Can microdosing cause heart problems?

According to Kelan Thomas, PharmD, MS, BCPS, BCPP,  

Associate Professor of Clinical Sciences at Touro University California College of Pharmacy,

“Given the current evidence for psychedelic “microdosing,” the risks may outweigh the benefits for many people….”

How Sway?

“After spending some time researching this topic in detail, I became concerned about the potential risk of valvular heart disease (VHD) due to chronic psychedelic-induced changes of heart valve cells via serotonin 2B receptor (5HT2B) activation.”

“...This is because there is compelling theoretical evidence to suggest prolonged and repeated microdosing may cause valvular heart disease (VHD), and only weak survey evidence that it provides the benefits microdosers typically seek, such as enhanced cognition, or relief from depression and anxiety.”

“psychedelic-induced changes of heart valve cells”

This is a valid concern, lets unpack this together.

Let’s ask a few important questions about the Microdosing and heart problems.

What drugs trigger 5ht2B activation?

What conditions trigger 5ht2B activation?

What is 5ht2B activation ?

How does cardiac binding differ from CNS binding?

5ht 2B receptor activation.

Psilocybin STRONGLY binds to the 5ht2a receptor in humans, it also shows binding affinities to other serotonin receptors such as the 5ht2B.

The graphics below answer all the questions surrounding these concerns about drug induced 5ht2B heart changes. Sources at the bottom of the page, the video highlights the concerns medical professionals had about Phen fen.

Phen Fen & 5ht2b activation.

 
 
 

Mouse models use 100% bioavailabile psilocybin (IV). In humans, psilocybin is 53% orally bioavailable. The half life of Psilocybin is 50 minutes. Shrooms need to go through first pass metabolism before exerting effects on the central nervous system (CNS). How do ALL these things come to lay in creating a regiment?

To settle the argument once and for all:

It’s important to ask your own questions.

Please check out these papers that assisted me with this “new” discovery.

“ Functional Consequence of Serotonin/5-HT2B Receptor Signaling in Heart.” https://pubmed.ncbi.nlm.nih.gov/12810....

“Phospholipase C-linked receptors regulate theATP-sensitive potassium channel by means of phosphatidylinositol 4,5-bisphosphate metabolism” https://www.pnas.org/doi/10.1073/pnas...

“Evidence for Possible Involvement of 5-HT2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications” https://www.ahajournals.org/doi/10.11...