Wellbutrin (buproprion) is a relatively weak antidepressant and has a low reported rate of withdrawal syndrome compared to the SSRIs and SNRIs such as Paxil, Effexor, or Cymbalta.
However, patients have reported withdrawal symptoms, sometimes severe, from too-short tapering.
Buproprion is a bit of an oddball because it "is thought to be" a dopamine and norepinephrine reuptake inhibitor and a nicotinic receptor antagonist, which is why it is sometimes used to help people stop smoking.
Buproprion adverse effects
Like Chantix, as a smoking cessation aid (Zyban), buproprion has been found to cause suicidal thoughts or actions and displays an FDA black box warning accordingly.
Buproprion tends to be energizing and often causes anxiety, agitation, nervousness, loss of appetite, and insomnia as side effects. Buproprion usually is not an appropriate treatment for withdrawal symptoms, as it can aggravate them.
While it is less likely to cause sexual dysfunction like other antidepressants, other side effects are: lowers the seizure threshold (very bad for brain zaps), increases blood pressure, tremors, tinnitus, unusual behaviour changes, agitation, and hostility.
Bupropion as an adjunct to antidepressants to counter sexual side effects
Way back in ancient history, around the year 2000, it became apparent these fabulous wonder drugs, the SSRIs, which were supposed to alleviate depression with almost no side effects, had a huge drawback that might slow sales: They caused sexual dysfunction in a high percentage of those who took them.
This caused great consternation among the pharmaceutical companies, who went through varying cycles of denying that sexual dysfunction was a frequent consequence of SSRIs, claiming the sexual dysfunction was due to the underlying depression, and searching for pharmaceutical solutions to this adverse effect.
It was also observed that buproprion had fewer sexual side effects and that some patients found it sexually stimulating. Seizing the opportunity to preserve their sales, the drug companies initiated campaigns to educate doctors that, in the rare cases where sexual dysfunction was a problem, buproprion might be added to an SSRI to alleviate the problem.
It did seem to help some, but its usefulness for this purpose is mostly a product of drug company propaganda. Also, to preserve sales of SSRIs, the drug companies neglected to inform doctors that being an antidepressant itself, Wellbutrin might replace the SSRI, and there was no reason to keep people on two drugs when one drug would do.
(Later, when Viagra and Cialis became available, much research and furor was generated to recommend them as adjuncts to SSRIs -- adding yet another profitable drug. Alas, they proved to be ineffective for women.)
Buproprion, unfortunately, comes with a few common adverse effects of its own, such as jitteriness, agitation, nervousness, and sleeplessness. Doctors were advised to add benzodiazepines to the mix for these symptoms. (Later, these symptoms were judged to be possible symptoms of bipolar disorder, indicated the addition of antipsychotics such as Seroquel.)
This ushered in the era of the common combination of an SSRI, buproprion, and a benzo (or low-dose Seroquel) for many people complaining of any kind of "depression." As all of these drugs incur physiological dependency, this cocktail is very well represented on this site.
But some doctors noticed buproprion was also an antidepressant as effective or ineffective as any other, without the sexual side effects. They began to prescribe buproprion first, before resorting to an SSRI. Wellbutrin or its generic buproprion is a very popular antidepressant. And that is why our Tips for tapering off Wellbutrin, IR, SR, XR, XL (buproprion) is the most frequently viewed topic in the Tapering forum. (Tips for tapering off Pristiq (desvenlafaxine) is a distant second, probably because tapering Pristiq is so difficult.)
There are 3 buproprion formulations: IR, SR, XL or XR
Name-brand Wellbutrin or generic buproprion is available in 3 variations with different half-lives -- the amount of time they last in your body (see below).
From the manufacturers' and the FDA's information (see below), the different versions are bio-equivalent. The only difference is the frequency of the dosage:
- Immediate release (IR): 3 times a day dosing
- Sustained release (SR): 2 times a day dosing
- Extended release (XR or XL): Once a day dosing
Name-brand Wellbutrin XL was manufactured by GlaxoSmithKline but is currently manufactured by Valeant Pharmaceuticals. Name-brand Wellbutrin SR is still manufactured by GlaxoSmithKline. Generic manufacturers also make their own versions of IR, SR, and XR or XL buproprion.
There may be slight differences in formulation between brand-name Wellbutrin and the generic versions, and among the generic versions. For exact information about formulation of a generic version, you would have to contact the generic manufacturer.
