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Home > Health Conditions > Aromatization.
Aromatization/Gynecomastia
Related Topics:
Prescription aromatase inhibitors:
The Really Important Stuff:
- Anastrozole (Arimidex) - anabolic-androgenic-steroids.com -
"Anastrozole (Arimidex) is the
aromatase inhibitor of choice ...With moderate doses of testosterone 0.5 mg/day is usually sufficient and in some cases may be too much" - Femara (letrozole) may not have been available at the time this article was written.
- Chrysin: Is It
An Effective Aromatase Inhibitor? - vrp.com - "Unfortunately, there does not
appear to be any effective natural inhibitor of aromatase"
-
Letrozole once a week normalizes serum testosterone in obesity-related male
hypogonadism - Eur J Endocrinol. 2008 May;158(5):741-7 -
"Isolated hypogonadotropic hypogonadism (IHH) is
frequently observed in severely obese men, probably as a result of increased
estradiol (E(2)) production and E(2)-mediated negative feedback on pituitary
LH secretion. Aromatase inhibitors can reverse this process ... treated with
2.5 mg letrozole once a week for 6 months ... Six weeks of treatment reduced
total E(2) from 123+/-11 to 58+/-7 pmol/l (P<0.001, mean+/-s.e.m.), and
increased serum LH from 4.4+/-0.6 to 11.1+/-1.5 U/l (P<0.001). Total
testosterone rose from 5.9+/-0.5 to 19.6+/-1.4 nmol/l (P<0.001), and free
testosterone from 163+/-13 to 604+/-50 pmol/l (P<0.001). Total testosterone
rose to within the normal range in all subjects, whereas free testosterone
rose to supraphysiological levels in 7 out of 12 men ... Letrozole 2.5 mg
once a week produced a sustained normalization of serum total testosterone
in obese men with IHH. However, free testosterone frequently rose to
supraphysiological levels. Therefore, a starting dose <2.5 mg once a week is
recommended" - See
Femara (letrozole) at OffshoreRX
 .
I've been taking a quarter table a day but it sounds like that's way to much
an a quarter tablet every other day might be best which comes to 2.5 mg
every 8 days. People complain about the hassle to get doctors to
prescribe testosterone. It sounds like letrozole will give you the
same or better numbers without the hassle. Plus testosterone
replacement increases estrogen but letrozole has the advantage of decreasing
it. See my aromatization page.
-
Long-term
Consequences of the Aromatase Inhibitors - Medscape, 11/16/05 -
"The "short-term toxicities," such
as vasomotor symptoms, venothromboemboli, and gynecologic complications,
favor the use of AIs. However, long-term bone loss, altered lipid profiles,
and possible compromise in sexual functioning appear to be adversely
affected by the AIs"
-
Letrozole normalizes serum testosterone in severely obese men with
hypogonadotropic hypogonadism - Diabetes Obes Metab. 2005 May;7(3):211-5
- "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" - Note: A
half tablet per day would be 8.75 mg/week. I believe 40 pmol/l of
estradiol is
11.54
pg/mL and the normal value for men is
10 to 52 pg/mL (Quest
says
10 to 50). The way I read that,
testosterone tripled. I take a half tablet a day of
Femara
(letrozole). See Femara at International Anti-aging Systems
or Letrozole at OffshoreRX.com.
- Can Broccoli Prevent Lupus? - WebMD, 11/6/03 -
"I3C is believed to act as an anti-estrogen ... I3C-fed mice had far fewer kidney problems than the
mice whose diets were not supplemented, and researchers say this is the reason that they lived much longer. Kidney disease is one of the main, life-threatening complications of lupus" - See
iHerb
 I3C products.
