Pregnenolone, Progesterone And Androsterone Are Aromatase Inhibitors

[Ddixon3]

Hi Haidut, you're right! I don't know. Just my attempt at interpretation. Thank you for the suggestion. Ill give it a shot and report back.

 

[haidut]

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.

 

[Bluebell]

Btw, if you take such large doses of pregnenolone a good chunk of it will convert into progesterone

haidut, if that happens, then should women avoid taking pregnenolone in the 1st half of their cycle? Because their progesterone levels are supposed to be lower then, and only rise after ovulation for the 2nd half of the cycle ...

 

[haidut]

Btw, if you take such large doses of pregnenolone a good chunk of it will convert into progesterone

haidut, if that happens, then should pre-menopausal woman avoid taking pregnenolone in the 1st half of their cycle? Because their progesterone levels are supposed to be lower then, and only rise after ovulation for the 2nd half of the cycle ...

I don't know the answer to that, but Ray said that high levels of progesterone before ovulation act like a contraceptive. So, at the very least you may end up affecting ability to conceive.

 

[Bluebell]

but Ray said that high levels of progesterone before ovulation act like a contraceptive. So, at the very least you may end up affecting ability to conceive.

that makes sense. And how about successful efforts to lower estrogen (all the things we do in Peat land like aspirin, vitamin E, pregnenolone etc) ... could that adversely affect fertility, because women need a short burst of estrogen just before ovulation to trigger the egg release?

 

[ilovethesea]

Btw, if you take such large doses of pregnenolone a good chunk of it will convert into progesterone

haidut, if that happens, then should pre-menopausal woman avoid taking pregnenolone in the 1st half of their cycle? Because their progesterone levels are supposed to be lower then, and only rise after ovulation for the 2nd half of the cycle ...

I don't know the answer to that, but Ray said that high levels of progesterone before ovulation act like a contraceptive. So, at the very least you may end up affecting ability to conceive.

Progesterone is higher during the 1st half of the cycle. It's the 2nd half when it tanks.

“For example, the follicular phase is a time of low steroid production by the ovary, until near the end of the phase, just before ovulation, when estrogen rises. The luteal phase is a time of high estrogen and high progesterone synthesis. Many publications describe the follicular phase as a time of high estrogen, and the luteal phase as a time of low estrogen, roughly the opposite of the actual situation. And an even larger number of studies get the results they want by using a short exposure to estrogen to study something which takes a long time to develop.”

I don't understand, wouldn't you want to take extra pregnenolone when progesterone is low, before your period? I've been doing so the past week premenstrually with great results.

 

[MIP1950]

I see this is an old thread but pregnenolone is one of RP's go to prohormones, so I wanted to share my experiences.

I'm now 65, a five year history of erectile dysfunction and poor libido, though it was declining several years before that. Testosterone levels, total and free have been borderline low to mid range normal. Been on and off testosterone shots. Twelve years ago I had a raging libido and excellent erectile function. Also have treatment resistant rapid cycling bipolar illness and my sleep has been in the toilet for years. On Klonopin for eight years. Nasty drug.

Regarding pregnenolone. at low doses(10-30mg)feel hot, edgy and in recent times, have developed edema & weight gain, via conversion to estradiol. The experiences of other forum members finding no sides with high doses is fascinating. HPTA dysfunction is an established fact in bipolar illness. I also have a history of hypothyroidism and an episode of adrenal insufficiency(diagnosed by an endocrinologist almost thirty years ago). I know, or I doubt, there's a cure for bipolar, but if I can reboot my HPTA, perhaps I'll experience improved sleep, lowered stress levels, and a return of sexual function, whose loss, is painful and depressing. I feel like a dead man walking.

 

[MIP1950]

Update/I have 3 bottles of 50mg pregnenolone capsules from Puritan's Pride that I bought last October. Yes, it has silica and magnesium stearate, along with rice flour, unlike Swanson brand which just has rice flour, but I'm on Disability and the only viable option is to buy pharma grade bulk but I'm not ready for that. Anyway...I ate two eggs, sunny side up, cooked in butter, with lots of salt, finished it off with apple sauce to which I added a teaspoon of sugar, then I took 10 capsules/500mg. It was crazy, risky, but the medications I've been prescribed over the years have had nasty, frightening sides and I figured even if things got weird, I've been there before and didn't end up on a psych ward.

I took this dose at 7:45. An hour passed. Nothing strange. And I only slept four hours because I didn't eat before going to bed, so I was already wiped out. Went shopping. No problem driving. Felt calm, not spacey. It's now almost four hours since I ingested the preg. Feel okay. My urine output, which has been low for the past few days, has increased. I'm hoping it's the beginning of the end of my bloat from my recent testosterone pellet implantation, otherwise, my urologist will offer me Lasix. Also, no increase in libido or erectile function. That'll probably happen when I'm trying to sleep! Bipolar is so much fun. Day becomes night, night becomes day and you don't know what planet you're living on.

