Thread: Here's some Anti-e information
05-19-2002, 01:11 PM #1
Here's some information an Femara an other anti-e's
I'm trying to decide what anti-e to use and here's some of what I found. I hope this can help others also.
Drug and hormone interactions of aromatase inhibitors
The clinical development of aromatase inhibitors has been largely confined to postmenopausal breast cancer patients and strongly guided by pharmacological data. Comparative oestrogen suppression has been helpful in circumstances where at least one of the comparitors has caused substantially non-maximal aromatase inhibition. However, the triazole inhibitors, letrozole and anastrozole, and the steroidal inhibitor, exemestane, all cause >95% inhibition. Comparisons between these drugs therefore require more sensitive approaches such as the direct measurement of enzyme activity by isotopic means. None of these 3 agents have significant effects on other endocrine pathways at their clinically applied doses. Pharmacokinetic analyses of the combination of tamoxifen and letrozole have revealed that these drugs interact resulting in letrozole concentrations c. 35 to 40% lower than when letrozole is used alone.
Aromatase inhibitors in men
The effect of aromatase inhibition on male gonadotrophin and sex steroid concentrations is illustrated in the paper by Trunet et al. (1993): 2.5 mg letrozole suppressed plasma oestradiol concentrations to less than 50% of pretreatment after 2 days, with recovery to approximately pretreatment values after 6 days. These decreases were accompanied by increased gonadotrophin concentrations, with resultant increases of approximately 50% in plasma testosterone . These results, and those previously published (Bhatnagar et al. 1992) on the effects of fadrozole in men, indicate that the aromatization pathway is of major importance in the regulation of gonodotrophin secretion by aromatically androgens.
Full text of this article can be downloaded in PDF format.
Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
The androstenedione derivative, exemestane (FCE 24304), is a new orally active irreversible aromatase inhibitor. Fifty-six post-menopausal advanced breast cancer patients entered this study to evaluate the activity of four low exemestane doses in reducing oestrogen levels. The drug's tolerability and clinical efficacy were also assessed. Exemestane was orally administered to four consecutive groups at daily doses of 25, 12.5, 5 and 2.5 mg, and the changes in oestrogen, gonadotrophins, sex-hormone binding globulin and dehydroepiandrosterone sulphate levels were evaluated. Drug selectivity was studied by measuring 17-hydroxycorticosteroid urinary levels. After 7 days of treatment, mean oestrone and oestradiol levels had decreased by respectively 64% and 65% (a decrease which was maintained over time); in the 2.5 mg group, oestrone sulphate levels also decreased by 74%. Gonadotrophin levels were significantly higher, whereas no changes in the other serum hormone levels or any interference with adrenal synthesis were detected. Treatment tolerability was satisfactory: nausea and dyspepsia were reported in 16% of patients. The overall objective response rate was 18%. In conclusion, exemestane is effective in reducing oestrogen levels at all of the tested doses and shows interesting clinical activity.
Aromatase inhibitors: a dose response effect?
Aminoglutethimide, the first aromatase inhibitor, was established in the 1970s as an active treatment for patients with advanced breast cancer, but its lack of specificity was associated with side effects. Since that time, a series of much more specific non-steroidal aromatase inhibitors have been developed which are up to 10 000 times as potent as aminoglutethimide in vivo with no evidence of inhibition of other steroid pathways at doses required to inhibit oestrogen. Two of these, letrozole (Femara; Novartis) and anastrozole (Arimidex ; Zeneca) are now well established in the treatment of advanced breast cancer and are under investigation as adjuvant therapy. These agents achieve 98-99% aromatase inhibition in patients, and reduce serum levels of oestrone and oestradiol beyond the limit of detection in many patients (Iveson et al. 1993). Until recently, it had been assumed that no clinical dose response effect could exist beyond levels of maximum serum oestrogen suppression but recent data have suggested this may not be the case. If a dose response effect does indeed exist for modern aromatase inhibitors, then it has important implications for their future development.
Full text of this article can be downloaded in PDF format. At http://journals.endocrinology.org/er...erc0060245.pdf
Hope this helps.
Last edited by JohnnyB; 01-22-2003 at 09:18 AM.
05-19-2002, 01:31 PM #2
nice post brother.
05-20-2002, 04:42 AM #3
05-21-2002, 11:20 AM #4
01-22-2003, 09:17 AM #5
Re: Here's some information an Femara an other anti-e's
Here's a study comparing Femara to Clomid.
A randomized double-blind comparison of the effects of clomiphene citrate and the aromatase inhibitor letrozole on ovulatory function in normal women.
Fisher SA, Reid RL, Van Vugt DA, Casper RF.
Division of Reproductive Endocrinology and Infertility, Department of Obstetrics and Gynecology, Queen's University, Kingston General Hospital, Ontario, Canada.
