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Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Doxepin Pharmacology

Real Life Pharmacology - Pharmacology Education for Health Care Professionals

Eric Christianson, PharmD; Pharmacology Expert and Clinical Pharmacist

Education, Health & Fitness, Medicine

5716 Ratings

🗓️ 9 January 2020

⏱️ 14 minutes

🧾️ Download transcript

Summary

Doxepin is under the class of tricyclic antidepressants. It can inhibit the reuptake of serotonin and norepinephrine.



In addition to the serotonin and norepinephrine reuptake inhibition mechanism, doxepin also has antihistamine type effects.



Because of the anticholinergic activity of doxepin, it is recommended to avoid this medication in the elderly, particularly at high doses.



Be aware that anticholinergics like doxepin can reduce the benefit of dementia medications.



CYP2D6 is an important enzyme in the metabolism of doxepin and drugs like bupropion that inhibit CYP2D6 can increase the concentrations of doxepin.

Transcript

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0:00.0

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

0:06.8

and I thank you so much for listening today. Hopefully you can pick up some practice pearls and good medication education here.

0:15.8

So today I'm going to cover doxapin. So doxapin, brand name Cinequin, that's an older brand name,

0:24.9

and there's also a newer brand name product, Cilinor as well, which is a lower dose medication

0:32.0

intended for sleep. They are both forms of doxapin there.

0:47.5

In my mind, way for a drug company to make a little bit more money off the sale of Cillinor, the low dose that they've studied for sleep.

0:52.3

But anyway, we do have, this medication is a TCA.

0:55.1

So it's a tricyclic antidepressant.

1:01.0

So mechanistically, how this drug works, you know, it's going to be like your amatryptolines,

1:06.5

your nortriptolines, which you can go back and listen to those podcasts in the past. But essentially, it's inhibition of serotonin and norophenephinectake,

1:12.4

which in the end increases the amount in that synapse

1:18.2

and available for activation and physiological effects.

1:23.5

So that's the primary class that doxapin comes from.

1:28.8

However, it does have other mechanisms of action,

1:34.2

and one of those primary mechanisms of action,

1:38.1

other than the TCA effect with the SNR- or with the SNRI type effect,

1:46.3

is it can block histamine.

1:54.8

Now, if you remember from previous episodes, that blockade of histamine can lead to a couple of different effects.

1:56.1

So one is anticholinergic, so we'll talk about that in adverse effects.

2:07.3

But antihistamine effects can cause sedation and sleepiness.

2:13.5

So antihistamine, good for itch, good for insomnia.

2:18.4

And that is the situation where I've seen this medication used the most.

...

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