What is Wellbutrin?
Wellbutrin is a trade name of bupropion, which is a generic name.
Depression affects about fourteen million people in the United States and we don't know what causes depression. Is it an environmental condition, a developmental condition, a genetic condition? Or is it as things are getting popularized in an epigenetic condition?
What chemicals are involved in depression? Is it the serotonin, noradrenaline, dopamine or what other kinds of the monoamine is involved in this condition?
Popularly people talk about how they're depressed, but in medicine, you have to have at least five of nine symptoms. And those symptoms include feeling depressed, having a low mood, feeling tearful, having a decreased interest or pleasure in most activities. Sometimes there's significant weight change, change in your sleep pattern, in your level of activity. Maybe you have fatigue or loss of energy, feelings of guilt or worthlessness, a decreased ability to concentrate or the feeling you want to commit suicide.
You have to have at least five of nine of symptoms and one of them has to be either depressed mood or a loss of interest. If you see the family doctor with those kinds of symptoms chances are only 50/50 that you'll have that diagnosis.
Remember, bupropion is not the same thing as buprenorphine that's to help get you off of the opioids. When we're talking about the antidepressant, the Wellbutrin or the bupropion is one of the most frequently used antidepressants in the United States and in Canada. It's used by itself or as an add-on medicine to one of the SSRIs drugs like Lexapro, Prozac, Zoloft.
It's sold as Wellbutrin to treat depression, but the exact same thing is sold as Zyban to help get you off cigarettes. It doesn't seem to work very well for that, by the way.
The drug was initially synthesized 1969 and then it went through a series of different owners. Now it happens to be owned by Valeant Pharmaceuticals.
The Food and Drug Administration approved it as an antidepressant in 1989. In 2003 it came out as the extended release form. In 2006 it was approved for treatment of the seasonal affective disorder syndrome - the wintertime depression.
It became very popular because it was thought that compared to the other antidepressants, there was less weight gain taking this pill. That's, probably, not actually true. Over the course of a year, you lose about five pounds more than you lose with the placebo. It was thought to make you less sleepy, to cause less sexual dysfunction than the SSRIs.
Actually, that got him into a lot of trouble. It was being promoted off-label and actually ended up with the owners of the drug at the time, GlaxoSmithKline GSK, paying a three billion dollar fine because they were paying doctors.
Which of the antidepressants is best?
Is it better if you take Effexor, Zoloft, Lexapro, Remeron, Paxil or Prozac or Wellbutrin?
Actually, overall there seems to be relatively little difference. It's a trial and error approach. This equal opportunity disease affects people less than age 20 and more than age 60. It also affects women about three times more often than men. And 10% of the people who take the drug take are going to end up stopping it because of side effects and adverse reactions to the drug.
When Is Wellbutrin Effective?
Wellbutrin seems to help with different aspects of cognition, mood and behaviour. If you happen to have depression, sleepiness or fatigue maybe you would opt for bupropion rather than an SSRI. But if you have depression with some anxiety, maybe drugs like Lexapro would be a better choice.
If you happen to have pneumonia and you take penicillin, you get better. If you happen to have depression and you take an antidepressant, chances are you'll have about 50% symptom reduction in about half of the people, maybe three-quarters of the people. You'll have remission in only about 1/3 of the peopled. Compared that to the placebo where you have significant symptom reduction in somewhere between a quarter and a half of the people and remission in somewhere between 1 in 3 and 1 in 6.
Oftentimes people don't get better with first, the second antidepressant they take. Question is the add-on or do you substitute for - there's no good data even today about this.
We rate depression on the Hamilton depression score. It is a test that has 21 items, 17 of them are graded and you get a different kind of score. A score goes from a very severe depression to severe depression, moderate depression, mild depression or normal, It's rated on the type of symptoms you have. That tells us how bad your depression is.
