Much of the reason for occurrence of side-effects in those taking the anti-parkinsonian drugs in the dopamine-agonist class ; is either the A.) polypharmacological effects and / or unspecified actions of the drug in question, or B.) paradoxically, the selectivity of the drug to only occupy the dopamine D2 class of receptors and thus causing too much cAMP reduction.
However, there are some other factors...
I will speak of specific side-effects and how to counter-act them efficiently, and safely.
You will need to evaluate these methods with your physician and also weigh them in your current situation and with other factors such as your age, blood pressure etc
1.) Sedation, somnolence and / or fatigue ; Dopamine agonists seem to upregulate, and the general, persistent activation of D2 receptors seems to also upregulate, the MU-OPIOID (MOR) receptors (1) (2) - which leads to inhibition of CNS activity; GABA alteration(3), acetylcholine(4) inhibition partly mediate this effect and result in respiratory depression as well as fatigue. Therefore, a mild-moderate mu antagonist may alleviate these unfavorable effects, but may also delay the onset of sleep, and thus should only be taken advantage of during the day.
A simple solution is often overlooked, simply drink Coffee during the day, coffee in it's whole form, either instantized or ground and brewed contains mu-opioid antagonist compounds - CAFFEINE is NOT the chemical responsible for this effect, but rather other chemicals found in the bean / in coffee. <see citation here>
<second source>
You can also use forskolin during the day , or in severe cases, forskolin plus coffee, however, forskolin should be used with caution if on high blood pressure medication(!) (!) (!).
2.) Constipation. (less common than diarrhea)
This also seems to be related to the mu upregulation and also can be counter-acted by drinking coffee(4)(5), however, it could also be related to the reduction in Adenylate Cyclase caused by dopamine agonist drugs - an alternative method besides only coffee consumption is to add FORSKOLIN - which activates adenylate cyclase....because dopamine receptors possess OTHER PROPERTIES besides being negatively coupled to G-Proteins, they do other things besides adenylate cyclase inhibition..using forskolin will NOT diminish the beneficial effects of dopamine agonists - in fact, it may enhance the beneficial effects ...however, forskolin should be used with caution in those on blood pressure medication.
3.)Paradoxical reduction in libido.
Some have reported decreased libido on dopamine agonists, normally, these drugs increase sex drive, but in those that it does the opposite - it probably is due to an over-inhibition of cAMP and / or an overlooked predisposition such as estrogen dominance.
In which case, look for estrogen issues in blood work - if it is high, then using an aromatase inhibitor will be necessary...if it is low - using D-Aspartic acid with your dopamine agonist will help. If no estrogen imbalance exists..then it is probably due to cyclic AMP reduction, in which case...forskolin addition to your dopamine agonist should alleviate the issue.
However, there are some other factors...
I will speak of specific side-effects and how to counter-act them efficiently, and safely.
You will need to evaluate these methods with your physician and also weigh them in your current situation and with other factors such as your age, blood pressure etc
Doing so will ensure a clean counteraction, without diminishing beneficial properties of the drug etc.
1.) Sedation, somnolence and / or fatigue ; Dopamine agonists seem to upregulate, and the general, persistent activation of D2 receptors seems to also upregulate, the MU-OPIOID (MOR) receptors (1) (2) - which leads to inhibition of CNS activity; GABA alteration(3), acetylcholine(4) inhibition partly mediate this effect and result in respiratory depression as well as fatigue. Therefore, a mild-moderate mu antagonist may alleviate these unfavorable effects, but may also delay the onset of sleep, and thus should only be taken advantage of during the day.
A simple solution is often overlooked, simply drink Coffee during the day, coffee in it's whole form, either instantized or ground and brewed contains mu-opioid antagonist compounds - CAFFEINE is NOT the chemical responsible for this effect, but rather other chemicals found in the bean / in coffee. <see citation here>
<second source>
You can also use forskolin during the day , or in severe cases, forskolin plus coffee, however, forskolin should be used with caution if on high blood pressure medication(!) (!) (!).
Your doctor should be fully aware of the interaction with dopamine agonists and opioid analgesics, dopamine agonist drugs should not be used with opiate narcotics or used with extreme caution and careful dose titration.
2.) Constipation. (less common than diarrhea)
This also seems to be related to the mu upregulation and also can be counter-acted by drinking coffee(4)(5), however, it could also be related to the reduction in Adenylate Cyclase caused by dopamine agonist drugs - an alternative method besides only coffee consumption is to add FORSKOLIN - which activates adenylate cyclase....because dopamine receptors possess OTHER PROPERTIES besides being negatively coupled to G-Proteins, they do other things besides adenylate cyclase inhibition..using forskolin will NOT diminish the beneficial effects of dopamine agonists - in fact, it may enhance the beneficial effects ...however, forskolin should be used with caution in those on blood pressure medication.
3.)Paradoxical reduction in libido.
Some have reported decreased libido on dopamine agonists, normally, these drugs increase sex drive, but in those that it does the opposite - it probably is due to an over-inhibition of cAMP and / or an overlooked predisposition such as estrogen dominance.
In which case, look for estrogen issues in blood work - if it is high, then using an aromatase inhibitor will be necessary...if it is low - using D-Aspartic acid with your dopamine agonist will help. If no estrogen imbalance exists..then it is probably due to cyclic AMP reduction, in which case...forskolin addition to your dopamine agonist should alleviate the issue.
Effect of a dopamine agonist on luteinizing hormone receptors, cyclic AMP production and steroidogenesis in rat Leydig cells.
4.) NAUSEA :: Nausea is probably the most common side effect of dopamine agonist drugs, but can be counter-acted easily...though the effects may be prominent and / or annoying, fret not, using high-dose ginger capsules along with ginkgo biloba daily can easily counter act this effect. Use ginger and ginkgo twice a day. Ginger can be taken at night as well.
You can also ask your doc for medications. Some anti-nausea drugs can potentially block the benefits of dopamine agonists - however, there are two exceptions...serotonin antagonists; TROPISETRON and ONDANSETRON(Zofran)
Wow this actually took care of a majority of what made Bromocriptine unbearable- thank you! Question though: I've seen most Forskolin capsules standardized to 250mg, is this the dose you recommend? The dosages I've seen promoted are usually anywhere from 50mg to 250mg so I'd love to have some clarity on the matter from you guys.
ReplyDeleteThank you again!
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