31 replies to this topic

[drg]

There is pretty decent research for the use of tamoxifen (estrogen antagonist) in the use of bipolar disorder. It is apparently has quick onset as an antimanic and works in 5 days.

 

http://www.jad-journ...0549-5/abstract

 

http://www.researchg...d=0CB0QgAMoADAA

 

It is even recommended as an offlabel med in the CANMAT treatment guidelines for bipolar disorder.

 

I was wondering if anyone has used it for that purpose? If no one has I probably will try in the future.

[FocusPocus]

please keep us posted in this thread if you do.

[drg]

Tamoxifen is used as an anti estrogen to battle breast cancer and in bodybuilding to prevent gynecomastia.

 

I have known people to be on it for years for breast cancer. And the side effect profile seems better than other options we have available, it can cause fatigue though. 

 

For bipolar here are your options::

 

Anti-psychotics / Dopamine antagonists : sounds like voodoo to expect to feel good while inhibiting dopamine, unless the goal is not feeling?

 

Quetiapine : highly sedating, very common offlabel sleep med

Aripiprazole, Risperidone, olanzapine ?? these will make you fat on the inside and out

 

Anticonvulsants : heavy cognitive side effects

divalproex : this med is so old, be prepared not to think straight

carbamazepine: worst side effect profile of all the listed meds

lamotrigine : many people can't stay on it because of a deadly rash, but cognitively not as bad as the others

 

Lithium : the gold standard mood stabilizer

severe cognitive side effects, kidney toxic at high doses, dehydration

 

NAC N-acetyl cysteine :  its a supplement, so it is not as potent as the above meds but side effect wise its good to go, perhaps you can augment it with other meds and reduce their dosage, it is fairly well researched

 

 

Anyways, now with tamoxifen I am wondering how much of that other bullshit you can cut out of your pill wheels. Maybe augment and lower their doses?

Edited by drg, 25 September 2014 - 03:32 AM.

[drg]

I got my doc to prescribe tamoxifen, I am taking 20mg for 2 weeks then 40mg. Just started a week ago. 

The study used doses starting at 20mg x 2 daily ending at 40mg x 2 daily.
 

On it I noticed zero side effects, and felt good. The low side effects is particularly encouraging because I could increase the dose as high as 200mg a day. My greatest hope is being able to reduce my other meds. Anyways I will chart my mood so I can get some real idea how it affects my mood.  

 
---

Also I also heard that inhibiting estrogen up increases testosterone... maybe its bro science though but i'll take it.
 

[drg]

I am at 80mg it is a very good mood stabilizer. Suggested max dose is 200mg /d 

 

Only side effects : mild weight gain, though oddly I feel stronger cardiovascular on it
 

And on the bright side I am well set up to supplement testosterone at ridiculous doses if I ever feel like it.

 

Anywaysthis is my last update cause no one is particularly interested.
 

[FocusPocus]

thanks for the update. 

[Nemo888]

I know a few steroid body builders. Guys who regularly take horse steroids and think they are great.

 

The only drugs they fear are anti-aromatizers like tamoxifen and anastrozole. Watch for side effects, especially increased blood pressure, joint pain and even cardiac arrhythmia. Discontinue immediately if you get these.

 

Get your estradiol checked. Since you are not supplementing T your estrogen can fall so low you it can also be a cardiovascular risk factor.

Edited by Nemo888, 24 October 2014 - 02:59 PM.

[drg]

Why would they fear tamoxifen, they'd get boobs if they don't take something like that

[Nemo888]

Side effects, they can be extreme. Atrial fibrillation is no joke

[drg]

are u tlaking about tamoxifen or steriods :/  ?

 

I see there is a marginal increase in chance of stroke but I don't really see many heart issues associated with tamoxifen.

 

Edited by drg, 24 October 2014 - 03:12 PM.

[Nemo888]

Tamoxifen and anastrozole, yes.

