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Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Brexpiprazole (Rexulti) Pharmacology Podcast

Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Eric Christianson, PharmD; Pharmacology Expert and Clinical Pharmacist

Education, Health & Fitness, Medicine

5716 Ratings

🗓️ 8 December 2022

⏱️ 16 minutes

🧾️ Download transcript

Summary

Brexpiprazole (Rexulti) is a second generation antipsychotic. I discuss its pharmacology, adverse effects, drug interactions, and more in this podcast episode.



I like to associate brexpiprazole with aripiprazole. They have a lot of overlapping characteristics, particularly in relation to the adverse effect profile.



Brexpiprazole tends to have a low incidence of metabolic adverse effects which makes it a nice selection for patients who have diabetes, hypercholesterolemia, or who are overweight.



CYP3A4 and CYP2D6 are the two primary enzymes that break down brexpiprazole. I discuss the pharmacogenomic considerations associated with this medication.

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.

0:05.7

Thank you so much for listening today. Head on over to real life pharmacology.com. We've got that

0:12.1

free 31 page PDF. It is a study guide on the top 200 drugs. No-brainer, just simply an email. We will get you access to that. Great if you're taking

0:24.0

board exams or going through pharmacology classes or just want a refresher and you're out in clinical

0:29.2

practice. So again, go check that out. RealLife Pharmacology.com. If you subscribe there with simply an

0:35.8

email, you'll get access to that free resource.

0:40.1

All right, let's get into the drug of the day today, and this is by request.

0:45.7

The drug is Brexpiprosol.

0:48.9

Brand name of this medication is Rexalti, and this medication is a second generation antipsychotic so from a mechanism of action

1:00.1

standpoint understand that antipsychotics will have action on dopamine receptors and specifically

1:08.5

dopamine two receptors.

1:12.0

Now, Brexprizol varies a little bit compared to most traditional antipsychotics in its mechanism of action.

1:21.7

So it is a partial agonist or has partial agonist activity for serotonin 1A receptors.

1:33.2

In addition, it's got partial agonist activity to those D2 receptors.

1:39.7

So again, this is agonist activity.

1:42.1

So partial agonist activity means so partial agonist activity,

1:48.1

means it stimulates that receptor to a certain extent, but also prevents or can help reduce the action of full agonist on those dopamine receptors.

2:00.0

So it can kind of limit the activity in being a partial agonist.

2:06.1

It also has some antagonist activity at 5HT2A receptors.

2:12.6

Again, 5HT stands for serotonin.

2:16.8

Just kind of another way to abbreviate that.

2:19.5

So if you see that in the literature, that's what that's referring to.

...

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