by Robert Mason Ph.D.
mesylates, co-dergocrine, dihydroergotoxine,
are all ergot
derivatives that share a common
ancestry; they all derive from a type of fungus that grows on
article evaluates three of the most commercially used ergots: bromocriptine (pronounced brome-o-cript-teen), Hydergine, and
Hydergine- the most popular ergot
we move onto one of the most popular and widely used smart-drugs that has been
in use for over 40-years- Hydergine (pronounced hi-der-gene).
has received only “mild” reviews whilst being used to treat senile
dementias, (although it is widely regarded to have been used in dosages that
were far too small for those purposes). However, Hydergine presents itself as a
remarkable anti-aging medicine and a adjunct for the treatment of age-related
is known to have all the following effects:
blood supply to the brain.
oxygen delivered to the brain.
metabolism of brain cells.
the brain from insufficient oxygen supply.
the deposit of the age pigment lipofuscin in the brain.
free radical damage to brain cells.
intelligence, memory, learning and recall.
is unique in that it is both a free radical generator and a free radical
scavenger. At optimum concentrations, oxygen neutralizes more free radicals than
it produces. Either too much or too little can upset the balance and generate
the production of free radicals, which in turn can lead to aging. One of the
major ways in which oxygen generates free radicals is its reaction with
unsaturated fats, a process called peroxidation.
Unfortunately, our brain
cells contain more unsaturated fats than any other part of the body, therefore
it is our brains that are most susceptible to peroxidation. Here are some
conditions that can cause major peroxidation and the formation of massive
amounts of potent free radicals:
(Carbon monoxide greatly reduces the oxygen carrying ability of the blood).
cigarettes (Nicotine constricts blood vessels and decreases oxygen supply to
the brain. It is estimated that those who smoke more than 20 cigarettes a
day lose at least 7% of the normal blood flow to the brain).
European countries use Hydergine for emergencies and accidents that involve
shock, hemorrhage, strokes, heart attacks, drowning, electrocution and drug
over-dose. Hospitals give Hydergine to patients before an operation in order to
gain time in case of any ensuing crises. This is because Hydergine helps to
stabilize brain oxygen levels, if they are too high Hydergine
lowers them, if they are too low then Hydergine
improves them. This was graphically illustrated in a cat experiment.
groups of cats were anaesthetized and their brains electronically monitored. The
scientists reduced the brain’s blood supply (and therefore oxygen supply). The
cats in the control group (i.e. no Hydergine ) had brain damage within 5-minutes
and died within 15-minutes. However, the cats in the pre-Hydergine treated group
had strong brain wave patterns up to 45-minutes later. This experiment proved
two things, firstly that a decrease in the normal oxygen balance results in
tremendous free radical damage and secondly that Hydergine protects against this
free radical damage when the oxygen level is upset.
has also been shown to increase the level of neurotransmitters in the brain,
whilst this may not be significant enough for the treatment of senile dementia,
such action has implications and benefits for the treatment and prevention of
age-related mental decline.
is also evidence that
the growth of dendrite nerve fibers. Dendrites can normally be expected to
decline with aging and some scientists have associated the number and density of
dendrites with intelligence.
decrease in brain cell connection has been hypothesized to be due to an
impairment in the energy supply at synaptic regions. Because of Hydergine’s
known ability to improve nerve cell metabolism, a group of Italian scientists
studied the ultra-cellular features of synaptic mitochondria to see if long-term
Hydergine treatment could delay or prevent the loss of synaptic connections.
mitochondria are the “intracellular powerhouses” where the universal energy
molecule- ATP (adenosine triphosphate) is produced. The scientists found that
the number of mitochondria are greatest at about 12-months of age in rats (equivalent
to a 25-year old in human terms) and then progressively decreases. However, the
size of the mitochondria increased progressively after 12 months. Thus in young
adult rats, the energy required at synaptic regions is provided by a large
number of small, highly efficient mitochondria, whereas in old rats, energy is
produced by a smaller number of larger, less efficient mitochondria.
astonishingly after treatment with
it can be seen that the total mitochondrial volume of old rats was nearly the
same as the young rats. Furthermore, the mitochondrial size was altered to a
more youthful direction.
its ergot relatives, Hydergine has also shown itself to be a mild vasodilator
(it enhances brain blood flow) and improves the uptake of the brain energy
molecule- glucose. Hydergine also reduces the accumulation of the age-related
and again, clinical trials indicate that Hydergine can improve cognitive
functions, mental alertness, clarity and mood.
