Why is aripiprazole (Abilify) considered a third-generation atypical antipsychotic?

 

 

 

 

 

 

 

Well, first off, Aripiprazole defines a structural class distinct from FGAs (Butyrophenones, Thioxanthenes, Benzamides, Phenothiazines, etc.) and SGAs (Dibenzepines, Benzisoxalderivatives).

Unlike FGAs and SGAs, Aripiprazole is a partial agonist instead of a full antagonist. This means its effect is inherently limited (ceiling) and it has a very good profile of unwanted sideeffects (no net weight gain, good function in terms of negative symptoms, etc.).

The partial agonism also leads to aripiprazole being able to (when added to the regimen) actually reduce EPS in patients receiving high-dosed FGAs because it competitively inhibits FGA function.

 

 

The term "third generation" antipsychotic is something I haven't heard of yet.

But Aripiprazole is so much unlike the other antipsychotics due to its partial agonism that I guess you could call it that.

OK. Thanks for this information, jbn22.

Is aripiprazole a selective FAAH inhibitor/endocannabinoid enhancer?

 

See:

 

https://en.wikipedia.org/wiki/Endocannabinoid_enhancer

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2704579/

Edited March 23, 20178 yr by tkadm30

Since the endogenous cannabinoid anandamide is a substrate of the CYP2D6 enzyme, can we assume aripiprazole is activated by anandamide biosynthesis?