New odorless Topical Spironolactone
August 25, 2001 - Los
Spiro what? It's been firmly established that
male pattern baldness is initiated by DHT attaching to the receptor sites on the hair follicles. Genetically, only the follicles on the top of the head are encoded
with the receptor sites, which explains why hair along the side of the
head and in the back of the head is not lost with age. The attached DHT on the receptor site is perceived as a foreign body and the immune system begins to destroy the hair follicle, shortening the growth phase and causing the hair shaft to become progressively finer in
texture. In extreme cases, only a vellus hair remains. The good news is that the follicles have the inherent
capacity to mature to their former size.
Encouraged with the success of Propecia (Finasteride) to reduce the amount of DHT in the scalp of patients with male pattern baldness (MPB), doctors and scientific researchers took another look at existing medications that are known to act as anti-androgens.
However, there have to be stringent criteria for an anti-androgen that can be used to combat or even reverse pattern alopecia. The ideal anti-androgen should have the following properties:
(1) It has to have potent anti-androgen
(2) It should selectively prevent or successfully compete with DHT without changing testosterone
(3) It should be effective topically, so it can be conveniently applied with minoxidil solutions and
(4) Even though it's easily absorbed into the skin, it should not have any systemic effects.
That's a tall order. Surprisingly enough, there is such a medication:
Spironolactone. For over thirty years Spironolactone has been used as an antihypertensive and a diuretic. More recently, it has been used to treat hirsutism
(excess body hair) in women. Using Spironolactone to treat hirsutism may sound contradictory, but body hair (e.g. chest, face, axilla, pubis, etc.) is promoted by testosterone and since
Spironolactone is a potent anti-androgen, it's successfully used to eliminate unwanted hair on the
On the top of the head, where the hair is adversely affected by DHT,
Spironolactone has just the opposite effect. Spironolactone exhibits anti-androgenic effects in both males and females. Taken orally, it is such a potent anti-androgen that, although it is an effective
anti-hypertensive drug, it is rarely used to treat men with hypertension because of its feminizing properties, including painful gynecomastia.
However, applied topically, Spironolactone does not have any systemic side effects.
Among its other properties as an anti-androgen, Spironolactone also effectively prevents DHT from attaching to the receptor sites on the hair
follicles. As a result, the follicles no longer atrophy and can mature again to their normal size. And it does so without decreasing the circulating levels of DHT in the body. By comparison,
Finasteride inhibits the formation of DHT, causing troublesome side effects in many patients.
What's that Smell?
its obvious potential, there have been some minor drawbacks with the use of topical
Spironolactone. The Spironolactone has an inherent disagreeable
mercaptan-like odor. Several people complain that after
creating a topical Spiro solution themselves, an egg-like odor
permeates their hair after application, which can be both
embarrassing and inconvenient. This same odor has been seen in
previous versions of Topical Spiro put out by the REGROWTH group and
Fortunately, Dr. Lee
and his team have produced a stable Topical Spironolactone product
in the form of a lotion which does not have an offensive smell. We
had the opportunity to speak with Dr. Lee regarding Spiro and the
release of this new and improved version of Topical Spironolactone
soon to come...
Tell us about Topical Spironolactone.
Lee: Spironolactone is not a new medication at all. It's
been used for decades, well over 30 years. It has been used
for many purposes. It has been used as a diuretic, an
antiandrogen, and it has pretty much always been administered orally
- that is - taken as a tablet. For the most part it has always
only been indicated for use in women because it has very potent
antiandrogen properties which can cause feminization in men.
However, there have been fairly recent studies dating back to the
late 80's, which show that it works quite well topically and can be
used by men in this fashion. Since it gets metabolized in the
skin, it doesn't have the systemic side effects men would see if
taking it orally. The advantage of using Spironolactone over
other antiandrogens is multi-fold: It can prevent the
synthesis of DHT from Testosterone, it actually blocks the androgen
receptor site, so that if there is DHT around, carried by the
bloodstream from the prostate or whatnot, the site is blocked.
So it actually binds to the receptor itself, rather than allowing
DHT to do so, which as we know, is one of the root causes for hair
loss in men?
Lee: Yes. It binds at the receptor site. The third thing
Spironolactone can do, and this may be the most important, is that
it actually converts some of the Testosterone into an
estrogen. So it has a very good effect on stopping the
processes occurring in the scalp which cause hair loss. In
fact, before I made Xandrox, which is a combination of Minoxidil and
Azelaic Acid, I was trying to make a combination of Minoxidil and
Spironolactone. It didn't work. In the same base, the
two eventually reacted with each other and created an awful smell,
so it still has to be applied separately.
For someone using Minoxidil and Spiro, how would they avoid the
Lee: Well they
can be applied, essentially, one right after the other, fairly close
together in time. It takes several hours for Spironolactone to
react with Minoxidil, so by that time, it will already have been
Spiro blocks the receptor site from DHT attaching, but what about
Lee: Spironolactone effectively blocks
the receptor site so that neither DHT nor Testosterone can bind to
HairlossSucks: In your
experience, how do Oral Finasteride (Propecia/Proscar) stack up to
Topical Spiro as far as hair maintenance and regrowth?
