Piromelatine: Difference between revisions

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'''Piromelatine''' is a [[sedative]] and [[anxiolytic]] drug that is used in the treatment of [[insomnia]]. It is a [[melatonin receptor agonist]] and [[serotonin receptor antagonist]], which means it works by affecting certain chemicals in the brain that help promote sleep.
== Piromelatine ==


== Pharmacology ==
[[File:Piromelatine.svg|thumb|right|Chemical structure of Piromelatine]]


Piromelatine has a unique mechanism of action, acting as a [[melatonin receptor agonist]] and a [[serotonin receptor antagonist]]. This dual action is thought to contribute to its effectiveness in treating insomnia.
'''Piromelatine''' is a novel investigational drug that acts as an agonist at [[melatonin receptor|melatonin receptors]] and [[serotonin receptor|serotonin receptors]]. It is being studied for its potential use in the treatment of [[insomnia]], [[depression]], and other [[central nervous system]] disorders.


=== Melatonin receptor agonism ===
== Mechanism of Action ==


Piromelatine binds to and activates the [[melatonin receptor]], a protein in the brain that is involved in regulating the sleep-wake cycle. By activating this receptor, piromelatine can help to promote sleep.
Piromelatine is a multimodal agent that primarily targets the [[MT1]] and [[MT2]] melatonin receptors, as well as the [[5-HT1A]] and [[5-HT1D]] serotonin receptors. By activating these receptors, piromelatine is thought to regulate the [[circadian rhythm]], promote sleep, and exert antidepressant effects.


=== Serotonin receptor antagonism ===
=== Melatonin Receptors ===


In addition to its action on the melatonin receptor, piromelatine also acts as an antagonist at certain [[serotonin receptor]]s. This means it blocks the action of serotonin, a neurotransmitter that can promote wakefulness.
The [[melatonin receptor|melatonin receptors]] MT1 and MT2 are involved in the regulation of the sleep-wake cycle. Activation of these receptors by piromelatine can help synchronize the [[circadian rhythm]] and improve sleep quality.


== Clinical use ==
=== Serotonin Receptors ===


Piromelatine is used in the treatment of [[insomnia]], a sleep disorder characterized by difficulty falling asleep or staying asleep. It is typically used when other treatments have not been effective.
Piromelatine's action on the [[5-HT1A]] and [[5-HT1D]] receptors is believed to contribute to its potential antidepressant effects. These receptors are part of the [[serotonin receptor]] family, which plays a crucial role in mood regulation.


== Side effects ==
== Potential Therapeutic Uses ==


Like all medications, piromelatine can cause side effects. These may include dizziness, headache, and daytime drowsiness. If these side effects persist or worsen, patients should contact their healthcare provider.
Piromelatine is being investigated for several therapeutic applications:


== See also ==
* '''[[Insomnia]]''': By acting on melatonin receptors, piromelatine may help improve sleep onset and maintenance.
* '''[[Depression]]''': Its action on serotonin receptors suggests potential antidepressant properties.
* '''[[Cognitive disorders]]''': There is interest in its use for [[cognitive impairment]] and [[neurodegenerative diseases]].


* [[Melatonin receptor agonist]]
== Clinical Trials ==
* [[Serotonin receptor antagonist]]
 
Piromelatine is currently undergoing clinical trials to evaluate its efficacy and safety in humans. These trials aim to determine the optimal dosing, therapeutic benefits, and potential side effects of the drug.
 
== Related Pages ==
 
* [[Melatonin receptor]]
* [[Serotonin receptor]]
* [[Insomnia]]
* [[Insomnia]]
* [[Depression]]
* [[Circadian rhythm]]


[[Category:Drugs]]
[[Category:Investigational drugs]]
[[Category:Sleep disorders]]
[[Category:Melatonin receptor agonists]]
[[Category:Pharmacology]]
[[Category:Serotonin receptor agonists]]
 
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Latest revision as of 10:48, 15 February 2025

Piromelatine[edit]

Chemical structure of Piromelatine

Piromelatine is a novel investigational drug that acts as an agonist at melatonin receptors and serotonin receptors. It is being studied for its potential use in the treatment of insomnia, depression, and other central nervous system disorders.

Mechanism of Action[edit]

Piromelatine is a multimodal agent that primarily targets the MT1 and MT2 melatonin receptors, as well as the 5-HT1A and 5-HT1D serotonin receptors. By activating these receptors, piromelatine is thought to regulate the circadian rhythm, promote sleep, and exert antidepressant effects.

Melatonin Receptors[edit]

The melatonin receptors MT1 and MT2 are involved in the regulation of the sleep-wake cycle. Activation of these receptors by piromelatine can help synchronize the circadian rhythm and improve sleep quality.

Serotonin Receptors[edit]

Piromelatine's action on the 5-HT1A and 5-HT1D receptors is believed to contribute to its potential antidepressant effects. These receptors are part of the serotonin receptor family, which plays a crucial role in mood regulation.

Potential Therapeutic Uses[edit]

Piromelatine is being investigated for several therapeutic applications:

Clinical Trials[edit]

Piromelatine is currently undergoing clinical trials to evaluate its efficacy and safety in humans. These trials aim to determine the optimal dosing, therapeutic benefits, and potential side effects of the drug.

Related Pages[edit]