Aromasin - I don't get it

[cutting_king]

Ok so out of all the AI's there are I've only ever used l-Dex and letro,however i was looking into Aromasin and when reading about it in the profiles section and other places it says its works differently than other AI's because it blocks the aromatase enzyme in a "time dependant and irreversible manner" and this is why its called a suicide aromatase inhibitor. can someone explain what this means? i'm just a bit unsure of what it means by irreversible? don't get me wrong i know what the word irreversible means but i don't get which part of this drugs actions are irreversible and what effect that has. someone like to part some wisdom?

[clements22]

from what i know... Aromasin removes estrogen.. where others just simply block the estrogen receptors... people usually combine Aromasin and nolva because it makes a good pct combo

[shortie]

As I understand it, and I may be wrong, but I believe that Aromasin binds permanently to the aromase enzyme, whereas other AIs merely inhibit the ability of Testosterone to bind with the aromatase enzyme. Once the AI has "degraded" to the point it is absorbed by the body and released the Aromatase enzyme is still there to bind with free Test. Suicide inhibitors bind and never release and only when the body produce more aromatse is it replaced.

[cfiler]

As I understand it, and I may be wrong, but I believe that Aromasin binds permanently to the aromase enzyme, whereas other AIs merely inhibit the ability of Testosterone to bind with the aromatase enzyme. Once the AI has "degraded" to the point it is absorbed by the body and released the Aromatase enzyme is still there to bind with free Test. Suicide inhibitors bind and never release and only when the body produce more aromatse is it replaced.

That's the way I understand it.

[Swifto]

This will clarify:

"To understand why Aromasin may be useful in conjunction with Nolvadex while both Letro and A-dex suffer reduced effectiveness, we’ll need to first understand the differences between a Type-I and Type-II Aromatase Inhibitor. 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."

Anthony Roberts.

[Swifto]

.....Sometimes I'm just going to take credit for these things....

Yep.....I wrote it......

[cutting_king]

Sounds interesting. From peoples experience is there any benefit from the way it works to say l-Dex then? i understand now how they work differently but considering Aromasin costs about $25 more would it be worth it? i'm just playing around with different AI's to get a feel for them thats all

[Random]

Cutting King....i think if you are prone to gyno then it would be worth it...i was actually planning on using aromasin on my future cycles from now on until i was reading on how eliminating estrogen can significantly affect your cholesterol levels..(while nolva can improve them)....still havent found a definitive answer yet but im curious on how much aromasin would affect your cholesterol....