Idomethacin as a Hair Loss Treatment?

[JulioGP]

someone already tested this substance?over 60 pages on the subject, there is a fantastic results

http://foro.recuperarelpelo.com/viewtopic.php?t=44029

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Results 8 months later

http://foro.recuperarelpelo.com/viewtopic.php?t=44029&start=960

 

[squeegee]

someone already tested this substance?over 60 pages on the subject, there is a fantastic results

http://foro.recuperarelpelo.com/viewtopic.php?t=44029

- - - Updated - - -

Results 8 months later

http://foro.recuperarelpelo.com/viewtopic.php?t=44029&start=960

Sick recovery indeed!!! Thanks for the posting JulioGP!!

Indometacin (INN) or indomethacin (USAN and former BAN) is a non-steroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling. It works by inhibiting the production of prostaglandins, molecules known to cause these symptoms. It is marketed under more than seventy different trade names.[1

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Indomethacin, a NSAIA, with analgesic and antipyretic properties exerts its pharmacological effects by inhibiting the synthesis of prostaglandins involved in pain, fever, and inflammation. Indomethacin inhibits the catalytic activity of the COX enzymes, the enzymes responsible for catalyzing the rate-limiting step in prostaglandin synthesis via the arachidonic acid pathway. Indomethacin is known to inhibit two well-characterized isoforms of COX, COX-1 and COX-2, with greater selectivity for COX-1. COX-1 is a constitutively expressed enzyme that is involved in gastric mucosal protection, platelet and kidney function. It catalyzes the conversion of arachidonic acid to prostaglandin (PG) G2 and PGG2 to PGH2. COX-1 is involved in the synthesis pathways of PGE2, PGD2, PDF2a, PGI2 (also known as prostacyclin) and thromboxane A2 (TXA2). COX-2 is constitutively expressed and highly inducible by inflammatory stimuli. It is found in the central nervous system, kidneys, uterus and other organs. It also catalyzes the conversion of arachidonic acid to PGG2 and PGG2 to PGH2. In the COX-2-mediated pathway, PGH2 is subsequently converted to PGE2 and PGI2 (also known as prostacyclin). PGE2 is involved in mediating inflammation, pain and fever. Decreasing levels of PGE2 leads to decreased inflammation.

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Indomethacin is a prostaglandin G/H synthase (also known as cyclooxygenase or COX) inhibitor that acts on both prostaglandin G/H synthase 1 and 2 (COX-1 and -2). Prostaglandin G/H synthase catalyzes the conversion of arachidonic acid to a number of prostaglandins involved in fever, pain, swelling, inflammation, and platelet aggregation. Indomethacin antagonizes COX by binding to the upper portion of the active site, preventing its substrate, arachidonic acid, from entering the active site. Indomethacin, unlike other NSAIDs, also inhibits phospholipase A2, the enzyme responsible for releasing arachidonic acid from phospholipids. Indomethacin is more selective for COX-1 than COX-2, which accounts for its increased adverse gastric effects relative to other NSAIDs. COX-1 is required for maintaining the protective gastric mucosal layer. The analgesic, antipyretic and anti-inflammatory effects of indomethacin occur as a result of decreased prostaglandin synthesis. Its antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

 

[elephant_knight]

Squeege, what do you think about this, (is a disscussion from hair site about indomethacin):


It seems that many people are unfamiliar with the word "agonist".
Indomethacin is a CRTH42 agonist, not an antagonist.
An AGONIST is the exact opposite of an antagonist.
An antagonist inhibits the action of the receptor. An agonist actually
promotes or activates the receptor.
This is exactly what you DON'T want.

I have been following this site for a while and also buy bodybuilding related products from ID.

I know a little bit about how they work based on interactions in the past and can say they do not

put out products that are not well thought out.My biochem background also helps.

It appears indomethacin is included in the formulation for its effects on PGD synthase, which is significant.

Local expression of PGD2 will be reduced by reducing PGD synthase and mast cell release of PGD2.

Whether this will only halt balding or whether it will induce regrowth is impossible to say.

As for the agonist effect of indomethacin, this is why I joined the site - because sometimes

it gets old hearing things get repeated by those who do not fully understand them.

Dude, you may know enough to explain what an agonist is, but it is clear you either

don't have the knowledge or the willingness to dig deeper.

