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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 14 of 14. This is the beginning of the thread.
Posted by joe f on January 26, 2014, at 11:59:15
I know that all ssri's/snri's have different monographs but do they all consist of at least one chemical compound that is the same...challenging question.
Posted by linkadge on January 26, 2014, at 13:20:19
In reply to ssri's/snri/s, posted by joe f on January 26, 2014, at 11:59:15
No, each SSRI is an entirely different chemical - except in the case of isomer or metabolite drugs (citalopram / escitalopram, venlafaxine / desvenlafaxine).
Luvox, for example, has no relation to Paxil. The two drugs just happen to have affinity for common targets (namely the serotonin transporter), but that's where the similarity ends. Luvox is a sigma agonist, which paxil is not. Paxil has affinity for the norepinephrine trasporter, which luvox has negligible affinity. There are other individual differences as well.
Linkadge
Posted by SLS on January 26, 2014, at 14:38:16
In reply to Re: ssri's/snri/s, posted by linkadge on January 26, 2014, at 13:20:19
> Luvox is a sigma agonist...
Is there any therapeutic benefit to this?
Thanks.
- Scott
Posted by linkadge on January 26, 2014, at 15:09:32
In reply to Re: ssri's/snri/s » linkadge, posted by SLS on January 26, 2014, at 14:38:16
Yes, from what I've read there is.
Selective sigma agonists demonstrate neuroprotective, pro-cognitive, anxiolytic, antidepressant, and neurotrophic properties.
Sigma receptors interact with nerve growth factors like NGF and BDNF.
Posted by SLS on January 26, 2014, at 16:48:04
In reply to Re: ssri's/snri/s, posted by linkadge on January 26, 2014, at 15:09:32
> Yes, from what I've read there is.
>
> Selective sigma agonists demonstrate neuroprotective, pro-cognitive, anxiolytic, antidepressant, and neurotrophic properties.
>
> Sigma receptors interact with nerve growth factors like NGF and BDNF.
>That sounds too good to be true.
:-)
I hope we get to see some selective sigma drugs soon.
- Scott
Posted by Phillipa on January 26, 2014, at 17:12:26
In reply to Re: ssri's/snri/s » linkadge, posted by SLS on January 26, 2014, at 16:48:04
So taking luvox instead of another antidepressant is better? Phillipa
Posted by Phillipa on January 26, 2014, at 17:20:06
In reply to Re: ssri's/snri/s, posted by Phillipa on January 26, 2014, at 17:12:26
Posted by europerep on January 27, 2014, at 9:53:30
In reply to Re: ssri's/snri/s » linkadge, posted by SLS on January 26, 2014, at 16:48:04
> I hope we get to see some selective sigma drugs soon.
What about opipramol?
Posted by SLS on January 27, 2014, at 10:35:20
In reply to Re: ssri's/snri/s » SLS, posted by europerep on January 27, 2014, at 9:53:30
> > I hope we get to see some selective sigma drugs soon.
>
> What about opipramol?
>
>Very, very interesting. Where is it available?
- Scott
Posted by europerep on January 27, 2014, at 10:51:49
In reply to Re: ssri's/snri/s » europerep, posted by SLS on January 27, 2014, at 10:35:20
> Very, very interesting. Where is it available?
It is definitely available as a cheap generic in Germany, and probably in some other European countries as well. The brand name used to be Insidon, but in Germany it's no longer available under that name as far as I know.
I'm sure ed knows whether it's available in the UK. Either way, you can get it imported to the USA if that's your question. ;-)
Posted by phidippus on January 27, 2014, at 19:46:12
In reply to Re: ssri's/snri/s » linkadge, posted by SLS on January 26, 2014, at 14:38:16
Yes. some individuals find sigma receptor agonists euphoric with significant anti-depressive effects.
Other individuals, however, experience dysphoria and often report feelings of malaise or anxiety.
Recently selective sigma receptor agonists were shown to produce antidepressant-like effects in mice.
Eric
Posted by phidippus on January 27, 2014, at 19:47:02
In reply to ssri's/snri/s, posted by joe f on January 26, 2014, at 11:59:15
Most medications are a single molecule.
Eric
Posted by jono_in_adelaide on January 27, 2014, at 23:55:22
In reply to Re: ssri's/snri/s » joe f, posted by phidippus on January 27, 2014, at 19:47:02
I think opipramole (sp?) or Incidon is now mainly abaliable in continental europe
Posted by jono_in_adelaide on January 28, 2014, at 0:13:08
In reply to Re: ssri's/snri/s, posted by jono_in_adelaide on January 27, 2014, at 23:55:22
http://biopsychiatry.com/opipramol.htm
Opipramol, a drug widely prescribed in Germany, is a tricyclic compound with no reuptake-inhibiting properties. However, it has pronounced D2-, 5-HT2-, and H1-blocking potential and high affinity to sigma receptors (sigma-1 and sigma-2). In early controlled trials, anxiolytic effects were revealed. However, those studies were performed before the concept of generalized anxiety disorder (GAD) was established. Because of the interesting receptor-binding profile and promising results of the early clinical trials, the authors performed a state-of-the-art placebo-controlled trial using alprazolam as an active control. Three hundred seven outpatients with GAD were included. After a 7-day single-blind placebo washout, patients were randomly assigned to receive either opipramol (final dose, 200 mg/day), alprazolam (2 mg/day), or placebo and were treated for 28 days. The efficacy of both active compounds was higher than the effects with placebo treatment. There were statistically significant differences (p < 0.05, according to the analysis of covariance) in the main outcome criterion (baseline-adjusted final means of an intent-to-treat analysis of the total scores on the Hamilton Rating Scale for Anxiety) and in secondary efficacy parameters, with global improvement of 47% for placebo and significantly more for opipramol (63%) and alprazolam (64%). Regarding safety and tolerability, no substantial differences in the number of adverse events observed between treatment groups were obvious. Sedation seemed more pronounced with alprazolam treatment than with opipramol or placebo. In this trial, it was demonstrated for the first time that opipramol, a strong but nonselective sigma site ligand, possesses anxiolytic efficacy superior to placebo in the treatment of GAD.
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