Zafuleptine

Zafuleptine

Zafuleptine is a tricyclic antidepressant (TCA) that was developed in the 1970s by the French pharmaceutical company Lafon Laboratories. It is a serotonin-norepinephrine reuptake inhibitor (SNRI), which means it increases the levels of serotonin and norepinephrine in the brain by inhibiting their reuptake into neurons. This results in an increase in the extracellular concentrations of these neurotransmitters and therefore an increase in neurotransmission.

Pharmacology

Zafuleptine is a potent inhibitor of the reuptake of serotonin and norepinephrine, two neurotransmitters that are known to be involved in the pathophysiology of depression. By inhibiting their reuptake, zafuleptine increases the levels of these neurotransmitters in the synaptic cleft, which leads to increased neurotransmission. This is thought to be the mechanism by which zafuleptine exerts its antidepressant effects.

Zafuleptine is also a weak inhibitor of the reuptake of dopamine, another neurotransmitter that is thought to be involved in the pathophysiology of depression. However, the clinical significance of this action is unclear.

Clinical Use

Zafuleptine was marketed in France for the treatment of depression in the 1970s and 1980s. However, it was withdrawn from the market due to concerns about its safety profile, particularly its potential to cause hepatotoxicity.

Side Effects

The most common side effects of zafuleptine include nausea, vomiting, dizziness, and sedation. In rare cases, it can cause serious side effects such as hepatotoxicity, which can lead to liver failure.

See Also

• Tricyclic antidepressant
• Serotonin-norepinephrine reuptake inhibitor
• Depression