A legal
GHB for
America?
An Interview with Ward Dean MD The Regenerative Effects of
GHB, the elixir of life! by James South
MA GHB: The First Authentic
Antidepressant by Claude Rifat
The First
Authentic Antidepressant by Claude Rifat
GHB was
discovered by a friend of mine (the late Dr Henri Laborit who introduced the use
of chlorpromazine in psychiatry around 1952) in 1961 in France.
GHB is a
remarkable molecule because it can suppress depressive ideation and anxiety,
sometimes within less than 30 minutes. It also seems to be immediately active on
the most severe and treatment-resistant forms of depression. Because of such
remarkable properties I jokingly used to call GHB "Or Potable", which means
"drinkable gold" in French! Indeed a molecule which can block your depression
and suicidal ideas, anxiety, etc, in such an efficient way is as precious as
gold because it can save your life. GHB saved my own life many times when all
other antidepressants failed. For years I suffered of depressive episodes which
did not react to conventional "antidepressants". Why? Because, in fact, most
antidepressants (an antidepressant is also called a thymoanaleptic, which is a
molecule that stimulates mood) are not really "antidepressants" per se but
thymoanaesthetics. A thymoanaesthetic is a molecule which anaesthetises emotions
and which thus blunts feelings. For instance, if you give "antidepressants" to,
say, two lovers together, you will notice that their love feelings towards one
another become anesthesised, blunted. Clearly, a molecule which blunts
rewarding emotions is definitely not an authentic antidepressant but rather a
"mind Xylocaine" (xylocaine is an anesthesiser). A thymoanaesthetic takes away a
part of your personality and makes you a bit similar to people suffering from
negative schizophrenia. On the contrary if you administer gamma-hydroxybutyrate
to a pair of lovers you will notice that it will enhance their love feelings
because it stimulates sociability.
After years of reflexions on
depression I realised one day that a real antidepressant should stimulate
sociability. Why? Because depression is basically a defect of sociability.
Depression is a state of lowered sociability and when natural sociability is
lowered in a human brain (for instance through competition, etc) then this brain
starts to suffer morally. Experience has shown that when sociability is
enhanced, depression vanishes. GHB is the first molecule ever discovered which
does just this: it stimulates sociability. This is why GHB is called a
sociabiliser. GHB is hypothesised to cure depression by stimulation of brain
oxytocin neurotransmission. Oxytocin is a very important molecule responsible of
sociable states, of the maternal instinct and of all activities related to the
maintainance of life. For instance, oxytocin is involved in sex and orgasm and
orgasm intensity seems directly linked to enhanced oxytocin neurotransmission.
GHB suppresses depressed ideation with amazing rapidity. You may feel uncurable
dysphoria with suicidal ideation, anxiety, etc, and think that no medicine or no
one could help you until you try gamma-hydroxybutyrate! Afterwards you might
just think how crazy you were and feel how life is beautiful and deserves to be
lived and enjoyed! Gamma-hydroxybutyrate strongly stimulates the desire to be
and to remain alive despite unfavourable circumstances. No conventional
so-called antidepressant does that. GHB is the fastest antidepressant known and
can, often, suppress severe depressive ideation within just hours while
conventional thymoanaesthetics take weeks or months to alleviate
suffering. GHB therapy is also very short: less than a month of treatment
is effective, as opposed to months or years of treatment with other treatments.
How to use GHB
GHB should be used as follows: Three doses of 2g
per day on an empty stomach. For instance, 2g in the morning, then 2g before
eating your first meal, at noon, then the last dose at around 6 in the
evening. If you suffer from intractable moral pain you will be surprised
to feel that your blocked gratifying emotions come back very, very fast! GHB is
a self-limiting medicine, which means that you discover by yourself when it is
time to stop medication. Why? Because GHB induces emotional satiety and when you
are emotionally satiated you do not feel like asking for more joy as you feel
already fed up with happiness!!! Yes, you can be fed up with happiness! This is
why people using GHB do not become addicted. In fact, GHB is even used to treat
alcohol and opiate addicts.
GHB gives you a strong desire to live
whatever the circumstances. This is why it is the only authentic antidepressant
available. Gamma-hydroxybutyrate was the first sociabiliser which I discovered
through Henri Laborit. Laborit is well-known in France for his many books on
society. He used to drink GHB 3 times a week, which kept him in amazing shape!
However, GHB cannot normally be taken for a long period of time continuously as
it tends to induce fatigue and sometimes anxiety. So emotional satiety or
fatigue, etc, make GHB a non-addictive medicine as people will, spontaneously,
stop medication when they feel these phenomena!
GHB is a so-called
GABA-B agonist and a tyrosine hydroxylase activator. At pharmacological doses,
it has recently been found, in Strasbourg (France), to be a tryptophan
hydroxylase activator. At the normal doses used for depression and anxiety GHB
has a small regulatory dopaminergic activity: it regularises dopaminergic
activity. GHB is found naturally in the brain together with another more rigid
analogue called gamma-hydroxy-trans-crotonate (GHTC). GHTC is a close analogue
of gamma-amino-trans-crotonate (GATC) which is one of the most potent agonist of
the newly discovered GABA-C receptors. It is not known yet whether GHB or GHTC
bind to these GABA-C receptors. There are specific receptors to 4-OHB (another
name of GHB!) and GHTC in the brain. These receptors are called GHB receptors.
French scientists have found that some benzamide neuroleptics bind with high
affinity to these receptors. Nobody knows yet what 4-OHB and GHTC do, exactly,
in the brain! They may serve as neuromodulators. The only rather clear thing we
know is that stimulation of these receptors could be involved in the generation
of "petit mal" epilepsy. GHB can induce, very rarely (and this is not
dose-dependent!), slight subjective effects reminiscent of petit mal epilepsy.
These effects are adequately blocked by clonazepam and this is the reason why
GHB should always be better absorbed with clonazepam or other benzodiazepines.
Benzodiazepines seem to have a good protective effects against the eventual
minor side-effects of GHB. For instance, short term use of GHB is strongly
anxiolytic and a very effective medication for panic attacks which are reversed
within 15 to 20 minutes (on an empty stomach only). However, if GHB is taken for
weeks it can induce what looks like a "rebound" anxiety phenomenon. This anxiety
manifests itself as plain anxiety or a panic attack just when the psychotropic
effects of GHB start to wane. GHB invariably induces vomiting in people
chronically intoxicated with alcohol or people having liver problems. In fact,
GHB can be used as a test of liver functioning! However, as GHB stimulates
dopamine activity it can give rise to nausea and vomiting with very slight
increases in the normal dose range which should never exceed 2.5g within 6
hours. Italians have used GHB to treat alcoholics and opiate addicts, without
serious side effects. They have been using shorter time intervals than that
which I recommend and big daily doses with heroin addicts with no apparent
serious side-effects. This is in contradiction to what Americans have reported.
So is there now an American and a European science??? Why are GHB side-effects
"serious" in North-America and "negligible" in Europe (Italy)? Are these
differences of opinions related to science OR culture??? My opinion is that
demonisation of so-and-so is strongly entrenched in North American culture. In
North America things have to be good or bad, black or white. Something cannot be
good and bad at the same time, out there . This is an ayatollah way of thinking:
it is cultural Inquisition. We are more realistic and pragmatic in Europe. Even
water can lead to intoxication if taken in sufficient amounts.
Many years ago I discovered a second class of Sociabilisers (though less
potent because of a mixed pro-serotoninergic action) called the tryptophan
hydroxylase inhibitors, such as MDMA (3,4
methylenedioxymethylphenylisopropylamine) or MDAI (5,6
methylenedioxyaminoindane). The sociabilising actions per se of MDMA are similar
but GHB is more potent and perfectly safe while MDMA is neurotoxic and
cardiotoxic. MDAI is a non-neurotoxic analogue of MDMA. New analogues of both
GHB and MDMA have been invented but not yet tested. The sociabilising action of
MDMA is related to its indirect blocking of serotonin neurotransmission in a
brain structure called the median raphe nucleus. When the median raphe nucleus
is inactivated then sociability spontaneously appears. In fact, both GHB and
MDMA could act at a common site modulating oxytocinergic neurotransmission. I
have now a hypothesis which could link the effects on sociability of these two
molecules. Basically this hypothesis states that MDMA might be an indirect
tyrosine hydroxylase activator by suppressing the action of serotonin at
post-synaptic 5-HT1A heteroreceptors, thus enhancing the activity of tyrosine
hydroxylase in some unidentified locus. There exists a molecule, NAN-190, which
could help in evaluating this hypothesis. GHB is a pure sociabiliser while MDMA
and MDMA-mimetics are partial sociabilisers. At low doses of MDMA the
sociabilising action of this substance is masked by a pro-serotoninergic action
as MDMA is also a serotonin releaser. This effect of MDMA produces a
psychotropic action similar to the serotoninergic thymoanaesthetics such as
fluvoxamine, citalopram, sertraline, etc. At higher dosage the sociabilising
action of MDMA becomes manifest. Subjectively speaking 2.5g of GHB ia equivalent
to 200mg of MDMA. GHB might, theoretically, be also effective against the
negative symptoms of schizophrenia but this remains to be tested.
If GHB
is demonstrated to be the superior antidepressant which I claim, then it would
throw away most of the antique antidepressants! GHB is sometimes very
effective against migraines but only for an hour and a half! The activity of GHB
against migraines is not predictable, like many other medicines used for that.
GHB should never be mixed with alcohol, opiates, antibiotics, or
anything else except benzodiazepines, Amineptine, or Fluvoxamine. The
psychotropic effects of 100mg of fluvoxamine will be suppressed for about an
hour and a half by a dose of 2.5g of GHB. Amineptine does not seem to modify the
psychotropic effects of GHB while L-dopa intensifies the hypnotic effects of
this molecule. The recommended dose of GHB should not be exceeded. If you
overdose, you fall into a hypnotic sleep from which you cannot awaken for hours.
Moreover, it could promote "petit mal" epilepsy in such overdoses, plus nausea
and vomiting. Vomiting is a clear sign of relative over-dosage of GHB and is
related, apparently, both to the dopaminergic activity of this molecule and to
liver function. Anyhow, there is no need for overdosing. If used as prescribed
here it is a very safe antidepressant and anti-panic medication. I advise
those people who see everything in term of white or black to look into the
considerable benefits for sufferers that GHB could bring if it is demonstrated
to be the superior antidepressant I claim here. Afterwards, more research will
certainly lead to refined versions of GHB with minimal side-effects.
