Bupropion

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Belgium: Wellbutrin, Zyban; Czech Republic: Elontril, Wellbutrin, Zyban; Denmark: Wellbutrin, Zyban; Estonia: Elontril, Zyban; Finland: Zyban; France: Zyban; Germany: Elontril, Zyban; Greece: Wellbutrin, Zyban; Hungary: Elontril, Wellbutrin; Ireland: Zyban; Italy: Elontril, Wellbutrin, Zyban; Lithuania: Elontril, Wellbutrin; Luxembourg: Quomen, Zyban; Netherlands: Bupropion, Elontril, Quomem, Wellbutrin, Zyban; Poland: Zyban; Portugal: Elontril, Wellbutrin, Zyban; Romania: Wellbutrin, Zyban; Slovakia: Elontril, Wellbutrin; Slovenia: Wellbutrin, Zyban; Spain: Bupropión, Elontril, Geronplase, Quomen, Zyntabac; Sweden: Voxra, Zyban; UK: Zyban.

North America

Canada: Bupropion, Wellbutrin, Zyban; USA: Aplezin, Bupropion, Wellbutrin, Zyban.

Latin America

Argentina: Lung, Odranal, Wellbutrin; Brazil: Bupropiona, Wellbutrin, Zetron-Libbs, Zyban; Mexico: Butrew, Wellbutrin.

Drug combinations

Chemistry

Bupropion Hydrochloride: C~13~H~18~ClNO HCl. Mw: 276.20. (1) 1-Propanone, 1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-, hydrochloride, (±)-; (2)(±)-2-(tert-Butylamino)-3′-chloropropiophenone hydrochloride. CAS-34911-55-2 (amfebutamone)(1974).

Pharmacologic Category

Antidepressants, Miscellaneous; Dopamine-Reuptake Inhibitor. (ATC-Code: N06AX12).

Mechanism of action

Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine.

Therapeutic use

Major depressive disorder (including seasonal episodes). Refractory depression. Adjunct in the cessation of smoking.

Pregnancy and lactiation implications

A significant increase in major teratogenic effects has not been observed following exposure to bupropion during pregnancy; however, the risk of spontaneous abortions may be increased. Bupropion should be used during pregnancy only when the potential benefits justify the potential risks to the fetus. Use not recommended during lactation.

Unlabeled use

Attention-deficit hyperactivity disorder (ADHD). Depression associated with bipolar disorder.

Contraindications

Hypersensitivity to bupropion or any component of the formulation. Seizure disorder. Anorexia/bulimia. Use of MAO inhibitors within 14 days. Abrupt discontinuation of ethanol or sedatives (including benzodiazepines). Patients receiving other dosage forms of bupropion.

Warnings and precautions

Antidepressants increase the risk of suicidal thinking and behavior in children, adolescents, and young adults (18-24 years of age) with major depressive disorder and other psychiatric disorders. May worsen psychosis, or precipitate a shift to mania or hypomania in bipolar disorder. May cause CNS stimulation (restlessness, anxiety, insomnia) or anorexia. May cause motor or cognitive impairment. The risk of seizures is dose-dependent and increased in history of seizures, anorexia/bulimia, head trauma, CNS tumor, severe hepatic cirrhosis, abrupt discontinuation of sedative-hypnotics or ethanol, medications which lower seizure threshold (antipsychotics, antidepressants, theophyllines, systemic steroids), stimulants, or hypoglycemic agents. May increase the risks associated with electroconvulsive therapy. Delayed hypersensitivity reactions resembling serum sickness reported. May cause weight loss. Use with caution in cardiovascular disease, history of hypertension, or coronary artery disease. Caution in hepatic/renal impairment. Use with caution in the elderly (risk of accumulation during chronic dosing). Do not discontinue abruptly in patients receiving high doses chronically (withdrawal symptoms may occur). In patients being treated with bupropion for nicotine dependence, consider that depressed mood may be a symptom of nicotine withdrawal. Anaphylactoid reactions reported. Possible arthralgia, myalgia, and fever with rash and other symptoms suggestive of delayed hypersensitivity. Smoking may induce enzymes and increase metabolism of some drugs (cessation of smoking, with or without use of bupropion, may decrease enzyme induction and alter metabolism of some drugs, such as theophylline or warfarin).

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