Ketoconazole Pharmacology

Ketoconazole is an imidazole antifungal that works by inhibiting fungal cytochrome P450 14α-demethylase, an enzyme essential for ergosterol synthesis, which disrupts fungal cell membrane integrity.

Common adverse effects of ketoconazole include nausea, vomiting, abdominal pain, and elevated liver enzymes, with hepatotoxicity being a notable concern.

Ketoconazole carries a boxed warning for severe hepatotoxicity, including cases of liver failure and death, and should not be used as a first-line treatment for fungal infections when other safer antifungals are available.

Another boxed warning highlights ketoconazole’s potential to prolong the QT interval, increasing the risk for life-threatening ventricular arrhythmias such as torsades de pointes.

Ketoconazole is a strong inhibitor of CYP3A4 and can cause significant drug interactions by increasing serum concentrations of medications metabolized by this pathway, including statins, certain benzodiazepines, and some antiarrhythmic.

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Top 200 Drugs Podcast – Medications 151-155

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On this episode of the Top 200 Drugs Podcast, I cover medications 151-155. This podcast includes; cefuroxime, ketoconazole, pregabalin, esomeprazole, and ipratropium/albuterol.

Cefuroxime is a 2nd generation cephalosporin that has a very similar bacterial coverage profile to amoxicillin. It has significant gram positive coverage.

Ketoconazole is an azole antifungal medication. It is well known for causing hepatotoxicity as well as interactions via CYP3A4.

Pregabalin has a lot of similarities with gabapentin. It can be used fo various pain syndromes such as neuropathy and fibromyalgia.

Esomeprazole is a PPI and has a similar profile to omeprazole. It inhibits CYP2C19 and has a few notable interactions that I cover in this episode.

Ipratropium and albuterol is a combination of a short acting anticholinergic and short acting beta agonist.

Be sure to check out our free Top 200 study guide – a 31 page PDF that is yours for FREE!

Support The Podcast and Check Out These Amazing Resources!

NAPLEX Study Materials

BCPS Study Materials

BCACP Study Materials

BCGP Study Materials

BCMTMS Study Materials

Meded101 Guide to Nursing Pharmacology (Amazon Highly Rated)

Guide to Drug Food Interactions (Amazon Best Seller)

Pharmacy Technician Study Guide by Meded101