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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 10 of 10. This is the beginning of the thread.
Posted by Brainbeard on April 23, 2011, at 6:18:43
I'm experimenting with both options, and have come to some preliminary conclusions. First, let's have a look at this table, showing the pharmacokinetic profile of immediate-release methylphenidate (twice/day) compared with that of the branded and generic sustained-release products (Ritalin immediate release has the little greyish squares and has the highest peaks - hang on, it's a looong web address): http://www.google.nl/imgres?imgurl=http://img.medscape.com/fullsize/migrated/462/703/pharm462703.fig5.gif&imgrefurl=http://www.medscape.com/viewarticle/462703_5&usg=__edIz6njlhSxqSPHFqJtfFLNVZPU=&h=363&w=491&sz=17&hl=nl&start=0&zoom=1&tbnid=tgYVCMkfDaxmvM:&tbnh=118&tbnw=159&ei=TfexTb6_KcjpOdSeuf4I&prev=/search%3Fq%3DPharmacokinetic%2Bprofile%2Bof%2Bimmediate-release%2Bmethylphenidate%2B(twice/day)%2Bcompared%2Bwith%2Bthat%2Bof%2Bthe%2Bbranded%2Band%2Bgeneric%2Bsustained-release%2Bproducts.%26um%3D1%26hl%3Dnl%26sa%3DN%26biw%3D1111%26bih%3D538%26tbm%3Disch&um=1&itbs=1&iact=hc&vpx=115&vpy=71&dur=2326&hovh=193&hovw=261&tx=182&ty=81&page=1&ndsp=18&ved=1t:429,r:0,s:0.
This table shows that Ritalin, i.e. methylphenidate instant release, has blood levels peak up to the second hour, after which they steeply decline. It's around the two hour-mark that I begin to lose the benefits of the drug; this apparently correlates with blood levels beginning to decline.
Now, I experience the same twist of fate on Concerta, after about eight hours, whereas the drug is supposed to cover a twelve-hour time-span. But have a look at this table, where Concerta's pharmacokinetic profile is shown: http://www.google.nl/imgres?imgurl=http://img.medscape.com/fullsize/migrated/462/703/pharm462703.fig6.gif&imgrefurl=http://www.medscape.com/viewarticle/462703_5&usg=__z80IrPU5BiTFOiPF1Tl_LGkfCME=&h=438&w=500&sz=23&hl=nl&start=0&zoom=1&tbnid=msV9HhMcF-DiJM:&tbnh=128&tbnw=146&ei=xO-xTZqRDcuWOqqW1YkJ&prev=/search%3Fq%3DPatrick%2BKS,%2BStraughn%2BAB,%2BJarvi%2BEJ,%2BBreese%2BGR,%2BMeyer%2BMC.%2BThe%2Babsorption%2Bof%2Bsustained-release%2Bmethylphenidate%2Bformulation%2Bcompared%2Bto%2Ban%2Bimmediate-release%2Bformulation.%2BBiopharm%2BDrug%2BDispos%2B1989%253B10:165-71.%26um%3D1%26hl%3Dnl%26sa%3DN%26biw%3D1111%26bih%3D538%26tbm%3Disch&um=1&itbs=1&iact=hc&vpx=443&vpy=65&dur=827&hovh=210&hovw=240&tx=124&ty=122&page=1&ndsp=6&ved=1t:429,r:2,s:0.
As you can see, Concerta, because it is a mixture of instant and extended release, yields an initial peak in blood levels as Ritalin does, only less high. The it plateaus for a while; and then, blood levels continue to rise slowly until they begin to wear off after some eight hours. There we have it again: declining blood levels is what my brain doesn't like.
Interestingly, methylphenidate affects the amygdala - that part of the brain where emotions and memories are intertwined: http://ukpmc.ac.uk/abstract/MED/20208527/reload=0;jsessionid=0CE8457BBD94C9A2D3B10E2B43F5C790.jvm4. The euphoria I experience with peaking blood levels may have its counterpart in the dysphoric meltdown that begins when blood levels start waning.
Now, Concerta has a very innovative delivery system, based on research findings that show that climbing blood levels are most effective for improving performance. I could prevent the eight-hour u-turn by adding Ritalin before blood levels drop.
