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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 16 of 16. This is the beginning of the thread.
Posted by Amigan on March 22, 2008, at 12:08:38
Hello.
Has anyone noticed an increase on his blood pressure while he/she is on Selegiline?
I do, although i'm not 100% sure that Selegiline is responsible for this, but it is the prime suspect. I only take a micro dose of Sulpiride with it, currently.
I take 10-15mg orally. Although, dietary restriction is not nessecary at this dosage, i do avoid tyramine-rich foods, so the rise in my BP is not tyramine related.
So.. I basically want to ask 2 things:a)Has anyone else experienced this?
b) what is the best medical approach to treat Seleiline-induced hypertension?
Ca-blockers?
B-blockers?
ACE inhibitors + a diuretic?
Don't suggest clonidine, please. I know that it should be effective, but it also kind-of cancels the effect of Selegiline due the sedation it causes.
Posted by dbc on March 22, 2008, at 16:29:38
In reply to High blood pressure on Selegiline!, posted by Amigan on March 22, 2008, at 12:08:38
NAIUs abd Blood Pressure meds dont play well together im not sure what you can do.
Posted by dbc on March 22, 2008, at 16:30:16
In reply to Re: High blood pressure on Selegiline!, posted by dbc on March 22, 2008, at 16:29:38
That previous message should read "MAOIs and"
Posted by bulldog2 on March 22, 2008, at 19:24:57
In reply to High blood pressure on Selegiline!, posted by Amigan on March 22, 2008, at 12:08:38
> Hello.
> Has anyone noticed an increase on his blood pressure while he/she is on Selegiline?
> I do, although i'm not 100% sure that Selegiline is responsible for this, but it is the prime suspect. I only take a micro dose of Sulpiride with it, currently.
> I take 10-15mg orally. Although, dietary restriction is not nessecary at this dosage, i do avoid tyramine-rich foods, so the rise in my BP is not tyramine related.
> So.. I basically want to ask 2 things:
>
> a)Has anyone else experienced this?
>
> b) what is the best medical approach to treat Seleiline-induced hypertension?
> Ca-blockers?
> B-blockers?
> ACE inhibitors + a diuretic?
> Don't suggest clonidine, please. I know that it should be effective, but it also kind-of cancels the effect of Selegiline due the sedation it causes.
>Yes I've noticed an increase in BP on as little as 10 mg. Might be the amphetemine in it. Wonder if the liquid would be better as it has no amphetemine.
Posted by undopaminergic on March 23, 2008, at 14:15:59
In reply to High blood pressure on Selegiline!, posted by Amigan on March 22, 2008, at 12:08:38
> Hello.
> Has anyone noticed an increase on his blood pressure while he/she is on Selegiline?
> I do, although i'm not 100% sure that Selegiline is responsible for this, but it is the prime suspect. I only take a micro dose of Sulpiride with it, currently.
> I take 10-15mg orally. Although, dietary restriction is not nessecary at this dosage, i do avoid tyramine-rich foods, so the rise in my BP is not tyramine related.
> So.. I basically want to ask 2 things:
>
> a)Has anyone else experienced this?Transiently, at some point when starting it, I noticed such a tendency. On the other hand, many people have experienced a hypotensive effect (even more so with L-dopa).
> b) what is the best medical approach to treat Seleiline-induced hypertension?
> Ca-blockers?
> B-blockers?
> ACE inhibitors + a diuretic?
> Don't suggest clonidine, please. I know that it should be effective, but it also kind-of cancels the effect of Selegiline due the sedation it causes.The most logical agents would seem to be alpha1-adrenergic antagonists (doxazosin, prazosin, etc.) and alpha2-adrenergic agonists (guanfacine, guanabenz). I've used guanfacine, as it has been shown to improve working memory and ADHD (those benefits are more subtle, however, than with stimulants - especially in cases complicated by other symptroms such as apathy and lack of energy).
Posted by Amigan on March 23, 2008, at 16:07:57
In reply to Re: High blood pressure on Selegiline!, posted by undopaminergic on March 23, 2008, at 14:15:59
> > Hello.
> > Has anyone noticed an increase on his blood pressure while he/she is on Selegiline?
