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Concerta (methylphenidate) Time released Ritalin - 10 hour long acting tablet.

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Old 11-02-12, 09:04 AM
alanreyes alanreyes is offline
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A theory as to why many people don't respond to Concerta

The term 'non-responder' pertains to individuals who: feel nothing subjectively while on the drug and those who have not experienced a significant reduction in symptoms.

As for those who suffer from headaches and what-not: make sure to eat something prior to taking the drug, and if you can, eat small meals throughout the duration of your dosage. You might also be taking too much.

Going back to the topic, did a little research regarding the subjective qualities of the drug, and I believe I know the reason why many people generally don't respond to it.

First of all, a large number of people generally won't respond to 18 mg. People are started on this amount in order to gauge their reaction to the drug - so if you feel 'nothing' while on that dosage, that is normal. Your doctor will pull you up.

Now we have the individuals who are on 36 - 72 mg. Many anecdotes do confirm the efficacy of the drug within this dosing range, and I have seen many a happy testimonial amongst individuals on this dosing regimen.

So why does it seem like some people don't respond to dosages as high as 72 mg? I mean, when you calculate the instant release portion of this dosage, you get around 15 mg - the typical dosage for someone using Ritalin, and for those of us who have tried the instant release variant, we can attest to the strength of this amount.

So why isn't the 15 mg instant release portion of a 72 mg, one time Concerta dosage, comparable to 15 mg of Ritalin? The answer is simple: the drug's delivery mechanism.

The instant release component of Concerta is really just its hard shell casing. Once this is dissolved, the osmotic pump mechanism is revealed. Kind of like an edible candy wrapper.

Did an experiment a few days ago. Created a semi-acidic solution, poured it into two translucent cups. Then I put an 18 mg Concerta tablet into one cup, and a 10 mg instant release into the other.

The Ritalin dissolved almost instantaneously, the outer shell of the Concerta, on the other hand, took some time to do so. This explains why people don't get as much as a 'jolt' from the drug as opposed to regular instant release Ritalin, and this is to be expected - the drug was made to prevent these very spikes by letting the instant release portion dissolve slowly.

Which is why a lot of people take instant release Ritalin boosters to go along with their Concerta in the morning - they generally don't have the time to wait for the drug to process, in addition, dosages below 54 mg generally don't release much of the drug instantaneously - you will generally get only around 5 to 6 milligrams from a 32 mg Concerta tablet for example.

Now, second question: I'm on 72 mg of Concerta a day. I should be wired. Why does it feel like 20 to 30 mg a day instead?

Well this is mostly because, again, the drug is released slowly, little by little, like the narrow portion of an hourglass, as to prevent any sudden spikes or highs. But the point is generally moot to some extent seeing as the half-life of methylphenidate is somewhere around 3 hours - the small amounts should stack over the course of this time, so why does it seem to lose its subjective efficacy in such a severe manner over the course of its metabolization?

Again, the delivery mechanism is to blame. It isn't perfect - a portion of the slow release portion of the drug is often not released at all - but there is a solution to this.

Let us assume that you fail to absorb 4 mg for every 18 mg tablet you take - in other words, a certain percentage of the drug is not properly released from the tablet.

Most people take multiples of 18 mg tablets to get to their daily dosages (I.E four 18 mg tablets to get to 72 mg). This is a bad idea. Taking multiples of each tablet multiplies the proportion of the drug lost because of each tablet's mechanical faults.

And a study done by Jansenn has indeed shown that the equivalence values of two 27-mg Concerta tablets with three 18-mg Concerta tablets isn't all that exact, although it is within acceptable parameters.

So the best course of action generally, would be to take a single tablet equivalent to that of your daily dosage. That way, the failure rate of the drug isn't multiplied on to many other tablets. If you are on 36 mg for example, take the 36 mg tablet, if you are on 54 mg, take the 54 mg tablet, and if you are on 72 mg on the other hand, take two of the 36 mg tablets as opposed to multiples of the smaller variants.
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Old 11-02-12, 11:15 AM
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Re: A theory as to why many people don't respond to Concerta

What about the theory that the methylphenidate active ingredient just isn't effective for some people (like my child)?
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Old 11-02-12, 11:28 AM
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Re: A theory as to why many people don't respond to Concerta

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Originally Posted by ConcertaParent View Post
What about the theory that the methylphenidate active ingredient just isn't effective for some people (like my child)?
The theory does indeed have some validity, most especially when speaking from the context of stronger sympathomimetic variants such as Adderall and Dexedrine.