But my question for you is: what are your experiences with Ritalin IR and Concerta? Do you think there still is a place for Ritalin? Is Concerta tailor fit for your needs? Or do you rely on DIY Ritalin performance-management? Or combine both?
Thanks in advance for any answers and/or feedback.
Posted by pedr on April 27, 2011, at 13:35:19
In reply to Ritalin And/Or Concerta - Which Works For You?, posted by Brainbeard on April 23, 2011, at 6:18:43
Hi BrainBeard,
great post - very illuminating. I'd been looking for such graphs since I have been experiencing very pronounced highs and lows on generic Methylphenidate (i.e. immediate release) which I started taking recently for daytime somnolence from 90mg Nardil. I had previously very happily been taking Provigil but it's effect lessened and ceased, sadly.My experience exactly fits that of the graph. I feel activated, less down and optimistic about MPH from T+30 through T+120 minutes (T is Time taken). However, from T+120 onwards I start to feel anxious, I get tremors, I feel under threat and sometimes I feel pretty depressed too. If I take another dose at this point, this rapidly changes back to optimism and activation.
Seemingly so far, the higher the dose, the more intense these feelings are. 10mg can provide a gentle alertness rather than mood-altering functions. T+120 onwards at that dose often is not that noticeable - no horrible dip into anxiety and negativity. However on other days it provides no alertness at all and I fall asleep at work as usual. Other days it gives me pretty bad Acid Reflux. I think this is to do with how empty my stomach is when I take it.
I'm seeking some kind of stability (aren't we all) and am thinking 120 minute duration up's and down's aren't it. So the ER version seems the next logical step. However I can't get hold of generic MPH ER/LA/CD due to this crazy shortage the US is experiencing. Every pharmacy I've tried has it on back order and do not know when it will next be available!
Cheers,
Pete
Posted by Brainbeard on April 27, 2011, at 16:35:02
In reply to Re: Ritalin And/Or Concerta - Which Works For You? » Brainbeard, posted by pedr on April 27, 2011, at 13:35:19
Hi Pete,
Thanks a lot for your reply.
MPH IR indeed doesn't seem to offer any stability. It might, though, if you'd take it often enough and would time the doses right. But that could mean coming across as a pill junkie...Concerta is only partly covered by health insurance here in Holland, which makes it a very expensive drug.
Posted by mtdewcmu on April 28, 2011, at 19:16:57
In reply to Ritalin And/Or Concerta - Which Works For You?, posted by Brainbeard on April 23, 2011, at 6:18:43
> Now, Concerta has a very innovative delivery system, based on research findings that show that climbing blood levels are most effective for improving performance. I could prevent the eight-hour u-turn by adding Ritalin before blood levels drop.
>Do you have a reference for the finding that increasing blood levels are best? I have noticed that with Ritalin and similar drugs, but I did not know that it was universal or had been studied. Do you know if the same applies to d-amphetamine? Since I got my prescription, it's the first time I've had an ample supply of it, so I haven't figured it out yet. It seems to have benefits even on the way down. With Ritalin, I didn't really get attention benefits from it, but going by the buzz, it seemed as though the benefit was in proportion to the rate of increase (1st derivative) of blood level, rather than blood level itself. That is a real liability if true, because you can only increase so much before you have to come back down. If you need effects for a sustained period, you could end up with excessive levels and suffer a long and unpleasant crash. d-amph seems better all around for me, and effects seem to plateau along with levels and fall off fairly gracefully. But the problem with d-amph is that the half-life is so long that I have to allow like 8 hours to come down enough to sleep.
Posted by Brainbeard on April 29, 2011, at 15:58:12
In reply to Re: Ritalin And/Or Concerta - Which Works For You? » Brainbeard, posted by mtdewcmu on April 28, 2011, at 19:16:57
> Do you have a reference for the finding that increasing blood levels are best?
I read that on Dr. Kenny Handelman's blog: http://www.addadhdblog.com/concerta-ritalin/#a637f.
Posted by Brainbeard on April 29, 2011, at 16:51:29
In reply to Re: Ritalin And/Or Concerta - Which Works For You?, posted by Brainbeard on April 29, 2011, at 15:58:12
> > Do you have a reference for the finding that increasing blood levels are best?
