The history of Modafinil began with the development of Adrafinil, a stimulant drug that was originally developed in France in the 1970’s by Lafon laboratories who later leased its rights to Cephalon, a United States company in 1993. The development of Adrafinil followed the invention of a series of chemicals categorized as benzhydrylsulfinyl. Adrafinil was used to treat narcolepsy and temporarily reduce the need for sleep among healthy individuals. This was in 1986 after it was discovered to enhance wakefulness and vigilance. However, as chance would have it, Modafinil was later on discovered as the primary metabolite and active component of Adrafinil. It was also observed that Modafinil as treatment for narcolepsy had fewer side effects and greater strength compared to Adrafinil.
Key Medical Uses
The new discovery forced France to adopt Modafinil for medical use back in 1994 and discontinue use of Adrafinil for clinical purposes. However, in the United States, it was not until 1998 that the FDA officially approved it and it started to sell under the name Provigil as a relief for narcolepsy and hypersomnia. Early studies reveal that Modafinil helped persons with these conditions stay awake during the day and still have normal sleep patterns at night. The study showed no sign of tolerance or dependency on the drug. Later, people with obstructive sleep apnea and shift work sleep disorder were also noted to benefit from use of Modafinil.
Common Occupational Use/Cognitive-Enhancing Applications
Today however, the uses of Modafinil go beyond treating sleeping disorders. It is now widely used off-license as a cognitive enhancing drug where qualities such as concentration and alertness are needed. Previous studies showed that individuals that used Modafinil to treat sleep disorders benefited from these qualities but there is still little scientific consensus on its effectiveness as a cognitive enhancer in healthy individuals.
An evaluation of research papers written between 1990 and 2004 on cognitive enhancement related to Modafinil on non-sleep deprived individuals, found that the performance-enhancing ability of Modafinil varied depending on the task. It emerged that Modafinil consistently conferred cognitive abilities when a task was longer and more complex. It made no difference to working memory, but it did improve decision making and planning.
Modafinil is also thought to help with conditions such as ADHD, neurodegenerative disorder, cocaine addiction, weight loss and motion sickness. Studies on its particular effects on these conditions are however still ongoing. The drug has also stirred some controversy in the sporting scene which made World Anti-Doping Agency (WADA) include it among banned substances back in 2004.
Modafinil’s Action Mechanisms (Pharmacokinetics)
With a bioavailability of more than 80% of the dose taken, Modafinil permeates the brain system by inducing and inhibiting various body components such as enzymes. However, this percentage changes with variations in concentration. For instance, most clinical forms of the pill show that only about 60% of the drug is bound to the consumer’s plasma proteins. Further, medical observations have established that the tablet is among the fastest-working nootropics as it reaches peak levels an estimated 2 to 3 hours after intake.
Like any other mind-stimulating formula out there, certain factors may markedly slow down the rate at which the dose is absorbed into the body. As opposed to many other pharmaceutical labels in the modern market, the mind enhancer can still spread to all the targeted anatomical sections even if the consumer hasn’t eaten any food. With a half-life that ranges between 10 and 12 hours, Modafinil’s ultimate effectiveness depends on three main considerations: CYP genotypes, the user’s kidney function, and the healthiness of one’s liver.
The substance, like most other orally consumed chemical blends, is metabolized in the liver and the resultant metabolite is taken out of the body through the kidney. According to several clinical studies, the amount of unaltered Modafinil that comes out of the body by urination ranges between 0% and 18.7% – varying from one user to another due to different physiological reasons. Besides the foregoing points, two of its major metabolites – Modafinil acid and Modafinil sulfone – have been found to be quite inactive. However, the latter has certain anticonvulsant effects. Nonetheless, none of the two contributes to the drug’s strong wakefulness-promoting qualities.
After the patented Modafinil tablet was launched and widely circulated among increasing millions of consumers for about 10 years, a number of other off-label variations started hitting the market. While these variations worked like Provigil (the original brand name) they were remarkably cheaper. In addition, these less costly began being mass-produced in many third world nations such as India and Pakistan. Although the general labels still produced the characteristic after-effects associated with Provigil, some users treated them with a little suspicion. However, some of them have so far satisfied thousands of devoted fans from across the world and thus established a great deal of consumer trust. While there are tens of these over-the-counter Modafinil versions, Armodafinil has become the most rave-reviewed of these off-label modifications.
The mass-produced tab is internationally considered as a highly potent enantiomer of Provigil – the patented trademark. While Provigil was initially viewed as the only okayed treatment for narcolepsy and shift-work sleep disorder by experienced medics worldwide, Armodafinil gradually established incomparable fame as an endearingly cheaper and more effectual Modafinil form, especially among non-prescription customers seeking cognitive enhancement.
As this non-patented brand name continued to gain greater acceptance in majorly informal circles among swelling thousands of nootropic fans, its consistent qualities as a truly more reliable cure for excessive daytime sleepiness and shift-work sleep problems became clearly evident as well. Today, Armodafinil is accepted as a perfected replacement that is not only markedly less expensive but also one that’s more widely available because it’s massively manufactured outside of Europe and North America. Nowadays, anyone can easily purchase the generic tablet over the internet even without necessarily needing a doctor’s prescriptive permit.
In 2007, Armodafinil received a raft of quite notable approvals that allowed its use in some clinical circumstances after a few medical studies proved its near-double effectiveness. Particularly, America’s FDA approved the pill’s use for alleviating key symptoms linked to obstructive sleep apnea, abnormal daytime sleepiness, and narcoleptic attacks. With Provigil’s patent expiry 9 years after inception, Cephalon(the patent-bearing Modafinil inventors) thoughtfully designed Armodafinil so as to create a relatively new pharmaceutical brand that could see them hold the older patent over for an extra 10 years.
According to many casual surveys and hundreds of conclusive scientific observations, Armodafinil is far stronger than Modafinil owing to its more purified version of the drug’s active enantiomer – the most wakefulness-promoting component of Modafinil. As such, this general pill occurs in relatively smaller doses of 50mg, 150mg, and 250mg. In contrast, Modafinil – comparably weaker based on laboratory studies – comes in conventional doses of 100mg and 200mg.
The foregoing dosage differences portray Armodafinil as a much more potent variation of Modafinil because a mere 50mg of the former is universally deemed to be able to confer palpable cognitive-boosting feelings on a first-time user. As a result of these thorough inquests that indicated that the newer form was evidently stronger than the original brand, Cephalon sought further FDA approvals with the ultimate goal of getting it registered as a certified treatment for mitigating jetlag. However, these concerted efforts proved less fruitful when health authorities finally refused to license Armodafinil for this largely unverified purpose.