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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 4 of 4. This is the beginning of the thread.
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
Posted by SLS on September 2, 2016, at 19:09:54
In reply to Buspirone breakthrough?, 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.What about vortioxetine (Trintellix)?
- Scott
Posted by linkadge on September 3, 2016, at 9:38:41
In reply to Re: Buspirone breakthrough?, posted by SLS on September 2, 2016, at 19:09:54
>What about vortioxetine (Trintellix)?
vortioxetine is also a reuptake inhibitor. I guess what I mean is that buspar is the most selective 5-h1a agonist we have.
Trazodone and its metabolites also have 5-ht1a agonist actions, but again, some reuptake inhibition and receptor antagonism.
Linkadge
Posted by jonhed on September 4, 2016, at 5:47:29
In reply to Re: Buspirone breakthrough?, posted by linkadge on September 3, 2016, at 9:38:41
I had the chance to start with brintellix when it was in phase 3 but was to paranoid to start it.
Have someone had success with it?
Cause i am willing to try it together with my current regimen: Memantine, methadone and clonazepam.
This is the end of the thread.
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