After 1 year on RU (45 mg night) my body has crashed (very serious)

[melanopsin]

When I used bigger dosages (way bigger than you) I also noticed cognitive changes. Quit and you'll be fine. Might take a while that's all.

Hi Swooping, how do you think RU influences cognition? How does blocking the androgen receptor lead to brain fog and inability to think as critically? Also, how long did it take you to reach base line again after quitting, cognitively?

[Swooping]

Hi Swooping, how do you think RU influences cognition? How does blocking the androgen receptor lead to brain fog and inability to think as critically? Also, how long did it take you to reach base line again after quitting, cognitively?

RU is a pretty potent anti-androgen. In the macaque model it has shown to go systemic to some extent in some monkeys (not all of them). 93% of RU is metabolized to a very weak anti-androgen and 1% is metabolized apparently to a potent anti-androgen. Perhaps systemic accumulation over time has led to some cognitive impairment in your case due to androgen deprivation (unnoticeable in the beginning but noticeable after a while). That being said I don't think it's worth full to hypothesize about what happened.

Anyway as you probably know RU isn't the only anti-androgen out there. There are several others like flutamide, enzulatamide, cyproterone acetate, nilutamide etc. Studies have shown that androgen deprivation may induce cognitive changes (mixed results in studies). Here is a study for instance that talks about this; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2853938/. Although that is based literally on systemic (full) anti-androgen therapy.

To my knowledge there are not even case reports of long term cognitive changes after cessation of anti-androgens though, so you'll be fine.

[FGF11]

Hi Swooping, how do you think RU influences cognition? How does blocking the androgen receptor lead to brain fog and inability to think as critically? Also, how long did it take you to reach base line again after quitting, cognitively?

GABA receptors have been identified electrophysiologically and pharmacologically in all regions of the brain. GABA is a chemical messenger that is widely distributed in the brain. GABA's natural function is to reduce the activity of the neurons to which it binds. The GABA-A receptors are the major inhibitory neurotransmitter receptors in mammalian brain.

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists. [http://onlinelibrary.wiley.com/doi/1...1263/abstract] It's important for the anti-androgen to not cross the blood-brain barrier. Unfortunately many of them cross this barrier (Finasteride and RU, included), These anti-androgen usually activate GABA-A receptors, causing brain fog. A couple of anti-androgen do not cross blood-brain barrier (such as ODM-201), and will not cause brain fog or seizures.

Many prostate cancer patients on MDV3100 experience life threatening seizures.

Also, for an anti-androgen to work topically, it should inhibit AR and not 5 alpha reductase. DHT is available in the blood stream, so for example topical finasteride will not work, however, topical RU will work.

I would say based on genetic make up of people, it's quite possible some of these anti-androgen, will induce depression as well as less focus, and sleeping disorders. But it may happen in small cases and is usually dose dependent.

So I believe you when you say RU might have had some side effects on you, however, MOST Likely, in a lot and a lot of cases those side effects should disappear upon discontinuing the use of the drug.


I suggest you stop it NOW, and wait for a month or so to see if you would feel betters.

Most doctors are not aware about the connection between GABA receptors and anti androgens, so i thought to give you a heads up.

[Swooping]

GABA receptors have been identified electrophysiologically and pharmacologically in all regions of the brain. GABA is a chemical messenger that is widely distributed in the brain. GABA's natural function is to reduce the activity of the neurons to which it binds. The GABA-A receptors are the major inhibitory neurotransmitter receptors in mammalian brain.

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists. [http://onlinelibrary.wiley.com/doi/1...1263/abstract] It's important for the anti-androgen to not cross the blood-brain barrier. Unfortunately many of them cross this barrier (Finasteride and RU, included), These anti-androgen usually activate GABA-A receptors, causing brain fog. A couple of anti-androgen do not cross blood-brain barrier (such as ODM-201), and will not cause brain fog or seizures.

Many prostate cancer patients on MDV3100 experience life threatening seizures.

