Split View Cite Permissions Share Abstract Nonsuppressed levels of testosterone are seen in up to a quarter of transgender women on gender-affirming feminizing hormonal treatment. For all analyses, the significance level was set at 5%. [157], Spironolactone is relatively safe in acute overdose. The issue is systemic. [96][97][272], Spironolactone is also known by its developmental code names SC-9420 and NSC-150339. [62] Although apparently effective, not all cases of female-pattern hair loss are dependent on androgens. [95][97] Spironolactone has poor water solubility, and for this reason, only oral and topical formulations have been developed; other routes of administration such as intravenous injection are not used. Careers, Unable to load your collection due to an error. [280], Spironolactone has been studied in the treatment of rosacea in both males and females. [159] Physicians must be careful to monitor potassium levels in both males and females who are taking spironolactone as a diuretic, especially during the first twelve months of use and whenever the dosage is increased. [128][129] The medication reportedly has no birth control effect. Sociodemographic and clinical characteristics of transgender adults in Australia. 12 Spironolactone is valued for its ability to feminize patients in a way that matches the assumptions of a predominately cisgender, male, white, and heterosexual medical community: by deflating your muscles, softening your dick, stunting your hair growth, and shrinking your balls. [270] The formulation was eventually changed to a micronized formulation with particle sizes of less than 50g, which resulted in approximately 4-fold increased potency. [192][196][197], In response to the antimineralocorticoid activity spironolactone, and in an attempt to maintain homeostasis, the body increases aldosterone production in the adrenal cortex. [182] Although useful as an antiandrogen in women, who have low testosterone levels compared to men,[183][184] spironolactone is described as having relatively weak antiandrogenic activity. Cyproterone is highly effective at lowering endogenous total testosterone concentrations in transfeminine individuals undergoing feminising hormone therapy. [medical citation needed], Unlike with some other diuretics, potassium supplementation should not be administered while taking spironolactone, as this may cause dangerous elevations in serum potassium levels resulting in hyperkalemia and potentially deadly abnormal heart rhythms. Other parameters of interest included serum oestradiol concentration, potassium, urea and creatinine, haemoglobin, liver function (alanine transaminase (ALT)), oestradiol valerate dose and blood pressure. [57][58] Oftentimes, for women treating acne, spironolactone is prescribed and paired with a birth control pill. Spironolactone is used to treat heart failure, high blood pressure (hypertension), or hypokalemia ( low potassium levels in the blood). In transfeminine individuals wishing to inhibit androgenic physical characteristics, choice of anti-androgen agent is a common clinical scenario faced by patients and treating clinicians alike. [123] Conversely, in studies of healthy men given high-dose spironolactone, gynecomastia occurred in 3 of 10 (30%) at 100mg/day, in 5 of 8 (62.5%) at 200mg/day, and in 6 of 9 (66.7%) at 400mg/day, relative to none of 12 controls. Correspondence should be addressed to A S Cheung: Received 2019 Jun 4; Accepted 2019 Jun 11. transgender persons, transsexualism, gender identity, gender dysphoria, androgens. Development of androgen- and estrogen-responsive bioassays, members of a panel of human cell line-based highly selective steroid-responsive bioassays. [275][276][277] It was found to be better than placebo in terms of symptom relief following three months of treatment. In this retrospective cross-sectional analysis, transfeminine individuals undergoing feminising hormone therapy with oestradiol achieved the lowest total testosterone concentrations with additional cyproterone acetate when compared to additional spironolactone or oestradiol alone. [102][119][121][122] At low doses, the rate is only 5 to 10%,[122] but at high doses, up to or exceeding 50% of men may develop gynecomastia. Savidou I, Deutsch M, Soultati AS, Koudouras D, Kafiri G, Dourakis SP. Why? The data with spironolactone are limited, but this is a relatively nontoxic therapy that can be considered for treatment of persistent alopecia following cancer therapy. Improve quality of life. Nevertheless, spironolactone is still the drug of choice, for reasons that remain a bit of a mystery. [99] In rare cases, hyponatremia, hyperkalemia, or hepatic coma may occur in individuals with severe liver disease. There are a number of limitations to this retrospective cross-sectional analysis inherent in the design and small numbers of individuals. Its an unfortunate fact of transgender health care (especially in the United States) that marginalized communities and women