Su alt.baldspot ho trovato questo, voi che ne dite?
FLURIDIL,
A NOVEL DERMO-COSMETIC AGENT FOR TOPICAL APPLICATION IN ANDROGENIC
HAIR LOSS, i.e. EFFLUVIUM AND ALOPECIA
Our lives depend on our hormones. Of those, the sex hormones,
estrogens in women and androgens in men, are of major importance on
influencing almost every aspect of our physiology and social life. The
sex hormone levels physiologically change with age. Thus, after levels
of testosterone and its much more potent derivative,
dihydrotestosterone (DHT), peak in the twenties, a continuous decline
is observed throughout the remainder of life. In women, estrogen
levels peak in their twenties, and then slowly decline until
menopause, where the drop is sometimes drastic. Women also produce
some male sex hormones and inversely, men produce estrogens, initially
in very small quantities, but with years the levels increase until
around 60, women actually produce about as much male sex hormone as
men at that age. As it happens, it is the male hormones which are
responsible for the most usual form of hair loss in both men and
women.
The relationship between the sex hormones and the scalp hair is not
yet fully understood. Early in life, estrogens in women and androgens
in males make scalp hair grow. Then, usually after 30, for reasons not
yet explained, in genetically predisposed males the androgens start
pushing the hair out of the follicles, thus causing hair loss. A
similar phenomenon occurs in women who have reached a stage in their
life when they also produce substantial levels of androgens. Hair
loss, which dermatologists call effluvium, ultimately results in
alopecia. There are also other reasons for alopecia which
dermatologists diagnose and often can treat, but by far the most
prevalent is alopecia caused by the male hormone and therefore called
androgenic.
Testosterone by a small chemical modification normally occurring in
the body changes into an analog, the so-called dihydroxytestosterone
(DHT). As an androgen, this compound is much more powerful. One
approach to the treatment of hair loss, therefore, has been to inhibit
this conversion by a drug. Such a drug has been developed and is
currently marketed as Propecia. The effectiveness of Propecia has been
reported as varying from 30-50% in arresting hair loss, but clearly
there is a disadvantage of a chronic systemic administration and the
uncertainty of what changing basic physiological mechanisms may cause.
Although there are no such indications in the current clinical
studies, no one is certain what manipulation of the normal hormonal
turnover in the body will produce after extended use.
It has always been obvious to researchers that an agent acting only on
the skin and not penetrating into the body would be much preferable
for prevention of hair loss and/or restoration of hair growth. There
have been countless attempts to achieve this goal. One drug originally
developed to decrease blood pressure, minoxidil, was found to induce
upon longer use some hair growth, but only in the vertex area. The
efficacy was reported as somewhere around 30%; the effect was
attributed to a number of factors, most prominently an incidental
increase of blood flow in the scalp. Various vitamins, plant extracts
and other preparations were also developed, but none really could
overcome the essential effect of the male hormones affecting the hair
follicles.
It has been known for a long time that the male hormones can act only
after attaching themselves to a messenger, a small protein, the
so-called androgen receptor. The androgen receptors can be blocked by
certain drugs. These were developed for therapeutic purposes, among
others, to keep in check the cancer of the prostate, which squarely
depends upon the androgen hormones for its growth. These compounds are
given orally and are resorbed from the gut. They act directly by
blocking the androgen receptor. It should be noted that such
inactivation is always temporary since the cells of our body in their
daily cycles continuously manufacture the androgen receptor. Further,
there is the problem that androgen receptors are distributed
throughout our bodies and are also copious in the brain, where their
blockade invariably induces loss of interest in matters of sex, i.e.,
loss of libido. When applied on the scalp these drugs either had no
effect or they were resorbed and passed into the body eliciting
systemic side effects. This is why none of these drugs were developed
into a safe dermo-cosmetic product to combat hair loss.
In an effort to develop a more powerful inhibitor of the androgen
receptor, the biomedical laboratories Biophysica in California, in
collaboration with the research laboratories of a Czech biotech pharma
company, Interpharma Praha, developed a new class of substances which
proved to render the androgen receptor inactive in a novel way. A
large number of new molecules were synthesized and tested. Some were
not resorbed when given orally or topically. The most promising
molecule was structurally modified so that minor amounts of water
would cause the molecule's decomposition, thus rendering it
pharmacologically inactive and incapable to act inside the body. To
prove that this substance, now called Fluridil, once resorbed into the
skin would not enter into the body, a number of experimental studies
were conducted using rats and rabbits, who are capable of taking up
substances through their skin 6 to 10 times more than humans. We
applied large quantities of Fluridil, far surpassing the highest
conceivable dose in humans. Using sophisticated equipment of high
sensitivity no trace of Fluridil or its fragments were ever found in
the blood.
Many studies were conducted to ascertain the systemic and topical
toxicity in animals and finally in human volunteers at the specialized
Experimental Dermatology Institute of the University of California in
San Francisco, under the leadership of Professor Howard Maibach. The
result of this study was remarkable in that no irritation whatsoever
was observed, thus confirming the data we previously gleened from
experimental animals.
By then, news had spread and several of our colleagues of ours on
their own started applying the compound to their scalp, soon to report
the unusual efficacy of the alcoholic solution of Fluridil. We have
thereafter optimized the composition of the solution, conducted all
required safety tests and after having presented our findings to the
authorities, gained marketing approval in the Czech Republic.
In a study with human volunteers, not even trace levels of Fluridil
were detected in the serum; therefore, it cannot be expected to have
systemic effects. This was also confirmed by the clinical study
conducted presently at the Medical School dermatology department
(Chairman: J. Bucek, M.D., Palacky University, Olomouc, Czech
Republic): in most subjects, increase in anagens (growing hair) and
decrease in telogens (dying hair) after 3 months of daily application
of 2 ml Fluridil was substantial; there were no changes in the
hematological and hormonal profiles and there were no adverse effects.
From what has been said above, it is obvious that the mechanism of
Fluridil as a dermo-cosmetic device is sufficiently clear to judge
Fluridil's prospective usefulness. Surely, when hair has been missing
from the scalp for a long time and the hair follicles were obliterated
by the ingrowth of connective tissue, there is very little chance for
growing new hair. Here only transplants can reasonably work. Fluridil
is therefore useful only when the hair follicles are still active and
their androgen receptors are still intact.
So far, the most successful findings were reported by volunteers who
started using Fluridil at the time when the first loss of hair was
encountered. With men, this can start any time after 30 years of age;
with women very often the hair effluvium sometimes dramatically and
suddenly appears concurrently with menopause. In these clients we find
that the hair loss ceases after a few weeks of once-a-day application.
Perhaps, unfortunately, but understandably based on what had been said
above, in order to keep the androgen receptor in check it is necessary
to continue applying Fluridil daily. In a number of volunteers we
found that after some 3 to 4 months of use, new hair growth, "peach
fuzz" - the appearance of baby hair - was induced in the scalp, unless
it had been hairless for many years. With time and patience which the
hair growth cycle requires - and which may be as long as one year - we
often observe a gradual transformation of the "baby hair" into hair of
normal appearance.
il sito è: http://www.interpharma-praha.com/html/spec..._wissentext.htm
voi ne sapete qualcosa? magari qualcuno è andato a Praga e l'ha comprato?!?
