Health

Anastrozole: Everything You Should Know About This Research Liquid

Anastrozole, a non-steroidal AI (aromatase inhibitor), is a research liquid quite similar to letrozole. It helps decrease the circulation of estrogen levels in treating postmenopausal women. The aromatase inhibitor is known to work in breast cancer patients responsive to estrogen.

Anastrozole also shares some of its characteristics with the steroidal aromatase inhibitor, exemestane. But the non-steroidal nature of anastrozole equips it with certain advantages, including the lack of side effects like acne and weight gain. Keep reading to expand your knowledge about anastrozole.

Pharmacodynamics

Anastrozole has the potential to stop the conversion of testosterone and other adrenal androgens into estrogen. Several breast cancers are triggered by the presence of estrogen in tumors and peripheral tissues. Since anastrozole has a long-term effect, taking one dosage daily is more than enough.

One dosage can reduce serum estradiol by around 70% within 24 hours of starting the therapy. The estrogen levels will remain low for up to 6 days after ending the therapy course. It is preferable for breast cancer treatment in postmenopausal women due to its higher efficacy rate than tamoxifen and other estrogen receptor modulators.

Postmenopausal women with an advanced stage of breast cancer experiencing disease progression despite taking tamoxifen are prescribed anastrozole. It is an adjunct for hormone receptor-positive early breast cancer treatment in postmenopausal women. It is also the first line of treatment in postmenopausal women with metastatic or locally advanced breast cancer.

Mechanism of Action

Anastrozole applies its anti-estrogenic effects through competitive and selective inhibition of aromatase. The aromatase enzyme is primarily found in the liver, fatty tissues, and adrenal glands. You should know that most breast cancers are hormone-receptor-positive.

It means that their growth is stimulated under the presence of hormones like progesterone and estrogen. Anastrozole reduces estrogen levels by competitively inhibiting the biosynthesis of estrogens. With decreasing estrogen levels, hormone receptor-positive tumors also stop growing.

Metabolism

Anastrozole mainly gets metabolized inside the liver through glucuronidation and oxidation to a few inactive metabolites. The inactive metabolites can include free and glucuronidated hydroxy anastrozole, anastrozole glucuronide, and more.

Oxidation to hydroxy anastrozole is mainly catalyzed by CYP3A4. CYP2CB and CYP3A5 also catalyze oxidation to some extent. The direct glucuronidation of anastrozole is predominantly catalyzed by UGT1A4.

Sometimes anastrozole undergoes N-dealkylation to produce benzoic acid and triazole. The main metabolite found in plasma after administration is triazole. But recent pharmacokinetic studies fail to detect N-dealkylation products.   

Absorption

On an empty stomach, anastrozole gets rapidly absorbed. Within 2 hours of dosage, it can typically reach Tmax. When administered with food, the rate of absorption reduces a little bit. But administration after 30 minutes of ingesting food can again increase the absorption rate.

Drug Interactions

Keep scrolling to discover the interaction of anastrozole with a few drugs:

  • Abiraterone: It can decrease the metabolism of anastrozole.
  • Acetyldigitoxin: It can reduce the cardiotoxic activities of anastrozole.
  • Capecitabine: A combination of capecitabine and anastrozole can increase the risk of the severity of cardiotoxicity.
  • Canakinumab: It can increase the metabolism of anastrozole.
  • Treprostinil: It can decrease the metabolism of anastrozole.
  • Selexipag: Anastrozole can decrease the metabolism of selexipag.
  • Selumetinib: Anastrozole can decrease the metabolism of selumetinib.
  • Selpercatinib: It can increase the serum concentration of anastrozole.
  • Synthetic Conjugated Estrogens A and B: They can reduce the therapeutic efficacy of anastrozole.

Findings

Research is ongoing about the uses of anastrozole. It is particularly beneficial for the treatment of gynecomastia. You can purchase this from Loti Labs which is an authentic site that provides high-quality peptides and research liquids. Even though tamoxifen and other selective estrogen receptor modulators fail to control the enlargement of the breast in men, anastrozole is quite successful at it.

Several clinical trials were also going on regarding the usage of anastrozole for treating female infertility. However, anastrozole was never approved for such usage due to a lack of development in clinical trials.

It was also under development to be used for treating endometriosis and as a hormonal contraceptive. However, anastrozole did not receive a clearing for either of these uses.

Anastrozole succeeds at increasing testosterone levels in men. Clinical trials have been performed to use it as an alternative to androgen replacement therapy for hypogonadism in men. However, concerns arose about its long-term impact on the density of bone minerals.

Ending Note

In the US, anastrozole was approved for medical usage in 1995. Trials are still going on to detect its further usage

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