Kenny doesn't give a reference in the blog post, but he does in one of the comments - reference for the ascending blood levels study is http://www.jaacap.com/article/S0890-8567(09)60635-3/abstract
Posted by mtdewcmu on April 29, 2011, at 17:57:18
In reply to Re: Ritalin And/Or Concerta - Which Works For You?, posted by Brainbeard on April 29, 2011, at 16:51:29
> > > Do you have a reference for the finding that increasing blood levels are best?
>
> Kenny doesn't give a reference in the blog post, but he does in one of the comments - reference for the ascending blood levels study is http://www.jaacap.com/article/S0890-8567(09)60635-3/abstractThat's interesting. (Of course, it looks like a small study and was paid for by ALZA.) I am wondering whether it would be better to take a instant-release pill at the end of the day to extend the effects, or if you should take two Concertas a few hours apart. It seems to me that if you add a Ritalin IR at the end of the day as the Concerta stops increasing, you would only wind up with another spike followed by a decline. It may be better to take two Concertas staggered in the morning and midday, but I can't prove this, as my brain is refusing to do the math.
Posted by Brainbeard on April 30, 2011, at 10:47:32
In reply to Re: Ritalin And/Or Concerta - Which Works For You? » Brainbeard, posted by mtdewcmu on April 29, 2011, at 17:57:18
>It may be better to take two Concertas staggered in the morning and midday, but I can't prove this, as my brain is refusing to do the math.
I was playing with the same idea, but when I tried to do the math, I believe I found that it would probably not be all that ideal. My father used to take |Concerta 54mg twice a day, to make sure that any rebound could only happen while he was asleep. That's probably the most practical way to avoid a crash: make sure you crash in your sleep. But this might go hand in hand with insomnia for some, or most. I haven't got much trouble falling asleep even when loaded with stims - my clomipramine plus fluvoxamine get me to dream country soon enough when \I lie down.
On Ritalin, my mood is rather unstable. Concerta yields more consistent results. On Ritalin, I can get an unheimisch, eerie feel about things. On Concerta, my mood is more stable, but I do feel bored sooner than on Ritalin.
I'm trying to get used to a Ritalin-crash, to become immune to it, as it were. Mind over brain, something like that.
Posted by mtdewcmu on April 30, 2011, at 11:52:43
In reply to Re: Ritalin And/Or Concerta - Which Works For You?, posted by Brainbeard on April 30, 2011, at 10:47:32
> I was playing with the same idea, but when I tried to do the math, I believe I found that it would probably not be all that ideal. My father used to take |Concerta 54mg twice a day, to make sure that any rebound could only happen while he was asleep. That's probably the most practical way to avoid a crash: make sure you crash in your sleep. But this might go hand in hand with insomnia for some, or most. I haven't got much trouble falling asleep even when loaded with stims - my clomipramine plus fluvoxamine get me to dream country soon enough when \I lie down.
>That's nice that you aren't given to insomnia. My ability to fall asleep is brittle.
I gave this problem some more thought. The way to properly extend the concentration curve might be to take a dose of Concerta in the morning, followed by twice that dose around midday. So you could take a 27mg tab upon awakening, and a 54mg tab at noon. That way your levels would keep ascending even as the first one gave out.
> On Ritalin, my mood is rather unstable. Concerta yields more consistent results. On Ritalin, I can get an unheimisch, eerie feel about things. On Concerta, my mood is more stable, but I do feel bored sooner than on Ritalin.
>Ritalin didn't really do anything good for me at all, except for an occasional, fleeting buzz at the beginning. I've never tried Concerta, but I wonder how much better it might be.
Posted by torridcalm on May 5, 2011, at 18:54:39
In reply to Ritalin And/Or Concerta - Which Works For You?, posted by Brainbeard on April 23, 2011, at 6:18:43
concerta lasts a bit longer and maybe the rebound isn't as bad can't say for sure it's been to long since I've been on ritilin. I've been trying to potentitate concerta with zanax and magnesiun glynate, I read something about calcium chanels and magnisium, I also read something about B-2 blockers. I think my rebound is milder, but maybe the constant state of anxiety I'm in right now is masking the rebound. doing my best with spelling.
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