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Re: Here's a bunch of stuff all about Adrafinil

Posted by JohnL on August 2, 2001, at 5:46:03

In reply to What is Adrafinil and what is it suppose to do?, posted by gldngodess on August 1, 2001, at 23:39:57

> Does anyone know about Adrafinil and what it is suppose to be good for?
> Thank you-
> KL


Rapidly restores vigilance and alertness in older people and the physically and mentally tired. Has a powerful
antidepressant action far superior to that of fluoxetine (Prozac) and clomipramine (Anafranil) and is without any serious
side effects. Adrafinil restores your powers of concentration, memory and intellectual function. When administered to
older people who have lost interest in life, adrafinil makes them want to take part in life again and they find that they
have renewed energy and vigor. Adrafinil may be correctly described as an anti-aging drug because it directly combats
degeneration in the part of the brain that allows you to take pleasure in life. Elderly people very often have disturbed
sleep patterns and take many naps during the day. Adrafinil restores a youthful sleep/wake cycle of full alertness in the
daytime and deep restorative sleep at night. After several weeks of treatment with Adrafinil daytime sleepiness
disappears, interest in intellectual activity is restored and depression lifts. It is very important to note that this improved
quality of alertness is NOT accompanied with mental excitation and insomnia as occurs with amphetamine or caffeine.
The correct dosage is 300 to 600 mg per day. The dosage can be adjusted according to response. Remember it takes
three weeks for all the effects of Adrafinil to become apparent. Do not use Adrafinil if you have any type of kidney or liver
problem or if you suffer from epilepsy.

ADRAFINIL: What is; (a.k.a. Olmifon) (Description & information below)
NOTE:not to be confused with "Anafranil (a.k.a. clomipramine)" the Antidepressant.

Adrafinil provides alertness in most without the feeling often felt with stimulants that usually are prescribed for a person with
narcolepsy. Such as amphetamines etc. Also the possibility of tolerance is low with its continued use. There is however a
need for certain Liver function tests
on a regular basis with its continued use. Normally the same types of required testing as with the medication " cylert " which is
commonly prescribed in the USA. It is also used in certain parts europe as a "antidepressant". It is the combination of
Adrafinil's releasing stimulantive arousal effect(s), and its antidepressant effects that some doctors in europe recommend
Adrafinil over its newer form of Modafinil. There have been studies done in the United States "measuring depression in
individuals with sleep disorders",. In one study it was suggested that the
"rate of narcolepsy and depression is estimated to be between 30-52%".


Adrafinil: Alertness Without Stimulation

Adrafinil is the prototype of a new class of smart drug - the eugeroics (ie, "good arousal") - designed to promote vigilance
and alertness. Developed by the French pharmaceutical company Lafon Laboratories, adrafinil (brand name, Olmifon) has
been approved in many European countries for treating narcolepsy, a condition characterized by excessive daytime sleepiness
and other unusual symptoms.

Non-narcoleptic users generally find that adrafinil gives them increased energy and reduces fatigue, while improving cognitive
function, mental focus, concentration, and memory. It has been reported that quiet people who take adrafinil become more
talkative, reserved people become more open, and passive people become more active.

Of course, many stimulant drugs, ranging from caffeine to methamphetamine, are known to produce similar alerting/energizing
effects. Adrafinil has been described by some users as a "kinder, gentler" stimulant, because it provides these benefits but
usually with much less of the anxiety, agitation, insomnia, associated with conventional stimulants.

Adrafinil's effects are more subtle than those of the stimulants you may be used to, building over a period of days to months.
They appear to be based on its ability to selectively stimulate 1-adrenergic receptors in the brain.2 These receptors normally
respond to norepinephrine (noradrenaline), a neurotransmitter linked to alertness, learning, and memory. This is in contrast to
conventional stimulants, which stimulate a broader spectrum of brain receptors, including those involving dopamine. Its more
focused activity profile may account for adrafinil's relative lack of adverse side effects.