OBJECTIVE: To evaluate the ovarian follicular dynamics of cycle modification with the aromatase inhibitor letrozole compared with clomiphene citrate in normal ovulatory women.
DESIGN: Randomized double-blind controlled trial.
SETTING: Tertiary care hospital.
PATIENT(S): Nineteen ovulatory female volunteers, ages 18-35 years.
INTERVENTION(S): Subjects were monitored in one control cycle. Subjects then received either letrozole 2.5 mg daily or clomiphene citrate 50 mg daily on days 5-9 after menses.
MAIN OUTCOME MEASURE(S): Number of mature follicles, endometrial thickness and endometrial pattern at ovulation, and follicular profiles of LH, FSH, and E(2).
RESULT(S): The number of mature follicles at the LH surge in natural cycles was 1.0 with an exaggerated response seen for treatment both with clomiphene and letrozole. There was no difference in the endometrial thickness at midcycle during either the natural cycles or the medicated cycles. LH surges and spontaneous ovulation were documented in all natural and medicated cycles. When measured daily, follicular profiles of LH and FSH are similar between the groups in both the natural and medicated cycles. In the medicated cycles, clomiphene results in a significant increase in E(2) levels, while E(2) levels in letrozole-stimulated cycles appeared lower than in natural cycles.
CONCLUSION(S): Transient inhibition of aromatase activity in the early follicular phase with the aromatase inhibitor letrozole results in stimulation of ovarian folliculogenesis similar to that seen with clomiphene citrate with no apparent adverse effect on endometrial thickness or pattern at midcycle.
Last edited by JohnnyB; 01-22-2003 at 09:20 AM.
01-22-2003, 09:21 AM #6
Femara and test.
The role of sex steroids in the regulation of insulin sensitivity and serum lipid concentrations during male puberty: a prospective study with a P450-aromatase inhibitor.
Wickman S, Saukkonen T, Dunkel L.
Hospital for Children and Adolescents, University of Helsinki, PL281, FIN-00029 HUS, Helsinki, Finland. firstname.lastname@example.org
OBJECTIVE: Our purpose was to study the sex steroid -mediated changes in serum insulin and lipid concentrations in boys during puberty.
DESIGN AND METHODS: We treated boys with constitutional delay of puberty either with testosterone plus placebo or with testosterone plus an aromatase inhibitor, letrozole , which inhibits the conversion of androgens to oestrogens. We demonstrated previously that during treatment with testosterone plus letrozole the increase in testosterone concentration was more than 5-fold higher than during treatment with testosterone plus placebo. The concentrations of 17beta-oestradiol, IGF-I and IGF-binding protein-3 increased during testosterone-plus-placebo treatment, but during testosterone-plus-letrozole treatment the concentrations remained unchanged. These divergent changes in the two groups enabled us to study the effects of sex steroids and GH on insulin sensitivity and lipid concentrations.
RESULTS: The insulin concentration in the testosterone-plus-placebo-treated group did not change. In contrast, in the testosterone-plus-letrozole-treated group, the concentration decreased during letrozole treatment, indicating improved insulin sensitivity. Changes in insulin and IGF-I concentrations within 12 and 18 months were correlated. In the testosterone-plus-placebo-treated group, the high-density lipoprotein cholesterol concentration did not change but in the testosterone-plus-letrozole-treated group the concentration decreased. The concentrations of low-density lipoprotein cholesterol (LDL-cholesterol) and triglycerides did not change in either of the groups.
CONCLUSIONS: The findings indicate that androgens do not directly alter insulin sensitivity in boys during puberty. In contrast, the observations suggest tight regulation of glucose--insulin homeostasis by GH in boys at this stage. Furthermore, our findings indicate that sex steroids do not significantly participate in the regulation of serum concentrations of LDL-cholesterol or triglycerides in boys during early and mid-puberty.
01-22-2003, 02:27 PM #7
Thanks for the post JB...I've been trying to find more info on this.
01-22-2003, 02:56 PM #8
The one question that I havent been able to find an answer to is wether clomid has any side effects. Meds for cancer patients doesnt have a nice ring to it. If I do 5-6 cycles then that means that Ill have done ballpark @1800mg X 6. You get what I mean?
If somenone has testicular canceer or prostate cancer they dont really have a lot of options so they're not really worried as far as sides go.
These are the reasons clomid is taken in men correct?
And nolvadex , what are the sides of that? And if there are any do they come from prolonged use or from high dosages?
01-22-2003, 03:12 PM #9
great post bro...Madmax..
01-22-2003, 03:39 PM #10
Clomid is used for fertility also. When my Dr. gave me my scrip for test he asked if I was trying to have children. If I would have answered yes, he was going to give me clomid also. Hope that helps.
01-22-2003, 03:45 PM #11
Nice post bro
03-26-2003, 10:48 PM #12
its been a while but i searched for a while to find this so lets bump it again for everyone else to see..... also I think that we should put Femara in the drug profiles...
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