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Medical Consequences of Anabolic Steroids
Published in John Brick, Handbook of the Medical Consequences of Alcohol and Drug Abuse, 2012
James Langenbucher, Thomas Hildebrandt, Sasha J. Carr
The partial synthesis in the 1930s of abundant, potent, stable, oil-based testosterone esters permitted the characterization of the hormone’s effects, so that Kochakian (1937) was able to show that testosterone raised nitrogen retention (a mechanism central to anabolism) in the dog, after which Charles Kenyon’s group (Kenyon et al., 1938) was able to demonstrate both the anabolic and androgenic effects of testosterone propionate in eunuchoidal men, boys, and women. The period of the early 1930s to the 1950s has been called the “Golden Age of Steroid Chemistry” (Schwarz, Onken, and Schubert, 1999), and work during this period progressed quickly. The class of oil-based testosterone esters developed then that are still familiar include testosterone propionate, phenylpropionate, caproate, isocaproate, cypionate, enanthate, undecanoate, and many others. They differ principally in rapidity of action; esterases require more time to cleave away long acid chains (e.g., cypionate) than shorter ones (e.g., propionate).
p, p′-DDE and HCB: Mechanisms of Toxicity to Fetal and Embryonic Mammalian Cells
Published in Rajesh K. Naz, Endocrine Disruptors, 2004
Michael A. Edelbrock, Martha J. Fernstrom, Kandace J. Williams
Nevertheless, the effects of chronic environmental DDE exposure to the human fetus are not well characterized. Several researchers have demonstrated, however, that prenatal exposure to DDE in mammalian models can result in developmental defects. In particular, feminization of male rats exposed to DDE has been measured by a reduction in the anogenital distance and increased retention of thoracic nipples.12,13 Other developmental effects of DDE exposure to prenatal rats include reduced sperm production, delayed onset of puberty, and reduced seminal vesicle, prostate, and testicular weight.12,14 The ability of DDE to act as an antiandrogen has been experimentally demonstrated by both in vitro and in vivo studies.12,15 In these experiments, DDE was demonstrated to bind to the androgen receptor (AR) with high affinity and competitively inhibit the expression of androgen-regulated genes. Other experiments have shown that DDE is antiandrogenic by its ability to attenuate the effects of testosterone propionate.16
Synthesis, Enzyme Localization, and Regulation of Neurosteroids
Published in Sheryl S. Smith, Neurosteroid Effects in the Central Nervous System, 2003
The AASs, like the endogenous androgens, have a four-ringed backbone structure with 19 carbon atoms (Figure 6.1). Modifications of this androstane backbone have been introduced to prolong the metabolic half-life and thus the efficacy of synthetic AASs. Three main classes of AASs have been described.2,3 The first, used primarily as injectable compounds, is derived from esterification of the 17P-hydroxyl group of testosterone and includes testosterone propionate and testosterone cypionate. Esterification retards absorption and prolongs the duration of action after injection of the hormone by slowing its release into circulation. Testosterone esters can be hydrolyzed into free testosterone, reduced to 5α-dihydrotestosterone, an androgen with higher biological activity at brain androgen receptors than testosterone,20-22 or aromatized to estrogens21 (for review, see Kochakian and Yesalis22). Molecules that have been 5α-reduced cannot be metabolized into estrogens but may be metabolized into other androgenic compounds such as 3a-androstanediol.
Testosterone for women: certainties and uncertainties
Published in Climacteric, 2023
Surprisingly, one of the first applications of testosterone pellets was for the treatment of vulvovaginal atrophy in postmenopausal women. Greenblatt reported treating oophorectomized and postmenopausal women aged 19–53 years with testosterone proprionate [5]. He observed that ‘In 2 menopausal patients with castrate smears in whom larger doses (400 mg) were employed it was noted that testosterone propionate had an estrogenic effect’ [5]. He also described patients having improvement in their appetites and general well-being [5]. In 1950, Salinger reported that testosterone pellet therapy exerted a proliferative effect on the vaginal epithelium [6]. He reported that administration of intramuscular testosterone proprionate at a total dose of 50 mg to 12 postmenopausal women, aged 54–85 years with atrophic vaginitis, restored their vaginal tissue to premenopausal appearance, with increased superficial vaginal epithelial cells and an increase in the number of large glycophilic cells [6].
An overview on performance and image enhancing drugs (PIEDs) confiscated in Italy in the period 2017–2019
Published in Clinical Toxicology, 2021
Sara Odoardi, Serena Mestria, Giulia Biosa, Valeria Valentini, Sofia Federici, Sabina Strano Rossi
Quantitative analysis was performed only for selected compounds, as described in the materials and methods section. The quantitative determinations showed discrepancies between the declared and the actual amount present in the preparation. For androgen anabolic steroids AASs, the quantitative content of the single compound was always lower than the one stated on the label. Nevertheless, these preparations generally consisted of mixtures of various AASs esters. Testosterone propionate concentration ranged from 20 to 100 mg/mL, testosterone decanoate from 10 to 100 mg/mL, testosterone enanthate from 10 to120 mg/mL. Stanozolol was detected in tablets at 1–10 mg, and in injectable depot preparation at 10–100 mg/mL. Methandienone was detected at 3–5 mg in tablets and methenolone at 1–5 mg. Sildenafil concentrations in the tablets ranged between 70 and 120 mg per table, while it was always reported as 100 mg preparations. Ephedrine amount ranged from 22 to 50 mg per capsule/tablet. In some of them its presence was not declared, other products reported its dosage at 25 mg.
Bioidentical hormones
Published in Climacteric, 2021
F. Z. Stanczyk, H. Matharu, S. A. Winer
Because compounding pharmacies are not regulated by the FDA, hormonal products prepared by them can vary substantially from batch to batch, as shown in one of our studies described earlier25. Thus, women might be potentially overdosed or underdosed when using those products. In another one of our studies28, healthy postmenopausal women were treated for 2 weeks with a custom-compounded testosterone preparation, either a gel containing 1 mg of testosterone or a lozenge containing 1 mg of testosterone propionate. The serum testosterone levels observed in these women after treatment were substantially above the upper reference range for women, and in some women they were in the upper male range. Obviously, such high testosterone levels present for prolonged periods may lead to deleterious effects.