The
demonisation of GHB in North America: A New Form of Inquisition
We have
been living, since the 1960s, in a world of Inquisition against all psychotropic
molecules which generate some forms of pleasure. This modern Inquisition started
in America as a puritanical expression of American society to ban pleasure from
life. This Inquisition should be fought against as it has halted the development
of scientific research on the mind. 30 years of research have been lost because
Americans imposed an intellectual embargo on many forms of research involving
the mind. For instance, all research on the hallucinogens was stopped, thanks to
this perverse Inquisition. This intellectual embargo should be lifted and
scientists and laymen should fight for that.
No Inquisition can be
accepted in the scientific field. American society has systematically demonised
all psychotropic molecules which can give pleasure. (Even alcohol was demonised
but this demonisation was not successful and was abandoned when it was noticed
that the creation of Al Capone and other similar people was a consequence of
this demonisation!) This is sheer madness and should strongly be opposed. The
right to use our brain in the way we want should be a fundamental right of man
and put in the Declaration of Human Rights. I hope this goal will be achieved in
the future. One of the reason which motivated me to write what you are reading
is that GHB has been in use, by knowledgeable people in Europe, for decades. Now
it has reached the USA, unfortunately because, as usual, some American
inquisitors are trying to demonise this very useful molecule. These
pseudo-scientific ayatollahs should be put back in their medieval churches. In
Iran, ayatollahs are condemning sex. In America, the ayatollahs want,
desperately, to control the use of our mind. This is an untolerable situation.
Progress is made through freedom and knowledge, not under the guidance of any
ayatollah. Let us make a grassroot movement against all these ayatollahs!
Ayatollahs and similar Inquisitors should go back into their dungeons!!! The
Middle Ages are over. The quest for Freedom is a never-ending quest. It is
surprising that you do not yet need a prescription for champagne, wines and
other alcohols in North America because if alcohol were judged by pharmaceutical
standards it would have been banned a long time ago...
GHB in France and
North-America
GHB was invented by Dr Wermuth, in France, for Dr Henri
Laborit who is the father of chlorpromazine and modern psychopharmacology.
Wermuth created gamma-hydroxybutyrate in 1961 in the search of a GABA analogue
which could readily penetrate the blood-brain barrier. Gamma-OH soon went on the
market as an hypnotic which could be obtained with no medical prescription. The
French, until I started to study this molecule, were unable to classify it under
any existing class, because sometimes it was an hypnotic inducing a form of
sleep very similar to normal sleep, then it became a pre-anaesthetic, etc. About
15 years ago, I finally discovered that GHB was, in fact, a molecule to be
classified under the novel class of the Sociabilisers, together with its
butyrolactone form which is readily transformed into GHB in the blood by a non
specific lactonase. In fact, butyrolactone is a pro-drug giving rise to
gamma-hydroxybutyric acid. GHB has a recognised peripheric oxytocinergic action
while its central oxytocin properties are still to be demonstrated but seem very
likely.
GHB is known in France through the many books of Henri Laborit
and his conferences! Laborit always praised the properties of GHB and, as France
is definitely not a puritanical society banning pleasure from existence, GHB has
always been available, even though its stimulates pleasure. Laborit always
advocated the general use of GHB in society, like butter or milk! Why? Because
it takes away your stress, makes you more positive towards life, suppresses
selectively, like a kind of "psychological diode", your painful feelings,
stimulates your sociability and makes you more tender, more loving, more
concerned by others. Also you become keenly aware that you have only one life
and that life should be a quest for happiness. GHB makes you realise how much
you need others (not something for businessmen and militaries or gangsters!!!)
and this is a highly positive thing. I always knew that when GHB arrived in
puritanical North America it would one day be demonised... Unfortunately for
North Americans, the ayatollahs of the pleasure Inquisition have struck again
and banned gamma-hydroxybutyrate! Laborit just died, recently, a few months ago
at an old age. Sometimes he used to joke that GHB made him live longer as he
would suppress his stress with this "drinkable gold" in cases of need!!! He
always said that his two greatest discoveries were chlorpromazine and GHB but he
never fully realised that GHB could open a new era in the management of
depression and anxiety. He never fought to promote the study of the psychotropic
effects of GHB, he never discovered that GHB was the first molecule of a novel
class: the Sociabilisers. He just enjoyed GHB, with his friends, while
conducting other researches. All the people who have surrounded Laborit have
naturally more or less been exposed to GHB! I was lucky to be one of these
people. GHB is still a crude medicine. It should be properly studied and better
analogues should be invented. The use of sociabilisers may have tremendous
effects on our societies, reducing intra-specific aggression and enhancing
cooperation instead of competition. GHB is a convivial medicine as it shows you
that you need others to be happy. Long term on-and-off use seems to make you
more immune to stress and dysphoria, more loving towards people in general, more
active in your life as it stimulates your enthusiasm because you are so aware
that life can be a fantastic thing, every day. The general use of sociabilisers
may be a temporary solution for the intra-specific aggressivity of the human
kind. Can GHB and novel analogs reduce wars, at last? I leave this question
opened for your reflexion.
I will now summarise the psychotropic
profile of GHB, something which I did in a lengthy paper many years ago, in
French.
Description of the Psychotropic Effects of GHB (1985)
GHB
has the following properties:
1) GHB
stimulates sociability, which means that you feel like communicating with other
people in all ways: emotionally, intellectually, sexually. And from this
communication you feel a very strong and deep happiness.
2) GHB gives you a strong desire to touch
others, physically and psychologically. 3)
Communication becomes extremely gratifying as you feel you want to become close
to people, not to isolate yourself. 4) GHB induces a
strong sense of beauty. Everything looks so beautiful, so vivid, so enjoyable,
so pleasurable, so important, so "deep". 5) The
perception of movement is enhanced. 6)
Three-dimensional perception is enhanced and vision seems more clear, better
than usual. 7) The contrast of colours
between objects is increased. A yellow "pissenlit" (dandelion), or a rose, etc,
situated in front of, say, green grass, looks brighter, more real, closer to
you. 8) If you are a man, a woman will
look magnificent and very attractive. She may become just like a goddess to your
eyes. Women will experience the same feelings towards men. However, these kinds
of feelings depend of your cultural background. For instance, a simple Siamese
woman will not feel such intense feelings but will report that she feels drunk!
GHB is a very important tool in investigating the emotional background of a
person. For instance loving people will become more loving while people devoid
of these feelings will just feel in good mood, only. Some people may cry, which
demonstrates that they have a lot of repressed material in themselves, etc.
Crying under GHB is a very liberating experience because you can take out and
release things which you normally keep deep inside and which thus hurt you.
Crying under GHB takes away accumulated inner moral
pains. 9) Sensuality becomes very intense.
You want to touch, to kiss, to caress, to hold, to love, to hug, to make love.
In summary, you want to contact others through any means available because you
are just highly sociable! 10) According to
Henri Laborit, GHB renders the clitoris more sensitive. Moreover, GHB increases
love and sexual desires both in women and men.
11) You can sometimes feel a deep sense of
"meaningfulness". Things become meaningful to you, even you are unable to
scientifically define such a mystical feeling. This meaningfulness of reality is
a very interesting phenomenon from a scientific point of view as it seems to
show that there exists a "circuit" of meaningfulness in our nervous system.
Non-specific activation of this circuit, under GHB, would give us a "deep" sense
of "meaningfulness" which is, of course, imaginary.
12) GHB stimulates your recall abilities
related to previous GHB experience. Each time you take GHB you can often clearly
remember memories stored under another GHB context. Emotions are especially
well-remembered and reexperienced. From these and other observations, I think
GHB should be a tool of choice in psychoanalysis.
13) Some people feel an urge to defecate after
GHB, probably because of muscle relaxation! One of the first reactions
from a colleague of mine, after GHB, is to go to the toilet!!!
14) In fact, GHB induces a very pleasant sense
of muscle relaxation, especially in the legs.
15) One of the most remarkable action of GHB is
that it gives you a strong desire to live and to remain alive, despite
unfavourable conditions.
When is GHB contraindicated?
Untreated
epilepsy, eclampsia, hypokalemia, severe hypertension, alcoholism, association
with opiates, antibiotics. For depressed patients, GHB should be taken only
under medical supervision.
Claude Rifat, biologist, Gen & Egraveve,
Suisse.
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A legal GHB for America?
An
Interview with Ward Dean MD By Phil Micans PharmB
Recently I had the pleasure to visit Dr. Ward
Dean at his home in Pensacola, Florida. Many subjects were covered especially in
relation to Gamma-Hydroxy-Butyrate or GHB. In the United States there are
ludicrous legal problems that prevent the use of GHB in most of the states.
Therefore many American Citizens may be fascinated to learn about a legal GHB
alternative called Renewtrient®. This interview focuses on GHB and
Renewtrient®.
PHIL
"Dr. Dean I understand you have
recently released a new book. Can you tell us a little bit about
it?" "Dr. Dean I understand you have recently
released a new book. Can you tell us a little bit about it?"
Dr. DEAN "Yes certainly, the book is
called GHB, the Natural Mood Enhancer. Anybody who has followed the American
news recently may have heard that GHB is touted as a terrible-highly-toxic
date-rape drug. "Yes certainly, the book is
called GHB, the Natural Mood Enhancer. Anybody who has followed the American
news recently may have heard that GHB is touted as a terrible-highly-toxic
date-rape drug.
Allegedly hundreds if not thousand of
nefarious ill-intentioned males have been using it to place their acquaintances
into unconsciousness. My book places the real facts before the
public."
PHIL "I believe I read in the media
some ridiculous nick-names being used to describe GHB. Names such as liquid
ecstasy and grievous bodily harm! Is this the same substance?" "I believe I read in the media some ridiculous nick-names being
used to describe GHB. Names such as liquid ecstasy and grievous bodily harm! Is
this the same substance?"
Dr. DEAN "Yes, that's it, but this
dangerous toxic date-rape drug is actually one of the safest, most beneficial
substances known to man. It occurs naturally in the body and it actually fits
the FDA's definition of a food supplement!" "Yes,
that's it, but this dangerous toxic date-rape drug is actually one of the
safest, most beneficial substances known to man. It occurs naturally in the body
and it actually fits the FDA's definition of a food supplement!"
PHIL "Goodness, that couldn't be more
completely different from what we've been hearing. On one hand we seem to have
the American authorities going around saying how lethal this substance is and
yet I know from my pharmacology studies that there are over 30-years of
efficacious use of GHB in European clinical literature. What's more in Europe
we've never ever come across any of these problems that the FDA claim are
afflicting the United States!" "Goodness, that
couldn't be more completely different from what we've been hearing. On one hand
we seem to have the American authorities going around saying how lethal this
substance is and yet I know from my pharmacology studies that there are over
30-years of efficacious use of GHB in European clinical literature. What's more
in Europe we've never ever come across any of these problems that the FDA claim
are afflicting the United States!"
