Bupropion hydrochloride - CAS 31677-93-7
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Not Intended for Therapeutic Use. For research use only.
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Amfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4μM for the reuptake of dopamine and norepinephrine, respectively
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Bupropion hydrochloride
1.Single-dose pharmacokinetics of bupropion hydrobromide and metabolites in healthy adolescent and adult subjects.
Oh DA1, Crean CS1. Clin Pharmacol Drug Dev. 2015 Sep;4(5):346-53. doi: 10.1002/cpdd.195. Epub 2015 Jul 20.
Data from 2 pediatric single-dose studies, conducted at the same center, were combined to evaluate exposure levels of bupropion and metabolites in adolescents 12-17 years old, compared with adults > 18 years. Pharmacokinetic analyses of bupropion and its metabolites were performed using normalization and pharmacological/convulsive weighting methods on exposure. When compared with adults (>18 years), subjects 12-14 years had an increase in weight-normalized exposure to bupropion (ie, Cmax , 78%; AUC0-t , 83%; and AUCinf , 85%). Variability in this younger age group was also higher, with observations of a 3- to 4-fold increase in exposure. When the changes in metabolites were accounted within pharmacological and convulsive-weighted exposures, the relative ratio of 12-14 years to adults in body weight-normalized Cmax was 127% and 110%, respectively. Subjects 15-17 years did not exhibit a difference in exposure compared with adults. The influence of age on bupropion pharmacokinetics demonstrates that, in general, healthy adolescent subjects cannot be considered smaller healthy adult subjects; the increase in exposure is inversely related to age and appears to be solely associated with bupropion, not with its metabolites.
2.HPLC enantioseparation of racemic Bupropion, Baclofen and Etodolac: Modification of conventional ligand exchange approach by 'pre-column formation of chiral ligand exchange complexes'.
Singh M1, Bhushan R1. Biomed Chromatogr. 2016 Apr 23. doi: 10.1002/bmc.3746. [Epub ahead of print]
Separation of racemic mixture of (RS)-Bupropion, (RS)-Baclofen and (RS)-Etodolac, commonly marketed racemic drugs, has been achieved by modifying the conventional ligand exchange approach. The Cu(II) complexes were first prepared with a few L-amino acids, namely, L-proline, L-histidine, L-phenylalanine, and L-tryptophan and to these was introduced mixture of enantiomer pair of (RS)-bupropion, or (RS)-baclofen or (RS)-etodolac. As a result, formation of a pair of diastereomeric complexes occurred by 'chiral ligand exchange' via the competition between the chelating L-amino acid and each of the two enantiomers from a given pair. The diastereomeric mixture formed in the pre-column process was loaded onto HPLC column. Thus, both the phases during chromatographic separation process were achiral (i.e., neither the stationary phase had any chiral structural feature of its own nor the mobile phase had any chiral additive). Separation of diastereomers was successful using C18 column and a binary mixture of MeCN and TEAP buffer of pH 4.
3.Bupropion: a systematic review and meta-analysis of effectiveness as an antidepressant.
Patel K1, Allen S1, Haque MN1, Angelescu I1, Baumeister D2, Tracy DK3. Ther Adv Psychopharmacol. 2016 Apr;6(2):99-144. doi: 10.1177/2045125316629071. Epub 2016 Feb 18.
Bupropion has been used as an antidepressant for over 20 years, though its licence for such use varies and it is typically a third- or fourth-line agent. It has a unique pharmacology, inhibiting the reuptake of noradrenaline and dopamine, potentially providing pharmacological augmentation to more common antidepressants such as selective serotonergic reuptake inhibitors (SSRIs). This systematic review and meta-analysis identified 51 studies, dividing into four categories: bupropion as a sole antidepressant, bupropion coprescribed with another antidepressant, bupropion in 'other' populations (e.g. bipolar depression, elderly populations) and primary evaluation of side effects. Methodologically more robust trials support the superiority of bupropion over placebo, and most head-to-head antidepressant trials showed an equivalent effectiveness, though some of these are hindered by a lack of a placebo arm. Most work on the coprescribing of bupropion with another antidepressant supports an additional effect, though many are open-label trials.
4.Neuropsychiatric safety and efficacy of varenicline, bupropion, and nicotine patch in smokers with and without psychiatric disorders (EAGLES): a double-blind, randomised, placebo-controlled clinical trial.
Anthenelli RM1, Benowitz NL2, West R3, St Aubin L4, McRae T4, Lawrence D4, Ascher J5, Russ C4, Krishen A6, Evins AE7. Lancet. 2016 Apr 22. pii: S0140-6736(16)30272-0. doi: 10.1016/S0140-6736(16)30272-0. [Epub ahead of print]
BACKGROUND: Substantial concerns have been raised about the neuropsychiatric safety of the smoking cessation medications varenicline and bupropion. Their efficacy relative to nicotine patch largely relies on indirect comparisons, and there is limited information on safety and efficacy in smokers with psychiatric disorders. We compared the relative neuropsychiatric safety risk and efficacy of varenicline and bupropion with nicotine patch and placebo in smokers with and without psychiatric disorders.
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CAS 31677-93-7 Bupropion hydrochloride

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