If you take Wellbutrin and you have very severe depression, statistically you're going to end up with moderate depression. If you take a placebo you'll still have severe depression. There were several tests and we've come up with the same answer all the time. Symptoms do not go away, they just seem to get better.
If you happen to have seasonal affective disorder syndrome and you know it's going to come, you take the pills in advance and take them for several months throughout wintertime. Some people even take it forever.
The Mechanism Of Action
It prevents the reuptake of norepinephrine and dopamine, so there's more of that floating around the cell. That is why we call Wellbutrin an atypical antidepressant. It also works on the nicotinic receptor.
The drug doesn't seem to change the serotonin, histamine or the acetylcholine. Actually, it appears that this drug is altered inside the body to at least three metabolites. And the metabolites are actually even more effective than the drug itself.
You can take Wellbutrin SR in the regular immediate release. You take 100 milligrams twice a day, then you go up to 100mg 3 times a day with up to 450 milligrams total. It takes about four weeks for the full antidepressant activity.
If you're taking the extended-release the XL version, you take 150 milligrams. Then after four days, you can bump it up to 300 milligrams with a maximum dose 150mg.
Be cautious if you have liver or kidney abnormalities. In this case, you should take it only if it's absolutely necessary.
If you're pregnant or bread feeding and you're taking the drug, you better not suddenly discontinue it.
Taking alcohol, seizure medicine or a sedative together with Wellbutrin is dangerous because you might have a seizure.
The drug is the same thing as Zyban. You shouldn't combine the two. If you happen to take an MAO inhibitor, then you shouldn't take Wellbutrin for at least two weeks.
Wellbutrin Side Effects
Side effects are observed in 1 people of 10 people who take the drug. Most common side effects include dry mouth, nausea, dizziness, weight loss or some constipation.
Other rarer side effects include agitation, rash, ringing in the ears, blurred vision, feeling tired, changing your taste, more urination than normal. You don't feel well, you get restless or you have anxiety.
The drug can increase your blood pressure, activate the manic phase of bipolar disease. If you take the drug it might increase the manic portion of the disease.
It can also cause acute angle closure of glaucoma in people who have narrow angles.
The likelihood of a serious allergic reaction to the pill is relatively small, but since we know it can cause seizures, have to be very careful.
We know it can cause mania. If you have racing thoughts, excessive energy or you're reckless and your behaviour is impulsive, it is a risk of developing mania or hypomania. Obviously, go see your doctor right away.
If you have any blurred, tunnel vision, you see halos around lights then you might be having glaucoma.
Certainly, some people who take the drug can develop agitation, hostility, paranoia, confusion.
Interestingly, the drug can cause a false positive test for methamphetamine. The major problem with the drug is the potential for suicide or suicidal thoughts, especially if you're under age 25.
When the drug originally came on the market back in the late 1980s, there seemed to be an increased incidence of seizures associated with the drug, but only with the immediate release form and only at a relatively high dose. It was taken off the market for a short period of time.
Obviously, there's a problem with epilepsy. Anything that predisposes to epilepsy should mean that you shouldn't take this pill. If you have bulimia, brain tumour, if you drink too much alcohol, used benzodiazepines or if you're withdrawing from alcohol or a benzodiazepine, probably, shouldn't be taking these kinds of drugs. They can lower the threshold seizure, especially, if you happen to be taking drugs that you wouldn't even think could be associated with epilepsy. For. instance if Cirpo, corticosteroids, the tricyclic antidepressants, drugs like theophylline for asthma or alcohol.
Thre is a bupropion-induced psychosis. That's where you can develop delusions, hallucinations, paranoia or confusions. Who are at risk? People taking a high dose, having bipolar disease, taking lithium. Also, people who are older and are abusing substances.
That's a potentially major problem because seizures can develop in a third of the people. They can also experience hallucinations, loss of consciousness, abnormal heart rate. If you take another kind of medicines, in addition, you can develop fever, muscle rigidity, extreme fall in your blood pressure or extreme elevation in your blood pressure, stupor, coma and respiratory problems. You can die from this stuff.