> > I do, although i'm not 100% sure that Selegiline is responsible for this, but it is the prime suspect. I only take a micro dose of Sulpiride with it, currently.
> > I take 10-15mg orally. Although, dietary restriction is not nessecary at this dosage, i do avoid tyramine-rich foods, so the rise in my BP is not tyramine related.
> > So.. I basically want to ask 2 things:
> >
> > a)Has anyone else experienced this?
>
> Transiently, at some point when starting it, I noticed such a tendency. On the other hand, many people have experienced a hypotensive effect (even more so with L-dopa).
>
> > b) what is the best medical approach to treat Selegiline-induced hypertension?
> > Ca-blockers?
> > B-blockers?
> > ACE inhibitors + a diuretic?
> > Don't suggest clonidine, please. I know that it should be effective, but it also kind-of cancels the effect of Selegiline due to the sedation it causes.
>
> The most logical agents would seem to be alpha1-adrenergic antagonists (doxazosin, prazosin, etc.)Interesting. I know about this agents. I didn't include them on the list because i thought that they are not effective for the treatment of hypertension. Mainly because i haven't yet see/hear a doctor prescribing them to a patience with high BP.
> and alpha2-adrenergic agonists (guanfacine, guanabenz). I've used guanfacine, as it has been shown to improve working memory and ADHD (those benefits are more subtle, however, than with stimulants - especially in cases complicated by other symptroms such as apathy and lack of energy).
Yes but, isn't guanfacine awfully similar to Clonidine?.. :)
Posted by undopaminergic on March 25, 2008, at 16:58:00
In reply to Re: High blood pressure on Selegiline!, posted by Amigan on March 23, 2008, at 15:07:57
>
> > and alpha2-adrenergic agonists (guanfacine, guanabenz). I've used guanfacine, as it has been shown to improve working memory and ADHD (those benefits are more subtle, however, than with stimulants - especially in cases complicated by other symptroms such as apathy and lack of energy).
>
> Yes but, isn't guanfacine awfully similar to Clonidine?.. :)There are important differences that make their characterisation as "awfully similar" a definite exaggeration. For exmaple, in contrast to clonidine, guanfacine has preferential affinity for the alpha2A-adrenoceptor subtype and little affinity to imidazoline receptors. These differences may explain some of the results described in:
http://www.nature.com/npp/journal/v21/n4/abs/1395372a.html
http://www.nature.com/npp/journal/v20/n5/abs/1395310a.htmlInterestingly, the EMSAM prescribing information suggests that selegiline is an alpha2B-agonist.
Posted by Amigan on March 26, 2008, at 16:05:08
In reply to Re: High blood pressure on Selegiline!, posted by undopaminergic on March 25, 2008, at 17:58:00
> >
> > > and alpha2-adrenergic agonists (guanfacine, guanabenz). I've used guanfacine, as it has been shown to improve working memory and ADHD (those benefits are more subtle, however, than with stimulants - especially in cases complicated by other symptroms such as apathy and lack of energy).
> >
> > Yes but, isn't guanfacine awfully similar to Clonidine?.. :)
>
> There are important differences that make their characterisation as "awfully similar" a definite exaggeration. For exmaple, in contrast to clonidine, guanfacine has preferential affinity for the alpha2A-adrenoceptor subtype and little affinity to imidazoline receptors. These differences may explain some of the results described in:
> http://www.nature.com/npp/journal/v21/n4/abs/1395372a.html
> http://www.nature.com/npp/journal/v20/n5/abs/1395310a.htmlI see. Ok.
> Interestingly, the EMSAM prescribing information suggests that selegiline is an alpha2B-agonist.
Never heard of it before. I don't even know what this means. I use to think that selegiline could cause hypertension due to its "catecholamine-enhancing" properties. NE enhancing in this case. I mean, Dopamine alone, can even cause a drop in blood pressure, which is consistent with what you posted earlier in this thread.
Right?
Posted by undopaminergic on March 27, 2008, at 3:58:20
In reply to Re: High blood pressure on Selegiline! » undopaminergic, posted by Amigan on March 26, 2008, at 16:05:08
> > Interestingly, the EMSAM prescribing information suggests that selegiline is an alpha2B-agonist.
