Pregnenolone, Progesterone And Androsterone Are Aromatase Inhibitors

[Coldhandsandfeet]

PREGNENOLONE DOES NOT LOWER ESTROGEN LEVELS. IT RAISED THEM FOR ME. MADE ME VERY ANGRY AND IRRITABLE. MADE MY LIBIDO PLUMMET. MY LIBIDO AND MOOD WERE EXCELLENT BEFORE PREGNENOLONE.

 

[Such_Saturation]

Why'd you take it then

 

[answersfound]

post 101503 Why'd you take it then

Lol good point.

 

[haidut]

post 101498 PREGNENOLONE DOES NOT LOWER ESTROGEN LEVELS. IT RAISED THEM FOR ME. MADE ME VERY ANGRY AND IRRITABLE. MADE MY LIBIDO PLUMMET. MY LIBIDO AND MOOD WERE EXCELLENT BEFORE PREGNENOLONE.

Do you have blood tests or other reliable method that showed pregnenolone increased estrogen?
Lower libido is usually from the increased progesterone that pregnenolone causes. The irritability is from allopregnanolone and pregnanolone. These are both well-documented side effects in people.
So, how do you know pregnenolone raised your estrogen?

 

[Fetch]

post 101643 Do you have blood tests or other reliable method that showed pregnenolone increased estrogen?
Lower libido is usually from the increased progesterone that pregnenolone causes. The irritability is from allopregnanolone and pregnanolone. These are both well-documented side effects in people.
So, how do you know pregnenolone raised your estrogen?

This is interesting to me, the first time I tried pregnenolone this is the reaction I got along with asthma like symptoms. That was about a year ago so I stayed away from it for about 9 months and over that time I took Cypro for 4 months and refined my diet a bit. Then I tried Pansterone while still on Cypro this has been a success even though I think I started on to high of a dose at first. Just took a few days off and started really low and increased slowly being maybe even to cautious. Recently I have slowly stopped take Cypro (as my allergy season is over) and have been adding a little stressNon about 5mg extra to my pansterone dose. With no problems.

I am wondering are there any theories of why allopregnanolone and pregnanolne may cause this reaction in some people? Or ways to counter it?

I have noticed some sleepiness when I believe I have raised my progesterone from things like high amounts of caffeine taken for a few months. A strong cup of coffee in the morning would make it hard to keep my eyes open when driving to work plus at the time I was on 4mg cypro 3 times a day. I actually avoid coffee now in some situations because it makes me too relaxed. I have also noticed some of the same effects from preg+dhea or just preg these aren't necessarily a bad thing but I am wondering if there is a way to counter them. Maybe Thyroid?

I have also experienced a slightly lower libido overall. Not so low as to be a huge concern but I wouldn't mind if it was a little higher. Would the best way to counter progesterones libido lowering effects be increasing dopamine? I think in the past I may have been a little hyper sexual possibly from high estrogen so maybe I should just get use to a more even libido. It's still overall positive but some of my "kinks" aren't as interesting to me anymore. I am still attracted to a wide variety of people and enjoy sex. I just don't want it 2 or 3 times a day maybe that's not a bad thing.

The irritability and aggression link to allopregnenolone and pregnenolone is interesting to me also. Does it hint to anything else maybe high adrenaline?

 

[haidut]

post 101842

post 101643 Do you have blood tests or other reliable method that showed pregnenolone increased estrogen?
Lower libido is usually from the increased progesterone that pregnenolone causes. The irritability is from allopregnanolone and pregnanolone. These are both well-documented side effects in people.
So, how do you know pregnenolone raised your estrogen?

This is interesting to me, the first time I tried pregnenolone this is the reaction I got along with asthma like symptoms. That was about a year ago so I stayed away from it for about 9 months and over that time I took Cypro for 4 months and refined my diet a bit. Then I tried Pansterone while still on Cypro this has been a success even though I think I started on to high of a dose at first. Just took a few days off and started really low and increased slowly being maybe even to cautious. Recently I have slowly stopped take Cypro (as my allergy season is over) and have been adding a little stressNon about 5mg extra to my pansterone dose. With no problems.

I am wondering are there any theories of why allopregnanolone and pregnanolne may cause this reaction in some people? Or ways to counter it?

