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Info on SERMs

CatSnake

Well-known member
hello all,

thought I would start a thread with some clinical studies showing recommendations for various SERMs.... hopefully this will help some folks answer some questions as to what is best or what dosage is best.

EDIT: side note-in order to mitigate side effects (blurred vision, drowsiness, etc), here are my suggestions...

1. use reasonable dosages. the data below on clomid shows that higher doses are not always better, and in that case, far worse...

2. take the SERMs at night


In general, one can expect a SERM to increase testosterone, estradiol, FSH, LH, SHBG and decreasing IGF1... there might be some direct action on the testes, as well as interaction with the hypothalamus and/or pituitary.

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Side note:

AI Thread:

http://anabolicminds.com/forum/post-cycle-therapy/288969-info-ais.html

HCG Thread:

http://anabolicminds.com/forum/post-cycle-therapy/297449-info-hcg.html#post5870442
 
Clomid

clomiphene acts on the hypothalamus to increase GnRH, which then signals the pituitary to increase LH and FSH, which then signal the testes to increase testosterone, etc.


25 mg/day increased testosterone from 247 to 610 in 4-6 weeks

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25 mg/day increased testosterone from 309 to 642 in 3 mo

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25/50 mg EOD increased testosterone from 192 to 485 in 19 mo (but E2 is up 50%)

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But, 150 mg caused desensitization of GnRH (not good!)

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Clomid might improve liver health

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*** Recommended dose for PCT: 25 mg/day ***
 
Nolvadex

Tamoxifen acts on the pituitary to increase LH and FSH, which then signal the testes to increase testosterone, etc.


20 mg increased testosterone from 496 to 835 in 2 mo.... but stops working by 3 mo.

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20 mg increased testosterone by 52% in 2-4 wks (but IGF-1 is lowered 25%)

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Might cause liver issues

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*** Recommended dose for PCT: 20 mg/day ***

*** Recommended dose for gyno: 10 mg/day ***

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maybe less is needed of nolva for gyno?




.
 
Toremefine

Toremeine acts on the pituitary to increase LH and FSH, which then signal the testes to increase testosterone, etc.


60 mg increased testosterone from 498 to 743 in 3 mo

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Might improve bone density

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Might cause liver issues

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*** Recommended dose for PCT: 60 mg/day ***
 
Raloxifene

Raloxifene acts on the pituitary to increase LH and FSH, which then signal the testes to increase testosterone, etc.


60 mg increased testosterone from 583 to 630 in 1 mo

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120 mg increased testosterone 20% in 3 months

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120 mg increased testosterone 13% in 6 weeks (but E2 is up 11%)

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Might improve bone density

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*** Recommended dose for gyno: 60 mg/day ***
 
^in looking at that data, clomid appears to be the strongest for raising testosterone, then nolva, then tore and then finally ralox.

however, when using a SERM for gyno, only 2 have very much clinical data-nolva and ralox. and this is where ralox shines...

Nolvadex

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Raloxifene

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Ralox/Nolva

"Some improvement was seen in 86% of patients receiving tamoxifen and in 91% receiving raloxifene, but a greater proportion had a significant decrease (>50%) with raloxifene (86%) than tamoxifen (41%)."

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FWIW, tore should be effective for gyno due to it's similarity to nolva…..
 
I forgot to mention the newest SERM, enclomiphene citrate (Androxal). personally, I don't know anybody that has used it yet, and the price is still at least twice what I can get regular clomid for.

it seems to be pretty comparable in results, although the dosage might be more effective at 12.5 mg vs 25 mg (testosterone went from 217 to 471 vs 209 to 405).

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EDIT: an interesting thing I just read about the half-life of encomiphene is that the half-life is 10 hours, whereas the half life of clomid is 5-7 days....
 
CatSnake said:
I forgot to mention the newest SERM, enclomiphene citrate. personally, I don't know anybody that has used it yet, and the price is still at least twice what I can get regular clomid for.

it seems to be pretty comparable in results, although the dosage might be more effective at 12.5 mg vs 25 mg.

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EDIT: an interesting thing I just read about the half-life of encomiphene is that the half-life is 10 hours, whereas the half life of clomid is 5-7 days....
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Another study on enclompiphene....

