Toremifene Citrate

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    Toremifene Citrate


    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, improves bone mineral density, can lower prolactin, great at ER binding in breast tissue (seems to be just as good as Nolva, not as good as Ralox though), no progesterone receptor sensitivity issues like with Nolva ie you can use it with Deca and Tren (19-nors ect), it increases pituitary sensitivity to GnRH just like Tamox ie more LH over time (side note: Clomid seems to decrease sensitivity), it’s the easiest on the liver, you get none of the emotional sides or possible optical disturbances like Clomid, and it seems to be amazing at rebooting HPTA ect ect... Personally, I feel like you get all the benefits of Clomid and Nolva with far less of the negative, but as always, to each their own.

    Edit: there was a study done by some Greek researchers showing that Tamox was slightly better than Torem at increasing testosterone and LH, which would indicate that it was better at restoring HPTA. Though, the Torem dosage was lower than most use. (The study used 20 mg of Tamoxifen and 60 mg of Toremifene. Where most would use something like: 120/90/60/30 for Toremifene.) Regardless, the results for 4 weeks of use were still pretty comparable ([1] Tamox - FSH: 8.23+/-2.71 LH: 7.65+/-3.37 T: 740.27+/-227.98 || Torem - FSH: 8.15+/-4.59 LH: 6.62+/-2.99 T: 696.13+/-202.21.) Also, I wanted to note that I am unsure if Torem leads to a direct increase in the amplitude of LH release like with Clomid. Though over a extend period of time this mechanism does lead to LHRH insensitivity and a decrease LH.

    Regardless, overall Torem seems to be very effective at rebooting HPTA, and is much safer. Plus, most users seem to feel like Torem kicks in a lot sooner, thus helping you recover faster. Though, one downside is it does increase SHBG, which could lower circulating testosterone after extended use. Even so, I still feel like Toremifien is the best overall candidate for PCT.



    Now in terms of enzyme activity 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 inhibited by most SSRI. Also, many 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 as piperine, milk thistle, and quercetin (this initially inhibits, but later induces expression. Either way it should be avoided). These are found in a vast variety of supplements currently available on the market, all of which you should stay away from when consuming Tamox.


    Toremifene- only seems to require CYP3A4, not CYP2D6, to convert to it’s primarily metabolite: N-demethyltoremifene. Again, without this metabolite the SERM would be left more or less essentially ineffective. You are looking at around a 30-100x decrease in effectiveness. Thus, again you should avoid bioperine, milk thistle, and quercetin or anything else that affects CYP3A4. Though, since Torem doesn’t use CYP2D6 most anti depressants seem to be okay. For example: Cymbalta, Prozac, Paxil, Wellbutrin, Zoloft ect


    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 to add the point that in addition to having the least side effects, Toremifene also seems to be the only SERM that can be safely taken with most anti depressants and seems to have the least overall drug interactions. 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 you may want to avoided when taking the above SERMs: MyoTEST, Zeus, TestoPRO, original BioForge, PCT Assist, N1-T, Triazole, Stoked, Recycle ect you get the idea just check the ingredient list

    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 an effect on CYP3A4. Stating, [2] "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 an impact on CYP3A4 activity, and thus you’re SERM.

    Additional edit: I want to note that in the second half of this post I am claiming that the intake of various products on the market could lead to a possible interaction with how efficient many SERMs work. I believe this interaction is dependent on many variables, and to what degree it occurs will vary significantly based on a lot of factors. Though, I am in no way claiming that addition PCT products like: AI's, Test boosters, Liver/Organ support, and antioxidant products ect, should not be used with SERMs or during PCT. I just generally feel that if alternative products that don't inhibit enzyme activity are present on the market, they should be utilized as a first choice. I also want to note that everything I have written has been based on what I have personally concluded from reading various publications, posts and speaking with a few company representatives; whether or not you chose to agree is your choice.

