Thread: AIs and lipids

Originally Posted by theCaptn'

Do all AIs mess with lipids or just Adex?

I believe that one of the main advantages of Aromasin is less sides, including lipids, and the major negative being price. Adex helps me with bloat during cycle, but I like Aromasin during PCT. Letro is hard on your lipid profile also.

Originally Posted by MDR

I believe that one of the main advantages of Aromasin is less sides, including lipids, and the major negative being price. Adex helps me with bloat during cycle, but I like Aromasin during PCT. Letro is hard on your lipid profile also.

Aromasin is cheap as a research chem . . I might revert back to Aromasin then swap in either Adex or Letro when my test dosage hits the high range.

GYCH!

Originally Posted by theCaptn'

Aromasin is cheap as a research chem . . I might revert back to Aromasin then swap in either Adex or Letro when my test dosage hits the high range.

GYCH!

I usually have trouble finding Aromasin as cheap as Adex, but I think all-around it is the better product. Stronger, with less sides. Adex helps me more with bloat, but that is the only real benefit over Aromasin I can think of offhand. I don't care for Letro too much unless I'm running a very heavy cycle, because it is so strong. Just my personal preferences, for whatever they're worth. Good luck.

thanks MDR . . I hear Aromasin is a lot weaker . . IDK

You really should get some bloods done to see what they're doing. On just a TRT dose I use 0.5 mg letro every 3rd day and my estradiol is mid to low normal. Everyone is a lkittle different. Easy to overdue it with letro though. I took to much when first using it and it killed my gains.

Originally Posted by theCaptn'

thanks MDR . . I hear Aromasin is a lot weaker . . IDK

Interesting-I think it is Letro-Aromasin-Adex as far as order of strength, but I find that Adex is useful for bloat. Not much experience with Letro 'cause it is so strong. Overall, I do think that Aromasin is the "best" of the three as far as overall effectiveness.

I find Aromasin to be the same price as Adex.
From what i hear Aromasin is stronger than Adex

Originally Posted by theCaptn'

thanks MDR . . I hear Aromasin is a lot weaker . . IDK

It's not weaker, in fact it's stronger. It's also a suicidal A/I unlike adex which may have an E2 rebound after stopping it.

Aromaisn is a suicidal inhibitor, it seeks out estrogen and kills it, it does not suppress it like adex does.

They all work pretty much the same for E2 suppression but aromasin permanantly deactivates the aromatase enzyme but letro and adex don't. This is a cool feature to avoid E2 rebound.

Anticancer Res. 2009 Aug;29(8):3337-46.

Effect of aromatase inhibitors on lipid metabolism, inflammatory response and antioxidant balance in patients with breast carcinoma.

Melichar B, Kalábová H, Krcmová L, Urbánek L, Hyspler R, Solichová D, Melicharová K, Pecka M, Zadák Z.
Department of Oncology, Palacký University Medical School & Teaching Hospital, I.P. Pavlova 6, 77520 Olomouc, Czech Republic. bohuslav.melichar@fnol.cz

Abstract

BACKGROUND: Aromatase inhibitors may affect lipid metabolism, inflammatory response and antioxidant balance.
PATIENTS AND METHODS: One hundred and eighty-six post-menopausal patients with breast carcinoma underwent evaluation of parameters of lipid metabolism, inflammatory response and antioxidant balance immediately before as well as 2 and 4 months after the start of therapy with aromatase inhibitors.
RESULTS: A significant increase in total, very low density lipoprotein (VLDL) and low density lipoprotein (LDL) cholesterol, lipoprotein (a), retinol, C-reactive protein and fibrinogen was observed. The changes of serum lipid concentrations were restricted mostly to the patients pre-treated with tamoxifen who had significantly lower baseline levels of these parameters.
CONCLUSION: An increase of serum cholesterol, lipoprotein (a), C-reactive protein and fibrinogen in patients treated with aromatase inhibitors is the result of tamoxifen withdrawal rather than a direct effect of therapy. No significant changes in serum lipids were observed in patients treated with aromatase inhibitors in the first-line setting.


PMID: 19661353 [PubMed - indexed for MEDLINE]

Aromasin

(Exemestane)


Aromasin is a steroidal aromatase inactivator used to lower circulating estrogen. It was developed to help fight breast cancer as estrogen plays a role in the growth of cancer cells. Aromasin binds irreversibly to the aromatase enzyme. This suppresses the conversion of androgens into estrogen. Circulating estrogen can be reduced by nearly 85% in women using Aromasin. A common misconception is that aromatase inhibition is similar in men than women. However in trials when males were administered 25mg of Aromasin daily maximal estradiol suppression of 62 ± 14% was observed at 12 hours. Aromasin acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." In other words, Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogens. When we compare this mode of action against other AI’s the benefit becomes clear. Arimidex can unbind from the aromatase enzyme when you stop taking it but Aromasin will not therefore there is less chance of estrogen rebound with Aromasin.

Aromasin can be employed during a steroid cycle when aromatizing compounds such as testosterone are administered in order to control estrogen from getting out of control. During the course of a typical steroid cycle estrogen can rise quite high. Estrogen has been measured as much as 7 times higher than normal in men on steroids. This is excessive and can potentially cause water retention, gynecomastia (the formation of female breast tissue) or benign prostatic hyperplasia. Therefore in order to avoid these side effects estrogen must be controlled.