Dr. DEAN "Right, GHB was developed in
France in 1961 as a way of getting GABA (Gamma amino butyric acid) across the
blood-brain barrier and it was found to have a very highly anaesthetic,
hypnotic-sleep inducing affect. "Right, GHB was
developed in France in 1961 as a way of getting GABA (Gamma amino butyric acid)
across the blood-brain barrier and it was found to have a very highly
anaesthetic, hypnotic-sleep inducing affect.
Professor Henry Laborit first synthesised GHB
and he utilized it for paediatric anaesthesia. Tens of thousands of cases of
anaesthesia were administered with GHB without any adverse
effects."
PHIL "We know GABA is natural product,
can we say that GHB is a natural product too?" "We know GABA is natural product, can we say that GHB is a
natural product too?"
Dr. DEAN "Yes we can, GHB is a natural
product because after it was synthesised by Professor Laborit he discovered that
it was already in the brain and in fact in every other mammalian cell! He had
actually reversed the usual course of the development of drugs, normally we
identify something in the body, for example insulin, and then we synthesise it.
In GHB's case it was synthesised first and then it was discovered to be
natural!" "Yes we can, GHB is a natural product
because after it was synthesised by Professor Laborit he discovered that it was
already in the brain and in fact in every other mammalian cell! He had actually
reversed the usual course of the development of drugs, normally we identify
something in the body, for example insulin, and then we synthesise it. In GHB's
case it was synthesised first and then it was discovered to be
natural!"
PHIL "Oh, how unusual! I've read your
book about GHB and I understand that it has a wide variety of uses. I know that
in Europe and in particular in Italy GHB in small doses is used to wean people
off alcohol or help alleviate their depression. I understand also that small
doses can have a re-energising affect." "Oh, how
unusual! I've read your book about GHB and I understand that it has a wide
variety of uses. I know that in Europe and in particular in Italy GHB in small
doses is used to wean people off alcohol or help alleviate their depression. I
understand also that small doses can have a re-energising affect."
Dr. DEAN "Right and those are just a
few of its many affects. Probably its most widely used effect is as a
sleep-inducing agent. It is the most powerful and safest sleep-inducing agent
there is. It's totally non-addictive; non-habit forming and breaks down
completely into carbon dioxide and water and has absolutely no toxic
affects. "Right and those are just a few of its
many affects. Probably its most widely used effect is as a sleep-inducing agent.
It is the most powerful and safest sleep-inducing agent there is. It's totally
non-addictive; non-habit forming and breaks down completely into carbon dioxide
and water and has absolutely no toxic affects.
But it's also used as you suggested in cases
of anxiety and as an anti-depressant and for treating migraine headaches and for
Parkinson's disease and it's even being evaluated for Alzheimer's disease.
In fact I know some scientists who believe it
is a brain-normalizer. It makes every brain related disease better, it has been
discovered to be one of the few natural substances that enhances the
natural-physiological action, especially in the case of sleep, because it
enhances all phases of sleep. So people can actually get by on less sleep,
because their sleep is so much more effective.
Furthermore GHB's uses include an aid to
fibromyalgia; a potent growth hormone stimulant, a lowerer of cholesterol, a
reducer of oxygen requirements for the heart and brain and as you've already
elicited it is a useful aid in alcohol and opiate detoxification programs. In
many cases the individual totally loses his or her desire to use illegal
substance and replaces them with a much more beneficial substance.
I recently read a report on experimental mice
that were given extremely large doses of a closely related substance that
prevented cancer and indicated a potential extension in life span of the
animals."
PHIL "It seems quite amazing and it
appears to me that GHB has the broadest range of efficacious useful aspects of
any pharmacological or indeed natural substance that I have ever come across. "It seems quite amazing and it appears to me
that GHB has the broadest range of efficacious useful aspects of any
pharmacological or indeed natural substance that I have ever come across.
I appreciate that we could fill several
bulletins with information about GHB and that you did an earlier article about
GHB in the July 1997 Anti-Aging Bulletin and indeed James South MA is writing a
major piece about GHB for this Anti-Aging Bulletin. Therefore we really should
suggest that people who want to know the full story of GHB read your current
book, GHB, the Natural Mood Enhancer. But how is GHB able to accrue all these
different affects? Is it very much dose dependant?"
Dr. DEAN "Yes it is, a very small dose,
especially taken in the morning, particularly when someone hasn't gotten enough
sleep; it manages to take that rough edge off the nerves and actually produces
an energizing effect. "Yes it is, a very small
dose, especially taken in the morning, particularly when someone hasn't gotten
enough sleep; it manages to take that rough edge off the nerves and actually
produces an energizing effect.
A slightly higher dose induces a state of mild
euphoria, similar to the effect when one has had a glass or two of wine. Higher
doses, in the 2 to 3 gram range will cause sleep to occur and even higher doses
will force a very profound sleep which you cannot be awakened from until the
substance has worn off. But the safety range is extremely high; in fact the
toxic dose is less than that of table salt!
One individual was reported in the literature
having taken 75 grams (PHIL- Good God!) allegedly by accident and that's pretty
tough to do by accident because that's about 15 heaped-tablespoons (Ed. That's
the equivalent of drinking 3-bottles of Alcover at once). He was hospitalized
and woke up 24 hours later feeling somewhat sedated with a
headache!"
PHIL "That's incredible, I also
understand that the FDA have Investigational New Drug Status (IND's) on file
where patients were using something like 30 grams a day under their
guidance." "That's incredible, I also understand
that the FDA have Investigational New Drug Status (IND's) on file where patients
were using something like 30 grams a day under their guidance."
Dr. DEAN "Correct, in fact the FDA has
been the biggest prosecutor of users of GHB. In many trials where health food
owners were being prosecuted for selling GHB, the FDA at first denied that there
were any IND's for GHB. It was at the appeal that they found that there were
IND's which the FDA then said were totally irrelevant to the case! When we read
them we saw that there were over 15 different conditions that were being
investigated and over and over again, repeatedly in these IND's GHB was
introduced as a totally natural, non-toxic substance. In fact in some of these
IND studies they had patients taking GHB from anything from 3g to 8g per night
for years on-end without adverse side-effects. They even had some studies where
people were taking up to 30g daily for months on end without adverse side
effects. "Correct, in fact the FDA has been the
biggest prosecutor of users of GHB. In many trials where health food owners were
being prosecuted for selling GHB, the FDA at first denied that there were any
IND's for GHB. It was at the appeal that they found that there were IND's which
the FDA then said were totally irrelevant to the case! When we read them we saw
that there were over 15 different conditions that were being investigated and
over and over again, repeatedly in these IND's GHB was introduced as a totally
natural, non-toxic substance. In fact in some of these IND studies they had
patients taking GHB from anything from 3g to 8g per night for years on-end
without adverse side-effects. They even had some studies where people were
taking up to 30g daily for months on end without adverse side effects.
I have two patients who have been taking in
excess of 50g per day! Both of these patients were alcoholics who had been
totally dysfunctional because they required tremendous amounts of alcohol,
without which they literally became psychotic. However by taking very large
doses of GHB they now completely avoid the use of alcohol and function extremely
well and for some reason they have this tremendous physiological requirement for
very large dosages of GHB.
All aspects of their life have now been
greatly improved, except one. They feel guilty about taking such large doses of
a substance that the American media have conned them into believing is a highly
addictive and dangerous substance! So I asked them, if the same thing had been
done with vitamin-C and they were suffering from scurvy would they feel guilty
about using vitamin-C?"
PHIL "But they must be better off than
using the copious amounts of alcohol that was pickling their
brains?" "But they must be better off than using
the copious amounts of alcohol that was pickling their brains?"
Dr. DEAN "Absolutely." "Absolutely."
PHIL "I guess that's the
difference between smart-drugs and dumb-drugs!" (Everyone laughs)
PHIL "I'm sure that many of the readers
of the Anti-Aging Bulletin know that natural products are virtually
unenforceable when it comes to a patent. So I believe that we can all read
between the lines and guess it's the usual profit-relationship story. I'm
also sure that IAS's clientele realize that IAS won't ship GHB or any other
product to an area where it is classified as a controlled or scheduled
substance. "I'm sure that many of the readers of
the Anti-Aging Bulletin know that natural products are virtually unenforceable
when it comes to a patent. So I believe that we can all read between the lines
and guess it's the usual profit-relationship story. I'm also sure that
IAS's clientele realize that IAS won't ship GHB or any other product to an area
where it is classified as a controlled or scheduled substance.
To me it is quite phenomenal that States such
as Georgia and Rhode Island not only have scheduled GHB but also have scheduled
it as a class I controlled drug! That is the same schedule as heroin and
cocaine! It also appears that as every month goes by we become aware of
another State joining the schedule list.
As IAS won't ship to those affected areas for
the protection of its clientele, it becomes a very sad situation for many
insomniacs, depressives' etc. living in America. Are you aware of any substances
that are legal in the USA but will have very similar properties to
GHB?"
Dr. DEAN
"Absolutely, although we didn't discuss this
in our book about GHB, there is a substance called Renewtrient® that is the precursor
of GHB but actually contains no GHB, it is on the GRAS list, the generally
recognised safe-substance list.
Renewtrient® converts naturally in the body
into GHB and the two substances inter-convert back and forth in the body. It has
the exactly the same beneficial affects as GHB and is totally non-toxic in the
recommend doses, and was shown to be non-toxic in trials with experimental
animals even at very high doses, far beyond the normal useful recommended
dosages."
PHIL "That's fascinating, so I
understand that Renewtrient® may be a legal alternative for American Citizens
and State Sovereigns to be able to use and it has the benefits of GHB. Am I
correct?" "That's fascinating, so I understand
that Renewtrient® may be a legal alternative for American Citizens and State
Sovereigns to be able to use and it has the benefits of GHB. Am I
correct?"
Dr. DEAN "You would be absolutely
correct, what we have now is a substance totally legal in all 50 states of the
united states of America and it possesses all of the benefits of GHB and is
non-toxic." "You would be absolutely correct,
what we have now is a substance totally legal in all 50 states of the united
states of America and it possesses all of the benefits of GHB and is
non-toxic."
PHIL "That's fantastic
news." "That's fantastic news."
Dr. DEAN "That's fantastic news for
you, me and all the potential users; it is terrible news for the prohibitionists
and the promoters of the police state in America." "That's fantastic news for you, me and all the potential users;
it is terrible news for the prohibitionists and the promoters of the police
state in America."
PHIL "So perhaps what is required is to
make as many people as possible aware of these facts. I would imagine that one
of the problems with GHB is that very few people are aware of its beneficial
actions, and therefore it has become very easy to demonise it." "So perhaps what is required is to make as many people as
possible aware of these facts. I would imagine that one of the problems with GHB
is that very few people are aware of its beneficial actions, and therefore it
has become very easy to demonise it."
