.Pharmacolibrary.Drugs.H_SystemicHormonalPreparationsExclSexHormonesAndInsulins.H02C_AntiadrenalPreparations.H02CA03_Ketoconazole.Ketoconazole

Information

Ketoconazole is a synthetic imidazole antifungal agent primarily used for the treatment of fungal infections. It inhibits fungal steroid synthesis, particularly ergosterol, by blocking the cytochrome P450-dependent enzyme lanosterol 14-α-demethylase. Due to its risk of hepatotoxicity and adrenal insufficiency, oral ketoconazole is largely discontinued or restricted and is now rarely used systemically but still approved in some countries for severe systemic mycoses when other antifungals are unavailable.

Pharmacokinetics

Pharmacokinetic parameters in healthy adult volunteers after single oral dose.

References

1. David, OJ, et al., & Schmouder, RL (2012). Clinical pharmacokinetics of fingolimod. Clinical pharmacokinetics 51(1) 15–28. DOI:10.2165/11596550-000000000-00000 PUBMED:https://pubmed.ncbi.nlm.nih.gov/22149256

2. Harris, RZ, et al., & Padhi, D (2007). Pharmacokinetics of cinacalcet hydrochloride when administered with ketoconazole. Clinical pharmacokinetics 46(6) 495–501. DOI:10.2165/00003088-200746060-00003 PUBMED:https://pubmed.ncbi.nlm.nih.gov/17518508

3. Noh, YH, et al., & Bae, KS (2012). Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers. Clinical therapeutics 34(5) 1182–1194. DOI:10.1016/j.clinthera.2012.04.001 PUBMED:https://pubmed.ncbi.nlm.nih.gov/22534255

Revisions

• 06/2025 initial generated model