• N&PD Moderators: Skorpio | thegreenhand

Can anyone explain the low peak plasma conc of vynase

aced126

Bluelighter
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May 18, 2015
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http://www.ncbi.nlm.nih.gov/pubmed/18991468

In that study they take some measurements to determine pharmacokinetic properties of lisdexamphetamine.

They administer a 70mg oral dose, but measure that average peak plasma concentration is 58ng/ml.

There's ~5000ml blood in humans, and 10^6 nanograms in 1 mg, so that works out to be 0.29mg peak concentration. This seems very low. If I iv administered even 10 times less than the oral dose, I would still have 7mg in my blood instantly, several times higher than the oral peak plasma concentration. This occured 1 hour after administration.

If this is because most of the lisdex has been metabolised to dex already (at t=1 hour), then what even is the point of having the prodrug substitution if it has barely any amphetamine to release after only 1 hour? I've got to be missing something
 
The lisdexamphetamine is rapidly absorbed and the transformation to d-amp occurs in the blood via RBCs. The rate of how the RBCs either take in or transform the lisdexamphetamine is the rate limiting step and any lisdexamphetamine not being involved is rapidly eliminated.
 
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