Also, for an anti-androgen to work topically, it should inhibit AR and not 5 alpha reductase. DHT is available in the blood stream, so for example topical finasteride will not work, however, topical RU will work.

I would say based on genetic make up of people, it's quite possible some of these anti-androgen, will induce depression as well as less focus, and sleeping disorders. But it may happen in small cases and is usually dose dependent.

So I believe you when you say RU might have had some side effects on you, however, MOST Likely, in a lot and a lot of cases those side effects should disappear upon discontinuing the use of the drug.


I suggest you stop it NOW, and wait for a month or so to see if you would feel betters.

Most doctors are not aware about the connection between GABA receptors and anti androgens, so i thought to give you a heads up.

You are bringing up things that are irrelevant. First of all not many cancer patients experiences seizures with MDV3100 only around 1% of patients do. Secondly it is thought that this happens because some anti-androgens happen to have (weak) off target binding to the GABA-A receptor. Certainly not all of them, MDV3100 happens to be one of them apparently. Depends on the dosage too.

Do you have any literature or case report of such a thing happening with a compound like flutamide? Doesn't happen, while it crosses the BBB.

RU58841 in the meantime has probably been tried by 1000's of people. Perhaps it would display some affinity to the GABA-A receptor at extremely high dosages. But there is no proof for that and observational evidence doesn't even point towards that. It seems RU58841 is rather selective and doesn't display any affinity to the GABA-A receptor at least at the "normal" dosages.

If we go by your reasoning we might as well argue that 17a-estradiol will induce the same feminine changes as 17b-estradiol will do. Doesn't work like that. Again though, it's irrelevant.

[FGF11]

You are bringing up things that are irrelevant. First of all not every cancer patient experiences seizures with MDV3100 only around 1% of patients do. Secondly it is thought that this happens because some anti-androgens happen to have (weak) off target binding to the GABA-A receptor. Certainly not all of them, MDV3100 happens to be one of them apparently. Depends on the dosage too.

Do you have any literature or case report of such a thing happening with a compound like flutamide? Doesn't happen, while it crosses the BBB.

RU58841 in the meantime has probably been tried by 1000's of people. Perhaps it would display some affinity to the GABA-A receptor at very high dosages, most certainly not at the "normal" dosages.

If we go by your reasoning we might as well argue that 17a-estradiol will induce the same feminine changes as 17b-estradiol will do. Doesn't work like that. Nonetheless it's irrelevant.

#1 When I said Many I did not mean percentage wise, I meant many cases are known, but I did not meant majority (which means percentage),

#2 It clearly depends on dosage. But not all GABA-A receptors are equal. When I said genetic make up, I meant that some of these anti-androgens might have higher cognitive impact on some people (which is in general low).

#3 No, I don't. My argument doesn't need that proof, I know some anti-androgens have low or zero binding to GABA-A.

#4 RU58841 is safe unless proven otherwise. As in take it, if you experienced side effects, then stop it. The dosage differ in every person.

#5 I showed this guy what could have caused his apparent side effect, He clearly asked for it, he put [serious] in his title, so I wanted to help him. Why are you angry?

[melanopsin]

RU is a pretty potent anti-androgen. In the macaque model it has shown to go systemic to some extent in some monkeys (not all of them). 93% of RU is metabolized to a very weak anti-androgen and 1% is metabolized apparently to a potent anti-androgen. Perhaps systemic accumulation over time has led to some cognitive impairment in your case due to androgen deprivation (unnoticeable in the beginning but noticeable after a while). That being said I don't think it's worth full to hypothesize about what happened.

Anyway as you probably know RU isn't the only anti-androgen out there. There are several others like flutamide, enzulatamide, cyproterone acetate, nilutamide etc. Studies have shown that androgen deprivation may induce cognitive changes (mixed results in studies). Here is a study for instance that talks about this; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2853938/. Although that is based literally on systemic (full) anti-androgen therapy.

