Psycho-Babble Medication Thread 879789

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Sertindole up for approval mid-year

Posted by jrbecker76 on February 12, 2009, at 21:52:44

This AP is due to be reviewed by the FDA in late Spring. As some might recall, this drug was pulled from the EU market after its brief introduction in 1998 due to some concerns over heart arrhythmia. Sertindole has since been re-approved in in the EU and Mexico.

Its pharmacology is as a D2 antagonist/5-HT2 antagonist/alpha1&alpha2 adrenergic antagonist. Reports suggest negligible EPS, minor weight gain, sedation; has pro-cognitive effects and might have an impact on negative symptoms.

It be interesting to align these claims with any subjective feedback from experienced users.

JB

 

Re: Sertindole up for approval mid-year

Posted by jrbecker76 on February 12, 2009, at 23:13:05

In reply to Sertindole up for approval mid-year, posted by jrbecker76 on February 12, 2009, at 21:52:44

> This AP is due to be reviewed by the FDA in late Spring. As some might recall, this drug was pulled from the EU market after its brief introduction in 1998 due to some concerns over heart arrhythmia. Sertindole has since been re-approved in in the EU and Mexico.
>
> Its pharmacology is as a D2 antagonist/5-HT2 antagonist/alpha1&alpha2 adrenergic antagonist. Reports suggest negligible EPS, minor weight gain, sedation; has pro-cognitive effects and might have an impact on negative symptoms.
>
> It be interesting to align these claims with any subjective feedback from experienced users.
>
> JB
>

correction to the above...should read "lack of sedation"

 

Re: Sertindole up for approval mid-year » jrbecker76

Posted by Phillipa on February 13, 2009, at 0:03:20

In reply to Re: Sertindole up for approval mid-year, posted by jrbecker76 on February 12, 2009, at 23:13:05

Thanks jr will google it now. Love Phillipa

 

low dose combined with pimavanserin... » jrbecker76

Posted by iforgotmypassword on February 13, 2009, at 19:19:11

In reply to Sertindole up for approval mid-year, posted by jrbecker76 on February 12, 2009, at 21:52:44

...theoretically may be a very good combination. pimavanserin is supposed to allow a lower dose of antipsychotics, but while retaining the efficacy. a lower dose may possibly eliminate cardiac worries completely, below the level of occurances in other antipyschotic drugs currently available.

also pimavanserin is a very curious drug that may become a very unique cognitive enhancer in itself. it is even an agonist at the M1 receptor. it is in phase III, so it won't be available for a while, but it may be the most interesting drug in the pipeline to seek FDA approval at the moment.

 

Re: low dose combined with pimavanserin...

Posted by Sigismund on February 16, 2009, at 1:22:42

In reply to low dose combined with pimavanserin... » jrbecker76, posted by iforgotmypassword on February 13, 2009, at 19:19:11

>has pro-cognitive effects

That is unexpected.

 

Re: pimavanserin - eplivanserin - sertindole » iforgotmypassword

Posted by jrbecker76 on February 17, 2009, at 13:44:37

In reply to low dose combined with pimavanserin... » jrbecker76, posted by iforgotmypassword on February 13, 2009, at 19:19:11

> ...theoretically may be a very good combination. pimavanserin is supposed to allow a lower dose of antipsychotics, but while retaining the efficacy. a lower dose may possibly eliminate cardiac worries completely, below the level of occurances in other antipyschotic drugs currently available.
>
> also pimavanserin is a very curious drug that may become a very unique cognitive enhancer in itself. it is even an agonist at the M1 receptor. it is in phase III, so it won't be available for a while, but it may be the most interesting drug in the pipeline to seek FDA approval at the moment.

Pimavanserin is only a weak agonist of muscarinic receptors, however, being a strong 5-HT2a inverse agonist will provide some cognitive, hypnotic, anxiolytic and mild antidepressant effects. Unfortunately, it is not on track to reach the marketplace before '12/'13.

Eplivanserin, a moderate 5-HT2a antagonist, is in FDA/EMEA review currently. It is expected to be approved and launched early next year (2010) for sleep maintenance. Presumably, this will also make an interesting augmentation candidate.

Back to Sertindole (marketed as Serdolect in EU), on paper, it is intriguing as a potential augmentor for AD-induced side effects such as apathy/avolition/cognitive dysfunction. It's antagonism for 5-HT2A/2C as well as 5-HT6 should promote significant prefrontal activity that would counteract SSRI/SNRI-induced side effects. In terms of tolerability, Sertindole has showed non-significant sedation in comparison to placebo (the only atypical AP to do so), mild weight gain, and minimal EPS and increase in prolactin levels. As for possible AD effects, although it will probably prove to not be as powerful a compound as clozapine or olanzapine is for negative symptoms, it has shown a decent impact for this side of the condition. I'll certainly be curious to see how the field takes to using this drug for Bipolar and TRD conditions.

JB


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