Dr. DEAN "That's true and also I think
that its irresponsible use by a few people has heightened the demonization. Like
all substances it needs to be used responsibly, its combination with other drugs
and alcohol should be avoided and children without the supervision of their
parents shouldn't use it. I personally have administered it to my kids many
nights, to ensure that they stimulate the release of growth hormone and that
they get plenty of good solid sleep, so they can get up earlier and get to
school on time. "That's true and also I think
that its irresponsible use by a few people has heightened the demonization. Like
all substances it needs to be used responsibly, its combination with other drugs
and alcohol should be avoided and children without the supervision of their
parents shouldn't use it. I personally have administered it to my kids many
nights, to ensure that they stimulate the release of growth hormone and that
they get plenty of good solid sleep, so they can get up earlier and get to
school on time.
I firmly believe the people who are going to
benefit the most from this are people with age-related sleep disorders.
As you know most people as they get past their
50's have an increasingly difficult time getting to sleep at night, and of
course that adversely affects the quality of their time during the day. They
tend to drag around feeling tired, fatigued, confused and constipated and yet
getting a good 7 or 8 hours of quality sleep at night adds tremendously to the
overall quality of their life."
PHIL "Yes that is obviously so
important. If we look at Melatonin many people are now aware of its beneficial
properties for sleep. Yet GHB is even more beneficial! IAS has more
correspondence from physicians and patients on the subject and benefits of GHB
than any other substance in its line-up. As you have already stated Dr. Dean
there are so many positive uses." "Yes that is
obviously so important. If we look at Melatonin many people are now aware of its
beneficial properties for sleep. Yet GHB is even more beneficial! IAS has more
correspondence from physicians and patients on the subject and benefits of GHB
than any other substance in its line-up. As you have already stated Dr. Dean
there are so many positive uses."
Dr. DEAN "Just one comment Phil for the
readers, comparing GHB with Melatonin shouldn't preclude the use of Melatonin
with GHB. I believe that they should both be used at night because they both
enhance sleep and Melatonin is a powerful anti-oxidant and acts as a normalizer
of the hormonal rhythms." "Just one comment Phil
for the readers, comparing GHB with Melatonin shouldn't preclude the use of
Melatonin with GHB. I believe that they should both be used at night because
they both enhance sleep and Melatonin is a powerful anti-oxidant and acts as a
normalizer of the hormonal rhythms."
PHIL "Do you think that the two are
synergistic together and that perhaps the dosage could or should be
reduced?" "Do you think that the two are
synergistic together and that perhaps the dosage could or should be
reduced?"
Dr. DEAN "Well you could, but I don't
believe that you need to. Melatonin is extremely safe and is probably the only
hormone we've found that does not cause negative feedback inhibition. Even in
very high doses it doesn't reduce the pituitary's normal output, unlike say
adrenal hormone which in excess would tend to shutdown the adrenal gland. "Well you could, but I don't believe that you
need to. Melatonin is extremely safe and is probably the only hormone we've
found that does not cause negative feedback inhibition. Even in very high doses
it doesn't reduce the pituitary's normal output, unlike say adrenal hormone
which in excess would tend to shutdown the adrenal gland.
There appears to be no-such feedback mechanism
for Melatonin. So the tremendous benefits of Melatonin as an immune stimulant
and to promote normal chrono-biological hormonal rhythms are in addition to its
sleep inducing affects."
PHIL "That's very interesting, but
getting back to Renewtrient® what precise chemical description would you
describe it by?" "That's very interesting, but
getting back to Renewtrient® what precise chemical description would you
describe it by?"
Dr. DEAN "Precisely it’s
2(3)-furanone di-hydro 2(3)FDH"
PHIL "I would like to talk if I may a
bit about HGH (Human Growth Hormone). We discussed HGH in the November 1997
issue of the Anti-Aging Bulletin. In the July 1997 issue of the Anti-Aging
Bulletin we reproduced a graph of a Japanese clinical study that showed that a
dose of 2.5 grams of GHB dramatically increased growth hormone levels sixteen
times within 60 minutes. There are now so many clinically documented beneficial
anti-aging uses for a healthy, perhaps youthful maintained growth hormone level.
What sort of amounts of Renewtrient® may be required to reproduce these kinds of
results?" "I would like to talk if I may a bit
about HGH (Human Growth Hormone). We discussed HGH in the November 1997 issue of
the Anti-Aging Bulletin. In the July 1997 issue of the Anti-Aging Bulletin we
reproduced a graph of a Japanese clinical study that showed that a dose of 2.5
grams of GHB dramatically increased growth hormone levels sixteen times within
60 minutes. There are now so many clinically documented beneficial anti-aging
uses for a healthy, perhaps youthful maintained growth hormone level. What sort
of amounts of Renewtrient® may be required to reproduce these kinds of
results?"
Dr. DEAN "Well basically 1 fluid ounce
of Renewtrient® is more-or-less equivalent to 2 grams of GHB, so if you know
your GHB dose then you can extrapolate it to find your Renewtrient® requirement.
In fact recently the manufacturers of Renewtrient® sponsored a clinical-trial to
discover precisely by how much and how quickly Renewtrient® can increase growth
hormone levels in adults. "Well basically 1 fluid
ounce of Renewtrient® is more-or-less equivalent to 2 grams of GHB, so if you
know your GHB dose then you can extrapolate it to find your Renewtrient®
requirement. In fact recently the manufacturers of Renewtrient® sponsored a
clinical-trial to discover precisely by how much and how quickly Renewtrient®
can increase growth hormone levels in adults.
PHIL "What other less-well known
improvements do you believe that aging people may derive from the growth hormone
agonist properties of GHB or Renewtrient®?" "What
other less-well known improvements do you believe that aging people may derive
from the growth hormone agonist properties of GHB or
Renewtrient®?"
Dr. DEAN "One is darkening of the hair,
another is the restoration of normal youthful hair patterns in male pattern
baldness. Men with prostate problems have had their enlarged prostate and their
symptoms related to their enlarged prostates totally resolved with youthful
urination patterns returned. Of course use at bedtime can naturally help restore
youthful lean body-mass and reduce fat levels." "One is darkening of the hair, another is the restoration of
normal youthful hair patterns in male pattern baldness. Men with prostate
problems have had their enlarged prostate and their symptoms related to their
enlarged prostates totally resolved with youthful urination patterns returned.
Of course use at bedtime can naturally help restore youthful lean body-mass and
reduce fat levels."
PHIL "I think we're all beginning to
see why they want it banned! With all these clinical uses it impinges on so-many
pharmaceutical categories and substances!" "I
think we're all beginning to see why they want it banned! With all these
clinical uses it impinges on so-many pharmaceutical categories and
substances!"
Dr. DEAN "Right and look at just the
euphoria producing affects; there is only one legal substance that will help you
unwind after a hard day at the office and that's alcohol and look at the number
of adverse social and physical effects associated with alcohol. "Right and look at just the euphoria producing affects; there is
only one legal substance that will help you unwind after a hard day at the
office and that's alcohol and look at the number of adverse social and physical
effects associated with alcohol.
GHB and Renewtrient® represent a new class of
drugs called socialibizers; these actually enhance interpersonal relations and
elevate the mood. Whilst they have similar euphoric effects to alcohol and
enhance sociability when the effects wear off instead of leaving you with a
hang-over, headache and gastric distress, you are clear-headed, alert and
feeling exhilarated!"
PHIL "So would you like to recommend
any doses? I appreciate that with such a broad array of uses that these will be
very varied. Indeed I appreciate that anti-aging medicine in general requires a
kind of self-experimentation within the established guidelines, and as you have
already stated being responsible is a key-factor." "So would you like to recommend any doses? I appreciate that with
such a broad array of uses that these will be very varied. Indeed I appreciate
that anti-aging medicine in general requires a kind of self-experimentation
within the established guidelines, and as you have already stated being
responsible is a key-factor."
Dr. DEAN "Certainly, we recommend
starting with very low doses, learning your own tolerance and your own response.
For energy enhancement GHB doses are anywhere from 250mg to 500mg. Euphoria/
libido-enhancing effects are anywhere from 500mg to 1000mg and doses larger than
that may cause profound relaxation or indeed sleep. Typical GHB sleep doses are
from 1g to 3g, this is a safe dose and many people will find that they will wake
up 3 or 4 hours later and if they so wish they can take a second
dose." "Certainly, we recommend starting with
very low doses, learning your own tolerance and your own response. For energy
enhancement GHB doses are anywhere from 250mg to 500mg. Euphoria/
libido-enhancing effects are anywhere from 500mg to 1000mg and doses larger than
that may cause profound relaxation or indeed sleep. Typical GHB sleep doses are
from 1g to 3g, this is a safe dose and many people will find that they will wake
up 3 or 4 hours later and if they so wish they can take a second
dose."
PHIL "I think this comes back to the
responsibility thing again. I inform people that they should tell their
bed-partner that they are taking an agent that may make them sleep 3 to 5 hours
and its likely that they may not be able to be woken and that there is nothing
to panic about. As we know from the clinical literature the oxygen levels remain
normal, even though the breathing rhythm may slow a little and at high doses
some people experience a few body twitches, but these are all quite
normal." "I think this comes back to the
responsibility thing again. I inform people that they should tell their
bed-partner that they are taking an agent that may make them sleep 3 to 5 hours
and its likely that they may not be able to be woken and that there is nothing
to panic about. As we know from the clinical literature the oxygen levels remain
normal, even though the breathing rhythm may slow a little and at high doses
some people experience a few body twitches, but these are all quite
normal."
Dr. DEAN "This is exactly what happens
when people normally go to sleep and I'm glad you brought the subject up. Even
though the breathing rate may be slow, the depth of breathing is increased, so
there's absolutely no change in the oxygen levels in the blood. This is one of
the things that makes GHB absolutely unique as a sleep-inducing agent. Drugs
that are used for sleep, such as benzodiazepines, (i.e. Valium), are drugs that
suppress the respiratory systems and they don't have the compensatory mechanism
to increase the depth of respiration and therefore carbon dioxide levels can
build up and oxygen levels can go down." "This is
exactly what happens when people normally go to sleep and I'm glad you brought
the subject up. Even though the breathing rate may be slow, the depth of
breathing is increased, so there's absolutely no change in the oxygen levels in
the blood. This is one of the things that makes GHB absolutely unique as a
sleep-inducing agent. Drugs that are used for sleep, such as benzodiazepines,
(i.e. Valium), are drugs that suppress the respiratory systems and they don't
have the compensatory mechanism to increase the depth of respiration and
therefore carbon dioxide levels can build up and oxygen levels can go
down."
