Posted by linkadge on September 2, 2016, at 15:44:44
Hey all,
Buspar is an interesting drug. It is the only available 5-ht1a agonist.
However, buspar has a metabolite (1-pp) that significantly detracts from the effectiveness of buspar (and can add a number of cardiac / activation side effects).
Buspar is metabolised extensively by cyp3a4 and so I wondered what effect a cyp3a4 inhibitor might have on the ratio of buspar to it's metabolite 1-pp.
I think it I may have found an answer:
According to:
http://www.sigmaaldrich.com/catalog/papers/10068153
"The mean ratio of the AUC of the piperazine metabolite to that of buspirone was decreased 34-fold (P<0.05) by itraconazole"
Itraconazole is a cyp3a4 inhibitor (like grapefruit juice). Taking itraconazole meant much higher levels of buspar (good) to 1-pp (bad).
It's not a stretch to suggest that taking grapefruit juice *may* make buspar work more effectively (at a lower dose) with fewer side effects.
Linkadge
poster:linkadge
thread:1091661
URL: http://www.dr-bob.org/babble/20160819/msgs/1091661.html