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Home > Health Conditions > Breast Cancer > Femara.

Femara (letrozole) - 1/01

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CME:

For Aromatization (in males):

  • Drugs for hair loss and benign prostatic hyperplasia may result in loss of libido, erectile dysfunction in men - Science Daily, 1/11/11 - "5a-reductase inhibitors (5a-RIs), while improving urinary symptoms in patients with benign prostatic hyperplasia (BPH) and possible hair loss prevention, produces significant adverse effects in some individuals including loss of libido, erectile dysfunction (ED), ejaculatory dysfunction and potential depression" - Note:  That goes back and forth.  One study claimed that finasteride improved sex after after six months of taking it.  Regarding gynaecomastia, if you're taking low dose letrozole to increase testosterone and to prevent aromatization it many also help prevent gynaecomastia.
  • Aromatase Inhibition Offers Little Benefit, Possible Harm to Men With Lo... - Medscape, 12/22/09 - "The inescapable conclusion from these data is that the 50% increase in testosterone levels was trumped by the much more modest 20% reduction in estradiol levels, leading to negative skeletal effects of anastrozole therapy in aging men" - Note:  I'm not sure that thought this though thoroughly.  Mortally in men is best when estrogen is around 25pg/mL.  I suspect that most have higher estrogen than that.  See:

    • High, Low Estradiol Levels and Mortality in Men With Systolic HF - Medscape, 5/19/09 - "Both low and high serum levels of estradiol, compared with mid-range levels, are significantly and independently associated with increased all-cause mortality in men with chronic systolic heart failure"
      Serum Estradiol Concentration Quintiles as Predictors of All-Cause Mortality in Men (With Quintile 3 as the Reference Group)
      Parameter Quintile 1 Quintile 2 Quintile 3 Quintile 4 Quintile 5
      Estradiol concentration (pg/mL) <12.903 12.90–21.79 21.80–30.11 30.12–37.39 >37.40
      3-y survival* (%) 44.6 65.8 82.4 79.0 63.6
      Quintile as mortality predictor,* HR (95% CI) vs quintile 3 4.17 (2.33–7.45) 2.15 (1.16–3.99) -- 1.22 (0.64–2.31) 2.33 (1.30–4.18)
      HR= hazard ratio
  • High, Low Estradiol Levels and Mortality in Men With Systolic HF - Medscape, 5/19/09 - "Both low and high serum levels of estradiol, compared with mid-range levels, are significantly and independently associated with increased all-cause mortality in men with chronic systolic heart failure" - Note:  See my aromatization page for ways to reduce it.  I take a quarter tablet of letrozole every day.  See letrozole at OffshoreRX.com.
  • Serum Estradiol Concentration Quintiles as Predictors of All-Cause Mortality in Men (With Quintile 3 as the Reference Group)
    Parameter Quintile 1 Quintile 2 Quintile 3 Quintile 4 Quintile 5
    Estradiol concentration (pg/mL) <12.903 12.90–21.79 21.80–30.11 30.12–37.39 >37.40
    3-y survival* (%) 44.6 65.8 82.4 79.0 63.6
    Quintile as mortality predictor,* HR (95% CI) vs quintile 3 4.17 (2.33–7.45) 2.15 (1.16–3.99) -- 1.22 (0.64–2.31) 2.33 (1.30–4.18)
    HR= hazard ratio
  • Obesity Linked To Hormone Imbalance That Impacts Sexual Quality Of Life - Science Daily, 3/3/09 - "In our study population, we found that lower testosterone levels and diminished ratings for sexual quality of life were correlated with increased BMI ... Subjects who lost weight through bariatric surgery experienced a reduction in estradiol levels, an increase in testosterone levels and an increase in ratings of sexual quality of life" - See my aromatization page
  • Short-term aromatase inhibition: effects on glucose metabolism and serum leptin levels in young and elderly men - Eur J Endocrinol. 2008 Dec 2 - "Ten elderly and nine young healthy men were randomized to receive letrozole 2.5 mg daily or placebo for 28 days in a crossover design. Results: Both in young and elderly men, active treatment significantly increased serum testosterone (+128 and +99%, resp.) and decreased estradiol levels (-41 and -62%, resp.). Fasting glucose and insulin levels decreased in young men after active intervention (-7 and -37%, resp.) compared to placebo. Leptin levels fell markedly in both age groups (-24 and -25%, resp.), while adiponectin levels were not affected by the intervention. Lipid profile was slightly impaired in both groups, with increasing LDL-cholesterol levels (+14%) in the younger age group and 10% lower levels of ApoA1 in the elderly. A decline in IGF-1 levels (-15%) was observed in the younger age group. No changes in weight or BMI were observed in either young or old men" - See letrozole at OffshoreRX.com.
  • 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 .
  • 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 .
  • Comparative assessment in young and elderly men of the gonadotropin response to aromatase inhibition - J Clin Endocrinol Metab. 2005 Oct;90(10):5717-22 - "As assessed after 28 d of treatment, letrozole lowered E2 by 46% in the young men (P = 0.002) and 62% in the elderly men (P < 0.001). In both age groups, letrozole, but not placebo, significantly increased LH levels (339 and 323% in the young and the elderly, respectively) and T (146 and 99%, respectively) (P value of young vs. elderly was not significant). Under letrozole, peak LH response to GnRH was 152 and 52% increase from baseline in young and older men, respectively"
  • 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.  See Femara at International Anti-aging Systems or Letrozole 2.5mg (Generic Equivalent of Femara 2.5mg ), at OffshoreRx.com.
  • Influence of letrozole and anastrozole on total body aromatization and plasma estrogen levels in postmenopausal breast cancer patients evaluated in a randomized, cross-over study - J Clin Oncol. 2002 Feb 1;20(3):751-7 - "estrone (E(1)), estradiol (E(2)), and estrone sulfate (E(1)S) ... Treatment with anastrozole suppressed plasma levels of E(1), E(2), and E(1)S by a mean of 81.0%, 84.9%, and 93.5%, respectively, whereas treatment with letrozole caused a corresponding decrease of 84.3%, 87.8% and 98.0%, respectively. The suppression of E(1) and E(1)S was found to be significantly better during treatment with letrozole compared with anastrozole"
  • Open dose-finding study of a new potent and selective nonsteroidal aromatase inhibitor, CGS 20 267, in healthy male subjects - J Clin Endocrinol Metab. 1993 Aug;77(2):319-23 - "A reduction in estradiol levels by about 30% from baseline was observed at the lowest dose (0.02 mg)" - CGS 20 267 is Letrozole.
  • Letrozole-Femara - isteroids.com - "Letrozole is probably the most powerful Aromatase Inhibitor used by athletes today"
  • Femara (Letrozole) clinical pharmacology - RxList.com - "Letrozole's terminal elimination half-life is about 2 days and steady-state plasma concentration after daily 2.5 mg dosing is reached in 2-6 weeks"

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