PHIL "Okay, so would you therefore
think its prudent that when someone starts on GHB for the very first time, in
case they might suffer from hypersensitivity, that they take it in an
environment where they are safe? "Okay, so would
you therefore think its prudent that when someone starts on GHB for the very
first time, in case they might suffer from hypersensitivity, that they take it
in an environment where they are safe?
For example they shouldn't be driving or
operating machinery and should be prepared for bed, just in case they become
drowsy."
Dr. DEAN "I would, and especially avoid
driving, of course this is true of any substance that may impair your abilities,
whether its alcohol, GHB, Renewtrient® or even a cold
medication." "I would, and especially avoid
driving, of course this is true of any substance that may impair your abilities,
whether its alcohol, GHB, Renewtrient® or even a cold medication."
PHIL "I don't know if our readers can
ascertain the mood Dr. Dean, but you are talking very enthusiastically about GHB
and Renewtrient®. I'm fully aware that you are one of the leading physician's in
the anti-aging field, but how would you rate GHB or Renewtrient® in say a top-10
of anti-aging supplements?" "I don't know if our
readers can ascertain the mood Dr. Dean, but you are talking very
enthusiastically about GHB and Renewtrient®. I'm fully aware that you are one of
the leading physician's in the anti-aging field, but how would you rate GHB or
Renewtrient® in say a top-10 of anti-aging supplements?"
Dr. DEAN "Well I would certainly rate
it in the top-5, perhaps in the top-3." "Well I
would certainly rate it in the top-5, perhaps in the top-3."
PHIL "Really! That
important?" "Really! That
important?"
Dr. DEAN "Yes indeed, it certainly is
not a life-shortening substance, Professor Laborit who took GHB every day, died
at the age of 91 without suffering from any chronic disease. "Yes indeed, it certainly is not a life-shortening substance,
Professor Laborit who took GHB every day, died at the age of 91 without
suffering from any chronic disease.
One aspect of GHB that we haven't even touched
on is that it actually induces a state of hibernation and lowers body
temperature by 2-3 degrees during sleep. Professor Roy Walford from UCLA
speculated that if we could find a safe non-toxic substance that would lower
body temperature and induce a state of hibernation, like GHB does, that we might
actually increase our life-spans."
PHIL "Very interesting, so we may just
have Professor Walford's life-extending substance! If I can I'd just like to
talk very briefly again about the problems of GHB in the United States. Now I'm
not a US citizen, but if I were, or if I lived in the United States would you
advise me to use Renewtrient® in place of GHB because of the legal
status?" "Very interesting, so we may just have
Professor Walford's life-extending substance! If I can I'd just like to talk
very briefly again about the problems of GHB in the United States. Now I'm not a
US citizen, but if I were, or if I lived in the United States would you advise
me to use Renewtrient® in place of GHB because of the legal
status?"
Dr. DEAN "Definitely, we can never
guess the whims of the arbitrary and capricious enforcement authorities. So
rather than have a substance that is illegal or quasi-legal in your state (i.e.
GHB) you're much better having a substance that is totally legal (i.e.
Renewtrient®) that possess the same effects and benefits." "Definitely, we can never guess the whims of the arbitrary and
capricious enforcement authorities. So rather than have a substance that is
illegal or quasi-legal in your state (i.e. GHB) you're much better having a
substance that is totally legal (i.e. Renewtrient®) that possess the same
effects and benefits."
PHIL "Dr. Dean I know that its
important to you to get this message out to as many people as possible, apart
from the obvious health benefits are there any other reasons?" "Dr. Dean I know that its important to you to get this message
out to as many people as possible, apart from the obvious health benefits are
there any other reasons?"
Dr. DEAN "Yes, and this can be seen
with DHEA, Pregnenolone, Progesterone, 5-HTP and Melatonin. As soon as
thousands, indeed millions of people are enjoying the benefits of these natural
products supplementation, so it will become very difficult if not impossible for
the FDA to remove them from the market-place, especially under a misguided
pretence of safety or toxicity problems." "Yes,
and this can be seen with DHEA, Pregnenolone, Progesterone, 5-HTP and Melatonin.
As soon as thousands, indeed millions of people are enjoying the benefits of
these natural products supplementation, so it will become very difficult if not
impossible for the FDA to remove them from the market-place, especially under a
misguided pretence of safety or toxicity problems."
PHIL "I can foresee tremendous demand
for Renewtrient® in the United States, and I hope there won't be too-many supply
problems. I'm also confident that the price may fall as the benefits of
mass-production are enjoyed. How important do you feel it is that people have
affordable and ready access to Renewtrient® in the USA?" "I can foresee tremendous demand for Renewtrient® in the United
States, and I hope there won't be too-many supply problems. I'm also confident
that the price may fall as the benefits of mass-production are enjoyed. How
important do you feel it is that people have affordable and ready access to
Renewtrient® in the USA?"
Dr. DEAN "I think this is one of the
overall beneficial substances that everybody, and I mean everybody, from
children to senior citizens should be taking to improve all aspects of their
health." "I think this is one of the overall
beneficial substances that everybody, and I mean everybody, from children to
senior citizens should be taking to improve all aspects of their
health."
PHIL "I've really enjoyed this
interview with you and we've never actually done anything quite like this in the
Anti-Aging Bulletin before. Perhaps if the readers have enjoyed this type of
informal format they could contact IAS and let us know. Then we would be
prepared to do some other subjects or products along a similar
line." "I've really enjoyed this interview with
you and we've never actually done anything quite like this in the Anti-Aging
Bulletin before. Perhaps if the readers have enjoyed this type of informal
format they could contact IAS and let us know. Then we would be prepared to do
some other subjects or products along a similar line."
Dr. DEAN "Sure it's been fun and
perhaps the next interview can take place at the IAS Regeneration Center in
Monte Carlo?" "Sure it's been fun and perhaps the
next interview can take place at the IAS Regeneration Center in Monte
Carlo?"
PHIL "Why not indeed! Dr. Dean thank
you very much for your time and hospitality." "Why not indeed! Dr. Dean thank you very much for your time and
hospitality."
Dr. DEAN "My pleasure." "My pleasure."
ALL INFORMATION IS EDUCATIONAL AND
PROVIDED UNDER IAS TERMS AND CONDITIONS. IT DOES NOT AND SHOULD NOT
REPLACE THE ADVICE OF YOUR PHYSICIAN.
------------------------------------------------------------------------------------------------------------------------------------------------------------ The
following article is copyrighted and cannot be copied without the written
permission of International Antiaging Systems, Box 337A GY1, Channel
Islands, Great Britain
Discover the Regenerative
Effects of GHB, the elixir of life! By
James South MA
GHB (Gamma-Hydroxybutyric Acid) is a
hydroxylated form of the short-chain fatty acid. GHB is also closely related to
GABA (Gamma-Aminobutyric Acid), the chief inhibitory neurotransmitter of the
mammalian nervous system. GHB was first synthesised in 1960 by H. Laborit, a
French physician. Laborit was interested in studying the action of GABA in the
nervous system, but GABA was known to be unable to cross the blood-brain
barrier. Laborit hoped that by adding a hydroxyl (OH) group to butyric acid, the
resulting molecule-GHB-would be protected from being destroyed by beta-oxidation
(the process by which cells ‘burn’ fat), would cross the blood-brain barrier,
and then serve as a precursor to GABA once in the brain. (1). However, GHB
turned out to be pharmacologically distinct in many of its actions from GABA,
even though later research showed that GABA and GHB are interconvertible in the
brain through a common metabolite- Succinic Semialdehyde (SSA).
(2,4).
Somewhat surprisingly, in 1963 Bessman and
Fishbein first reported GHB to be a naturally occurring molecule in the brain,
and by 1970 the work of Roth and Giarman had proven conclusively that GHB is a
normal, natural brain metabolite. (3),
It is now known that 0.08% to 0.16% of whole
brain GABA is normally converted to GHB each minute. (4). And in a 1992
‘mini-review’ of the significance of GHB in the brain, G. Tunnicliff concluded:
"There is little doubt that GHB is not merely a by-product of GABA metabolism.
Clearly it has distinct neuro-physiological and pharmacological actions, many of
which are undoubtedly the result of the activation of specific GHB receptors....
The evidence is fairly substantial that GHB plays a role in the functioning of
the central nervous system, perhaps as an inhibitory transmitter acting on
dopaminergic neurons.... The ...actions of GHB make it a viable candidate as a
neurotransmitter or neuromodulator in the CNS." (5).
Also somewhat surprisingly, research has shown
that GHB is naturally present in kidney, heart, skeletal muscle, and brown fat,
often at levels 10 to 20 times higher than whole brain GHB levels.
(2,4).
In his detailed 1989 review of GHB as an
endogenous regulator of energy metabolism, pioneer GHB researcher M.Mamelak
stated: "Clinical and experimental work indicate that GHB can protect both
central and peripheral tissues from the damaging effects of hypoxia or excessive
metabolic demand.... GHB could function naturally to regulate cell activity when
metabolic energy is in short supply." (4).
GHB has been the subject of hundreds of
published scientific papers since 1960 (see the bibliographies in references 4
and 6). GHB is a legal drug in various European countries, including France and
Italy, where it has been in clinical use since the early 1960’s. It has been
widely used as an anaesthetic- Laborit summarized the anaesthetic benefits of
GHB in 1964, based on 6000 (!) case-reports. (1). GHB is also used to treat
alcoholism, alcohol withdrawal syndrome, opiate addiction and opiate withdrawal
syndrome. (7,27-29). GHB has also proved useful in obstetrics. (8). GHB is also
used in Europe to treat narcolepsy, a serious and disabling sleep disorder, as
well as insomnia. (7). Yet in spite of the mere 40-year history of safe clinical
and experimental use of GHB, in November 1990 the U.S. Food and Drug
Administration (FDA) declared-through a press release-that GHB was an ‘illegally
marketed drug’, and claimed that it was a danger to public health.
Since the U.S. Dietary Supplement Health and
Education Act of 1994 (DSHEA) in effect classified GHB as a dietary supplement,
not to be regulated only as a drug, and because the FDA had not bothered to
legally classify GHB as a drug before DSHEA, the FDA has now backed off its
claims that GHB is illegal at the federal level in the U.S. Instead, the FDA has
orchestrated a campaign to get the various U.S. states to declare GHB an illegal
drug, since DSHEA does not operate at the state level. The FDA’s smear-and-fear,
disinformation and demonization campaign has been based in significant part on a
brief 1992 paper by California medical bureaucrats Chin, Kreutzer and Dyer that
claimed "The drug GHB is a substance with documented clinical actions consistent
with severe neurotoxicity." It is therefore necessary to look closely at the
clinical and experimental record of GHB to ascertain if there is any documented
evidence or general consensus of GHB as a "severe neurotoxin."