I have noticed some sleepiness when I believe I have raised my progesterone from things like high amounts of caffeine taken for a few months. A strong cup of coffee in the morning would make it hard to keep my eyes open when driving to work plus at the time I was on 4mg cypro 3 times a day. I actually avoid coffee now in some situations because it makes me too relaxed. I have also noticed some of the same effects from preg+dhea or just preg these aren't necessarily a bad thing but I am wondering if there is a way to counter them. Maybe Thyroid?

I have also experienced a slightly lower libido overall. Not so low as to be a huge concern but I wouldn't mind if it was a little higher. Would the best way to counter progesterones libido lowering effects be increasing dopamine? I think in the past I may have been a little hyper sexual possibly from high estrogen so maybe I should just get use to a more even libido. It's still overall positive but some of my "kinks" aren't as interesting to me anymore. I am still attracted to a wide variety of people and enjoy sex. I just don't want it 2 or 3 times a day maybe that's not a bad thing.

The irritability and aggression link to allopregnenolone and pregnenolone is interesting to me also. Does it hint to anything else maybe high adrenaline?

https://en.wikipedia.org/wiki/Allopregnanolone
"...Increased levels of allopregnanolone can produce paradoxical effects, including negative mood, anxiety, irritability, and aggression.[24][25][26] This appears to be because allopregnanolone possesses biphasic, U-shaped actions at the GABAA receptor – moderate level increases (in the range of 1.5–2 nM/L total allopregnanolone, which are approximately equivalent to luteal phase levels) inhibit the activity of the receptor, while lower and higher concentration increases stimulate it.[24][25] This seems to be a common effect of many GABAA receptor positive allosteric modulators.[26][21] In accordance, acute administration of low doses of micronized progesterone (which reliably elevates allopregnanolone levels), have been found to have negative effects on mood, while higher doses have a neutral effect.[27]"

DHEA is one way to inhibit this effect and hence the (one of many) reason DHEA is in Pansterone.

 

[Fetch]

Thanks for using wikipedia for me! haidut is not raygoogle, Haidut is not raygoogle. haidut is no etc...
I'll probably screw up again!

So would that mean if I had raised the dose it may have helped?

Also any ideas on decreasing the sleepy effects of progesterone? maybe even more caffeine?

 

[haidut]

post 101864 Thanks for using wikipedia for me! haidut is not raygoogle, Haidut is not raygoogle. haidut is no etc...
I'll probably screw up again!

So would that mean if I had raised the dose it may have helped?

Also any ideas on decreasing the sleepy effects of progesterone? maybe even more caffeine?

Yes, a higher dose should reduce the anxiety/irritability. Progesterone is a GABA "agonist" so this is how it makes you sleepy. So taking things that antagonize GABA should negate some of these effects. Caffeine should do it, but in low doses only since in high doses it raises progesterone a LOT and even though it is still antagonistic to GABA the progesterone effect outweighs its wakefulness effects.

 

[Philomath]

post 42796 I took a large dose after work today and I must say I'm pleased. I've been taking it since discovering Peat but it had been awhile since I had used a large dose. I feel very calm and warm. I'm considering going back up on my daily dosage for awhile as it seems I still need more than I had previously been taking. I took 500mg today and I think I'll go to 100 daily for a bit. Thanks goes to haidut and j. for bringing this topic to the discussion today.

Are you still using the Pregnenolone in larger doses and weekly? How is it working for you?

 

[Blossom]

post 102016

post 42796 I took a large dose after work today and I must say I'm pleased. I've been taking it since discovering Peat but it had been awhile since I had used a large dose. I feel very calm and warm. I'm considering going back up on my daily dosage for awhile as it seems I still need more than I had previously been taking. I took 500mg today and I think I'll go to 100 daily for a bit. Thanks goes to haidut and j. for bringing this topic to the discussion today.

Are you still using the Pregnenolone in larger doses and weekly? How is it working for you?

I've been taking about 100 mg several days per week. It does still help me. If I skip it for too long I tend to get cold easier and I feel it's beneficial for my mood and mental functioning. Glad to 'see' you around Philomath!

