To Michael Barry

blaze

Experienced Member
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Hey Michael,

I know you used to use Flutamide, I was just wondering at what strength you were using it at?

And also, do you know how long is the half life of Flutamide? When I apply it to my scalp, how long will my follicles have protection for?

thanks for any help you can give. :)
 

michael barry

Senior Member
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Blaze,

I tried flutamide for all of one week once. I got it from lipoxidil.com's order page, http://www.lipoxidil.com/site/order.php . It was the 1.5% concentration.

Like Bryan has said, it gets absorbed systemically. I had no libido whatsoever in about three days, some nausea and diarreaha. I dont know how some guys use this and deal with the side effects which are horrible. Much better it would be just to take finasteride. If finas gives you sides, flutamide damn sure will.

Note on lipoxidil. Its an overpriced site and the amounts they give you are too small. I bought a 2% spironolactone bottle from them that was supposed to be 50mgs, but it was only full to about 30 mgs. I ordered two and got one. Ive ordered from lipoxidil three or four times to try some stuff (alpecin was one) and have noticed if you specify 2 of something, you might only recieve one in the mail. If you order just one, they want you to pay some kind of extra charge for not buying more. I dont like the site to be honest, and most others dont either. They sell nanosomal/liposomal minoxidil formulations, roxythromicyn (I got some of that from them) and topical dutasteride and finasteride formulations (you could drop a few tablets of these in minoxidil and get the same thing delivered topically with the minoxidil's delivery system as long as you only did about 20 days worth at a time to protect from degradation). Lots of people regard lipoxidil as a rip-off site. I'll say this, only hairmedics.com is more expensive. Hairmedics is outrageously priced. Like a 2% bottle of nizoral thats only 100 mgs (half the size of the drug store) for 23 bucks plus shipping........that would equate with about a sixty dollar bottle of shampoo once you add the shipping charges. Thats par for the course with them.
 

blaze

Experienced Member
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thx michael.

I just started using Flutamide at a 2% strength for about 3 weeks now. I make it myself.

I havent noticed any weird sides yet.

Do you happen to know what the hlaf life of Flutamide is Michael? How long will the follicles stay protected from androgens once you apply it?
 

docj077

Senior Member
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blaze said:
thx michael.

I just started using Flutamide at a 2% strength for about 3 weeks now. I make it myself.

I havent noticed any weird sides yet.

Do you happen to know what the hlaf life of Flutamide is Michael? How long will the follicles stay protected from androgens once you apply it?

http://www.pharmgkb.org/do/serve?objId= ... Properties

Flutamide: The half-life of the active metabolite hydroxyflutamide is approximately 6 hours. Values are prolonged in geriatric patients to approximately 8 hours following administration of a single dose and approximately 9.6 hours at steady-state , and are slightly prolonged in patients with chronic renal function impairment (creatinine clearance < 29 mL/min) . In geriatric patients, the half-life of the parent compound, flutamide, is approximately 7.8 hours at steady-state.

There are many things that confuse me in this world and one of them is the topical application of a drug that has to be activated in the liver before it's useful to the body. I sure do hope that the topical that people are using is hydroxyflutamide.

At least, that's what would make sense to me.
 

blaze

Experienced Member
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6
thanks Doctor.

I guess I stuffed up then. Im just using regular flutamide crushed up and dissolved it in an alchol/glycerin base at a 2% strength.

Where would I get hydroxyflutamide from?

Do Lipoxidil use hydroxyflutamide?
 

docj077

Senior Member
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blaze said:
thanks Doctor.

I guess I stuffed up then. Im just using regular flutamide crushed up and dissolved it in an alchol/glycerin base at a 2% strength.

Where would I get hydroxyflutamide from?

Do Lipoxidil use hydroxyflutamide?

You might want to check that website I posted to see if flutamide is absorbed through the skin. I'm pretty sure that it is as a lot of people have side effects from topical administration of it. You should be okay. That just means that the flutamide has to be absorbed, biotransformed in the liver, and then it has to make its way out to your androgen receptors. I don't even know if they make topical hydroxyflutamide or if such a chemical is even lipid soluble.

