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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 18 of 18. This is the beginning of the thread.
Posted by B2chica on November 29, 2007, at 14:06:01
please what meds are dopamine agonists?
Posted by Sigismund on November 29, 2007, at 14:41:49
In reply to dopamine agonists??, posted by B2chica on November 29, 2007, at 14:06:01
Posted by B2chica on November 29, 2007, at 15:12:16
In reply to Here's one! » B2chica, posted by Sigismund on November 29, 2007, at 14:41:49
thanks sig. i was kinda looking in the parkinson area but was wondering if there were others, i think that restirol...or what's the one for the restless leg thing, was one.
anyway. trying to look at a case study from a different angle.
not for me.
thanks for the info.
Posted by Phillipa on November 29, 2007, at 19:03:15
In reply to Re: Here's one!, posted by B2chica on November 29, 2007, at 15:12:16
Friend doing real well on requip.5mg. He's had ECT long time ago too.And EMSAM. Phillipa
Posted by mikez on November 30, 2007, at 0:44:58
In reply to dopamine agonists??, posted by B2chica on November 29, 2007, at 14:06:01
Requip like Philippa suggested...
and also Mirapex..
By the way, Philippa...is your friend who is having success with Requip suffering from major depression or another disease? Because I am looking to ask my pdoc about augmenting with d agonists.
All the best,
Mike
Posted by B2chica on November 30, 2007, at 8:53:08
In reply to Re: dopamine agonists??, posted by mikez on November 30, 2007, at 0:44:58
i found a good list of some examples of dopamine agonists:
Parlodel (bromocriptine)
Dostinex (cabergoline)
Permax (Pergolide) - Removed from market
Mirapex (Pramipexole) (RLS)_
Requip (Ropinirole) (RLS)
Apokyn (apomorphine)
Neupro (rotigotine)
Posted by Phillipa on November 30, 2007, at 20:04:51
In reply to Re: dopamine agonists??, posted by mikez on November 30, 2007, at 0:44:58
Hi Mike oh boy was he ever depressed. ECT, EMSAM and so many combos. Then his doc hit on trying the requip. It's been a year. Was or may still be on desipramine tiny dose too. And some lithium again tiny. Still on vyanase too was on providgil. I wish he'd come back to the boards but won't. To busy working again as he was suicidal at one point now working in law as an attorney again. It's his miracle med and he has something a lot of us don't have a great pdoc who is willing to try things. Phillipa
Posted by banga on December 1, 2007, at 5:47:41
In reply to dopamine agonists??, posted by B2chica on November 29, 2007, at 14:06:01
Very very interesting, regarding the Requip. When pregnant I had horrid, horrid, HORRID restless legs syndrome but could not take Requip due to the pregnancy. Vitamin B12 helped the RLS a little....but given that Adderall seems to help my depression a bit, I wonder how Requip would do for my depression......
Posted by anonymoose on December 1, 2007, at 12:16:34
In reply to Re: dopamine agonists??, posted by banga on December 1, 2007, at 5:47:41
My $.02 regarding dopamine agonists and MAO-B inhibitors. Dopamine agonists would be preferable for those who have low levels of dopamine synthesis, whereas MAO-B inhibition would be preferable for those with normal synthesis but overactive MAO-B activity. Is this correct?
Both can be quite effective in increasing dopaminergic function, but all other things being equal, a dopamine agonist might be better to try first, because it doesn't require normal dopamine production to work.
If a person has low dopamine function due to inadequate dopamine synthesis and not overactive MAO-B activity, an MAO-B inhibitor may not seem to help as much because it doesn't actually help increase dopamine synthesis. It just prevents MAO-B from metabolizing whatever dopamine the body already produces. It doesn't actually directly improve the problem of low production.
Comments or corrections?
Posted by Phillipa on December 1, 2007, at 17:56:03
In reply to Re: dopamine agonists??, posted by anonymoose on December 1, 2007, at 12:16:34
Well don't understand the chemical part of it but before the requip he was on wellbutrin as the only thing that would do a think and it wrecked a lot of his life hence he was suicidal it was back to that or nothing. Phillipa
Posted by kingcolon on December 2, 2007, at 23:32:02
In reply to dopamine agonists??, posted by B2chica on November 29, 2007, at 14:06:01
> please what meds are dopamine agonists?
>
I was on both Requip and Mirapex and found them fairly helpful for depression with anhedonic symptoms. However, I stopped them recently because there was an article in the New England Journal of Medicine that showed that even non-ergot dopamine agonists can cause mitral valve dysfunction (ergot agonists cause severe mitral regurgitation, and are no longer recommended-eg, Parlodel was withdrawn I believe). Neurologists are concerned that the non-ergots like Requip could be a problem, but they are all they have left for Parkinsons patients. I'm not going to take any chances as there are other alternatives for anergic depression--Wellbutrin, modafinil, adrafanil, amphetamines and Ritalin, perhaps others.Here's a quote from the last paragraph of the article:
In conclusion, we found a significant increase in the risk of heart-valve regurgitation in patients taking ergot-derived dopamine-receptor agonists for Parkinson's disease. The finding of a significantly increased mean mitral tenting area, not only in patients receiving ergot-derived dopamine agonists but also in patients treated with non–ergot-derived dopamine agonists, suggests that follow-up echocardiographic monitoring is advisable in all patients with Parkinson's disease who are treated with dopamine agonists.