The thing is, methylphenidate isn't really anything more than just a norepinepherine and dopamine reuptake inhibitor. It increases synaptic concentrations of the aforementioned neurotransmitters, but in an indirect and passive fashion - hence it's mild nature as a medication in comparison to that of the latter mentioned ADHD medications.

Adderall does this as well, but more importantly, it also acts as a dopamine pump - moving dopamine intracellularly in a proactive fashion in concert with that of glutamate.

I see you have yet to find a solution for your child's issues. Would you like to talk about his or her case?
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Old 11-02-12, 11:36 AM
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Re: A theory as to why many people don't respond to Concerta

Personally I find that it takes my anxiety away immediately but the other effects such as being able to concentrate, start task and sort of finish them, I have to wait over 7 hours for this.

I forget my meds today and boy was I suffering with anxiety, thatīs when I realised I hadnīt taken it. I went home and took it and was fine without half and hour.
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Old 11-02-12, 11:47 AM
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Re: A theory as to why many people don't respond to Concerta

And I dont find that surprising. The MOA of the drug fits the profile of an anti-depressant - more so than classic 'productivity' enhancer like Adderall for example, primarily due to the aforementioned reason posted above.
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Old 11-04-12, 09:40 AM
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Re: A theory as to why many people don't respond to Concerta

I take 27mg. My problem is that I totally crash by 5:00.

I see my pdoc tomorrow and am going to ask him if I can add an IR in the afternoon to get me through the evening hours.

I tried taking 2 18mg tablets for a couple of days earlier this week, but it felt like too much medication.
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Old 11-04-12, 09:53 PM
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Re: A theory as to why many people don't respond to Concerta

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Originally Posted by alanreyes View Post
The thing is, methylphenidate isn't really anything more than just a norepinepherine and dopamine reuptake inhibitor. It increases synaptic concentrations of the aforementioned neurotransmitters, but in an indirect and passive fashion - hence it's mild nature as a medication in comparison to that of the latter mentioned ADHD medications.

Adderall does this as well, but more importantly, it also acts as a dopamine pump - moving dopamine intracellularly in a proactive fashion in concert with that of glutamate.
I would agree to that testament. I'm no expert and haven't done enough reading on the subject, but this would be my take. The key difference here is dopamine. One increases dopamine production, and one does not. I don't know whether it's been conclusive that a lack of dopamine production and disposal (what's the more technical word for this?) contributes to ADHD or not.

So, let's say a lack of dopamine contributes to ADHD. One person's brain produces a normal amount, but it is quickly absorbed back into neurons. Concerta would work well for this person. Another person has the same problem, but also produces a lower-than-normal amount of dopamine. Amphetamines would work better for this person because they will have higher levels of dopamine, whereas Concerta will not work as well since they still have low levels of dopamine.

This is my completely uneducated guess, I have very little knowledge in chemistry and neuroscience and could be completely wrong!

I agree with your original theory however, because it is exactly what happened to me. I was started on 27mg by an inexperienced provider, bumped up to 54 because there wasn't much of an effect, then decided I wanted off because the side effects were too much. I went to a new doctor who told me he never would have started me on Concerta anyway though...
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Old 11-11-12, 09:35 AM
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Re: A theory as to why many people don't respond to Concerta

And or Concerta could be focusing more on Norepinephrine (Norepinephrine reuptake inhibitor), while Ritalin on the other hand may focus more on the Dopamine side.

or that that's just a little piece of it, its about what your doing and if your focusing,etc
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Old 11-11-12, 09:41 AM
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Re: A theory as to why many people don't respond to Concerta

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Originally Posted by alanreyes View Post
Adderall does this as well, but more importantly, it also acts as a dopamine pump - moving dopamine intracellularly in a proactive fashion in concert with that of glutamate.

I see you have yet to find a solution for your child's issues. Would you like to talk about his or her case?
The thing is when I was on Ritalin it always worked. There were about 5 days in total where Ritalin would make me feel like the Concerta effect. (just calm/slow/etc) -> not wanting to do stuff in a way but was slow.

When Ritalin worked I felt calm/slow/motivated . <- AVG: 98% ~ of the time .
With Concerta I most of the time just feel slow/calm and not wanting to do stuff kinda. <- AVG 85% ~ of the time
- Concerta other times around 30-50% would give little to no effect (if so = the slow effect)
- Concerta rarely would work like the Ritalin (2-4% of the time) / calm/slow/motivated.