Dosages, Side Effects, and Contraindications
literally thousands of published clinical research papers and Hydergine ’s
decades of use around the world, it has proven itself to be nontoxic and
relatively safe. Its potential side effects include mild nausea, gastric
disturbances and bradycardia. It should be avoided by people who suffer from
psychosis, or those with low blood pressure or abnormally slow heartbeat. Seek a
health professional’s advice if combining Hydergine (at dosages in excess of
9mg per day) with other ergot derivatives or vasodilators.
people do well at dosages of around 2.25mg to 4.5mg per day with occasional
breaks. The most common side effect of stomach upset can be avoided with the use
of specially coated tablets (known as FAS) or sublingual liquid versions.
its beneficial affects, mild side effects and few contraindications, Hydergine
is ranked as one of the most important anti-aging medicines available today.
is a semi-synthetic derivative of the ergo group of ergot alkaloids is a dopamine
receptor agonist and a prolactin inhibitor. It is a potent D2 agonist
but also displays partial action on D1 receptors) and a prolactin inhibitor.
first major anti-aging use is the enhancement of dopamine, (a key brain
neurotransmitter that undergoes an age-related decline). It
is estimated past the age of 40, people undergo a dopamine
decline of approximately 13% per decade (Ward, Fowkes & Morgenthaler).
Accordingly, some neurologists have stated that “if we all live long enough
we shall all become senile.” This is due to the fact that abnormally low
levels of dopamine (70% to 80% loss) are then diagnosed as Parkinson’s
disease, hence protection and enhancement of the dopamine producing neurons is a
key strategy for anti-aging medicine. Not surprisingly, bromocriptine is
used in conjunction with drugs such as deprenyl and L-dopa
in the management of Parkinson’s disease. But bromocriptine can be used
for anti-aging purposes also.
is also used to inhibit prolactin, one
of the few hormones that actually increases with age. Prolactin is produced by the pituitary gland and
bromocriptine inhibits its release.
has been described as a “fat synthesis hormone” because one of its
primary functions is to trigger lactation (milk production) and weight gain in
pregnancy. In women, bromocriptine has been used to help restore ovulation,
but it also helps to reduce serum prolactin levels in men (although the
precise role of prolactin in men is unclear).
further possible need to control age-related prolactin levels is offered by some
researchers who believe that prolactin is an immune system suppressant.
Bromocriptine increases growth hormone secretion in individuals with normal
growth hormone concentrations, but paradoxically suppresses GH secretion in some
patients with acromegaly (a condition of excessive-production of
GH). Studies indicate that bromocriptine does not affect the release of any
other anterior pituitary hormones.
to its dopamine enhancement bromocriptine has even been cited as an aphrodisiac,
although little effort has been made to study and confirm this action. There
have been several reports of “better controlled” orgasms and “almost
orgasms” before the real orgasm occurs. If any countries allow for more
medical categories such as “weak orgasm syndrome” or perhaps “clinical
sex-drive loss” then dopamine agonists such as bromocriptine are going to
receive a lot of attention from the pharmaceutical manufacturers, especially in
the wake of Viagra sales.
Another interesting clinical
study administered a component of tobacco called DMBA to rats at a level where
it is known to be very effective in producing breast cancer. However, rats that
had been pretreated with bromocriptine completely avoided any cancer
development. Bromocriptine therefore appears to be a very
potent free radical quencher.
of the most recent studies indicates that bromocriptine may be a candidate for
the treatment of Type-2 diabetes. This is because bromocriptine has been shown
to suppress lipogenesis and improve glucose tolerance and insulin resistance.
animal study suggested that a further action of bromocriptine is to alter CNS
(central nervous system) regulating metabolism and as such has another important
use in helping to prevent weight gain (this would be in addition to its
improvement of diabetic conditions).
