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Endocrine, paracrine and intracrine mechanisms of growth regulation in normal and malignant breast epithelium
Published in A. R. Genazzani, Hormone Replacement Therapy and Cancer, 2020
J. R. Pasqualini, G. S. Chetrite
For many years endocrine therapy in breast cancer has been mainly by the utilization of antiestrogens, which block the estrogen receptor. Treatment with the antiestrogen tamoxifen (Nolvadex: tamoxifen citrate) of millions of women with breast cancer has had a benefit of 30–35% free of symptoms of the disease and a 20–25% reduction in mortality.
Menopausal Vulvovaginitis
Published in William J. Ledger, Steven S. Witkin, Vulvovaginal Infections, 2017
William J. Ledger, Steven S. Witkin
In this diagnostic evaluation, it is also important to get a detailed medical history and current use of drugs by these patients. Women with a history of breast or endometrial cancer will not ordinarily be candidates for systemic or local estrogens. Some liver illnesses, such as cirrhosis from a chronic hepatitis B or C infection, can preclude the use of oral estrogens as a treatment option. Tamoxifen citrate can cause vaginal symptomatology for patients under care for breast cancer. Any history of allergy is important. If local estrogens have been used, inquiries need to be made to see if the patient has had any adverse reactions to them. They can cause severe vaginal or vulvar burning after the application of an estrogen cream that contains propylene glycol as a preservative. In these situations, the vaginal estrogen tablet that has no propylene glycol would seem to be an ideal choice, but menopausal women with reduced vaginal secretions can develop vaginal or vulvar irritation within a day or two of inserting the vaginal estrogen tablet from the gritty discharge of an incompletely dissolved tablet.
What must be considered when prescribing hormonal pharmacotherapy for male infertility?
Published in Expert Opinion on Pharmacotherapy, 2022
Olivia Holtermann Entwistle, Aditi Sharma, Channa N. Jayasena
A meta-analysis of 16 studies examining the effect of SERMs, such as clomiphene, tamoxifen, toremifene, and raloxifene, in a variety of dosing regimens, in men with idiopathic infertility, observed a significant increase in sperm concentration from baseline in the treatment group [16]. The pooled data also observed a significant increase in pregnancy rates in the treatment group versus placebo/no treatment, although investigators did not specify the mode of pregnancy (ART vs. spontaneous) [16]. Similarly, an earlier meta-analysis of 11 studies found a significant increase in sperm motility and concentration, and spontaneous pregnancy rate, in men with idiopathic infertility treated with either clomiphene citrate 25 mg or 50 mg doses daily, or tamoxifen citrate 20–30 mg daily in comparison with controls [17]. General side effects included headaches, dizziness, and rashes [17]. Sexual side effects included loss of libido and impotence [17], which are important to consider if the goal of hormonal therapy is to increase the chances of pregnancy.
Development and evaluation of polymeric micelle containing tablet formulation for poorly water-soluble drug: tamoxifen citrate
Published in Drug Development and Industrial Pharmacy, 2020
Kıvılcım Öztürk-Atar, Meryem Kaplan, Sema Çalış
Tamoxifen citrate (TMX), an antiestrogenic compound, is the first choice of hormonotherapy for estrogen (ER) and progesterone (PR) receptor-positive premenopausal breast cancer treatment [10]. Several randomized studies showed that TMX use as hormonotherapy at least 5 years in ER and PR positive breast cancer patients statistically significantly decreased the relapse rates in the adjuvant setting and progress rates in the metastatic setting with an increase in overall survival [11]. TMX is an ER receptor agonist in bone, the cardiovascular system, and the endometrium, but for breast cancer, it shows an antiestrogenic effect. It is also approved as a prophylactic agent in women at high risk of developing breast cancer. Following long-term therapy, it has several side effects including endometrial carcinoma, thromboembolic effect, liver cancer, venous thrombosis, pulmonary emboli, and ocular side effects including retinopathy and corneal opacities [12,13]. According to BCS, TMX is Class II drug with low water solubility (approx. 0.3 mg/L) and has a poor oral bioavailability in the range of 20%–30% due to its precipitation as free base in the acidic environment of stomach and also due to extensive hepatic and intestinal first-pass metabolism [14]. Loading of TMX into polymeric micelle will improve its biopharmaceutical properties by increasing water solubility, chemical stability, and bioavailability. In considering the above-given side effects of TMX, a dose reduction in long-term therapies will be an important progress in the treatment of breast cancer.
Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen
Published in Expert Review of Clinical Pharmacology, 2019
A.B. Sanchez-Spitman, J.J. Swen, V.O. Dezentje, D.J.A.R. Moes, H. Gelderblom, H.J. Guchelaar
In Table 1, all these differences and comparisons are summarized. Tamoxifen is normally formulated as tamoxifen citrate, whilst endoxifen, is orally formulated as z-endoxifen hydrochloride. Elimination half-life of tamoxifen is 5–7 days on average. In contrast, endoxifen’s half-life varies between 49.0 and 68.1 h for the dose of 20 mg and 160 mg [23], respectively. Also, minor difference in Tmax and Cmax have been reported. While tamoxifen has a longer Tmax (4–7 h), endoxifen as z-endoxifen hydrochloride requires a shorter time to reach Tmax (2–4 h). Also, differences in Cmax values are reported: when a 20 mg single dose of tamoxifen is administered a Cmax value of 40 ng/ml is reached [48], whilst a single dose of 20 mg and 160 mg of z-endoxifen hydrochloride reaches Cmax of 64.8 and 635 ng/ml, respectively [23].