When scientists wish to determine the relative
safety of a drug or nutrient, they perform experiments to establish a substance
LD50. This is the amount of the substance (lethal dose) necessary to kill 50% of
the test animals. The LD100 is the lethal dose that kills 100% of the test
animals. In his 1964 GHB review, Laborit reported: " In rat, the LD50 is
1.70gm/kg [of animal bodyweight]; the LD100, 2 gm/kg. The cause of death is
respiratory depression, and under artificial respiration, rabbits can tolerate
up to 7gm/kg. The dog is less sensitive.... In the rat no significant
differences are observed between controls and the group injected daily with a
1/10th of the LD50, particularly with respect to weight, bone marrow, liver and
kidneys [where toxic effects frequently show up]."(1)
In his 1969 review on GHB, anaesthesiologist
M. Vickers wrote: "In acute experiments in animals, the LD50 has been 5 to 15
times the dose necessary to produce coma. Death was probably due to sodium
intoxication rather than to any effect of the active drug.... No deaths have
been reported in man attributable to acute toxicity. The author [Vickers] has
used doses of 20g to 30 g. [28,4 g = 1 oz] per 24 hours for several days without
ill effect.... No toxic effect on the liver or kidney have been reported.... Its
low acute toxicity may make it a safer sedative drug to prescribe when suicide
is a possibility." (8)
While extrapolation from animal LD50 studies
is at best an approximation of a drug’s toxicity for humans, the rat LD50 of 1.7
g/kg of bodyweight would translate into 85 g (3 ounces) for a 50 kg (110 pound)
person. This would equate to roughly 10 to 15 heaping teaspoons of GHB - rather
more than anyone is likely to ingest at one time. It should also be noted that
Laborit’s LD50 was based on injecting the GHB, rather than taking it orally, as
humans normally do. Injecting GHB at least doubles its effect, as Laborit noted.
(1) Thus a 50 kg/110 pound person would really need 170g (6 ounces) or 20 - 30
heaped teaspoons of GHB taken orally, to equal the rat LD50.
Another estimate of the human lethal dose is
provided by the official package insert for the legal French GHB drug (Gamma-
OH™), where the human LD50 is stated as 4.28 g/kg. This would equate to an oral
lethal dose in excess of 200 g (7 ounces) for a 50 kg/110 pound
person.
A perusal of the published GHB literature
attests to the safety and low toxicity of GHB. In a 1977 report measuring the
effect of 2.5g intravenous GHB given to 6 healthy young men, Takahara et al
reported: "All volunteers except one fell asleep ... after GHB injection and
slept for 30 to 150 min. As side effects, one volunteer complained of nausea and
another volunteer had orthostatic hypotension [dizziness upon arising] after
test." (9) In a 1979 report on the use of GHB to treat 16 narcolepsy patients
Mamelak and Broughton stated: "There have been very few adverse clinical effects
with [GHB] treatment [3.75 to 6.25 gm, divided into 2 or 3 oral doses] and no
abnormal laboratory findings. Minor side effects of GHB have been seen for the
first few days in a number of patients which consisted of a ‘thick head’, ocular
discomfort, and other apparent hangover effects, but these were rare after one
week.... The main disadvantage at present is its [GHB] short duration of
action." (10) (Hardly a sign of "severe neurotoxicity a la chin and
colleagues!)
In a 1985 report on treating 30 patients with
narcolepsy, Scharf and co-workers specifically emphasize the toxicity and side
effects of standard drugs used to treat narcolepsy (amphetamines, Ritalin™, and
tricyclic antidepressants). They note that in contrast "Our results confirm
those of previous clinical studies of GHB, namely, that it is a safe, non-toxic
substance...." (11). And in a 1986 review of 48 patients who took GHB for 6
months to 9 years as a narcolepsy treatment, Mamelak, Scharf and Woods report
that: "Few adverse effects have been observed. All patients have been followed
with serial liver, renal, and blood studies, periodic chest X-rays, and
electrocardiograms; no abnormalities have been noted. On the first few nights of
treatment with GHB, two patients had enuresis [bed-wetting].... Patients who
resist the sleep-inducing properties of the drug may become confused and
emotionally [upset]...." (12).
In their 1989 double-blind study on GHB to
treat narcolepsy, Scrima et al note: "The total number of adverse reactions
[primarily upset stomach, muscle weakness, urinary urgency and dizziness]
reported during GHB treatment was less than during the placebo treatment [!]....
No patient discontinued participation in the study because of side effects. The
blood test results... indicated that GHB did not cause hypokalemia [low blood
potassium] or other marked changes in blood chemistry." (13). And in their 1990
paper on GHB use with narcoleptics, Scrima et al remark: "GHB is a more
appealing treatment for narcolepsy patients than other alternative
treatments.... GHB has been found to cause only minor side effects that usually
occur only during the first few days of treatment." (14).
In this remarkable paper integrating masses of
GHB study data, Mamelak makes observations that clearly cast doubt on any claim
that GHB is a ‘severe neurotoxin’. "In man, oral or intravenous doses greater
than 50mg/kg [=3.5g for a 70kg/154 pound person] produce anaesthesia.... The
drug is rapidly metabolized and the central [nervous system] effects of an
intravenous dose of 60-70mg/kg run their course in about 2 hours.... In the
rat... 600mg/kg [=42g for a 70kg person]... produces a reversible continuum of
EEG changes... Complete recovery occurs about 2 hours after the drug has been
given.... As much as 1000mg/kg [=70g for a 70kg person] have been given to
monkeys without harmful effects.... As has been demonstrated in other
circumstances, GHB appears to promote survival under hypoxic [low oxygen]
conditions." (4). Does that sound like any ‘severe neurotoxins’ you
know?
Mamelak has also noted the unique ability of
GHB to reduce brain glucose consumption, without toxic effect. Thus, he states:
"An intravenous dose of 600mg/kg of [GBL, which is converted to GHB by an enzyme
in the blood], for example, reduces glucose utilization in grey matter by 68%
compared with 44% in white matter [of the brain]. Similar results have been
reported with GHB. It is remarkable that in spite of these extraordinary degrees
of metabolic depression full tissue recovery can take place.
Other [CNS] depressants such as the
barbiturates also produce comparable effects on... energy metabolism, but doses
of barbiturates which would be necessary to inhibit cerebral glucose utilization
as much as that observed with [GBL] and GHB would likely be lethal."
(4).
By now it should be evident that (to put it
politely) Chin et al may have exaggerated when they suggested (only by
implication, if you read their statement carefully) that GHB might be a ‘severe
neurotoxin’. And ironically comments made by Chin et al in their paper seem to
contradict the implication that GHB might be a ‘severe neurotoxin’. They point
out that "The prognosis for those who experience GHB poisoning [sic] is quite
good. There are no documented or anecdotal reports of long-term adverse effects
or fatalities...." (2).
Don’t you wish all ‘severe neurotoxins’ (e.g.
Cobra venom) were that benign? (For a detailed dissection and critique of the
Chin paper on GHB ‘poisoning’, see references 7 and 26).
Far from acting like a toxin or poison, GHB
has shown a remarkable range of protective effects in a diverse array of
experimental and clinical conditions. Laborit reported in 1973 that "we
observed... that GHB possesses a definite protective action against convulsions
produced by strychnine, cardiazol and isoniazide," (3). While Mamelak notes that
"GHB can block seizure activity induced by a variety of agents. Those induced by
Kainic acid, strychnine, isoniazide and mercaptoproprionate may be cited as
examples." (4).
Mamelak also reports a wide range of
tissue-protecting actions of GHB. For example "500mg/kg of intravenous GHB
protected rats against the lethal effects of 30 minutes of hypoxia. Under these
conditions none of the GHB-treated rats died in comparison with 45% of the
untreated control rats. Even lower doses of GHB, 200mg/kg, significantly reduced
the subcellular response of the brain to hypoxia in rats exposed to [low oxygen]
atmospheric pressures comparable to those at 10,000 meters [32,000 feet]."
(4).
Mamelak concludes his section on GHB brain
tissue protection by noting that "More so than any protective agent studied,
including the barbiturates with which it is so often compared, GHB retards the
disappearance of oxygen from anoxic cerebral tissue, again demonstrating the
potent [and highly protective] energy sparing effects of this agent."
(4).
Laborit reported in 1964 the anti-convulsive
effects of GHB in protecting mice exposed to pure oxygen under 3.5 times normal
atmospheric pressure. In the control animals this procedure routinely produced
convulsions in all the (non-GHB) animals. "A hypnotic dose of 500mg/kg [GHB]
protects all animals against convulsions (10 mice). With 250mg/kg doses, a
convulsion is noted in one mouse out of 10; the seizure is retarded and of short
duration. In 20 mice, with 200mg/kg, there were three slight and one typical
convulsion." (1).
GHB has also shown a wide range of protective
effects outside the nervous system, especially in conditions of anoxia or energy
insufficiency. GHB has been used to reduce the pain of angina pectoris and
myocardial infarction (heart tissue death). (4). GHB has also been shown to
minimize the deterioration of heart function produced by massive haemorrhage.
(4). Sodium and lithium GHB have been used to prolong the viability of kidney to
be used for organ transplant. (4).
A 1990 study found an amazing effectiveness of
GHB in preventing the intestinal lining damage that normally occurs when blood
supply to the tissue is cut off (ischemia), and then blood is allowed to return
to the tissue (reperfusion). Eight groups of 6 hamsters were studied in a blind
experiment. After 30 minutes of intestinal ischemia, 3 hours of reperusion were
allowed. The animals’ intestines were then subject to careful histological
examination. In untreated animals, 75% +/-6% of the villi (microscopic
finger-like intestinal lining projections) were damaged (haemorrhage and
necrosis). In GHB-treated hamsters, only 8% +/- 3% of the villi were damaged.
Administration of the GHB following ischemia but before reperfusion also
provided significant protection to the controls, with 26% +/- 3% of the villi
damaged. In contrast, Vitamin E failed to provide any protection against the
injury, with 71% +/- 4% of villi damaged. (15).
In a 1991 report Pierrefiche, Laborit and
co-workers detailed the profound protective effect of GHB against
alloxan-induced diabetes. Alloxan is a substance that is routinely used
experimentally to destroy the insulin-producing beta cells of the pancreas. The
rapid uptake of alloxan and an exquisite sensitivity to free radicals (which
alloxan produces en masse) are unique features of these cells. The toxic effects
of alloxan, namely elevated blood glucose due to beta cell destruction, are
prevented by a number of anti-oxidants. Different levels of GHB, from 1.5
mmoles/kg to 4.2 mmoles/kg, provided almost complete protection from the
hyperglycaemia induced in the mice which received alloxan but no GHB. Fasting
blood sugar in the alloxan-but-no-GHB mice typically tripled at 48, 72 and 96
hours after alloxan treatment, compared to control mice given only saline (salt)
injection, but neither GHB or alloxan. In the GHB-plus-alloxan mice, blood sugar
levels at 48, 72 and 96 hours after injection remained virtually identical to
the normal fasting blood sugar levels displayed by the saline-control
mice.
