Bupropion

Bupropion

Information about Bupropion

Bupropion is an aminoketone antidepressant widely used in the treatment of depression and as an aid for smoking cessation. It was approved for use in the United States in 1985 and is currently prescribed under the brand names Welbutrin and Zyban, as well as in several generic forms.

Pharmacology

The precise mechanism of action of bupropion is not well understood. Unlike many other antidepressants, it has no activity against monoamine oxidase and only weak inhibition of serotonin and norepinephrine reuptake. Bupropion appears to exert its therapeutic effects primarily through noradrenergic or dopaminergic mechanisms.

Indications

Bupropion has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of moderate to severe depression, seasonal affective disorder, and as an aid in smoking cessation. It is available in immediate-release, sustained-release, and extended-release tablet formulations.

Dosage and Administration

For the treatment of depression in adults, the recommended dosage of bupropion ranges from 75 to 300 mg daily, administered either as immediate-release tablets twice daily or as extended-release or sustained-release tablets once daily. For smoking cessation, sustained-release tablets of 150 mg are available under the brand name Zyban, with a recommended dosage of 150 to 300 mg daily.

Side Effects

Common side effects of bupropion include drowsiness, dizziness, agitation, headache, nausea, abdominal pain, and dry mouth. In some cases, bupropion therapy may be associated with transient, usually asymptomatic elevations in serum aminotransferase levels. Rare instances of clinically apparent acute liver injury have also been reported.

Precautions and Contraindications

Patients should consult their healthcare provider before starting bupropion therapy, particularly if they have a history of liver disease, seizure disorders, or other medical conditions that may increase the risk of side effects. Bupropion should be used with caution in patients with a history of substance abuse, as it may have some potential for abuse or dependence.

Brand Names and Availability

Bupropion is available in several generic forms and under the brand names Welbutrin (for depression) and Zyban (for smoking cessation). The drug is available in immediate-release and sustained-release tablets of 75, 100, 150, 200, and 300 mg.

Liver Safety

Although bupropion therapy is generally well-tolerated, it can occasionally be associated with transient, asymptomatic elevations in serum aminotransferase levels. Clinically apparent acute liver injury has been reported in rare cases The following are antidepressant subclasses and drugs

MAO Inhibitors Isocarboxazid, Phenelzine, Tranylcypromine

SNRIs Duloxetine, Levomilnacipran, Venlafaxine

SSRIs Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Vilazodone, Vortioxetine

Tricyclics Amitriptyline, Amoxapine, Clomipramine, Desipramine, Doxepin, Imipramine, Nortriptyline, Protriptyline, Trimipramine

Miscellaneous Bupropion, Flibanserin, Mirtazapine, Nefazodone, Trazodone

• Dailymed label info on Bupropion
• FDA Bupropion