Use of bupropion SR in a pharmacist-managed outpatient smoking-cessation program. Bupropion hydrochloride: the development of a chiral separation using an ovomucoid column. Modification of norepinephrine and serotonin, but not dopamine, neuron firing by sustained bupropion treatment. Rx drugs

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Pharmacotherapy. 2001 May;21(5):636-41.
Use of bupropion SR in a pharmacist-managed outpatient smoking-cessation program.

Roth MT, Westman EC.

Ambulatory Care Clinics, Durham Veterans Affairs Medical Center, North Carolina, USA.

We administered bupropion sustained-release (SR) in a pharmacist-managed outpatient smoking-cessation program. Patients were referred to the program by their primary care physician. All patients completed initial visit questionnaires, received behavioral counseling by a clinical pharmacist, and were provided educational materials on smoking cessation. Seventy-one patients received bupropion SR for treatment of nicotine dependence and were followed for 6 months. Point prevalence abstinence rates were 28.2% and 25.4% at 8 weeks and 6 months, respectively. The trend was toward lower cessation rates in patients with a documented psychiatric diagnosis at 6 months (p=0.064). Bupropion SR was fairly well tolerated, with the most common adverse effects being dry mouth and bad taste. The agent appears to have better success for smoking cessation in patients free of psychiatric comorbidities, but further research is required to support this finding.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11349752&dopt=Abstract

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J Chromatogr A. 2001 Apr 13;913(1-2):275-82.
Bupropion hydrochloride: the development of a chiral separation using an ovomucoid column.

Munro JS, Walker TA.

Atrix Laboratories, Fort Collins, CO 80525-4417, USA.

The separation of bupropion enantiomers on an ovomucoid stationary phase was investigated. The mobile- and stationary-phase parameters that may influence the separation were identified. The parameters that were studied include: type and concentration of organic modifier, mobile phase pH, ionic strength, type of buffer, and column temperature, as well as the effect that the amount of sample injected had on the separation. The optimized chiral separation baseline-resolved the enantiomers in less than 10 min. Calibration curves for a standard were linear over a range of 0.27-53.0 microg/g (ppm) with a correlation coefficient of 0.999 for both enantiomers. A detection limit of 0.13 microg/g and a quantitation limit of 0.27 microg/g were also found. The system precision of the method was 0.2%.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11355823&dopt=Abstract

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Psychopharmacology (Berl). 2001 Apr;155(1):52-7.
Modification of norepinephrine and serotonin, but not dopamine, neuron firing by sustained bupropion treatment.

Dong J, Blier P.

Department of Psychiatry and Neuroscience, McKnight Brain Institute, University of Florida, P.O. Box 100256, Gainesville, FL 32610, USA.

RATIONALE: Bupropion is widely used in the treatment of depression and as an anti-craving medication for the cessation of tobacco smoking. Because it is a very weak inhibitor of norepinephrine (NE) and dopamine (DA) reuptake, its mechanisms of action remain to be elucidated. METHODS: Bupropion was administered subcutaneously via osmotic minipumps over 2 days to determine its effects on the spontaneous firing activity of NE, serotonin (5-HT), and DA neurons in the brain of anaesthetised male Sprague-Dawley rats. This treatment was used in order to obtain levels of the parent compound and its putatively active metabolites that would more adequately reflect the clinical condition than utilizing acute injections. RESULTS: When given by minipump for 2 days, bupropion produced a dose-dependent attenuation of the mean spontaneous firing NE neurons (7.5 mg/kg per day: 15%; 15 mg/kg per day: 61%; 30 mg/kg per day: 80%) which was reversed by the alpha 2-adrenoceptor antagonist idazoxan. At the highest regimen, the mean firing rate of 5-HT neurons was 100% higher than in control rats, but unaffected in NE-lesioned rats. In contrast, DA neurons in the ventral tegmental area displayed a normal firing rate during the latter bupropion treatment. CONCLUSIONS: Sustained bupropion administration decreased the firing rate of NE neurons due to an increased activation of their inhibitory somatodendritic alpha 2-adrenoceptors. This effect of the bupropion treatment would be attributable mainly to an enhancement of NE release and not to reuptake inhibition. This contention is based essentially on the observation that NE reuptake blockers leave unaltered the firing rate of 5-HT neurons, whereas bupropion enhanced it via a NE-dependent mechanism. The present study did not put into evidence any DA activity of bupropion at the level of the cell body of mesolimbic/cortical DA neurons at a regimen exerting profound alterations of the firing activity of NE and 5-HT neurons.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11374336&dopt=Abstract

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