 

If a group of guys thinks taking a veterinary grade horse steroid from Mexico(Equipoise) is cool and they fear anti-aromatizers I would heed the warnings. The drugs are made to stop the growth of cancer in women. The genius of their design means even some of their secondary metabolites interfere with your hormones like IGF for instance. Never tested on men and never will be as they are too risky unless you have an average of five years to live from your breast cancer returning.

 

Just saying take care and watch out for side effects.

 

Low estradiol can also be very bad news, ie highest mortality rate. You may need to start the T if you go under 20 pg/mL.

http://www.medscape....warticle/703027

 

Edited by Nemo888, 24 October 2014 - 03:25 PM.

[fntms]

tamoxifen has been tested on men...

[Nemo888]

My understanding was that the trials were incomplete as the sample size of men with breast cancer is relatively small. That could have changed. I also know that removing the testicles is an accepted medical intervention for stopping breast cancer recurrence in men. Being approved under such circumstances means little. I know of no attempts to get it approved for hormone replacement therapy. If you know where to find some studies I would be interested in reading them.

Of the antiaromatizers I think Aromasin is probably the best for males taking HRT. It does not interfere with IGF like Arimedex and increases it IIRC. Arimedex hikes my systolic by over 30 points and I've seen it give people atrial fibrillation. Also gave me killer head aches.

[fntms]

They have been tested in cases of azospermia with some success it seems... both serms and letrozole, maybe others.

[Nemo888]

That is an interesting off label use.

[nowayout]

Tamoxifen will generally raise testosterone and raise serum estradiol significantly.  It is used for this reason by bodybuilders after they stop injecting steroids to bring back the body's production of these hormones.   Since these hormones are psychoactive, this may be one way tamoxifen may affect some mental illnesses.  

 

Serum estradiol is not lowered on tamoxifen, it is usually raised.  Tamoxifen will block the effect of estradiol on estrogen receptors in certain tissues, though, including some areas of the brain (which the brain tries to compensate by signaling the testicles to make more testosterone and thus indirectly estrogen) and breast tissue.  In some other tissues, tamoxifen itself actually acts as an estrogen. 

[Nemo888]

Tamoxifen will generally raise testosterone and raise serum estradiol significantly.  It is used for this reason by bodybuilders after they stop injecting steroids to bring back the body's production of these hormones.   Since these hormones are psychoactive, this may be one way tamoxifen may affect some mental illnesses.  

 

Serum estradiol is not lowered on tamoxifen, it is usually raised.  Tamoxifen will block the effect of estradiol on estrogen receptors in certain tissues, though, including some areas of the brain (which the brain tries to compensate by signaling the testicles to make more testosterone and thus indirectly estrogen) and breast tissue.  In some other tissues, tamoxifen itself actually acts as an estrogen. 

That is completely wrong. It is not possible for an aromatase inhibitor to raise estrogen. It is a breast cancer therapy for cancers that are estrogen dependent.

 

http://en.wikipedia....atase_inhibitor

 

Every single statement in your post is wrong. Wow.

Edited by Nemo888, 28 October 2014 - 04:32 PM.

[drg]

I also heard that inhibiting estrogen slightly increases testosterone. Body builders do use clomid a selective estrogen receptor modulator to help get their testosterone levels back to normal after ending their steriod cycle. I wouldn't be surpised it that remained true for anti estrogens.

 

http://www.ncbi.nlm..../pubmed/9168075 it does increase free estrodiol1 and 2.

 

Also increases DHEA which in turn increases testosterone and estrogen.

 

---

 

But tamoxifen is used during the steriod cycle more importantly than after it.

 

 

Tamoxifen will generally raise testosterone and raise serum estradiol significantly.  It is used for this reason by bodybuilders after they stop injecting steroids to bring back the body's production of these hormones.   Since these hormones are psychoactive, this may be one way tamoxifen may affect some mental illnesses.  

