Serotonin and Drugs



Some of the new relations between serotonin

Some of the new relations between serotonin and drugs under development are discussed and drugs under development are discussed above; however, the historical association of above; however, the historical association of serotonin and psychotropic drugs was first serotonin and psychotropic drugs was first made with the tricyclic drugs and the MAOIs, as made with the tricyclic drugs and the MAOIs, as described for norepinephrine and epinephrine. described for norepinephrine and epinephrine.

The tricyclic drugs and the MAOIs, respectively, The tricyclic drugs and the MAOIs, respectively, block the uptake and the metabolism of block the uptake and the metabolism of serotonin and norepinephrine, thus increasing serotonin and norepinephrine, thus increasing the concentration of both neurotransmitters in the concentration of both neurotransmitters in the synaptic cleft. the synaptic cleft.

 Fluoxetine is one of the selective serotonin

Fluoxetine is one of the selective serotonin reuptake inhibitors (SSRIs) that are used in the reuptake inhibitors (SSRIs) that are used in the treatment of depression. Other drugs in that treatment of depression. Other drugs in that class include paroxetine (Paxil), sertraline class include paroxetine (Paxil), sertraline (Zoloft), fluvoxamine (Luvox), and citalopram (Zoloft), fluvoxamine (Luvox), and citalopram (Celexa), all of which are usually associated (Celexa), all of which are usually associated with minimal adverse effects, especially in with minimal adverse effects, especially in

Venlafaxine blocks the reuptake of both serotonin and Venlafaxine blocks the reuptake of both serotonin and norepinephrine. With respect to serotonin, both norepinephrine. With respect to serotonin, both trazodone (Desyrel) and nefazodone block the reuptake trazodone (Desyrel) and nefazodone block the reuptake of serotonin and directly antagonize 5-HT2 receptors, of serotonin and directly antagonize 5-HT2 receptors, with the net effect stimulating 5-HT1 receptors. with the net effect stimulating 5-HT1 receptors.

Trazodone and nefazodone and the 5-HT1 receptor

Trazodone and nefazodone and the 5-HT1 receptor agonist buspirone are the first of what will likely be a agonist buspirone are the first of what will likely be a series of drugs that target subtypes of serotonin series of drugs that target subtypes of serotonin rreceptors. eceptors.

 Another serotonergic drug that has been used in Another serotonergic drug that has been used in psychiatry is L-tryptophan. Because the concentration psychiatry is L-tryptophan. Because the concentration of L-tryptophan is the rate-limiting function in the of L-tryptophan is the rate-limiting function in the synthesis of serotonin, ingestion of L-tryptophan can synthesis of serotonin, ingestion of L-tryptophan can increase the concentration of serotonin in the CNS. L- increase the concentration of serotonin in the CNS. Ltryptophan was withdrawn from the market in 1990 in tryptophan was withdrawn from the market in 1990 in the United States by the Food and Drug Administration the United States by the Food and Drug Administration (FDA) because a contaminant from the production (FDA) because a contaminant from the production process at one particular manufacturing site caused an process at one particular manufacturing site caused an eosinophilia-myalgia syndrome in some patients taking eosinophilia-myalgia syndrome in some patients taking the drug. Recent data suggest the drug. Recent data suggest