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Old 12-03-2005, 04:03 PM
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Default A PubMed article on lowering E2 in obese men.

Letrozole normalizes serum testosterone in severely obese men with hypogonadotropic hypogonadism.

de Boer H, Verschoor L, Ruinemans-Koerts J, Jansen M.

Department of Internal Medicine, Ziekenhuis Rijnstate, Wagnerlaan 55, 6800 TA Arnhem, The Netherlands. hdeboer@alysis.nl

BACKGROUND: Morbid obesity is associated with increased estradiol production as a result of aromatase-dependent conversion of testosterone to estradiol. The elevated serum estradiol levels may inhibit pituitary LH secretion to such extent that hypogonadotropic hypogonadism can result. Normalization of the disturbed estradiol-testosterone balance may be beneficial to reverse the adverse effects of hypogonadism. AIM: To examine whether aromatase inhibition with Letrozole can normalize serum testosterone levels in severely obese men with hypogonadotropic hypogonadism. PATIENTS AND METHODS: Ten severely obese men, mean age 48.2 +/- 2.3 (s.e.) years and body mass index 42.1 +/- 2.6 kg/m(2), were treated with Letrozole for 6 weeks in doses ranging from 7.5 to 17.5 mg per week. RESULTS: Six weeks of treatment decreased serum estradiol from 120 +/- 20 to 70 +/- 9 pmol/l (p = 0.006). None of the subjects developed an estradiol level of less than 40 pmol/l. LH increased from 4.5 +/- 0.8 to 14.8 +/- 2.3 U/l (p < 0.001). Total testosterone rose from 7.5 +/- 1.0 to 23.8 +/- 3.0 nmol/l (p < 0.001) without a concomitant change in sex hormone-binding globulin level. Those treated with Letrozole 17.5 mg per week had an excessive LH response. CONCLUSION: Short-term Letrozole treatment normalized serum testosterone levels in all obese men. The clinical significance of this intervention remains to be established in controlled, long-term studies.

Publication Types:
Clinical Trial

PMID: 15811136 [PubMed - indexed for MEDLINE]
Here is a the Link.
http://tinyurl.com/dh3jy
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Old 12-03-2005, 06:46 PM
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Yes, Letrozole is in a class of drugs known as aromatase inhibitors; it prevents formation of estrogen. That is the same class of drugs that Arimidex belongs to, it also is an "aromatase inhibitor".

From what I have gathered from various posters (TRT as well as even checking AAS Boards), it seems that Letrozole is considered by most to be quite a bit stronger than Arimidex - and many cautions about being careful with the dosing so that E2 levels aren't lowered too much!

I haven't been over there for a while but there was a posting on the H2 Board about a TRT patient going on Letrozole and quickly getting "crashed" with the E2 (I think it was possibly by "Rachel" in regards to her husband???). You might want to do a search on Letrozole and see if that's over there.

Testolactone is also another medication that is an aromatase inhibitor and blocks the conversion of androgens (testosterone) to estrogens.

I imagine that any one of them - properly dosed - would have had the same results as the Letrozole demostrated in this study...

Also, this was an awfully small study and of very short duration... I was also bothered by the frequency of the use of "may" (as in it "may do this" or "may have 'such-and-such' results").

Also that they didn't publish the reference ranges for estradiol or testosterone. I noted that E2 levels were reduced from an average of 120 to 70, so that's great... but if the reference range is 10 - 50, then levels are still unacceptably elevated...

Quote:
Six weeks of treatment decreased serum estradiol from 120 +/- 20 to 70 +/- 9 pmol/l (p = 0.006). None of the subjects developed an estradiol level of less than 40 pmol/l.


For testosterone:

Quote:
Total testosterone rose from 7.5 +/- 1.0 to 23.8 +/- 3.0 nmol/l (p < 0.001) without a concomitant change in sex hormone-binding globulin level.


Reference ranges with those measurements and that Lab??? If normal range is 15 - 60 (just for example), then 23 would still be pretty low normal...

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Old 12-03-2005, 06:51 PM
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Yes I read Rachel's post and talked to her. Her husband is not on TRT and that is way he crashed so fast. I tried to tell her to do a 1/4 of a pill once a week. Now she is trying a 1/16 dose evey few days.
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Old 12-03-2005, 07:12 PM
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Other info from a study that actually used AAS levels of testosterone with weightlifters (not that I am in any way recommending this mode of action, just quoting the study to show AI effects of medication utilized):

In the present study, we tested the hypothesis that aromatization of androgen to estrogen blunts the lipid and lipase effects of exogenous testosterone. Fourteen male weightlifters received testosterone enanthate (200 mg/wk intramuscularly), the aromatase inhibitor testolactone (250 mg four times per day), or both drugs together in a randomized cross-over design. Serum testosterone level increased during all three drug treatments, whereas estradiol level increased only with testosterone alone (+47%, P < .05), demonstrating that testolactone effectively inhibited testosterone aromatization...

