Nordoxepin

Overview of Nordoxepin

Nordoxepin

Nordoxepin is a tricyclic antidepressant (TCA) and the primary active metabolite of doxepin. It is used in the treatment of depression and anxiety disorders.

Pharmacology

Nordoxepin functions primarily as a serotonin-norepinephrine reuptake inhibitor (SNRI), which means it increases the levels of the neurotransmitters serotonin and norepinephrine in the brain by inhibiting their reuptake into neurons. This action is believed to contribute to its antidepressant and anxiolytic effects.

Mechanism of Action

Structural formula of Nordoxepin

Nordoxepin binds to the serotonin transporter (SERT) and the norepinephrine transporter (NET), preventing the reuptake of these neurotransmitters into the presynaptic neuron. This results in increased concentrations of serotonin and norepinephrine in the synaptic cleft, enhancing neurotransmission and improving mood and anxiety symptoms.

Clinical Use

Nordoxepin is primarily used in the management of major depressive disorder and anxiety disorders. It may also be used off-label for other conditions such as chronic pain and insomnia.

Side Effects

Common side effects of Nordoxepin include dry mouth, constipation, drowsiness, and dizziness. Like other TCAs, it can also cause cardiovascular side effects such as orthostatic hypotension and tachycardia.

Metabolism

Nordoxepin is metabolized in the liver by the cytochrome P450 enzyme system, primarily by CYP2D6. It is further metabolized to other compounds, which are then excreted in the urine.

Related Compounds

Nordoxepin is closely related to its parent compound, doxepin, and other tricyclic antidepressants such as amitriptyline and nortriptyline.

Related pages

• Doxepin
• Tricyclic antidepressant
• Serotonin-norepinephrine reuptake inhibitor
• Major depressive disorder
• Anxiety disorder