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Has anyone tried Bupropion Immediate-Release?


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I've been taking Bupropion for 3 months now. I've tried 300mg-XL, 2x150mg-SR, and both times (though I'd take the morning dose at 6AM) had a hard time falling asleep at night, tossing around in bed an hour or so. I normally don't have a sleeping problem. So, I now take only one 150mg-SR around 7AM and no afternoon dose. I can fall asleep fine now, but my energy runs out in the late afternoon ...
 
I'm wondering if I should take 2x100mg(immediate-release) instead, at 7AM and 2PM or something ... I heard that the effect of one dose should last about 6-8 hours, as opposed to SR lasts for 12 hours ... am I correct?
 
If anyone has tried immediate-release, could you share your experience with me? Did it work okay (gave you energy and focus)?  Did you feel the side effects (anxiety, irritability, etc) were worse than XL or SR? Did your mood sink when it started to wear off?  

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No you can't take 200mg of Bupropion as immediate-release, the limit for a single dose of  immediate-release formulation is 150 mg. It is clearly stated in the prescribing information. This is to lessen the chance of a seizure. For single doses higher than 150 mg you must move to the SR formulation and the maximum single dose of the SR is 300 mg. To get to 450 mg taking SR you would take 300 mg SR as one dose and 150 SR latter in the day. Or move to one of the once a day pills, like the XL formulation. 

If you want to take 300 mg total daily and do it with  immediate-release tabs, you would need to do 3 evenly spaced doses of 100 mg IR or 4 evenly spaced doses of 75 mg.

 

 

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Thank you for your reply. Perhaps the way I wrote was misleading ... 

I meant "2x" as "twice a day", not 2 tablets as one dose. So, what I'm currently thinking is,
100mg(immediate-release) twice a day at 7AM and 2PM ...
 
Sorry for the confusion.

Edited by Irene Iesu
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On 9/2/2016 at 8:09 PM, Irene Iesu said:

If anyone has tried immediate-release, could you share your experience with me? Did it work okay (gave you energy and focus)?  Did you feel the side effects (anxiety, irritability, etc) were worse than XL or SR? Did your mood sink when it started to wear off?  

I am currently on IR and have never had one bad experience on it, and no bad side effects (no anxiety, no irritability).  Yes, it did give me energy and it allowed me to focus, but only on the IR kind.  The SR which I took a long time ago did not help me at all (I know it helps some people, just not me).  If I take my current IR dose separated, then no, my mood does not sink.

I currently take 100 mg 2x/day of the IR, and am allowed to go up to 300mg/day divided into 3 doses.  I have never had any problems with doing so, and the IR is the only kind of buproprion that helps me.

 

 

 

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12 hours ago, melissaw72 said:

I currently take 100 mg 2x/day of the IR, and am allowed to go up to 300mg/day divided into 3 doses.  I have never had any problems with doing so, and the IR is the only kind of buproprion that helps me.

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Thank you Melissa, that's good to know! I was kind of afraid that, since so many people taking either XL or SR, there must be some negative aspects about IR (other than the frequency of administering) ... I'm thinking of regularly taking 100mg-IR 2x/day and take an extra evening dose when working late or attending social events ... (I wonder if it's okay that the daily dosage fluctuates ...?) 

So, do you feel a surge of energy right after taking it, and it gradually subsides in about 6 hours? No sudden drop? How long an interval do you usually take between the doses, 6 hours? One site suggested you can take another dose in 4 hours (before the previous dose wears off) ... I want to avoid ups and downs in my mood if I can ...  Around what time do you usually take your second dose? ... Sorry for many questions!

Edited by Irene Iesu
I don't know why but I can't delete those 2s in the middle.
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2 hours ago, Irene Iesu said:

I'm thinking of regularly taking 100mg-IR 2x/day and take an extra evening dose when working late or attending social events ... (I wonder if it's okay that the daily dosage fluctuates ...?) 

(in bold) I would ask your pdoc about this.  I'm not sure.  Daily doses for me sometime go between the 200 mg and 300 mg/day without problems.  But everyone is different when it comes to meds.  So I'd ask your DR if s/he agrees (or not) with the way you are taking the med.  Do you have enough pills to cover you for the month if you take an extra evening dose?  If you only have enough for 2x/day, you'll run out of pills before the month is over with and before you can refill next.

No, I don't feel a surge of energy when I take it.  Even when I first started it, I didn't feel like that.  It just kind of slowly "woke me up" so I wasn't so tired all the time.  My body is used to it now, so I think I'm just maintaining levels in my body.  No sudden drop.

