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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 12 to 36 of 36. Go back in thread:
Posted by linkadge on December 23, 2005, at 18:10:35
In reply to Re: Effexor metabolite submitted for FDA approval » jrbecker, posted by ed_uk on December 23, 2005, at 17:47:42
How does the half life compare to that of the parent compound ? Will this be a more or less addictive effexor ?
Linkadge
Posted by Larry Hoover on December 23, 2005, at 18:15:40
In reply to Re: Effexor metabolite submitted for FDA approval, posted by linkadge on December 23, 2005, at 18:10:35
> How does the half life compare to that of the parent compound ? Will this be a more or less addictive effexor ?
>
> LinkadgeBecause they're marketing what ought to be the product of the cytochrome 2D6 enzyme, just how much this new product will resemble the older Effexor depends directly on how functional your 2D6 is. If you're a poor metabolizer, this will be a novel drug.
Lar
Posted by linkadge on December 23, 2005, at 18:30:51
In reply to Re: Effexor metabolite submitted for FDA approval » linkadge, posted by Larry Hoover on December 23, 2005, at 18:15:40
Do they have reason to believe that normal 2D6 metabolizers respond better to Effexor? Do normal 2D6 metabolizers experience more or fewer side effects on Effexor?
I know with celexa->lexapro, there was supposedly some reason to believe that the S enatomer was less anxiogenic than citalporam.
Linkadge
Posted by blueberry on December 23, 2005, at 18:33:00
In reply to Effexor metabolite submitted for FDA approval, posted by jrbecker on December 23, 2005, at 13:27:14
It's so disappointing when they come out with another antidepressant that is just another reuptake inhibitor. I mean, there are so many flaws in the reuptake monoamine theory (example only 60%ish get a 50% improvement; tianeptine, a reuptake enhancer, is equally effective in trials; on and on, etc). I wish one of these companies would think outside the box for a change. You know, those people get paid big bucks. You would think they could come up with something better than just another variation.
That being said, I am sure there will be a certain population of patients who will be helped bigtime by this new version. But still.
Posted by linkadge on December 23, 2005, at 18:52:44
In reply to Re: Effexor metabolite submitted for FDA approval, posted by blueberry on December 23, 2005, at 18:33:00
Effexor for me was very anxiogenic. I remember it raised my puse well over 20 bpm. It became hard to ignore the pulse at times. It also made me sweaty, and generally on edge. It also seemed to induce this strange but persistantly smouldering fear.
I'd like to see some work into compounds that can more directly influence neurotrophic molecules.
Anyone see that 60 minautes episode on GDNF in Parkinsons ?
Linkadge
Posted by ed_uk on December 23, 2005, at 18:56:57
In reply to Re: Effexor metabolite submitted for FDA approval » linkadge, posted by Larry Hoover on December 23, 2005, at 18:15:40
>........just how much this new product will resemble the older Effexor depends directly on how functional your 2D6 is. If you're a poor metabolizer, this will be a novel drug.
.......but venlafaxine *itself* has pretty much the same pharmacological effects as desvenlafaxine. They're both SNRIs of comparable potency.
Regards
Ed
Posted by jamestheyonger on December 23, 2005, at 20:56:19
In reply to Re: Effexor metabolite submitted for FDA approval, posted by blueberry on December 23, 2005, at 18:33:00
" You know, those people get paid big bucks. You would think they could come up with something better than just another variation. "
>It also takes big bucks to bring a novel medication to market.
Posted by Phillipa on December 23, 2005, at 21:01:33
In reply to Re: Effexor metabolite submitted for FDA approval, posted by linkadge on December 23, 2005, at 18:10:35
Link, good question was wondering the same. And is cymbalta stronger than the current effexer I've heard both. Fondly, Phillipa
Posted by Larry Hoover on December 23, 2005, at 22:37:06
In reply to Re: Effexor metabolite submitted for FDA approval » Larry Hoover, posted by ed_uk on December 23, 2005, at 18:56:57
> >........just how much this new product will resemble the older Effexor depends directly on how functional your 2D6 is. If you're a poor metabolizer, this will be a novel drug.
>
> .......but venlafaxine *itself* has pretty much the same pharmacological effects as desvenlafaxine. They're both SNRIs of comparable potency.
