Arimidex (Ldex, Anastrozole), Femara (Letrozole), Nolvadex(Tamoxifen) & Cholesterol

ORIGINALLY POSTED BY SUPERCHICKEN, stolen by tony touch from crankenstein, and pilfered by BASK8KACE

There has been a lot of talk on other boards about this lately, and a lot of bad information thrown out as well. I wanted to share the good info.

Somone keeps posting how letrozole is the strongest and doesnt negatively affect cholesterol. This is not true. Letrozole is NOT the strongest and it DOES affect cholesterol/lipid profile negatively.

Aromasin (Exemestane) is the best. This is why:

Both Arimidex/Ldex/Anastrozole and Femara/Letrozole hurt your cholesterol. The way these 2 anti e's 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 F***ed.

Aromasin (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 gyno. The estrogen is crippled due to exemestane. However, since the estrogen is still floating around, it will not negatively affect your lipid/cholesterol profile.

Anastrozole (Arimidex) doesnt cause a rebound effect, and neither does exemestane, but letrozole does. This means after you stop the letrozole, your estrogen rebounds and goes pretty high for a while, eventually it normalizes. You can avoid this by tapering your letro dose down before stopping it, but that is a pain in the ass. Higher than normal can mess many things up post cycle when you stop. Since the HPTA has a feedback loop is primarily controlled by estrogen, high estrogen will tell your HPTA to produce less testosterone, because it thinks the high estrogen is caused by too much testosterone. This is fact. Now post cycle, dont we want to raise our test levels, not lower them? Of course! So, rebounds are bad. If you use letro taper the dose off to zero over a couple weeks.

FYI- Nolvadex(Tamoxifen) is a SERM(Selective Estrogen Receptor Modulator). This means on certain tissue it can act antagonisticaly or agonistically. In the case of lipid profiles, It acts agonistically. So, running tamoxifen with your anti e's will IMPROVE your cholesterol profile even if not on cycle or using any gear or other anti e's. It's just plain good for cholesterol.

One thing to keep in mind though when runing tamoxifen with letro is that letro reduces blood levels of tamoxifen by over 50%. a study showed 2.5mg letro ED made nolva levels drop to 40% of what they were before adding letro. This does not mean you cant use tamoxifen with letro, it just means you need to use more, about double. In other words, 20mg of nolva will act like 8mg if running letro. So, make sure you are aware of this because you will need to buy more nolva to compensate. This does not happen when mixing tamoxifen with anastrozole or exemestane, it only hppens with letro.
NOTE: After this was posted, Pheedno mentioned the following which has been placed here to shed light on this possible mistake made by the original author of this postNolva in full clinical doses(20mgED) reduces letro plasma levels by 37.6%(Not the other way around at 50%). Nolva in full clinical doses reduces anastrozol plasma levels by 27%.

Also, many people experince a reduction of libido on letro. This doesnt happen w/ ldex or exmestane as far as I know, and in my own experience, and I've run all 3 quite a bit.

The best combo is exemestane and tamoxifen together. Your cholesterol will be as good as can be considering your on a cycle of steroids. The dose of aromasin will vary depending on the users needs and how much aromatizing gear is being taken. Usually 10-25mg ed works well. Run 10mg ed nolva to improve your cholesterol.

Second best combo i feel is anastrozole(Ldex, Arimidex) and tamoxifen. Ldex dose ranges from usually .15mg ed to 1mg ed. run 10mg nolva ed to improve cholesterol.

Third best is letro and nolvadex. Letro doses usually range from 1-2.5mg ed. run 20mg ed nolva to improve cholesterol w/ letro.

You do not need to run nolva with any of these 3, i do recomend it though as it will improve cholesterol compared to using the anti e's alone without nolva.

So, in order of strength, on a dose per dose basis(not mg per mg) aromasin is def the strognest, next is letro, and then ldex.

I've been running aromasin now for about 4 months, I wont switch back to ldex or letro. It works much better and it's much healthier for cholesterol profiles.

I think we all need to stop only worrying about side effects that we can see visually. Cholesterol KILLS many people around the world everyday(well not directly kills but leads to it). steroids are hUrting us badly in this sense. steroids do mess our cholesterol up pretty badly, and we will pay for it later in life. Now not many of us are going to stop using gear because of that, but we should at least take the proper other drugs to help minimize.

Aromasin is only a little bit more expensive than ldex or letro, and its actually about the same price as many places sell ldex or letro for. But it's more powerful and healthier. People spend money all the time on steroids which dont have as many side effects as some of the harsher, cheaper steroids. A few extra bucks for the proper anti e's is def money well spent.

**** you know im still going to use femara man.
Because it just keeps me so dry and yes u do drop
the dose at the end of the cycle. TO help with the
rebound and clomid still works.

