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Where Does It Come From?
In the early 70’s a drug was discovered that would promote wakefulness in a similar way to Amphetamines, without the same nasty side effects. This drug was called Adrafinil.
Later on, scientists discovered that once the drug entered the body, it would be converted into 2 compounds; modafinil, and modafinilic acid. The later compound was found to be inactive, but the first metabolite remained active for several hours in the bloodstream. The research team behind the discovery, Lafon Labs, then decided to shift their focus to this active metabolite.
Since this time, Lafon Labs has been bought out by a much larger pharmaceutical company that went on to develop the drug, and made it available for use throughout the rest of the world. Hundreds of millions of dollars profit has since been made on this medication as a treatment for narcolepsy and ADD/ADHD. The United States military has even conducted research on the drug for use with its special forces military operations as an aid to help them stay awake and alert on tough, overnight missions.
The original Modafinil offered for sale was the brand name product by Cephalon Inc called Provigil®, which is still available today with a doctors prescription.
A few years after its launch, Cephalon Inc developed another drug, called R-Modafinil, which was in fact a specific enantiomer (R-modafinil) of modafinil.
In other modafinil products, there are both the R- and S- enantiomers of the drug. Researchers believe that the R- enantiomer is the most psychologically active, leading them to the development of a product they call Nuvigil®.
There are now over 20 different modafinil and R-Modafinil (AKA Armodafinil) generic drugs available for purchase. Most of these can be purchased online without the need for a prescription.
Indications
- ADD/ADHD
- Narcolepsy
- Shift workers experiencing sleep disturbances
- As a study aid for getting through tough projects (note recommended long term)
- To improve overall productivity
- Chronic fatigue syndrome
Contraindications
- Hypertension
- If taking other psychotropic drugs or medications
- Long term use not recommended
Drug/Nutrient Interactions
- SSRIs
- SNRIs
- Tricyclic antidepressants
Chemical Description:
Modafinil is a synthetic benzhydryl sulfinyl compound. It is sold as a racemic mixture of its R- and S-enantiomers, whereas armodafinil contains only the longer-acting R-enantiomer.
Pharmacodynamics:
Modafinil promotes wakefulness without the strong stimulant profile of amphetamines. It acts as a dopamine reuptake inhibitor and engages hypothalamic pathways that regulate the sleep–wake cycle.
Pharmacology & Medical Research
Modafinil is understood to promote wakefulness primarily by inhibiting dopamine reuptake and by influencing hypothalamic wakefulness pathways. It has been studied for narcolepsy, shift-work sleep disorder and the effects of sleep deprivation on cognitive performance and alertness.
Synergy:
Modafinil is generally used on its own under medical supervision rather than combined with other stimulants, which can increase the risk of side effects.
Modafinil Alternatives:
Closely related options include adrafinil, a prodrug that the body converts into modafinil, and armodafinil (brand name Nuvigil®), the longer-acting R-enantiomer of modafinil.
References:
- Loland, C. J., Mereu, M., Okunola, O. M., Cao, J., Prisinzano, T. E., Mazier, S., … & Newman, A. H. (2012). R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse. Biological psychiatry, 72(5), 405-413.
- Wesensten, N. J. (2006). Effects of modafinil on cognitive performance and alertness during sleep deprivation. Current pharmaceutical design, 12(20), 2457-2471.
- Wesensten, N. J. (2006). Effects of modafinil on cognitive performance and alertness during sleep deprivation. Current pharmaceutical design, 12(20), 2457-2471.