Bupropion SR (Zyban)
Generic Name: Bupropion hydrochloride
Brand Names: Wellbutrin, Wellbutrin SR
What is Bupropion?
Bupropion hydrochloride is an antidepressant of the aminoketone class with distinctive pharmacologic properties. It blocks the reuptake of norepinephrine and dopamine without significant effect at serotonin receptors. Its structure closely resembles that of the stimulant diethylpropion, and is related to phenylethylamines.
Bupropion Sustained-Release is indicated for the treatment of major depressive disorder and smoking cessation. Sometimes it is prescribed for weight loss and bipolar depression. Also, bupropion is frequently used to augment the efficacy and lessen the side effects of other antidepressants.
Most noteworthy about bupropion is the absence of weight gain, daytime drowsiness, sexual disturbances, and anticholinergic action. Evidence shows that other than the rare incident of seizures, bupropion causes no serious adverse reactions or clinical laboratory changes.
Good candidates for Bupropion (Wellbutrin)
Those who experience cravings, excessive eating, attention deficit hyperactivity disorder (ADHD), low libido, orgasm dysfunction 2, lethargy, or lack of motivation 3 may benefit from bupropion. It is a worthy choice if tobacco cessation or weight loss is a secondary goal. It may help to overcome retarded depression, depression with coexisting cognitive slowing or pseudo-dementia.
When Bupropion (Wellbutrin) is not appropriate
Bupropion is not a prescription of choice for excessively activated and agitated persons, those who use any other bupropion-containing product (ie, coadministration of Zyban for smoking cessation and Wellbutrin for depression).
It is contraindicated for those who have:
Although overshadowed by the SSRIs as first-line treatment for major depression, the efficacy of bupropion in depression is well established and is comparable to that of SSRIs.
Immediate-release: 100 mg two times per day initially; may increase to 100 mg tree times per day after 3 days (maximum 450 mg daily).
Sustained-release: 150 mg once daily initially; may increase to 150 mg two times per day as early as day 4 of therapy (max daily dose, 400 mg; max single dose, 200 mg).
Extended-release: 150 mg once daily in the morning initially; can increase to 300 mg once daily after 4 days; maximum single dose 450 mg once daily.
Dosing conversion between immediate, sustained, and extended release products: Convert using same total daily dose (up to the maximum recommended dose for a given dosage form), but adjust frequency as indicated for sustained (twice daily) or extended (once daily) release products.
Foods: May be taken without regard to meals.
How long until Bupropion works?
Onset of antidepressive effect usually not immediate, but often delayed 2-4 weeks. If it is not working within 6–8 weeks, it may require a dosage increase or it may not work at all.
By inhibiting dopamine reuptake, bupropion ensures anticraving and antiwithdrawal effects thanks to which it helps in a long-term abstinence from smoking.
Initial dose is 150 mg once a day, increase to 150 mg twice a day after at least 3 days (maximum 300 mg per day). Begin 1–2 weeks before smoking is discontinued and take for up to 6 months.
Most common side effects include: agitation (32%); insomnia (31%); dry mouth (28%); headache (26%); weight loss (23%), nausea, vomiting (23%), dizziness (22%); sweating (22%); tremor (21%); sedation (20%); anorexia (18%), tachycardia (11%); abdominal discomfort (9%); and rash (8%).
Pregnancy & Lactation
Pregnancy category C
One study has been conducted in pregnant women. This retrospective, managed-care database study assessed the risk of congenital malformations overall, and cardiovascular malformations specifically, following exposure to bupropion in the first trimester compared to the risk of these malformations following exposure to other antidepressants in the first trimester and bupropion outside of the first trimester. The study showed no greater risk for congenital malformations overall, or cardiovascular malformations specifically, following first trimester bupropion exposure compared to exposure to all other antidepressants in the first trimester, or bupropion outside of the first trimester. The results of this study have not been corroborated.
Last updated: February, 2015