J Clin Psychiatry. 1983 May;44(5 Pt 2):143-7.
Private practice evaluation of the safety and efficacy of bupropion in depressed outpatients.

Kirksey DF, Harto-Truax N.

A multicenter uncontrolled 4-week trial of bupropion in depressed outpatients was conducted in the private practices of 25 internists, 9 family practitioners, and 3 psychiatrists. Minimum exclusion criteria were used with respect to concurrent medical ailments, age, and concomitant medications. Of the 380 patients admitted to the study, 325 were included in efficacy analyses, and 359 provided data for safety analyses. The average patient was a 51-year-old married white woman with a high school education and a skilled job. Bupropion administered in doses of 150-450 mg/day was highly effective in reducing depressive symptomatology as evaluated by the Hamilton Depression and Clinical Global Impressions scales, and the Zung Self-Rating Scale. No clinically significant bupropion-related changes in blood pressure, pulse rates, respiration rate, body temperature, or laboratory parameters were recorded; only 41 patients were discontinued due to intolerance to adverse experiences. There was a notable absence of daytime sedation, and of anticholinergic and cardiovascular side effects.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6406446&dopt=Abstract Bupropion Wellbutrin




J Clin Psychiatry. 1983 May;44(5 Pt 2):157-62.
Long-term preventive care in depression: the use of bupropion in patients intolerant of other antidepressants.

Gardner EA.

The safety and efficacy of bupropion in the preventive care of depression was studied in a long-term open trial. Forty patients from an active general psychiatric practice which emphasizes the treatment of affective disorders have been followed for an average of 336 days (range, 44-791) and seen at least monthly for evaluation with the Hamilton Depression Scale, Zung Self-Rating Scales for Depression and Anxiety, Clinical Global Impression Scale and an adverse reaction report form. One third of the patients had received a diagnosis of bipolar disorder and 50% a diagnosis of recurrent major depressive disorder by DSM-III criteria; all patients were intolerant of tricyclic and other antidepressants. Although several patients were not severely depressed when placed on bupropion, there was a significant improvement on the Zung Self-Rating Scales. There was a striking reduction in the frequency and intensity of adverse reactions, particularly anticholinergic effects, appetite and weight gain, and sexual dysfunction, compared to tricyclics. Also, there were no cardiovascular changes and no physical, ECG, EEG, or laboratory evidence of toxicity. Bupropion represents a significant advance in the treatment of depression, particularly for patients who require long-term preventive care and in whom adverse reactions, which might be tolerated in acute treatment, may lead to noncompliance.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6406449&dopt=Abstract Bupropion Wellbutrin




J Clin Psychiatry. 1983 May;44(5 Pt 2):56-9.
The chemistry of bupropion.

Mehta NB.

The chemical structure and synthesis of bupropion are described and compared with typical polycyclic antidepressants to point up the novelty and simplicity of this drug. The features of bupropion's substructure are discussed to help in understanding the observed pharmacological differences among bupropion, tricyclic antidepressants, and psychostimulants.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6406464&dopt=Abstract Bupropion Wellbutrin




J Clin Psychiatry. 1983 May;44(5 Pt 2):67-73.
The pharmacologic basis for therapeutic interest in bupropion.

Soroko FE, Maxwell RA.

Bupropion, a compound chemically dissimilar to tricyclic antidepressants and monoamine oxidase inhibitors, was found to be active in animal models that are predictive of antidepressant activity in man. Bupropion was also found to be pharmacologically and biochemically distinct from tricyclics and monoamine oxidase inhibitors. Furthermore, it lacked anticholinergic activity, was not sympathomimetic, and was at least 10-fold weaker as a cardiac depressant than the tricyclic antidepressants. It was concluded that bupropion would be better tolerated and safer in man than standard therapies and that its pharmacologic and biochemical profile held out the possibility of novel antidepressant actions.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6406467&dopt=Abstract Bupropion Wellbutrin




J Clin Psychiatry. 1983 May;44(5 Pt 2):79-81.
Metabolism and kinetics of bupropion.

Schroeder DH.

Studies of bupropion in rats, dogs, and normal volunteers showed that bupropion was rapidly and completely absorbed, widely distributed in tissues, and metabolized extensively prior to its excretion. Metabolism in rats and dogs appeared to be predominantly by side chain oxidative cleavage, while reduction of the intact parent aminoketone to an aminoalcohol was an additional major pathway in man. Most of the metabolites were excreted in urine. Bupropion, but not its metabolites, was concentrated in many tissues, with a brain to plasma ratio of about 25:1. Plasma protein binding of bupropion (75%-80%) did not seem to limit its tissue distribution. Bupropion was found to be a weak to moderate inducer of drug metabolism.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6406469&dopt=Abstract Bupropion Wellbutrin