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FLURIDIL


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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?!? tongue.gif

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Hall..hai letto quando sara sul mercato????? mi pare di aver letto ke in europa ha gia ottenuto la licenza di commercializzazione come cosmetico.....ne sai qualcosa??????????

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a.chindano..io ho fatto un piccolo ragionamento...se non si hanno controindicazioni...si risparmia un bel po di soldini per l'approvazione ministeriale...(costa un sacco di soldiiiiiiiiiiii!!!!!!! biggrin.gif ).....ti sembra una motivazione valida?

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