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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 13 of 13. This is the beginning of the thread.
Posted by Netch on December 12, 2008, at 11:22:42
A new sleeping pill is coming to town:
"Eplivanserin's developer, Sanofi-Aventis, is gearing up for the European launch of the drug in 2009 based upon favorable comments from the European drug agency. In addition, the company, which has funded three completed phase III clinical trials, is preparing to file for marketing approval in the United States and Canada, Pierre Gervais said at the annual American Psychiatric Association Institute on Psychiatric Services.
Eplivanserin is the furthest along in development of a new nonsedating drug class known as ASTARs, or Antagonists of Serotonin Two A Receptors. Many sleep disorder experts expect the ASTARs to take over a major chunk of the insomnia treatment market now dominated by zolpidem and other drugs acting on the γ-aminobutyric acid-A receptor, said Mr. Gervais, a pharmacist at Q&T Research of Sherbrooke, Quebec, an independent clinical research firm hired by Sanofi-Aventis to participate in an eplivanserin trial.
He reported on a trial of 351 adults with chronic insomnia who were randomized double blind to 4 weeks of either 1 mg or 5 mg of eplivanserin or placebo in the evening. The 5-mg dose, which is what will be marketed, resulted in a mean 39-minute reduction in the baseline 84-minute wake time after sleep onset. This was significantly greater than the mean 26-minute reduction with placebo.
Also, eplivanserin at 5 mg/day resulted in a 64% reduction in the number of nocturnal awakenings, compared with a 36% decrease with placebo. More eplivanserin-treated patients reported a significant improvement in the refreshing quality of sleep.
The side effect profile of eplivanserin mimicked that of placebo. The exception was dry mouth, which was reported by 1.7% of the placebo group and 5.3% of patients on 5 mg/day of eplivanserin.
The ASTAR was not associated with next-morning drowsiness or difficulty in concentration."
http://www.clinicalpsychiatrynews.com/article/S0270-6644(08)70780-X/fulltext
Posted by SLS on December 12, 2008, at 11:38:16
In reply to Eplivanserin - new sleep med, posted by Netch on December 12, 2008, at 11:22:42
Eplivanserin?
Woohoo!
A selective 5-HT2 antagonist!
Perfect for augmenting antidepressants and the older antipsychotics.
I was always disappointed that ritanserin would never make it to the pharmacy shelves. It is the poster drug for selective 5-HT2 antagonists.
Thank you for posting this.
- Scott
Posted by Netch on December 12, 2008, at 11:52:25
In reply to Re: Eplivanserin - new sleep med, posted by SLS on December 12, 2008, at 11:38:16
Hi Scott
It looks pretty good compared to older sleep meds with all their harsh side effects
Netch
> Eplivanserin?
>
> Woohoo!
>
> A selective 5-HT2 antagonist!
>
> Perfect for augmenting antidepressants and the older antipsychotics.
>
> I was always disappointed that ritanserin would never make it to the pharmacy shelves. It is the poster drug for selective 5-HT2 antagonists.
>
> Thank you for posting this.
>
>
> - Scott
Posted by Phillipa on December 12, 2008, at 12:25:19
In reply to Eplivanserin - new sleep med, posted by Netch on December 12, 2008, at 11:22:42
Netch sounds promising. So it's basically like ambien or lunesta without the side effect profile and provides longer sleep cycles? Phillipa
Posted by desolationrower on December 12, 2008, at 23:16:49
In reply to Eplivanserin - new sleep med, posted by Netch on December 12, 2008, at 11:22:42
> Eplivanserin is the furthest along in development of a new nonsedating drug class known as ASTARs, or Antagonists of Serotonin Two A Receptors. Many sleep disorder experts expect the ASTARs to take over a major chunk of the insomnia treatment market now dominated by zolpidem and other drugs acting on the γ-aminobutyric acid-A receptor, said Mr. Gervais, a pharmacist at Q&T Research of Sherbrooke, Quebec, an independent clinical research firm hired by Sanofi-Aventis to participate in an eplivanserin trial.ASTARs? I would like to punch the Advanced Sales Strategy for Marketing Ugly Names for Corporate Headquarters who came up with ASTARs. Almost as bad as NaSSA and reuptake inhibitors naming mess.