(From: Renzo Zanettini, M.D., Valvular Heart Disease and the Use of Dopamine Agonists for Parkinson's Disease NEJM Volume 356:39-46 (2007))
Posted by strugglingsteve on December 3, 2007, at 0:57:43
In reply to Re: dopamine agonists??, posted by kingcolon on December 2, 2007, at 23:32:02
I am phillippa's anonymous friend. I came on here looking for information about how others are doing on either requip or mirapex. As to the heart valve concern mentioned, you need to keep in mind that from what I know the dosages being used for parkinsons are significantly above what I am taking. I take .5 mg a day and most patients are at 3-5 mg a day and up evidently although I am not positive on that as I dont keep up on this stuff as much. I take 50 mg of desipramine with it and its kind of like a pseudo wellbutrin concoction but am wondering if I need the desipramine. I was at 125 mg when the requip combo gig kicked in and started slowly reducing it down to 50 mg and held there since September, was chicken to stop it as I was afraid of going back down into the pit again. I am working on other meds right now such as geodon which has replaced zyprexa for my agitation thankfully but still am not up and motivated. I'm ok but just not upbeat and optimistic. So may try to get off the desipramine soon but we'll see. Have a good day...
Posted by Phillipa on December 3, 2007, at 18:55:56
In reply to Re: dopamine agonists??, posted by strugglingsteve on December 3, 2007, at 0:57:43
Hi so glad to see you here!!!!!!! And feeling well. Shall I tell them you just home from vacation too? Phillipa
Posted by Ledgekay on December 4, 2007, at 14:25:32
In reply to Re: dopamine agonists??, posted by banga on December 1, 2007, at 5:47:41
Hi. I just wanted to respond to side-effects that are not known by doctors. I am currently dealing with that after stopping the antidepressant, Lexapro. It has been "hell" for me in that the side-effects never stopped, even after stopping the drug (they only diminished). I have developed even more problems trying to get rid of the first of the problems. I wanted to read what was written about Lamictal, since I was recently put on that, but found that my lips started to quiver. But, back to the Lexapro, I am going to do some more searching on this site to see if others have had any similar experiences. It is disheartening when doctors haven't had any experience with your situation and you have a hard time getting someone to take you seriously. That has been my case, even though I did well on antidepressants for 10 years and am an educated woman, with an educated, stable, family. Thanks for your post. It helps to know I'm not alone.
Posted by florence on December 6, 2007, at 0:58:14
In reply to Re: Here's one!, posted by B2chica on November 29, 2007, at 15:12:16
FWIW amisulpride (Solian) is used as an antipsychotic and also used for depression and dsythmia per SLS's drug sheets....
renal excretion-- 12 hr half-life...Yrs ago I took notes that said: amisulpride: D2 agonist (opposite of pramipexole (Mirapex)
It stimulates all POST synaptic DA receptors including D3- indirectly by raising DA levels--
Mirapex, however, lowers DA levels but stimulates D3 receptors directly and therefore more selectively.Don't know if this still applies....I only know I had no luck with Ser and Norep drugs so Dopamine seemed only option.....Hopes dashed when a poster told me it was not available in the USA.
I have the binding affinity comparisons for Mirapex and Requip...somewhere if anyone wants me to post them.....basically D2 and D3 differences.
florencethanks sig. i was kinda looking in the parkinson area but was wondering if there were others, i think that restirol...or what's the one for the restless leg thing, was one.
> anyway. trying to look at a case study from a different angle.
> not for me.
> thanks for the info.
Posted by Anonymoose on December 6, 2007, at 1:33:31
In reply to Re: Here's one!, posted by florence on December 6, 2007, at 0:58:14
Hm, selective D2Sh autoreceptor antagonism sounds enticing. It would be nice to be able to not have to rely on Mirapex over the long run, but I'd need something to kickstart my dopamine synthesis into gear. I think I have low levels of dopamine synthesis since Deprenyl has only a minor effect on me, yet Mirapex ("synthetic dopamine") is already giving me around 80% symptomatic remission.
If you're right about Mirapex lowering DA synthesis/release through its binding at D2Lh, that's a bit bothersome. Hopefully the low-dose Deprenyl can keep enough of the precious DA around long enough to replenish vesicular stores through DAT reuptake over time.