-
Why
Testosterone Levels Decline - Life Extension Magazine, 11/99 -
"Clinical studies using testosterone injections, creams, or patches have often failed to provide a long-lasting, libido-enhancing effect in aging men (98). We now know why. The testosterone can be
converted to estrogen. The estrogen is then taken up by testosterone receptor sites in cells throughout the body. When an estrogen molecule occupies a testosterone receptor site on a cell membrane, it blocks the ability of serum testosterone to induce a healthy hormonal signal. It does not matter how much serum free
testosterone is available if excess estrogen is competing for the same cellular receptor sites"
-
Correcting
A Hormone Imbalance - Life Extension Magazine, 11/99 -
"If all of the above fail to increase free testosterone and lower excess estradiol, then ask your doctor to prescribe the potent aromatase inhibiting drug Arimidex (anastrozole) in the very low dose of one-half
(0.5 mg) mg, twice a week"
- Androgel prescribing information - androgel.com -
"Serum estradiol (E2) concentrations increased significantly within 30 days of starting treatment with AndroGel® 5 or 10 G/day and remained
elevated throughout the treatment period but remained within the normal range for eugonadal men" - Yeah, but what if you are taking DHEA and what about testosterone/estrogen ratios. See:
- Biotransformation of oral dehydroepiandrosterone in elderly men: significant increase in circulating estrogens - J Clin Endocrinol Metab 1999 Jun;84(6):2170-6 -
"Serum testosterone and dihydrotestosterone remained unchanged after DHEA administration. In contrast, 17beta-estradiol and estrone significantly increased in a dose-dependent manner to concentrations still within the upper normal range for men [placebo vs. 50 mg DHEA vs.
100 mg DHEA; AUC 0-12 h for 17beta-estradiol, 510 +/- 198 vs. 635 +/- 156 vs. 700 +/- 209 pmol/L x h (P < 0.0001); AUC 0-12 h for estrone, 1443 +/- 269 vs. 2537 +/- 434 vs. 3254 +/- 671 pmol/L x h (P < 0.0001)]"
- Estrogen: The Unrecognized Male Hormone - IAS
-
Testosterone
Deficiency & Depression, Does DHEA Raise the Levels of Bioavailable Testosterone in Men? - Life Extension Magazine, 8/02 -
"Some men on testosterone drug replacement therapy develop dangerously high
estrogen levels. Estrogen can be suppressed by taking an aromatase-inhibiting drug like Arimidex (0.5 mg twice a week) or using a supplement like Super Mira Forte (six capsules daily)"
- See
Arimidex at International Anti-aging Systems.
- Biotransformation of oral dehydroepiandrosterone in elderly men: significant increase in circulating estrogens - J Clin Endocrinol Metab 1999 Jun;84(6):2170-6 -
"Serum testosterone and dihydrotestosterone remained unchanged after DHEA administration. In contrast, 17beta-estradiol and estrone significantly increased in a dose-dependent manner to concentrations still within the upper normal range for men
[placebo vs. 50 mg DHEA vs. 100 mg DHEA; AUC 0-12 h for 17beta-estradiol, 510 +/- 198 vs. 635 +/- 156 vs. 700 +/- 209 pmol/L x h (P < 0.0001); AUC 0-12 h for estrone, 1443 +/- 269 vs. 2537 +/- 434 vs. 3254 +/- 671 pmol/L x h (P < 0.0001)]" - That's a 40% increase in the bad estrogen!
On top of that, if you are taking testosterone, that increases estrogen also.
- Aromatase Inhibition Corrects Endocrinopathy In Infertile Men - Doctor's Guide, 4/9/01 -
"investigators found that men with severe infertility had significantly lower
testosterone (328 versus 543 ng/dl) and significantly higher oestradiol (58.4 versus 43.5 ng/l) than the fertile controls. As a result, the infertile men had much lower testosterone-to-oestradiol ratios ... These abnormalities were corrected in the 45 men who received testolactone and their testosterone-to-oestradiol
ratios rose into the normal range"
- Evidence of a Treatable Endocrinopathy in Infertile Men - J. of Urology, 3/01 -
"We identified an endocrinopathy in men with severe male factor
infertility that is characterized by a decreased serum testosterone-to-estradiol ratio. This ratio can be corrected by aromatase inhibition, resulting in a significant improvement in semen parameters in oligospermic patients"
-
Replenish
Testosterone Naturally - Life Extension Magazine, 1/00 -
"Through a variety of mechanisms, aging men suffer from the dual effects of having too little testosterone and excess estrogen. The result is a testosterone/ estrogen imbalance that can severely inhibit sexual desire
and performance ... Too much estrogen plays havoc with a man's sex life by binding to testosterone receptor sites and may contribute to the over-production of SHBG. SHBG binds free testosterone in a way that makes it unavailable to receptor sites in the brain, nerves and genitals."
