11 replies to this topic

[linda82]

Hi!

First of all I have to say that I'm impressed by all the knowledge here! I've learned so much over the past few weeks.

That said...I have a small issue with my wellbutrin. My doctor is on holiday for the next 6 weeks but he said it's ok to experiment with nootropics....uhh..ok.

 

What I'm taking:

 

morning

150mg Wellbutin

vit c 1000mg

vit E 400mg

vit D 4000iu

Omega 3

 

afternoon

primrose oil

vit b6 50mg (these 2 for severe PMS)

 

I take L theanine 300mg in the evening. My doctor told me to take this in the morning but it literally makes me fall asleep.

 

So wellbutrin at first was great, I take this for adhd and anxiety. For 6 months it was awesome. But it has stabilized (i guess) and I have noticed a lack of concentration and motivation. Also I seem to forget a lot but it seems to be normal when on Wellbutrin. Decreased energy level as well. Not as bad as it was before but it's just not enough to keep working. I keep being distracted.

 

I'v read about Modafinil but as my doc is on Holiday I can't get that for now. So I was thinking about Noopept. Could that just give me that extra boost that I need? Or is there something else that I could add?

Thank you so much!

 

 

[psychejunkie]

You have developed tolerance to Wellbutrin because of dopaminergic and noradrenergic receptors down-regulation, meaning lowered density/number/metabolism/activity of these receptors in presence of Wellbutrin has made them less sensitive.

 

You can either get some time off from Wellbutrin or lower the dosage to let the receptors recover; or take another medication/supplement/nootropics to up-regulate Dopaminergic/Noradrenergic receptors, like Sulbutiamine which is available OTC.

 

btw, increasing the dosage only helps in short-time as those receptors will again start to down-regulate further!

 

Good luck

[linda82]

Thanks! I'll talk to my doctor about lowering the dosage. As for now I have the extended release version so I can't splitt the capsule. I have indeed tried to take 2 pills but it made me feel horrible!

I'll check out Sulbutiamine.

 

Would Noopept be an option?

Edited by linda82, 19 June 2016 - 11:22 AM.

[psychejunkie]

Thanks! I'll talk to my doctor about lowering the dosage. As for now I have the extended release version so I can't splitt the capsule. I have indeed tried to take 2 pills but it made me feel horrible!

I'll check out Sulbutiamine.

 

Would Noopept be an option?

 

Noopept would modulate AMPA Receptors and Acetylcholine Neurotransmission, won't really help with AD/HD symptoms!

But you can try Pramiracetam, Its an stimulant and not really a racetam which might help you. Although Pramiracetam may worsen Anxiety. So, start by taking low dose and increase it gradually to find the effective dosage.

 

Good luck

[linda82]

Thanks! I'm defenitely checking that out.

Will tell here what it does when I've tried it.

[Finn]

What ADHD meds, anxiolytics or antidepressants had you tried before, or was Wellbutrin the first one? How did you react to those?

 

 

At least for atomoxetine (Strattera) there doesn't seem tolerance.

 

http://www.jpeds.com...0095-3/abstract

Two-year data from this ongoing study indicate that atomoxetine maintains efficacy among adolescents with ADHD, with no evidence of drug tolerance and no new or unexpected safety concerns.

 

 

My guess is that non-stimulant ADHD medication are more like antidepressants than stimulants when it comes to tolerance, many people benefit from them for years or decades, for some people they might just poop out at some point, same could apply to bupropion (Wellbutrin).

[Finn]

Thanks! I'll talk to my doctor about lowering the dosage. As for now I have the extended release version so I can't splitt the capsule. I have indeed tried to take 2 pills but it made me feel horrible!

I'll check out Sulbutiamine.

 

Would Noopept be an option?

 

 

Methylphenidate and Atomoxetine Enhance Prefrontal Function Through α₂-Adrenergic and Dopamine D₁ Receptors 

 

http://www.sciencedi...890856710005228

 

 

The stimulants, methylphenidate, Concerta and amphetamine, lisdexamphetamine (Vyvanse, Elvanse), and the nonstimulant, atomoxetine, increase norephinedrine (NE) and dopamine (DA) transmission in the prefrontal cortex whereas guanfacine and clonidine mimic NE actions at α2A receptors

 

 

https://en.wikipedia...harmacodynamics

The occupancy of dopamine transporter (DAT) ) sites by bupropion and its metabolites in the human brain as measured by positron emission tomography was just 14% in an independent study, a subsequent study looked at the actual extracellular concentrations of dopamine in the human brain after an acute oral treatment of bupropion and failed to observe any increase, concluding that the weak DAT occupancy was not sufficient to increase dopamine level.

 

The most important example of this is bupropion's most major metabolite, hydroxybupropion, a selective norepinephrine reuptake inhibitor (and likely releasing agent) and nACh receptor antagonist that lacks significant dopaminergic actions, which, with oral bupropion treatment, can reach area under the curve (AUC) plasma concentrations that are as much as 16–20 times greater than those of bupropion itself.

 

So bupropion is more like a pro-drug of hydroxybupropion. 

 

Most likely it relieved your ADHD through it's NRI mechanism.

 

α₂ agonists, guanfacine and clonidine were to the markets as blood pressure medication to treat hypertension, so their side effect profile is in someways opposite to the side effect profile of other ADHD meds, stimulants and non-stimulant NRIs, which can actually cause hypertension. The bad thing is that in Europe guanfacine is only accepted as in the extended release formulation for ADHD, so there is no cheap generic instant blood pressure medication version like in USA. Clonidine, which is available in cheap form in Europe, is less "precise" it targets more other receptors and is also metabolized mostly by CYP2D6, CYP2D6 is inhibited by bupropion (Wellbutrin), so this could lead to too high clonidine levels

 

Since guanfacine's side effect profile is somewhat opposite to that of bupropion, you might even be able to take 300 mg of bupropion it while on it.

