Those in the know are forecasting a sweep of the gold for the Swiss pharmaceutical company Actelion in the coming 2012 Olympics of Sleep. Their candidate, Almorexant, has been in serious training since his discovery in 1998. He is expected to take gold medals in all of the following events:
- Prescription for Insomnia
- Enhancer for Dreams
- Catalyst for Memory
- Stimulant for Creativity
- Accelerant for Performance
- Depressant for Obesity
No single country, nor any sleep medication currently available has come close to winning in all categories. Most have left participants sluggish, depressed, agitated, confused, and complaining of muscle aches during the day.
Almorexant, already in Phase III testing and development, will probably take home the gold in the competition for sleep in 2012. The testing now is to determine low dosage levels, effects of increasingly higher dosage levels, and side effects compared to currently used sleep medications. Amorexant, was discovered and developed by the Swiss pharmaceutical company, Actelion. Imagine the worldwide market for a drug that will help insomnia victims, that will improve REM sleep and therefore enhance your dream state, that will act as a catalyst to improve memory consolidation, that will stimulate your creativity through reorganization of memory parcels, that will accelerate performance, and will also depress the brain’s feeding regulation and therefore depress 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 feeding regulation or appetite. Almorexant’s main ingredient acts as an antagonist to the orexin receptors in the brain.
The active ingredient, orexin-RA-1, when given to rats, was found to stimulate sound sleep and peak performance in maze tests the following morning. They outperformed all of the rats given conventional sleep medications, suggesting improved memory capacity. “Measurements of muscle tone and brain activity revealed an increase in the dream phase of sleep. The dream phase of sleep is when memory is hardwired in the brain,” says Actelion CEO Jean Paul Clozel.
Shahrad Taheri, at 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 the orexin neurons of the brain are active during waking hours and that they are silent during sleep. The orexin antagonist, orexin-RA-1, has been proven to be much more effective than melatonin, benzodiazepines, opiates, and histamines in brain penetration, increasing total sleep time, REM stage sleep time, acceleration time to fall asleep, and it does not cause motor impairment like the other sleep medications.
Isaac Kobrin, M.D. and previous Head of Clinical Development at Actelion and now Chief Medical Officer at Actelion, concluded in Medicalnewstoday.com attests to almorexant’s positive affects on both REM and non-REM sleep. He believes it results in better next day performances than benzodiazeprine medications.
So far there have been no reports of adverse effects or safety issues in the tests that have been completed. With over 80 million Americans suffering from sleeplessness and 25 million or more of those with chronic insomnia, almorexant is poised to take the gold medals expected in 2012 and to 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 decrease of 1.2% from 2007. The second most popular sleep aid, Lunesta, was #47, recording $771,019 in retail sales and an increase of 8.2% from 2007. Just to compare #’s, the #1 prescribed drug in 2008 was Lipitor, the cholesterol depressor, which recorded $5,880,128 in retail sales, and that was a decrease of 4.6% from 2007. Ambien CR and Lunesta can both 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 Champion of Sleep, the Wonder Drug of Dreams, and its name will become as familiar on television as Michael Phelps. The millions of sleep deprived people in the world will finally obtain the “good night’s rest” they deserve as well as the sweet dreams to improve memory, creativity, and performance.