Aromasin not only lowers circulating estrogen and sex hormone binding globulin but it also increases free testosterone by a whopping 117%! Total testosterone increases about 60%. Check out the performance of Aromasin after just 10 days of treatment in males.

FIG. 1. Estrogen and androgen plasma levels after 10 d of daily exemestane (25 or 50 mg) in healthy young males (mean ± SD; n = 9–11). To convert to Systeme International units: estradiol, picomoles per liter (x3.671); estrone, picomoles per liter (x3.699); androstenedione, nanomoles per liter (*0.003492); and testosterone, nanomoles per liter (x0.03467).

Aromasin may be used during a steroid cycle with aromatizing compounds and during PCT to help keep the estrogen to testosterone balance in favor of testosterone. Out of all the medications to control estrogen, Aromasin seems to be the most well balanced. It raises testosterone slightly better than Arimidex and lowers estradiol about 12% better than arimidex in men and is likely to cause less estrogen rebound than Arimidex. Keep in mind that 50mg of Aromasin daily kept estradiol in the normal range for men so if you think using an aromatase inhibitor will crush estrogen too much this science supports the opposite. From the data I have read and my years of experience with this medication 25mg of Aromasin every other day is a good starting point on moderate doses of testosterone. If testosterone doses are raised then 25mg daily may be needed to control estrogen. Since either high and low estrogen can cause side effects such as low libido only labs can determine the appropriate dose of Aromasin.

Written by heavyiron

Originally Posted by heavyiron

Anticancer Res. 2009 Aug;29(8):3337-46.

Effect of aromatase inhibitors on lipid metabolism, inflammatory response and antioxidant balance in patients with breast carcinoma.

Melichar B, Kalábová H, Krcmová L, Urbánek L, Hyspler R, Solichová D, Melicharová K, Pecka M, Zadák Z.
Department of Oncology, Palacký University Medical School & Teaching Hospital, I.P. Pavlova 6, 77520 Olomouc, Czech Republic. bohuslav.melichar@fnol.cz

Abstract

BACKGROUND: Aromatase inhibitors may affect lipid metabolism, inflammatory response and antioxidant balance.
PATIENTS AND METHODS: One hundred and eighty-six post-menopausal patients with breast carcinoma underwent evaluation of parameters of lipid metabolism, inflammatory response and antioxidant balance immediately before as well as 2 and 4 months after the start of therapy with aromatase inhibitors.
RESULTS: A significant increase in total, very low density lipoprotein (VLDL) and low density lipoprotein (LDL) cholesterol, lipoprotein (a), retinol, C-reactive protein and fibrinogen was observed. The changes of serum lipid concentrations were restricted mostly to the patients pre-treated with tamoxifen who had significantly lower baseline levels of these parameters.
CONCLUSION: An increase of serum cholesterol, lipoprotein (a), C-reactive protein and fibrinogen in patients treated with aromatase inhibitors is the result of tamoxifen withdrawal rather than a direct effect of therapy. No significant changes in serum lipids were observed in patients treated with aromatase inhibitors in the first-line setting.


PMID: 19661353 [PubMed - indexed for MEDLINE]

Lots of great information here. Interesting that pretreatment with Nolva is the real cause. I'd always understood that Adex and Letro were tough on your blood lipid profile. Interesting to read otherwise. Since I never use Nolva, I guess it is a non-issue for me.

My other question is about using Adex during my cycle and Aromasin during PCT. Do you think this is effective? The hope was to switch to Aromasin in order to avoid the estrogen rebound associated with Adex, or at least lessen it. Adex always seems to work better for me with the water bloat during cycle, which is why I tend to use it.

Originally Posted by MDR

Lots of great information here. Interesting that pretreatment with Nolva is the real cause. I'd always understood that Adex and Letro were tough on your blood lipid profile. Interesting to read otherwise. Since I never use Nolva, I guess it is a non-issue for me.

My other question is about using Adex during my cycle and Aromasin during PCT. Do you think this is effective? The hope was to switch to Aromasin in order to avoid the estrogen rebound associated with Adex, or at least lessen it. Adex always seems to work better for me with the water bloat during cycle, which is why I tend to use it.

Nolva improves lipids so when you stop using it they return to previous levels. It was at one time thought that the AI's negatively effected lipids because they were used right after the patients stopped using Nolva.

Switching to Aromasin is fine at the end.

Originally Posted by heavyiron

Nolva improves lipids so when you stop using it they return to previous levels. It was at one time thought that the AI's negatively effected lipids because they were used right after the patients stopped using Nolva.

Switching to Aromasin is fine at the end.

Thanks very much. I love going from misinformed to informed. I really need to do more reading and keep up on this stuff. Seems like something is always changing. Thanks again for your help.

Originally Posted by CT

It's not weaker, in fact it's stronger. It's also a suicidal A/I unlike adex which may have an E2 rebound after stopping it.

Aromaisn is a suicidal inhibitor, it seeks out estrogen and kills it, it does not suppress it like adex does.

I was down with it being an inhibitor . .. going into a big cycle I was under the impression Aromasin was 'weaker', hence the preference for adex or letro.

Ive been using aromasin for 7 months . . it's g2g.

The only reason people use adex more is because its cheaper. Honestly, I see a lot of decisions made because shit is cheap. Not very intelligent if you ask me.