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Old 03-31-2011, 01:13 AM
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Aromasin - Exemestane Profile

Aromasin - Exemestane
Pharmaceutical Name: Exemestane
Drug Class: Aromatase Inhibitor
Active Life: 24-30 hours
Exemestane is a steroidal suicide aromatase inhibitor/irreversible aromatase inactivator, lowering production of estrogen in the body by blocking the aromatase enzyme. Similar in structure to formestane, exemestane’s medical use like most aromatase inhibitors is for treatment of estrogen-dependent breast cancer. It is usually only prescribed in those cases where therapies using less aggressive compounds have not produced the results hoped for, such as selective estrogen receptor modulators.

For use by strength athletes and bodybuilders, exemestane has several properties that would be beneficial. First, exemestane reportedly can lower estrogen 85% on average (1). In doing so of course this will aid in the prevention of estrogen related side effects caused by aromatizing steroids. The drug also raises testosterone levels in users which can be advantageous if used during post-cycle therapy (2). Add to this the fact that there is some evidence that exemestane may elevate levels of insulin growth factor [IGF] (3).

Like other aromatase inhibitors, there is also conflicting information and studies regarding the effect that exemestane has on users blood lipids/cholesterol, with some studies indicating that the compound has little to no effect while others say that it is quite harsh (4,5).


Use/Dosing

Exemestane reaches peak plasma concentrations within 2 hours following the oral administration of a 25 mg dose (1). 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 (1). 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 (1, 4).

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 (2). 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.

It appears that the only negative aspect of the compound in terms of the dosing schedule is that it takes approximately seven days for it to reach steady blood plasma levels. However, this is not a major hindrance to its use. It just simply requires that a user begin using exemestane a week prior to when they want the effect of the compound to be full realized.


Risks/Side Effects

Exemestane has no significant drug toxicity at doses up to 600 milligrams per day. It is well tolerated by most users with the maximum tolerated dose toxicity not yet being identified (1). Negative side effects related to the use of this compound are usually quite mild and can include things such as transient gastrointestinal effects, hot flashes, nausea, and/or fatigue (1, 2). As previously mentioned, the effect of exemestane on the blood lipids/cholesterol are unknown due to the conflicting research and therefore should be monitored when using the compound. Sexual dysfunction is also a possibility due to the lowering of estrogen levels as well. However reports of this are relatively rare.

Due to the mild negative side effects associated with the compound, as well as the potency of the drug in alleviating estrogen-related side effects when administering aromatizing anabolic steroids, exemestane is seemingly a relatively safe choice when looking for an aromatase inhibitor.

By ~ Aboot

References

1. Brueggemeier RW. Overview of the pharmacology of the aromatase inactivator exemestane. Breast Cancer Res Treat 2002;74:177-185.

2. Mauras N, Lima J, Patel D, Rini A, di Salle E, Kwok A, Lippe B. Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.

3. Martinetti A, Zilembo N, Ferrari L, Massimini G, Polli A, La Torre I, Giovanazzi R, Pozzi P, Bidoli P, De Candis D, Seregni E, Bombardieri E, Bajetta E. Bone turnover markers and insulin-like growth factor components in metastatic breast cancer: results from a randomised trial of exemestane vs megestrol acetate. Anticancer Res. 2003 Jul-Aug;23(4):3485-91.

4. Buzdar AU. An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. 2002 Nov 1;95(9):2006-16.

5. Atalay G, Dirix L, Biganzoli L, Beex L, Nooij M, Cameron D, Lohrisch C, Cufer T, Lobelle JP, Mattiaci MR, Piccart M, Paridaens R. The effect of exemestane on serum lipid profile in postmenopausal women with metastatic breast cancer: a companion study to EORTC Trial 10951, 'Randomized phase II study in first line hormonal treatment for metastatic breast cancer with exemestane or tamoxifen in postmenopausal patients'. Ann Oncol. 2004 Feb;15(2):211-7.
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Old 03-31-2011, 01:14 AM
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Aromasin (exemestane)
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.

~Unknown
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