"Ketoconazole Shampoo: Effect of Long-Term Use in Androgenic Alopecia", Pierard-Franchimont et al, Dermatology 1998;196:474-477.
"...Left untreated, androgen-dependent alopecia progressively deteriorates. This was found in the Androgenetic Alopecia subgroup using the nonmedicated shampoo alone. In contrast, both present studies concur to show an unequivocable effect of a 2% KCZ shampoo on hair variables affected by Androgenetic Alopecia. Hair density and size, and proportion of anagen follicles were all improved. Although the number of subjects was limited in the second study, results obtained compare with minoxidil. It has been stated that medications capable of maintaining the existing hair population should be regarded as effective treatments for Androgenetic Alopecia. The present data suggest that KCZ should enter this group of drugs".
"Ketocazole as an adjunct to finasteride in the treatment of androgenetic alopecia in men".
Hugo Perez BS.
California College of Podiatric Medicine, 371 Columbus Avenue, 94133, San Francisco, CA, USA
Dihydrotestosterone (DHT) binding to androgen receptors (AR) in hair follicles is commonly accepted as the first step leading to the miniaturizing of follicles associated with androgenetic alopecia (Androgenetic Alopecia). Testosterone is converted to DHT by the enzyme 5alpha-reductase. Finasateride a 5alpha-reducase inhibitor blocks the production of DHT and is currently used to treat Androgenetic Alopecia. The inhibition is not complete but a reduction of DHT systemically and in the scalp is accomplished. Ketoconazole has been clinically shown to be effective in the treatment of Androgenetic Alopecia. In this paper, evidence is presented to support the hypothesis that ketoconazole 2% shampoo has a local disruption of the DHT pathway. It is proposed that using ketoconazole 2% shampoo as an adjunct to finasteride treatment could lead to a more complete inhibition of DHT and thus better treat Androgenetic Alopecia.
PMID: 14729013 [PubMed - as supplied by publisher]
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Hair Loss Study Abstract: Ketoconazole binds to the human androgen receptor.
Title
Ketoconazole binds to the human androgen receptor.
Author
Eil C
Address
Department of Internal Medicine, Naval Hospital, Bethesda, Maryland.
Source
Horm Metab Res, 24: 8, 1992 Aug, 367-70
Abstract
Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections. Based on these potent effects on gonadal function in vivo as well as previous work in vitro demonstrating affinity of ketoconazole for receptor proteins for glucocorticoids and 1,25(OH)2 vitamin D3 and for sex steroid binding globulin (SSBG), the binding of ketoconazole to human androgen receptors (AR) in vitro was also examined. Ketoconazole competition with [3H]methyltrienolone (R1881) for androgen binding sites in dispersed, intact cultured human skin fibroblasts was determined at 22 degrees C. Fifty percent displacement of [3H]R1881 binding to AR was achieved by 6.4 +/- 1.8 (SE) x 10(-5) M ketoconazole. Additional binding studies performed with ketoconazole in the presence of increasing amounts of [3H]R1881 showed that the interaction of ketoconazole with AR was competitive when the data were analyzed by the Scatchard method. It should be noted, however, that the dose of ketoconazole required for 50% occupancy of the androgen receptor is not likely to be achieved in vivo, at least in plasma. Finally, androgen binding studies performed with other imidazoles, such as clotrimazole, miconazole, and fluconozole, revealed that in this class of compounds only ketoconazole appears to interact with the androgen receptor. Ketoconazole appears to be the first example of a non-steroidal compound which binds competitively to both SSBG and multiple steroid hormone receptors, suggesting that the ligand binding sites of these proteins share some features in common.
Language of Publication
English
Unique Identifier
92406209
