Can anyone explain (interpret) this about aromasin (exemesane)?

[Heavy_Duty]

Here is the link to the article.....it's the third topic down.....and read near the very end of the article..........here is the link to the entire article which I've posted elsewhere....exemesane is the real name for aromasin....supposedly the "best of the best" when it comes to Anti-E's...........could someone please interpret this.

http://freakymuscle.com/cgi-bin/ikonboard/ikonboard.cgi?act=ST;f=20;t=47

Pharmacodynamics

Effect on Estrogens: Multiple doses of exemestane ranging from 0.5 to 600 mg/day were administered to postmenopausal women with advanced breast cancer. Plasma estrogen (estradiol, estrone, and estrone sulfate) suppression was seen starting at a 5-mg daily dose of exemestane, with a maximum suppression of at least 85% to 95% achieved at a 25-mg dose. Exemestane 25 mg daily reduced whole body aromatization (as measured by injecting radiolabeled androstenedione) by 98% in postmenopausal women with breast cancer. After a single dose of exemestane 25 mg, the maximal suppression of circulating estrogens occurred 2 to 3 days after dosing and persisted for 4 to 5 days.

Effect on Corticosteroids: In multiple-dose trials of doses up to 200 mg daily, exemestane selectivity was assessed by examining its effect on adrenal @#%$. Exemestane did not affect cortisol or aldosterone secretion at baseline or in response to ACTH at any dose. Thus, no glucocorticoid or mineralocorticoid replacement therapy is necessary with exemestane treatment.

Other Endocrine Effects: Exemestane does not bind significantly to steroidal receptors, except for a slight affinity for the androgen receptor (0.28% relative to dihydrotestosterone). The binding affinity of its 17-dihydrometabolite for the androgen receptor, however, is 100-times that of the parent compound. Daily doses of exemestane up to 25 mg had no significant effect on circulating levels of testosterone, androstenedione, dehydroepiandrosterone sulfate, or 17-hydroxy-progesterone. Increases in testosterone and androstenedione levels have been observed at daily doses of 200 mg or more. A dose- dependent decrease in sex hormone binding globulin (SHBG) has been observed with daily exemestane doses of 2.5 mg or higher. Slight, nondose-dependent increases in serum lutenizing hormone (LH) and follicle-stimulating hormone (FSH) levels have been observed even at low doses as a consequence of feedback at the pituitary level.

[superchicken]

well i dont know what specifically you want us to interpret, that would be a few pages of writing.

ill assume your asking about the last paragraph.

exemestane does bind and occupy the androgen receptor, however it is very wek in that respect, meaning dont even bother mentioning it cause it aint significant. they showed this by giving people 25mg exem daily and it did not sig increase free test, if it was keeping test from binding, free test would be higher since it wouldnt be binding to the androgen receptor, and would therefore be free floating inactive test. THIS IS GOOD

shbg levels decreased starting at a dose of 2.5mg daily and this effect increased(meaning less and less shbg) as the exem dose was raised. THIS IS GOOD.

the increase in lh and fsh were a result of lowered estrogen. lower the estro level in the body, and the pitutiary thinks not enough test is in the body, so it increases lh and fsh so the gonads will make more test(lh and fsh is how it communicates to the gonads to tell them how much test to make) this is why we take anti e's post cycle, to keep estrogen from binding to the pituitary, tricking it into thinking theres no test, so it pumps the lh out raising our test levels. yes you can use an anti e such as clomid or nolva, which bind to the hpta, or an anti aromatose, which just plain stop the conversion of test to estro. THIS IS EXPECTED, ITS NORMAL. NOT REALLY GOOD OR BAD, IT JUST AN EFFECT.

the reason the increase in test and lh was not sig from exem dosing, was because i assume these were not post cycle bodybuilders lol, they were reg males with reg test levels, so your body can only make so much test on its own via lowering estrogen.

however, i have seen studies showing ldex at 1mg ed and also clomid both raised NATURAL test levels up to 50% over baseline. many variables on that so results will vary.

if you werent asking about the last paragraph, well i hate you. cause i spent alot of time posting this lol

[bigjim33]

Originally posted by superchicken
if you werent asking about the last paragraph, well i hate you. cause i spent alot of time posting this lol

hahaha.....if he wasn't asking about it, it is cool cuz that was a good reply

[Heavy_Duty]

Actually, that last paragraph isn't what I wanted answered...that part doesn't really interest me at all..................................




ah you guys......i just thought it would make more sense to put in the entire article even though the last paragraph is the one that i was questioning about and thanks for your answer SuperChicken....I think you need your chickes b goking again under your posts! Get to it!

[Billy_Bathgate]

Effect on Estrogens: Multiple doses of exemestane ranging from 0.5 to 600 mg/day were administered to postmenopausal women with advanced breast cancer. Plasma estrogen (estradiol, estrone, and estrone sulfate) suppression was seen starting at a 5-mg daily dose of exemestane, with a maximum suppression of at least 85% to 95% achieved at a 25-mg dose. Exemestane 25 mg daily reduced whole body aromatization (as measured by injecting radiolabeled androstenedione) by 98% in postmenopausal women with breast cancer. After a single dose of exemestane 25 mg, the maximal suppression of circulating estrogens occurred 2 to 3 days after dosing and persisted for 4 to 5 days

Some studies with Ari, and Fem..only about 50-60% suppression in aromatation has been noted. Here we see an 85%-95%. This is very important. In my opioninon, That makes 25mg Aromasin = 2mg ARimidex or = 5mg Femera. Iw worked all throughout the body, not specifically targeted like Nolva is in mammary tissue. It takes about 2-3 days to kick in, and the effects are noted 4-5 days later, making it active for about 2 days off a single dose.

Effect on Corticosteroids: In multiple-dose trials of doses up to 200 mg daily, exemestane selectivity was assessed by examining its effect on adrenal @#%$. Exemestane did not affect cortisol or aldosterone secretion at baseline or in response to ACTH at any dose. Thus, no glucocorticoid or mineralocorticoid replacement therapy is necessary with exemestane treatment.

as it said, it didnt affect them. One type are known as mineralcorticols. They basically regulate the salt and water balance in the body as long with other minerals. WE dont want that to be all distrurbed or may have to supplement, which it also states is not nessicary. Too low of levels can also lead to joint pain (sometimes present with tren because of this reason).


My man superchicken has the 3rd part covered