>
> Never heard of it before. I don't even know what this means.It means that selegiline can stimulate one of the three known subtypes of alpha2-adrenoceptor. The A subtype is the one relevant for lowering BP, regulating noradrenaline release (autoreceptor) and enhancing spatial working memory, and also functions as a presynaptic receptor on at least some serotonergic and glutamatergic terminals. I don't have a good understanding of what the B and C subtypes do, and they appear to be much less common. However, the B-type may play a role in regulating pupil size - have you noticed any effect of selegiline on your pupils? I've seen a clear tendency to a reduction.
> I use to think that selegiline could cause hypertension due to its "catecholamine-enhancing" properties. NE enhancing in this case. I mean, Dopamine alone, can even cause a drop in blood pressure, which is consistent with what you posted earlier in this thread.
> Right?Yes. The relative contributions of MAO-B inhibition (ie. phenylethylamine) and selegiline and its metabolites remain an interesting question. Could the cardiovascular effects be avoided by replacing selegiline with rasagiline? Last time I checked, there were no reports on the matter except as regards anaesthetised rats and very high doses (incidentally co-authored by the inventor of rasagiline).
Posted by Amigan on March 27, 2008, at 16:50:59
In reply to Re: High blood pressure on Selegiline!, posted by undopaminergic on March 27, 2008, at 3:58:20
> I don't have a good understanding of what the B and C subtypes do, and they appear to be much less common. However, the B-type may play a role in regulating pupil size - have you noticed any effect of selegiline on your pupils? I've seen a clear tendency to a reduction.
I haven't notice a change, but i'm not sure.
Posted by Dopamine123 on April 3, 2008, at 15:50:56
In reply to Re: High blood pressure on Selegiline!, posted by undopaminergic on March 23, 2008, at 14:15:59
You could try lowering the dose. MAO-A inhibition kicks in at a higher dose of selegiline and leads to an increase in norephinephrine. At a lower dose, you are more likely to just get the MAO-B inhibition and dopamine increase.
Probably a beta blocker would be the best drug to try to prevent the increase in blood pressure due to norepinephrine.
Posted by Amigan on April 3, 2008, at 16:06:01
In reply to Re: High blood pressure on Selegiline!, posted by Dopamine123 on April 3, 2008, at 15:50:56
> You could try lowering the dose. MAO-A inhibition kicks in at a higher dose of selegiline and leads to an increase in norephinephrine. At a lower dose, you are more likely to just get the MAO-B inhibition and dopamine increase.
I believe that i already receive a relatively low dose, but,
> Probably a beta blocker would be the best drug to try to prevent the increase in blood pressure due to norepinephrine.how sure are you about this? From what i have read, beta blockers can have exactly the opposite results in the present of a sympathomimetic factor and perhaps in cases of excessive NE, too.
The Beta receptors in blood vessels are responsible for vasodilation, while the Alpha receptors for vasoconstriction. THUS, if you block the B receptors, while the Alpha ones remain stimulated by the excessive N,NE or the SM factor, you have an increase in blood pressure.
Posted by undopaminergic on April 3, 2008, at 22:04:23
In reply to Re: High BP on Selegiline! B-Blockers, good?, posted by Amigan on April 3, 2008, at 16:06:01
>
> > Probably a beta blocker would be the best drug to try to prevent the increase in blood pressure due to norepinephrine.
>
> how sure are you about this? From what i have read, beta blockers can have exactly the opposite results in the present of a sympathomimetic factor and perhaps in cases of excessive NE, too.
> The Beta receptors in blood vessels are responsible for vasodilation, while the Alpha receptors for vasoconstriction. THUS, if you block the B receptors, while the Alpha ones remain stimulated by the excessive N,NE or the SM factor, you have an increase in blood pressure.
>Beta2-adrenoceptors mediate many of the (usually) desirable effects of adrenaline - including vasodilation, bronchodilation, and reduction of allergic responses, although they also increase heart rate, and their improvement of muscular blood flow may have undesirable side-effects (e.g. tremor). Selective beta1-adrenergic antagonists ("cardioselective" beta-blockers) should leave the beta2-receptors alone, but their primary effect is to reduce heart rate, which will reduce blood pressure, but not reverse the effects of vasoconstriction caused by selegiline-induced noradrenaline release (assuming that is the cause of your elevated BP).
