Tamoxifen Review – Buy Tamoxifen Liquid 20mg per ml (30ml)Admin
Tamoxifen is an antineoplastic nonsteroidal selective estrogen receptor modulator (SERM). Tamoxifen competitively inhibits estradiol binding to estrogen receptors, thereby preventing the receptor from binding to the estrogen-response element on DNA.
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Tamoxifen is a nonsteroidal antiestrogen, a tertiary amine compound, and a stilbenoid widely used in treating and preventing breast cancer.
Long-term tamoxifen therapy is associated with fatty liver, steatohepatitis, cirrhosis, and rare cases of clinically apparent acute liver injury.
STRUCTURE OF TAMOXIFEN
Molecular formula: C26H29NO
Molecular weight: 371.5 g/mol
CAS number: 10540-29-1
IUPAC name: 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine
MECHANISM OF ACTION
Tamoxifen is a selective estrogen receptor modulator that inhibits growth and promotes apoptosis in estrogen receptor-positive tumors.
Data from animal studies suggest that It is absorbed slowly following oral administration, with peak serum concentrations generally occurring about 3-6 hours after a single dose, and its metabolites undergo extensive enterohepatic circulation.
It has a long duration of action as the active metabolite N-desmethyl tamoxifen has a half-life of approximately two weeks.
Tamoxifen benefits include:
- Improving blood flow, reducing uterine contractility and pain in dysmenorrhea
- Treating early and advanced estrogen receptor-positive (ER-positive or ER+) breast cancer in pre-and postmenopausal females. Additionally, it is the most common hormone treatment for male breast cancer.
- Ovulation induction for treating infertility in females with anovulatory disorders.
- Improving fertility in males with infertility
- Tamoxifen is used to prevent and treat gynecomastia.
- For treating peripheral precocious puberty
TAMOXIFEN SIDE EFFECTS
Tamoxifen has a narrow therapeutic index as higher doses can lead to many problems. These include:
- An increased risk of postmenopausal bleeding, endometrial polyps, hyperplasia, and endometrial cancer
- A rapid increase in triglyceride concentration in the blood
- An increased risk of thromboembolism
- Unsteady gait
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- Tamoxifen is an estrogen antagonist on gonadotropin secretion and responsiveness of the hypothalamic-pituitary- adrenal axis in female monkeys. Endocrine 22, 305-315 [PubMed:14709804]
- Sanchez-Spitman AB, Swen JJ, Dezentje VO, Moes DJ, Gelderblom H, Guchelaar HJ (June 2019). “Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen”. Expert Review of Clinical Pharmacology. 12 (6): 523–536. doi:10.1080/17512433.2019.1610390. PMID 31008668.
- “NCI Drug Dictionary”. 2 February 2011. Archived from the original on 8 December 2015. Retrieved 12 September 2021.
- Klein DJ, Thorn CF, Desta Z, Flockhart DA, Altman RB, Klein TE (November 2013). “PharmGKB summary: tamoxifen pathway, pharmacokinetics”. Pharmacogenetics and Genomics. 23 (11): 643–647. doi:10.1097/FPC.0b013e3283656bc1. PMC 4084801. PMID 23962908.