At any rate, its nice a clean drug like this may become availible, and hopefully replaces most of the offlabel use of neuroleptics. Still, many docs can't do polypharmacy so i expect it to be underutilised.
-d/r
Posted by yxibow on December 13, 2008, at 0:08:22
In reply to Re: Eplivanserin - new sleep med, posted by desolationrower on December 12, 2008, at 23:16:49
Curious all these -anserins that are around in testing: volinanserin, eplivanserin, pruvanserin and pimavanserin, the end stems of drugs are actually classified now :
http://www.ama-assn.org/ama/pub/category/4782.html
-anserin serotonin 5-HT2 receptor antagonists
Yet mianserin which I believe was discontinued and is related to Remeron, mirtazapine (which isnt in the list) is primarily alpha-2, and serotonin blockade secondarily.
Posted by Sir Dugald on December 14, 2008, at 10:32:33
In reply to Re: Eplivanserin - new sleep med, posted by yxibow on December 13, 2008, at 0:08:22
Hey you psychopharmacologists out there. Do you know why eplivanserin will be a non-sedating sleep aid when Mirtazapine which is also a Serotonin 2 blocker is unbelievably sedating?
Posted by iforgotmypassword on December 14, 2008, at 10:49:18
In reply to Re: Eplivanserin - new sleep med, posted by Sir Dugald on December 14, 2008, at 10:32:33
but we have yet to try such a selective 5-ht2a antagonist or inverse agonist, so it is hard to speculate what it's side effects may be.
it has comparable affinity to the the 5-ht2c where it is an simple antagonist (not an inverse agonist), but how that translates into occupancy, i don't know.
the effects of this drug on executive function, apathy and anhedonia, EPS (especially SSRI induced EPS, "RLS", and every type of long term EPS), and general functionning, will be something to watch out for.
i am seriously considering ziprasidone, but despite it's high selectivity for 5-ht2a (by several times over D2), it's occupancy of D2 is still high. i am particularly worried about this because risperidone gave me a scary feeling that it was supressing my breathing.
i worry that we may see another case of a french drug being too interesting for the united states, and therefore also its dependency to its north, to let through.
Posted by Netch on December 15, 2008, at 9:24:21
In reply to Re: Eplivanserin - new sleep med, posted by Sir Dugald on December 14, 2008, at 10:32:33
Eplivanserin probably has a shorter half-life
/Netch
Posted by Netch on December 15, 2008, at 9:27:21
In reply to Re: Eplivanserin - new sleep med » Netch, posted by Phillipa on December 12, 2008, at 12:25:19
> Netch sounds promising. So it's basically like ambien or lunesta without the side effect profile and provides longer sleep cycles? Phillipa
I think it would be more like Seroquel, but with shorter half-life
/Netch
Posted by iforgotmypassword on December 15, 2008, at 10:42:44
In reply to Re: Eplivanserin - new sleep med » Sir Dugald, posted by Netch on December 15, 2008, at 9:24:21
i think eplivanserin has a long half-life. i could try to dig it up. eplivanserin, if it gets released in united states (which i have my doubts about, it is probably too broadly useful a drug,) will be the first selective 5-ht2 antagonist, sparing H1, cholinergic, and dopamine receptors.
Posted by Phillipa on December 15, 2008, at 19:01:12
In reply to Re: Eplivanserin - new sleep med » Phillipa, posted by Netch on December 15, 2008, at 9:27:21
Netch I see. Thanks Phillipa
Posted by psychobot5000 on December 16, 2008, at 22:26:34
In reply to Re: Eplivanserin - new sleep med, posted by Sir Dugald on December 14, 2008, at 10:32:33
> Hey you psychopharmacologists out there. Do you know why eplivanserin will be a non-sedating sleep aid when Mirtazapine which is also a Serotonin 2 blocker is unbelievably sedating?
Though the H1 thing has already been noted in other posts, I just wanted to add that Mirtazipine's H1 effects are apparently extremely powerful, comparable to doxepin's. Apparently, taking mirtazipine's like walking around under a triple dose of benadryl all day, at least in terms of the antihistamine effects.
Of course it also increases noradrenaline. Big, complicated drug.
This is the end of the thread.
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