Pharmacological Profile Reuptake Blockade

Early in the history of the tricyclic and tetracyclic antidepressants, the ability of these compounds to block the transporter site for norepinephrine was described (Axelrod et al. 1961) (see Table 12-1). The tertiary amines have greater affinity for the serotonin transporter, whereas the secondary amines are relatively more potent at the norepinephrine transporter. During the administration of amitriptyline, imipramine, or clomipramine, these tertiary amines are demethylated to secondary amines; thus, both serotonergic and noradrenergic effects occur. In addition, because dopamine is inactivated by norepinephrine transporters in the frontal cortex (Bymaster et al. 2002), norepinephrine reuptake inhibitors would be expected to increase dopamine concentrations in that region.

Defeat Depression

Defeat Depression

Learning About How To Defeat Depression Can Have Amazing Benefits For Your Life And Success! Discover ways to cope with depression and melancholic tendencies! Depression and anxiety particularly have become so prevalent that it’s exceedingly common for individuals to be taking medication for one or even both of these mood disorders.

Get My Free Ebook


Post a comment