Bupropion hydrochloride

Chemical properties

Bupropion hydrochloride powder is white, crystalline, and highly soluble in water. It has a bitter taste and produces the sensation of local anesthesia on the oral mucosa.

Originator

Bupropion hydrochloride,AroKor Holdings Inc.

The Uses of Bupropion hydrochloride

Bupropion hydrochloride is indicated for the treatment of MDD. Bupropion hydrochloride SR (Zyban) is indicated as an aid to smoking cessation treatment.

Drug interactions

Relatively few data are available on interactions of bupropion hydrochloride with other drugs. Increased adverse experiences were reported when the drug was administered concomitantly with l-dopa. MAOIs may increase the acute toxicity of bupropion.
Although bupropion is not metabolized by the CYP2D6 enzyme, the drug and its metabolite, morpholinol, inhibit this enzyme in vitro. Therefore, extreme caution should be exercised when coadministering any drug metabolized by that enzyme, and initial dosage of the drug should be as low as possible.

brand name

Wellbutrin (GlaxoSmithKline); Zyban (GlaxoSmithKline).

Therapeutic Function

Antidepressant; Smoking cessation aid

Biological Activity

Non-selective inhibitor of dopamine and noradrenalin transporters (K i values are 1.4, 2.8 and 45 μ M for NET, DAT and SERT transporters respectively). Also inhibits neuronal nicotinic acetylcholine receptors. Displays antidepressant activity and augments nicotine self-administration at low doses in vivo .

Side Effects

Bupropion hydrochloride can cause serious side effects. The most common side effects of Bupropion hydrochloride include:
headache
dizziness
dry mouth
sore throat
nausea
constipation
trouble sleeping

Mode of action

The exact mechanism of the antidepressant action of bupropion is not known, but is presumed to be related to noradrenergic and/or dopaminergic mechanisms. Bupropion is a relatively weak inhibitor of the neuronal reuptake of norepinephrine and dopamine, and does not inhibit the reuptake of serotonin. Bupropion does not inhibit monoamine oxidase.