5HT+ and NE+ drugs were no good for me either. I suspect neither are any good for someone with already normal 5HT and NE levels. The 5HT+ meds did nothing for me but increase apathy, and the NE+ meds did nothing other than make me really jumpy and send my blood pressure through the roof.
It's too bad Solian's not avail in the US. Are there any others w/similar action? Maybe Zyprexa exhibits D2Sh antagonism, too. I haven't been able to find much solid info on it, other than it possibly exhibits antagonistic effects at 5HT-2 and DA receptors.
Mirapex and Requip are pretty similar in their affinities, right? Which one has a lower affinity for D2Lh?
Posted by Anonymoose on December 6, 2007, at 3:09:59
In reply to Re: Here's one! » florence, posted by Anonymoose on December 6, 2007, at 1:33:31
Actually, I couldn't resist looking it up myself. From the PDSP Database:
RECEPTOR | TEST LIGAND | K(i)
-----------------------------
D2Sh Pramipexole 954.992586
D2Sh Ropinirole 676.082975
D2L Pramipexole 1,698.243652
D2L Ropinirole 933.254301
D3 Pramipexole 10.471285
D3 Ropinirole 37.153523All values taken from the same study: http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=Retrieve&db=PubMed&list_uids=12388666&dopt=AbstractPlus
So, if I'm reading this right, it looks like Pramipexole has a weaker affinity for D2Sh/L, but a stronger affinity for D3.
Oh wow, it looks like Amisulpride is a really strong D2/D3 antagonist:
RECEPTOR | TEST LIGAND | K(i)
-----------------------------
D2 Amisulpride 1.300000
D3 Amisulpride 2.400000I wonder how the mood-brightening effects show through the D-receptor antagonism, though. Wouldn't the extra dopamine still have to compete with the Amisulpride for binding at the necessary receptor sites to improve mood/motivation? Confused.
Posted by florence on December 6, 2007, at 15:42:51
In reply to Re: Here's one!, posted by Anonymoose on December 6, 2007, at 3:09:59
Thanks for more info. Not sure if I can answer your last question. Could it be similar to Remeron (mirtazapine)- in this explanation.. It is an SNRI but I could not figure out why it acted on serotonin..
"By blocking the inhibitory PREsynaptic alpha 2 adrenergic autoreceptors and stimulating only the 5HT1A receptors, it ENHANCES noradrenaline and serotonin release while also blocking 2 specific serotonin receptors: 5HT2 and 5HT3 implicated in dark moods and anxiety.
By contrast, stimulation of the 5HT2A receptors accounts for the INITIAL anxiety, insomnia and sexual dysfunction sometimes reported with the other SSRIs. Stimulation of the 5HT3 receptors causes nausea.
Unfortunately, remeron (mirtazapine) is a potent blocker of the histamine H1 receptors, too. So, it tends to have a somewhat sedative effect. This profile may be good for agitated depressives and insomniacs. Again, it is scarcely a recipe for life-affirmation."
? Increase in D2D3 receptor responsiveness may also be responsible for the clinical AD action of SSRIs.
Not sure where I got the above info...maybe on this site yrs ago.This is from biospychiatry.com Don't know if it is still around...
The Dopamine Connection
What's missing, crucially is vigorous and prolonged stimulation of meso cortico limbic dopamine function. Mesolimbic dopamine system serves as the final common pathway for pleasure in the brain. Enhanced responsiveness of POST-synaptic dopamine D2/D3 receptors is crucial to long term emotional well-being.In so far as they work, all "serotonergic" and "noradrenergic" mood brighteners eventually act on the mesolimbic dopamine pathway, albeit in differing degrees and with varying delay."
Can anyone verify this theory?
I always wondered why Provigil binds to the DA reuptake site and causes an increase in extracellular dopamine, but no increase in DA release......I don't get this..Anyway:sorry I didnt write my sources down all the time. Here's a chart showing affinities to bind to the different receptor subtypes.
Mirapex- D1 0 D2 ++ D3 +++ D2:D3 1:10
Permax- D1 + D2+++ D3 +++ D2:D3 1:1
Parlodel-- D2+++ D3 ++ D2:D3 10:1
Requip- D1 0 D2 ++ D3 +++ D2:D3 1:10Other notes I scribbled down: Mirapex and Requip can induce sleepiness (DUH)
Non-ergotoline drugs Mirapex and RequipPermax which is pergolide) and Parlodel (which is Bromocriptine) are "ergot" drugs......Nausea can occur.
I took a migraine med decades ago called Cafergot which made me vomit/diarhe for over 2 weeks. I only took one dose of 2 pills........I watched a PBS show on the Salem witches and there was a new theory that they were poisoned from ergot- a mold/fungus that grew on the rye grain......Well, guess botox and other junk can be toxic too.I invite any and all corrections to the above info-thank goodness I took notes and eventually printed info on-line.....So much has been taken off the web. florence
This is the end of the thread.
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