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Adrafinil: A Novel Vigilance Promoting Agent
Norton W. Milgram, Heather Callahan, and Christina Siwak
Division of Life Sciences, University of Toronto at Scarborough,
Toronto, Ontario, Canada
INTRODUCTION
Behavioral stimulants have widespread potential application in the treatment of af-
fective disorders, disorders of vigilance, and disorders of sleep. Most behavioral stimu-
lants, however, must be used with extreme caution because of undesirable side effects that
include stereotypy, anxiolytic effects, and addiction. Adrafinil, developed in France by
Louis Lafon Laboratories, is a novel pharmaceutical that has behavioral-activating effects
but lacks the undesirable side effects of other stimulants. Peripheral sympathomimetic ef-
fects are also absent in subjects treated with adrafinil. Jouvet (36) introduced the term
iheugrégoriquelv (eugregoric in English) to characterize this unique type of arousal-pro-
ducing agent, but the term is not widely used in the scientific literature. 1 There have not
been many published studies on adrafinil, and the large majority of studies have been pub-
lished in French. Human studies indicate that adrafinil has clinical efficacy as a vigi-
lance-promoting and mood-enhancing agent in the elderly. As an area for therapeutic in-
tervention, vigilance enhancement has received much more attention in Europe than in
North America. Somewhat surprisingly, perhaps, adrafinil is known to a larger nonscienti-
fic audience, where it is considered to be a nootropic agent.
The literature on modafinil, the primary metabolite of adrafinil is much more ex-
tensive. This work has largely focused on the potential application of modafinil in the
treatment of sleep disorders, and modafinil has recently received regulatory approval for
the treatment of narcolepsy in the United States. Since the types of clinical trials that have
been conducted differ (vigilance enhancement for adrafinil vs. narcolepsy for modafinil),
it is not clear whether modafinil effectively replaces adrafinil or whether the two com-
pounds are uniquely valuable for different applications. Most investigators assume that
193
CNS Drug Reviews
Vol. 5, No. 3, pp. 193Œ212
© 1999 Neva Press, Branford, Connecticut
Address correspondence and reprint requests to Prof. N. W. Milgram, Division of Life Sciences, University of
Toronto at Scarborough, 1265 Military Trail, Scarborough, Ontario M1C 1A4, Canada.
Fax: (416) 287-7642. E-mail: [email protected].
1 The origins come from the Greek ireuln meaning good and ingregorl. meaning wakening.
Adrafinil
Amazing Breakthrough In
Perception Stimulation.
Reprinted from Offshore Medical Therapies
Even though the aging process does not always lead to dementia, it is a sad fact that unusual fatigue and lowered mental energy are often very common, even amongst so-called "middle-aged" people1.
The good news is that a French drug therapy is now available to combat this worrying condition. This new breakthrough is called ADRAFINIL, and is usually sold under the brand name OLMIFONTM. Thus, it has now become possible to effectively treat this decline in mental ability.
WHY DOES ADRAFINIL WORK?
Adrafinil works directly on special receptors in the brain, these are called postsynaptic receptors2,3. Since adrafinil works directly on those sites which control alertness and does not interfere with any other brain function, it has been a very successful treatment. (It should be noted that this direct action means that mental stimulation is achieved WITHOUT raising blood pressure or affecting heart rate).
Adrafinil acts on the chemical processes of the brain to prevent the loss of alertness and the depression that occurs with increasing age 4,5.
Adrafinil is a completely new substance, unique in its special action on alertness.
NEW DRUG DISCOVERY.
You will note that adrafinil is the first of, what will almost certainly be, a whole new generation of safe, non-addictive antidepressants.
Adrafinil is the founder member of this new generation of drugs, which are known as "eugregorics" (eu=good, gregor=arousal)6.
The main properties of a eugregoric substance are:
improved short term memory. improved attention and concentration.
enhanced clarity of thought.
normalization of sleep patterns.
less mental fatigue.
higher quality of self-awareness.
raised levels of optimism and enthusiasm for day to day life.
freedom from depression.
