Norketamine: Difference between revisions

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'''Norketamine''' is a [[metabolite]] of the [[anesthetic]] drug [[ketamine]]. It is formed in the body after administration of ketamine, and has similar effects to the parent drug. Norketamine is less potent than ketamine, but has a longer half-life.
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== Norketamine ==
[[File:Norketamine.svg|thumb|right|Chemical structure of Norketamine]]
'''Norketamine''' is a [[metabolite]] of the [[anesthetic]] and [[analgesic]] drug [[ketamine]]. It is formed in the body through the process of [[N-demethylation]] by the [[cytochrome P450]] enzyme system, primarily in the [[liver]]. Norketamine retains some of the pharmacological properties of ketamine, contributing to its overall effects.


== Pharmacology ==
== Pharmacology ==
Norketamine acts on the [[central nervous system]] and has been shown to interact with the [[N-methyl-D-aspartate receptor|NMDA receptor]], similar to its parent compound, ketamine. However, it has a lower affinity for the NMDA receptor compared to ketamine. This interaction is believed to contribute to its [[analgesic]] and [[dissociative]] effects.


Norketamine acts as an [[NMDA receptor antagonist]], which means it blocks the action of the [[neurotransmitter]] [[glutamate]] at NMDA receptors. This is thought to be the main mechanism by which it produces its anesthetic effects. Norketamine also has activity at other receptors, including the [[opioid receptor]]s and the [[sigma receptor]]s, which may contribute to its effects.
=== Metabolism ===
The metabolism of ketamine to norketamine occurs primarily in the liver. The enzyme [[CYP3A4]] is mainly responsible for the N-demethylation of ketamine to norketamine. Once formed, norketamine can undergo further metabolism to produce other metabolites, such as [[dehydronorketamine]].


== Metabolism ==
== Clinical Significance ==
Norketamine is considered to have a role in the therapeutic effects of ketamine, particularly in its use as an [[antidepressant]]. The presence of norketamine in the body may prolong the effects of ketamine, contributing to its [[antidepressant]] and [[analgesic]] properties.


Norketamine is formed from ketamine in the body by the action of the enzyme [[CYP3A4]]. This is a major metabolic pathway for ketamine, and the amount of norketamine formed can vary depending on the activity of this enzyme in individual people.
== Research ==
 
Research into norketamine has focused on its potential therapeutic effects and its role in the overall pharmacological profile of ketamine. Studies have investigated its effects on [[pain management]] and its potential use in treating [[depression]].
== Clinical significance ==
 
Norketamine is less potent than ketamine, but because it has a longer half-life, it can contribute to the effects of ketamine administration, particularly during prolonged infusions. It is also possible that norketamine could contribute to the side effects of ketamine, such as hallucinations and other [[psychotomimetic]] effects.
 
== See also ==


== Related pages ==
* [[Ketamine]]
* [[Ketamine]]
* [[Metabolite]]
* [[NMDA receptor]]
* [[Anesthetic]]
* [[Analgesic]]
* [[NMDA receptor antagonist]]
* [[Antidepressant]]


[[Category:Drugs]]
[[Category:Anesthetics]]
[[Category:Anesthetics]]
[[Category:Metabolites]]
[[Category:Analgesics]]
[[Category:Pharmacology]]
[[Category:Pharmacology]]
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Latest revision as of 03:55, 13 February 2025


Norketamine[edit]

Chemical structure of Norketamine

Norketamine is a metabolite of the anesthetic and analgesic drug ketamine. It is formed in the body through the process of N-demethylation by the cytochrome P450 enzyme system, primarily in the liver. Norketamine retains some of the pharmacological properties of ketamine, contributing to its overall effects.

Pharmacology[edit]

Norketamine acts on the central nervous system and has been shown to interact with the NMDA receptor, similar to its parent compound, ketamine. However, it has a lower affinity for the NMDA receptor compared to ketamine. This interaction is believed to contribute to its analgesic and dissociative effects.

Metabolism[edit]

The metabolism of ketamine to norketamine occurs primarily in the liver. The enzyme CYP3A4 is mainly responsible for the N-demethylation of ketamine to norketamine. Once formed, norketamine can undergo further metabolism to produce other metabolites, such as dehydronorketamine.

Clinical Significance[edit]

Norketamine is considered to have a role in the therapeutic effects of ketamine, particularly in its use as an antidepressant. The presence of norketamine in the body may prolong the effects of ketamine, contributing to its antidepressant and analgesic properties.

Research[edit]

Research into norketamine has focused on its potential therapeutic effects and its role in the overall pharmacological profile of ketamine. Studies have investigated its effects on pain management and its potential use in treating depression.

Related pages[edit]