I take the first dose in the early morning when I wake up.  About 4-5 hours later I take the 2nd dose, and that covers me until the next morning.

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I have an appointment with my doctor in a few days, I'll ask her. My current prescription is 150mg-SR twice a day, so I think she wouldn't have a problem prescribing me for 100mg-IR three times a day. I'll try to limit to two tablets most days, unless taking three would give me only extra energy but no unwanted side effects and/or no interference with my sleep.

I'm encouraged to know someone is using IR tablets and getting a satisfying result. If I can take the next dose in 4 hours, then I can take the last dose of the day by 3PM even when I take three tablets a day, so that would be nice. I'm relieved to hear that you don't experience ups and downs. Well, I know everyone reacts to the meds differently, so I'll try it and see it for myself. Your replies helped me make the decision. Thank you!!

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When I think I need to take the extra one to make it 3/d, and I do, and then start having tremors and just feel jittery, I know that I didn't need it and go right back to 200/d.  I'd watch out for stuff like that. 

Your DR might recommend starting out at 2/day, then go up to 3/d if needed.  From personal experience.

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I had an appointment with my Pdoc yesterday. And you were right, Melissa, she prescribed me 100mg-IR x2/day to start. She wants to see how I'll do for a month before increasing it to x3/day. 

I took one this morning at 6:30 while I was still in bed, and in 15 min. or so I was able to get out of bed easily. I didn't particularly feel a "surge" or anything ... just that the heavy fogginess I usually have in my head wasn't there. I kind of felt my body getting warm and a little sweaty, but not to the point that was too uncomfortable.

It's the first time in a long while that I didn't need a caffeine pill to get out of bed in the morning! And I didn't experience any restlessness or anxiety, just calm steady energy so far ... It's only just one day, but seems to be a good start :)
 

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5 hours ago, Irene Iesu said:

I had an appointment with my Pdoc yesterday. And you were right, Melissa, she prescribed me 100mg-IR x2/day to start. She wants to see how I'll do for a month before increasing it to x3/day. 

I took one this morning at 6:30 while I was still in bed, and in 15 min. or so I was able to get out of bed easily. I didn't particularly feel a "surge" or anything ... just that the heavy fogginess I usually have in my head wasn't there. I kind of felt my body getting warm and a little sweaty, but not to the point that was too uncomfortable.

It's the first time in a long while that I didn't need a caffeine pill to get out of bed in the morning! And I didn't experience any restlessness or anxiety, just calm steady energy so far ... It's only just one day, but seems to be a good start :)
 

That is great to hear that is it helping!  I hope it works for you past the first day.  Starting the med off on 200 mg IR is a good idea, because going to 300 mg first try might cause unwanted side effects.

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2 hours ago, JustNuts said:

Bupropion IR is generally considered to have a negative risk-benefit equation because of the higher risk of seizures, suboptimal pharmacokinetic profile, and need for tid/qid dosing. It's a bit odd for your pdoc to RX it.

 
 
 

 

It was not my doctor's idea to suggest IR tabs, but mine. I've tried both XL and SR for the daily dosage of 300mg. Both times I had a hard time falling asleep at night (I took the second dose of SR at 2PM). SR tabs are said to last for 12 hours, so technically the effect won't wear off until 2AM and I thought that might be the reason that I'm tired in the morning. So I asked my doc if I can try IR (only lasts for 6 hours, so the effect will subside by my bedtime).
 

It's only been a few days, but taking 100mg-IR twice a day seems to be working for me. I think my sleep quality has gotten better since I can get out of bed without taking a caffeine pill. I was worried that IR would give me too much energy all at once (thus make me jittery and excitable) and later I'd have a sudden mood drop ...  But no, I don't feel any ups and downs ... just steady wakefulness ...

 

P.S. I like your description of your condition/medication :)  You must be a very witty, creative person!  

Edited by Irene Iesu
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8 hours ago, JustNuts said:

Bupropion IR is generally considered to have a negative risk-benefit equation because of the higher risk of seizures, suboptimal pharmacokinetic profile, and need for tid/qid dosing. It's a bit odd for your pdoc to RX it.

(in bold) Why?  If the XL and SR don't work, what is the problem for trying the IR?  Sometimes (at least personally) it helps better than any other form of buproprion.  And what does the "need for tid/qid dosing mean?"  A lot of (most) other meds have to be split in doses also, so what makes wellbutrin IR any different (regarding the dosing)?  And who takes Wellbutrin IR qid (4 times a day)?  I have never heard of any person taking more than 300 mg / day (100 mg, 3/day) of the IR version.  Someone please correct me if I am wrong.