are often forced to take whatever treatment they can, and the providers working with them are generally unable to devote the necessary time and energy to helping them determine the right treatments for their goals and lifestyles. [16] Spironolactone is dethioacetylated into canrenone. [275][276] Gynecomastia was observed in about 5% of people. [211][212][213][8][214][215][216][217], The bioavailability of spironolactone when taken by mouth is 60 to 90%. A linear mixed model was also fitted to compare total testosterone concentrations between the three treatment groups, adjusting for corresponding oestradiol concentrations, doses and age. Anti-androgens such as cyproterone acetate or spironolactone are commonly added to oestradiol, lowering or blocking the effects of testosterone to aid development of feminising physical characteristics. [280] This effect of spironolactone was determined to be independent of its antimineralocorticoid actions. Serum oestradiol concentrations achieved were no different between the groups and were generally between 250 and 350pmol/L on a relatively high median dose of oral oestradiol valerate of 6mg daily. Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. On univariate analysis, the cyproterone group had significantly lower serum total testosterone concentrations than the spironolactone group and the oestradiol-alone group. Each participant received oral estradiol valerate 4 mg/day combined with anti-androgen, spironolactone 100 mg/day or cyproterone acetate 25 mg/day, depending on which group they were randomized to. [8][11] Spironolactone and its metabolite 7-thiospironolactone show very low or negligible affinity for sex hormone-binding globulin (SHBG). Oral estrogen. On univariate analysis, the cyproterone group had significantly lower total testosterone concentrations (0.8nmol/L (0.61.20)) compared with the spironolactone group (2.0nmol/L (0.99.4), P=0.037) and oestradiol alone group (10.5nmol/L (4.917.2), P<0.001), which remained significant (P=0.005) after adjustments for oestradiol concentration, dose and age. [240][241][242] These structural modifications of progesterone confer increased oral bioavailability and potency,[243] potent antiandrogenic activity, and strongly reduced progestogenic activity. [151][152][153] Because it is an antiandrogen, however, spironolactone could theoretically have the potential to cause feminization of male fetuses at sufficient doses. This kind of specialized care has been hugely beneficial. [30] Spironolactone is also used to treat Bartter's syndrome due to its ability to raise potassium levels. Bethesda, MD 20894, Web Policies A typical dose of spironolactone is 100 mg per day, though doses utilized range . Feminizing hormone therapy can: Improve psychological and social well-being. Most of the side effects of spironolactone are dose-dependent. [163] In any case, spironolactone has been found to reduce the bioavailability of oral estradiol, which could be due to induction of estradiol metabolism via CYP3A4. Whilst both anti-androgen agents, cyproterone acetate and spironolactone, have been shown to lower serum testosterone concentrations if added to oestradiol treatment, there is little evidence to guide the superiority of one anti-androgen over another (6). Until our capitalist medical system changes, trans women will continue to get substandard care. Further prospective studies are required. [78][55], There is insufficient clinical evidence to compare the effectiveness of spironolactone with other antiandrogens for female-pattern hair loss. [45] In accordance with the preceding, antiandrogens are highly effective in the treatment of the aforementioned androgen-dependent skin and hair conditions. Most doctors working with transgender patients typically have a set regimen in mind, geared toward adjusting their patients testosterone and estrogen levels to within certain set parameters. Spironolactone tablets are indicated for treatment of NYHA Class III-IV heart failure and reduced ejection fraction to increase survival, manage edema, and reduce the need for hospitalization for heart failure. [56] These irregularities include metrorrhagia (intermenstrual bleeding), amenorrhea (absence of menstruation), and breakthrough bleeding. [151][156], A 2019 systematic review found insufficient evidence that spironolactone causes birth defects in humans. [57] Likewise, a 10-year observational study found that the incidence of depression in 196transgender women taking high-dose spironolactone in combination with an estrogen was less than 1%. [79][103] For example, about 20% of women experienced menstrual irregularities with 50 to 100mg/day spironolactone, whereas about 70% experienced menstrual irregularities at 200mg/day. Federal government websites often end in .gov or .mil. [78] In addition, some clinical research has found that flutamide is more effective than spironolactone in the treatment of acne. [61] As an example, spironolactone has been reported