Drugs online research references
Pol J Pharmacol Pharm. 1985 May-Jun;37(3):243-52.
Central effects of repeated treatment with bupropion.
Klimek V, Nowak G, Czyrak A.
The effect of bupropion, a new clinically active antidepressant drug, administered repeatedly to rats and mice, was compared with that of imipramine. The drugs were given orally twice a day for 14 days, bupropion in a dose of 20 mg/kg, imipramine--10 mg/kg. The action of bupropion was studied in the following tests: clonidine-induced aggression in mice, open field in rats, amphetamine-induced hypermotility in rats, clenbuterol-induced hyperthermia in rats kept at high ambient temperature. Moreover, the effect of bupropion on 3H-prazosin binding to membranes from the cerebral cortex was measured. On the basis of the results obtained it may be concluded that in some tests chronically administered bupropion acts like imipramine; as both drugs potentiate the amphetamine-enhanced locomotor activity, attenuate the hyperthermic response to clenbuterol and increase the number of 3H-prazosin binding sites in the cerebral cortex.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3934652&dopt=Abstract
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Ann Neurol. 1985 Nov;18(5):544-51.
Stress-induced neurological impairments in an animal model of parkinsonism.
Snyder AM, Stricker EM, Zigmond MJ.
Adult rats were given the neurotoxin 6-hydroxydopamine (6-HDA) by means of cerebrospinal fluid to produce large dopamine-depleting brain lesions. Although the animals behaved normally in their home cages, they became akinetic after such treatments as glucoprivation, tail shock, and exposure to severe cold. The neurological impairments were related both to the extent of dopamine depletion and to the intensity of the stress. Drugs known to enhance dopaminergic function were found to reverse the stress-induced neurological deficits, while dopaminergic antagonists potentiated the debilitating effects of stress. After focal lesions were produced by injecting 6-hydroxydopamine directly into specific brain regions, stress-induced akinesia was found to correlate best with dopamine depletion in the corpus striatum, especially the lateral portion of that structure. These and other findings suggest that the acute emergence of parkinsonian symptoms during stress may reflect extensive damage to the dopaminergic nigrostriatal pathway that had been concealed in a preclinical phase, owing to compensatory neurochemical changes in the dopaminergic neurons that yet remain intact.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3935041&dopt=Abstract
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Ther Drug Monit. 1985;7(4):447-50.
Stability of bupropion and its major metabolites in human plasma.
Laizure SC, DeVane CL.
Bupropion (BUP) is a new, monocyclic, second-generation antidepressant with efficacy comparable with that of the tricyclics but possessing a more favorable side-effect profile. Therapeutic drug monitoring services are expected to be widely available following the marketing of BUP, yet relatively little has been published on its clinical pharmacokinetics. The purpose of this study was to assess the drug's plasma stability and to determine the best storage conditions for conducting pharmacokinetic studies of BUP and its major metabolites. Human plasma was spiked with known concentrations of BUP and its major basic metabolites, threo-amino alcohol (TB), erythro-amino alcohol (EB), and hydroxy metabolite (HB), and incubated under varying conditions of temperature and pH. BUP showed a log linear degradation that was both temperature and pH dependent. BUP half-life in pH 7.4 plasma stored at 22 and 37 degrees C was 54.2 and 11.4 h, respectively. Incubation at 37 degrees C, pH 2.5 to 10, for 48 h had minimal effect on metabolite concentrations. These results indicate that drug degradation must be considered in studies involving the incubation of plasma for protein binding determinations and the collection and storage of plasma samples for drug concentration analysis during therapeutic drug monitoring.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3936237&dopt=Abstract
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