Fukin awesome post, Thanks

Thank you for the info.

BassMuscle

good info man im not dissing you but im just saying
I think femara is very good at keeping you from getting
gyno and water retention.

Slightly incorrect. Nolva in full clinical doses(20mgED) reduces letro plasma levels by 37.6%(Not the other way around at 50%). Nolva in full clinical doses reduces anastrozol plasma levels by 27%

I just ordered femara for my M1T cycle becuase Im uping the dose of 4derm to 600mg ed and am taking fem 1.25mg eod. Nolva 40mg ED wk 5/6 and 20mg ED wk 7/8 and clomid 300/100/50 pct also. Change anything?

This is why I run Nolva with my SERMS, although right now I'm on Aromasin so I guess it's not neccessary.

Great post bro.

Quote:

---

Originally Posted by Pheedno

Slightly incorrect. Nolva in full clinical doses(20mgED) reduces letro plasma levels by 37.6%(Not the other way around at 50%). Nolva in full clinical doses reduces anastrozol plasma levels by 27%

---

Pheedno,

I copied this post. I didn't realize that that was incorrect. Could you post that study so others can see it and realize that that portion of the post is incorrect? Thx.

BTW...I've edited the post to highlight what you've mentioned.

....

Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromatase inhibitor letrozole in postmenopausal women with breast cancer.

Dowsett M, Pfister C, Johnston SR, Miles DW, Houston SJ, Verbeek JA, Gundacker H, Sioufi A, Smith IE.

Department of Biochemistry, Royal Marsden Hospital, London, United Kingdom.

This study examined whether the addition of tamoxifen to the treatment regimen of patients with advanced breast cancer being treated with the aromatase inhibitor letrozole led to any pharmacokinetic or pharmacodynamic interaction. Twelve of 17 patients completed the core period of the trial in which 2.5 mg/day letrozole was administered alone for 6 weeks and in combination with 20 mg/day tamoxifen for the subsequent 6 weeks. Patients responding to treatment continued on the combination until progression of disease or any other reason for discontinuation. Plasma levels of letrozole were measured at the end of the 6-week periods of treatment with letrozole alone and the combination and once more between 4 and 8 months on combination therapy. No further measurements were done thereafter. Hormone levels were measured at 2-week intervals throughout the core period. Marked suppression of estradiol, estrone, and estrone sulfate occurred with letrozole treatment, and this was not significantly affected by the addition of tamoxifen. However, plasma levels of letrozole were reduced by a mean 37.6% during combination therapy (P<0.0001), and this reduction persisted after 4-8 months of combination therapy. Letrozole is the first drug to be described in which this pharmacokinetic interaction occurs with tamoxifen. The mechanism is likely to be a consequence of an induction of letrozole-metabolizing enzymes by tamoxifen but was not further addressed in this study. It is possible that the antitumor efficacy of letrozole may be affected. Thus, sequential therapy may be preferable with these two drugs. It is not known whether tamoxifen interacts with other members of this class of drugs or with other drugs in combination.

Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: a sub-protocol of the 'ArimidexÔ and Tamoxifen Alone or in Combination' (ATAC) trial

The ATAC Trialists' Group

CRC and UCL Cancer Trials Centre, University College London, Stephenson House, 158-160 N Gower Street, London, NW1 2ND, UK



Received 20 September 2000; revised 22 April 2001; accepted 2 May 2001



The ATAC trial evaluates in a randomized, double-blind design, ArimidexÔ (anastrozole) alone or in combination with tamoxifen, relative to tamoxifen alone as 5-year adjuvant treatment in postmenopausal women with early breast cancer. Patients included in the pharmacokinetic (PK) sub-protocol had been in ATAC for 3 months, taking their medication in the morning and were 100% compliant for the preceding 14 days. Blood samples were collected 24 ± 4 h after last dose. Trough (Cmin) plasma concentrations of anastrozole, tamoxifen and desmethyltamoxifen (DMT) were measured by validated methods. The PK results were based on a total of 347 patients (131 anastrozole (1 mg o.d.), 111 tamoxifen (20 mg o.d.), 105 anastrozole and tamoxifen (1 and 20 mg o.d. respectively)). The geometric mean steady-state trough plasma concentrations of tamoxifen and DMT were statistically equivalent in patients receiving tamoxifen alone or in combination with anastrozole: geometric mean tamoxifen = 94.8 ng ml-1and 95.3 ng ml-1in tamoxifen alone and combination groups, respectively; geometric mean DMT = 265.1 and 277.6 ng ml-1in the tamoxifen and anastrozole and tamoxifen groups, respectively. The geometric mean anastrozole levels were 27% lower (90% Cl 20-33%;P< 0.001) in the presence of tamoxifen than with anastrozole alone. Baseline plasma oestradiol levels were not obtained in the PK sub-protocol, however, such information was available from a similar ATAC sub-protocol, which evaluated bone mineral density. Mean oestradiol levels were 21.3, 19.3, and 21.6 pmol l-1prior to treatment and 3.7, 20.9 and 3.6 pmol l-1after 3 months in the anastrozole, tamoxifen, and combination groups, respectively (n = 167). On-treatment values were below the detection limit (3 pmol l-1) in 43.6 and 38.5% of the anastrozole alone and anastrozole in combination with tamoxifen groups, respectively. As a result of (a) the lack of effect of anastrozole on tamoxifen and DMT levels and (b) the observed fall in blood anastrozole levels having no significant effect on oestradiol suppression by anastrozole, we conclude that the observed reduction in anastrozole levels by tamoxifen is unlikely to be of clinical significance when anastrozole and tamoxifen are administered together