to reduce symptoms of acne in males. [101][124][131][188] That is, it inhibits steroidogenic enzymes, or enzymes involved in the production of steroid hormones. Unfortunately, thats not an option in our current prevailing medical system, where there are incentives on even the most high-minded of practitioners to treat individual patients as problems to solve and boxes to check rather than as complete and complex human beings with unique desires and goals. [18][237] It was originally thought to be hydrolyzed by PON1, but this was due to contamination with PON3. [99] Hyperkalemia in these people can present as a normal anion-gap metabolic acidosis. [285][286] It has also been studied in bulimia nervosa in women, but was not found to be effective.[287]. [8][9] The major metabolites of spironolactone are 7-thiomethylspironolactone (7-TMS), 6-hydroxy-7-thiomethylspironolactone (6-OH-7-TMS), and canrenone (7-desthioacetyl-6-spironolactone). Not every doctor defers to their patients in this way, instead trusting (often outdated) research that fails to recognize the agency or specificity of individual transgender patients. and transmitted securely. [57] However, this was based on low- to very-low-quality evidence. By doing so, the drug can reduce some of the characteristic male traits (like facial hair and male-pattern baldness). [40] Spironolactone should not be used to treat primary aldosteronism in pregnancy due to its antiandrogen-related risk of teratogenicity in male fetuses. This disconnect illuminates how often transition-related care fails to account for the ways in which trans women seek to live full and varied lives. [31], Spironolactone has antiandrogenic activity. It also includes taking the hormone estrogen. [101][124][131][188] Spironolactone and/or its metabolites have been found in vitro to weakly inhibit a broad array of steroidogenic enzymes including cholesterol side-chain cleavage enzyme, 17-hydroxylase, 17,20-lyase, 5-reductase, 3-hydroxysteroid dehydrogenase, 11-hydroxylase, 21-hydroxylase, and aldosterone synthase (18-hydroxylase). Notably, although cyproterone has been used internationally for many years, it is not available in the US due to rare case reports of hepatotoxicity in men receiving high doses for prostate cancer (9). The serum total testosterone concentrations for the three groups are shown in Fig. This dose is certainly higher than that used in the European Network for Investigation of Gender Incongruence (4mg) (18), yet oestradiol concentrations achieved are lower than the recommended concentrations (367734pmol/L) in international guidelines (3). [45][46] In demonstration of this, women with complete androgen insensitivity syndrome (CAIS) do not produce sebum or develop acne and have little to no body, pubic, or axillary hair. [219][222][223] The relationship between a single dose of spironolactone and plasma levels of canrenone, a major active metabolite of spironolactone, has been found to be linear across a dose range of 25 to 200mg spironolactone. [226][227] In accordance, a study of high-dosage spironolactone treatment found no change in steroid binding capacity related to SHBG or to corticosteroid-binding globulin (CBG), suggesting that spironolactone does not displace steroid hormones from their carrier proteins. Reasons for the variable effects of spironolactone and cyproterone on serum testosterone concentrations may well be related to differing mechanisms of action. [8][98], Spironolactone is a potent antimineralocorticoid. [56] However, since often the condition treated (acne or hair loss) is merely a cosmetic concern, whereas the potential side effects pose serious health risks, a healthy person shouldn't take this drug. [54][79], Spironolactone is a moderate antiandrogen. In the first few months on this dosage, she experienced a number of unpleasant side effects, ranging from a plummeting sex drive to painful headaches, memory loss, dietary disruptions, and such difficulty focusing that she found it hard to read. Read more here. Another friend, M Zavos, is a transsexual woman and an artist based in Arizona. Sonneveld E, Jansen HJ, Riteco JA, Brouwer A, van der Burg B. Before [192][193] It is notable that spironolactone has been found in vitro to act as a weak inhibitor of 17-hydroxysteroid dehydrogenase 2, an enzyme that is involved in the conversion of estradiol into estrone. [102] As with breast enlargement caused by spironolactone in women, gynecomastia due to spironolactone in men is often although inconsistently accompanied by breast tenderness. [176][224], Little or no systemic absorption has been observed with topical spironolactone. For a while I had thought that this was just what HRT was likethat Im not going to be able to read anymore, and Im not going to have a sex drive. Than spironolactone in the treatment of the side effects of spironolactone and its metabolite 7-thiospironolactone show very low or affinity... 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