An update on ketamine and its two enantiomers as rapid-acting antidepressants

@article{Zhang2018AnUO,
  title={An update on ketamine and its two enantiomers as rapid-acting antidepressants},
  author={Kai Zhang and Kenji Hashimoto},
  journal={Expert Review of Neurotherapeutics},
  year={2018},
  volume={19},
  pages={83 - 92}
}
ABSTRACT Introduction: Depression is one of the most disabling diseases worldwide. Approximately one-third of depressed patients are treatment-resistant to the currently available antidepressants and there is a significant therapeutic time lag of weeks to months. There is a clear unmet need for rapid-acting and more efficacious treatments. (R,S)-ketamine, an old anesthetic drug, appears now to be going through a renaissance. Areas covered: This paper reviews recent literature describing the… Expand
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47 Citations
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Paper Mentions

Interventional Clinical Trial
The Effect of S-ketamine for Patients Undergoing Electroconvulsive Therapy (ECT)
This study will determine the effectiveness and safety of S-Ketamine in depression patients undergoing electroconvulsive therapy.  
ConditionsDepression, Bipolar, Depression, Unipolar, Major Depressive Disorder, (+1 more)
InterventionDrug
West China Hospital
August 2020 - January 2021

47 Citations

Citation Type

Citation Type

Rapid‐acting antidepressant ketamine, its metabolites and other candidates: A historical overview and future perspective
  • K. Hashimoto
  • Medicine
  • Psychiatry and clinical neurosciences
  • 2019
TLDR
The author reviews the historical overview of the antidepressant actions of enantiomers of ketamine and its major metabolites norketamine and hydroxynorketamines and discusses the other potential rapid‐acting antidepressant candidates to compare them with ketamine. Expand
A historical review of antidepressant effects of ketamine and its enantiomers
TLDR
Clinical studies of (R)-ketamine in humans are now underway by Perception Neuroscience Ltd, and accumulating evidence from preclinical studies show that (R)ketamine has greater potency and longer lasting antidepressant effects than (S)-ketamines in animal models of depression, and that (S)ketamines has fewer detrimental side effects than either (R,S)- ketamine or (S-ketamine. Expand
Antidepressant Actions of Ketamine and Its Two Enantiomers
TLDR
Recent findings on the antidepressant actions of two enantiomers of ketamine are discussed, including (R,S), which has been reported to have a greater potency and longer-lasting antidepressant effects than (S)-ketamine in rodent models of depression. Expand
Molecular mechanisms of the rapid-acting and long-lasting antidepressant actions of (R)-ketamine.
TLDR
The author reviews the mechanisms of the antidepressant actions of the enantiomers of ketamine and its metabolites, (S)-norketamine and (2R,6R)-hydroxynorketamines (HNK) and discusses the role of the brain-gut-microbiota axis and brain-spleen axis in stress-related psychiatric disorders, such as depression. Expand
Ketamine as an antidepressant: overview of its mechanisms of action and potential predictive biomarkers
TLDR
An overview of ketamine with regard to pharmacology/pharmacokinetics, toxicology, the current state of clinical trials on depression, postulated antidepressant mechanisms and potential biomarkers for predicting response to and/or monitoring of therapeutic outcome with ketamine is provided. Expand
Repurposing of Drugs-The Ketamine Story.
  • J. Das
  • Medicine, Chemistry
  • Journal of medicinal chemistry
  • 2020
TLDR
Repurposing of ketamine for treating TRD provided a new understanding of the pathophysiology of depression-a paradigm shift from monoamine to glutamatergic neurotransmission, thus making it a unique tool to investigate the brain and its complex neurocircuitries. Expand
An update on NMDA antagonists in depression
TLDR
The present review aims to summarize and provide an update on published preclinical data evaluating the antidepressant efficacy of various NMDA antagonists and their mechanisms of action based on published results from clinical studies. Expand
Ketamine: Leading us into the future for development of antidepressants
TLDR
With the hippocampus being a key target for ketamine's beneficial antidepressant effects, behavioral and neurochemical effects of drugs that act selectively on the hippocampus due to the preferential location of their receptor targets are examined. Expand
Rapid-Acting Antidepressants.
TLDR
The preclinical and clinical literature strongly suggests that rapid-acting antidepressants are the current focus of antidepressant drug discovery, and promising clinical findings exist for several compounds including ketamine and other NMDA receptor antagonists, scopolamine, and psilocybin. Expand
Esketamine for treatment resistant depression
TLDR
Both esketamine’s approval for use in TRD and longer-term safety data may position it preferentially above racemic ketamine, although factors such as cost and monitoring requirements may limit its use. Expand
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