 

[Philomath]

post 42718 I have seen some people in the forum claim that they thought pregnenolone increased their estrogen levels. According to this study, pregnenolone should in fact lower estrogen by inhibiting aromatase. Peat has already written extensively on progesterone being a known aromatase inhibitor, so that is no news:

http://www.ncbi.nlm.nih.gov/pubmed/3084693

"...Other steroids such as pregnenolone and progesterone were inhibitory, but testosterone and diethylstilboestrol were stimulatory."

I have a friend who had her thyroid removed (irradiated) and she's been on Synthroid for a while. She has recently been hit with what I believe are symptoms of high estrogen. I'd like to suggest something to help her. Is Pregnenolone the easier supplement to recommend since one can't really overdose? It seems that the doctors don't like women tinkering with estrogen/progesterone levels on their own so progesterone may have to wait .

 

[haidut]

post 102020

post 42718 I have seen some people in the forum claim that they thought pregnenolone increased their estrogen levels. According to this study, pregnenolone should in fact lower estrogen by inhibiting aromatase. Peat has already written extensively on progesterone being a known aromatase inhibitor, so that is no news:

http://www.ncbi.nlm.nih.gov/pubmed/3084693

"...Other steroids such as pregnenolone and progesterone were inhibitory, but testosterone and diethylstilboestrol were stimulatory."

I have a friend who had her thyroid removed (irradiated) and she's been on Synthroid for a while. She has recently been hit with what I believe are symptoms of high estrogen. I'd like to suggest something to help her. Is Pregnenolone the easier supplement to recommend since one can't really overdose? It seems that the doctors don't like women tinkering with estrogen/progesterone levels on their own so progesterone may have to wait .

Higher dose vitamin E acts both like estrogen antagonist and aromatase inhibitor. You could suggest pregnenolone but the doctor will probably frown upon that too. Nettle root is also aromatase inhibitor and Peat talked about it several times. Zinc, all the fat soluble vitamins are all anti-estrogenic as well.

 

[docall18]

Just want to note. I wrote earlier about pregnenolone raising estrogen etc and making me feel like rubbish.

Well, I have trialed preg again. As usual it raised my temps, energy etc for the first few days. Then I fell back into the bloated, cold, high estrogen effects i get from preg. However, i realized if preg doesnt directly raise estrogen something else was doing it.

What was happening was preg was raising my metabolism. This was causing a release of PUFA's as my detox systems etc ramped up. The increased PUFA's then caused high estrogen, serotonin, low metabolism etc.

After supplementing with a high dose of vitamin E, aspirin, coconut oil etc., my temperatures started to come back up and my distended stomach started to shrink back down.


So, the lesson from that is, increasing your metabolism can cause an increase in circulating PUFA's making you worse off than when you started..

 

[haidut]

post 105924 Just want to note. I wrote earlier about pregnenolone raising estrogen etc and making me feel like rubbish.

Well, I have trialed preg again. As usual it raised my temps, energy etc for the first few days. Then I fell back into the bloated, cold, high estrogen effects i get from preg. However, i realized if preg doesnt directly raise estrogen something else was doing it.

What was happening was preg was raising my metabolism. This was causing a release of PUFA's as my detox systems etc ramped up. The increased PUFA's then caused high estrogen, serotonin, low metabolism etc.

After supplementing with a high dose of vitamin E, aspirin, coconut oil etc., my temperatures started to come back up and my distended stomach started to shrink back down.


So, the lesson from that is, increasing your metabolism can cause an increase in circulating PUFA's making you worse off than when you started..

Amen. I think this should be a sticky, as this also happens in high dose caffeine users and many people blame caffeine for their symptoms while caffeine is simply raising metabolism just like pregnenolone and progesterone.

 

[tomisonbottom]

Just want to note. I wrote earlier about pregnenolone raising estrogen etc and making me feel like rubbish.

Well, I have trialed preg again. As usual it raised my temps, energy etc for the first few days. Then I fell back into the bloated, cold, high estrogen effects i get from preg. However, i realized if preg doesnt directly raise estrogen something else was doing it.

What was happening was preg was raising my metabolism. This was causing a release of PUFA's as my detox systems etc ramped up. The increased PUFA's then caused high estrogen, serotonin, low metabolism etc.

After supplementing with a high dose of vitamin E, aspirin, coconut oil etc., my temperatures started to come back up and my distended stomach started to shrink back down.
So, the lesson from that is, increasing your metabolism can cause an increase in circulating PUFA's making you worse off than when you started..