 

Serum estradiol is not lowered on tamoxifen, it is usually raised.  Tamoxifen will block the effect of estradiol on estrogen receptors in certain tissues, though, including some areas of the brain (which the brain tries to compensate by signaling the testicles to make more testosterone and thus indirectly estrogen) and breast tissue.  In some other tissues, tamoxifen itself actually acts as an estrogen. 

That is completely wrong. It is not possible for an aromatase inhibitor to raise estrogen. It is a breast cancer therapy for cancers that are estrogen dependent.

 

http://en.wikipedia....atase_inhibitor

 

Every single statement in your post is wrong. Wow.

 

 

Edited by drg, 28 October 2014 - 04:54 PM.

[drg]

I guess a further update:

 

There are some effects on cognition, fairly minor but similar to lithium. Some memory blanks, and some mental fatigue (lithium is 100x worse though for these effects). It is definately doing its job for mood stabilization and side effect wise still worth taking.

 

I am at 80mg it is a very good mood stabilizer. Suggested max dose is 200mg /d 

 

Only side effects : mild weight gain, though oddly I feel stronger cardiovascular on it
 

And on the bright side I am well set up to supplement testosterone at ridiculous doses if I ever feel like it.

 

 

Edited by drg, 28 October 2014 - 05:43 PM.

[Nemo888]

I also heard that inhibiting estrogen slightly increases testosterone. Body builders do use clomid a selective estrogen receptor modulator to help get their testosterone levels back to normal after ending their steriod cycle. I wouldn't be surpised it that remained true for anti estrogens.

http://www.ncbi.nlm..../pubmed/9168075 it does increase free estrodiol1 and 2.

Also increases DHEA which in turn increases testosterone and estrogen.

---

But tamoxifen is used during the steriod cycle more importantly than after it.

Tamoxifen will generally raise testosterone and raise serum estradiol significantly. It is used for this reason by bodybuilders after they stop injecting steroids to bring back the body's production of these hormones. Since these hormones are psychoactive, this may be one way tamoxifen may affect some mental illnesses.

Serum estradiol is not lowered on tamoxifen, it is usually raised. Tamoxifen will block the effect of estradiol on estrogen receptors in certain tissues, though, including some areas of the brain (which the brain tries to compensate by signaling the testicles to make more testosterone and thus indirectly estrogen) and breast tissue. In some other tissues, tamoxifen itself actually acts as an estrogen.

That is completely wrong. It is not possible for an aromatase inhibitor to raise estrogen. It is a breast cancer therapy for cancers that are estrogen dependent.

http://en.wikipedia....atase_inhibitor

Every single statement in your post is wrong. Wow.

In men it increases T by blocking aromatization. Aromatization is where men get all their estrogen since they do not have ovaries. I know competitors who take estrogen blockers during cycles and some who take them all the time. Never known one who took them after. Maybe that is why they didn't win. They were doing it wrong.

That study is from women with ovaries. Not men.

[nowayout]

 

Tamoxifen will generally raise testosterone and raise serum estradiol significantly.  It is used for this reason by bodybuilders after they stop injecting steroids to bring back the body's production of these hormones.   Since these hormones are psychoactive, this may be one way tamoxifen may affect some mental illnesses.  

 

Serum estradiol is not lowered on tamoxifen, it is usually raised.  Tamoxifen will block the effect of estradiol on estrogen receptors in certain tissues, though, including some areas of the brain (which the brain tries to compensate by signaling the testicles to make more testosterone and thus indirectly estrogen) and breast tissue.  In some other tissues, tamoxifen itself actually acts as an estrogen. 

That is completely wrong. It is not possible for an aromatase inhibitor to raise estrogen. It is a breast cancer therapy for cancers that are estrogen dependent.

 

http://en.wikipedia....atase_inhibitor

 

Every single statement in your post is wrong. Wow.

 

 

No.

 

Tamoxifen is not an aromatase inhibitor.  Even a cursory Wikipedia search will tell you this.   As for the rest, drg already posted a link explaining that tamoxifen raises E1 and E2.  It also raises testosterone in men, as a cursory search of pubmed will show.  