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they use 3 doses to raise testosterone (6.25 12.5 and 25), which results in a pretty big increase in testosterone (265 to 420, 295 to 404 and 253 to 604)... kinda odd numbers in there. IGF-1 is also significantly decreased as well (about 50% for all doses, I believe...
 
CatSnake said:
Another study on enclompiphene....

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they use 3 doses to raise testosterone (6.25 12.5 and 25), which results in a pretty big increase in testosterone (265 to 420, 295 to 404 and 253 to 604)... kinda odd numbers in there. IGF-1 is also significantly decreased as well (about 50% for all doses, I believe...
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Very informative article I can see this becoming a sticky eventually very useful knowledge I always worried about a iGF being lower my strength went up on Clomid but I felt like complete **** after every workout.
 
bighulksmash said:
Very informative article I can see this becoming a sticky eventually very useful knowledge I always worried about a iGF being lower my strength went up on Clomid but I felt like complete **** after every workout.
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bummer... what time of the day did you take your clomid?

i think the interesting thing about the enclomiphene, is that the half life being shorter means that if it has the same side effects, then they will be gone so much quicker, and we might not even notice them. I'm going to give it a chance on my next PCT, and see what I think....

EDIT: I just read a post by Bill Roberts on another site, and he said that clomid exerted estrogenic effects in some tissue, and antiestrogenic in other tissue. apparently enclomiphene only exerts antiestrogenic effects, so I would assume it has less side effects, as well...
 
CatSnake said:
bummer... when did you take your clomid?

i think the interesting thing about the enclomiphene, is that the half life being shorter means that if it has the same side effects, then they will be gone so much quicker, and we might not even notice them. I'm going to give it a chance on my next PCT, and see what I think....
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I have tried morning noon and night. I find noon empty stomach works best. Good luck keep us updated.
 
CatSnake said:
EDIT: I just read a post by Bill Roberts on another site, and he said that clomid exerted estrogenic effects in some tissue, and antiestrogenic in other tissue. apparently enclomiphene only exerts antiestrogenic effects, so I would assume it has less side effects, as well...
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The tricky thing with clomid is the z-isomer (zuclomiphene). This isomer can linger in the body up to two months after the last dose of clomid (case studies report a wide range of rate-of-elimination which tends to be very individualistic), and is estrogenic.

Theres a couple of hrt clinic docs who post on some of the forums, who regularly prescribe clomid for secondary hypo patients. They note the difficulty zuclomiphene poses. Apparently zuclo is an agonist of certain brain areas responsible for libido/mood; the patient will present complaining of ED/low libido/etc which typically may be thought to be due to generally too high E2 levels (which of course is a potential).

However, an AI will be ineffective if the symptoms are due to an accumulation of zuclomiphene which is then agonising the relevant brain regions. The only solution is to decrease the dose of clomid.

In other words: sometimes clomid sides are not E2 related per se (and easily treated with an AI) but rather are dose related, ie its too high.
 
NewAgeMayan said:
The tricky thing with clomid is the z-isomer (zuclomiphene). This isomer can linger in the body up to two months after the last dose of clomid (case studies report a wide range of rate-of-elimination which tends to be very individualistic), and is estrogenic.

Theres a couple of hrt clinic docs who post on some of the forums, who regularly prescribe clomid for secondary hypo patients. They note the difficulty zuclomiphene poses. Apparently zuclo is an agonist of certain brain areas responsible for libido/mood; the patient will present complaining of ED/low libido/etc which typically may be thought to be due to generally too high E2 levels (which of course is a potential).

However, an AI will be ineffective if the symptoms are due to an accumulation of zuclomiphene which is then agonising the relevant brain regions. The only solution is to decrease the dose of clomid.

In other words: sometimes clomid sides are not E2 related per se (and easily treated with an AI) but rather are dose related, ie its too high.
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interesting.... so enclomiphene will likely not have the normal clomid sides at all then, huh?
 
CatSnake said:
interesting.... so enclomiphene will likely not have the normal clomid sides at all then, huh?
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Yeah exactly. The studies suggest the benefits will still be there, and a 12.5mg dose of androxal seems almost as equi-potent as a 25mg one (as you too noted).
 
