Modafinil, known chemically as benzhydrylsulphinylacetamide, is a central stimulant (psychostimulant). It is FDA approved for the treatment of narcolepsy (a disorder characterized by sudden and uncontrollable attacks of deep sleep, mental fatigue, or excessive sleepiness), sleep apnea, and SWSD (Shift Work Sleep Disorder). It is being investigated for a number of other uses, including the treatment of Alzheimer’s disease, depression, and attention deficit disorder. Modafinil belongs to a group of drugs known as Eugeroics (“good arousal"), designed to promote a mental state of vigilance and alertness. One of its known mechanisms is to work as an alpha-1 adrenoceptor agonist, exerting its mood and energy enhancing effects through the increased release of dopamine in the CNS. It also results in alterations in local GABA and glutamate levels. The use of modafinil as a stimulant has been shown in studies to have many advantages over amphetamines. To begin with, it is believed to have a much lower potential for abuse due to the fact that it produces a lower sense of euphoria. It also displays lower peripheral CNS stimulation (less side effects), has minimal effects on blood pressure, produces no interruptions in normal sleeping patterns (no hangover or needing “catch-up” sleep), and has an overall greater safety profile according to clinical trials. This drug is of interest even to the U.S. military, which is looking at it as an energy enhancer for pilots and combat soldiers that need to operate for long periods of time without sleep.This is not as unusual as it may seem at first, as military combat pilots and soldiers have used Dexedrine (an amphetamine) extensively in the past when sleep was inconvenient. Soldiers on modafinil often report that they maintain excellent cognitive functioning for up to 40 hours without sleep, and have fewer side effects than Dexedrine. Modafinil has been tested in recent combat situations such as in Afghanistan and Iraq, and seems poised for official acceptance as a battlefield drug. Recently, modafinil has become a popular drug among competitive athletes. They use it not simply to “stay awake” but as a performance enhancing agent with both stimulant and endurance-increasing properties. This type of use probably comes as a surprise to those who developed this drug, as early reports suggested that this was a “mild” alertness drug, without strong stimulant properties that would improve athletic performance. Recent studies contradict this determination. A study conducted in Canada shows a very strong athletic benefit inherent in modafinil. During this double-blind investigation, a dose of 4 mg per kg of bodyweight (this equates to 200 mg for a 220lb man) of modafinil, or placebo, was given to a group of 15 male volunteers. Three hours after ingestion, aerobic exercise was conducted on a cycle ergometer at 85% V02max (maximum aerobic power), and the amount of time until exhaustion was determined. While taking modafinil, the men were able to exercise for significantly longer periods of time (~30%), and had greater oxygen intake at exertion. They also reported lower subjective ratings of perceived exertion (RPE), which suggests that the increased performance was in part due to a significantly less pronounced sensation of fatigue during exercise.
| Brand name | Provigil, Modafinil, Modiodal, Vigil, Alertec, Modasomil |
Modafinil History
Modafinil was developed by Lafon Laboratories in France. It was approved for sale in the United States by the FDA in 1998, where it was introduced under the Provigil brand name. Modafinil is also found internationally under this and several additional trade names including Modiodal, Vigil, Alertec, and Modasomil. Although the drug appears to have a favorable safety record and profile, it was quickly considered a drug of potential abuse in the U.S. It is presently classified as a schedule IV controlled substance, which places modafinil in the same category as Valium and Xanax. This is intended to limit its diversion for nonmedical purposes by placing considerable legal penalties on its possession and importation. The medical applications for the drug are fairly broad, however, including SWSD, which refers to sleep disturbances caused by changing- or late-shift work. Prescriptions for the drug are, likewise, commonly granted by physicians in general medical practice.
Modafinil quietly became popular among competitive athletes between 2000 and 2004, before the athletic bodies were aware of the drug. Its use as a performance-enhancing agent was revealed to the public during the designer steroid (BALCO) doping scandal of 2004, however, when it was disclosed that many of the same athletes who tested positive for THG also used modafinil.The IOC quickly banned its use, and with the help of a number of researchers a methodology for detecting this chemical in the urine was developed. This test is now implemented as part of the standard Olympic level drug screening process. Most of the other international athletic bodies have followed the IOC’s lead in banning and testing for modafinil. The drug has since lost all appeal as an “invisible” performance-enhancing agent, although is still being used by many athletes that are not subject to random urine testing.
How is Modafinil Supplied
Modafinil is most commonly supplied in tablets of 100 mg and 200 mg each.
Structural Characteristics of Modafinil
Modafinil is a central nervous system stimulant related to adrafinil. It has the chemical designation 2- [(diphenylmethyl)sulfinyl]acetamide.
Modafinil Side Effects
Side effects associated with modafinil are commonly the result of its central nervous system stimulating activities, and may include nervousness, insomnia, shakiness, euphoria, personality changes, and excitation. The drug may also produce gastrointestinal disturbances such as nausea, vomiting, abdominal pain, dry mouth, anorexia, and headache. Hypertension, heart palpitations, or abnormal heart rate may also be noticed. In rare instances allergic rash, increases in alkaline phosphatase, or impaired voluntary movement have been reported.
Modafinil Administration
When used clinically to treat excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea, the recommended dose is typically 200 to 400 mg per day. This may be given in a single morning application, or in two divided doses (morning and at midday). When used to enhance physical performance, the typical effective dose is in the range of 100-400 mg. This is often given at least 2-3 hours prior to athletic competition. Note that side effects can be dose dependant. It is often advised to start using modafinil on the low end of the effective dosage range, and increase by 50-100 mg per application until an optimal level is determined.
The arenas in which this drug is applied are vast, and essentially include any sport focused on aerobic activity or endurance. It may also work well with those athletes focused on short repeat bursts of strength or speed (anaerobic activities), such as shot-putting, pole-vaulting, or long-jumping. Modafinil is not a popular drug among bodybuilders, as it holds little direct value for building muscle or reducing body fat levels. Some, however, do find it to be an effective pre-workout stimulant, especially during periods when fatigue or loss of physical drive may be noticed subsequent to a busy work or personal schedule.
Modafinil Availability
Modafinil is presently available in more than two dozen countries. The drug is not highly diverted for black market sale, however, and is not a lucrative target for drug counterfeiting operations.
References
Wlliam Llewellyn (2011) - Anabolics
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