China Greatvista Chemicals

Bupropion Hydrochloride

Bupropion hydrochloride, an antidepressant of the aminoketone class, is chemically unrelated to tricyclic, tetracyclic, or other known antidepressant agents. Its structure closely resembles that of diethylpropion; it is related to phenylethylamines. It is designated as (±)-1-(3-chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride. The molecular weight is 276.2. The emperical formula is C13H18CINO*HCl. Bupropion 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.

Bupropion is used to treat depression. This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information. Bupropion regulates certain brain chemicals--dopamine and norepinephrine--to elevate mood. It is believed that depression is caused by chemical imbalances in the brain. Controlling these chemical imbalances will help improve depressive symptoms. Bupropion is considered a 'second generation' or 'atypical' anti-depressant because its action is different from the previous generation of psychoactive medications. It was first introduced in the US in 1985 but was quickly withdrawn because of the high incidence of seizures, it was reintroduced in 1989 at a much lower prescription dose. It is generally found stimulating by users and reactions to it vary greatly, with some users experiencing panic attacks and other acute negative reactions to the drug.

The pharmacokinetics of bupropion is best described by a two-compartment model with a distribution phase (how long it takes for the drug to be absorbed into the body and begin working) having a mean half-life of 3-4 hours, and an elimination phase (how long it takes for it to be metabolised and broken down to inert waste products) which has a half-life of 21 hours. Bupropion is extensively metabolized into three active metabolites. At least one of these metabolites is formed by an enzyme called cytochrome P-450 2B6 enzyme. The terminal half-life of the three metabolites ranges from 21 to 37 hours. This means that it may interact with other drugs which also effect this enzyme, such as orphenadrine and cyclophosphamide. The main known side-effects of zyban are dry mouth and dizziness, although there are a few others.

Bupropion selectively inhibits dopamine reuptake, much like cocaine, but, arguably, without the reinforcing effects. It has been used to treat children with ADHD, but there is a high incidence of severe skin rashes when used in this manner. It has also been effective in the treatment of smoking cessation (under the trade name Zyban). Unlike many antidepressants, Bupropion is not used to treat panic attacks, however, patients who have suffered sexual dysfunction as a result of serotonin-specific reuptake inhibitors may show some improvement if switched to bupropion. Its ability to treat cocaine addiction appears promising, though controversial. Bupropion is not an MAOI.