Methods and compositions for treating depression and other disorders using optically pure (-)-bupropion

Abstract

Methods and compositions are disclosed utilizing the optically pure (-)-isomer of bupropion, which is a potent drug for treating depression, Parkinson's disease, obesity, weight gain and other disorders.

Description

1. FIELD OF THE INVENTION[0001] This invention relates to methods of treatment and pharmaceutical compositions employing the compound (-)-bupropion.2. BACKGROUND OF THE INVENTION2.1. STERIC RELATIONSHIPS AND DRUG ACTION[0002] Many organic compounds exist in optically active forms, i.e., they have the ability to rotate the plane of plane-polarized light. In describing an optically active compound, the prefixes D and L or R and S are used to denote the absolute configuration of the molecule about its chiral center(s). The prefixes (+) and (-) or d and l are employed to designate the sign of rotation of plane-polarized light by the compound, with (-) or l meaning that the compound is. levorotatory. A compound prefixed with (+) or d is dextrorotatory. For a given chemical structure, these compounds, called stereoisomers, are identical except that they are mirror images of one another. A specific stereoisomer may also be referred to as an enantiomer, and a mixture of such isomers is ofte...

AI Technical Summary

Benefits of technology

The optically pure (-)-isomer of bupropion provides effective antidepressant activity and weight management with a clearer dose-response and reduced adverse effects, improving the therapeutic index compared to the racemic mixture.

Problems solved by technology

Furthermore, optical purity is important since certain isomers may actually be deleterious rather than simply inert.

Psychosis may have, as a secondary symptom, a change in mood, and it is this overlap with depression that causes much confusion in diagnosis.

The disease produces a slowly increasing disability in purposeful movement.

Treatment has included psychostimulants, which while effective are controversial, and may cause troubling side effects such as dysphoria, headache and growth retardation.

Other drugs, including the tricyclic antidepressants, appear to improve attention, but may be less effective than the psychostimulants.

Treatment with bupropion is consistently associated with a lack of weight gain.

The causes of excess body weight and / or obesity are complex; however, a common denominator in the overweight person's diet is a caloric intake which exceeds that person's body expenditures.

This method may be limited in its effectiveness since many overweight or obese people have developed eating and activity patterns which are counterproductive to achieving weight reduction.

The drawback to this method is that many appetite suppressant drugs produce undesirable adverse effects which limit their usefulness.

Among these disadvantages are adverse effects in addition to those described above.

The most serious adverse effect associated with the racemic mixture of bupropion is the increased incidence of seizures.

In addition, other frequently reported adverse effects associated with the use of racemic bupropion include nausea, vomiting, excitement, agitation, blurred vision, restlessness, postural tremor, and some hallucinations / confusional states with the potential for abuse.

These effects are dose limiting in a number of patients.

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