Its like Concerta most of the time takes away/does not give the motivation/focus effect. I'm not saying there needs to be a motivation effect for it to "work" but when you have the slow/calm/ effect you don't want to do stuff kinda. When you do have the motivation effect you do want to do stuff. Its like the motivation effect stops the side effects/not wanting to do stuff. -> Ritalin = worked perfectly kinda and stopped the not wanting to do stuff/spaced out effect/side effects/etc <-- along those lines ??


So could it be like Ritalin (mph) focuses more/same on the norepinephrine and dopamine while Concerta some time/mostly focuses more on the norepinephrine?

??

(just an example kinda)
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Old 11-11-12, 12:21 PM
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Re: A theory as to why many people don't respond to Concerta

I kind of feel similar to above, i have taken concerta for a few weeks now going from 18mg up to 54mg and have noticed NO dopamine effects whatsoever... The only significant effects were increased anxiety but those could have been largely exacerbated by other factors.
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Old 11-12-12, 05:52 PM
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Try Adderall if Vyvanse & methylphenidate negative?

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Originally Posted by alanreyes View Post
Adderall does this as well, but more importantly, it also acts as a dopamine pump - moving dopamine intracellularly in a proactive fashion in concert with that of glutamate.

I see you have yet to find a solution for your child's issues. Would you like to talk about his or her case?
If Vyvanse, Concerta, Biphentin and Strattera (so far) have not had significant benefits for my 11-year old daughter, is there any point to trying Adderall or other medication? The school wants her on any medication since they think she is even worse without any medication, but her ADHD ratings continue to be very high and the oppositional defiant behaviours are getting worse compared to pre-medication.
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Old 11-13-12, 04:09 AM
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Re: A theory as to why many people don't respond to Concerta

@Wutun

Ritalin and Concerta are the same. They're methylphenidate. The variances between them have nothing to do with their molecular structure.

Both of them share a preference for the reuptake dopamine and norepinepherine - and yes, both involve the transport of the aforementioned neurotransmitters throughout the synapse much like Adderall.

Adderall is better suited for this role, however. Primarily because apart from fulfilling the aforementioned roles, albeit, to a greater extent, it is also a monoamine oxidase inhibitor.

Monoamine oxidase is responsible for the breakdown of dopamine, adrenaline and serotonin. When this is factored with the presence of a proactive dopamine pump and a potent reuptake mechanism, what one comes across is a stronger sympathomimetic response and yes - a higher risk of neurotoxicity and abuse.

As per the query regarding the difference between Concerta and Ritalin?

How they differ falls on their release mechanism. One of the main reasons why Ritalin has a much more pronounced 'kick' is because it is readily dissolved and absorbed by the GI upon consumption.

When you take 20 mg, you get 20 mg - immediately.

Concerta is different. The drug releases small percentages of methylphenidate throughout the course of the day, thereby accounting for its partial anxiolytic effect without the stimulant-associated sympathomimetic spikes.

Methylphenidate follows a dose-dependent curve. Smaller dosages generally lead to behavioral symptom attenuation and a partial anxiolytic effect.

Larger dosages result in a proverbial tunnel vision and amongst some individuals, particularly first-time takers - euphoria. Once you cross this threshold, you come across most of the non-glucose connected side-effects (jitters, anxiety, palpitations).
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Old 11-13-12, 04:18 AM
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Re: Try Adderall if Vyvanse & methylphenidate negative?

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Originally Posted by ConcertaParent View Post
If Vyvanse, Concerta, Biphentin and Strattera (so far) have not had significant benefits for my 11-year old daughter, is there any point to trying Adderall or other medication? The school wants her on any medication since they think she is even worse without any medication, but her ADHD ratings continue to be very high and the oppositional defiant behaviours are getting worse compared to pre-medication.

Concerta and Biphentin are generally tame sympathomimetic drugs. Vyvanse is simply dextroamphetamine with a lysine group.

Strattera is a norepinepherine reuptake inhibitor. I generally have no idea why this is recommended as an ADHD drug, and I do believe that it will only exacerbate pre-existing anxiety issues by virtue of its mechanism of action.

So getting to the point, I believe this is your question: is there any significant difference between all of the aforementioned and Adderall? And are the differences worth bothering with?

Adderall is considerably more potent than all of the aforementioned drugs, primarily because of its profile. A quarter is composed of the L-amphetamine isomer while the rest is pure d-amphetamine. Both isomers have a similar mechanism of action, yet the former, L-amphetamine, has a preference for norepinepherine and to some extent, a weak effect on dopamine (which is not a problem as the d-amphetamine isomer will cover this role).

If you've gone through Methylphenidate, Strattera and Vyvanse, then I'd try Adderall.
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