It's metabolized to a series of other compounds that are active in the body and present and higher concentrations than the bupropion. Interestingly, even though we've known about the drug for an awfully long time, just in 2016 we found three new metabolites that also are very active in the body. And they're as important as the metabolites we knew about beforehand.
The concentration in the body can range about fivefold different in different people. There's a question about - how the drug works? How much of the drug is going to be in your system? If you happen to take certain kind of medicines that inhibit an enzyme used to metabolize the drug, then you might end up with more drug in your system than you bargained for.
If you happen to also be taking Paxil, Prozac or Zoloft, Valium - they all increase the concentration of bupropion in the system. On the other hand, if you're taking alcohol, St. John's wort, Dilantin or phenobarbital, that can decrease the amount in the system.
Generic bupropion or Wellbutrin came out in 2006. It was said to be bioequivalent, but they only tested the 150-milligram pill. They didn't test the 300 pill, they just figured that it was going to be the same thing, just twice as much of it.
Unfortunately, the delivery system was different. It didn't seem to be as effective, it caused an increased incidence of seizures and people had a headache, gastrointestinal disorders. fatigue and anxiety. This was all reported in about 2007.
The FDA said now it's just the natural variation of the disorder. But actually, they asked the drug companies to check to see if there was any problem. The drug companies didn't do it. So, the FDA took it upon itself.
By 2012 it found that the 300-milligram pill was equivalent to the generic only by 2 different manufacturers out of 10. This problem has now been taken care of.
Wellbutrin For Other Disorders
Some people say it helps for attention deficit disorder – ADHD. Teachers think it works, the parents and the clinicians don't think it works. It is not even a first, second or third choice.
Some people use it as an add-on treatment with the mood stabilizer. And People who have bipolar disorder doesn't seem to be any significant harm, maybe benefit, maybe not.
Some people tried it for discontinuation of cocaine use. It didn't seem to work. There's very weak evidence that it'll help you get off methamphetamine. There is no evidence that it helps for low back pain, no evidence that it really is good for neuropathies.
How Much Does Wellbutrin Cost?
The cost of the medicine will make you sick. If you want to take the brand name and you want the Wellbutrin XL - one month of therapy at 150 milligrams is going to cost you cash price $1400. If you take the 300-milligram pill it will cost you cash about $2000 dollars.
If you want to go get the generic product, it is going to cost you about with 22 bucks or something like that.
Valeant Pharmaceuticals owns the brand name. They charge almost $50 cash price for that pill. The generic variety cost $1.50.
Valeant Pharmaceuticals has had some funny business that's gone on. They have the network of affiliated pharmacies that were selling this drug. And there are unanswered questions related to some of the business practices of Valiant.
The relationship has persisted even though they got in trouble several years ago because of a special relationship they had with Philidor, which was a speciality pharmacy. It was selling some of their dermatologic products.
Even though the drug company continues to raise the price of this drug, that's been available forever. Even though the number of prescriptions has fallen by about 50% over the past two years, the revenue has risen by about a third just something because they keep jacking up the price.
On the other hand, if you want to take Prozac with the coupon, get that for between $2 and $5 dollars. Zoloft cost you with the coupon around 9 – 12 bucks.
In summary, it seems that the antidepressants almost are a trial-and-error type drug. You take one for a month or so if you have a depression and see if it helps. If it doesn't, you can stop it and start another one.
There's nowhere near 100% efficacy of any of these drugs. In fact, if you have a 50% reduction in the symptoms, you can consider yourself lucky. That only happens in about half of the people who are taking the drug.
Unfortunately, the symptoms are just reduced. If you stop the drug, the symptoms tend to recur.
Fortunately, there's a lot of research being done in this area and, hopefully, we're going to have some better therapies in the relatively near future.