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Urinary tract disorders
Published in Henry J. Woodford, Essential Geriatrics, 2022
Patients with distant metastases have a poor prognosis, with mean survival times of between 24 and 48 months.147 Anti-androgen treatment (e.g. bilateral orchidectomy or gonadorelin analogues) is indicated. Around 75% of men will have some symptomatic relief from this (e.g. reduced bone pain).147 Adverse effects of anti-androgen treatments include fatigue, depression, erectile dysfunction and hot flushes. They are also associated with an increased risk of osteoporosis. Other effects of long-term treatment may include an increased risk of vascular disease and diabetes.150 The addition of the chemotherapy drug, docetaxel, to antiandrogen therapy may have a survival benefit for selected men aged over 70.151 The antiandrogen drugs, abiraterone or enzalutamide, may be used in men with prostate cancer who are unsuitable for other chemotherapy. Surgery (radical prostatectomy) and radiotherapy may be appropriate in some men with high-grade tumours.
Mesotherapy: Dutasteride, Minoxidil, Vitamins
Published in Rubina Alves, Ramon Grimalt, Techniques in the Evaluation and Management of Hair Diseases, 2021
David Saceda, Claudia Bernárdez
Some antiandrogens have been proven to be effective in stopping this mechanism and also to revert hair thinning. Peripheral antiandrogens are the most used drugs, especially the inhibitors of 5-alpha-reductase. Oral finasteride, which inhibits type II enzyme, is an FDA approved drug to treat AGA. Oral dutasteride inhibits both types, I and II enzymes, and its use in AGA is out-of-label. The use of both drugs has been related to side effects such as sexual impotence, ejaculation disorders, and decrease of libido. Although evidence-based medicine has not demonstrated a clear correlation between the use of these drugs and those side effects, they are the main concern for many patients and the main cause to refuse them.
Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Anti-androgens (or androgen antagonists) inhibit the binding of testosterone, DHT and other androgens to the Androgen Receptors in target tissues which are located in all areas of the body that depend on androgens. Examples include the prostate, male genital skin, the seminal vesicles, fatty tissues, and breast tissue, as well as the hypothalamus and pituitary glands. Anti-androgens bind to the AR, creating a ligand-AR complex that is unable to bind to, or elicit a response at, the DNA response element, so androgen-dependent gene transcription and protein synthesis is inhibited. Thus, anti-androgens block the tropic effect of all androgens, not only peripherally (e.g., in the prostate) but also centrally (e.g., in the hypothalamus and pituitary gland). They are typically used in combination with GnRH analogues to reduce the initial “tumor flare”, and also the effects of androgens produced by the adrenal glands that are not under Luteinizing Hormone control. Therefore, anti-androgens are an important class of therapeutic agents for men with hormonally responsive prostate cancer but are also used to treat noncancer conditions such as benign prostatic hyperplasia (BHP), seborrhea, hirsutism, acne, and androgen-associated alopecia. Also, research has suggested that ARs may be involved in the progression of triple-negative breast cancer, and so anti-androgens have been investigated in this context.
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.
The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism
Published in Expert Review of Clinical Pharmacology, 2021
Giovanni Grandi, Maria Chiara Del Savio, Fabio Facchinetti
Anti-androgens can affect each step of the molecular action of androgens. It was demonstrated that NGM permits green fluorescent protein AR transport into the nucleus, but less efficiently than with natural ligands. In a cell line well-known as a useful tool for studying androgen and anti-androgen actions, it was observed in competitive studies that the half-maximal inhibition (Ki) of NGM (4.2 + 0.561078 M) was close to that of cyproterone acetate (CPA) (6.6 + 0.861078 M), which is the gold standard for hyperandrogenism treatment. If we consider the dosage of NGM and its intracellular concentration in target tissue, this Ki is compatible with a biological effect of NGM on AR. Moreover, these data show that NGM and NGMN decreased AR transcriptional activity (24%), although less efficiently than that observed with CPA at the same concentration (47%) (Figure 4) [15].