 

[narouz]

Very interesting, MIP.
Hang in there
and keep us posted. :)

 

[haidut]

Update/I have 3 bottles of 50mg pregnenolone capsules from Puritan's Pride that I bought last October. Yes, it has silica and magnesium stearate, along with rice flour, unlike Swanson brand which just has rice flour, but I'm on Disability and the only viable option is to buy pharma grade bulk but I'm not ready for that. Anyway...I ate two eggs, sunny side up, cooked in butter, with lots of salt, finished it off with apple sauce to which I added a teaspoon of sugar, then I took 10 capsules/500mg. It was crazy, risky, but the medications I've been prescribed over the years have had nasty, frightening sides and I figured even if things got weird, I've been there before and didn't end up on a psych ward.

I took this dose at 7:45. An hour passed. Nothing strange. And I only slept four hours because I didn't eat before going to bed, so I was already wiped out. Went shopping. No problem driving. Felt calm, not spacey. It's now almost four hours since I ingested the preg. Feel okay. My urine output, which has been low for the past few days, has increased. I'm hoping it's the beginning of the end of my bloat from my recent testosterone pellet implantation, otherwise, my urologist will offer me Lasix. Also, no increase in libido or erectile function. That'll probably happen when I'm trying to sleep! Bipolar is so much fun. Day becomes night, night becomes day and you don't know what planet you're living on.

If you can break a pregnenolone capsule into 5mg doses and can get DHEA also in 5mg doses then try taking 5mg of each on one dose (preferably with food but empty stomach should work as well). This regimen has been shown to cure andropause and unipolar depression in Russia. You can repeat that same dose 2-3 times a day for stronger effect. If you get edgy you can drop the 5mg pregnenolone from later doses in the day but it is crucial that you take at least some pregnenolone with the DHEA. Pregnenolone both amplifies the effects of DHEA 3-4 times, prolongs its action and prevents it from converting into estrogen if you are uunder stress. I will release a supplement next week that has both pregnenolone and DHEA but if you have the ingredients you can do it yourself.

 

[narouz]

If you can break a pregnenolone capsule into 5mg doses and can get DHEA also in 5mg doses then try taking 5mg of each on one dose (preferably with food but empty stomach should work as well). This regimen has been shown to cure andropause and unipolar depression in Russia. You can repeat that same dose 2-3 times a day for stronger effect. If you get edgy you can drop the 5mg pregnenolone from later doses in the day but it is crucial that you take at least some pregnenolone with the DHEA. Pregnenolone both amplifies the effects of DHEA 3-4 times, prolongs its action and prevents it from converting into estrogen if you are uunder stress. I will release a supplement next week that has both pregnenolone and DHEA but if you have the ingredients you can do it yourself.

This is interesting, haidut.
As was your advice in another thread recently
to take pregnenolone with magnesium.

That latter advice might deserve a thread of its own.
Many here are hypothyroid
and there have been many threads about their difficulties taking/assimilating magnesium properly.
That would include me.

I've been experimenting with the magnesium + pregnenolone
and so far seems to be working.

Do you have any ideas about why/how the pregnenolone helps with magnesium absorption?

 

[haidut]

If you can break a pregnenolone capsule into 5mg doses and can get DHEA also in 5mg doses then try taking 5mg of each on one dose (preferably with food but empty stomach should work as well). This regimen has been shown to cure andropause and unipolar depression in Russia. You can repeat that same dose 2-3 times a day for stronger effect. If you get edgy you can drop the 5mg pregnenolone from later doses in the day but it is crucial that you take at least some pregnenolone with the DHEA. Pregnenolone both amplifies the effects of DHEA 3-4 times, prolongs its action and prevents it from converting into estrogen if you are uunder stress. I will release a supplement next week that has both pregnenolone and DHEA but if you have the ingredients you can do it yourself.

This is interesting, haidut.
As was your advice in another thread recently
to take pregnenolone with magnesium.

That latter advice might deserve a thread of its own.
Many here are hypothyroid
and there have been many threads about their difficulties taking/assimilating magnesium properly.
That would include me.

I've been experimenting with the magnesium + pregnenolone
and so far seems to be working.

Do you have any ideas about why/how the pregnenolone helps with magnesium absorption?

