Popular Anti-Estrogen Steroids Anastrozole Arimidex For Steroid Cycle PCT CAS 120511-73-1

Arimidex (anastrozole) is the aromatase inhibitor of choice. Arimidex’s mechanism of action - blocking conversion of aromatizable steroids to estrogen - is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) or tamoxifen (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others.

Anastrozole, sold under the trade name Arimidex among others, is a medication used in addition to other treatments for breast cancer. Specifically it is used for hormone receptor-positive breast cancer. It has also been used to prevent breast cancer in those at high risk. It is taken by mouth.

Applications:

The drug is appropriately used when using substantial amounts of aromatizing steroids, or when one is prone to gynecomastia and using moderate amounts of such steroids. Arimidex does not have the side effects of aminoglutethimide (Cytadren) and can achieve a high degree of estrogen blockade, much moreso than Cytadren. It is possible to reduce estrogen too much with Arimidex, and for this reason blood tests, or less preferably salivary tests, should be taken after the first week of use to determine if the dosing is correct.

Arimidex is a hormonal therapy used to treat breast cancer in women who have been through the menopause.
Hormones are substances produced naturally in the body. They act as chemical messengers and help control the activity of cells and organs. Hormonal therapies work by interfering with the production or action of particular hormones in the body.

Anastrozoles Arimidex is the aromatase inhibitor of choice. Arimidex's mechanism of action - blocking conversion of aromatizable steroids to estrogen - is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid) or (Nolvadex), which block estrogen receptors in some tissues, and activate estrogen receptors in others.

Anastrozoles is an aromatase-inhibiting drug approved for treatment of breast cancer after surgery, as well as for metastasis in both pre and postmenopausal women. The severity of breast cancer is increased by estrogen, as sexhormones cause hyperplasia, and differentiation at estrogen receptor sites. Anastrozoles works by inhibiting the synthesis of estrogen.

How does Anastrozole work?

Anastrozole reversibly binds to the aromatase enzyme, and through competitive inhibition blocks the conversion of androgens to estrogens in peripheral (extra-gonadal) tissues.

Anastrozole is an inhibitor for the triazole aromatase with a strong selectivity. It can inhibits aromatase which is prerequisite for the synthesis of pigment cells P-450 thereby blocking the biosynthesis of estrogens, and the estrogen is the essential part of the growth of breast cancer cells. The 50% inhibitory concentration (IC50) value of anastrozole to placental aromatase is 15nmol/L.

Usage of Anastrozole:

(1) It is the third-generation’s aromatase inhibitors, used for the treatment of advanced breast cancer of postmenopausal patients.

(2) Its used to cure the breast cancer.

(3) Anastrozole is the third-generation’s aromatase inhibitors, used for the treatment of advanced breast cancer of postmenopausal patients. It is an inhibitor for the triazole aromatase with a strong selectivity. It can inhibits aromatase which is prerequisite for the synthesis of pigment cells P-450 thereby blocking the biosynthesis of estrogens, and the estrogen is the essential part of the growth of breast cancer cells. Its used to cure the breast cancer, particularly suitable for postmenopausal women with advanced breast cancer who recrudescent after hormone adjuvant therapy.


Anastrozole Medical uses:

The ATAC trial was of localized breast cancer and women received either anastrozole, tamoxifen, or both for five years, followed by five years of follow-up. After more than 5 years the group that received anastrozole had better results than the tamoxifen group.[8] The trial suggested that anastrozole is the preferred medical therapy for postmenopausal women with localized breast cancer, which is estrogen receptor (ER) positive.

Another study found that the risk of recurrence was reduced by 40%, but was associated with an increased risk of bone fractures. The study concluded that ER positive patients benefited from switching from tamoxifen to anastrozole in patients who have completed 2 years' adjuvant tamoxifen.

A more recent trial found that anastrozole significantly reduced the incidence of breast cancer in postmenopausal women relative to placebo, and while there were side effects related to estrogen deprivation observed, the researchers concluded that this was probably not related to the treatment. Lead author Jack Cuzick was quoted by the BBC as saying, "This class of drugs is more effective than previous drugs such as tamoxifen and crucially, it has fewer side effects," adding that he thought there was now enough evidence to support offering the drug.


Side effects:

(1) Common side effects include hot flashes, altered mood, joint pain, and nausea. Severe side effects include an increased risk of heart disease and osteoporosis. Use during pregnancy is known to harm the baby.

(2) Bone weakness has been associated with anastrozole. Women who switched to anastrozole after two years on tamoxifen reported twice as many fractures as those who continued to take tamoxifen (2.1% compared to 1%). Bisphosphonates are sometimes prescribed to prevent the osteoporosis induced by aromatase inhibitors. The level of circulating estradiol is likely causal here and not the anastrozole itself, and so the dose will determine likelihood of osteoporosis (estradiol inhibits osteoclasts, which resorb bone). Acne, constricted pupils and water retention have also been attributed with use of this anti-estrogen.

(3) The suppression of estrogen, specifically the hormone estradiol, is often necessary for men who have hormone disorders. Elevated levels of the female hormone in men can be manifested in gynecomastia or growth of breasts in males and hypogonadism or the reduced function of the testes. In worse cases, excessive estrogen may put men at higher risk for having prostate cancer and cardiovascular diseases. Prescribing anastrozol for men in these situations has shown significant decrease of estradiol levels and, therefore, a decrease in symptoms and risks.
 

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