Since the beginning of GHB studies in the
early 1960’s, GHB has been shown to have a wide range of metabolic effects in
animals and man.
Perhaps the most well-documented effect of GHB
on brain metabolism is the increase GHB causes in brain dopamine. "Systemic
administration of GHB leads to decreased dopaminergic [nerve] activity. This is
probably a reflection of GHB’s inhibitory action on the cell body of
dopamine-releasing neurons. In the substantia nigra [the chief dopamine brain
area where damage leads to Parkinson’s disease] this initially leads to a
decrease in dopamine release and an accumulation of dopamine at nerve terminals.
Finally, a stimulation of dopamine release occurs." (5). Because of GHB’s
dopaminergic actions, it has been used with limited success in treating
Parkinson patients. "Major studies were conducted in Italy. One study showed
that in 9 patients out of 10 a single dose of 400mg/kg... produced some
improvement... within 24 hours, resulting in a sensation of comfort and
regulation with improved ideation and renewed initiative. Within 2-7 weeks
following initiation of treatment,... there was an improvement in tremors,
hypertonia [muscle rigidity] and in the writing test. One female patient
regained normal gait [walking] after having been confined to bed.... These
results were confirmed by Ferrari et al." (17). GHB has moderate or little
effect (depending on dosage) on acetylcholine, noradrenanlin and serotonin
activity. (4).
GHB has been shown to induce major increases
in plasma growth hormone (GH) levels. In 10 patients scheduled for surgery,
intravenous GHB anaesthesia (100-150mg/kg) increased plasma GH levels 6-fold,
from 2.2ng/ml pre-induction, to 13.8ng/ml at 45 minutes after GHB injection. GHB
induced only slight increase in plasma cortisol levels, from 14mcg/ml to
23.6mcg/ml. (18). In a 1977 report Takahara et al injected 2.5g GHB into 6
healthy men (25-40 years old). Compared to the GH levels after saline injection
in the same 6 men, plasma GH levels rose 16-fold, from about 2ng/ml to 32ng/ml
by 60 minutes after GHB injection. Plasma GH levels were still 6 times normal
(13ng/ml) 2 hours after GHB injection. Plasma prolactin levels rose to a maximum
of 5 times base-line levels at 60 minutes. (9). It has been known since the
1960’s that slow-wave sleep (EEG sleep stages 3 and 4) induces GH-release. Thus
Sassin et al reported in 1969: "Those subjects with more frequent slow-wave
cycles had initial peaks [of GH release] of greater magnitude and more frequent
secondary [GH] rises.... We conclude from our data that [GH] release is related
not only to sleep but particularly to non-REM portions of... sleep,
especially... EEG stages 3 or 4.... Release of GH in sleep suggests an anabolic
function of slow-wave sleep...." (30). And as is discussed in more detail below,
GHB in normal subjects speeds up onset and increases amount of slow-wave (stage
3 & 4) sleep. (19).
GHB typically induces a slight slowing of the
heartbeat (bradycardia). GHB also slows and deepens breathing, but does not
depress the breathing centers in the brain stem, unlike e.g. barbiturates and
benzodiazepines. Even with high doses of GHB the respiratory centers in the
brain do not lose their sensitivity to carbon dioxide in the blood-the normal
stimulus to breathing. (17). GHB also induces a remarkable hypotonia, or extreme
relaxation of the musculature. In medical contexts where GHB is used
anaesthetically, this promotes easier insertion of breathing tubes into the
throat. (17). GHB also induces a mild hyperthermia, apparently due to its
decrease in brain and muscular metabolic rate. (4).
Perhaps the most striking physiologic feature
of GHB is its rapid induction of sleep, even when given orally. Studies done in
the 1960’s showed GHB sleep to be essentially identical to normal physiologic
sleep. Thus Okada et al in 1967 reported their study with 19 men who received
GHB intravenously. They slept deeply, with EEG records similar to natural sleep.
"Awakening took place very rapidly, 3 hours after administration, without
disorientation. The authors believe that the therapeutic effect of GHB is very
similar to that of physiological sleep." (17).
GHB has been used therapeutically since the
1970’s to treat narcolepsy, (a severe and disabling sleep disorder), with
generally excellent results. It is generally agreed that GHB seems to
consolidate and make more efficient the night-time sleep of narcoleptics, so
that they don’t fall asleep uncontrollably in the daytime. (10-14). In a 1990
double-blind study, Lapierre and colleagues reported that GHB induced normal
sleep in their subjects, but with an increase in the restorative (and GH-release
promoting) slow-wave sleep (stages 3&4), and a more efficient REM (rapid eye
movement) sleep, as well, while lessening time in the shallow initial stage of
sleep (EEG stage 1). (19).
GHB is not a foreign substance which must be
detoxified through the liver’s detoxification system, unlike most other
psychoactive drugs (e.g. barbiturates, benzodiazepines, SSRI’s like Prozac,
phenothiazines, etc.). As Vickers notes, "[GHB] represents a unique development
in the pharmacology of anaesthesia. It is the first compound to exert a
pharmacological action which is at the same time fully metabolized as an
energy-producing substrate." (8). When GHB is catabolized (broken down), it is
first converted into Succinic Semialdehyde (SSA). SSA is then converted to
Succinic Acid, a Krebs cycle metabolite. The Succinic Acid is then oxidized
through the Krebs cycle in the ATP-producing mitochondria, eventually becoming
water and carbon dioxide, as has been experimentally verified following
radioactively-labelled GHB administration. (17). Thus, GHB leaves no ‘toxic
residue’ in the body, unlike virtually all other drugs. GHB is rapidly
metabolized in the human body, with a half-life of only 35-40 minutes. (7).
Because it is so rapidly metabolized, its acute effects typically last only 2-3
hours.
The pioneering work of H. Laborit on GHB over
several decades has led him to elaborate on extremely detailed explanation of
the homeostatic normalizing, restorative, regenerative effects of GHB. (1,3,17).
Laborit discovered that in effect, GHB serves as a switching agent to cycle
brain/muscle activity from its high-energy output, "yang", daytime activities to
a "yin," restorative/recuperative repair and rebuilding (anabolic) phase during
night-time sleep. Virtually all of the known properties of GHB, including its
slowing of heartbeat and respiration, mild hypothermia, muscle relaxation,
lowered brain and muscle energy consumption, increasing of the deep and
restorative sleep phases (stage 3 & 4 slow-wave sleep), increasing growth
hormone output, to name just a few, are involved in this integrated
‘regeneration reflex’. At the center of Laborit’s explanation of the therapeutic
nature of GHB-induced sleep is what he terms the ‘neuron-neuroglia as a
metabolic and functional pair’. (3)
The human brain is generally ‘guesstimated’ to
contain 10-100 billion neurons. Yet it also contains roughly 10 times as many
glial or neuroglial cells, also called ‘astrocytes’. The astrocytes completely
surround neurons, and in effect comprise the second half of the blood-brain
barrier. Astrocytes completely surround blood vessels feeding the brain, and
play a role in distributing at least some blood-borne nutrients to the neurons,
as well as having key roles in disposing of some neuronal metabolite wastes.
(20). Astrocyte neuroglia also secrete a number of growth factors for neurons.
Some, like nerve growth factor, may stimulate the neuron as a whole, while
others may increase growth of axons. (20). Neurons are the electrically active
signalling cells in the brain, transmitting billions of electrical impulses
between each other every second. Neurons have the highest metabolic rate of any
cells in the body, and are furious ‘burners’ of glucose (blood sugar) in the
glycolytic-mitochondrial energy cycles to generate the massive ATP energy
supplies they run on. Glial cells are metabolically more passive, ‘burning’
sugar primarily through the glycolytic and pentose shunt pathways.
(3).
Drawing upon his own laboratory’s research as
well as the published research of hundreds of other scientists, Laborit
discovered that GHB reverses the normal daytime pattern of energetic activity in
the brain. When we’re awake, the glial cells are relatively quiescent, while the
billions of neurons are intensely metabolically and electrically active. During
normal sleep, and even more so during GHB sleep, the electrical-metabolic
activity of neurons quiet down (especially during slow-wave sleep) and glial
cells become more active. (metabolizing glucose through the pentose shunt, a
non-oxygen using pathway). The pentose shunt generates two key substances that
are critically important for neurons to regenerate themselves during sleep, when
they must restore their ion balances (sodium/potassium) and neurotransmitter
stores, as well as engage in new protein synthesis. The pentose pathway
generates the 5-carbon sugar, ribose, which is the base of RNA. RNA in turn, as
messenger, transfer, and ribosomal RNA, is the key to new protein synthesis.
During sleep, neurons must repair the damage to their protein structures (e.g.
the antenna-like neurotransmitter receptors on their cell membrane surfaces,
microtubules, etc.) as well as elaborate new protein involved in memory
consolidation.
The pentose pathway also generates NADPH, the
chief ‘reducing equivalent’ of cells. (25). It is NADPH that ultimately allows
neurons to repair the free radical damage created by the combination of their
high daytime oxygen-using metabolic activity and the high polyunsaturated fat
content of brain mitochondrial and cell membranes.
In the course of mitochondrial ATP bioenergy
metabolism, neurons inevitably generate masses of hydrogen peroxide (H2O2).
(22). Neurons are particularly vulnerable to damage by H2O2. (21,22). The main
detoxifier of H2O2 is an enzyme called ‘glutathione peroxidase’ (GSH-Px). (21).
GSH-Px in turn requires reduced glutathione (GSH) to dispose of H2O2 and the
lipid peroxides (‘rancid fats’) that H2O2 creates in brain cell and
mitochondrial membranes. (21). GSH is also involved in protecting
against/repairing oxidized proteins. (21). Unfortunately, neurons are unable to
create GSH by themselves, and must depend upon glial cells to provide them with
it. (24). When the neurons use GSH to detoxify H2O2, lipid peroxides, oxidized
proteins, etc., the reduced glutathione (GSH) is ‘burned up’ and becomes
oxidized glutathione (GSSG). And this is where the neuroglia ‘come to the
rescue’. When GHB stimulates glial pentose pathway metabolism, this produces
NADPH. The NADPH then combines with the oxidized glutathione (GSSG),
regenerating it back to the free radical-quenching reduced glutathione (GSH).