    [1] Fertil Steril. 2009 Apr;91(4 Suppl):1427-30
    [2] 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.

    *If you would like to see additional references or studies, please let me know.

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    Fantastic post
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    So using something like cycle assist with torem would be contraindicated? What would be another option?
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    lol
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    Good post. I just started taking Torem and I can vouch for the prolactin suppression. My nips are like diamonds now. Hopefully it will be more widely available and legit if demand increases.
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    Have nolva on hand for whenever I care to start a cycle and I've been reading into Torem as well so I'm glad you posted this. Most people who use Torem are instantly won over, I just wanted to go with the tried and true method. :P
    But most likely for my second cycle I'll pick up some. Found it for like $30
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    Quote Originally Posted by Killler View Post
    lol
    Dumb question?
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    my research torem was bunk. Total test 60 and free 2.9 after 3 weeks pct. One of the lower points in my life
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    Quote Originally Posted by threeFs
    my research torem was bunk. Total test 60 and free 2.9 after 3 weeks pct. One of the lower points in my life
    Buuuuut if it had been real, you would have known
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    But you never know. Just sayin
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    Quote Originally Posted by threeFs
    But you never know. Just sayin
    My balls got huge in 2 days on torem and I started getting random boners, but I guess my next bottle from the exact same source could be bunk so I see your point...
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    yeah, I read reviews like that up and down. That's why I bought it. It's that whole not regulated by the FDA thing
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    Quote Originally Posted by threeFs
    yeah, I read reviews like that up and down. That's why I bought it. It's that whole not regulated by the FDA thing
    Man... Don't you wish the FDA would regulate that things are what they say they are at the dose they say they are, then STAY the HECK out of my choices of what I take? That'd be nice
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    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

    Quote Originally Posted by uvawahoowa View Post
    So using something like cycle assist with torem would be contraindicated? What would be another option?
    Theoretically yes, since cycle assist contains Milk Thistle... another available option would be Talos, which will be released in the coming weeks
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    Do you know if the metabolism issues apply to SNRI's as well as the SSRI's? If I'm, for example, on Effexor XR, what should I expect these products to do to me?
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    Any of you guys know of a place to test research chems for purity?
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    Quote Originally Posted by rayjay View Post
    Do you know if the metabolism issues apply to SNRI's as well as the SSRI's? If I'm, for example, on Effexor XR, what should I expect these products to do to me?
    It really depends on the SNRI... But generally effexor doesn't seem to inhibit enzyme activity, but it does seem to compete for binding. Regardless, I think there may be some issues with irregular heart beat ect. I would google drug interactions or talk to a doctor.
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    Quote Originally Posted by rayjay View Post
    Do you know if the metabolism issues apply to SNRI's as well as the SSRI's? If I'm, for example, on Effexor XR, what should I expect these products to do to me?
    There are plenty of ppl using these products who take anti depressants. I'm on lexapro 40mg
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    Quote Originally Posted by JD261985 View Post
    There are plenty of ppl using these products who take anti depressants. I'm on lexapro 40mg
    Lexapro does cause enzyme inhibition, but I do not know to what degree. Might be best to avoid Clomid and Tamox. Both may still work and effectiveness will vary from person to person, but generally speaking lexapro should make the two serms less effective
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    Quote Originally Posted by Veritatis View Post

