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Bupropion, sold under the brand names Wellbutrin and Zyban among others, is an atypical antidepressant primarily used to treat major depressive disorder and to support smoking cessation.

Indications

Bupropion 150 mg is indicated in the treatment of depression. Bupropion is also indicated in smoking cessation.

Therapeutic Class

Atypical anti-depressant drugs

Pharmacology

Bupropion is a selective inhibitor of the neuronal re-uptake of catecholamines (noradrenaline and dopamine) with minimal effect on the re-uptake of indolamines (serotonin) and does not inhibit monoamine oxidase.

While the mechanism of action of bupropion, as with other antidepressants is unknown, it is presumed that this action is mediated by noradrenergic and/or dopaminergic mechanisms.

Dosage & Administration

The usual adult target dose for Bupropion 150 mg/day, given as 150 mg, twice daily. Dosing should begin at 150 mg/day given as a single daily dose in the morning.

If the 150 mg initial dose is adequately tolerated, an increase to the 300 mg/day target dose, given as 150 mg twice daily, may be made as early as day 4 of dosing.

Increasing the dosage above 300 mg/day: As with other antidepressants, the full antidepressant effect of Bupropion Hydrochloride may not be evident until 4 weeks of treatment or longer.

An increase in dosage to the maximum of 400 mg/day, given as 200 mg twice daily, may be considered for patients in whom no clinical improvement is noted after several weeks of treatment at 300 mg/day.

Maintenance: The lowest dose that maintains remission is recommended. Although it is not known how long the patient should remain on Bupropion Hydrochloride,

it is generally recognized that acute episodes of depression require several months or longer of antidepressant drug treatment.

Interaction

Bupropion should not be given concurrently with or within 14 days of stopping an MAOI. The use of alcohol should be minimized or avoided completely because it may alter the seizure threshold.

Similarly, other drugs that lower the seizure threshold, such as other antidepressants, antimalarials, antipsychotics, sedating antihistamines, Quinolones, Tramadol, Theophylline.

Interaction may occur between Bupropion and Orphenadrine, Cyclophosphamide, and Ifosfamide. Caution should be exercised when it is given with drugs such as some antidepressants, antipsychotics, β blockers, and type 1C antiarrhythmics.

Contraindications

It is contraindicated in patients with a seizure disorder. Bupropion 150 mg is contraindicated in patients treated with other medications that contain Bupropion because the incidence of seizure is dose dependent.

The drug is also contraindicated in patients with a current or prior diagnosis of bulimia or anorexia nervosa because of a higher incidence of seizures noted in such patients treated for bulimia with Bupropion 150 mg.

Side Effects

Agitation, anxiety, and insomnia often occur during the initial stages of Bupropion therapy. Other relatively common side effects reported with Bupropion include fever, dry mouth, headache or

migraine, dizziness, nausea and vomiting, constipation, tremor, sweating, and skin rashes. Hypersensitivity reactions, ranging from pruritus and urticaria, less commonly, angio-edema, dyspnea, and anaphylactoid reactions have been reported.

Pregnancy & Lactation

Pregnancy Category C. There are no adequate and well controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed.

Lactation: Bupropion and its metabolites are secreted in human milk. Because Bupropion is excreted in human milk, a decision should be made whether to discontinue breast feeding or to discontinue the drug.

Precautions & Warnings

It should be used with extreme caution, in patients with history of seizure disorders or in patients with other predisposing factors such as severe hepatic cirrhosis or a CNS tumor, and in those undergoing abrupt withdrawal from alcohol or Benzodiazepines.

Bupropion should be used with caution in patients with bipolar depression or psychoses and in patients with a recent history of myocardial infarction or unstable heart disease and in hepatic or renal impairment.

Use in Special Populations

Child and adolescent: Not recommended for child and adolescent under 18 years of age

Overdose Effects

Symptoms: In addition to those events reported under Adverse Reactions, overdose has resulted in symptoms including drowsiness, loss of consciousness and electrocardiogram (ECG) changes eg, conduction disturbances or (including QRS prolongation) arrhythmias; cases of fatal outcome have been reported.

Treatment: In the event of overdose, hospitalization is advised. ECG and vital signs should be monitored. Ensure an adequate airway, oxygenation and ventilation. The use of activated charcoal is recommended.