 

[nowayout]

 

I also heard that inhibiting estrogen slightly increases testosterone. Body builders do use clomid a selective estrogen receptor modulator to help get their testosterone levels back to normal after ending their steriod cycle. I wouldn't be surpised it that remained true for anti estrogens.

http://www.ncbi.nlm..../pubmed/9168075 it does increase free estrodiol1 and 2.

Also increases DHEA which in turn increases testosterone and estrogen.

---

But tamoxifen is used during the steriod cycle more importantly than after it.
 

 

Tamoxifen will generally raise testosterone and raise serum estradiol significantly. It is used for this reason by bodybuilders after they stop injecting steroids to bring back the body's production of these hormones. Since these hormones are psychoactive, this may be one way tamoxifen may affect some mental illnesses.

Serum estradiol is not lowered on tamoxifen, it is usually raised. Tamoxifen will block the effect of estradiol on estrogen receptors in certain tissues, though, including some areas of the brain (which the brain tries to compensate by signaling the testicles to make more testosterone and thus indirectly estrogen) and breast tissue. In some other tissues, tamoxifen itself actually acts as an estrogen.

That is completely wrong. It is not possible for an aromatase inhibitor to raise estrogen. It is a breast cancer therapy for cancers that are estrogen dependent.

http://en.wikipedia....atase_inhibitor

Every single statement in your post is wrong. Wow.

In men it increases T by blocking aromatization. Aromatization is where men get all their estrogen since they do not have ovaries. I know competitors who take estrogen blockers during cycles and some who take them all the time. Never known one who took them after. Maybe that is why they didn't win. They were doing it wrong.

 

No, it does not block aromatization.  It is not an aromatase inhibitor.  It is a SERM that blocks certain estrogen receptors, notably in the brain, which stimulates the HPTA axis to increase production of testosterone (and thus, indirectly, estrogens).

 

Tamoxifen is used by some men while they are on steroid cycles to prevent gynecomastia, since tamoxifen blocks estrogen receptors in breast tissue.  It is also used by many men after steroid cycles to recover the body's own production of testosterone via the above mechanism (inhibition of HPTA negative feedback).  Either tamoxifen or clomifene (another SERM) can be used for this purpose.  Bothe are components of common PCT (post-cycle therapy) protocols.

[nowayout]

That study is from women with ovaries. Not men.

 

 

Here are studies in men.  Estradiol, also called E2, is the estrogen that was tested in these studies.  It increased in response to tamoxifen.  Of course the effect of that increase is also blocked by tamoxifen at the receptor in some tissues (including at breast and areas of the brain), though not in others. 

 

 

Fertil Steril. 1978 Mar;29(3):320-7.

Hormonal effects of an antiestrogen, tamoxifen, in normal and oligospermic men.

Vermeulen A, Comhaire F.

Abstract

The administration of tamoxifen, 20 mg/day for 10 days, to normal males produced a moderate increase in luteinizing hormone (LH), follicle-stimulating hormone (FSH), testosterone, and estradiol levels, comparable to the effect of 150 mg of clomiphene citrate (Clomid). However, whereas Clomid produced a decrease in the LH response to LH-releasing hormone (LHRH), no such effect was seen after the administration of tamoxifen. In fact, prolonged treatment (6 weeks) with tamoxifen significantly increased the LH response to LHRL. Treatment of patients with "idiopathic" oligospermia for 6 to 9 months resulted in a significant increase in gonadotropin, testosterone, and estradiol levels. A significant increase in sperm density was observed only in subjects with oligospermia below 20 X 10(6)/ml and normal basal FSH levels. When basal FSH levels were increased or oligospermia was moderate (greater than 20 X 10(6)/ml); no effect on sperm density was seen. As sperm density increased, FSH levels decreased, suggesting an inhibin effect. Sperm motility was not improved by tamoxifen treatment. In five boys with delayed puberty, tamoxifen treatment appeared to activate the pituitary-gonadal axis and pubertal development.

