The term SERM stands for Selective Estrogen Receptor Modulator, and AI's , stand for Aromatase inhibitor.
SERM's compete for the space that Estrogen binds to(receptors). When this occurs, the receptor is then full and hence blocks out the estrogen. Here are some SERM's .
Tamoxifen (Nolvadex)
Clomiphene Citrate (Clomid),
Toremifene Citrate (Fareston),
Raloxifene hydrochloride (Evista).
Nolva is Commonly dosed at 10-40 mgs. It has a high affinity for binding to breast tissue receptors. It can significantly raise Testosterone levels. However, it can reduce IGF-1 levels. Something to keep in mind. It will reduce the blood levels of Arimidex and Letro by up to 40% rendering them less effective. It does not affect Aromasin.
Clomid: Usually dosed from 25-150 mgs during pct for support of natural Testosterone levels
Clomid acts as both an agonist/ antagonist -- Clomid is an effective antagonist in the hypothalamus and in breast tissue. It is an effective agonist in bone tissue, and for improving blood cholesterol.
It should also be noted that Clomid has an estrogenic effects on mood,be ready to cry watching your favorite commercial.
Evista: Evista is a second-generation SERM. It is approved by the FDA for this use in women. Although it has structural and mechanistic similarities to other SERMs which have been approved either as fertility drugs (Clomid) or Breast Cancer medication (Nolvadex), it has not been approved for either of those uses. Ralixofene exerts its effects by antagonizing the estrogen receptor in some tissues, and agonizing it in others. In this way, certain estrogenic pathways are activated and others are blocked. It seems to exert estrogenic effects on blood lipids, reducing LDL and total cholesterol, as well as estrogenic effects on bone.
Toremifene: Usually dosed around 60 mg. Its androgenicity:estrogenicity ratio is 5x that of Nolvadex. It is prescribed to female patients for breast cancer and has shown a high affinity for binding to the Estrogen receptors in breast tissue. Male patients treated with toremifene citrate 80 mg compared to placebo demonstrated statistically significant increases in bone mineral density in the lumbar spine, hip, and femur skeletal sites. . Toremifene citrate 80 mg treatment compared to placebo also resulted in a decrease in total cholesterol, LDL, and triglycerides, and an increase in HDL. There were also statistically significant improvements in gynecomastia. This data is from an ongoing study of men receiving treatment for ADT (androgen depravation therapy). These men are receiving ADT for advanced prostate cancer. ADT removes much of the testosterone and estrogen in the body which helps the prostatic cancer cells grow.. Some studies have even suggested that Toremifene doesn't regulate progesterone receptors and we may see in the future the possibility of using it with 19-nors.
Some possible side effects include the risk of stroke, pulmonary embolism, and cataracts.
A typical post cycle therapy (pct) of Toremifene would look similar to this:
Week 1: 120mg ED
Week 2: 90mg ED
Week 3: 60mg ED
Week 4: 30mg ED
Toremifene is by far my favorite serm. Its to bad more people dont care it.
Aromatase inhibitors:
AIs are categorized into two types:
Type 1: steroidal inhibitors such as exemestane/aromasin form a permanent or irreversible bond with the aromatase enzyme
Type 2: inhibitors (such as anastrozole, letrozole) inhibit the enzyme by reversible competition.
AI's work by inhibiting the action of the enzyme aromatase, which converts androgens into estrogens by a process called aromatization. By inhibiting aromatase they increase Testosterone and reduce Gynecomastia.
1. Letrozole ( Femara) is a type 2
Letro: Letrozole has been shown to reduce estrogen levels by 98% or more.Administration of Letrozole lowered Estrogen by 46% in the young men tested, and 62% in the elderly subjects. Because estrogen is part of the negative feedback loop of the HPTA, Letrozole (and other anti-estrogens) are able to raise testosterone in male subjects. Letrozole was found to significantly increase LH levels to a 339% and 323% in the young and the elderly, respectively and Testosterone by 146 and 99%, respectively.
Letro has a 2-4 day half life
Normal dosing is .25 - 2.5mg ed
Arimidex type 2:
Arimidex: seems to be the most popular aromatase inhibitor of choice. Usually doesed from 0.25 - 1.0mg eod it is effective even when not used every day. 0.5mgs per day can get rid of up to 50% estrogen.
AROMASIN type 1: Exemestane (Aromasin)
History: Initially researched as a treatment option for breast cancer in the late 90’s, Aromasin was demonstrated to be superior to Tamoxifen and was subsequently released by Pfizer. A fairly recent addition to the anti-estrogen marketplace.
Aromasin is usally doesed from 20-50 mgs per day. It can raise blood testosterone by 60%, and also help out your free to bound testosterone ratio by lowering levels of Sex Hormone Binding Globulin (SHBG), by about 20%! It can suppress estrogen by 65-80%
Method of Administration: Aromasin is administered in oral form.
Drug Class: Suicidal Aromatase Inhibitor.
Primary Use: Aromasin, like all anti-estrogens, is used to help normalize/maintain estrogen levels within the body. Aside from the prevention of estrogenic side effects, estrogen management can assist users in maintaining a hard & dry appearance when using aromatizable drugs. This is especially useful prior to a contest, when displaying this looks is essential to success. Aromasin accomplishes this function by binding with the aromatase enzyme, which is responsible for converting testosterone (and other aromatizable drugs) into estrogens. Once bound, Aromasin will permanently deactivate the aromatase enzyme, preventing any further interaction and eliminating the possibility of experiencing estrogen rebound. This ability to permanently deactivate the aromatase enzyme is what classifies Aromasin as a suicide inhibitor, as not all anti-estrogens have this effect. This advantage is one of the key differences between Aromasin and several other anti-estrogens. However, Aromasin needs to be dosed frequently in order to maintain adequate blood levels of the drug; preferably twice per day, or every 12 hours. This is in significant contrast to several other AI’s, which only need to be dosed every few days. Additionally, unlike all other AI’s, which have been shown to potentially have a negative impact on cholesterol levels, Aromasin is neutral in this regard, making it the more heart health alternative.
Anabolic-Androgenic Ratio: N/A.
Aromatizable: No. Exhibits anti-estrogenic activity.
Progestagenic Activity: No.
Methylated: No.
Standard Dosing Range and Cycle Length: Aromasin is commonly administered at a dosage of 12.5-50 mg per day. Dosing requirements will be determined by the number, type, and amount of aromatizable drugs being used. The drug is typically administered as long as aromatizable drugs are present.
Frequency of Administration: Daily usage; split into 2 equally divided doses.
Remember when comparing ai 's
2.5mg of letro = 1mg adex = 25mg araomasin.