>
> Regards
>
> EdPerhaps without sufficient evidence, I am presuming some activity (side-effects) from N-desmethylvenlafaxine. The relative proportion of venlafaxine being N-desmethylated would be inversely propotional to 2D6 activity. (I.e. 2D6 being major route or minor route to didesmethylated structure).
I would like to retract my earlier statement re: novelty, as I can find no supporting evidence for my assertion. Binding affinities of venlafaxine and the o-desmethyl structure are virtually identical.
Lar
Posted by Sonny Liston on December 24, 2005, at 12:52:33
In reply to Re: Effexor metabolite submitted for FDA approval, posted by jamestheyonger on December 23, 2005, at 20:56:19
> " You know, those people get paid big bucks. You would think they could come up with something better than just another variation. "
> >
>
> It also takes big bucks to bring a novel medication to market.
It's not like Big Pharma doesn't have the big bucks and won't receive a high rate of return on their "novel" investment. Maybe the money would be be better spent on R&D, instead of the legions of drug reps, pushing samples, pens, note pads, clocks, coffee mugs, key chains and other numerous office supplies to buy their doctors preferences when dispensing said drugs.
Posted by linkadge on December 24, 2005, at 13:06:07
In reply to Re: Effexor metabolite submitted for FDA approval, posted by Sonny Liston on December 24, 2005, at 12:52:33
I am still interested in the triple uptake inhibitor mentioned a few years back. DOV 21947 or whatever.
I don't really understand why a subset of doctors contend that dopamine uptake inihibition has no antidepressant effect. I am not convinced. I think it is probably more due to their inability to filter out a possably addictive profile.Sleep deprivation, for instance, seems to slow the metabolism of serotonin norepineprine and dopamine.
Linkadge
Posted by jamestheyonger on December 24, 2005, at 13:30:07
In reply to Re: Effexor metabolite submitted for FDA approval, posted by Sonny Liston on December 24, 2005, at 12:52:33
> > " You know, those people get paid big bucks. You would think they could come up with something better than just another variation. "
> > >
> >
> > It also takes big bucks to bring a novel medication to market.
>
>
> It's not like Big Pharma doesn't have the big bucks and won't receive a high rate of return on their "novel" investment.And a high rate of losses on meds that do not make it past phase one trials
Maybe the money would be be better spent on R&D, instead of the legions of drug reps, pushing samples, pens, note pads, clocks, coffee mugs, key chains and other numerous office supplies to buy their doctors preferences when dispensing said drugs.
>
It doc are ***allowing*** themselves to be bought
then blame the docs.
Posted by linkadge on December 24, 2005, at 14:04:15
In reply to Re: Effexor metabolite submitted for FDA approval, posted by jamestheyonger on December 24, 2005, at 13:30:07
I can agree in that it seems like an unnaturally slow proces.
What happened to RU-486. Wasn't that supposed to have been put in the fast-track process for depression.
If that is the fast track process then I'd hate to see the slow track process.
I remember reading about citalopram in a book writtain in 1983!
Linkadge
Posted by jamestheyonger on December 24, 2005, at 15:25:03
In reply to Re: Effexor metabolite submitted for FDA approval, posted by linkadge on December 24, 2005, at 14:04:15
" If that is the fast track process then I'd hate to see the slow track process."
The fast track process is problematic. AIDS drugs were fast tracked and lacking research info were only given to those who were very sick.
Years later, after research, we discovered the drugs worked best given when people were not yet very sick.If we fast track and hurt or kill some people then, of course, the "big pharma" will be taken to task for that. Just like we are doing now because they take too long.
Posted by ed_uk on December 24, 2005, at 17:14:55
In reply to Re: Effexor metabolite submitted for FDA approval » ed_uk, posted by Larry Hoover on December 23, 2005, at 22:37:06
Hi Lar
Effexor has been associated with arrhythmias - especially in overdose. I wonder how desvenlafaxine compares.
Ed
Posted by linkadge on December 24, 2005, at 19:34:09
In reply to Re: Effexor metabolite submitted for FDA approval, posted by jamestheyonger on December 24, 2005, at 15:25:03
I am not suggesting that they release a drug prematurely, I just wish the decision to take a risk with a new drug wasn't calculated solely in terms of $.
The approval of a metabolite is probably a lot more likely then the approval of a novel drug.