- Estrogen suppression in males: metabolic effects - J Clin Endocrinol Metab. 2001 Apr;86(4):1836-8 -
"First, a dose-response study of 12 males (mean age, 16.1 +/- 0.3 yr) was conducted, and blood withdrawn at baseline and after 10 days of oral Arimidex given as two different doses (either 0.5 or 1 mg) in random order with a 14-day washout in
between. A sensitive estradiol (E2) assay showed an approximately 50% decrease in E2 concentrations with either of the two doses ... There was a 58% increase in serum T"
-
Male
Hormone Modulation Therapy - Life Extension Magazine, 11/99 -
"One cause of hormone imbalance in men is that their testosterone is
increasingly converted to estrogen. One report showed that estrogen levels
of the average 54-year-old man are higher than those of the average
59-year-old woman . . . . High levels of estrogen have been implicated as a
cause of benign prostatic hypertrophy (BPH)"
- Arimidex - Rxlist.com -
"ARIMIDEX 1 mg, reduced estradiol by approximately 70% within 24 hours and by approximately 80% after 14 days of daily dosing"
General Information:
-
Gynecomastia - American Academy of Family Physicians
- Aromatization - emedicine.com
-
Gynecomastia - familydoctor.org
- Drugs and Medications that cause Gynecomastia - Big Male Breasts - plasticsurgery4u.com
News & Research:
-
Letrozole suppresses plasma estradiol and estrone sulphate more completely
than anastrozole in postmenopausal women with breast cancer - J Clin
Oncol. 2008 Apr 1;26(10):1671-6 - "Letrozole reduces
plasma E2 and E1S levels to a significantly greater extent than anastrozole"
- See
Femara (letrozole) at OffshoreRX.
-
Male Breast Enlargement May Be Common - WebMD, 9/19/07 -
"Underlying the condition is an imbalance of
estrogen and testosterone. When estrogen levels get too high, the breasts
can begin to grow"
-
The red clover (Trifolium pratense) isoflavone biochanin A inhibits
aromatase activity and expression - Br J Nutr. 2007 Aug 29;:1-8 -
"Biochanin A is an isoflavone isolated from red
clover (Trifolium pratense) ... Isoflavones resemble the structure of
oestrogen, and display agonistic and antagonistic interactions with the
oestrogen receptor. Overexposure of oestrogen is a major contributing factor
in the development of breast cancer ... In the present study the effect of
biochanin A on the gene regulation and enzyme activity of aromatase was
investigated. By assaying MCF-7 cells stably transfected with CYP19,
biochanin A inhibited aromatase activity and hampered cell growth
attributing to the enzyme activity" - See
red clover products at iHerb
 .
-
Management of
Gynaecomastia: An Update - Medscape, 8/7/07
-
Elevated Serum Estradiol Ups Stroke Risks - Physician's Weekly, 5/7/07 -
"High levels of serum estradiol may
increase the risk of stroke in elderly men"
-
High
Estrogen Levels Associated With Dementia In Older Men; No Association
Observed With Testosterone - Science Daily, 7/24/06 -
"Levels of bioavailable testosterone
were not associated with risk of cognitive decline and incident dementia,"
they report. "In contrast, higher levels of bioavailable estradiol were
associated with an increased risk for cognitive decline and Alzheimer's
disease." For each standard deviation increase in estradiol level, the risk
for the disease went up by 25 percent" - I take a quarter tablet of
Femara (OffshoreRX.com)
to keep estrogen low. - Ben
-
Drug
Combination May Slow Male Breast Cancer Growth - Science Daily, 7/7/06
- Five
Years on Anastrozole Can Promote Progression to Osteoporosis - Medscape,
6/12/06 - "Women taking
anastrozole also
had about a 40% increased risk of fractures while on the study ... At 5
years, women taking anastrozole lost 6.1% of BMD at the hip and 7.2% at the
spine ... women with a normal BMD at baseline did not develop osteoporosis"
- It's something to think about for men taking anastrozole for
aromatization.
