Those in the know are forecasting a gold sweep for Swiss pharmaceutical company Actelion at the upcoming 2012 Sleep Olympics. Their candidate, Almorexant, has been in serious training since his discovery in 1998. He is expected to win gold medals. in all of the following events:
- Recipe for insomnia
- Dream enhancer
- Memory catalyst
- Stimulating for creativity
- Accelerator for performance
- Depressant for obesity
No country, nor any currently available sleep medication, has come close to winning in all categories. Most have left participants lazy, depressed, agitated, confused, and complaining of muscle aches during the day.
Almorexant, already in phase III testing and development, will likely take home the gold in the sleep competition in 2012. Testing now is for low dose levels, effects of higher and higher dose levels and side effects compared to currently used sleep medications. Amorexant, was discovered and developed by the Swiss pharmaceutical company Actelion. Imagine the world market for a drug that will help insomnia sufferers, that will improve REM sleep and thus improve their sleep state, that will act as a catalyst to improve memory consolidation, that will stimulate their creativity to through the reorganization of memory packages, which will speed up performance, and also depress the brain’s regulation of eating and thus reduce obesity. The drug has already shown that it can improve all of the above. Orexin, a neuropeptide produced by the hypothalamus, affects the body’s sleep-wake cycle, as well as the regulation of eating or appetite. The main ingredient in Almorexant acts as an antagonist of orexin receptors in the brain.
The active ingredient, orexin-RA-1, when administered to rats, was found to stimulate deep sleep and peak performance in maze tests the next morning. They outperformed all the rats given conventional sleep medications, suggesting better memory capacity. “Measurements of muscle tone and brain activity revealed an increase in the sleep phase of sleep. The sleep phase of sleep is when memory is programmed into the brain.” says Actelion CEO Jean Paul Clozel.
Shahrad Taheri from the University of Bristol believes that blocking the orexin system would result in a decrease in appetite and therefore a decrease in obesity.
Studies have shown that orexin neurons in the brain are active during waking hours and silent during sleep. The orexin antagonist, orexin-RA-1, has been shown to be much more effective than melatonin, benzodiazepines, opiates, and histamines in brain penetration, increasing total sleep time, sleep time in REM stage, the acceleration time to fall asleep, and it does not cause motor impairment like the other sleep medications.
Isaac Kobrin, MD and former Head of Clinical Development at Actelion and now Actelion’s Medical Director, concluded at Medicalnewstoday.com attesting to the positive effects of almorexant on both REM and non-REM sleep. He believes it results in better next-day performance than benzodiazeprine medications.
So far there have been no reports of adverse effects or safety concerns in the trials that have been completed. With more than 80 million Americans suffering from insomnia and 25 million or more people with chronic insomnia, almorexant is set to take the gold medals expected in 2012 and become one of the top ten drugs of the future. According to drugs.com, in 2008 the most popular sleep aid, Ambien CR, was # 43, recording $ 865,719 in retail sales and a 1.2% decrease from 2007. The second most popular sleep aid, Lunesta, was the # 47, posting $ 771,019 in retail sales and an 8.2% increase since 2007. Just to compare the #s, the # 1 prescription drug in 2008 was Lipitor, the cholesterol depressant, which posted $ 5,880,128 in retail sales, and that was a 4.6% decrease from 2007 Ambien CR and Lunesta can have serious side effects such as sluggishness, depression, memory problems, agitation, rapid heartbeat, confusion, decreased coordination and muscle aches, and more.
Almorexant, after testing and approval, will become the 2012 Olympic Sleep Champion, the wonder drug of dreams, and his name will become as familiar on television as Michael Phelps. The millions of sleep deprived people in the world will finally get the “good night’s rest” they deserve, as well as sweet dreams to improve memory, creativity and performance.
