Sleep Replacement Miracle Drugs For Narcoleptics and the Sleep Deprived World

Two miracle drugs for narcoleptics and the sleepless and tired world are in the testing stages. Arena Pharmaceuticals announced on March 24, 2010 that they will be doing Phase 1 clinical trial testing of APD916. APD916 is an oral drug that targets the histamine H3 receptor in the brain and, as an agonist, it stimulates histamine production which increases arousal. The second drug, already in testing, is Orexin-A, which is a naturally occurring brain hormone which increases arousal and cognitive functions. Approximately one in every 2,000 Americans are narcoleptic and more than 70% of Americans get less than the recommended 8 hours of sleep a night. Until these drugs are approved the sleepless and tired will be endangering themselves as well as the millions of people on the road with them every day

Narcolepsy, as described by Wikipedia, “is characterized by excessive daytime sleepiness (EDS) in which a person experiences extreme fatigue and possibly falls asleep at inappropriate times, such as while at work or at school.” The narcoleptic usually has problems sleeping at night and, unlike most of us, they “generally experience the REM stage of sleep within 10 minutes; whereas most people do not experience REM sleep until after 30 minutes.” These rapid transitions into deep sleep can lead to extremely dangerous situations if they happen at work or on the road. Other symptoms that often accompany narcolepsy are cataplexy (muscle function loss), sleep paralysis, hallucinations, and “automatic behaviors” (normal waking functions performed while asleep, but not remembered when awakened).

The protein, Orexin, produced in the brain, is responsible for appetite control as well as the regulation of sleep patterns. The direct cause of narcolepsy has not been found yet, but there appear to be links to gene defects in one or more of the chromosomes responsible for the production of the hypocretins (orexins) in the brain. Orexin production peaks during the hours of wakefulness. Findings published by have shown that dogs born without functioning hypocretin genes develop many symptoms of narcolepsy. Similar links have been found in mice.

Amphetamines are the current solution offered to sleep deprived individuals. They are often given to pilots, to truck drivers, and to military personnel on critical missions. These stimulants have many harmful side effects and they are also addicting. The more serious physical side effects are: headache, tachycardia, increased breathing rate, increased blood pressure, fever, diarrhea, blurred vision, dizziness, uncontrollable movements or shaking, insomnia, numbness, palpitations, arrhythmia, convulsions, and heart attack. The negative psychological side effects are: irritability, aggression, power and superiority feelings, obsessive behaviors, paranoia, and amphetamine psychosis. The side effects are frightening, the addiction problem is well documented, and the withdrawal problems can be even more problematical.

Modafinil (Provigil) is another stimulant used to treat narcolepsy and sleep deprived individuals. It was approved by the FDA in 1998 and it has been used effectively by the US, the French, the British, and the Canadian militaries. Our Air Force refers to it as the “Go Pill,” and it is used in aircraft where there are two pilots. Modafinil stimulates histamine production and it does not have the drastic side effects of the amphetamines. Nausea, dizziness, and vertigo have been reported in much lower frequency. The long term effects are still in question. Abuse potential is minimal, as is the cardiovascular stimulation found with the amphetamines.

Neither amphetamine treatments, nor modafinil treatments attack the orexin deficiencies linked to narcolepsy. A study presented to the Associated Professional Sleep Societies in 2007 showed that histamine producing neurons and orexin producing neurons have direct roles in the control of wakefulness. The research concluded that both neurons have “synergistic and complimentary” roles. APD916, from Arena Pharmaceuticals, assists the histamine producing neurons and Orexin-A is a naturally occurring peptide in the brain. Both attack the deficiencies responsible for our sleepless and tired feelings and the symptoms of narcolepsy.

A study conducted at Wake Forest University School of Medicine found that the effects of sleep deprivation were reversed when Orexin-A was administered to monkeys in either intravenous or intranasal formats. The intranasal spray produced superior results when compared to the intravenous injections. When the monkeys were not sleep deprived the Orexin-A did not have any effect on their performance levels. The potential for the intranasally administered Orexin-A is reported in Molecular Interventions. The spray’s potential is far greater due to its ease of application and its quick results.

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