Eltoprazine for generalized anxiety disorder?

[Xzbtya]

Being a long time sufferer of anxiety I was intrigued when I came across the wikipedia entry for this substance. It is describe as a "serenic" with the following properties:

Eltoprazine (DU-28,853) is a drug of the phenylpiperazine class which is a serenic or antiaggressive agent.[1] It acts as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.[2] It is closely related to fluprazine and batoprazine, which are similarly acting drugs.

In my case, most SSRIs have been ineffective in treatment of my anxiety and I understand that some of the reasoning behind this might be due to agonism of the 5-HT2C receptor. According to some of the reading I've done, after about 2 weeks, the receptor down regulates and the anxiety caused by most SSRIs goes away. I have yet to have been able to make it passed 1 week since I can hardly function on most SSRIs. On a side note I'm going to the doctors soon and may ask him if Fluoxetine may work because of its 5ht2c antagonist properties.

Anyway back on topic. It seems odd to be that this substance hasn't been tried as a treatment for anxiety. Apparently there was one study as a possible ADHD treatment which I found on pubmed but that's about it. It is well tolerated in the majority of study participants.

Abstract

INTRODUCTION: Approvals and availability of drugs and delivery systems to treat attention-deficit/hyperactivity disorder (ADHD) have increased steadily in the last decade. The development of new pharmacological agents to treat ADHD symptoms in adults allows for both single and combination therapy for optimal efficacy. Eltoprazine hydrochloride, a serotonergic agent currently under development, is the focus of the current paper. AREAS COVERED: This paper provides an overview of the pharmacokinetics (PK) of the non-stimulant medication eltoprazine. The PK profile of eltoprazine, based on standard PK sampling accompanied by safety monitoring, is described. A literature search and review of the studies published on eltoprazine were carried out using the PubMed database up to November 2010. EXPERT OPINION: Although clinical studies of eltoprazine did not conclusively demonstrate its efficacy in treating pathological aggression in humans, eltoprazine has shown to be a well-tolerated drug in both healthy volunteers and patients across several indications studied thus far. More recently, the role of eltoprazine in reducing symptoms of ADHD in adults has been explored in a clinical trial. Future research may provide endophenotypical characteristics to help identify specific subgroups of patients with ADHD, who can benefit from the development of eltoprazine, to maximize efficacy while minimizing adverse reactions.

Anyone have any thoughts on this or know of anymore information on this substance? It seems like it could have a number of interesting applications.

 

[Cloroxtastebad]

Eltoprazine has been shown to greatly decrease impulsivity, in turn this could mean a decrease in anxiety.


The current study addressed the possible efficacy of eltoprazine, an anti-aggressive agent and a
5-HT
1A/1B
receptor agonist (Olivier and van Oorschot, 2005), as an anti-impulsive drug. We
tested eltoprazine because of the links between aggressive and impulsive behavior. For example,
correlations have been found between delay aversion and aggression in both humans and rats
(Ramirez and Andreu, 2005; Solanto et al., 2001; Chapter 3). The results show that eltoprazine,
similarly to D-amphetamine, decreased response inhibition in a stop-signal task, but raised
inhibition in a delayed reward task. Because the effects of eltoprazine are highly similar to those
of D-amphetamine in these impulsivity tasks, it can be postulated that eltoprazine has anti-
impulsive properties.

 

[Cloroxtastebad]

Im unsure whether or not you can conclude that it has strong anxiolytic action. It is shown at higher doses to act on dopamine receptors as well. Im not sure why this drug hasnt seen more attention. There are a large number of studies showing its effectiveness in both treatment of ADHD and aggression and impulse.

 

[xvaltan]

I have been so interested in trying a selective 5HT1A full agonist... if only one would ever be widely available I'm surprised we haven't seen virtually anything from pharma here on the market yet.

 

[Cloroxtastebad]

As am i. I have struggled with anxiety and depression most of my life. SSRI's have never really helped me. They don't worsen my anxiety, but they do little to help. I aslo have a terrible time focusing on things that i have little interest in, my patience in near zero. Stimulant meds are great, but they lead to overwhelming depression once tolerance grows and you begin doses of 120mg of amphetamines.

Seems like a very practical medication that could be very well utilized. Someday soon i hope it will become widely available.

 

[PerekurPro]

A quick look over all family of piperazines in wikipedia, found Niaprazine, may be the good analog of trazodone, trazodone by itself is good as anxyolytic and sleep aid, but histaminergic ad muscarinic side-effects make it feel dirty and toxic.
I wonder if anybody had used Niaprazine as sleeping aid and anxyolytic.

 

[Cloroxtastebad]

A quick look over all family of piperazines in wikipedia, found Niaprazine, may be the good analog of trazodone, trazodone by itself is good as anxyolytic and sleep aid, but histaminergic ad muscarinic side-effects make it feel dirty and toxic.
I wonder if anybody had used Niaprazine as sleeping aid and anxyolytic.

You know you stumbled into some uncharted territory when you can mention the use of a medication found effective for the treatment of ADD, for a anxiolytic and sleep aid.

I would think it would be helpful, but by no means a sedative with primary use as a sleep aid. More of an aid to anxiety based insomnia.

 

[xvaltan]

You know you stumbled into some uncharted territory when you can mention the use of a medication found effective for the treatment of ADD, for a anxiolytic and sleep aid.

I would think it would be helpful, but by no means a sedative with primary use as a sleep aid. More of an aid to anxiety based insomnia.

Note also that (living in the US, they don't prescribe that here I believe) I couldn't find a site selling that anywhere (even legitimately) online..

It's listed as virtually inactive at 1A, but it's piperazine metabolite:
http://en.wikipedia.org/wiki/Para-Fluorophenylpiperazine

looked much more interesting. "pFPP has little stimulant effects, with its subjective effects derived mainly from its action as a 5-HT1A receptor agonist" Perhaps it would be more tolerable than the more common phenylpiperzines, and especially at low doses.