- Shrinking
Male Breasts? - Dr. Weil, 4/12/06
- Declining Estradiol Levels More Predictive of Fracture Risk Than Low Testosterone in Aging Men - Doctor's Guide, 10/8/04 -
"While low levels of free testosterone are a predictor of hip-bone loss, declines in estradiol levels play a stronger role than testosterone"
- New-Onset Depression Linked to Tamoxifen - Doctor's Guide, 5/25/03 -
"Results show a rate of new-onset depression of 17.82% in the
tamoxifen group and 14.34% in the no-tamoxifen group" - It seems like the same might be true for men taking tamoxifen to prevent aromatization.
- Procedure Removes Excess Breast Fat In Men - TheSanDiegoChannel.com, 5/14/03
- Several Options Available for Androgen Replacement Therapy - Doctor's Guide, 4/8/03 -
"Side effects of exogenous androgen therapies are mood
changes, polycythemia, gynecomastia, exacerbation of sleep apnea, and in some patients, acne"
-
I have read that Indole-3-Carbinol (I3C) actually increases
the activity of aromatase enzyme and that DIM does not - Life Extension Magazine, 3/01 -
"In one study, men received I3C for one week; a profile of 13 estrogens was measured. The results were that I3C significantly
increased the urinary excretion of C-2 estrogens. The urinary concentrations of nearly all other estrogen metabolites, including levels of estradiol, estrone, estriol and 16 alpha-hydroxyestrone, were lower after I3C treatment [J Natl Cancer Inst 1997 May 21;89(10):718-23]. On the other hand, studies have shown that
DIM can actually induce aromatase activity with a two-fold increase [Toxicol Sci 2001 May;61(1):40-8]" - The following are the two references for that statement:
- 2,3,7,8-Tetrachlorodibenzo-p-dioxin and Diindolylmethanes Differentially Induce Cytochrome P450 1A1, 1B1, and 19 in H295R Human Adrenocortical Carcinoma Cells - Toxicol Sci 2001 May;61(1):40-8 -
"DIM, but not TCDD, induced aromatase activity with an apparently maximal 2-fold increase at 10 µM; higher concentrations of DIM and many of its analogs were cytotoxic"
- Changes in levels of urinary estrogen metabolites after oral indole-3- carbinol treatment in humans - J Natl Cancer Inst 1997 May 21;89(10):718-23 -
"In both men and women, I3C significantly increased the urinary excretion of C-2 estrogens. The urinary concentrations of nearly all other estrogen metabolites, including levels of estradiol, estrone, estriol, and 16alpha- hydroxyestrone, were lower after I3C treatment"
- So if C-2 estrogens are increased, is that bad in men? I don't know. The following are all I could find:
- Estrogen Metabolism - immunacare.com -
"C-2 metabolites are essentially devoid of peripheral biological activity, as shown in studies on uterine weight, gonadotrophin
secretion, and cell proliferation {1}. 2-Hydroxyestrogen has even been found to exert a modest anti-estrogenic effect {2,3}, and has been called "the good estrogen" {4}. The 16a-hydroxylated metabolites, 16a-hydroxyestrone (16OHE1) and estriol
(E3), are estrogen agonists {5}."
- Effects of Pesticides on the Ratio of 16/2-Hydroxyestrone: A Biologic Marker of Breast Cancer Risk - Environmental Health Perspectives 103, Supplement 7, October 1995 -"Estradiol
metabolism proceeds by hydroxylation at one of two mutually exclusive sites at C-2 and C-16. The catechol pathway yields the weakly estrogenic 2-hydroxyestrone (2-OHE1), which inhibits breast cell
proliferation" - If that means, and I think it does, that the C-2 metabolites inhibit breast cell growth, that would definitely be a good thing for men.