    Lexapro does cause enzyme inhibition, but I do not know to what degree. Might be best to avoid Clomid and Tamox. Both may still work and effectiveness will vary from person to person, but generally speaking lexapro should make the two serms less effective
    Maybe hard to say though. Torem is a nolva derivative
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    Quote Originally Posted by threeFs View Post
    Maybe hard to say though. Torem is a nolva derivative
    Lexapro (escitalopram) inhibits the enzyme CYP2D6, which both tamox and clomid use to form there metabolites. Terom doesnt use CYP2D6, and to my knowledge CYP3A4 isn't inhibited by lexapro
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    Torem was always my go to serm. Balls got big in two days with random woodies. Never looked back at going to clomid again.
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    Quote Originally Posted by Veritatis
    Lexapro (escitalopram) inhibits the enzyme CYP2D6, which both tamox and clomid use to form there metabolites. Terom doesnt use CYP2D6, and to my knowledge CYP3A4 isn't inhibited by lexapro
    Wrong. Lexapro inhibits both metabolic pathways. I have said this before and will say it again. PH/AAS should not be used in conjunction with anti-depressants. I'm not trying to be a dick lol but it's easy to see. While being treated for social/anxiety/depression issues, why would a person take hormone modulating products at the same time.
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    Do you think if you took your PCT assist type product that contains Milk Thistle far away from the dosing of the Torem it would be okay?

    There are a few of those all in one type PCT products that look really good but most contain milk thistle or piperine....

    ex: PCT Assist, AD-3, PCT Revolution Black..

    Reboot and Testodrol X9 look good and don't appear to contain anything that interferes with SERMS.
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    Quote Originally Posted by av6258 View Post
    Wrong. Lexapro inhibits both metabolic pathways. I have said this before and will say it again. PH/AAS should not be used in conjunction with anti-depressants. I'm not trying to be a dick lol but it's easy to see. While being treated for social/anxiety/depression issues, why would a person take hormone modulating products at the same time.
    Wasnt aware... But, yea I would agree to a extent, but people are going to do what they are going to do, and should be aware of what combinations are the safest

    edit: could you please cite where found that lexapro inhibits CYP3A4.
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    Quote Originally Posted by Veritatis View Post

    Lexapro does cause enzyme inhibition, but I do not know to what degree. Might be best to avoid Clomid and Tamox. Both may still work and effectiveness will vary from person to person, but generally speaking lexapro should make the two serms less effective
    So what the **** am I supposed to take for PCT then?? Wtf
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    Quote Originally Posted by JD261985 View Post

    So what the **** am I supposed to take for PCT then?? Wtf
    Hold off on those medicines for 4 weeks lol probably what I would do. Get a nice libido booster instead like some epiandrosterone or w/e and have more sex if you are feeling down lmao
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    I just read that lexapro is not an inhibitor what so ever so I dont know who to believe at this point. There are more drugs for pct than just nolva , clomid and torem just saying. If ppl are going to tell me what doesn't work I would appreciate hearing what does. Just read someone's post who said he takes lexapro and nolva and recovers perfectly in PCT. So who's right and who's wrong here
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    Quote Originally Posted by JD261985 View Post
    I just read that lexapro is not an inhibitor what so ever so I dont know who to believe at this point. There are more drugs for pct than just nolva , clomid and torem just saying. If ppl are going to tell me what doesn't work I would appreciate hearing what does. Just read someone's post who said he takes lexapro and nolva and recovers perfectly in PCT. So who's right and who's wrong here
    -did he mention bloods?
    -why not try without and see how you feel? After 2 weeks you add an AI anyway (typical protocol) so by then it should matter less (my .02)
    -where's coop?!
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    Quote Originally Posted by JD261985 View Post
    I just read that lexapro is not an inhibitor what so ever so I dont know who to believe at this point. There are more drugs for pct than just nolva , clomid and torem just saying. If ppl are going to tell me what doesn't work I would appreciate hearing what does. Just read someone's post who said he takes lexapro and nolva and recovers perfectly in PCT. So who's right and who's wrong here
    Just wrote a edit... lexapro will inhibit CYP2D6, thus decreasing how effective the Nolva is... this does not mean you wont recover or that the SERM will be completely ineffective, it just simply increases the odds. I cant find anything stating that lexapro inhibits CYP3A4... Terom is probabaly the best option, but again Nolva could work. Though, it definitely wont be as effective

