Medications

Wellbutrin XL (Bupropion XL)

Author, Hen Caspi

Edited by, Ben Bauer, MD

November 4, 2016

Name (commercial and generic):

Commercial name: Aplenzin; Budeprion SR [DSC]; Buproban [DSC]; Forfivo XL; Wellbutrin SR; Wellbutrin XL; Zyban

       Generic name: Bupropion hydrochloride XL

Class:

Norepinephrine-dopamine reuptake inhibitor antidepressant

What disorder(s) is it often prescribed for (approved uses)?

Major depressive disorder

Smoking Cessation Aid

What symptoms does it treat?

Approved uses:

Helps with improving mood and feelings of well-being.
 Also used to prevent seasonal affective disorder (SAD).

Off-label uses:

Treat attention deficit hyperactivity disorder (ADHD)

Assist smoking cessation by decreasing cravings and nicotine withdrawal effects (Bupropion under the name Zyban)

Treat the depressive phase in bipolar disorder in combination with other mood stabilizers.

Treat anxiety in people with depression.

http://www.webmd.com/drugs/2/drug-76851/wellbutrin-xl-oral/details

Side effects:

Common:

Dry mouth; Sore throat; Dizziness; Drowsiness; Nausea; Vomiting
; Headaches
; Decreased appetite/weight loss; Constipation
; Trouble sleeping
; Increased sweating
; Shaking/tremor
; Fast heartbeat.

Rare:

Skin rash; Sweating; Ringing in the ears; Shaking/tremor; Muscle pain
; Hallucinations; Anxiety.

http://www.wellbutrinxl.com/

http://www.webmd.com/drugs/2/drug-76851/wellbutrin-xl-oral/details#interactions

http://www.nami.org/Learn-More/Treatment/Mental-Health-Medications/Bupropion-(Wellbutrin)

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

Additional Serious Side Effects:

Seizure- Increased risk with history of head injury, brain tumor, liver disease, alcohol dependency, or eating disorder. In order to reduce the risk of seizure, healthcare provider should assess the following particularly (among others) 
before prescribing the medication: patient factors, clinical situations, and 
concomitant medications.

Extra caution should be given before Wellbutrin XL is administered to 
patients with a history of seizure, cranial trauma, or other predisposition toward seizure, or patients treated with other agents (e.g., antipsychotics, other antidepressants, theophylline, systemic steroids, etc.) that increase seizure probability. Patients should cease taking Wellbutrin XL and contact their healthcare provider as soon as possible if a seizure occurs while on treatment.

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

Cardiac (heart) effects: high blood pressure, increased heart rate.

http://www.nami.org/Learn-More/Treatment/Mental-Health-Medications/Bupropion-(Wellbutrin)

Wellbutrin XL may increase suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder and other psychiatric disorders. Please see section about Black Box Warnings for further details.

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

http://www.wellbutrinxl.com/

Long Term Use:

As an antidepressant, the prescription of this drug is often times intended to be for long term use. Thus, developing of tolerance with time is likely, which may result in a desire to increase frequency or amount of Wellbutrin XL to obtain the desired effect(s). This may also lead to overdose. Hence, it is particularly important to adhere to the prescribed amount by your healthcare provider.

There are no other known problems associated with long term use. Wellbutrin XL is considered a safe and efficient medication when used as prescribed.

http://www.nami.org/Learn-More/Treatment/Mental-Health-Medications/Bupropion-(Wellbutrin)

Warnings (i.e. contact your doctor if you experience):

Patients with major depressive disorder, both adult and pediatric, may experience worsening of their depression and/or the emergence of suicidal ideation and behavior (suicidality) or unusual changes in behavior, whether or not they are taking antidepressant medications. This risk may persist until significant remission occurs.

Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; however, it did show an increase in participants younger than the age of 24. Among adults age 65 and older, there was a reduction in suicidality risk with antidepressants compared to placebo.

Especially in the first few months of treatment, patients, their families, and caregivers should be alert to the emergence of worsening symptoms, unusual changes, anxiety, restlessness, irritability, aggressiveness and insomnia. If these symptoms emerge, they should notify the patient’s healthcare provider.

http://www.nami.org/Learn-More/Treatment/Mental-Health-Medications/Bupropion-(Wellbutrin)

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

http://www.wellbutrinxl.com/

Info on use during pregnancy:

It is imperative for women taking Wellbutrin XL to communicate with their healthcare provider their plans to become pregnant. Thorough consideration of the risks and benefits of various options, with respect to the patient’s health condition is paramount, since both medication and untreated MDD holds potential risks for the fetus and mother.

Wellbutrin XL can pass into breast milk and may harm a nursing baby.

http://www.nami.org/Learn-More/Treatment/Mental-Health- Medications/Bupropion-(Wellbutrin)

What are alternative medications?

Prozac (fluoxetine)

Paxil (paroxetine)

Lexapro (escitalopram)

Zoloft (sertraline)

Effexor (venlafaxine)

Remeron (mirtazapine)

Drug interactions:

Drinking alcohol or using illegal drugs while taking Wellbutrin XL should be avoided. They may decrease the benefits and increase adverse effects (e.g.,sedation) of the medication.

Bupropion should not be taken with or within two weeks of taking monoamine oxidase inhibitors (MAOIs). These include: phenelzine, tranylcypromine, isocarboxazid, rasagiline, selegeline.