Thank you, Pheedno.

Quote:

---

Originally Posted by BASK8KACE

Thank you, Pheedno.

---

;) No problemo

bump,

GREAT read. thank you both.

Quote:

---

Originally Posted by BASK8KACE

...steroids do mess our cholesterol up pretty badly, and we will pay for it later in life.

---

Oh nice. Makes me wanna rush right out and do another cycle.

Excellent post BASK8KACE & thanks also for the info Pheedno...Bros'...The AI's L-zole & A-zole do screw up your profiles much more than most think...throw in a bulking diet.
I want to try Aromasin also...I need all the help I can get...again...great post...Thanks.

no one runs letro at 2.5 mg unless they have cancer. there is also no need to run nolva and letro together.... It doesn't mention the fact that Letrozole raises IGF levels by 27% ....there are many other things that make letrozole the better buy ....O the price

hey guys i was just wonderin i have a D-bol ,Test E, EQ cycle im going to hit in the off-season but im running the test at a gram a week and EQ at 600 mg a week...i want to stay dry and lean as hell as i have a competition coming up after that cycle so i was wondering if 1.25 EOD Femara will keep me lean and dry.....this isnt the show cycle as then i will be switching over to the prop/tre/winny/halo thing.....any suggestions on that? will be running nolva at 10 mg a day as well

Quote:

---

Originally Posted by JoeGuns27

hey guys i was just wonderin i have a D-bol ,Test E, EQ cycle im going to hit in the off-season but im running the test at a gram a week and EQ at 600 mg a week...i want to stay dry and lean as hell as i have a competition coming up after that cycle so i was wondering if 1.25 EOD Femara will keep me lean and dry.....this isnt the show cycle as then i will be switching over to the prop/tre/winny/halo thing.....any suggestions on that? will be running nolva at 10 mg a day as well

---

This is an outstanding informational thread....Don't hijack

great thread one of the best for sure but...pheedno i didnt understand a word on that post u made it was way to technecical for me... now after reading both i still feel a little confused... so is it best to take nolva with aromasin? or not ...

Yep no hijackers allowed. Start a thread of your own or better yet do a search.

not highjacking just asking for some clear up on what was said thats all.

Bump...since Letro seems to be pushed heavily lately by some.


~Pinnacle~

This advice seems a little over-simplified.

This study shows both anastrozole and tamoxifen increase good cholesterol (11% and 26% respectively), while tamoxifen alone reduces bad cholesterol (12%) and anastrozole has no significant effect:

http://annonc.oxfordjournals.org/cgi...act/16/10/1632

Low estrogen levels will reduce good cholesterol and increase bad cholesterol IN WOMEN, so women will benefit from taking adex and nolva together - but this effect does not occur in MEN. Estrogen is used in men to maintain bone density (something increased significantly just by lifting weights), so this statement is be incorrect when talking about men:

Quote:

---

The major drawback to this is without estrogen, your lipid profile gets F***ed.

---

The adex/nolva combination for men at least does not seem justified.

Quote:

---

Originally Posted by user1000

This advice seems a little over-simplified.

This study shows both anastrozole and tamoxifen increase good cholesterol (11% and 26% respectively), while tamoxifen alone reduces bad cholesterol (12%) and anastrozole has no significant effect:

http://annonc.oxfordjournals.org/cgi...act/16/10/1632

Low estrogen levels will reduce good cholesterol and increase bad cholesterol IN WOMEN, so women will benefit from taking adex and nolva together - but I can't find any mention of this effect in MEN. And this effect being present in men is the reason used above to justify using nolva with adex.



So the adex/nolva combination for me at least does not seem justified.

---

This is one of the reasons I bumped this thread.The original poster/posters have supplied no links to back their claims.
I'd like Hooker or Ossie to jump in and clear up some of this.