CatSnake said:
that seems like an odd dosing strategy, since enclomiphene has a pretty short half-life (10 hours or so).... or are you talking about regular clomid?
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A newer agent, enclomiphene citrate, is the transisomer of clomiphene ... with no statistically significant difference in testosterone levels ..... so its only my suggestion as IT was suggested to me this way NewAgeMayan is the man to ask !
 
Yeah Ive definitely seen 50mg eod for clomid in the studies and clinical setting but obviously nothing clinical has been established with androxal yet.
 
right on...

the half-life of clomid is 5-7 days, but enclomiphene is approx 10 hours, so I'm planning on going with daily dosing since that's what they used in all the stuff I've seen.
 
bighulksmash said:
Im weird .... I would pop clom over enclom
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I got some in the mail, so I'll let y'all know if there's any obvious difference between the two. I've had clomid work well for me in the past, but not recently, so I'm trying out the Androxal.

I typically use research chems, and the clomid I take is about 1/4 the price of the Androxal, so it's a bit of a gamble.
 
CatSnake said:
I got some in the mail, so I'll let y'all know if there's any obvious difference between the two. I've had clomid work well for me in the past, but not recently, so I'm trying out the Androxal.

I typically use research chems, and the clomid I take is about 1/4 the price of the Androxal, so it's a bit of a gamble.
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there are a few companies out there I would vouch for !!!! But when I cycle I always go PHARM after having 2 bunk exems man ... That sucked !!!


Keep us in the loop !
 
CatSnake said:
Another study on enclompiphene....

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they use 3 doses to raise testosterone (6.25 12.5 and 25), which results in a pretty big increase in testosterone (265 to 420, 295 to 404 and 253 to 604)... kinda odd numbers in there. IGF-1 is also significantly decreased as well (about 50% for all doses, I believe...
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and here's another study I found:

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got some bloodwork back on the enclomiphene....

starting testosterone was: 292 (348-1197)

after 6 weeks: 661 (348-1197)


so it works pretty well.... I personally don't feel any different then when I used clomid before (regular clomid was slightly more effective for me, but I also took A-dex with it). but, I never had any sides before either, so if that's an issue, then I'd give it a whirl.... or, if you have a drug test (USADA, etc) to worry about....

my plan is to finish this out and switch back to regular clomid, which is about 1/4 of the price for me.
 
CatSnake said:
hello all,

thought I would start a thread with some clinical studies showing recommendations for various SERMs.... hopefully this will help some folks answer some questions as to what is best or what dosage is best.

EDIT: side note-in order to mitigate side effects (blurred vision, drowsiness, etc), here are my suggestions...

1. use reasonable dosages. the data below on clomid shows that higher doses are not always better, and in that case, far worse...
Click to expand...

Agree.

Clomifene no more than 50 mg/day. Tamoxifen no more than 20 mg/day. Toremifene no more than 60 mg/day.


2. take the SERMs at night (FWIW, estrogen potentates the excitatory hormones, which is part of the reason SERMs and AIs make people tired).
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Disagree. With a half-life of 5 days, time of administration makes no difference. And you have zero research to support your claim about SERMs and excitatory neurotransmitters. There's no such thing as an "excitatory hormone"

in general, one can expect a SERM to increase testosterone, estradiol, FSH, LH, SHBG and decreasing IGF1...
Click to expand...

Neither toremifene nor raloxifene decrease IGF-1
 
Spurfy said:
Neither toremifene nor raloxifene decrease IGF-1
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no, they both lower IGF1, just like other SERMs.


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Comparison of effects of the rise in serum testosterone by raloxifene and oral testosterone on serum insulin-like growth factor-1 and insulin-like growth factor binding protein-3.

.
RESULTS:
Compared to placebo raloxifene increased serum testosterone by 20% but it decreased serum IGF-1 levels by 24.5% (95% confidence interval (CI): -13.0 to -36.1%). No significant change in serum IGFBP-3 levels was found. The effect of raloxifene on serum IGF-1 has been observed with other oral oestrogens, and, therefore, is likely to be ascribed to the partial oestrogen agonist activity of raloxifene.
.