These benefits are experienced by almost all adult age groups.
Adrafinil is the only eugregoric drug that is currently available.
Adrafinil allows a restoration of daytime alertness and studies indicate that it helps to prevent brain aging7,8. Adrafinil can be effectively used to correct ALL of the following conditions:
general physical and mental fatigue.
loss of initiative.
reduction of motor activity.
lack of, or decline of interest in social events.
a drop in intellectual ability and a lack of new ideas.
memory problems and a fall in efficiency, productivity and creativity.
WHAT ARE THE BENEFITS?
A fascinating aspect of adrafinil is its unusual way of working - different effects occur as the course of treatment is continued.
Adrafinil has three distinct effects which occur at different times during the treatment period. We list below an approximate timetable of events:
1) After 8 to 10 days of treatment, motor effects are seen:
Increased "get up and go", which permits the return of full physical activity.
An improvement in the ability to "get things done".
Muscular fatigue and motor blocks disappear.
2) After 15 days of treatment, there is a powerful re-energizing effect on activity, which allows a full restoration of functional ability, improved desire to take a full part in life and enhanced energy levels.
3) After 1 to 3 months of treatment, cognitive effects are seen. Intellectual function is improved, in particular, the ability to formulate new ideas and recall information.
AN ALERTNESS BOOST.
The effects of adrafinil are totally different from the other psychostimulants such as amphetamine, caffeine etc. Common stimulants like caffeine, only lead to fleeting and sterile stimulation, not to mention the problems of tolerance which occur when they are used for long periods.
ATTITUDE IMPROVEMENT.
Adrafinil can produce amazing improvements in a person's general attitude:
absent-mindedness becomes concentration
irritability becomes tranquillity.
bad moods become good moods.
quiet people become talkative.
reserved people become open.
passive people become active.
drowsy people become wide-awake.
Adrafinil's stimulating properties are NOT produced by amphetamine methods, thus it can be safely used without fear of addiction. In addition to this adrafinil benefits are both therapeutic and long-lasting, helping to restore decision making abilities and the mental functions which allow a better adaptation to both the working and social environments
SUMMARY.
Adrafinil (sold as OlmifonTM) is an exciting and unique development in the battle against brain aging and the subsequent decline in mental function. For the past 3 years adrafinil has been used to treat Alzheimer's victims in France9,10. Sadly, although it cannot cure the disease, initial indications are that it can certainly arrest the development of senile dementia during the early stages of mental decline.
Whilst adrafinil is not a cure for senile dementia, scientific studies show that it may well be the much sought after preventative to mental deterioration. This is in addition to its remarkable antidepressant effects.
Adrafinil can be used to increase intellectual ability and creativity and could be of special value to the following groups:
computer enthusiasts.
artists and writers or any involved in creative activities.
those studying for examinations.
those looking to increase their social skills.
DOSAGE.
2 to 4 tablets per day. Adrafinil is a powerful brain stimulant and this dose should not be exceeded. In contrast to stimulants like amphetamine and caffeine, adrafinil does not disturb sleep patterns.
Some people can experience mild agitation and feelings of aggression or excitement when they first start the treatment. If this occurs, the dose is reduced until the symptoms disappear. Gradually increase the dose over a period of time until the best tolerated level is reached.
Most people find that adrafinil is well tolerated.
Under 65 years of age take 1 to 2 tablets in the morning and at midday, preferably with food.
70 years of age and above take 1 tablet in the morning and at midday, preferably with food.
The reduced dosage for the older person is due to the increased sensitivity of the elderly to this therapy.
CAUTIONS.
Adrafinil has a good safety record, however, there a number of important precautions. Those with epilepsy, liver or kidney impairment should not use adrafinil.
Adrafinil should not be used along with major tranquillizers, e.g. pimozide, haloperidol, chlorpromazine etc.
Prolonged treatment (i.e. in excess of 5 months) should be avoided unless the level of the enzyme alkaline phosphatase is monitored.
