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Chemical Compound Review:

Nizoral 1-[4-[4-[[(2R,4R)-2-(2,4- dichlorophenyl)-2...

Synonyms: Brizoral, Fungoral, Ketoderm, Ketozole, Sebazole, ...

Morita, K. et al., Powlin, S.S. et al., Schnorr, J.A. et al., Poelma, F.G. et al., Neumann, H.A. et al.

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Disease relevance of ketoconazole

Treatment of pityrosporum folliculitis with ketoconazole (R 41400) [1].

High impact information on ketoconazole

Using only the in vitro assessment with the criteria of steroid biosynthesis inhibition, four of nine compounds were correctly identified in the testis explant assay (17beta-E2, KETO, FLUT, and HALO) [2].
These results suggest that MCZ, but not KCZ, has inducing activity for hepatic cytochrome P-450-dependent oxidative metabolism of steroids and xenobiotics, in addition to its known inhibitory activity [3].

Analytical, diagnostic and therapeutic context of ketoconazole

KTCZ exposure alone drove a 3-fold increase in serum LH concentrations (P < 10(-3)) and a 2.5-fold rise in FSH secretion (P = 0.015), as assessed by high-specificity immunoradiometric assays [4].
The addition of concentrations of TC above the CMC in the perfusion solution resulted in a reduction of the absorption rate of GF and KE [5].

References

Treatment of pityrosporum folliculitis with ketoconazole (R 41400). Neumann, H.A., Berretty, P.J. Mykosen. (1981) [Pubmed]
Ex vivo and in vitro testis and ovary explants: utility for identifying steroid biosynthesis inhibitors and comparison to a Tier I screening battery. Powlin, S.S., Cook, J.C., Novak, S., O'Connor, J.C. Toxicol. Sci. (1998) [Pubmed]
Effects of antimycotics on hepatic steroid metabolism. Morita, K., Ono, T., Shimakawa, H. J. Pharmacobio-dyn. (1988) [Pubmed]
Aromatization mediates testosterone's short-term feedback restraint of 24-hour endogenously driven and acute exogenous gonadotropin-releasing hormone-stimulated luteinizing hormone and follicle-stimulating hormone secretion in young men. Schnorr, J.A., Bray, M.J., Veldhuis, J.D. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
Intestinal absorption of drugs. III. The influence of taurocholate on the disappearance kinetics of hydrophilic and lipophilic drugs from the small intestine of the rat. Poelma, F.G., Breäs, R., Tukker, J.J. Pharm. Res. (1990) [Pubmed]

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