~Pinnacle~

The only thing I can find about low estrogen levels in men is that abnormally low levels may increase the risk of prostate cancer and osteoporosis. Taking nolva with adex could potentially worsen this risk.

So better advice might be not to overdo it with the adex in the first place.

letro is ok.

1º

Ann Oncol. 2005 May;16(5):707-15. Epub 2005 Apr 7.

The influence of letrozole on serum lipid concentrations in postmenopausal women with primary breast cancer who have completed 5 years of adjuvant tamoxifen (NCIC CTG MA.17L).

Wasan KM, Goss PE, Pritchard PH, Shepherd L, Palmer MJ, Liu S, Tu D, Ingle JN, Heath M, Deangelis D, Perez EA.

Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, BC, Canada. [email protected]

BACKGROUND: The purpose of this study was to evaluate changes in serum lipid parameters {cholesterol, high-density lipoprotein (HDL) cholesterol, low-density lipoprotein (LDL) cholesterol, triglycerides and lipoprotein(a) [Lp(a)]}, in postmenopausal women receiving letrozole or placebo after adjuvant tamoxifen for early stage breast cancer (NCIC CTG MA.17L). PATIENTS AND METHODS: MA.17L is a substudy of MA.17, a randomized, double-blind, placebo-controlled trial of letrozole 2.5 mg taken daily for 5 years in postmenopausal women with primary breast cancer completing approximately 5 years of prior adjuvant tamoxifen. Patients consenting to participate in this companion study had blood drawn and lipid parameters (total cholesterol, HDL cholesterol, LDL cholesterol, Lp(a), triglycerides) evaluated at baseline, 6 months, 12 months and yearly thereafter until completion of protocol therapy. It was required that women be non-hyperlipidemic and not taking lipid-lowering drugs at time of entry on this trial. RESULTS: Three hundred and forty seven women were enrolled in the study. The letrozole and the placebo groups demonstrated marginally significant differences in the percentage change from baseline in HDL cholesterol at 6 months (P=0.049), in LDL cholesterol at 12 months (P=0.033) and triglycerides at 24 months (P=0.036). All comparisons of lipid parameters at other time points were not significantly different between the two treatment groups. No statistically significant differences in the number of patients exceeding the thresholds defined for the lipid parameters were found between the two treatment groups. CONCLUSIONS: The MA.17 trial demonstrated a significant improvement in disease-free survival with the use of letrozole as extended adjuvant therapy post tamoxifen. Results from this study suggests that letrozole does not significantly alter serum cholesterol, HDL cholesterol, LDL cholesterol, triglycerides or Lp(a) in non-hyperlidiemic postmenopausal women with primary breast cancer treated up to 36 months following at least 5 years of adjuvant tamoxifen therapy. These findings further support the tolerability of extended adjuvant letrozole in postmenopausal women following standard tamoxifen therapy." ----------------------------------
it will come more.

aromasin,lentaron,arimidex,femara are all aromatase inhibitors.

arimidex and femara are competitive inhibitors.

aromasin and lentaron are suicide inhibitors.



[QUOTE=BASK8KACE]


Both Arimidex/Ldex/Anastrozole and Femara/Letrozole hurt your cholesterol. The way these 2 anti e's 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 F***ed.

Aromasin (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 gyno. The estrogen is crippled due to exemestane. However, since the estrogen is still floating around, it will not negatively affect your lipid/cholesterol profile.

*ignorance.
both inhibit the enzime,one binding to it , the other destroy it.

so if you take 0.5 aramidex daily is it bad??????????

good post...book marking for me.

Definition of Aromatase inhibitor:





Aromatase inhibitor: A drug that inhibits the enzyme aromatase and by that means lowers the level of the estrogen estradiol. Aromatase inhibitors represent a class of antiestrogens. Aromatase catalyzes the conversion of testosterone (an androgen) to estradiol (an estrogen) in many tissues.

there are too, antagonis/agonists.

Quote:

---

Originally Posted by joevette

This is why I run Nolva with my SERMS, although right now I'm on Aromasin so I guess it's not neccessary.

---

nolva is a serm:
Selective Estrogen Receptor Modulators.

1 º generation nolva,clomid
2º generation evista,fareston.

everybody researchs.

see anyway:

from drummerboy
http://forums.anabolicreview.com/sho...d.php?t=198848

So Ossie,I take it this post that has been passed from board to board is just Brotelligence at it's worst?Correct?


~Pinnacle~

correct !

Quote:

---

Originally Posted by oswaldosalcedo

correct !

---

LOL...just as I suspected....


~Pinnacle~

Sometimes it just seems like you have to look at conflicting research and guess who is the better scientist. Thankfully I don't believe gear needs to be made this complicated, but then again I don't compete.

objective knowledge=no ignorance.