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Thread: Anti-estrogen ?

  1. #1
    JD5096 is offline New Member
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    Question Anti-estrogen ?

    Since anti-estrogens attach themselves to estrogen receptors and you still have free floating estrogen running through your blood stream does that mean that you are still prone to water retention, or does it have to attach to the receptor first for this to happen?

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    Pinnacle's Avatar
    Pinnacle is offline AR-Hall of Famer ~ Cocky motherF*cker!
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    Quote Originally Posted by JD5096
    Since anti-estrogens attach themselves to estrogen receptors and you still have free floating estrogen running through your blood stream does that mean that you are still prone to water retention, or does it have to attach to the receptor first for this to happen?
    That's why we use l-dex.To combat that free estrogen that causes water retention.Nolv and l-dex work in harmony.


    ~Pinnacle~

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    Quote Originally Posted by Pinnacle
    That's why we use l-dex.To combat that free estrogen that causes water retention.Nolv and l-dex work in harmony.


    ~Pinnacle~
    Actually they do the opposite...the Nolv reduces the effectiveness of the 'Dex.

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    Pinnacle's Avatar
    Pinnacle is offline AR-Hall of Famer ~ Cocky motherF*cker!
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    Quote Originally Posted by hooker
    Actually they do the opposite...the Nolv reduces the effectiveness of the 'Dex.
    How so?This combo has been a proven favorite for ages.


    ~Pinnacle~

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    Here's the highlights of the studies:


    There is known drug-drug interaction of tamoxifen with anastrozole and letrozole . Concomitant administration of either anastrozole or letrozole with tamoxifen decreases the plasma level of the AI. Concomitant administration of letrozole and tamoxifen decreased the level of letrozole by 38% (90% confidence interval, 32–43%; ). Anastrozole and tamoxifen administrated concomitantly in the ATAC trial lowered the plasma anastrozole level in the combined arm by 27% (90% confidence interval, 20–30%. Whereas the combined therapy arm of the ATAC trial demonstrated a decrease in the plasma concentration of anastrozole, systemic E2 suppression was similar to that observed in patients treated with anastrozole alone. Based on the observed drug-drug interaction and the lack of clinical data demonstrating the superiority of the combined arm, this arm of the study is being discontinued.
    In the ATAC study in early-stage breast cancer, a third combination arm of tamoxifen plus anastrozole was studied. Early results from the trial suggested that women receiving the combination had a comparable outcome in terms of disease recurrence compared with those taking tamoxifen alone. The concept behind this trial was total estrogen blockade in the hope of improving the therapeutic efficacy while exploiting the positive effects of tamoxifen on bone and lipid metabolism to counter the putative negative effects of the aromatase inhibitor. Before the ATAC trial, Brodie et al.had used a nude mouse model bearing aromatase up-regulated MCF-7 cells to predict that the combination arm would be less effective than the aromatase inhibitor alone. This was true for both anastrozole and letrozole in this preclinical model. The most popular hypothesis for failure of tamoxifen to add to the aromatase inhibitor’s effects is the suggestion that tamoxifen’s agonist effects are provoked or exaggerated in the presence of low estrogen levels.

    Dowsett M., Pfister C., Johnson S. R. D., Miles D. W., Houston S. J., Verbeek J. A. Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromatase inhibitor letrozole in postmenopausal women with breast cancer. Clin. Cancer Res., 5: 2338-2343, 1999.

    The ATAC Trialists’ Group. Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a sub-protocol of the "Arimidex and Tamoxifen Alone or in Combination" (ATAC) trial. Br. J. Cancer, 85: 317-324, 2001

    Clinical Cancer Research Vol. 10, 372S-379S, January 2004

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    Two4the$$ is offline Senior Member
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    Quote Originally Posted by hooker
    Here's the highlights of the studies:





    Dowsett M., Pfister C., Johnson S. R. D., Miles D. W., Houston S. J., Verbeek J. A. Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromatase inhibitor letrozole in postmenopausal women with breast cancer. Clin. Cancer Res., 5: 2338-2343, 1999.

    The ATAC Trialists’ Group. Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a sub-protocol of the "Arimidex and Tamoxifen Alone or in Combination" (ATAC) trial. Br. J. Cancer, 85: 317-324, 2001

    Clinical Cancer Research Vol. 10, 372S-379S, January 2004

    Correct me if I'm wrong... but from the prospective of a BB, that is actually a positive affect - reducing the affectiveness of Arimidex or Letro ... and getting SERM like benefits while still reducing the Estrogen more than a SERM alone can (I'm thinking of a person doing a highly estrogenic cycle, or high dosages of moderately estrogenic cycles...)

    Hooker, while we're here ... have you seen anyone trading in Faslodex. No source needed, no PM's, nothing like that - but have you seen ANYONE with it? Or is it just too early in it's intro to our world to expect to find? And if not, what would you recommend as an anti progestin?

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    Quote Originally Posted by TrumanHW
    Correct me if I'm wrong... but from the prospective of a BB, that is actually a positive affect - reducing the affectiveness of Arimidex or Letro ... and getting SERM like benefits while still reducing the Estrogen more than a SERM alone can (I'm thinking of a person doing a highly estrogenic cycle, or high dosages of moderately estrogenic cycles...)


    Possibly, yeah, you get the benefits of the Nolv, but you are wasting some money on your Arim dose, because some of it is being blocked by the Nolv...

    There is, however, an AI that works synergistically with Nolvadex ; I was with System_Admin and Lion this week in Maryland, and I brought up adding that AI into the AR-R product line to Lion...we'll see if anything comes of that...

    Hooker, while we're here ... have you seen anyone trading in Faslodex. No source needed, no PM's, nothing like that - but have you seen ANYONE with it? Or is it just too early in it's intro to our world to expect to find? And if not, what would you recommend as an anti progestin?
    No...too expensive...nobody carries it. You can use Letro, though, for that.

  8. #8
    Two4the$$ is offline Senior Member
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    You're KILLING ME!!! What's it called??? You GOTTA say the name man!!! lol

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