GSH is also essential for regenerating vitamin E and vitamin C after they have
‘sacrificed’ themselves to quench various types of free radicals. (21). Thus,
because GHB is such a powerful and effective stimulator of glial pentose pathway
metabolism, (1,3,4,16,17,23). and because GHB simultaneously slows down the
free-radical producing mitochondrial energy metabolism in neurons, (3,4). GHB,
far from being a ‘severe neurotoxin’, in effect becomes the anabolic agent to
promote healing and restoration of neurons during sleep!
GHB: Other Uses
Given the space limitations of this article,
it is impossible to present an in-depth summary of the many uses of GHB reported
in the scientific literature. From a life extension/enhancement perspective, the
unique ability of GHB to promote brain structure/function regeneration during
sleep must surely be its most important general use. Laborit details other uses
for it, including psychotherapy, (17) anti-depressive and anti-anxiety therapy,
(17) and sexual disorders. (17) With regard to sexual disorders he notes: "Since
GHB causes disruption of neocortical pathways, it suppresses inhibition and
creates a special condition relaxing neurotic controls and defences. Greater
emotional liability may thus develop and produce readiness for stronger
affectivity [feelings]. This ‘relaxing’ effect has been used very efficiently in
certain sexual inhibitions that produce anxiety syndromes or real infirmities
(premature ejaculation, frigidity). This effect is not aphrodisiac, but rather
an effective or libidinal action-stimulating relationship, associated with an
objective... sensitivity which produces stronger [clitoral] and vaginal
sensitivity in women and marked delay of ejaculation in men."
GHB:
Cautions! The published literature on GHB
stretching almost 40 years has consistently shown it to be a safe and non-toxic
substance, rapidly metabolized, usually within 2 or 3 hours. However, because of
its powerful sleep inducing and muscle relaxant effects, it must be used with
care and caution! In addition, GHB may potentate the neuro-depressive effects of
other agents (e.g. alcohol, opiates, benzodiazepines, barbiturates, etc.), all
of which can by themselves severely depress-or even stop!-breathing. Thus the
following cautions must be observed to ensure safe and responsible GHB
use.
1) Do not EVER mix GHB with central nervous
system depressants including but not limited to: benzodiazepines- ‘minor
tranquillisers’ such as Valium, Librium, Xanax, or Halcion; ‘major
tranquillisers’ such as Thorazine, Haldol or Stellazine; opiates-such as
codeine, morphine, heroin, opium, or Vicodin; barbiturates such as
phenobarbital; alcohol; or even various non-prescription allergy and sleep
remedies.
2) Do not drive or operate dangerous devices
or machinery (e.g. chainsaws, guns, power tools, construction machinery, etc.)
while under the influence of GHB.
3) GHB has a rapid, but variable, onset of
action when taken orally, and taking GHB after food may delay its action.
Therefore it is unwise to delay going to bed after taking GHB. You may literally
pass out on the couch, at the dinner table, going upstairs, etc. if you delay
after taking GHB. Indeed, in most GHB sleep studies, subjects are advised to
take GHB once they’re already in bed. It is also best NOT to take GHB right
after a meal (wait 2-4 hours, depending on meal size) as this may cause nausea
or even vomiting in some individuals.
4) If you choose to ‘cancel’ your choice after
taking GHB, a large cup of strong caffeinated coffee may counteract the GHB,
depending on the dose of GHB taken. (4). This is not recommended as a ‘standard
practice’, though.
GHB: Side
Effects GHB is generally considered to be without
serious side effects. However, depending on unique individual health, emotional,
metabolic, psychoactive drug history and liver status effects, GHB can have
various ‘side effects’. These may include fatigue and drowsiness, dizziness and
‘light-headedness’, nausea, diarrhoea, and occasionally, vomiting. Ataxia
(clumsiness, poor co-ordination) may occur. Myoclonias (spasming or jerking of
muscles, especially of limbs or face) may occur during the onset of GHB sleep.
On rare occasions bed-wetting, confusion and sleepwalking may occur-although
sleepwalking has only been reported in narcoleptics. These effects are
temporary, and will usually dissipate with 4-24 hours after a GHB
dose.
GHB:
Contraindications "There are only very few
contraindications: severe alcoholics and epileptics..., patients with eclampsia,
severe arterial hypertension, or bradycardia caused by conduction modifications.
It should be noted that all hypolipemias with diarrhoea, vomiting, Cushing’s
syndrome, and renal duct lesions caused by chronic corticoid [cortisol,
prednisone, etc.] treatment must first be thoroughly diagnosed and have
potassium chloride prescribed before GHB treatment." (17).
GHB:
Dosage Sleep studies have typically used 1.5 to
3gms GHB at bedtime, with possibly a second or third (1-2.5gm) dose if subject
awakens during night and can’t return to sleep. Many people who use GHB as a
sleep aid/restorative find their sleep need decreases 1/2 to 2 hours/night, yet
they feel more rested than usual. Thus only those who demand their ‘full 8
hours’ of ‘coma’ before arising would be likely to need a third dose during the
night.
For use as a sexual aid, probably only 1/2gm
is needed (even slightly more, and sleep may ensue-that’s usually not a ‘sexual
aid’!).
Some people have reported 1/2gm, used
occasionally, is effective as an anti-anxiety aid, or to restore emotional
equilibrium after an intense shock or emotional ‘blow up’.
REFERENCES
-
H. Laborit (1964) ‘Sodium 4 - Hydroxybutyrate’ Int J
Neuropharmacol 3, 433-52.
-
M.-Y. Chin et al (1992) ‘Acute Poisoning from
Gamma-Hydroxybutyrate in California’ 156, 380-84.
-
H. Laborit (1973) ‘Gamma-Hydroxybutyrate, Succinic
Semialdehyde and Sleep’ Prog Neurobiol 1, 255-74.
-
M. Mamelak (1989) ‘Gammahydroxybutyrate: An Endogenous
Regulator of Energy Metabolism’ Neurosci & Biobehav Rev 13, 187-98.
-
G. Tunnicliff (1992) ‘Significance of
Gamma-Hydroxybutyric Acid in the Brain’ Gen Pharmacol 23, 1027-34.
-
C. Cash (1994) ‘Gammahydroxybutyrate: An Overview of the
Pros and Cons for it Being a Neurotransmitter and/or a Useful Therapeutic
Agent’ Neurosci & Biobehav Rev 18, 291-304.
-
W. Dean et al, GHB - The Natural Mood Enhancer’,
Petaluma, CA: Smart Pub., 1998.
-
M. Vickers (1969) ‘Gammahydroxybutyric Acid’ Int
Anaesthesia Clin 7, 75-89.
-
J. Takahara et al (1977) ‘Stimulatory Effects of [GHB] on
Growth Hormone and Prolactin Release in Humans’ J Clin Endocrinol Metab 44,
1014-17.
-
R. Broughton & M. Mamelak ‘The Treatment of
Narcolepsy-Cataplexy with Nocturnal Gamma-Hydroxybutyrate’ Can J Neurol Sci 6,
1-6.
-
M. Scharf et al (1985) ‘The Effects and Effectiveness of
Gamma-Hydroxybutyrate in Patients with Narcolepsy’ J Clin Psychiatry 46,
222-25.
-
M. Mamelak et al (1986) ‘Treatment of Narcolepsy with
Gamma-Hydroxybutyrate. A Review of Clinical and Sleep Laboratory Findings’
Sleep 9, 285-89.
-
L. Scrima et al (1989) ‘Efficacy of Gamma-Hydroxybutyrate
versus Placebo in Treating Narcolepsy-Cataplexy: Double-Blind Subjective
Measures’ Biol Psychiatry 26, 331-43.
-
L. Scrima et al (1990) ‘The Effects of
Gamma-Hydroxybutyrate on the Sleep of Narcolepsy Patients’ Sleep 13, 479-90.
-
A. Boyd et al (1990) ‘The Protective Effect of
Gamma-Hydroxybutyrate in Regional Intestinal Ischemia in the Hamster’
Gastroenterol 99, 860-62.
-
G. Pierrefiche et al (1991) ‘Protective Effects of
Gamma-Hydroxybutyrate on Alloxan Induced Diabetes in Mice’ Res Comm Chem Path
Pharmacol 71, 309-19.
-
J. Muyard & H. Laborit (1977) "Gammahydroxybutyrate’
in Psychotherapeutic Drugs, Vol. 2, part 2, E. Usdin & I. Forrest, eds.,
1339-75. N.Y: Marcel Dekker.
-
T. Oyama & M. Takiguchi (1970) ‘Effects of
Gamma-Hydroxybutyrate and Surgery on Plasma Human Growth Hormone and Insulin
Levels’ Aggressologie II, 289-98.
-
O. Lapierre et al (1990) ‘The Effect of
Gamma-Hydroxybutyrate on Nocturnal and Diurnal Sleep of Normal Subjects’ Sleep
13, 24-30.
-
H. Kimelberg and M. Norenberg (1989) ‘Astrocytes’ Sci Am
260, 66-76.
-
S. Levine & P. Kidd, Antioxidant Adaptation, S.F. :
Biocurrents Pub., 1985.
-
R. Bradford & H. Allen, Oxidology, Chula Vista, CA:
R.W. Bradford Foundation, 1997.
-
P. Taberner et al (1972) ‘The Action of
Gamma-Hydroxybutyric Acid on Cerebral Glucose Metabolism’ J Neurochem 19,
245-54.
-
J. Sagara et al (1993) ‘Maintenance of Neuronal
Glutathione by Glial Cells’ J. Neurochem 61, 1672-76.
-
D. Reed (1986) ‘Regulation of Reductive Processes by
Glutathione’ Biochem Pharmacol 35, 7-13.
-
J. Morgenthaler & D. Joy, Better Sex Through
Chemistry, Petaluma, CA: Smart Pub. 1995.
-
L. Gallimberti et al (1989) ‘[GHB] for Treatment of
Alcohol Withdrawal Syndrome’ Lancet, 9-30-89, 787-89.
-
L. Gallimberti et al (1993) ‘Gamma-Hydroxybutyric Acid
for Treatment of Opiate Withdrawal Syndrome’ Neuropsychopharmacol 9, 77-81.
-
L. Gallimberti et al (1994) ‘Gamma-Hydroxybutyric Acid in
Treatment of Opiate Withdrawal’ Eur Arch Psychiatr Clin Neurosci 244, 113-14.
-
J. Sassin et al (1969) ‘Human Growth Hormone Release:
Relation to Slow-Wave Sleep and Sleep-Walking Cycles’ Science #3892,
513-15.
ALL INFORMATION IS EDUCATIONAL AND
PROVIDED UNDER IAS TERMS AND CONDITIONS. IT DOES NOT AND SHOULD NOT REPLACE THE
ADVICE OF YOUR PHYSICIAN.
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