Pitolisant, A Wakefulness Enhancing Agent

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Pitolisant is an H3 histamine receptor inverse agonist/antagonist and it is currently being studied for its potential as a treatment for schizophrenia and Parkinson’s disease. Its inhibiting action against the H3-receptor promotes wakefulness, alertness, and vigilance. This compound has been researched for the treatment of narcolepsy for which it has been granted an orphan drug status in Europe and the United States. Being a wakefulness enhancing agent, Pitolisant also has the potential to be approved for the treatment of cataplexy, shift work sleep disorder, and obstructive sleep apnea.

Chatters in online communities, particularly among ADHD, Alzheimer’s disease, Parkinson’s disease, nootropic, and bluelighter forums reveal that some members were also able to acquire Pitolisant from independent labs through bulk buying. This means that Pitolisant have been tested, albeit informally, for other purposes other than what is approved by the USFDA.

PitolisantAmong the researchers who developed this compound is, Dr. Jean-Charles Schwartz the same French scientist who was credited with the discovery of the H3 histamine receptor in 1983. This discovery led to the development of Pitolisant, which is the very first H3-receptor inhibitor. According to experts, the effectiveness of Pitolisant is comparable to that of Modafinil and another H3-receptor antagonist, Ciproxifan. Some users of Pitolisant even claim that its effects are even better that Modafinil. Some studies do indicate that it is indeed better in the sense that Pitolisant is well-tolerated more than Modafinil.

Apart from being an effective wakefulness promoting agent, Pitolisant was also observed to have nootropic effects on an animal study conducted in 2007. In the same study, the animals were also observed to have higher levels of dopamine and acetylcholine, suggesting that Pitolisant may also have dopaminergic and cholinergic properties.

The ability of Pitolisant to promote wakefulness, alertness, and vigilance undoubtedly contributes to its cognitive enhancing abilities. Given this capacity, an individual will be able to focus and concentrate more on any given cognitive task. Its observed potential as a cholinergic compound indicates that it may have the ability to improve one’s memory retention and recall, learning abilities, logical reasoning, and verbal fluency. All these abilities of Pitolisant not only make it a potent nootropic agent, but it also has the potential of becoming an alternative treatment for cognitive decline associated with aging and other neurological conditions.

The drug apparently also gives positive results even for purposes other than promoting wakefulness. Users from the online nootropic forums report a feeling of wakefulness that is similar to the one you get a few minute after getting up from bed. The users reported no edgy or racy feeling that often comes with amphetamines and xanthenes. They reported a feeling of heightened coherence and mental clarity that makes the cognitive processes operate more smoothly and almost effortlessly. Others noted a feeling of lucidity and the absence of any worries and anxieties.

One of the restrictive factors in using Pitolisant as a cognitive enhancer is the cost. An online seller of Pitolisant is offering the drug at $480/50mg. Bulk buyers from online communities report spending approximately $50 per gram of pure Pitolisant powder, which is to be dissolved in saline solution and administered intravenously in 30 to 50mg doses daily. Pitolisant has been observed to make an individual more sensitive to cold temperatures. While Pitolisant is well-tolerated, it is known to have some mild side effects such as upset stomach, light headedness, nausea, and headaches.

PROS

  1. It is an effective wakefulness promoting agent.
  2. It can also improve alertness, mental lucidity, and vigilance.
  3. It has been observed to have cognitive enhancing properties.
  4. It has other potential medical applications.
  5. It has very low to no abuse potential.

CONS

  1. It is only available via prescription.
  2. It is expensive.
  3. Trustworthy online suppliers are very limited.
  4. Its long term effect is not known.

The doses for prescription Pitolisant is set at 5 to 20mg daily. Taking large doses like 30 to 50mg daily may be safe but is not advised. It is always best to consult your doctor first before trying out any supplement or drug.

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