The standard dose is 2 to 4 300-mg tablets per day for improving cognitive function, although some people may find lower
doses produce a desirable degree of improvement. Higher doses have been used to treat narcolepsy.

A unique substance which improves daytime alertness and vigilance
without altering the phases of sleep. Take 2 to 4 tablets per day. After
8 to 10 days of treatment feelings of fatigue disappear, after 15 days
there is a powerful effect on activity and after 1 to 3 months cognitive
effects are experienced. Intellectual function is improved particularly,
the ability to formulate new ideas and recall information. Avoid if you
suffer from epilepsy, kidney or liver impairment.

> Submitted to the BIAM: 2/18/98
> Final entry: 3/23/2000
> Status: Validated
> Identification of substance
> Pharmacological properties
> Mechanisms of action
> Researched effects
> Therapeutic indications
> Side effects
> Genetic toxicity
> Drug Dependence
> Precautions
> Routes of administration
> Dosage and administration
> Pharmacokinetics
> Bibliography
> Identification of substance:
> Chemical formula:
> 2-[(diphenylmethyl)sulfinyl]-N-hydroxyacetamide
> List of names:
> CAS: 63547-13-7
> Memorandum: Experimental code 2755: CRL 40028
> Dci: Adrafinil
> DCIp class: 69
> DCIr class: 22
> Chemical class:
> Acetohydroxyamic Acid
> Regulation: Class I
> 1. Psychostimulant (primary usage)
> Mechanisms of action:
> 1. Principal
> Stimulant, central nervous system alpha-1 adrenergic agonist. Causes release of
serotnin and dopamine at high doses.
> Researched effects:
> 1. Psychotonic (primary)
> Therapeutic indications:
> Cerebral Senescence (primary)
> 1) Treatment for the symptoms of age-related difficulties with vigillance and
depression. Double-blinded studies against placebo demonstrated an improvement in
mental state in elderly subjects.
> Side Effects:
> 1) Determined to be very rare: Skin eruptions, gastric distress, psychomotor
excitation, mental confusion, depression, mania (in manic-depressive patients),
increase in alkaline phosphatases (with prolonged treatment).
> Genetic toxicity:
> 1. Non-teratogenic in animals (studies done in rat and rabbit)
> 2. Information lacking in humans
> Dependance:
> 1. None.
> Contraindications:
> 1) Epilepsy
> 2) Severe hepatocellular deficiency
> 3) Cirrhosis (marked increase in biodisposal in cirrhotics)
> 4) Severe renal deficiency
> 5) Athletes (Prohibited substance, Journal Officiel, 3/7/2000)
> Routes of administration:
> 1 - Oral
> Dosage and administration:
> Usual dose for oral administration in adults:
> 600 to 1200 mg/day.
> In the case of renal or hepatic deficiencies, reduce the dosage to 300-600mg/day.
> Pharmacokinetics:
> 1. Half-life: 1 hour
> 2. Elimination: Renal
> Absorbtion:
> One hour after taking orally, plasma concentration is maximal.
> Distribution:
> Bound to plasma proteins: 80%
> Half-life
> 1 hour
> Metabolism
> 75% level of hepatic metabilism in the liver to an acid derivative, then glucoronic
acid conjugation.
> Elimination
> Renal, essentially in the form of a glucoronic acid conjugate
> Bibliography:
> -Prescrire 1991;11:68-69
> Patents
> Unique active constituent in the following current French patents:
> Olmifon, 300mg tablets.
> ..

I remember Serzone brought on depression and dumbing, despite the fact it was
increasing serotonin and NE. Based on above info on Adrafinil, stimulating alpha 1s
is good for altertness, intelligence, and mood. Serzone does the opposite as it antagonizes
alpha1. I wonder if Adrafanil would be a good antidote with Serzone? I wonder which
would compete the strongest?

Personal Comments: As with all meds, the listed side effects can look scary. In real life, I have found Adrafinil to have far fewer (if any) side effects compared to just about anything else on the market. The liver thing is also a concern to some people. I have been on Adrafinil for a long time, have had three blood liver tests in that time, and each test came back perfectly normal.




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