Zmuda JM, Fahrenbach MC, Younkin BT, Bausserman LL, Terry RB, Catlin DH, Thompson PD. Department of Medicine, Miriam Hospital, Providence, RI.



Some various informational links:

Aromatization - http://qualitycounts.com/fparomatization.html

Quote:
Arimidex (anastrozole) / Aromasin (exemestane) / Femara (letrozole) / Nolvadex (tamoxifen) / Faslodex (fulvestrant)
http://www.nature.com/ijir/journal/v.../3901154a.html

http://clincancerres.aacrjournals.or.../full/9/1/468S

http://jcem.endojournals.org/cgi/content/full/85/7/2370

http://jcem.endojournals.org/cgi/con...ull/86/10/4887


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Old 12-03-2005, 07:26 PM
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Default More Info on AIs

Quote:
Arimidex (anastrozole)

Arimidex is an oral aromatase inhibitor and has an active life of about 48 hours. The average dose is about .25 v 1.0 mg/day, as it is very potent. The drug was initially developed to treat advanced breast cancer in women and is manufactured by the drug company Zenica Pharmaceuticals and was approved for use in the United States in December 1995. Arimidex is the first in a new class of third-generation oral aromatase inhibitors, therefore some hail it as a revolutionary drug. Arimidex acts by blocking the aromatase enzyme, effectively blocking estrogen production in both males and females. Many forms of breast cancer cells are stimulated by estrogen, therefore the blocking of the production of estrogen may be able to halt the progression of the cancer. Arimidex is extremely powerful, as is evident by the very small dosage required to illicit a major effect. Because of its powerful effect, this drug is only used by post menopausal women whose disease has progressed despite treatment with Nolvadex. Side effects include hot flashes and thinning hair. When this drug is used in conjunction with strong, aromatizing androgens such as testosterone, the harsh side effects of the androgens such as gynecomastia and water retention can be diminished. However, while Arimidex will effectively reduce estrogenic side effects, too much can reduce estrogens too far, and will block the beneficial properties of estrogen (mainly estrogens effect on cholesterol).

Quote:
Aromasin (exemestane)

Aromasin has been used clinically to treat advanced breast cancer in postmenopausal whose disease has gotten worse after treatment with Tamoxifin. Aromasin is closely related to Arimidex and Femara, therefore the drug profiles of the two aforementioned drugs will give adequate insight into the action of Aromasin.

Quote:
Femara (letrozole)

Femara is an oral aromatase inhibitor with an active life of 2 to 4 days. Femara is a relatively new drug developed for the treatment of advanced breast cancer, much like Arimidex. Like Arimidex, Femara belongs to the class of third-generation selective oral aromatase inhibitors and acts by blocking the enzyme, aromatase and subsequently blocking estrogen production. A daily dose of 2.5 mg can illicit full estrogen suppression. For male athletes, Femara has good results, competing with drugs such as Nolvadex and Proviron. These drugs are more effective in combination. When Femara is used with powerful aromatizing androgens, such as testosterone, side effects such as gynecomastia and water retention can be effectively reduced. However, there are concerns with Femara. While it will reduce esterogenic side effects, it will also suppress HDL if used in full suppression doses. See Arimidex for more, as these compounds are very closely related, the side effects are similar.

Quote:
Teslac (testolactone)

Teslac has a similar structure of various androgenic steroids but does not have androgenic properties. Clinically, this estrogen antagonist was used to treat breast cancer in women and was used to block the effects of estrogen. In athletes, Teslac is used to block estrogen resulting from aromatizing steroid use and has been found to be quite effective. However, Nolvadex is by far the most popular, and as a result, Teslac is rarely seen... but can still be made available through a prescription. Effective dosages vary between 500 mg and 1000 mg a day. The side effects of this drug are currently unknown, so caution should be used when taking Teslac.
Larry

P.S. I thought that was Rachel's husband. Wasn't aware that he wasn't on some type of regular TRT.
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Old 12-03-2005, 11:30 PM
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I find it interesting that 2.5mg of letrozole lowers estradiol in women perhaps 97% but only roughly 50% in men.

And the same situation appears to exist with another AI, anastrozole:

http://jcem.endojournals.org/cgi/con...85/7/2370#SEC2

Curious if yet higher doses of the AIs would further suppress estradiol and/or total estrogen.
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Old 12-04-2005, 10:23 AM
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bump (not that im obese) good thread

the thing about aromasin it has minor androgenic properties..

what long term side effects it has i am not aware of...(haven't had a chance to read about it)

Last edited by ciobl; 12-04-2005 at 10:34 AM.
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Old 12-04-2005, 06:23 PM
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Quote:
Originally Posted by ciobl

the thing about aromasin it has minor androgenic properties..

what long term side effects it has i am not aware of...(haven't had a chance to read about it)
I think it is a working suicide inhibitor. Structurally, Aromasin is like an AAS. Someone should do a study on its effects in men with excessive E2.
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