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Endocrine Disorders, Contraception, and Hormone Therapy during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Methyltestosterone is a synthetic derivative of testosterone, the primary endogenous androgen. More than a dozen female infants were born to women treated with methyltestosterone during pregnancy, and they all had varying degrees of virilization of the external genitalia (clitoral enlargement and labioscrotal fusion) (Grumbach and Ducharme, 1960; Schardein, 2000). Paralleling other androgenic agents, clitoral enlargement may be induced by exposure to methyltestosterone throughout the postembryonic period, but labioscrotal fusion seems restricted to the period between the 8th and 13th weeks of gestation, and the degree of virilization appears dose related. Successful surgical correction of the defects associated with virilization is available. Sexual maturation seems normal, while menarche in virilized girls seems close to the median, following a healthy course.
Drugs Affecting the Endocrine System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: Methyltestosterone is used in the treatment of various diseases, such as endometriosis, hereditary angioedema, and fibrocystic breast disease. Nevertheless, Methyltestosterone is absolutely contraindicated during pregnancy due to the risk of developing female pseudohermaphroditism. Therefore, women planning to become pregnant should stop taking Methyltestosterone first.
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
Hypomania, mania, increased violence, and suicide attempts preceded by acute or extended use of AAS have been observed in several case reports (Conacher and Workman, 1989; Freinhar and Alverez., 1985; Schulte, Hall, and Boyer, 1993; Thiblin and Parlklo, 2002; Thiblin, Runeson, and Rajs, 1999; Weiss, Bowers, and Mazure, 1999), but there is mixed support from cross-sectional, experimental, and especially longitudinal research for a causal relationship between these psychiatric states, problematic behaviors, and AAS use. Only four blinded randomized controlled trials have indicated an increase in psychiatric symptoms, aggression, or adverse overt behavior (Hannan et al., 1991; Kouri et al., 1995; Pope, Kouri, and Hudson, 2000; Su et al., 1993), most of these trials used a very low or ambiguous standard of abnormal behavior (it must be noted that many “manic” symptoms are merely indicators of elevated mood, even well-being, and these may be regarded as benefits, rather than as untoward consequences, of AAS use), and still other studies have found no effect at all. In a recent study, Pope, Kouri, and Hudson (2000) found greater increases in “manic symptoms” in participants using 600 mg/wk of testosterone cypionate, but concluded that very few, only 4.0 percent, became markedly hypomanic. Su et al. (1993) investigated the effects of two doses (40 and 240 mg/day) of methyltestosterone and found a 10.0 percent incidence of mania or hypomania in normal, non-weight-training male volunteers. The greater incidence in manic or hypomanic states in the Su et al. study using methyltestosterone is of some clinical significance; an often overlooked factor is the chemical structure of the specific AAS used, as some have argued based on the animal literature that specific AAS chemistry is likely to be an important determinant of the specific psychiatric and psychological effects that remain has not been studied sufficiently in humans (Clark, Harrold, and Fast, 1997; Martinez-Sanchis, 1996).
International Society for the Study of Women's Sexual Health Clinical Practice Guideline for the Use of Systemic Testosterone for Hypoactive Sexual Desire Disorder in Women
Published in Climacteric, 2021
Sharon J. Parish, James A. Simon, Susan R. Davis, Annamaria Giraldi, Irwin Goldstein, Sue W. Goldstein, Noel N. Kim, Sheryl A. Kingsberg, Abraham Morgentaler, Rossella E. Nappi, Kwangsung Park, Cynthia A. Stuenkel, Abdulmaged M. Traish, Linda Vignozzi
Testosterone preparations, specifically intramuscular (IM), subcutaneous implants, and oral formulations (methyltestosterone 1.25–2.5 mg or testosterone undecanoate 40 mg), often in combination with estrogen therapies, have been evaluated in RCTs with relatively few participants and followed for relatively short periods of time. The longest duration placebo-controlled trial (24 months) included 331 subjects [110,111]. These preparations are not commonly used currently. IM administration is associated with wide excursions of serum testosterone concentrations well beyond physiological levels; subcutaneous implants occasionally yield markedly elevated testosterone levels with erratic release over time and difficulty locating for removal if necessary. Oral testosterone undecanoate was associated with unpredictable absorption and blood levels in the male range, even at the lowest dose studied [103].
An update on the available and emerging pharmacotherapy for adults with testosterone deficiency available in the USA
Published in Expert Opinion on Pharmacotherapy, 2021
Eliyahu Kresch, Mehul Patel, Thiago Fernandes Negris Lima, Ranjith Ramasamy
Oral formulations of testosterone offer the benefit of convenience, ease of use, and avoidance of transference and painful injections. Despite these advantages, early oral formulations have not been widely adopted as a viable treatment option due to high-dose requirements as a result of significant inactivation by first-pass liver metabolism [63]. Initial attempts at a viable oral testosterone option lead to the development of 17 α-methyltestosterone; however, this medication led to significant hepatotoxicity [64,65]. Subsequent attempts involved fatty-acid esterification into testosterone undecanoate which bypassed first pass portal metabolism by way of intestinal lymphatic absorption [66,67]. Although testosterone undecanoate avoided hepatotoxicity, absorption was highly dependent on fat consumption and led to variable responses [68,69]. For these reasons, oral testosterone has not been widely adopted.
The role of hormones in muscle hypertrophy
Published in The Physician and Sportsmedicine, 2018
Julius Fink, Brad Jon Schoenfeld, Koichi Nakazato
The major AAS used by athletes can be divided into three groups [30]: Testosterone derivatives (T, Methyltestosterone, Methandrostenolone, Chlorodehydromethyltestosterone, Fluoxymesterone, Boldenone): The compounds in this group are known to induce fast strength and muscle gains but show a high rate of aromatization. Due to the high water retention caused by aromatization, they are mainly used in bulking cycles for quick mass gains.Dihydrotestosterone derivatives (Stanozolol, Oxandrolone, Oxymetholone, Mesterolone, Methenolone, Drostanolone): Even though most of these compounds are highly androgenic, they have a high binding affinity to the androgen receptor and are potent strength and muscle mass builders. Due to the DHT structure, these compounds cannot aromatize to estrogen. Therefore, these compounds are often used for cutting cycles and pre-contest.Nandrolone derivatives (Nandrolone, Trenbolone): Compounds in this group show the highest anabolic to androgenic ratio and have strong muscle building effects. However, administration of nandrolone derivatives can result in elevated progestogenic activity. The use of this group of AAS is versatile and is used for both bulking and cutting cycles.