Methylene Blue (MB) Is A Potent Aromatase Inhibitor

haidut

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I can't find the original reference on PubMed or anywhere else, so if someone can dig that up for me I'd really appreciate it. For now, we'll have to accept the following statement from the book (the book seems rather legit btw).

https://books.google.com/books?id=plBoB ... se&f=false

"...Further evaluations showed miconazole [81] and methylene blue [82] are very potent aromatase inhibitors with IC50 values of 0.04 and 0.55 uM respectively."

While the pharmacokinetics of MB differ wildly from a person to person, an oral dose of about 10mg should achieve concentrations of at least 0.5uM in most people, and in fact probably closer to 1uM. Given that MB also uncouples mitochondria starting at concentrations of 0.5uM, it looks like you can get the weight loss and anti-estrogen benefits with a fairly low oral dose.
I know some people have reported that they cannot tolerate a dose over 1mg. I had the same experience originally, but just like cyproheptadine I found that it is a matter of acclimatization, at least for me. Now I can take 10mg three times a day and with the exception of intense sweating and high body temperatures I don't really notice any other side effects.
 
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jaa

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Good stuff thanks again haidut!

Do you take MB orally or topically?
 
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Do you find it gives you problems with liver or cheeses?
 

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jaa said:
Good stuff thanks again haidut!

Do you take MB orally or topically?

Would be useful to know if it works topically, because I might not experiment eating fish tank MB products I see sold online...
 
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haidut

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Such_Saturation said:
Do you find it gives you problems with liver or cheeses?

Yes, I get headache when I take MB and eat some cheddar cheese. Maybe it's the tyramine in the cheese interacting with MB or fueling its MAO effects.
 
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haidut

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jaa said:
Good stuff thanks again haidut!

Do you take MB orally or topically?

Both actually. Orally for the mitochondrial benefits and topically for removing things like lipofuscin spots.
 
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haidut

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jyb said:
jaa said:
Good stuff thanks again haidut!

Do you take MB orally or topically?

Would be useful to know if it works topically, because I might not experiment eating fish tank MB products I see sold online...

Why wouldn't it work topically? I posted a study in the Oxidal thread showing topical MB is absorbed and reaches the bloodstream. Not sure what the conversion factor between topical and oral would be, but MB certainly is absorbed topically.
 

jaa

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haidut said:
jaa said:
Good stuff thanks again haidut!

Do you take MB orally or topically?

Both actually. Orally for the mitochondrial benefits and topically for removing things like lipofuscin spots.

Good to know, thanks.
 
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haidut said:
Such_Saturation said:
Do you find it gives you problems with liver or cheeses?

Yes, I get headache when I take MB and eat some cheddar cheese. Maybe it's the tyramine in the cheese interacting with MB or fueling its MAO effects.

Ten milligrams should be I think fairly well into MAO-A territory, you need at least ten times that amount for MAO-B. I think perhaps at my doses I should stop being so careful with foods.
 
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haidut

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Such_Saturation said:
haidut said:
Such_Saturation said:
Do you find it gives you problems with liver or cheeses?

Yes, I get headache when I take MB and eat some cheddar cheese. Maybe it's the tyramine in the cheese interacting with MB or fueling its MAO effects.

Ten milligrams should be I think fairly well into MAO-A territory, you need at least ten times that amount for MAO-B. I think perhaps at my doses I should stop being so careful with foods.

I thought Peat said in an interview that MAO-A inhibition does not happen until you reach tens or even hundreds of milligrams in a single dose. I am pretty sure he said something along the lines of "most important therapeutic benefits lie in doses of a few hundred micrograms to a milligram" and then proceeded to say that MAO inhibition does not happen until you reach hundreds of milligrams.
On the other hand, this study says IC50 for MAO-A inhibition is just several hundred nanomols.
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2078225/

Anybody gotten symptoms of serotonin toxicity with MB in milligram doses?
 
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Well the tyramine thing I think is MAO-B only. The main takeaway from the molar tests is that the lag between the inhibition curves is just around one or two orders of magnitude, which I guess would translate well into a dosage spectrum. The serious cases involve serotonin reuptake inhibitors, tricyclic antidepressants, and MAO inhibitors along with intravenous methylene blue, apparently starting around 0.7mg per kilogram although what they use for thyroidectomy is a lot more.