Click this study and follow along: http://www.jimmunol.org/content/168/3/981.long

Now, IC50 and EC50 are terms used primarily in in vitro studies. IC50 is the concentration required

to inhibit 50% of the effect at the receptor level of 50% of a given effect observed. EC50 stands

for excitatory concentration, and is the opposite (required for activation of an effect.

From the study - there is some competitive effect, see below:

"indomethacin indeed inhibited [3H]PGD2 binding to K562/CRTH2 cells with the lowest IC50 value (8.1 ± 1.9 μM) among NSAIDs examined"

Now the agonist effect may be of concern, but the question becomes how potent the agonist is.

Some agonists are weak and others are strong... the ratio of activity compared to the usual ligand (in this case PGD2) is significant.

The below indicates a relative potency for chemotaxis (compared to PGD2) of about 1/20-1/50, though this excerpt does not speak to receptor binding directly:

"CRTH2-transfected Jurkat cells (Jurkat/CRTH2) were indeed attracted by indomethacin and PGD2 (approximate EC50, 50 nM and 1 nM, respectively)

but mock-transfected Jurkat cells (Jurkat/neo) were not (Fig. 3⇓A). DP-transfected Jurkat cells (Jurkat/DP) were suppressed in their spontaneous migration by PGD2,

as shown previously (8), but not by indomethacin (Fig. 3⇓A). Indomethacin and PGD2 also induced chemotactic migration of Th2 but not Th1

cells at submicromolar concentrations (EC50, 50–100 nM and 2–3 nM, respectively; Fig. 3⇓B)."

The below is a better indicator of the relative potency of indomethacin as opposed to PGD2...

"Indomethacin induced Ca2+ mobilization in K562/CRTH2 cells at submicromolar concentrations (approximate EC50, 50 nM) with around one order of magnitude lower potency than that of PGD2;"

This means one of two things. If receptor binding is equal or indomethacin is graeter, the fact that indomethacin is about 1/10 as potent as PGD2 (a "weak agonist" could be almost as good as an inhibitory effect.

If it is not equally strong-binding, which is likely the case, then its effects on the receptor are very minimal

to the point of being insignificant IF PGD2 is already active there (and the whole assumption of this thread is that that is the case in bald men).

The fact is that a receptor-binding antagonist is necessary in a formulation with or without indomethacin.

Seeing as this is the first PGD2 inhibitor product availalble, it was probably put out to meet demand - I would not be surprised

if subsequently the product improves, or competitors pick up on this.

However, the supposed agonist activity of indomethacin is not likely as significant a factor as the inhibitory effect on PGD synthase.

In allergy models of PGD2 inhibition it is equally effective to many CRTH2 receptor antagonists in efficacy; if it stimulated CRTH2 receptors in a meaningful way it would not likely be that effective.

 

[bornthisway]

Pretty amazing results, interesting.

 

[JulioGP]

Hi guys,

I agree with bornthisway. The results are impressive. I'll put the pictures here to make it easier to compare. Look:

I'm looking for what the trade name of the drug with the substance to be found in the pharmacy here in Brazil, but I believe that the United States is even easier. Has anyone tested this product before?

Really amazing and hard to believe.

 

[squeegee]

Hi guys,

I agree with bornthisway. The results are impressive. I'll put the pictures here to make it easier to compare. Look:

I'm looking for what the trade name of the drug with the substance to be found in the pharmacy here in Brazil, but I believe that the United States is even easier. Has anyone tested this product before?

Really amazing and hard to believe.

Was it in a topical solution??

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This proved again that male pattern baldness is a results of chronic inflammation in the skin.

 

[JulioGP]

I could not find in any topical solution. This user used in cream form, but have not found this ingredient in cream in Brazil, only in capsules.

He said he used 2% indomethacin cream.

Anyway...

 

[mj9]

If this is real, then those are incredible results! What was the guys regimen? Has anyone else tried it?

Hi guys,

I agree with bornthisway. The results are impressive. I'll put the pictures here to make it easier to compare. Look:

I'm looking for what the trade name of the drug with the substance to be found in the pharmacy here in Brazil, but I believe that the United States is even easier. Has anyone tested this product before?

Really amazing and hard to believe.

 

[bornthisway]

.

 

[elephant_knight]

But, to be honest, we can't still be sure if this are the results of indomethacin, as he started using indomethacin at the very same time he started using finasteride. He is using indomethacin two times a day and taking tree miligrams of finasteride per week

(Monday, Wednesday and Friday).