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Raloxifene did not affect basal GH secretion or response of GH to TRH, GHRH or glucose, but
it decreased circulating IGF-I by 16%

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GH significantly increased IGF1 bioactivity, an effect attenuated by co-treatment with raloxifene (-23%) and estrogen (-26%).

below is one on Tore.... it's likely that the action of the SERM reduced the IGF1 in the tumors, as they didn't listed the levels of IGF1 in the study:

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"Toremifene did not enhance pulsatile or stimulated GH secretion, but decreased IGF-I by 20% in men and women. IGFBP3 was unchanged, whereas while IGFBP1 and SHBG increased in both sexes to a similar extent."

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Spurfy said:
Disagree. With a half-life of 5 days, time of administration makes no difference. And you have zero research to support your claim about SERMs and excitatory neurotransmitters. There's no such thing as an "excitatory hormone"
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sorry-used the wrong term.

anyway, even though there's a long half-life, it doesn't ignore the fact that there's a rapid increase in the drug upon administration common amongst various compounds.

as far as estrogen and the excitatory neurotransmitters, there's this:

Estradiol acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism

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^anecdotally, I noticed the first time I took aromasin I became incredibly drowsy, which an acquaintance explained was due to the above listed effects.
 
CatSnake said:
sorry-used the wrong term.

anyway, even though there's a long half-life, it doesn't ignore the fact that there's a rapid increase in the drug upon administration common amongst various compounds.

as far as estrogen and the excitatory neurotransmitters, there's this:

Estradiol acutely potentiates hippocampal excitatory synaptic transmission through a presynaptic mechanism

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^anecdotally, I noticed the first time I took aromasin I became incredibly drowsy, which an acquaintance explained was due to the above listed effects.
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Okay. Are you talking about E2 or SERMs? You're using the two like they're interchangeable -- they are very much not. If you have data on SERMs and neurotransmitters, then cite it.
 
Spurfy said:
Okay. Are you talking about E2 or SERMs? You're using the two like they're interchangeable -- they are very much not. If you have data on SERMs and neurotransmitters, then cite it.
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ah, no. you're missing my point.... SERMs and E2 are not interchangeable, hence the aforementioned side effects when one takes a SERM (which blocks the ER and prevents it's normal effects on the brain).

make sense?

EDIT: I will clarify that in the original post....
 
CatSnake said:
ah, no. you're missing my point.... SERMs and E2 are not interchangeable, hence the aforementioned side effects when one takes a SERM (which blocks the ER and prevents it's normal effects on the brain).

make sense?
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You have no data to back up this claim.You're just speculating. The effects of SERMs on ER is much more complex than you're asserting -- they are mixed agonist/inverse-agonist, and ER-a and ER-b are widely distributed throughout the CNS and periphery. You're taking a tiny grain of knowledge and trying to grow an entire field of wheat with it.

I can just as easily argue that SERMs elevate cortisol, which then increases wakefulness.
 
Spurfy said:
You have no data to back up this claim.You're just speculating. The effects of SERMs on ER is much more complex than you're asserting -- they are mixed agonist/inverse-agonist, and ER-a and ER-b are widely distributed throughout the CNS and periphery. You're taking a tiny grain of knowledge and trying to grow an entire field of wheat with it.

I can just as easily argue that SERMs elevate cortisol, which then increases wakefulness.
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I think the obvious response is to point out that a common side effect of SERMs and AIs is drowsiness. like I said before, that was the complaint that got me investigating those effects in the first place...

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^interesting effect of nolvadex

below is a link to a book excerpt that points out some differing effects on the brain between SERMs and E2:

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CatSnake said:
Nolvadex

20 mg increased testosterone from 496 to 835 in 2 mo.... but stops working by 3 mo.


20 mg increased testosterone by 52% in 2-4 wks (but IGF-1 is lowered 25%)
Click to expand...

