Drugs online research references
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.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6406467&dopt=Abstract
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Pharmacol Biochem Behav. 1982 Jun;16(6):973-7.
Animal model of depression: tests of three structurally and pharmacologically novel antidepressant compounds.
Katz RJ, Sibel M.
Previous studies have identified behavioral and neuroendocrine abnormalities in chronically stressed rats which resemble some of the more prominent features of clinical depression. These abnormalities have proved responsive to pharmacotherapy by standard antidepressant drugs and related somatic treatments. Several structurally and pharmacologically atypical compounds, resembling neither standard agents, nor each other, have recently been identified as clinically effective antidepressants. There drugs do not show typical preclinical response profiles in other drug screening tests and, therefore, represent critical instances for evaluating the selectivity of the chronic stress model. Three drugs were tested, these being iprindole, bupropion, and mianserine; a tricyclic indole, propriophenone, and tetracyclic compound respectively. Four circulating measures, which previously proved most useful in discriminating antidepressant potential, and a measure of circulating corticosterone were obtained for subjects examined factorially in a 2x2x2 experimental design (chronic stress vs none, acute stress vs none, and drugs vs control). All compounds proved capable of reversing chronic stress induced behavioral deficits, and all but one compound reversed the attendant basal hypersecretion of corticosterone. These findings argue that the chronic stress model provides an accurate and selective assessment of the therapeutic potential of both standard and structurally novel compounds.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6810386&dopt=Abstract
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Clin Pharmacol Ther. 1985 Nov;38(5):586-9.
Pharmacokinetics of bupropion and its major basic metabolites in normal subjects after a single dose.
Laizure SC, DeVane CL, Stewart JT, Dommisse CS, Lai AA.
The pharmacokinetics of bupropion (BUP) and its three major basic metabolites (the erythroamino alcohol [EB], the threoamino alcohol [TB], and the hydroxy [HB] metabolites) were characterized after a single, oral, 200 mg dose of BUP in six healthy men. Twenty-one sequential plasma samples for analysis by HPLC were drawn from each subject over the 56-hour period after dosing. Pharmacokinetic analyses were by noncompartmental methods. The mean elimination t1/2 values of BUP, TB, EB, and HB were 9.8, 19.8, 26.8, and 22.2 hours, respectively. The mean plasma AUCs of TB and HB were 2.4 and 10.3 times greater, respectively, than that for BUP. Because of the substantial presence of these metabolites in systemic circulation, further studies are recommended to understand further their roles in the clinical profile of this new antidepressant.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3931955&dopt=Abstract
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