Urology
Gozie Offiah, Arnold Hill in RCSI Handbook of Clinical Surgery for Finals, 2019
Metastatic disease➣ Aim is palliation➣ Hormonal therapy might be considered in androgen dependant tumours: Luteinizing hormone-releasing hormone (LHRH) agonist.➣ Side effects include hot flushes, lethargy, osteoporosis, cardiovascular dysfunction and loss of sexual function.2. Antiandrogens.➣ Side effects include gynaecomastia and nipple tenderness.
The chemistry of the Body
Gail S. Anderson in Biological Influences on Criminal Behavior, 2019
These drugs are not without side effects. All reduce testosterone levels, and because testosterone is a critical hormone in many functions, its loss can cause many health issues. Anti-androgen drugs are frequently used medically in conditions such as prostate cancer, so there are many studies available on the side effects. Anti-androgen drugs reduce bone density and lean body mass, both of which increase the risk of bone fractures. Other side effects include femininization, loss of body hair, and breast development.50 Anti-androgen drugs have also been associated with the development of diabetes and increased risk for metabolic syndrome and cardiovascular disease.51 They cause andropause, the male equivalent of menopause, which results in hot flashes and other unpleasant effects; it can cause depression and, perhaps most concerning, severe mood instability.49
Integrative hyperthermia treatments for different types of cancer
Clifford L. K. Pang, Kaiman Lee in Hyperthermia in Oncology, 2015
Prostate cells without androgen stimulations will undergo apoptosis. Any treatment of androgen activity inhibition may be referred to as androgen deprivation therapy. Deprivation of androgen is primarily through the following strategies: (1) inhibition of testosterone secretion: surgical castration or medical castration (luteinizing hormone–releasing hormone analogs [LHRH-A]). (2) Block combination of androgen with receptor: application of antiandrogen drugs competitively closes the combination of androgen and prostate cells androgen receptor. The combination of the two can achieve the purpose of maximum androgen blockage. Other strategies include inhibition of adrenal gland source androgen synthesis as well as inhibition of the conversion of testosterone to dihydrotestosterone, and so on. Endocrine therapy aims to reduce the concentration of androgen in the body, inhibit adrenal gland source androgen synthesis, inhibit the conversion of testosterone to dihydrotestosterone, and block the combination of androgen with its receptor so as to suppress or control prostate cancer cell growth. Endocrine therapy methods include the following: castration, maximum androgen blockage, intermittent hormonal therapy, neoadjuvant endocrine therapy before radical treatment, and adjuvant endocrine therapy.
The cellular and molecular effects of the androgen receptor agonist, Cl-4AS-1, on breast cancer cells
Published in Endocrine Research, 2018
Mamoun Ahram, Ebtihal Mustafa, Shatha Abu Hammad, Mariam Alhudhud, Randa Bawadi, Lubna Tahtamouni, Faisal Khatib, Malek Zihlif
In recent years, attention has been directed toward alternative therapeutic targets. One such target is androgen receptor (AR). In fact, androgen therapy was a strategy of treating breast cancer decades ago till the emergence of targeted therapeutics such as SERMs9 and inhibitors of androgen aromatization into estrogen.11 There has recently been a revival of utilizing antiandrogen therapy due to a number of reasons. First of all, breast cancer is a heterogeneous disease with multiple subclasses, one of which is characterized by active AR signaling pathway and, hence, known a luminal AR and is represented by molecular apocrine breast cancer.9 In addition, AR is expressed in all subtypes of breast cancer, although the extent of expression varies according to the type.12 For example, up to 90% of luminal breast cancer is found to be AR-positive, relative to 32% of basal-like breast cancer.12 In fact, AR expression is associated with better prognosis of the disease12,13, although it has been suggested that it can also act as an oncogene in ER-negative breast cancers.14,15 It has been shown that treatment of TNBC cells with AR antagonists reduces cell proliferation.16 On the other hand, contradictory results have been reported on the effect of AR agonists on breast cancer cells (for review, see11,17). Nevertheless, clinical trials have shown promising results in treating breast cancer patients.18
Emulsions with alkyl polyglucosides as carriers for off-label topical spironolactone – safety and stability evaluation
Published in Pharmaceutical Development and Technology, 2021
Dusan Ilic, Maja Cvetkovic, Marija Tasic-Kostov
Spironolactone is a synthetic steroidal diuretic. As an anti-androgen drug, it has the ability to block DHT receptors and reduce the sebum secretion, which could be crucial in acne therapy (Sato et al. 2006; Chiu and Tsai 2011; Afzali et al. 2012). Its main side effects are dose-dependent and in correlation with its anti-androgen potential. In women, spironolactone may cause irregular menstruation, breast tenderness, gynecomastia, reduced libido, nausea, dizziness, as well as hyperpotassemia and hyponatremia, especially in patients with heart or kidney failure (Vargas-Mora and Morgado-Carrasco 2020). In order to avoid systemic side effects, spironolactone is being used in dermatology as off-label topical acne therapy. Topical skin disease therapy provides a high level of drug at the site of action (Schäfer-Korting et al. 2007; Gupta and Vyas 2012). Off-label drug use in dermatology is more common than in other medical specialties, but those drugs are basically available only as compounded formulations (Sugarman et al. 2002). The choice of a proper vehicle, in terms of physicochemical stability, is often neglected here.
An up-to-date evaluation of darolutamide for the treatment of prostate cancer
Published in Expert Opinion on Pharmacotherapy, 2021
Mohamad Moussa, Lazaros Lazarou, Athanasios Dellis, Mohamed Abou Chakra, Athanasios Papatsoris
Although it is difficult to make an appropriate selection among the novel antiandrogens, darolutamide seems like a reasonable option [41]. Since all novel drugs are similar in terms of clinical benefits, such as improvement in MFS and long-term survival, the selection should be made based on the safety and tolerability profile of the drugs. MFS is high with apalutamide and enzalutamide compared with darolutamide, although with slightly different absolute numbers. However, darolutamide has been proven to have the lowest probability of AEs and overall low incidences of grade 3 AEs [42]. Since it is rather unlikely for comparative studies to take place between the novel antiandrogens, treatment decisions among the available drugs should be based on their respective safety and tolerability profiles.