Pregnenolone raises metabolism and ATP production. In the body, magnesium is mostly associated with ATP so lower metabolism means low ATP and less magnesium retention. Thyroid helps with magnesium retention via the same mechanism - i.e. increased ATP. Progesterone does the same. Vitamin B6 also daramatically imrpoves magnesium retention, and in many countries it is sold as a drug in this combination. The effective ratio is 10:1 magnesium : Pyridoxine. If you are using P5P then the ratio can drop to 50:1 or even 100:1. So, taking 5mg P5P and 250mg+ magnesium should strongly improve absorption and have synergistic effects on metabolism.
I don't know the exact dosages for pregnenolone but I think taking 30mg - 50mg with each magnesium dose should be enough.

 

[MIP1950]

@haidut/Thanks for that protocol information. I do have a bottle of 10mg DHEA caps and 10mg pregnenolone caps, in addition to the three 50mg/per dose bottles. Too bad my wife has no interest in any of this. She has T2 diabetes and asthma, along with mood problems. She's also been a vegetarian since '86, which is long before we met. I can't even get her to eat shrimp. C'est la vie.

@narouz/Thanks for the encouragement. Updates to follow.

 

[Giraffe]

I bought pregnenolone recently. The tablets contain 50 mg pregnenolone and 21 mg vitamin C (as ascorbyl palmitate). Does this combo make senses?

 

[haidut]

Btw, I just realized that I made a mistake in my post for dose estimation here:
viewtopic.php?f=75&t=3596&start=60#p81564
In it I say that doses of 500mg+ of pregnenolone are needed to achieve concentrations of 0.5 microMol. That is not true, as pregnenolone is very well absorbed and this HUMAN study showed that a single oral dose of 175mg achieved exactly 0.5 microMol in humans ON AVERAGE.
http://www.ncbi.nlm.nih.gov/pubmed/7840775

However, the variability was quite high and in younger subjects (< 40 years old) the 175mg dose achieved 1 microMol concentrations. So, younger people may need only half as much. So, this means 100mg - 150mg pregnenolone is optimal for most people in terms of aromatase inhibition. Interestingly, this is the dose Ray recommends for most people.

 

[narouz]

Do you have any ideas about why/how the pregnenolone helps with magnesium absorption?

Pregnenolone raises metabolism and ATP production. In the body, magnesium is mostly associated with ATP so lower metabolism means low ATP and less magnesium retention. Thyroid helps with magnesium retention via the same mechanism - i.e. increased ATP. Progesterone does the same. Vitamin B6 also daramatically imrpoves magnesium retention, and in many countries it is sold as a drug in this combination. The effective ratio is 10:1 magnesium:pyridoxine. If you are using P5P then the ratio can drop to 50:1 or even 100:1. So, taking 5mg P5P and 250mg+ magnesium should strongly improve absorption and have synergistic effects on metabolism.
I don't know the exact dosages for pregnenolone but I think taking 30mg - 50mg with each magnesium dose should be enough.

So both pregnenolone and P5P help assimilate magnesium,
not just prevent diarrhea.
I guess they prevent diarrhea because they increase assimilation, you think?

Thanks a lot, haidut.
Magnesium has long been an obvious possible factor in my hypothyroidism.
But damned if I've been able to take much of it without diarrhea.
And the topical applications just didn't seem to help either.

So far your pregnenolone and P5P co-factoring seems to be working well!
I've tried it with both the maleate and the glycinate forms,
enough to give me diarrhea in the past.
Like I say...you might consider a thread devoted to this magnesium angle....

 

[narouz]

It might be new product for you, haidut.
The best pure form of magnesium plus pregnenolone plus P5P.
:)

 

[haidut]

It might be new product for you, haidut.
The best pure form of magnesium plus pregnenolone plus P5P.
:)

I am thinking about it. The problem is that magnesium is not very soluble in liquids so it will have to be a capsule supplement.

 

[jyb]

Thanks a lot, haidut.
Magnesium has long been an obvious possible factor in my hypothyroidism.
But damned if I've been able to take much of it without diarrhea.
And the topical applications just didn't seem to help either.[/font]

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.

 

[narouz]

...why are you so crap at retaining magnesium in the first place?!...

Damned if I know, jyb.
I have a lot of theories!

One is that I was overdosing T4&T3,
forcing my metabolism up,
and the high metabolism burned through my reserves of magnesium.
At the same time I had started drinking a lot of Cokes instead of orange juice--
so...drop in my magnesium supply.

Another theory is that the problem is centered in my gut.
I had to take a lot of antibiotics for my appendectomy.
Then I also experimented a little with some Peatish antibiotics.
Without my appendix to re-supply my gut with good bacteria...yeast took over.
And they somehow screw up magnesium assimilation....

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.

This "gbolduev"...is he on this forum?