 

[squeegee]

I had pretty much the same results with Miconazole Nitrate 4% but I don't have vertex balding. Indomethacin is a Nonsteroidal anti-inflammatory drugs which inhibits both COX expression in the skin.

 

[bornthisway]

squeegee how long did you use miconazole nitrate 4%, how often/when did you apply it? Are you still using it? I don't remember if there were any success stories with miconazole but I do remember when everyone was trying it. But if you got results similar to this that's pretty amazing.

 

[Sparky4444]

So what does this stuff apply like??? Is it thick and pasty like cortisteroid creme?? Or viscous like water/alcohol??

 

[elephant_knight]

Yes, it is a pasty cream. It is a real pain in the *** to apply it. The dudes at iron dragon are selling a liquid formula, but their price is waaay to high...

 

[casperz]

I tried miconazole nitrate a couple of years ago for a few weeks did not seem to do anything special but had severe insomnia and headaches after applying. It might have been a dosing issue and I might have tried longer if the sides could be avoided. Idomethacin looks good but they all do right after one guy has success. Anyone else trying it here? I'd consider it if I could find a legit source.

Just checked some online pharms and cost is about $10 month to mix your own. I think 24 tablets in 60ml would make a 2% solution but it might need to be a cream. Anyone have an online pharmacy other than Inhouse or United(does not have it in stock) that they like?

 

[squeegee]

squeegee how long did you use miconazole nitrate 4%, how often/when did you apply it? Are you still using it? I don't remember if there were any success stories with miconazole but I do remember when everyone was trying it. But if you got results similar to this that's pretty amazing.

Miconazole Nitrate works by inhibition of COX-1 and 2 in the skin as well as a inhibitor of cytochrome P450 which converts cholesterol into androgen in the skin. This is why MICO 4% works. It also has nitrate in it which is a NO donor just like minoxidil. I had really fast results when I first started taking it. I bought a bulk order of 45 grams tubes.. from egay back then when 4% was easily available. Nowadays it is tough to find , you can still get the 4% but in small application like 15 grams in vaginal applicators for yeast infection.. It is expensive.. When I stopped doing it.. I shed like mofo a month after.. so Mico was making a difference.. I also tried a lot of **** before. finasteride/MIN/dutasteride... Nowawdays I still using 2% but not as successful as 4%.

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So what does this stuff apply like??? Is it thick and pasty like cortisteroid creme?? Or viscous like water/alcohol??

Probably an ointment.. because it is use as anti-inflammatory..

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But, to be honest, we can't still be sure if this are the results of indomethacin, as he started using indomethacin at the very same time he started using finasteride. He is using indomethacin two times a day and taking tree miligrams of finasteride per week

(Monday, Wednesday and Friday).

elephant_knight.. it is probably the results of Indo..finasteride just boosted everything up.. just like using the big 3..

 

[bornthisway]

.

 

[squeegee]

In the past, hair loss forum members that used indomethacin didn't report anything encouraging.

This is why male pattern baldness is a pain in the arse.. But what is male pattern baldness? for me, I see it as a accelerating aging process caused by androgen.. we all know that older you get, the majority of the male population go bald.. even female .. What cause aging? Reactive oxygen species, upregulated NF-KappaB (inflammation). No wonders people with topical anti inflammatories have some success or anti-oxidant like l-carnitine, tocotrienols works to some extend. Glutathione is depleted on the scalp during male pattern baldness which is sign of chronic inflammation.Fibrosis and scarring is another sign of ROS/ chronic inflammation.

 

[bornthisway]

I can't find the old thread on indo. anymore. So I could have been mistaken about it being used before and confused it with something else.

 

[beaner]

You guys should check this thread out and look at page 2. These picture are fake. The first set (those posted here) the guy has a boatload of toppik on in the 'after' picture, and on page 2 of this linked thread the guy obviously is wearing a wig. These results are not possible in such a short period of time if at all. There is no way someone is going to reverse massive miniaturization, fibrosis, and grow a full head of hair on a slick bald crown in this short period of time. I really hope no one here is fooled by this because it seems that common sense is lost faster than hair on these forums. I'm not trying to be a douche, only being realistic. This is not possible.

http://www.hairlosshelp.com/forums/messageview.cfm?catid=10&threadid=104992&enterthread=y

I'm not saying this stuff won't have benefits, but the results being presented here are not real. If you think they are.....well good luck and let us know how this works out for you.