Lee: There are several studies which show the effectiveness of
each individually, but there are none which exist that compare the
two for hair loss. For those who have any reservations about
taking something systemically, or currently have side effects with
Propecia, it's a good alternative. But it has its advantages
and disadvantages. Advantages being that it does not have any
side effects, it is effective, and it's quite inexpensive compared
to Propecia. The downside is its less convenient to use... no
more inconvenient than minoxidil, but it does have to be applied
As we all know, there are many dangerous substances out there which
could be applied topically and regrow hair or inhibit its falling
out. The problem arises in that these substances absorb and
can cause serious systemic side effects. It's been said that
if scientists could find an effective topical that did not absorb
and stay in its original form, it would be the Holy Grail of topical
hair loss treatments.
Lee: (Laughs) .. It's
not that Spironolactone doesn't absorb, its just that it gets
metabolized, so it doesn't have any systemic effects.
When do you anticipate releasing this new Topical Spiro Lotion?
Lee: (Laughs) .. well we planned on having it out ....
yesterday. However there were some problems with the jars and
labels, so we're looking at Mid September now.
Will there be a difference in cost from the current liquid solution?
Lee: We haven't established a cost on it yet, so I really
don't know. It should not be expensive though.
What will be the most effective way for this lotion to be
applied. I know some people complain of difficulty applying
other lotion based topicals because it gets all over their hair -
especially those with diffuse thinning rather than receding or a
a lotion, so its not as thick as a cream, but with a lotion you can
put some on your fingertip and localize where you put it, unlike an
alcohol based liquid. It will be easier to apply for those who
have a well defined area of recession or thinning. With
diffuse thinning, of course, you have to cover the whole area, so
its a little bit more difficult. If you're just applying it to
the temples, its great. For diffuse thinning, its probably
better to use something like Propecia because you're dealing with
the entire scalp area that way.
Tell us about the new Topical Spiro product you plan to release
which will have no unpleasant smell.
Lee: The reason why Spiro smells so unpleasant in our current
solution is because it is in an alcohol base, so that it is quite
volatile. Consequently, the smell was sometimes sour. In
the new product, it is not volatile at all. The old product
seemed to increase in smell as time went on (sometimes only a few
days), however this new product has a shelf life of over a year.
Is the product going to be in a liquid solution like your current
Lee: Our Topical Spiro has always been in a liquid solution in the past,
in a 2% form, but the new product is going to be a Lotion.
The goal with Propecia
obviously is a systemic altering of hormonal balances. It
works from within the bloodstream to affect the levels of DHT
throughout the whole body. It takes time for it to actually
begin to affect the hormonal processes going on in the Scalp.
It's not instant in the scalp even though its bloodstream effects
are instant, and even when it has begun to work in the scalp, its
even longer before you notice anything aesthetically as far as
maintenance of hair or regrowth. Why is it that we have such
an effective systemic DHT inhibitor, and the concept of systemic DHT
inhibitors, especially with the upcoming release of Dutasteride is
very clear to us that it works... but its so difficult for
scientists to come up with a topical DHT inhibitor that comes
anywhere near to working as well? It would seem to us that
having to change your hormonal balances throughout your entire body
would be incredibly unnecessary just to achieve the goal of making a
change in the scalp. Why is it so hard for us to make
something work *locally* in a topical formulation? Is it an
issue of not enough absorption? Is it an issue of too much
absorption which results in the active ingredient being
"washed" away by the bloodstream, causing the treatment to
not be present a sufficient number of hours out of the day to
actually make a difference?
Lee: Actually its
both. By the way Finasteride (the active ingredient in
Propecia) does work topically. When Merck was doing their
trials, they had to make a decision as to what they felt would be a
better selling product: A pill, or a topical applied
solution. By far, people would rather take a pill, so this is
the route they took. To answer your question: Why don't
topicals work as well? It's for many reasons. One reason
is that it doesn't stay in the skin long enough. That's the
problem with progesterone. It's absorbed, metabolized, and
carried away so quickly that it's not effective when it's applied
topically. Another problem is absorption. There are very
few things that get absorbed into skin very well at all. Its
quite the protective device.
So the goal for researchers
as far as finding topical DHT inhibitors should be a focus more so
on finding one that, once absorbed, isn't metabolized so quickly?
Lee: Yes. One
that doesn't get carried away by the circulatory system. They
did that with progesterone by putting it into an oil base so that it
had a slow, timed release. I have been doing a lot of work
with a Biochemist in the Bay Area using liposome's, and that works
very well at keeping the active ingredients stationary in the scalp
once absorbed, but the expenses involved make it prohibitive.
So yes, we're still looking for the holy grail.
So why is it that Spiro still
works even though, as you mentioned, it gets metabolized so quickly?
Lee: It absorbs into
the skin and blocks the receptor site. Anything that gets into
the bloodstream, has already been degraded.
Is the new Topical Spiro
Lotion going to be a prescription product?
Lee: It is.
Spironolactone is definitely a prescription product. You can
obtain it through our site, and I can write the prescription for you
when you order.
you are interested in obtaining this new product, please send your
inquiry to info@HairlossSucks.com
and we will notify you once it has been made available.