I just finished a 10 week run of LGD 4033 a week ago at which point I opened a bottle of Erase Pro+ and then started BLR Rebirth three days ago. I'm intending to start a bottle of King's Blood on Monday but my clomid and nolvadex won't arrive until Wednesday. Given the extended run of LGD, I think I might need more than 4 weeks on SERMS, and am considering starting with some clomid to make sure that there's a restart if needed and to get my recovery started. After that though, do you think I should switch to nolvadex or continue on clomid? I also have some HCG en-route for undoing the atrophy I've had but I'm not sure when I should start taking it or when I should stop. What would you recommend?
 
u_e_s_i said:
I just finished a 10 week run of LGD 4033 a week ago at which point I opened a bottle of Erase Pro+ and then started BLR Rebirth three days ago. I'm intending to start a bottle of King's Blood on Monday but my clomid and nolvadex won't arrive until Wednesday. Given the extended run of LGD, I think I might need more than 4 weeks on SERMS, and am considering starting with some clomid to make sure that there's a restart if needed and to get my recovery started. After that though, do you think I should switch to nolvadex or continue on clomid? I also have some HCG en-route for undoing the atrophy I've had but I'm not sure when I should start taking it or when I should stop. What would you recommend?
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I don't think you need both Nolva and Clomid, but I definitely agree that you need more than 4 weeks on PCT. for a 10 week cycle I'd go with 6-8 weeks, personally.
 
CatSnake said:
I don't think you need both Nolva and Clomid, but I definitely agree that you need more than 4 weeks on PCT. for a 10 week cycle I'd go with 6-8 weeks, personally.
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I always run both nolva and Clomid for pct, got good results after. No other supps but arimicare pro and a.i as needed
 
livestrong82 said:
I always run both nolva and Clomid for pct, got good results after. No other supps but arimicare pro and a.i as needed
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are you kidding? you literally just posted a thread when you have low testosterone levels after PCT....

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CatSnake said:
are you kidding? you literally just posted a thread when you have low testosterone levels after PCT....

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Yes I did.
Since u can Read, pay attention to the details of the anabolics I ran and the length of the cycle.

Like I said I kept my gains and feel great. After running both Clomid and nolva. In that post I was asking on input for the lh levels
 
livestrong82 said:
Yes I did.
Since u can Read, pay attention to the details of the anabolics I ran and the length of the cycle.

Like I said I kept my gains and feel great. After running both Clomid and nolva. In that post I was asking on input for the lh levels
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the biggest detail to pay attention to, is that you didn't recover correctly.

you're 10 weeks post cycle and you have low testosterone. don't even pretend to think that you understand enough to give others advice of how to do their post cycle, as you clearly don't, as proven by your own bloodwork.
 
CatSnake said:
the biggest detail to pay attention to, is that you didn't recover correctly.

you're 10 weeks post cycle and you have low testosterone. don't even pretend to think that you understand enough to give others advice of how to do their post cycle, as you clearly don't, as proven by your own bloodwork.
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Why you mad bro?
 
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^high LH levels stimulate aromatase activity in the testes.

an example as to why mega-dosing or stacking multiple SERMs can cause an increase in E2 aromatization.....
 
CatSnake said:
Nolvadex

Tamoxifen acts on the pituitary to increase LH and FSH, which then signal the testes to increase testosterone, etc.


20 mg increased testosterone from 496 to 835 in 2 mo.... but stops working by 3 mo.

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20 mg increased testosterone by 52% in 2-4 wks (but IGF-1 is lowered 25%)

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Might cause liver issues

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*** Recommended dose for PCT: 20 mg/day ***

*** Recommended dose for gyno: 10 mg/day ***

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maybe less is needed of nolva for gyno?




.
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Lets say im using to get rid of gyno starting Nov 1 but plan on using thru next cycle prolly round 1st of January end of December. Should I use a 10mg a day or just jump on 20mg a day? Or wait to jump on 20mg till cycle? I have 6 months Tamo(pharmacy stuff) and 70ct 15mg tabs Tamo(research co). What cha think CatSnake maybe start w research tabs 1st then jump on pharmacy stuff during cycle till end of Tamo?? Thanks man your help and opinion have really helped me bf so what cha think, boss, lol ??
 
If 10 mg works, then I don't really see a reason to go up.

Unless you had like a bb show or something, and needed to deal with gyno quick....
 
CatSnake said:
If 10 mg works, then I don't really see a reason to go up.

Unless you had like a bb show or something, and needed to deal with gyno quick....
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I have a pill cutter so thats how ill do it and if I go that route ill have double the meds....hey im not complaining. ..and again thanks for ur input. Awesome log also ,man!!!
 
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