An interesting (but unrelated) question is the psychoactive effects of beta-blockers (some of them cross the blood-brain-barrier easily), and more generally, the role of beta-receptors in the brain.
Posted by Amigan on April 4, 2008, at 0:39:51
In reply to Re: High BP on Selegiline! B-Blockers, good?, posted by undopaminergic on April 3, 2008, at 22:04:23
> >
> > > Probably a beta blocker would be the best drug to try to prevent the increase in blood pressure due to norepinephrine.
> >
> > how sure are you about this? From what i have read, beta blockers can have exactly the opposite results in the present of a sympathomimetic factor and perhaps in cases of excessive NE, too.
> > The Beta receptors in blood vessels are responsible for vasodilation, while the Alpha receptors for vasoconstriction. THUS, if you block the B receptors, while the Alpha ones remain stimulated by the excessive N,NE or the SM factor, you have an increase in blood pressure.
> >
>
> Beta2-adrenoceptors mediate many of the (usually) desirable effects of adrenaline - including vasodilation, bronchodilation, and reduction of allergic responses, although they also increase heart rate, and their improvement of muscular blood flow may have undesirable side-effects (e.g. tremor). Selective beta1-adrenergic antagonists ("cardioselective" beta-blockers) should leave the beta2-receptors alone, but their primary effect is to reduce heart rate, which will reduce blood pressure, but not reverse the effects of vasoconstriction caused by selegiline-induced noradrenaline release (assuming that is the cause of your elevated BP).No. We are not talking about adrenoreceptors. I'm talking about ordinary, post-synaptic antagonism of the B adrenergic receptor (the standard pharmacological action of all B-Blockers)
Blockage of these receptors in the heart, does lead to decreased heart rate and output, but in the small blood vessels, COULD lead to vasoconstriction, (increased BP) especially in the presence of sympathomimetic drugs for the reasons which i have already explained in my previous post.
Posted by undopaminergic on April 4, 2008, at 4:16:47
In reply to Re: High BP on Selegiline! B-Blockers, good?, posted by Amigan on April 4, 2008, at 0:39:51
> > >
> > > > Probably a beta blocker would be the best drug to try to prevent the increase in blood pressure due to norepinephrine.
> > >
> > > how sure are you about this? From what i have read, beta blockers can have exactly the opposite results in the present of a sympathomimetic factor and perhaps in cases of excessive NE, too.
> > > The Beta receptors in blood vessels are responsible for vasodilation, while the Alpha receptors for vasoconstriction. THUS, if you block the B receptors, while the Alpha ones remain stimulated by the excessive N,NE or the SM factor, you have an increase in blood pressure.
> > >
> >
> > Beta2-adrenoceptors mediate many of the (usually) desirable effects of adrenaline - including vasodilation, bronchodilation, and reduction of allergic responses, although they also increase heart rate, and their improvement of muscular blood flow may have undesirable side-effects (e.g. tremor). Selective beta1-adrenergic antagonists ("cardioselective" beta-blockers) should leave the beta2-receptors alone, but their primary effect is to reduce heart rate, which will reduce blood pressure, but not reverse the effects of vasoconstriction caused by selegiline-induced noradrenaline release (assuming that is the cause of your elevated BP).
>
> No. We are not talking about adrenoreceptors. I'm talking about ordinary, post-synaptic antagonism of the B adrenergic receptor (the standard pharmacological action of all B-Blockers)
>Then you are talking about adrenoceptors - more precisely, you're talking about the blockade of post-synaptic beta-adrenoceptors (or beta-adrenergic receptors, if you prefer, but that's the same thing).
Anything else about what I wrote that needs further clarification?
Posted by bulldog2 on April 4, 2008, at 15:34:52
In reply to Re: High BP on Selegiline! B-Blockers, good?, posted by undopaminergic on April 4, 2008, at 4:16:47
Clonodine would probably help with bp but it might negate the effect of the selegiline.
Possibly magnesium to relax the blood vessels.
This is the end of the thread.
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