It is metabolized by P450 cyp2B6 liver enzyme, and conflicts with alcohol metabolism. Its half-life is complicated because it has a number of active metabolites and various versions that prolong release of the active ingredient.
How gradually should I taper buproprion?
There is little information about tapering off Wellbutrin, probably because it is assumed not much of a taper is needed.
As with all other psychiatric medications, do not skip doses to taper. If you're susceptible to withdrawal symptoms, this is an excellent way to trigger them.
If you are very sensitive, you may wish to start with a 10% reduction per month, as we recommend with other antidepresssants. Base your decrease on the last dosage: The amount of the decrease keeps getting smaller.
If you find 10%-per-month decreases cause no problem, you may wish to make them more often.
Personally, I found a 50mg taper per week to be sufficiently gradual. I had been taking 150mg-200mg for about a year and had adverse effects (blood pressure spikes). Although I had Paxil withdrawal syndrome at the time, quitting Wellbutrin in this fashion did not increase my symptoms. (Getting off Wellbutrin was a relief. I found ramping up on it a lot harder.)
If you wish to be moderately cautious, you may wish to taper at 18.75mg every two weeks, cutting up 75mg immediate-release or sustained-release tablets into quarters (see below).
If you get withdrawal symptoms when tapering by 18.75mg every 2 weeks, reduce the amount of your dosage decrease to 10% and extend the tapering interval to 4 weeks.
How to taper off Wellbutrin XR or XL or Budeprion XL (extended release)
From FDA information Wellbutrin: http://dailymed.nlm....21-2081cfd5ae3e
- Available as brand-name only [Wellbutrin XR or XL] in 150 mg, 300 mg extended-release tablets
- To be taken once a day. This is equivalent to 3-times daily immediate-release buproprion or twice-daily bupropion SR.
Switching Patients from WELLBUTRIN Tablets or from WELLBUTRIN SR Sustained-Release Tablets: When switching patients from WELLBUTRIN Tablets to WELLBUTRIN XL or from WELLBUTRIN SR Sustained-Release Tablets to WELLBUTRIN XL, give the same total daily dose when possible. Patients who are currently being treated with WELLBUTRIN Tablets at 300 mg/day (for example, 100 mg 3 times a day) may be switched to WELLBUTRIN XL 300 mg once daily. Patients who are currently being treated with WELLBUTRIN SR Sustained-Release Tablets at 300 mg/day (for example, 150 mg twice daily) may be switched to WELLBUTRIN XL 300 mg once daily.
From the manufacturer, GlaxoSmithKline http://public.gsk.co...er-information/
What WELLBUTRIN XR contains
The active substance is bupropion hydrochloride. WELLBUTRIN XR tablets come in different strengths. Each tablet contains either 150mg or 300mg of bupropion hydrochloride.
The other ingredients are:
- tablet core: polyvinyl alcohol, glyceryl dibehenate
- tablet coating: ethyl cellulose, povidone K-90, macrogol 1450, methacrylic acid ethyl ecrylate copolymer dispersion, silicon dioxide, triethyl citrate
- printing ink: shellac glaze, iron oxide black (E172) and ammonium hydroxide.
If you cut up Wellbutrin or buproprion XR, what's inside is regular immediate-release bupropion. When you break the time-release coating, the tablet loses its extended-release characteristic and you would be taking buproprion IR.
According to GSK regarding Wellbutrin XL http://us.gsk.com/pr...llbutrinXL.pdf:
For patients taking 300 mg/day....the dose should be tapered to 150 mg/day for 2 weeks prior to discontinuation.
This suggests a taper of 50% for two weeks, then quit at 150mg. We recommend a more gradual taper than this.
Tapering methods for extended-release versions:
- Cut up Wellbutrin XL or XR tablets
If you cut up a Wellbutrin XL or XR tablet, you get immediate-release buproprion.
Since the smallest XL/XR tablet is 150mg, we recommend converting to buproprion SR or immediate-release buproprion so you can cut up the tablets to make reductions by 25mg or less.
If you cut up a 150mg or 300mg XL/XR tablet into quarters to taper, you will need to take some 3 times a day, as it's become immediate-release bupropion. (We do not recommend tapering this fast, do this at your own risk.)