To my knowledge there are not even case reports of long term cognitive changes after cessation of anti-androgens though, so you'll be fine.

Thanks swoop, that article stated that " However, many but not all of these changes can return to baseline after cessation of ADT." That is pretty scary if not all of my cognitive functions return to baseline. Lets sat the toxic metabolite has accumulated in my body over the last year, is there any detox I can do to rid it faster?

Also I developed 3 bald patches on only one side my beard (look like alopecia aerata), could this be related to taking RU long term? This developed shortly after I "crashed" on Dec 11th. Keep in mind I had no problems with RU cognitively for 1 year, suddenly I woke up like a zombie Dec 11th.

[melanopsin]

#1 When I said Many I did not mean percentage wise, I meant many cases are known, but I did not meant majority (which means percentage),

#2 It clearly depends on dosage. But not all GABA-A receptors are equal. When I said genetic make up, I meant that some of these anti-androgens might have higher cognitive impact on some people (which is in general low).

#3 No, I don't. My argument doesn't need that proof, I know some anti-androgens have low or zero binding to GABA-A.

#4 RU58841 is safe unless proven otherwise. As in take it, if you experienced side effects, then stop it. The dosage differ in every person.

#5 I showed this guy what could have caused his apparent side effect, He clearly asked for it, he put [serious] in his title, so I wanted to help him. Why are you angry?

I really appreciate both your insights as you both are well read and up to date on the literature. I don't think swooping is angry, rather he is probably engaging in a "friendly" debate.

Anyway FGF11, so you are saying that it is possible that RU, the androgen blocker, can activate GABA receptors leading to inhibition? So if this is the case, why do you think that this happened suddenly after 1 year and never before? Is it due to an anti androgen metabolite accumulating and and staying in my body despite me dropping the drug for 4-5 days?

Why haven't the cognitive sides completely disappeared if the drug should be out of my system? Like I said its been 4-5 days of no RU and mentally I can not perform at high level and think critically at medical school level. Lastly, the bald patches on my beard that suddenly appeared, could it be related to this as well?

[Swooping]

@FGF11 I'm not angry lol. Good that you wanted to help OP but I assume you understand why I made that remark.

Thanks swoop, that article stated that " However, many but not all of these changes can return to baseline after cessation of ADT." That is pretty scary if not all of my cognitive functions return to baseline. Lets sat the toxic metabolite has accumulated in my body over the last year, is there any detox I can do to rid it faster?

Also I developed 3 bald patches on only one side my beard (look like alopecia aerata), could this be related to taking RU long term? This developed shortly after I "crashed" on Dec 11th. Keep in mind I had no problems with RU cognitively for 1 year, suddenly I woke up like a zombie Dec 11th.

I don't know. I can only refer you to literature about anti-androgens or androgen deprivation and what effect it may have. You should be totally fine, it just may take some time. Here is another study for example; http://www.ncbi.nlm.nih.gov/pubmed/14532781. If I were you I would just stop thinking about it, live healthy (exercise, food) and you should be totally fine. The other metabolite of RU58841 has quite a longer half life as far as I remember, don't quote me on that though. It may just take some time. Hypothesizing will only do you bad imo. The mind is a powerful thing, worrying will only make it worse I guess.

[Paul73]

Swooping,

Goid points about RU. I'm curious to know your thougts on CB-03-01. We still don't know if it will come to the market, but would you say that it's "safer" than RU considering the infos we have right now? Would you use it without fear of cancer?

Also, could you please share your thoughts about the post finasteride syndrome? Is it really possible that finasterida destroys enzymes making sexual and mental sides permanent and irrevirsible?

I'd appreciate your feedback. Thanks!

[Soonbald]

neogenic is expensive and so is RU itself..how can u afford this? guess u got a good job.. anyway do you think you got such good results because you mixed the RU with "neogenic"? is neogenic better vehicle than K&B or ethanol/pg ??