- Estrogen - the Unrecognized Male Hormone - Rick Cohen, MD
- The Cruciferous Choice: DIM or I3C? - Michael A. Zeligs, M.D. -
"It is well documented that estrogen accumulates in the prostate gland starting at age 50 (42) and that estrogen
is associated with the degree of prostate enlargement ... Using DIM in men avoids accelerating testosterone metabolism, especially regarding unwanted conversion of testosterone into estrogen. In the safety study reported (11), I3C and not DIM increased activity of "aromatase" (CYP19), the enzyme responsible for
converting testosterone into estrogen"
- Tamoxifen, Raloxifene Prove Effective In Pre-Pubertal Gynecomastia - Doctor's Guide, 7/12/01
- Anti-Aromatase Agents Cost-Effective For Women With Metastatic Breast Cancer - Doctor's Guide, 5/15/01
- Aromatase Inhibition Does Not Interfere With Serum Lipids In Metastatic Breast Cancer - Doctor's Guide, 5/14/01
- Aromatase Inhibition Corrects Endocrinopathy In Infertile Men - Doctor's Guide, 4/9/01 -
"investigators found that men with severe infertility had significantly lower
testosterone (328 versus 543 ng/dl) and significantly higher oestradiol (58.4 versus 43.5 ng/l) than the fertile controls. As a result, the infertile men had much lower testosterone-to-oestradiol ratios ... These abnormalities were corrected in the 45 men who received testolactone and their testosterone-to-oestradiol
ratios rose into the normal range"
-
Replenish
Testosterone Naturally - Life Extension Magazine, 1/00
- Evidence of a Treatable Endocrinopathy in Infertile Men - J. of Urology, 3/01 - "We identified an endocrinopathy in men with severe male factor
infertility that is characterized by a decreased serum testosterone-to-estradiol ratio. This ratio can be corrected by aromatase inhibition, resulting in a significant improvement in semen parameters in oligospermic patients"
- Femara (Letrozole) Significantly More Effective Than Tamoxifen In Treating Advanced Breast Cancer - Doctor's Guide, 12/7/00
- Diagnosis and Management of Male Breast Enlargement in Patients With HIV/AIDS - Medscape, 12/00
- Aromasin Now Available In US For Advanced Breast Cancer - Doctor's Guide, 1/24/00
-
Should
Aging Men Take Testosterone Drugs? - Life Extension Magazine, 11/99
- Inhibition of aromatase activity by flavonoids - Arch Pharm Res. 1999 Jun;22(3):309-12 -
"Over 50% of the flavonoids significantly inhibited
aromatase activity, with greatest activity being demonstrated with apigenin (IC50: 0.9 microg/mL), chrysin (IC50: 1.1 microg/mL), and hesperetin (IC50: 1.0 microg/mL)"
- I3C/DIM - Recurrent Respiratory Papillomatosis Foundation
- Flavonoid inhibition of aromatase enzyme activity in human preadipocytes - J Steroid Biochem Mol Biol. 1993 Sep;46(3):381-8 -
"Chrysin, the most
potent of the naturally-occurring flavonoids, was similar in potency and effectiveness to AG, a pharmaceutical aromatase inhibitor used clinically in cases of estrogen-dependent carcinoma."
- Inhibition of human estrogen synthetase (aromatase) by flavones - Science. 1984 Sep 7;225(4666):1032-4
- Testolactone (Teslac) - mesomorphosis.com
- Mesterolone (Proviron) - mesomorphosis.com
- Anastrozole (Arimidex) - anabolic-androgenic-steroids.com - "Anastrozole
(Arimidex) is the aromatase inhibitor of choice"
- Anti-estrogens - mesomorphosis.com -
"The most commonly used aromatase inhibitor in bodybuilding is aminoglutethimide (Cytadren)"
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