 

Fertil Steril. 1987 Jul;48(1):113-7.

Tamoxifen citrate therapy in male infertility.

AinMelk Y, Belisle S, Carmel M, Jean-Pierre T.

Abstract

A prospective, randomized, double-blind study with crossover, using tamoxifen (TAM) (Nolvadex, ici Pharma, Missisauga, Canada) 20 mg/day and placebo (p) for 6 months each, was conducted in 16 infertile men with idiopathic oligozoospermia. Baseline sperm count was 17.092 +/- 3.09 (10(6)/ml). Hormonal profile was performed and included follicle-stimulating hormone (FSH), luteinizing hormone (LH), estradiol (E2), testosterone (T), prolactin (PRL), thyroid-stimulating hormone (TSH), and luteinizing hormone-releasing hormone (LH-RH) stimulation tests. The sperm analysis and hormonal profile were repeated at 6 and 12 months of the study. A sperm penetration assay (SPA) was performed on zona-free hamster egg. Compared with the placebo group, the TAM group showed a significant increase in plasma FSH, LH, E2, and T levels (P less than 0.001), but not in PRL and TSH levels. However, LH-RH stimulation tests and SPA were found to be comparable in the two treatment groups, and there was no significant effect on sperm analysis. Tamoxifen appeared to be no more effective than the placebo in the treatment of idiopathic oligozoospermia.

 

Edited by nowayout, 28 October 2014 - 06:34 PM.

[Nemo888]

Ya I totally blew it. I thought tamoxifen was a first generation aromatase inhibitor, not a serm. No one up here seems to use it anymore. I originally thought that was a bad sign, but maybe it's because it is off patent. I should ask around. Thanks for correcting me.

[drg]

I got blood tests and my testosterone was well higher than the normal range. I don't remember the exact number it was about 50% higher than the high end of normal. I am sure it wasn't like that last time I checked my testosterone several years ago. It seems very likely the tamoxifen caused it. I should have gotten my estradiol levels checked just for curiosity. 

[sub7]

Any idea if Tamoxifen's anti-manic and andti-Bi Polar effects are likely to be equally strong in females?
 

Being a SERM -and if I recall correctly a mixed agonist/antagonist- it is probable that effect will be different in males vs females. And this is so in some aspects as we already know: for example the increase in testosterone from Tamoxifen occurs in men but not women...

[drg]

Tamoxifen MOA in bipolar is inhibiting protein kinase c. Lithium does this too. 

So the MOA of tamoxifen in bipolar has really nothing to do with the fact it also is an estrogen antagonist. I would suspect women would experience the antimanic effect as well. 

 

But there is much more downside for a female to take it for bipolar. Women need estrogen a lot more than men do and the risk/reward might not be worth it for women.

Edited by drg, 05 December 2014 - 04:43 PM.

[sub7]

But there is much more downside for a female to take it for bipolar. Women need estrogen a lot more than men do and the risk/reward might not be worth it for women.

 

Can you briefly elaborate on some of the downsides of Tamoxifen in women?

What are some side effects to be expected if taken at doses likely sufficient to help with manic disorders?

 

 

[drg]

It could cause menstrual cycle changes.

 

Umm, but realistically tamoxifen is used more commonly in women than men, as it is used for breast cancer. So I suppose a women could consider it for the purpose of an antimanic.

 

Umm, the dose I have been using is 20mg x 2 a day, the study uses 40mg x 2 a day. I noticed some cognitive effects at 80mg a day like an  mild lithium but not at the dose of 40mg a day.I have gained weight gain, like 10 pounds in a couple months. Nothing that would stop me from taking it as I notice a lot more side effects from a large dose of lithium.

 

Those are just the side effects I notice, there is a long list of them.

 

http://www.drugs.com...de-effects.html

[Area-1255]

Estrogen contributes to bipolar episodes, and Bipolar almost always correlates with HIGH estrogen.
If not estrogen, then Copper, which happens to be increased/prolonged by Estrogen!