Itraconazole 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

🗓️ 7 August 2025

⏱️ 11 minutes

🔗️ Recording | iTunes | RSS

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Summary

In this episode, we break down itraconazole—a potent antifungal with a lot of baggage. If you’re a pharmacist, clinician, or student who needs to understand how this drug works and why it can be tricky to use, this episode is for you.

We start with the basics. Itraconazole blocks 14α-demethylase, an enzyme fungi need to make their cell membranes. That disruption kills or slows the fungus. It works against tough bugs like Aspergillus, Histoplasma, and Blastomyces, plus common skin infections.

Side effects? Nausea, liver enzyme elevations, and more seriously, heart failure. Yes, itraconazole has a black box warning for worsening or causing congestive heart failure. If your patient has heart issues, think twice.

Drug interactions are everywhere. Itraconazole is a strong CYP3A4 inhibitor. It can raise levels of drugs like statins, benzos, calcium channel blockers, and immunosuppressants—sometimes to dangerous levels. Don’t co-prescribe without checking.

Transcript

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0:00.0	Hey all, welcome back to the Real Life Pharmacology podcast. I'm your host pharmacist,
0:04.4	Derek Christensen. Thank you so much for listening today. As always, go get the free PDF at
0:10.1	real life pharmacology.com. It is a study guide on the top 200 medications. I lay out some of the most
0:19.0	important things in clinical practice and in real life that you're going to see with those medications. I lay out some of the most important things in clinical practice and in real
0:21.8	life that you're going to see with those medications. A 31 page PDF, absolutely no cost to you,
0:27.3	simply email is all it takes to get access to that. Then we also get you emails out when we've
0:33.6	got new podcasts, new content available for you to benefit from.
0:41.0	All right, with that said, let's get into the drug of the day today.
0:43.6	That is itrikonazole.
0:46.2	Brand name of this medication is sporinox.
0:52.9	Classification is generalized as an antifungal medication.
0:56.8	More specifically, it's what's called an azol antifungal,
1:03.4	which you can probably deduce from the last five letters of the name of the drug,
1:04.1	at trachanazole.
1:08.7	So mechanistically, how do these azol antifungals work, they actually interfere with fungal
1:12.7	cytochrome p-450 activity, which decreases ergosterol synthesis. And if you remember,
1:21.8	ergosterol is an important sterol in fungal cell membrane formation. So essentially it inhibits fungal cell membrane formation.
1:33.6	And that's how it ultimately helps treat infection and kill the fungal infection.
1:41.3	Now what types of fungal infections is this typically used for? It can be used for a
1:47.7	variety of infections. The risk, and I'll talk about that more coming up here, but we've got
1:55.4	some boxed warnings for this medication. And so you really want to make sure that it's a serious infection or it's an
2:03.2	infection that, you know, we don't really have a lot of other good options to treat. So
	...

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