Amen. I think this should be a sticky, as this also happens in high dose caffeine users and many people blame caffeine for their symptoms while caffeine is simply raising metabolism just like pregnenolone and progesterone.

This is interesting......but I'm a little confused. Because wouldn't the E, aspirin, coconut oil, etc raise metabolism too? And If things that raise your metabolism release free fatty acids and cause symptoms, then how do more things which raise metabolism stop the FFA symptoms? Is this a U-curve type of effect where you just need to increase the amount of metabolic increasing agents until symptoms are gone?

 

[haidut]

This is interesting......but I'm a little confused. Because wouldn't the E, aspirin, coconut oil, etc raise metabolism too? And If things that raise your metabolism release free fatty acids and cause symptoms, then how do more things which raise metabolism stop the FFA symptoms? Is this a U-curve type of effect where you just need to increase the amount of metabolic increasing agents until symptoms are gone?

High dose aspirin can also trigger stress symptoms. Vitamin E is unique among these as it inhibits lipolysis (through its opposition to estrogen), and can inactivate the PUFA already in the bloodstream. So, vitamin E improve metabolism by lowering fat oxidation. I don't think it has direct effects on mitochondria like aspirin and caffeine do. Coconut oil improves metabolism acutely by increasing the SFA/PUFA ration in blood and displacing the PUFA from the cell mitochondria in the beta oxidation process. Since it can go directly inside the mitochondria and it needs no special transport, the cell prefers to burn it and leave PUFA for last or actually store it. Some fats in cocobut oil have uncoupling effect but not much to match aspirin and caffeine. So, there are different ways to improve metabolism but caffeine and aspirin are thyroid mimetics and just like a large dose of thyroid will trigger s stress response when energy stores run out.

 

[haidut]

I just updated the original post with some screenshots and additional information. It looks like androsterone was also studied and it was also found (unsurprisingly) to be an aromatase inhibitor. Also, pregnenolone and progesterone were found to be incapable of serving as source materials for aromatase and thus estrogen synthesis.

 

[Jsaute21]

Btw, based on the study significant inhibition of aromatase was seen with 0.5microMols concentration of pregnenolone. The pharmacokinetics of pregnenolone in humans are not known but it is assumed to be much better absorbed and retained than oral progesterone. Oral dose of 100mg micronized progesterone achieves 50nM concentration, so to get to 500nM (0.5uM) one would need probably close to 1,000mg of progesterone. Since pregnenolone is much better absorbed than progesterone, then one would probably need anywhere from 500mg to 1,000mg oral pregnenolone to achieve concentrations sufficient to inhibit aromatase.
Btw, if you take such large doses of pregnenolone a good chunk of it will convert into progesterone, so you'll end up inhibiting aromatase through the progesterone conversion anyways. So, probably no need for such large doses of pregnenolone but it does give some hints as to why Ray was taking pregnenolone in doses of more than one gram daily. Maybe he was aware of the aromatase aspect or maybe he just really wanted to raise his progesterone levels.

I mistakenly just took about a gram of pregnenolone. I was in a rush and just put it on to my teaspoon like it was niacinamide. I know, I know. Smooth. How fast would aromatase recover from this "OD" of sorts of Preg.

 

[haidut]

I mistakenly just took about a gram of pregnenolone. I was in a rush and just put it on to my teaspoon like it was niacinamide. I know, I know. Smooth. How fast would aromatase recover from this "OD" of sorts of Preg.

It depends on how much gets converted to progesterone, etc. But since neither pregnenolone nor progesterone are "suicidal" aromatase inhibitors, I'd say it will probably recover in about a day.

 

[Frankdee20]

I take magnesium chloride flakes in baths or footbaths sometimes. I put quite a lot in there. I find it relaxing so unless its placebo, it's absorbed. I doubt that it's a root cause of hypothyroidism (why are you so crap at retaining magnesium in the first place?! although when I read gbolduev posts I get the impression mineral imbalances can be caused even by diets that seem overall nutritious) but I can believe it helps a lot. There are other speculations out there about why some people strangely need lots of magnesium, one is related to carb metabolism.

It's amazing I can tolerate a lot of Magnesium (except Glycinate).