Risk of seizure increases when combined with:

Other antidepressants or antipsychotics

Theophylline

Tramadol

Steroids

Medications that lower blood sugar (including insulin) and antibiotics 
such as: ciprofloxacin, isoniazid.

Abrupt discontinuation of benzodiazepines (e.g., lorazepam).

Bupropion may increase the levels and effects of:

Certain antidepressants: nortriptyline , imipramine, desipramine, 
paroxetine, fluoxetine, sertraline.

Certain antipsychotics: haloperidol, aripiprazole, thioridazine.

Beta-blockers such as metoprolol and propranolol.

Certain antiarrhythmics: propafenone , flecainide.

http://www.nami.org/Learn-More/Treatment/Mental-Health- 
Medications/Bupropion-(Wellbutrin)

http://www.wellbutrinxl.com/

 Contraindications:

Patients with seizure disorders.

Patients with severe hepatic cirrhosis.

Patients treated with Zyban (bupropion hydrochloride) Sustained-Release Tablets; Wellbutrin (bupropion hydrochloride), the immediate-release formulation; Wellbutrin SR (bupropion hydrochloride), the sustained-release formulation; or any other medications that contain bupropion because the incidence of seizure is dose dependent.

Patients with a current or prior diagnosis of bulimia or anorexia nervosa because of a higher incidence of seizures noted in patients treated for bulimia with the immediate-release formulation of bupropion.

Patients undergoing abrupt discontinuation of alcohol or sedatives (including benzodiazepines).

The concurrent administration of Wellbutrin XL and a monoamine oxidase (MAO) inhibitor is contraindicated. At least two weeks should elapse between discontinuation of an MAO inhibitor and initiation of treatment with Wellbutrin.

Patients who have shown an allergic response to bupropion or the other ingredients that make up Wellbutrin XL.

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

Usage Facts

Usual Dosage:

Depressed mood and lack of interest in activities may need up to 6-8 weeks to fully improve. Improvements in sleep, energy and appetite may occur within the first 1-2 weeks and they can be an important early signal that the medication is working.

http://www.nami.org/Learn-More/Treatment/Mental-Health-Medications/Bupropion-(Wellbutrin)

Determining the right dose can take four weeks or longer.
 The usual daily dosage range is between 150-450 mg.
 The dosage is based on the patient’s medical condition, liver function, and response to treatment.

The total daily dose of Wellbutrin XL should not exceed 450 mg.

http://www.webmd.com/drugs/2/drug-76851/wellbutrin-xl-oral/details#uses

http://www.wellbutrinxl.com/

Overdose:

Symptoms of overdose may include: seizures (most common), severe confusion, hallucinations, rapid heart rate, and loss of consciousness.
 A specific treatment to reverse the effects of bupropion does not exist.
 At doses higher than 450 mg per day, there is a higher risk for seizures and other serious side effects.
 Overdose rarely results in death, but there have been several cases that indicate the possibility.

http://www.webmd.com/drugs/2/drug-76851/wellbutrin-xl-oral/details#overdose

http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=11137

Half-life:

The mean elimination half-life of bupropion after chronic dosing is 21 (±9 standard deviation) hours.

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

Steady state:

Steady-state plasma concentrations of bupropion are reached within about 8 days.

https://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=8985

Has there been recent research on it?

Dhillon, S., Yang, L.P., & Curran, M.P. (2008). Bupropion: A review of 
its use in the management of major depressive disorder. Drugs, 68 (5), 
653–689

http://www.ncbi.nlm.nih.gov/pubmed/18370448

Has there been recent coverage of it in the media?

The news broadcast attached below reviews recent trends in Ontario, Canada where individuals with addictions misused Wellbutrin XL by crushing the tablets, cooking it and injecting it to their body to obtain an intoxicated sensation, which is similar to crack or cocaine but at a fraction of the cost of crack. Wellbutrin XL injections are toxic to the skin and can result in severe skin abscesses, clogged veins and arteries and deadly complications. Public safety risk alert were sent to all physicians and pharmacists in Ontario due to the high availability of the drug, the increasing trend of its misuse and the lack of awareness to this trend among medical providers.

https://www.youtube.com/watch?v=B0dYEx58kGE


The articles below reveal the concerning practices the FDA used to approve drugs, among them include, Wellbutrin XL 300 mg. According to the articles, the
 FDA failed to test the efficacy of Wellbutrin XL 300 mg prior to its approval in 2006. Only after media attention and numerous patient complaints regarding the inefficacy of Wellbutrin XL 300 mg and the side effects, the FDA held their own study on the drug (rather than counting on the drug maker to provide their own study results). In 2012, more than 5 years after first reports of a problem with Wellbutrin XL 300 mg, the FDA announced that their approval of the Wellbutrin XL 300 mg was based on trials of the Wellbutrin XL 150 mg and the assumption that higher dosage would be effective for more severe cases of depression or for those who do not respond to lower dosages. Thus, the FDA admitted that studies were never directly conducted on Wellbutrin XL 300 mg (as well as other drugs). Therefore, the FDA will revise their drugs’ approval processes.

http://www.webmd.com/depression/news/20121005/teva-high-dose-generic-wellbutrin-xl-withdrawn

http://abcnews.go.com/Health/fda-finds-generic-antidepressant-original/story?id=17399399

Author, Hen Caspi

Author, Hen Caspi

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