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Dr. Bob is Robert Hsiung, MD,
[email protected]Shown: posts 1 to 9 of 9. This is the beginning of the thread.
Posted by Maria3667 on July 2, 2007, at 14:55:38
No! In fact, the manufacturer has refiled an application for it with the FDA last May.
This novel anti-depressant which acts as an agonist on the 5HT-1a-receptor and an antagonist on the N-2a-receptor is reputed to have much less side effects than the currently available SSRI's.
It's also reputed to be pro-sexual for FEMALES (hurray, our own Viagra at last???).
Read the press release below:
Fabre-Kramer refiles to OK antidepressant
HOUSTON, May 8 (UPI) -- Fabre-Kramer said Tuesday it refiled its new drug application for the antidepressant gepirone ER with the U.S. Food and Drug Administration.
The firm said the NDA includes an amendment responding to the FDA's 2004 request for an additional trial for gepirone ER. Fabre-Kramer is seeking an indication for the treatment of major depressive disorder.If gepirone ER ultimately wins approval, GlaxoSmithKline will co-market it worldwide, pursuant to an agreement Fabre-Kramer entered into with the pharmaceutical giant in February.
Fabre-Kramer acquired the rights to gepirone ER in 2005 from Organon after the FDA deemed the drug not approvable in 2004. Under the terms of that agreement, Organon will receive milestone and royalty payments if gepirone ER gets approved.
Posted by linkadge on July 2, 2007, at 16:08:43
In reply to Gepirone has not dissapeared!, posted by Maria3667 on July 2, 2007, at 14:55:38
I do hope this med makes it to the market. The effect of SSRI's is supposedly mediated throught 5-ht1a. The neurotrophic effect is certainly dependant on 5-ht1a receptors.
A lot of disorders could benifit from a potent 5-ht1a agonist, including anxiety, panic, epilepsy, shizophrenia, depression, and even parkinsons.
Linkadge
Posted by Maximus on July 2, 2007, at 16:15:35
In reply to Gepirone has not dissapeared!, posted by Maria3667 on July 2, 2007, at 14:55:38
> No! In fact, the manufacturer has refiled an application for it with the FDA last May.
>
> This novel anti-depressant which acts as an agonist on the 5HT-1a-receptor and an antagonist on the N-2a-receptor is reputed to have much less side effects than the currently available SSRI's.
>
> It's also reputed to be pro-sexual for FEMALES (hurray, our own Viagra at last???).I don't know if Gepirone is a potent Alpha 2 antagonist? On paper it looks good but in a day to day usage alpha 2 antagonists produce rage and/or irritability on a lot of patients.
Moreover several studies found that gepirone increases plasma corticosterone levels, which is "generally" bad.
Don't want to sound pessimistic but i would not hold my breathe for this stuff. Though its action on 5TH1a receptors could be beneficial for some...
Posted by Phillipa on July 2, 2007, at 16:22:33
In reply to Re: Gepirone has not dissapeared!, posted by Maximus on July 2, 2007, at 16:15:35
We need a new antidepressant so badly I do hope it makes it to the market what SSRI does it compare to or is it completely different in side effects etc? Love Phillipa
Posted by Maria3667 on July 2, 2007, at 16:59:31
In reply to Re: Gepirone has not dissapeared!, posted by Phillipa on July 2, 2007, at 16:22:33
Hi Phillippa,
Some 'knowledgeable people' think it is very similar to Buspirone (Buspar). This also is an agonist on the 5HT1a-receptors & an antagonist on the N-a2-receptors. However, the clinical studies show Gepirone has a different set of adverse events. The difference being that Buspirone also is a partial agonist for the D-a2-receptor. As you might know, 1 extra neurotransmitter could upset the whole system, so...
@ Maximus
Interesting theory about the N-a2-receptor tringering agression... However, I'm a bit puzzled. Taken loads of meds working on this particular receptor (and others), but never felt agression (i.e. Remeron, Dipiperone (Pipamperone). Got any links for me?Cheers,
Maria
Posted by Maximus on July 2, 2007, at 18:17:52
In reply to Re: Gepirone has not dissapeared!, posted by Maria3667 on July 2, 2007, at 16:59:31
> @ Maximus
> Interesting theory about the N-a2-receptor tringering agression... However, I'm a bit puzzled. Taken loads of meds working on this particular receptor (and others), but never felt agression (i.e. Remeron, Dipiperone (Pipamperone). Got any links for me?
>
> Cheers,
> Maria
Hi Maria,Actually i'm a bit tired to do it. But believe me it is a well known fact. Okay, "Google" it with the following key words: alpha-2, adrenergic, receptors, rage, violence, mirtazapine, gepirone. Have a good read. Bye.
Btw, even if it works for a minority, it is still worth to be marketed. Each depressive soul is a scar for the human mankind.
Posted by linkadge on July 2, 2007, at 18:43:48
In reply to Re: Gepirone has not dissapeared!, posted by Maximus on July 2, 2007, at 16:15:35
>I don't know if Gepirone is a potent Alpha 2 >antagonist? On paper it looks good but in a day >to day usage alpha 2 antagonists produce rage >and/or irritability on a lot of patients.
I think the ratio of 5-ht1a to alpha-2 is much higher for gepirone than for buspirone.
>Moreover several studies found that gepirone >increases plasma corticosterone levels, which >is "generally" bad.Short term administration of 5-ht1a agonists will increase cortistol, just as short term SSRI administration will increase cortisol via 5-ht1a.
Long term administration, supposedly has a favorable impact on HPA axis functioning. The cortisol response will downregulate, and the system will be less sensitive to environmental stressors. (at least in theory)
Linkadge
Posted by Maria3667 on July 3, 2007, at 16:34:48
In reply to Re: Gepirone has not dissapeared! » Maria3667, posted by Maximus on July 2, 2007, at 18:17:52
Hi Maximus
I have Googled on it some. But I can't really find contributing factors which imply that triggering the andrenergic a2-receptor is risky for 'healthy' people...
The best I can come up with is that the a2-receptors are impaired in patients with violent behavior with chronic brain syndromes (such as Alzheimer). I do not consider myself to be one of these cases. So, in your humble opionion, am I at risk?
Posted by Maximus on July 3, 2007, at 19:03:53
In reply to Re: Gepirone has not dissapeared!, posted by Maria3667 on July 3, 2007, at 16:34:48
> Hi Maximus
>
> I have Googled on it some. But I can't really find contributing factors which imply that triggering the andrenergic a2-receptor is risky for 'healthy' people...
>
> The best I can come up with is that the a2-receptors are impaired in patients with violent behavior with chronic brain syndromes (such as Alzheimer). I do not consider myself to be one of these cases. So, in your humble opionion, am I at risk?Hi Maria,
No, i have never said it was "risky" nor i didn't mean so. Sorry if i haven't been clear. In my humble opinion, there is a chance to have this side effect, no more. However it is a different game if you are bipolar. So in your case, if one day this stuff jumps to the market, i would give it a try as an add-on med.
Good luck!
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