does aromasin render aromatase dead forever?

[Simon1972]

hi guys have a read of this...maybe im not reading it right - need someone take on what they are saying here...

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 typeII 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 normalsubstrates (essentially androgens), allowing them to compete with the substrate for accessto the binding site on the aromatase enzyme. After this binding, thenext step is where things differ greatly for the two different types of AI’s. In the case of a type-I AI, the noncompetitive inhibitorwill bind, and the enzyme initiates a sequence of hydroxylation; this hydroxylation produces an unbreakable covalent bond betweenthe 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 enzymesite, and one of two things can happen: 1.) either no enzyme activity is triggered or 2.) the enzyme is somehow triggered withouteffect. The type II inhibitor can now actually disassociate from the binding site, eventually allowing renewed competition between the inhibitor and the substratefor binding to the site. This means that the effectiveness of competitive aromatase inhibitors depends on the relative concentrations and affinitiesof 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 (11).

are they saying using aromasin, kills the aromatse process effectively permanently? so it can be used temporarily with permanant results - effectively lowering E2 levels.

[HRTstudent]

if by permanent it would most certainly mean the life cycle of that enzyme, not the body's ability to make the aromatase enzyme in general. there are quite a few types of aromatase inhibitors - competitive, non competitive, suicidal, etc etc etc. probably more complicated than those of us on trt need to bog ourselves down with. what matters most is quality of life and then how our bodies react (blood work!).

so, it's not like you can take some aromasin once and never need an AI again.

[zaggahamma]

interesting thread...never came up before

[kelkel]

No, we make more. I have an article on it somewhere. If I can find it I'll add it here.

[Simon1972]

ahh so, aromasin kills the aromatase enzyme currently residing in the body- so my question would be by taking aromasin, are we now speeding up the production of enzymes to make up for the lack of enzymes in the body? or does the body simply replenish enzymes naturally at a steady rate anyway?
if enzymes do eventually replenish , im assuming the enzyme levels would max out at the pre-existing level prior to treatment. this also raises the question of why use either clomid or nolva if aromasin is better in regards to gyno flaring up.

[HRTstudent]

nolva specifically is used for gyno because it targets the breast tissue far more than these other drugs, and it COMPETES with estrogen already in the body. it is not an anti-aromatase actually, but a selective estrogen receptor modulator.

[kelkel]

Aromasin is Swifto's drug of choice in this arena.

[Simon1972]

Aromasin is 3rd gen and nov is 1st gen? ( or is it 2nd) in what way could tamoxifen be in any way better? aromasin seems to have all the competition beat.

considering yu dont need to taper off whennearing completion- you also dont suffer estrogen rebound on cessation.

[Optima25]

What about decreased IGF-1 levels when using aromasin?

[Simon1972]

What about decreased IGF-1 levels when using aromasin?

i didnt think it lowered igf- i think it increases it if anything? i might be wrong but if igf and igf1 is the same thing...then i read it increases it.

arimidex lowers igf-1 are you confusing arimidex for aromasin?


Arimidex decreases IGF-1 levels by around 18%

Femara icreases IGF-1 levels by 24%...

Aromasin is that it decreases IGF-1 levels by about 23-24%

[Babyslim]

So why not use Letro instead of Arimidex(the most popular AI here) since it has such a positive effect on IGF1 levels? Plus Arimidex seems more expensive than Letro as well, but thats another story.

[HRTstudent]

So why not use Letro instead of Arimidex(the most popular AI here) since it has such a positive effect on IGF1 levels? Plus Arimidex seems more expensive than Letro as well, but thats another story.

letrozole can have a very profound, and negative effect on libido for many (if not most) men.

[Simon1972]

So why not use Letro instead of Arimidex(the most popular AI here) since it has such a positive effect on IGF1 levels? Plus Arimidex seems more expensive than Letro as well, but thats another story.

aromasin has no effect on IGF-1 either- its reccomended because of that- this study proves it.


Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males

Nelly Mauras, John Lima, Deval Patel, Annie Rini, Enrico di Salle, Ambrose Kwok and Barbara Lippe

Nemours Children’s Clinic and Research Programs (N.M., J.L., A.R.), Jacksonville, Florida 32207; and University of Florida Health Sciences Center (D.P.) and Amersham Pharmacia Biotech (E.d.S., A.K., B.L.), Peapack, New Jersey 07977


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.


Abbreviations: AUC, Area under the curve; CBC, cell blood count; HDL, high density lipoprotein; LDL, low density lipoprotein; PK, pharmacokinetic.

[HRTstudent]

so this begs the question, is your guys insurance covering aromasin?

[HRTstudent]

And does anyone have any studies looking at the use of aromasin/exemestane in males for 1 year or more?

[Simon1972]

so this begs the question, is your guys insurance covering aromasin?

im not taking any medication t the moment- just taking an interest in it as it answers alot of the symptoms without sides that most on this board keep asking for- i thought maybe i was missing something when everyone talks clomid and nolvadex and never mentions aromasim. seems like old habits die hard and sometimes inspite of body builders being decades ahead of medical , we too can fall into the same trap of "thats the way its always been"

[HRTstudent]

Most people take clomid and nolvadex for totally different reasons than they would take aromasin for though.

[EZ E]

If one were to use aromasin instead of instead of adex for TRT, what would be a good dosage? As an example, I take .5mg of adex 2x/week for TRT.

Thanks.

[Simon1972]

If one were to use aromasin instead of instead of adex for TRT, what would be a good dosage? As an example, I take .5mg of adex 2x/week for TRT.

