Fwiw
I had bookmarked this - FWIW
TESTOSTERONE NATION | SERM and AI Sticky - Page 1
"Arimidex: A-dex, seems to be the aromatase inhibitor of choice. Usually doesed from 0.25 - 3.0 mg it is effective even when not used every day. 0.5mgs per day can get rid of up to 50% estrogen.
Aromasin: Aromasin is usally doesed from 20-50 mgs per day. It can raise blood testosterone by 60%, and also help out your free to bound testosterone ratio by lowering levels of Sex Hormone Binding Globulin (SHBG), by about 20%! It can suppress estrogen by 65-80%. It's a third generation Aromatase Inhibitor just like A-dex and Letro, but unlike these A-dex and Letro, it is a Type I inhibitor. Whats the difference in a Type I and II inhibitor? Well, Type I inhibitors (like Aromasin) are actually steroidal compounds, while type II inhibitors (like Letro and A-dex) are non-steroidal drugs.
Hence, androgenic side effects are very possible with Type-I AIs, and they should probably be avoided by women. Of course, there are some similarities between the two types of AIs�?�both type I & type II AIs mimic normal substrates (essentially androgens), allowing them to compete with the substrate for access to the binding site on the aromatase enzyme. After this binding, the next step is where things differ greatly for the two different types of AI's.
In the case of a type-I AI, the noncompetitive inhibitor will bind, and the enzyme initiates a sequence of hydroxylation; this hydroxylation produces an unbreakable covalent bond between the inhibitor and the enzyme protein. Now, enzyme activity is permanently blocked; even if all unattached inhibitor is removed. Aromatase enzyme activity can only be restored by new enzyme synthesis.
Now, on the other hand, competitive inhibitors, called type II AI's, reversibly bind to the active enzyme site, and one of two things can happen: 1.) either no enzyme activity is triggered or 2.) the enzyme is somehow triggered without effect. The type II inhibitor can now actually disassociate from the binding site, eventually allowing renewed competition between the inhibitor and the substrate for binding to the site. This means that the effectiveness of competitive aromatase inhibitors depends on the relative concentrations and affinities of both the inhibitor and the substrate, while this is not so for noncompetitive inhibitors.
Aromasin is a type-I inhibitor, meaning that once it has done its job, and deactivated the aromatase enzyme, we don�??t need it anymore. Letrozole and Arimidex actually need to remain present to continue their effects. This is possibly why Nolvadex does not alter the pharmacokinetics of Aromasin. "