posted Sun, 03/03/2013 - 23:33
3032
+ 2 Exemestane irreversibility
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Hey bro's,
ordered exemestane 2 weeks ago and can't wait. But there's is still something i don't get here...
Well, Wikipedia says exemestane is an irreversible, steroidal aromatase inactivator. Ok, how can it be irreversible? Does it mean it blocks my aromatase enzyme forever? Can't be, why would i have to take more than one or two, right? Does it block a little of the aromatase forever or what?
Need some advice 
thanks
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Just to let everyone know, just because Aromasin permanently binds to aromatase enzymes, DOES NOT MEAN your body will permanently have less aromatase enzymes.
When aromasin is used YOUR BODY SYNTHESIZES MORE AROMATASE ENZYMES.
This is why I prefer arimidex over aromasin.
means once its bound to the estrogen it shuts it off forever but once the drug clears your system you need more to continue to blocking effects of aromasin
opposed to arimidex which only temporary turns off the receptors and shuts off aromatase
Again another incorrect statement.
Arimidex does not "turn off receptors"
adex is an aromatase inhibitor. Aromatase enzyme is NOT an estrogen receptor. Nolvadex binds to the estrogen receptor not arimidex.
Adex temporarily binds to aromatase enzymes and gets cleaved off even during it's use this prevents the extra aromatase enzyme synthesis. However each dose adds new drug to be bound as the other previously bound arimidex begins to be cleaved off of the enzyme.
Wrong. Aromasin continues to lower estrogen even after its half life. However it varies between individuals. For one person it could take a week for new aromatase enzymes to be synthesized, for another person it can be daily.
This is one reason I do not like aromasin, because it is too variable in individuals. Arimidex is the tried and true AI that always does what it is supposed to do. You should never need to change your dose once you find a good dose for adex because it will always prevent the same amount of estrogen from being formed at the aromatase
Some people react horribly to aromasin and can never get dosing and estrogen right. Its short half life doesn't help especially since its usually in 12.5 or 25mg doses. Which is WAY too high for most people. Only very sensitive individuals should use the higher doses.
This information is completely incorrect.
just to clarify, arimidex doesn't function at the receptors. only binds to the enzyme. and you're right: adex's bond is only temporary.
yes mateo you are right. adex temporarily binds to the ENZYME
it means that when it binds to the enzyme that synthesizes e2, that bond is not reversible - it remains bound permanently. other ai's like letro and ardex do not have this characteristic. they work great from inhibiting conversion, but the bonds are broken when the drug wheres off, which releases the enzyme to begin doing its thing again. depending on the circumstances, this can cause e2 rebound
.
adding to this is:
exemestane is able to do this during the active life of the drug. when the drug where's off, it's no longer contributing. thus, the reason for multiple doses. the half life is roughly 27hrs.
the reason for multiple doses is because its active life is 26 hours and we like stability, plus its easier to dose once daily.
Aromasin exerts it's estrogen lowering properties even after its half life. Because it takes time for more aromatase enzymes to be synthesized. This is why people sometimes dose aromasin every other day
Great info +1
thanks bro
Thanks a lot! Can't thumb up, dunno why :S
wont be able to until you have over 5 karma. great post though, i had that same question. +1 that should help
actually, it's 50+, bro... but, karma points mean little to me for the most part. just here to learn, be able to have access to good src's, and hopefully pitch in from time to time. pretty much just a silent member for the most part.
Old non-functional aromatase is destroyed; new aromatase is made in its place.
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