Dosages, Side Effects, Contraindications
is a very potent substance and it mustn’t be used by pregnant or lactating
women unless under the guidance of a physician. Side effects include nausea,
dizziness, lowering of blood pressure, hypotension and confusion. The first
three are relatively common, especially when undertaking initial use. It is also
known to increase fertility, and thus “extra care” and contraception is
advised where necessary.
does contraindicate with psychoactive and hypotensive drugs and other dopamine
enhancing drugs (such as deprenyl and L-dopa etc) should only be administered
concurrently under a physician’s guidance. Its effects can also be exaggerated
when combined with other ergots including Hydergine and nicergoline.
there is little need to exceed a dosage in excess of 1.25mg or 2.5mg daily for
most people unless treating a serious medical disorder (and therefore only under
a physician’s guidance). Bromocriptine has a wide and diverse range of
clinically applications, it should be considered to only be an anti-aging
medicine for the serious longevist.
the latest ergot derivative
Nicergoline (pronounced nice-er-go-lean)
is perhaps the latest commercially available variation of all the ergot
preparations. It has become most popular in Japan and indeed many of its
clinical trials have been performed there.
Nicergoline appears to be a
potent vasodilator (improving brain blood flow). On the cerebral level it
prompts a lowering of vascular resistance, an increase in arterial flow and
stimulates the use of oxygen and glucose. However, clinical trials confirm that
nicergoline also improves blood circulation in the lungs and limbs and that
blood platelet aggregation is inhibited.
also indicate that nicergoline does not affect arterial tension and that in
cases of patients suffering from hypertension, it may induce a gradual lowering
of the tension.
approved uses to date have therefore included all of the following:
(of vascular origin).
aggregability and arterial hypertension.
disorders (retinal thromboses, diabetic retinopathy and macular
of a vascular nature (dizziness, auditory problems, hypoacusis).
of senile dementias.
interesting Japanese clinical study on rats showed that nicergoline increases
nerve growth factor in the brains of aged animals, but it shows no statistical
affect upon the brains of young animals!
studies indicate that nicergoline can enhance glutamate re-uptake and protect
the brain against ischaemia (lack of blood flow). This appears to be the main
action of nicergoline and it presents itself as a mild stimulant and enhancer
with long-term protection against brain disorders that may be due to blood,
glucose or oxygen deprivation.
Nicergoline- dosages, side effects and contraindications
effects are usually limited to nausea, hot flushes, mild gastric upset,
hypotension and dizziness. At high dosages bradycardia, increased appetite,
agitation, diarrhea and perspiration have been known to present themselves.
suffering from acute bleeding, myocardial infarction or bradycardia should avoid
nicergoline use. Persons using alpha or beta receptor agonists (such as
propranolol/ Inderal) should not
take nicergoline concurrently as nicergoline is known to enhance the cardiac
depressive effects. Nicergoline is also known to heighten the effects of
pharmaceutical products that produce hypotension, such as other ergot
preparations in high doses (i.e. Hydergine and bromocriptine).
not stated by the manufacturer, other potent vasodilatation agents such as
vinpocetine, xanthinol nicotinate or picamilon should only be used concurrently
under the guidance of a physician.
for known conditions are usually administered at 5-10mg three times a day,
however anti-aging preventative purposes may want to consider 5mg once or twice
a day more adequate.
These three ergot
preparations are all related and yet we can see their differences in the results
of their various clinical studies. Each have differing strengths of reaction and
indeed different effects.
from rye were used by our ancestors for many different reasons, some of them as
rites of passage into adulthood, most were considered to be
“mind-expanding.” Now we know many of the pharmacological actions and roles
they play in mental and memory enhancement and in the slowing of age-related
we understand that brain protection and enhancement is a most important factor-
if not the most important factor for anti-aging medicine and successful