caused controversy. Due to the side effects of sedatives or hypnotics, it shouldn’t be surprising to know that they’ve had their fair share of unwanted media attention.

For one, z-drugs have a high potential for medication misuse. There are also people who illegally use z-drugs for recreational use. This is due to the “high” that some patients get from using these drugs. The use of z-drugs can also lead to dependence. This happens when a patient uses these drugs for a long period of time at high doses. Although patients who have been dependent on other drugs in the past have a higher chance of getting dependent on z-drugs, dependence on z-drugs can develop in anyone who uses them in high dosages.

Ambien

Zolpidem is one of the most controversial sleep medications. This drug is better-known as the brand-name drug Ambien. In 2018, Ambien got dragged into the center of a controversy involving American comedienne Roseanne Barr. Roseanne Barr blamed Ambien for racist tweets that she sent. Sanofi US, the manufacturer of Ambien, has debunked her claims. Although they admitted that Ambien has pharmaceutical side effects, they denied that Ambien can cause racism.

More than a decade earlier, US Representative Patrick J. Kennedy of Rhode Island figured in a motor vehicle accident in 2006 in Washington, DC. Although authorities thought he was intoxicated on alcohol, the congressman claimed that the car crash was due to Ambien. Another member of the prominent Kennedy family, Kerry Kennedy, claimed in court that she figured in a separate car crash because of the effects of Ambien on her driving.

Z-drugs as a crime tool

Z-drugs can also be used as date rape drugs. These drugs are available legally by prescription. They are often slipped into drinks at nightclubs or bars. Because of their sedating effects, these drugs allow their users to overpower their victims. In most cases, victims under the sedating effects of z-drugs cannot fight back against their attackers. They also experience short-term amnesia that prevents them from remembering what happened to them. The use of z-drugs as date rape drugs got highlighted during the trial of Darren Sharper, an NFL player. Sharper used a potent mix of alcohol and sedating drugs to rape at least nine women. He got convicted of distributing controlled substances with intent to commit rape.

With the great number of people affected by sleep disorders, it is not surprising to find that new sleep disorder medications are always in development. Companies strive to come up with new medications that are effective and without adverse side effects. Unfortunately, Gaboxadol did not make it out of developmental stages. The number of unusual side effects and the lack of efficacy forced its researchers to abandon Gaboxadol trials.

And this may be good news for us. This means that companies are exerting efforts to ensure that we don’t get medications that won’t help us. They found out that the use of this drug might potentially harm patients, so they pulled the plug on it. Now, the rights to Gaboxadol belong to another company. We just hope that they can develop it for use as a treatment in other medical conditions and this time without any of the serious side effects.

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