    Edit: lexapro inhibition of CYP2D6 is weak and doesnt seem to effect Tamoxs effectivness...
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    Ok final statement. I just read an Oxford journal report stating that lexapro and effexor are NOT inhibitors from oxfordjournals.org

    Just Google lexapro cyp2d6 inhibitor and clickk on link tomoxifen, antidepressants and CYP2D6
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    Quote Originally Posted by Veritatis View Post

    Just wrote a edit... lexapro will inhibit CYP2D6, thus decreasing how effective the Nolva is... this does not mean you wont recover or that the SERM will be completely ineffective, it just simply increases the odds. I can find nothing stating that lexapro inhibits CYP3A4, it does compete for binding, but I dont believe that is as great of a issue... Terom is prob the best option, but again Nolva could work. Though, it definitely wont be as effective
    But ok so torem is the best way to go...got it
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    Quote Originally Posted by JD261985 View Post
    Ok final statement. I just read an Oxford journal report stating that lexapro and effexor are NOT inhibitors from oxfordjournals.org

    Just Google lexapro cyp2d6 inhibitor and clickk on link tomoxifen, antidepressants and CYP2D6
    plz pm me the the link
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    Google the full PI for lexapro. In table 12 you will see the pathway metabolization info. it goes through the liver through both the CYPs. Also check the drug interaction section in table 7. FYI if any of you guys are every looking for info on certain prescription drugs, just google the PI for the said product. Its all in there
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    Quote Originally Posted by rayjay

    Man... Don't you wish the FDA would regulate that things are what they say they are at the dose they say they are, then STAY the HECK out of my choices of what I take? That'd be nice
    The FDA doesn't monitor research chemicals because as you know, they are not intended for human consumption. If anything the FDA over regulates drugs.
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    Quote Originally Posted by av6258 View Post
    Google the full PI for lexapro. In table 12 you will see the pathway metabolization info. it goes through the liver through both the CYPs. Also check the drug interaction section in table 7. FYI if any of you guys are every looking for info on certain prescription drugs, just google the PI for the said product. Its all in there
    I found studies that show it has minimal effect through the pathway torem uses so I'm not sure what you're talking about. Plus it wasn't just one study I found it was multiples from various reputable sources. Ill go find the links and post them
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    Here's one go down to drug interactions

    http://www.healthyplace.com/lexapro/...opram-oxalate/

    Please post your link
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    Oh and also after doing some more research I'm coming under the impression that exemstane and arimidex are superior pct products to nolvadex. Any thoughts? Maybe an aromasin/torem stack would be a great pct for someone using lexapro or maybe just an AI. Could an AI alone act as a pct product to get everything back to normal?
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    Quote Originally Posted by av6258 View Post
    Google the full PI for lexapro. In table 12 you will see the pathway metabolization info. it goes through the liver through both the CYPs. Also check the drug interaction section in table 7. FYI if any of you guys are every looking for info on certain prescription drugs, just google the PI for the said product. Its all in there
    "In vitro enzyme inhibition data did not reveal an inhibitory effect of escitalopram on CYP3A4"

    escitalopram doesnt inhibit CYP3A4 it is metabolized by it ie it may compete for binding with all three serms. This could potentially decrease effectiveness depending on substrate concentration, but it wont stop the enzyme from doing its job... Which I believe is the more serious issue, but in all honesty there are some many variables to be accounted for...
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    Quote Originally Posted by Veritatis

    "In vitro enzyme inhibition data did not reveal an inhibitory effect of escitalopram on CYP3A4"

    escitalopram doesnt inhibit CYP3A4 it is metabolized by it ie it may compete for binding with all three serms. This could potentially decrease effectiveness depending on substrate concentration, but it wont stop the enzyme from doing its job... Which I believe is the more serious issue, but in all honesty there are some many variables to be accounted for...
    Exactly. So it comes down to this... DONT MIX ANTIDEPRESSANTS AND STEROIDS LOL. ITS DUMB.
  

  
 

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