The same holds true for drugs like finasteride and dutasteride. They have to be converted to active metabolites, as well. So, topical administration of those drugs probably isn't that efficacious either. I'd also be interested to hear how topical spironolactone works, as well. That drug is converted to active metabolites by the liver, too.

I'm probably making a big deal out of this and there is likely something I'm missing, but I'm just curious about this potential problem.
 

Bryan

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Staff member
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docj077 said:
There are many things that confuse me in this world and one of them is the topical application of a drug that has to be activated in the liver before it's useful to the body. I sure do hope that the topical that people are using is hydroxyflutamide.

I wouldn't go so far as to say that topical flutamide HAS to be activated in the liver. It may be that there are enzymes in the skin/scalp that convert flutamide to hydroxyflutamide, since there's one human study that showed no difference in effect between the topical application of flutamide and hydroxyflutamide. But whether that was a "local" activation in the skin or a remote activation in the liver was impossible to determine from the design of the study.

Bryan
 

Bryan

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Staff member
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docj077 said:
You might want to check that website I posted to see if flutamide is absorbed through the skin.

The animal evidence is unequivocal: topical flutamide IS absorbed sustemically to a significant extent in rodents like hamsters, rats, and mice.

docj077 said:
The same holds true for drugs like finasteride and dutasteride. They have to be converted to active metabolites, as well.

Doctor, I've never heard such a claim before. I think finasteride and dutasteride are active in their original forms.

docj077 said:
So, topical administration of those drugs probably isn't that efficacious either. I'd also be interested to hear how topical spironolactone works, as well. That drug is converted to active metabolites by the liver, too.

spironolactone is converted to a LESS active metabolite (canrenone). Furthermore, the topical application of spironolactone shows far greater "local" activity than flutamide in animal tests.

Bryan
 

docj077

Senior Member
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Bryan said:
docj077 said:
You might want to check that website I posted to see if flutamide is absorbed through the skin.

The animal evidence is unequivocal: topical flutamide IS absorbed sustemically to a significant extent in rodents like hamsters, rats, and mice.

docj077 said:
The same holds true for drugs like finasteride and dutasteride. They have to be converted to active metabolites, as well.

Doctor, I've never heard such a claim before. I think finasteride and dutasteride are active in their original forms.

docj077 said:
So, topical administration of those drugs probably isn't that efficacious either. I'd also be interested to hear how topical spironolactone works, as well. That drug is converted to active metabolites by the liver, too.

spironolactone is converted to a LESS active metabolite (canrenone). Furthermore, the topical application of spironolactone shows far greater "local" activity than flutamide in animal tests.

Bryan

As usual, I'm probably making a big deal out of nothing. My bad.

Isn't the less active metabolite (canrenone) the metabolite that has a half-life of 10-35 hours while spironolactone itself only has a half-life of 10 minutes? Is the androgen receptor/spironolactone binding process a covalent one, because I don't know? Otherwise, topical spironolactone will work for a short period of time and then its efficacy should increase as more of the longer lived, but less active canrenone builds in one's system.

I'd also like to know if flutamide is truly biotransformed in the scalp. Such a process requires the cytochrome P450 system and I'm not aware of any of those enzymes being present in the scalp. I'll have to look around some more.
 

docj077

Senior Member
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Bryan said:
docj077 said:
The same holds true for drugs like finasteride and dutasteride. They have to be converted to active metabolites, as well.

Doctor, I've never heard such a claim before. I think finasteride and dutasteride are active in their original forms.

Bryan

Yeah, you're right. Dutasteride and finasteride are extensively metabolized by the liver into many less active metabolites. What I'm actually trying to find is if any biotransformation takes place in either finasteride or dutasteride that activates the drugs. Dutasteride looks to be active as soon as it's absorbed, but I can't find anything on finasteride. I know that both drugs have less than appealing bioavailability and that both are highly protein bound, but there just isn't a lot of information out there about the drugs.
 
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