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Papers of the Week

Papers: 22 May 2021 - 28 May 2021

Human Studies, Pharmacology/Drug Development

2021 May 21


Chiral Pharmacokinetics and Metabolite Profile of Prolonged-release Ketamine Tablets in Healthy Human Subjects.


Hasan M, Modess C, Roustom T, Dokter A, Grube M, Link AS, Rey H, Adler S, Meissner K, Siegmund W
Anesthesiology. 2021 May 21.
PMID: 34019627.


The anesthetic ketamine after intravenous dosing is nearly completely metabolized to R- and S-stereoisomers of the active norketamine (analgesic, psychoactive) and 2,6-hydroxynorketamine (potential analgesic, antidepressant) as well as the inactive dehydronorketamine. Oral administration favors the formation of 2,6-hydroxynorketamines via extensive presystemic metabolism. The authors hypothesized that plasma exposure to 2,6-hydroxynorketamines relative to the psychoactive ketamine is greater after prolonged-release ketamine tablets than it is after intravenous ketamine.