Erase or Triazole or both?

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  1. Quote Originally Posted by Ninjo View Post
    Great info, thanks for this.

    I would think that the biggest challenge would be how to avoidi milk thistle as it is in most OTC cycle support products (e.g. Cycle Support, Cycle Assist, etc.) that many continue to take during PCT.


    Sent from my iPad using Tapatalk
    I've come across a good number of studies showing that milk of thistle has a significant effect on CYP3A4 activity. Some show anywhere from 50-100% inhibition, which essentially effects the activity all the above SERMs. Though, I have also come across one that stated "silybin concentrations after intake of milk thistle are too low to significantly affect the function of CYP3A4" ie the recommended doses of milk thistle are too low to have any effect. But, I do believe that any effective milk of thistle product on the market would have a significant effect.


  2. Soo I like to have a grapefruit a day.. Usually a half before 2 biggest meals...

    I'm not currently taking anything that it would be problematic with, but something OTC that I have used and would like to again in the future is ISATEST by gaspari- it says on label it has p450 aromatase inhibitor- would this be a product I would wantto avoid my grapefruit and bioprene, etc?? Thank you! Learning a lot right here
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  3. Quote Originally Posted by Veritatis View Post
    Like the 100th time I am editing this post but here we go:


    Wanted to add this just in case someone comes across this post in the future:


    First of all, after spending a few hours reading studies and reviews for Tamoxifen, Clomiphene, and Toremifene; Toremifene is now the only SERM I will ever recommend. For it definitely seems to be the most effective and safest overall... A few reasons being: it lowers ldl, increases hdl, can lower prolactin, great at ER binding in breast tissue (seems to be just as good if not better then Nolva, not as good as Ralox though), no progesterone issues, easiest on the liver, and it seems to be amazing at rebooting HPTA (some users have even claimed it to be better then clomid)... but as always, to each there own.

    Now in terms of enzymes and the following SERMs:

    Tamoxifen- requires both CYP2D6 and CYP3A4 to convert to its metabolites, such as 4-hydroxytamoxifen and N-desmethyl-4-hydroxytamoxifen. Without these metabolite there would be significantly less ER binding, leading to a substantial decrease in function. The enzyme CYP2D6 is used by most SSRI. Therefore, they compete for binding, and anti depressants seem to be able to bind more readily then tamoxifen. So, in general anti depressants should be avoided when using tamoxifen. In addition, the enzyme CYP3A4 is inhibited by things such piperine, milk thistle, and quercetin (this initially inhibits, but later induces expression. Either way it should be avoided). These are found a vast variety of supplements on the market, all of which should be avoided.

    Toremifene- only seems to require CYP3A4, not CYP2D6, to convert to its primarily metabolite: N-demethyltoremifene. Again without this metabolite the SERM would be left more or less essentially ineffective. We are looking at around a 30-100x decrease in effectiveness. Thus, again we want to avoid bioperine, milk thistle, and quercetin or anything else that effects CYP3A4, but most anti depressants seem to be okay.

    Clomiphene- The conversion of its metabolites depends on both CYP2D6 and CYP3A4 to produce 4-hydroxy-N-desethylclomiphene, 4-OH-DE-Clom, 4-hydroxyclomiphene ect. So, again you should avoid anti depressants, bioperine, milk thistle, and quercetin

    So, in conclusion stay away from bioperine, milk thistle, quercetin and even grapefruit juice with any of the above SERMs. (Grapefruit juice inhibits P450 enzyme activity, which may allow for greater initial build up/concentrations of the above SERMs, but in the long run using grapefruit juice will make them less effective and should thus be avoided.) Also, I want to note there are most likely other P450 enzymes involved ect. I am just trying add the point that Toremifene seems to be the only SERM that can be safely taken with most anti depressants. Though, always verify drug interactions and consult a doctor before taking anything.

    In addition here is a list of a few regularly used products that should be avoided when taking the above SERMs: MyoTEST, Zeus, TestoPRO, original BioForge, PCT Assist, N1-T, Triazole, Stoked ect you get the idea

    Edit: I have come across some contradicting studies with milk thistle and CYP3A4, some claim a 50-100% decrease in activity. Others say most products don't provide a significant amount of extract to have a effect on CYP3A4. Stating, [1] "Silybin concentrations after intake of milk thistle are too low to significantly affect the function of CYP3A4." Though, I do believe that any effective Milk of Thistle product on the market will have a impact on CYP3A4 activity and your SERM.

    [1] van Erp NP, Baker SD, Zhao M, et al.: Effect of milk thistle (Silybum marianum) on the pharmacokinetics of irinotecan. Clin Cancer Res 11 (21): 7800-6, 2005.
    Very goood info here!
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  4. Quote Originally Posted by kevinhy View Post
    Very goood info here!
    Thanks.. wanted to note that I made some minor changes to the write up... Also, I could theorize a bit more/add more details from publications, but I think I made my point

  5. Quote Originally Posted by chedapalooza View Post
    Soo I like to have a grapefruit a day.. Usually a half before 2 biggest meals...

    I'm not currently taking anything that it would be problematic with, but something OTC that I have used and would like to again in the future is ISATEST by gaspari- it says on label it has p450 aromatase inhibitor- would this be a product I would wantto avoid my grapefruit and bioprene, etc?? Thank you! Learning a lot right here
    I am not to familiar with how this product works and the best people to contact would be gaspari

  6. Quote Originally Posted by chedapalooza
    Soo I like to have a grapefruit a day.. Usually a half before 2 biggest meals...

    I'm not currently taking anything that it would be problematic with, but something OTC that I have used and would like to again in the future is ISATEST by gaspari- it says on label it has p450 aromatase inhibitor- would this be a product I would wantto avoid my grapefruit and bioprene, etc?? Thank you! Learning a lot right here
    Quote Originally Posted by Veritatis

    I am not to familiar with how this product works and the best people to contact would be gaspari
    Coop?? Lol

  7. Quote Originally Posted by chedapalooza View Post
    Coop?? Lol
    There's no issue. You can't compare clinical AIs to natty tboosters (and a junk one at that).

    it's also made by isatori btw

  8. Quote Originally Posted by mr.cooper69

    There's no issue. You can't compare clinical AIs to natty tboosters (and a junk one at that).

    it's also made by isatori btw
    Youre right, I knew that idk why I said gaspari

  9. Quote Originally Posted by chedapalooza View Post
    Youre right, I knew that idk why I said gaspari
    I was wondering why I couldnt find it...
  

  
 

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