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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Estradiol benzoate is a prodrug ester of estradiol, a naturally occurring hormone that circulates endogenously within the human body. Estradiol is the most potent form of all mammalian estrogenic steroids and acts as the major female sex hormone. Following absorption, the ester is cleaved, resulting in the release of estradiol bioidentical to endogenous estradiol (1). Indications for the use of estradiol (esters) are presented in Chapter 3.126 Estradiol.
The menopause
Published in Michael J. O’Dowd, The History of Medications for Women, 2020
In a brief look at the hormonal therapy for the ‘change of life’ Wilson wrote that ‘Investigation of the therapeutic uses of estrogens followed close upon Doisy’s historic discovery of these hormones in 1923. Curiously, the initial research was carried out largely in agricultural colleges with a hopeful view towards encouraging the sex life of chickens’. Wilson’s own initial experiments, in the late 1920s, were carried out with a crude extract made from dried sheep ovaries. Estrogen became available in the early 1930s and the German preparation, estradiol benzoate, that was relatively side-effect free, allowed patients to enjoy the benefits of estrogen therapy without discomfort. Some clinicians nicknamed it the ‘cadillac of hormones’, but unfortunately the preparation had to be given on an on-going basis by intramuscular injections. Natural conjugated estrogens became available shortly after the outbreak of World War Two. They were prepared from mares’ urine and soon the conjugated estrogens became available in convenient tablet form.
Reproductive Neuroendocrine Effects of Neuropeptide Y and Related Peptides
Published in Craig A. Johnston, Charles D. Barnes, Brain-Gut Peptides and Reproductive Function, 2020
Alterations in plasma levels of gonadal steroids also affect the concentration of NPY in the hypothalamus. Crowley et al. (1985) examined the effects of bilateral OVX followed by treatment with estrogen alone or the combination of estrogen and progesterone on NPY levels in several brain regions. Injection of 50 μg of estradiol benzoate significantly decreased NPY levels in the ME 48 h later. Injection of a single dose of progesterone (2.5 mg) at 10:00 AM into OVX and estrogen-treated animals induced a significant increase in NPY levels in the ME 1 h later followed by a gradual decline. The pattern of NPY alterations in the ME after progesterone administration was similar to that for LHRH. These changes in the levels of both peptides preceded the afternoon rise in plasma LH. A significant decline in NPY concentration was detected in the interstitial nucleus of the stria terminalis and in the arcuate nucleus following estrogen treatment, while no changes were observed in the preoptic, periventricular and ventromedial nuclei. Progesterone treatment further decreased NPY levels in the interstitial nucleus of the stria terminalis and in the ventromedial nucleus while transient declines were seen in the preoptic and arcuate nuclei (Crowley et al., 1985).
Long-term reproductive effects of benzo(a)pyrene at environmentally relevant dose on juvenile female rats
Published in Drug and Chemical Toxicology, 2023
Ana Carolina Casali Reis, Bárbara Campos Jorge, Beatriz Rizzo Paschoalini, Jéssica Nogueira Bueno, Julia Stein, Suyane da Silva Moreira, Beatriz de Matos Manoel, Glaura Scantamburlo Alves Fernandes, Hamilton Hisano, Arielle Cristina Arena
To evaluate a possible estrogenic activity of BaP, immature female rats on PND 21 (Odum et al.1997, Arena et al.2008) received 0.1 µg/kg/day of BaP for 3 consecutive days, by oral gavage. The vehicle was administered as a negative control, while estradiol benzoate (β-Estradiol 3-Benzoate, Sigma; 0.4 mg/kg/day) was used as a positive control for estrogenicity (Figure 1). Twenty-four hours after the final dose, the females were weighted and anesthetized with sodium pentobarbital (40 mg/kg, i.p.). Uteri were excised, trimmed free of fat, pierced, and blotted to remove fluid. The body of the uterus was cut just above its junction with the cervix and the junction of the uterine horns with the ovaries (Odum et al.1997). Wet uterus weights were determined and expressed as relative weights (wet uterus weight/body weight × 100).
Rosuvastatin exposure in female Wistar rats alters uterine contractility and do not show evident (anti)estrogenic effects
Published in Drug and Chemical Toxicology, 2022
Jorge Willian Franco de Barros, Patrícia Villela e Silva, Gustavo Venâncio da Silva, Katiussia Pinho da Silva, Cibele dos Santos Borges, André Mueller, Lethícia Valencise, André Sampaio Pupo, Wilma De Grava Kempinas
At weaning, on PND 21, female pups were randomly distributed among six experimental groups (one pup per litter for each group; n = 7/group), keeping the same mean body weight for each group. Primarily, experimental groups were treated with saline (Control); or rosuvastatin (purchased at a commercial pharmacy, Farmácia Cruz Vermelha, Botucatu/SP, Brazil) at two different doses: 3 or 10 mg/kg/d, diluted in saline. Additionally, the experimental groups received the treatment associated or not with 0.4 mg/kg/d of estradiol benzoate (β-estradiol 3-benzoate, Sigma, St. Louis, MO), diluted in corn oil. Groups that did not receive estradiol benzoate were treated with corn oil. The treatment was performed daily and by oral administration (gavage – First the saline or rosuvastatin gavage; Then the corn oil or estradiol gavage) from PND 21 to 23. The organization of the experimental groups for the uterotrophic assay is presented in Table 1.
Stress and steroid interaction modulates expression of estrogen receptor alpha in the brain, pituitary, and testes of immature Gallus gallus domesticus
Published in Stress, 2021
Kalpana Baghel, Rashmi Srivastava
One-day old chicks were taken and reared for 2 months under laboratory conditions, then randomly assigned into four groups (n = 8 each). First group served as a control (C) in which 0.9% saline was administered intraperitoneally for 12 days, food and water was provided ad libitum. The second group was food restricted (FR) for 9 h/day from sixth day till the last day of experiment. The third and fourth groups were administered with estradiol benzoate (EB) (Sigma-Aldrich, St. Louis, MO) at a dose (0.5 mg/100g body weight/day) intraperitoneally for 12 days continuously. But, the fourth group was treated with EB followed by food restriction (EB + FR) of 9 h/day from sixth day till last day of experiment. After 12 days of experimental duration, the body weights of all birds were measured and blood samples were collected from the wing vein in a heparinized syringe. Plasma was isolated and kept in −20 °C for further hormonal analysis of corticosterone and estradiol. Four chicks from each group were anesthetized using sodium phenobarbital and perfused with 0.02 M phosphate-buffered saline (PBS) followed by Zamboni’s fixative through left ventricle of the heart. Brain, pituitary and testes were excised and post fixed in Zamboni’s fixative for 24–48 h for histology and immuno-fluorescent localization.