[quote]cycobushmaster wrote:
[quote]Mr. Walkway wrote:
[quote]VTBalla34 wrote:
What are you basing this on?
I have never recommended Aromasin more frequently than EOD, and I have certainly never heard these claims here. It completely wipes out the E2, which doesn’t just grow back out of nowhere.[/quote]
you should certainly recommend aromasin more frequently than EOD. It does not “completely wipe out the E2”.
Suppression of estrogen, via estrogen receptor or aromatase blockade, is being investigated in the treatment of different conditions. Exemestane (Aromasin) is a potent and selective irreversible aromatase inhibitor. To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14�??�?�¢??26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg exemestane daily, orally, for 10 d with a 14-d washout period. Blood was withdrawn before and 24 h after the last dose of each treatment period. A PK study was performed (n = 10) using a 25-mg dose. Exemestane suppressed plasma estradiol comparably with either dose [25 mg, 38% (P �??�?�¢?�??�?�¤ 0.002); 50 mg, 32% (P �??�?�¢?�??�?�¤ 0.008)], with a reciprocal increase in testosterone concentrations (60% and 56%; P �??�?�¢?�??�?�¤ 0.003 for both). Plasma lipids and IGF-I concentrations were unaffected by treatment. The PK properties of the 25-mg dose showed the highest exemestane concentrations 1 h after administration, indicating rapid absorption. The terminal half-life was 8.9 h. Maximal estradiol suppression of 62 �??�??�?�± 14% was observed at 12 h. The drug was well tolerated. In conclusion, exemestane is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.
[quote]cycobushmaster wrote:
according to Pfizer, we’re both wrong, and the half-life is 24 hours.
http://labeling.pfizer.com/ShowLabeling.aspx?id=523[/quote]
that is the study conducted on postmenopausal women with breast cancer.
here is the full study conducted on men if you would like to read it
http://press.endocrine.org/doi/full/10.1210/jc.2003-031279
[quote]cycobushmaster wrote:
[quote]Paul33 wrote:
i thought it bound to estrogen and destroyed it not just suppressed it?[/quote]
it does. as a suicidal AI, it binds irreversibly to estrogen. this means that i removes estrogen without it bouncing back, and before estrogen can rise later, the body still needs to produce the aromatase enzyme to bind to testosterone…[/quote]
it binds irreversibly to aromatase, not estrogen. However, since the male body is constantly producing more aromatase, this is really a moot point. [/quote]
thanks for posting that…
i have to point out this from that study, as well: “Maximal suppression of estradiol (62 Ã??Ã?± 14%) was observed 12 h after a single 25-mg dose of exemestane. Estradiol remained suppressed by 58 Ã??Ã?± 21% at 24 h and returned to baseline 3-6 d after treatment.”
^based off that, i still don’t see how multiple doses are required. [/quote]
indeed, however 21% is a wide margin…
and if i recall correctly, the pharmacokinetics are different in men using large amounts of exogenous testosterone.