Posted by SLS on July 6, 2000, at 10:25:59
In reply to Re: Stim/Sulp. Question-AndrewB,SLS,JohnL,etc, posted by KarenB on July 5, 2000, at 22:42:02
> > Thanks for the info. about the consultant saying greater binding affinities may hobble the effectiveness of amisulpride. Could you ask what the implications of this may be for those who take amisulpride; 1) more non-responders vs. Sulpiride 2) a less robust effect 3) a greater chance of postsynaptic instead of presynaptic antagonism at low doses.
>
> Hey guys,
>
> You know, when you get into that binding, postsynaptics, presynaptics, etc., you kind of lose me. I'm just not that technical. So, please respond accordingly, OK? OR...write a really long one explaining that stuff?
Dear Karen,I will attempt to comply with the former, as I don’t have the mental resources to adhere to the latter.
> Question: Does the above question indicate that there may be a substantial difference in expected response between amisulpride and sulpiride? If so, why?It is my guess that there is not a substantial difference between these two drugs regarding their efficacy for treating depression or dysthymia. I have not come across any *clinical* information that indicates that there are. It is my opinion, however, that it is usually a good idea to treat any two drugs as being different simply because they are. The doctor who my doctor consulted with feels that sulpiride is a better choice for treating depression than is amisulpride.
> As you know, I did best on Amineptine/Sulpiride. Both are Dopamine reuptake
inhibitors right?Actually, Karen, they are not both DA reuptake inhibitors. This is probably why they are so effective in combination. They are complimentary rather than being additive. The guy or gal who thought to do this is brilliant IMHO.
Amineptine blocks the reuptake of dopamine molecules by the presynaptic neuron so that it may use them again when it comes time to release them to transmit its message to the postsynaptic neuron.
> At what receptors?
Sulpiride acts to fool the thermostat that helps to regulate the presynaptic neuron. If one were to consider the release of neurotransmitter as being the turning on of a furnace, the presynaptic “autoreceptors” would represent the thermostat that controls it. Sulpiride attaches to these receptors and prevents them from feeling the heat (neurotransmitter) present in the synaptic gap. It would be as if one were to enclose the thermostat in an insulated box in which the air is never warmed by the released heat to the point where it turns off the furnace. So… Sulpiride induces the presynaptic neuron to continue to manufacture and release “extra” dopamine because the furnace is never turned off by the autoreceptor thermostat.
> What then would this indicate about possibilities of successful medications for me?Andrew and I have devoted some thought to try to answer this question, so as to heal ourselves and anyone else would like to go along for the ride. The technical stuff has some relevance in trying to brainstorm a replacement for amineptine.
> Do you think Adrafinil is a good choice
Yes, but not because it does the same thing as amineptine. It doesn’t do it at all at relevant concentrations. It just seems to be a good drug that may potentiate dopamine activity in areas of the brain thought to be involved with depression – motivation, reward, vigilance, and mental energy. It might not work. It’s just that I can think of no reason why it wouldn’t be worth a try.
> ...or only good if augmented by another Dopamine blocker?
A group of 7 people whose depressions were resistant to treatment with various antidepressants were given modafinil (Provigil), a relative of adrafinil to augment them. It helped people for whom it was combined with SSRIs as well as Wellbutrin. From the posts currently appearing on Psycho-Babble, it appears that adrafinil may be more effective than Provigil.
> It seems to me it would enhance the energizing effects of the adrafinil. Is there another psychostimulant that is a Dopamine blocker to replace the Amineptine? Ritalin and Adderall just do not compare to the Amineptine.If you were willing to be a pioneer and a guinea pig, I would be interested to see how you would respond to mazindol (Mazinor, Sanorex). This drug has been used to treat obesity and has been looked at from time to time for treating depression. It has psychostimulating properties and is often used to evaluate dopamine reuptake, as it acts to inhibit it. Mazindol is also a potent reuptake inhibitor of norepinephrine (NE).
> What would you do if you had my brain (aside from considering a sex change)?Do you want to trade? :-) Actually, it is quite possible that we will both respond to similar drug regimens. Let’s stay in touch.
> Sorry for the deluge of questions but I plan to order one or the other soon and want to make the right choice.
Sulpiride vs adrafinil or sulpriride vs amisulpride?I am currently taking sulpiride. I just moved up to 100mg. I don’t know whether to be encouraged or discouraged by my lack of response to 50mg for two weeks. What do you think? How did you go about titrating the dosage? I would like to add either modafinil or adrafinil to sulpiride if it doesn’t work. If this strategy doesn’t work, I am considering combining Parnate (an MAOI) with sulpiride.
I hope I’ve helped in some way. Please post your decision. Good luck.
- Scott
poster:SLS
thread:39176
URL: http://www.dr-bob.org/babble/20000630/msgs/39557.html