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Adnexal Diseases
Published in Ayşe Serap Karadağ, Lawrence Charles Parish, Jordan V. Wang, Roxburgh's Common Skin Diseases, 2022
Hasan Aksoy, Jordan V. Wang, Ayşe Serap Karadağ
Hormonal therapies (i.e., antiandrogens) can be helpful in women with acne, regardless of whether hyperandrogenism is present. The most commonly used agents are combined oral contraceptive pills and spironolactone. Spironolactone can cause irregular menses, breast tenderness, headaches, nausea, and hypotension. Hyperkalemia is rare, and monitoring serum potassium is not indicated in low-risk individuals.
Respiratory, endocrine, cardiac, and renal topics
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Spironolactone is an aldosterone antagonist. It has weak diuretic action and increases potassium reabsorption. Because of this potassium-sparing effect, it is often associated with other diuretics, such as thiazides or furosemide (see above).
Spironolactone
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Spironolactone is a synthetic corticosteroid with potassium-sparing diuretic, antihypertensive, and antiandrogen activities. Spironolactone competitively inhibits adrenocortical hormone aldosterone activity in the distal renal tubules, myocardium, and vasculature. Spironolactone is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis, of primary hyperaldosteronism and hypertension. Off-label uses of spironolactone involving its antiandrogenic activity include hirsutism, female pattern hair loss, and adult acne vulgaris. It is also frequently used in medical gender transition (1). Topical spironolactone shows antiandrogenic effects by competitive inhibition of dihydrotestosterone receptors, and has been used to treat acne vulgaris, idiopathic hirsutism and androgenic alopecia (3).
Current and emerging pharmacotherapy for the management of hypertrophic cardiomyopathy
Published in Expert Opinion on Pharmacotherapy, 2023
Akiva Rosenzveig, Neil Garg, Shiavax J. Rao, Amreen K. Kanwal, Arjun Kanwal, Wilbert S. Aronow, Matthew W. Martinez
Spironolactone, a nonselective mineralocorticoid receptor antagonist used in the management and treatment of heart failure and hypertension, has shown clinical efficacy in the reduction of cardiac remodeling as a consequence of HCM [76]. Spironolactone binds to cytoplasmic mineralocorticoid receptors functioning as an aldosterone antagonist with antifibrotic activity. Spironolactone mediated reduction in cardiac fibrosis has shown clinical prowess in the management of heart failure. Limiting the aldosterone facilitated cardiac remodeling leads to decreased fibrosis, mortality, morbidity, and risk of sudden deaths in patients with HCM [77]. Spironolactone mean absorption time varies from 2.6 to 4.3 hours, with a mean half-life of about 1.4 hours. Spironolactone’s distribution is more than 90% bound to plasma proteins, demonstrating increased bioavailability with food intake [78]. Excretion of the drug primarily takes place in urine and bile. A study by Harbin Medical University enrolled 616 patients and monitored the effects of spironolactone on cardiac remodeling, LV function, and renal function. After 1 month and 1 year follow-ups, it was found that early low-dose spironolactone could prevent adverse late-stage cardiac remodeling as well as prevent heart failure [76]. Investigators at the Xinhau Hospital are currently administering a multicenter, randomized, open and control label study to better quantify the relationship between spironolactone administration and reversal of fibrosis as well as cardiac function and arrhythmia [79].
Efficacy and safety of finerenone for treatment of diabetic kidney disease: current knowledge and future perspective
Published in Expert Opinion on Drug Safety, 2022
Vincenzo Marzolla, Marco Infante, Andrea Armani, Manfredi Rizzo, Massimiliano Caprio
Steroidal MRAs have been used for decades in the management of hypertension, primary aldosteronism and heart failure [84–86]. Of note, they show a higher distribution in kidneys rather than in cardiovascular tissues [21]; differently, finerenone shows a balanced distribution between the heart and kidney [22]. The pharmacokinetic properties of finerenone are also different from those of steroidal MRAs; in addition, finerenone does not generate biologically active metabolites [22,23]. Unique and distinct pharmacokinetic properties of finerenone may confer to the molecule novel clinical indications, based on distinct mechanisms of action and pharmacological distribution. Spironolactone is indeed recommended as fourth-line therapy for the treatment of resistant hypertension [87]. Unfortunately, the potential risk of hyperkalemia has greatly limited the use of spironolactone in patients with resistant hypertension and heart failure [88]. Data from the FIDELIO-DKD and FIGARO-DKD trials reported the ability of finerenone to decrease the risk of CKD progression, independently from the glycemic control and insulin therapy, with additional benefits in reducing CVD progression, indicating that such non-steroidal MRA clearly confers renal and cardiovascular protection in patients with CKD and T2DM [25,80].
Pulmonary fibrosis secondary to COVID-19: a narrative review
Published in Expert Review of Respiratory Medicine, 2021
Suzana Erico Tanni, Alexandre Todorovic Fabro, André de Albuquerque, Eloara Vieira Machado Ferreira, Carlos Gustavo Yuji Verrastro, Márcio Valente Yamada Sawamura, Sergio Marrone Ribeiro, Bruno Guedes Baldi
Spironolactone is an anti-hypertensive and anti-androgenic drug that may present potential benefits in COVID-19, based on its following actions: 1) to increase the circulating levels of ACE-2 and prevent the entry of SARS-CoV-2 into the cells; 2) to block the mineralocorticoid receptor; 3) antiandrogenic activity through downregulation of transmembrane serine protease 2 (TMPRSS2); 4) anti-inflammatory, antioxidant, antifibrotic and antiviral properties [89,90]. ACE-2 and TMPRSS2 are key regulators for SARS-CoV-2 cell entry, and aldosterone is a mineralocorticoid receptor activator and potentially associated with hyperinflammatory response and fibrosis [87,88]. Additionally, a previous study in rats demonstrated that spironolactone may be beneficial in reducing inflammatory responses in the early phase of ARDS [91]. Therefore, spironolactone may lastly have a potential role in the hyper-inflammatory response associated with severe COVID-19, and in the prevention or attenuation of post-COVID-19 pulmonary fibrosis. Future trials are warranted to assess the potential benefits of spironolactone in such scenarios in COVID-19.