spironolactone.. a WEAK anti-androgen?

[DrGrow]

Reading on some Acne forums where spironolactone is suggested as a solution.. they continiously seem to refer to it as a "weak" anti-androgen.

Does anyone have any studies to say how strong it is?

 

[docj077]

Reading on some Acne forums where spironolactone is suggested as a solution.. they continiously seem to refer to it as a "weak" anti-androgen.

Does anyone have any studies to say how strong it is?

Internally, the molecule binds with enough affinity to the androgen receptor to prevent androgen binding. Not only that, but the interaction is strong enough that those androgens get shuttled into the pathway that ends with their eventual conversion into estrogens.

That's powerful enough for me.

Topically, I really don't know how efficient a solution containing spironolactone truly is in the long run.

 

[Jm0311]

i hope it is im a couple of days away from it

 

[eric2117]

I wanna make my own spironolactone cream but can't find a decent suggestion on how to? any ideas??

 

[barcafan]

i hope it is im a couple of days away from it

Have fun loosing ground.

 

[Jm0311]

barcafan....what your regime? how long? any sides?

 

[barcafan]

1 month on finasteride no sides.

3 weeks on 5% minoxidil i think i get dizzy but i doubt it i think its jsut in my head

Adding nizoral soon (Deciding between nizoral and revita.)

 

[Jm0311]

is money an option? if not i would get Revita if you use the pre wash method its worth it

 

[Bryan]

Reading on some Acne forums where spironolactone is suggested as a solution.. they continiously seem to refer to it as a "weak" anti-androgen.

Does anyone have any studies to say how strong it is?

It depends on exactly how you define "weak antiandrogen". There's an in vitro study with human cells showing that spironolactone has about 2/3 of the relative binding affinity for androgen receptors as DHT itself! That would appear to make it a very strong antiandrogen indeed.

However, a separate issue that's also very important is how easy is it for the spironolactone molecules to actually make their way into cells and do their job on the androgen receptors there, especially after topical application. I always like to point out that in tests in which drugs are applied topically to hamster flank organs, spironolactone seems to have about half the antiandrogenic effect that RU58841 has, so apparently some practical issue or issues (like how effectively it's absorbed into the skin, or how rapidly it's metabolized into less active substances, or whatever) seem to keep spironolactone from attaining its full theoretical effectiveness.

Bryan

 

[DrGrow]

Well whats the best way to dilute spironolactone?

I have 100x 100mg pills. I would assume each 10 pills to 100mL of liquid is 1% concentration.

If I want to mix these pills into a cream.. how can I get a 3 to 5% mix of spironolactone in a 250mg Cream tub? I have PG on hand.

 

[Beethoven]

It depends on exactly how you define "weak antiandrogen". There's an in vitro study with human cells showing that spironolactone has about 2/3 of the relative binding affinity for androgen receptors as DHT itself! That would appear to make it a very strong antiandrogen indeed.

Hi Bryan,

There's an article called "Other Antiandrogens" by J.B.Schmidt, from Dermatology 1998;196:153-157.
In the second page (page number 154), Schmidt write "the affinity of SP for DHT receptors is 10-20 less than that of DHT [9,10]."
In his reference list, reference 9 is:Corvol P, Michaud A, Menard J, Freifeld M,Mahardeau J :Antiandrogenic effects of spironolactones:Mechanism of action. Endocrinology 1975;97:7-52.
Reference 10 isita JC, Lippman ME, Thompson EB, Loriaux DL : Interaction of spironolactone and digitalis with 5-alpha-dihydrotestosterone(DHT) recptor of rat ventral prostate. Endocrinology 1975;97: 1521-1527.

I wonder which research is right? I guess we'll have to take a closer look at these references. Your study is with human cells and ref 10 is only with rats, I have no idea what were the methods of ref 9.

 

[Bryan]

Yeah, don't you just love it when we have "dueling studies" like that?

I would tend to go with the study I referenced, since they definitly used human cells; furthermore, they tested a wide range of substances under the same conditions, not just spironolactone, so I imagine (or hope) that they knew what they were doing.