Buproprion IR lowers the seizure threshhold, which is why the dose starts out slow.  Personally the IR is the only kind that works for me (I have a history of seizure activity too, with no problems), and my pdoc never found it "odd" to prescribe. (If he did, he would not have prescribed it).  The main thing my pdoc also told me was to not go off of it cold-turkey because that would make a person more likely to have a seizure. 

So why is it a "bit odd" for OPs DR to prescribe it to her?

 

5 hours ago, Irene Iesu said:

It's only been a few days, but taking 100mg-IR twice a day seems to be working for me. I think my sleep quality has gotten better since I can get out of bed without taking a caffeine pill. I was worried that IR would give me too much energy all at once (thus make me jittery and excitable) and later I'd have a sudden mood drop ...  But no, I don't feel any ups and downs ... just steady wakefulness ...

Works well for me too.  I'm glad you found something that helps you.

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Why ? It is all about steady state. Meds that can maintain a steady state work better and more consistently. The XL formulation wins this race hands down. IR is the worst.

Wellbutrin has multiple metabolites, many or all are active, some with long half lifes and some just measured in a few hours.  You want AD's to last all day and that is hard with a short half life. An extended release formulation smooths this out so you can be on a consistent blood level all day and night with just one dose.

 

 

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3 hours ago, notloki said:

Why ? It is all about steady state. Meds that can maintain a steady state work better and more consistently. The XL formulation wins this race hands down. IR is the worst.

Why make a blanket statement (in bold) like this?

Not true for everyone.  In no way does Wellbutrin SR work better and consistently for me.  IR is the best one for me to get any use out of.  Wellbutrin SR had hardly any effect on me.  It didn't change anything, being a steady-state med.  And it definitely didn't last a whole day in one dose.

 

3 hours ago, notloki said:

An extended release formulation smooths this out so you can be on a consistent blood level all day and night with just one dose.

With the SR what I did feel (which wasn't much) didn't last all day with one dose.  I could barely feel any change with the SR, which was why the change for IR.  And the IR works so much better for me.

Everyone metabolizes and reacts to meds differently, so not everyone has the best effect on the XL or SR. 

I think it should be a YMMV type-thing.  The statements you make aren't true for everyone.  And like I said YMMV.

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14 minutes ago, melissaw72 said:

Ok, so the XL has the lowest seizure rate, but I don't think there is a smooth stead state especially with just one dose for everyone, personally speaking.

 

XL is considered to have the most ideal PK profile. Source: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1163271/

XL is dosed ONCE DAILY. Some people may do better on SR, which has an acceptable PK profile but is generally considered inferior to XL for most people.

Edited by JustNuts
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59 minutes ago, notloki said:

The fact remains the XL has the lowest seizure rate due to it's smooth steady state.

 

From the link in above post (that JustNuts provided):

Source: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1163271/

 

Quote

The incidence of seizure with bupropion XL has not been evaluated

 

Other than that, I'm out of this conversation.

Edited by melissaw72
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Seizure is a concern for anyone who takes Bupropion. I researched about it a bit myself when I considered taking it. And I actually read the same article.

It states: 

"An important adverse event associated with bupropion use is seizure. With the IR formulation, the rate is 0.4% (4/1000) at doses of 300 to 450 mg/day; however, the rate increases substantially at doses above this level. With the SR formulation, the rate is 0.1% (1/1000) at the target dose of 300 mg/day."

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1163271/

So yes, IR has four times higher rate of occurrence of seizure than SR. But still the rate is 4 in 1000, which means that 996 people are not likely to experience seizure even from IR. 

Also, I found an article that seems to vouch for the safety of IR. But the funny thing is though, under my insurance coverage, the cost of IR for the same dosage is higher than SR, actually more than twice (perhaps the article was written before generic SR was available?) ... but being able to sleep better is more important to me — I want the effect to be gone by bedtime, which is not possible with SR. 

"Conversion from sustained-release bupropion to immediate-release bupropion appears to be safe. Single 200-mg doses of immediate-release bupropion can apparently be administered to some patients without inducing excessive adverse effects, including seizures. Marked reduction in drug acquisition costs can be achieved with this conversion."

http://www.ncbi.nlm.nih.gov/pubmed/15977913

 

The only thing I worried was, "Could IR cause a rollercoaster-like ups and downs in my mood?" ... and I've experienced nada of such mood-swings. So, I'm content with IR tabs so far. 

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