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Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Leflunomide Pharmacology

Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Eric Christianson, PharmD; Pharmacology Expert and Clinical Pharmacist

Education, Health & Fitness, Medicine

5716 Ratings

🗓️ 25 February 2021

⏱️ 12 minutes

🧾️ Download transcript

Summary

On this episode, I discuss leflunomide pharmacology. It is classified as a DMARD and is primarily used in rheumatoid arthritis.



Leflunomide carries a boxed warning for hepatoxicity. LFTs must be monitored with its use.



Leflunomide can inhibit CYP2C8 which plays an important role in pioglitazone metabolism. Concentrations of pioglitazone can go up on account of this interaction.



TB screening should be done prior to beginning the immunosuppressant leflunomide.

Transcript

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0:00.0

Hey all, welcome back to the Real Life Pharmacology podcast. I am your host, pharmacist, Derek Christensen.

0:06.4

Thank you so much for listening today. As always, go check out Real Life Pharmacology.com.

0:13.1

Snag your free Top 200 study guide. It's a 31-page PDF. And I really highlighted a lot of my clinical practice pearls and a lot of things

0:23.9

that just happen actually out in the real world when managing and following medications.

0:31.7

So go snag that for free simply for subscribing at real-life pharmacology.com. With that, let's get into the drug of the

0:41.1

day today. That is going to be leflunamide. Brand name of this medication is Arava. And I will say that I

0:51.7

don't see this medication used a ton anymore.

0:55.5

It is primarily used in clinical practice for rheumatoid arthritis,

1:01.0

and it is an oral demarred.

1:04.4

That's disease-modifying antiromatic drug.

1:09.3

Now, why you don't see this medication used, it does have some significant

1:14.3

warnings associated with it, and I'll mention those coming up here. But primarily, if you're

1:21.3

going to see an oral demarred being used, you're going to see methotrexate, hydroxychloroquine, and potentially sulfosalazine used as well,

1:32.1

typically, before we go to the flunamide. Now, there may be rare cases where we go to it for one

1:39.2

reason or another, but those three drugs along potentially with the biologics are definitely growing in popularity,

1:48.0

which you're probably seeing less and less of leflunamide being used for rheumatoid arthritis.

1:54.8

There are a couple of off-label uses like CMV, said amygolovirus, BK virus, and those really probably only occur in transplant patients.

2:06.7

And personally, I've never seen an actual case where they've been used for that off label.

2:12.9

But if you see a quirky off label use use that could be happening out there.

2:19.7

Mechanistically, this drug blocks perimidine synthesis,

2:24.3

which ultimately leads to an inhibition of cellular proliferation,

2:30.3

and ultimately the end goal, particularly in rheumatoid arthritis, we're looking to reduce inflammation and inflammatory responses.

...

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