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Pattern hair loss: Pathogenesis, clinical features, diagnosis, and management
Published in Jerry Shapiro, Nina Otberg, Hair Loss and Restoration, 2015
In 1997, the Food and Drug Administration (FDA) approved finasteride for use in the United States at a dose of 1 mg/day in men with AGA. Finasteride is the most common treatment approach for male AGA. It is a synthetic 4-azasteroid compound that is a specific inhibitor of type II 5α-reductase. 5α-Reductase type II is an intracellular enzyme that converts testosterone into dihydrotestosterone (DHT), resulting in significant decreases in serum and tissue DHT concentrations [106–112]. Finasteride does not have any hormonal properties in itself [106,107] and has no estrogenic, antiestrogenic, or progestational effects. A study by Roberts et al. [111] confirmed that finasteride 1 mg daily was the optimal dose, with 1 mg and 5 mg superior to lower doses such as 0.2 mg daily. The daily 5 mg dose was not more efficacious than the 1 mg dose.
Synthesis, Enzyme Localization, and Regulation of Neurosteroids
Published in Sheryl S. Smith, Neurosteroid Effects in the Central Nervous System, 2003
In some of the early work on benz[e]indenes, phenanthrene analogues, containing flexible side chains in place of the D ring, were tested and found to have very weak GABA-potentiating activity. In an effort to more systematically map the structural requirements associated with the D ring and necessary for strong biological activity, Covey and colleagues64 recently prepared several 17α-aza-D-homosteroids (Figure 5.1C). One of the eight synthesized azasteroids possessed properties in both [35S]TBPS displacement and electrophysiological assays equivalent to natural ste-roids.64 Several other azasteroids possessed reasonable electrophysiological activity but were weak displacers of TBPS binding. The basis for this discrepancy is not clear, as natural GABA-potentiating steroids correlate well in the two assays.
Preparation of topical bimatoprost with enhanced skin infiltration and in vivo hair regrowth efficacy in androgenic alopecia
Published in Drug Delivery, 2022
Laxman Subedi, Prashant Pandey, Jung-Hyun Shim, Ki-Taek Kim, Seung-Sik Cho, Kyo-Tan Koo, Beum Joon Kim, Jin Woo Park
The US Food and Drug Administration (FDA) has approved oral 5α-reductase inhibitors, including finasteride and dutasteride, and topical minoxidil, for immune (areata alopecia) as well as hormonal (androgenic alopecia) related alopecia, respectively. Finasteride is a synthetic 4-azasteroid compound that acts as a competitive and specific inhibitor of dihydrotestosterone receptors. Thus, it is contraindicated in women who are currently pregnant or hope to become pregnant in the future (Sallout & Al Wadi, 2009). In addition, many patients prefer to avoid oral medications due to possible adverse effects, such as decreased libido and erectile dysfunction in men (Kumar et al., 2011). Topical minoxidil is commonly used as an off-label treatment for male- and female-pattern baldness. Minoxidil increases blood flow to the hair follicles by dilating the arteries, thereby stimulating the production of growth factors from dermal papilla cells and activating the dermal papilla beta-catenin pathway, resulting in the induction and prolongation of the anagen phase, and stimulating the telogen-to-anagen transition (Choi et al., 2018). Topical minoxidil cannot prevent hair loss but may accelerate hair growth. Thus, it is not effective in all patients. Many patients consider topical minoxidil to be an outdated and ineffective treatment. Additionally, daily long-term use of minoxidil is poorly tolerated by patients as the hair becomes sticky and thus feels unclean; scalp irritation and itching also occur, mainly caused by propylene glycol (a key ingredient of topical minoxidil) (Suchonwanit et al., 2019; BinJadeed et al., 2021). Therefore, there is increasing demand for drugs that have few side effects and high efficacy.
Impact of formulation design and lyophilisation on the physicochemical characteristics of finasteride nanosystems
Published in Journal of Microencapsulation, 2023
Malik Muhammad Irfan, Shefaat Ullah Shah, Kifayat Ullah Shah, Nicolas Anton, Ysia Idoux-Gillet, Guillaume Conzatti, Kifayat Ullah Shah, Elise Perennes, Thierry Vandamme
Finasteride (FNS) belongs to azasteroid (4-aza-3-oxosteroid) compounds and is considered as the most potent 5α reductase inhibitor. It is effective against both benign prostatic hyperplasia and male pattern baldness or androgenic alopecia. Following the biopharmaceutical classification system, FNS is a class II therapeutic agent that had poor solubility and high permeability. FNS is a lipophilic drug that works by inhibiting the type II 5 α reductase enzyme, which prevents testosterone from being converted into its precursor dihydrotestosterone. The major side effects associated with the oral intake of FNS are erectile dysfunction, decreased libido and mental impairment.