- Switch from Wellbutrin XR/XL to other types of buproprion
This may be a little bumpy at first. A switch from XR/XL to SR probably would be smoother than a switch to immediate-release buproprion.
If you want to taper off Wellbutrin XL or XR, you can:
- Switch to the SR version and cut up tablets, take 2x a day
- Switch to the immediate-release version and cut up tablets or, for lower dosing, make a liquid with water, take 3x a day
- How to taper off Budeprion XL (extended release)
From FDA information: http://dailymed.nlm....fc-e70945a352ed
- Available as brand-name only (Budeprion XL) in 150 mg extended-release tablets
- To be taken once a day. This is equivalent to 3-times daily immediate-release buproprion or twice-daily bupropion SR.
Same as tapering Wellbutrin XL or XR, above.
How to taper off bupropion SR (sustained release)
From FDA information: http://dailymed.nlm....00-cb4832172ece
- Available as brand-name or generic in 100 mg, 150 mg, 200 mg sustained-release tablets
- To be taken twice daily, "at least 8 hours between successive doses." (This is equivalent to 3-times daily immediate-release buproprion.)
According to Merck http://www.merckmanu.../bupropion.html
"Data from the manufacturer states that dividing Wellbutrin SR® tablets resulted in an increased rate of release at 15 minutes: “However, the divided tablet retained its sustained-release characteristics with similar increases of released bupropion at each sampling point beyond 15 minutes when compared to the intact Wellbutrin SR® tablet...” Bupropion is hydroscopic and therefore should be stored in a dry place. Splitting of large quantities in advance of administration is not advised since loss of potency may result. If necessary, splitting should be done cleanly without crushing."
In the name-brand Wellbutrin SR, the sustained-release quality is in the binder, the glue that holds the tablet together. Generic versions (which would be called buproprion SR, not Wellbutrin SR) may be made differently. Contact the manufacturer to find out exactly how the tablet is formulated, or talk to a pharmacist specializing in psychopharmacology.
I personally found you CAN cut Wellbutrin SR (sustained release) tablets up -- the timed-release mechanism is mixed in with the drug. Put the pieces in a water-tight container and use them up within 24 hours because the time-release binder can absorb humidity and degrade.
For a short time, I cut up generic 100mg bupropion SR and took 50mg in the morning, Wellbutrin XL 150mg a couple of hours later, and another SR 50mg in the early evening for a total of 250mg/day. (I never tolerated Wellbutrin very well.)
To taper, convert your dosage to 100mg SR tablets, cut up the 100mg tablets, make reductions by 25mg or less, take 2 times a day.
(Note: If you cut an SR tablet in very small fragments or crush it, it won't to continue to be sustained-release -- the binder is extensively damaged. Take as though it was immediate-release.)
Taper with a mix of sustained-release (SR) and immediate-release (IR) tablets
As immediate-release tablets come in the smallest dosage of 75mg, which can be quartered into pieces of 18.75mg, you might want to convert part of your daily dose to IR tablets.
This will enable you to taper by 18.75mg at a time.
You might be able to get by with taking the SR tablet in the morning and the IR tablet at night.
Taper with immediate-release buproprion
From FDA information: http://dailymed.nlm....8d-647855c53dbb
- Available in generic form as 75 mg, 100 mg immediate-release tablets
- Half-life of 10 hours, plus some extension with the active metabolites, for a total half-life expressed as 21 (±9) hours
- "Bupropion should be administered 3 times daily, preferably with at least 6 hours between successive doses."
To taper, cut a 75mg or 100mg tablet into quarters, make reductions by 18.75mg-25mg, take 2 or 3 times a day.
If you get withdrawal symptoms at any point, slow down.
You may wish to taper more cautiously, by 10%. Using a liquid to taper makes measuring very small decreases much easier and precise. To make a liquid from immediate-release buproprion:
- Get a prescription from your doctor for a liquid from a compounding pharmacy
- Make a liquid yourself with water, see How to make a liquid from tablets or capsules
Weigh capsule fragments with a digital scale
If you can't do any of the above, you may wish to cut up tablets and weigh the fragments with a digital scale to control your tapering rate. This could apply to any type of buproprion -- remember that, when cut up, an XR tablet becomes immediate-release and an SR tablet may retain some of its sustained-release quality.
See Using a digital scale to measure doses
Edited by Altostrata, 22 February 2015 - 10:29 AM.