Edited by Finn, 22 June 2016 - 03:58 PM.

[Finn]

Guanfacine is also anxiolytic

 

https://en.wikipedia...iki/Guanfacine 

Another psychiatric use of guanfacine is for treatment of anxiety, such as generalized anxiety disorder and post-traumatic stress disorder symptoms. Guanfacine and other α2A agonists have anxiolytic-like action, reducing sympathetic arousal in the emotional responses of the amygdala, and strengthen prefrontal cortical regulation of emotion, action and thought.

 

 

 

Intuniv: ANNEX I SUMMARY OF PRODUCT CHARACTERISTICS

 

http://www.ema.europ...WC500195130.pdf

Adults and elderly

 

The safety and efficacy of guanfacine in adult and the elderly with ADHD has not been established and therefore should not be used in this group.

 

Safety concerns aspect is probably BS. Guanfacine has been used as blood pressure med for ages in USA, and adults and elderly tend to take more antihypertensives than 6-17 year olds do, so guanfacine is even more tested in adults/elderly group than it is 6-17 year olds.

 

In Finland, Intuniv (extended release guanfacine) is already in pharmacies, but even 6-17 year old ADHD patients, the only group for which European Medicinines Agency has approved this drug officially, don't get compensation automatically, though I would guess Pharmaceuticals Pricing Board will give 6-17 yearl old ADHD patients automatic compensation within year.

 

In Finland though, like probably in most western or northern European countries, you can do an individual compensation application for any pharmaceutical substance. For example, the only wakefulness substance for which narcoleptic patients get automatic compensation is modafinil, those who need methylphenidate, or dexamphetamine or lisdexamphetamine to stay awake, they have to make an individual compensation application Pharmaceuticals Pricing Board if they want to get compensation. Doctor states that modafinil was tested but it didn't help enough, etc. Since ADHD stimulants are cheaper than modafinil here, or in lisdexamphetamine's case about the same price, these applications tend be accepted pretty easily.

 

Here Intuniv is slightly cheaper than some other accepted adult ADHD medicines like Strattera (atomoxetine) and Elvanse (lisdexamphetamine), so I think chances of a proper application going through would be pretty high.

 

I would think that Netherlands or France has similar option to make a individual application. 

 

In the application your doctor could point out how guanfacine acts on α₂  receptors, just like the first line adult ADHD medication atomoxetine and methylphenidate do. 

http://www.sciencedi...890856710005228

 

Point out the reason why you can't use the first line ADHD medications, whether it is anxiety, blood pressure etc.

 

Maybe point out the extensive use of it in adults as antihypertensive, thus indication for it being safe for adults.

 

Also there seemed to be some positive articles of guanfacine for adult ADHD in Google Scholar, you could add some of them to application in addition to that methylphenidate atomoxetine  α₂  receptors article.

Edited by Finn, 22 June 2016 - 08:27 PM.

[linda82]

Hi,

 

So there it is, Modafinil. i got the prescription, it has costed me a fortune and I'm not sure that I'm happy about it....It makes me feel like a robot.

Not sure what to do now...Something else again or stop all the medication I have? What to do with this Modafinil. Can't believe the price of this stuff.

[Mind_Paralysis]

Sell it. People are always looking for Modafinil.

 

Anyways, Guanfacine, Intuniv is an excellent suggestion, I suggest you try that next. Which version of ADHD do you have though? ADHD-C, or ADHD-PI?

If you're mainly Predominantly Inattentive, then the traditional treatments may not work.

 

I am PI -  aka Sluggish Cognitive Tempo, and the stimulant drugs have limited effect on me - that includes Modafinil, sadly.

 

I think it might be worth it to try Strattera for you, since it was originally meant as an antidepressant, but showed insufficient effect (SSRI's were still better, even though it was better than placebo) and it does have a somewhat similar effect to Bupropion - being an NRI.

 

If you're classically hyper-active then your best bet is Focalin (dexmethylphenidate) though - all of the benefits, less of the side-effects.

[Finn]

Bupropion (Wellbutrion) usually isn't the first line ADHD med, anxiolytic or antidepressant prescribed in Europe. What ADHD meds, anxiolytics or antidepressants had you tried before, or was Wellbutrin the first one? How did you react to those? This information would make it easier to give advice.

 

 

Edited by Finn, 13 July 2016 - 06:56 AM.

[Finn]

It seems that in Netherlands, based on this one site, clonidine is also available in 25 micro gram tablets, whereas in many EU countries it is available only in 150 micro gram tablets. 

 

http://www.medicijnkosten.nl/

 

 

Clonidine is metabolized only 2/3 by CYP2D6, 1/3 is processed by other CYP enzymes. So if you have access to the smaller dose tablets, finding proper dosing with clonidine even when using CYP2D6 inhibitor like Wellbutrin, could be manageable. Clonidine is dirt cheap, about 6.5-8.5 cents per 25 micro gram tablet according to that site, so it could be a cheaper alternative to guanfacine. 

 

I don't know if France has 25 micro gram tablets, or just 150 micro gram ones, but as a Dutch I guess you visit Netherlands occasionally, you could get them from there if they are not available in France.

 

 

 

 

Edited by Finn, 13 July 2016 - 10:57 AM.