Moderate and severe toxicity may benefit from serotonin
receptor 2a (5-HT2A) blockade with cyproheptadine tablets
or parenteral chlorpromazine most often cited. There
are, however, also other potent 5-HT2A antagonists such
as olanzapine and ketanserin.12,13 Ketanserin does have
the benefit of intravenous availability and a lack of effect
on dopamine receptors which makes it a safer choice if
neuroleptic malignant syndrome cannot be excluded.
 
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haidut

haidut

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Such_Saturation said:
Well the tyramine thing I think is MAO-B only. The main takeaway from the molar tests is that the lag between the inhibition curves is just around one or two orders of magnitude, which I guess would translate well into a dosage spectrum. The serious cases involve serotonin reuptake inhibitors, tricyclic antidepressants, and MAO inhibitors along with intravenous methylene blue, apparently starting around 0.7mg per kilogram although what they use for thyroidectomy is a lot more.

Moderate and severe toxicity may benefit from serotonin
receptor 2a (5-HT2A) blockade with cyproheptadine tablets
or parenteral chlorpromazine most often cited. There
are, however, also other potent 5-HT2A antagonists such
as olanzapine and ketanserin.12,13 Ketanserin does have
the benefit of intravenous availability and a lack of effect
on dopamine receptors which makes it a safer choice if
neuroleptic malignant syndrome cannot be excluded.

Good point.
I was also thinking about using cypro to mitigate the risk, but I thought you said in another thread that it is contraindicated? Something about not using H1 antagonists with MAO-A inhibitors. Am I misremembering?
 
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haidut said:
Good point.
I was also thinking about using cypro to mitigate the risk, but I thought you said in another thread that it is contraindicated? Something about not using H1 antagonists with MAO-A inhibitors. Am I misremembering?

I found that bit on those "ehealth" sites that list drug information. But check out http://onlinelibrary.wiley.com/doi/10.1 ... x/abstract
 
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haidut

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Such_Saturation said:
haidut said:
Good point.
I was also thinking about using cypro to mitigate the risk, but I thought you said in another thread that it is contraindicated? Something about not using H1 antagonists with MAO-A inhibitors. Am I misremembering?

I found that bit on those "ehealth" sites that list drug information. But check out http://onlinelibrary.wiley.com/doi/10.1 ... x/abstract

Yep, that makes sense. In the abstract it says that only antihistamines known to have SSRI effects are contraindicated with MAO inhibitors. As such, diphenhydramine (Benadryl) is one of them since in doses of 150mg+ it has very pronounced SSRI effects. Some people are even using it as over the counter "Prozac" of sorts.
Cyproheptadine was one of the safe drugs, as listed by the study. So, it should be OK to use to balance the MAO effects of MB. I know of at least 2 case studies where cypro was used to reverse serotonin syndrome induced by IV administration of MB and it worked without side effects or causing more damage.
 

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So, would it still be safe to experiment with small amounts (a few drops) of MB while taking 75mg of diphenhydramine daily?
 

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Such_Saturation said:
You should probably ask the doctor :cool:

Yeah right, if I asked a doctor he'd ask me why the hell am I taking MB to begin with.
 
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Dean said:
Such_Saturation said:
You should probably ask the doctor :cool:

Yeah right, if I asked a doctor he'd ask me why the hell am I taking MB to begin with.

Tell him "You're welcome for my taxes and the public science funding that you used and then you put the information that we paid for behind a paywall".
 

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I should have also mentioned that I don't have a doctor or go to doctors. My experiences with them have always been wildly negative. So, if I was ever going to go and put him in his place, I would never be able to do it as gently as you suggest.
 
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Such_Saturation said:
You should probably ask the doctor :cool:

I would not risk taking Bendaryl and MB together. It is listed as one of the contraindicated drugs and even if you take a lower dose you still don't know how it may metabolize. If you accidentally ingest some food containing an inhibitor of cytochrome P450 (grapefruit, pears, some grapes), that 75mg of Benadryl may end up acting like a 300mg dose due to the inhibition of drug metabolism.
Cypro or one of the suggested 5-HT2 antagonists like mianserin, ketanserin, ritanserin, etc would be much safer.
 

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