Ketoconazole Pharmacology

Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Eric Christianson, PharmD; Pharmacology Expert and Clinical Pharmacist

Education, Health & Fitness, Medicine

5 • 716 Ratings

🗓️ 10 July 2025

⏱️ 14 minutes

🔗️ Recording | iTunes | RSS

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Summary

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.

Transcript

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0:00.0	Hey, all, welcome back to the real-life pharmacology podcast. I'm your host, pharmacist, Derek Christensen.
0:05.3	Thank you so much for listening today. As always, go check out real-life pharmacology.com. We got that
0:11.7	free 31-page PDF on the top 200 drugs. Simply an email. We'll get you access to that.
0:17.8	And of course, support our sponsor, metadata.101.com slash store. We've got tons of
0:22.8	resources there to help pharmacists studying for board exams, books, all sorts of different content
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0:33.4	slash store, support the sponsor and obviously help support this podcast keep it free and
0:39.2	available for all to benefit from all right the drug of the day today is ketoconazole
0:44.4	brand name is nizoril as you could expect from the ending ketoconazole this is an
0:51.4	azole antifungal so it's use typically going to be used for treating fungal infections.
0:58.9	I can't say I've really seen it used for anything else other than that in clinical practice.
1:05.6	And its use is pretty rare and I'll discuss the reasons for that coming up here.
1:11.3	But there are a couple off-label uses that have been reported, advanced prostate cancer,
1:17.1	as well as Cushing's syndrome.
1:19.9	So we have an oral formulation as well as a topical formulation.
1:23.6	So topical formulation we can utilize for cutaneous candidiasis, certain types of dermatitis, tini infection.
1:33.9	And I want to talk on the mechanism of action a little bit here.
1:37.6	So essentially as an antifungal, this medication alters the permeability of the fungal cell wall. So it blocks
1:48.1	fungal cytochrome P-450. In addition to that, it also inhibits biosynthesis of triglycerides and
1:56.8	phospholipids that are necessary for the fungus to grow and survive.
2:03.2	Now, I alluded to the off-label use of Cushing's syndrome.
2:07.8	So this medication actually inhibits some adrenal enzymes that are responsible for cortisol
	...

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