Norton W. Milgram, Heather Callahan, and Christina Siwak
Division of Life Sciences, University of Toronto at Scarborough,
Toronto, Ontario, Canada
INTRODUCTION
Behavioral stimulants have widespread potential application in the treatment of af-
fective disorders, disorders of vigilance, and disorders of sleep. Most behavioral stimu-
lants, however, must be used with extreme caution because of undesirable side effects that
include stereotypy, anxiolytic effects, and addiction. Adrafinil, developed in France by
Louis Lafon Laboratories, is a novel pharmaceutical that has behavioral-activating effects
but lacks the undesirable side effects of other stimulants. Peripheral sympathomimetic ef-
fects are also absent in subjects treated with adrafinil. Jouvet (36) introduced the term
iheugrégoriquelv (eugregoric in English) to characterize this unique type of arousal-pro-
ducing agent, but the term is not widely used in the scientific literature. 1 There have not
been many published studies on adrafinil, and the large majority of studies have been pub-
lished in French. Human studies indicate that adrafinil has clinical efficacy as a vigi-
lance-promoting and mood-enhancing agent in the elderly. As an area for therapeutic in-
tervention, vigilance enhancement has received much more attention in Europe than in
North America. Somewhat surprisingly, perhaps, adrafinil is known to a larger nonscienti-
fic audience, where it is considered to be a nootropic agent.
The literature on modafinil, the primary metabolite of adrafinil is much more ex-
tensive. This work has largely focused on the potential application of modafinil in the
treatment of sleep disorders, and modafinil has recently received regulatory approval for
the treatment of narcolepsy in the United States. Since the types of clinical trials that have
been conducted differ (vigilance enhancement for adrafinil vs. narcolepsy for modafinil),
it is not clear whether modafinil effectively replaces adrafinil or whether the two com-
pounds are uniquely valuable for different applications. Most investigators assume that
193
CNS Drug Reviews
Vol. 5, No. 3, pp. 193Œ212
© 1999 Neva Press, Branford, Connecticut
Address correspondence and reprint requests to Prof. N. W. Milgram, Division of Life Sciences, University of
Toronto at Scarborough, 1265 Military Trail, Scarborough, Ontario M1C 1A4, Canada.
Fax: (416) 287-7642. E-mail: [email protected].
1 The origins come from the Greek ireuln meaning good and ingregorl. meaning wakening.
Adrafinil
Amazing Breakthrough In
Perception Stimulation.
Reprinted from Offshore Medical Therapies
Even though the aging process does not always lead to dementia, it is a sad fact that unusual fatigue and lowered mental energy are often very common, even amongst so-called "middle-aged" people1.
The good news is that a French drug therapy is now available to combat this worrying condition. This new breakthrough is called ADRAFINIL, and is usually sold under the brand name OLMIFONTM. Thus, it has now become possible to effectively treat this decline in mental ability.
WHY DOES ADRAFINIL WORK?
Adrafinil works directly on special receptors in the brain, these are called postsynaptic receptors2,3. Since adrafinil works directly on those sites which control alertness and does not interfere with any other brain function, it has been a very successful treatment. (It should be noted that this direct action means that mental stimulation is achieved WITHOUT raising blood pressure or affecting heart rate).
Adrafinil acts on the chemical processes of the brain to prevent the loss of alertness and the depression that occurs with increasing age 4,5.
Adrafinil is a completely new substance, unique in its special action on alertness.
NEW DRUG DISCOVERY.
You will note that adrafinil is the first of, what will almost certainly be, a whole new generation of safe, non-addictive antidepressants.
Adrafinil is the founder member of this new generation of drugs, which are known as "eugregorics" (eu=good, gregor=arousal)6.
The main properties of a eugregoric substance are:
improved short term memory. improved attention and concentration.
enhanced clarity of thought.
normalization of sleep patterns.
less mental fatigue.
higher quality of self-awareness.
raised levels of optimism and enthusiasm for day to day life.
freedom from depression.