I just don't really think that the quality of life for the average person with depresson is all that much better than what it was 15 years ago.I just get bummed when I see good drugs like gepirone deemd "not approvable"
Linkadge
Posted by jamestheyonger on December 25, 2005, at 1:14:42
In reply to Re: Effexor metabolite submitted for FDA approval, posted by linkadge on December 24, 2005, at 19:34:09
> I am not suggesting that they release a drug prematurely, I just wish the decision to take a risk with a new drug wasn't calculated solely in terms of $.
>It is hard to develop new drugs when the biochemical process of mental illness is poorly understood.
Posted by linkadge on December 25, 2005, at 13:53:41
In reply to Re: Effexor metabolite submitted for FDA approval, posted by jamestheyonger on December 25, 2005, at 1:14:42
I realize what you are saying. As an example though, there is a drug like ritanserin, which nobody wants to bother with because it might not be able to stand on its own as an antidepressant. But it could be very usefull for say SSRI augmentation.
Linkadge
Posted by Sonny Liston on December 25, 2005, at 17:24:49
In reply to Re: Effexor metabolite submitted for FDA approval, posted by jamestheyonger on December 25, 2005, at 1:14:42
Do you work for a drug company?
Posted by jamestheyonger on December 25, 2005, at 20:11:43
In reply to Re: Effexor metabolite submitted for FDA approval » jamestheyonger, posted by Sonny Liston on December 25, 2005, at 17:24:49
> Do you work for a drug company?
No. I would like to like they work for me as I have been on psyco meds for 21 years and the meds are successful, for me.
Posted by Sonny Liston on December 26, 2005, at 15:47:34
In reply to Re: Effexor metabolite submitted for FDA approval, posted by jamestheyonger on December 25, 2005, at 20:11:43
> > Do you work for a drug company?
>
>
> No. I would like to like they work for me as I have been on psyco meds for 21 years and the meds are successful, for me.
>
I'm glad you have had success w/meds and wish you continued success. Please keep sharing your experiences and thoughts. Best wishes in the new year:)
Posted by TrishP on December 29, 2005, at 6:57:32
In reply to Effexor metabolite submitted for FDA approval, posted by jrbecker on December 23, 2005, at 13:27:14
Ok - I'm still not sure. Does this mean maybe they can make an off shoot of Effexor that won't have such an awful discontinuation syndrome?
Posted by Larry Hoover on December 29, 2005, at 9:17:26
In reply to Re: Effexor metabolite submitted for FDA approval, posted by TrishP on December 29, 2005, at 6:57:32
> Ok - I'm still not sure. Does this mean maybe they can make an off shoot of Effexor that won't have such an awful discontinuation syndrome?
It's pretty likely to have about the same discontinuation syndrome. It hits the same receptors, in almost an identical manner. It has a slightly longer half-life, but not enough to really make a difference.
I think it's just a way to extend patent protection, in any way they can feasibly do so.
Lar
Posted by law663 on December 30, 2005, at 17:41:08
In reply to Re: Effexor metabolite submitted for FDA approval » TrishP, posted by Larry Hoover on December 29, 2005, at 9:17:26
I've read with interest this thread. I agree with Linkage and Sonny -- this is nothing to be excited about. Just another way to extend the effexor patent. The problem as I see it is that there is no real carrot for a drug company to develop a truely novel compound when then can get a 20 year patent on a simple spin off. Perhaps a graduated patent system would be better -- really novel compounds could get 20 years, crap like celexa 5 years. Of course, who decides would be an issue, but I don't know anyone where I work who's excited about this latest AD or any that are likely to be in the pipeline for the next 5 years.
Posted by Sonny Liston on December 30, 2005, at 18:44:17
In reply to Re: Effexor metabolite submitted for FDA approval, posted by law663 on December 30, 2005, at 17:41:08
According to Pharmatimes, "studies presented at the American Society for Clinical Pharmacology and Therapeutics earlier this year showed that the sustained-release formulation of desvenlafaxine leads to higher blood levels of the active drug than the once-daily Effexor XR/ER formulation of venlafaxine, and had a lower tendency to cause nausea."
These are the main reported "advantages" over Effexor. Not much to write home about about.
In addition Pharmatimes notes "that desvenlafaxine is seen as a patent extension strategy for Wyeth as it defends its Effexor franchise."
This is the end of the thread.
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