Thanks.

the study says 25mg each day, but that was done over a few weeks,

probably safer to lower the dose to 12.5mg over 2 months.
i read somewhere a guy was taking 25mg for over 4 months no issues, Wish swifto would chime in here!

Aromasin? (exemestane) is the best, this is why, both Arimidex?/LiquidDex (anastrozole) and Femara? (letrozole) hurt your cholesterol. the way these two anti-estrogens work is they inhibit the aromatase enzyme. By inhibiting the enzyme which converts testosterone to estrogen, you reduce or even come close to eliminating estrogen production. we need some estrogen to be healthy. The major drawback to this is without estrogen, your lipid profile gets ****ed.

Exemestane works differently. it does not stop the body from producing estrogen, rather, it makes it so the estrogen is unable to bind to receptors by deactivating the binding enzyme. If the estrogen cannot bind, you simply will not get bloated or get gynocomastia. The estrogen is crippled due to Exemestane. However, since the estrogen is still floating around, it will not negatively affect your lipid/cholesterol profile.

Exemestane is a steroidal suicide aromatase inhibitor. It isvery similar in structure and action to formestane, although it is significantly more potent in comparison. As a class of drugs, aromatase inhibitors offer an anti estrogenic effect by blocking the enzyme responsible for synthesizing estrogens. Exemestane is approved by the FDA for the treatment of breast cancer in women, specifically in post menopausal patients whose cancer has progressed following therapy with tamoxifen (nolvadex). Male bodybuilders and athletes often use the drug for non approved purposes, namely to counter the estrogenic side effects associated with the use of aromatizable anabolic/androgenic steroids. This may include gynecomastia, fat buildup, and water retention. Exemestane is one of the most potent aromatase inhibitors presently available. The most commonly cited date reports a lowering of estrogen around 85% on average in clinical studies with women. Exemestane was developed by Pharmacia & Upjohn, which gained FDA approval for sale of the drug in late 1999. They introduced it under the Aromasin brand name in early 2000. Although the drug proved to be effective in doses as low as 2.5mg per day in some patients, the company developed it in a standard and near universally effective dosage of 25mg per tablet. The company has since introduced the drug to many other nations under the same trade name of Aromasin.

Aromasin, as it is most commonly called, is a very potent AI which works by blocking the aromatase enzyme in the body. This drug was originally developed to help fight breast cancer in women by reducing estrogen which some believe to aid in cancer cell growth. While not quite as strong as Letrozole, aromasin is considerably stronger than Anastrozole. Studies done with this substance typically show around an 85% reduction in estrogen levels in the body. This can be very useful to bodybuilders who are using aromatizing compounds such as testosterone. Typically, one will begin the use of aromasin the same day they begin their cycle. It is also important to note that Aromasin has shown to be very effective at increasing testosterone and IGF levels in the body. Because of this, this drug is also very useful during PCT regime when one is trying to restore natural testosterone levels in order to avoid a post cycle "crash". It is important to keep doses of aromasin reasonable, as too much estrogen suppression can result in hindered muscle gains and loss of sex drive. One 25mg tablet a day should be sufficient for effectively keeping estrogen related sides out of the picture, or for effectively raising natural testosterone levels during PCT.

Exemestane reaches peak plasma concentrations within 2 hours following the oral administration of a 25 mg dose. The active life of the drug is between 24 and 30 hours. This is significant since it is quite shorter than for the non-steroidal inhibitors. A single oral dose of 25 milligrams of exemestane causes a relatively long-lasting reduction in plasma and urinary estrogen levels, with maximal suppression occurring approximately 2 to 3 days after dosing and persists for about 4 to 5 days.It has been shown that 25 milligrams of exemestane is basically just as effective as 50 milligrams at suppressing estrogen, raising testosterone levels, and levels of IGF. It is therefore unnecessary to go higher in doses than 25 milligrams per day. Due to the active life of the compound exemestane should be administered roughly once every twenty-four hours. Users often start the drug on the first or second week of steroid use and continue to take it throughout the cycle and for a few weeks afterwards in order to prevent any type of estrogen rebound.

***Info from www.DrugsProfiles.com

[j2048b]

I have used aro since i began trt this past august, never did well with adex and refused to even try it again, found out about aro and it has been awesome! But eaxh person is different, i know a guy who used aro and after a while noticed when taking it in the am, by that night hos e2 was creeping high again, did bw to rationalize his feeling of high e2and was spot on, got to the point where he had to switch to letro,

For me i was on aro at a 1/2 pill every three days for the first couple weeks of trt and WHAM! Crashed my e2!! Joints hurt like hell, headaches (also a side of hcg usage) So low that i had to drop it for a few weeks untill i felt all bitchy again from no ai and creeping e2, so i had to switch it up and at the time pinning 200 mlg every monday of cyp, hcg on tuesdays at 500iu, and wed 1 whole aro at like 20-25 mlg if i remember correctly and felt awesome! Thats how i had to run it until about fedruary when i had to quit trt cold turkey!! Due to high bp and cholesterol at a whopping 309!!

Now with that being said would the aro at all conflict with cholesterol?

[HRTstudent]

If one were to use aromasin instead of instead of adex for TRT, what would be a good dosage? As an example, I take .5mg of adex 2x/week for TRT.

Thanks.

dosing an AI is very tricky and needs to be individualized... again I say it often but many, if not most, men do not need any AI on trt.

if you're on 1mg of anastrozole per week, that's a fairly decent dose. i really don't know enough about the pharmacokinetics of aromasin to give you a recommendation, but I would say start out small and move up unless you are very gyno sensitive.