These benefits are experienced by almost all adult age groups.
Adrafinil is the only eugregoric drug that is currently available.
Adrafinil allows a restoration of daytime alertness and studies indicate that it helps to prevent brain aging7,8. Adrafinil can be effectively used to correct ALL of the following conditions:
general physical and mental fatigue.
loss of initiative.
reduction of motor activity.
lack of, or decline of interest in social events.
a drop in intellectual ability and a lack of new ideas.
memory problems and a fall in efficiency, productivity and creativity.
WHAT ARE THE BENEFITS?
A fascinating aspect of adrafinil is its unusual way of working - different effects occur as the course of treatment is continued.
Adrafinil has three distinct effects which occur at different times during the treatment period. We list below an approximate timetable of events:
1) After 8 to 10 days of treatment, motor effects are seen:
Increased "get up and go", which permits the return of full physical activity.
An improvement in the ability to "get things done".
Muscular fatigue and motor blocks disappear.
2) After 15 days of treatment, there is a powerful re-energizing effect on activity, which allows a full restoration of functional ability, improved desire to take a full part in life and enhanced energy levels.
3) After 1 to 3 months of treatment, cognitive effects are seen. Intellectual function is improved, in particular, the ability to formulate new ideas and recall information.
AN ALERTNESS BOOST.
The effects of adrafinil are totally different from the other psychostimulants such as amphetamine, caffeine etc. Common stimulants like caffeine, only lead to fleeting and sterile stimulation, not to mention the problems of tolerance which occur when they are used for long periods.
ATTITUDE IMPROVEMENT.
Adrafinil can produce amazing improvements in a person's general attitude:
absent-mindedness becomes concentration
irritability becomes tranquillity.
bad moods become good moods.
quiet people become talkative.
reserved people become open.
passive people become active.
drowsy people become wide-awake.
Adrafinil's stimulating properties are NOT produced by amphetamine methods, thus it can be safely used without fear of addiction. In addition to this adrafinil benefits are both therapeutic and long-lasting, helping to restore decision making abilities and the mental functions which allow a better adaptation to both the working and social environments
SUMMARY.
Adrafinil (sold as OlmifonTM) is an exciting and unique development in the battle against brain aging and the subsequent decline in mental function. For the past 3 years adrafinil has been used to treat Alzheimer's victims in France9,10. Sadly, although it cannot cure the disease, initial indications are that it can certainly arrest the development of senile dementia during the early stages of mental decline.
Whilst adrafinil is not a cure for senile dementia, scientific studies show that it may well be the much sought after preventative to mental deterioration. This is in addition to its remarkable antidepressant effects.
Adrafinil can be used to increase intellectual ability and creativity and could be of special value to the following groups:
computer enthusiasts.
artists and writers or any involved in creative activities.
those studying for examinations.
those looking to increase their social skills.
DOSAGE.
2 to 4 tablets per day. Adrafinil is a powerful brain stimulant and this dose should not be exceeded. In contrast to stimulants like amphetamine and caffeine, adrafinil does not disturb sleep patterns.
Some people can experience mild agitation and feelings of aggression or excitement when they first start the treatment. If this occurs, the dose is reduced until the symptoms disappear. Gradually increase the dose over a period of time until the best tolerated level is reached.
Most people find that adrafinil is well tolerated.
Under 65 years of age take 1 to 2 tablets in the morning and at midday, preferably with food.
70 years of age and above take 1 tablet in the morning and at midday, preferably with food.
The reduced dosage for the older person is due to the increased sensitivity of the elderly to this therapy.
CAUTIONS.
Adrafinil has a good safety record, however, there a number of important precautions. Those with epilepsy, liver or kidney impairment should not use adrafinil.
Adrafinil should not be used along with major tranquillizers, e.g. pimozide, haloperidol, chlorpromazine etc.
Prolonged treatment (i.e. in excess of 5 months) should be avoided unless the level of the enzyme alkaline phosphatase is monitored.
