Drugs online research references
J Pharmacol Exp Ther. 1997 Apr;281(1):508-13.
Differential regulation of dopamine transporter after chronic self-administration of bupropion and nomifensine.
Tella SR, Ladenheim B, Cadet JL.
Department of Pharmacology, Georgetown University School of Medicine, Washington, DC 20007-2195, USA.
Inhibition of dopamine (DA) transporter function is thought to be the principal mechanism underlying cocaine's addictive effects. In contrast to cocaine, several other inhibitors of DA transporter function are not considered to possess abuse liability. One of the neuroadaptive changes to chronic cocaine self-administration is the up-regulation of DA transporters. In the present study, we investigated the reinforcing and neuroadaptive effects of two other DA reuptake inhibitors, namely bupropion and nomifensine. Drug-naive rats readily acquired and subsequently maintained consistent self-administration of 3 and 1 mg/kg/infusion doses of bupropion and nomifensine, respectively, during 2-hr daily sessions over a prolonged period. Similarly, self-administration responding at low doses of bupropion (0.75 and 1.5 mg/kg/infusion) and nomifensine (0.1 and 0.3 mg/kg/infusion) showed some consistency during the initial weeks of testing which gradually declined or tended to decline to levels similar to that of the water control group during the later weeks of testing. Bupropion self-administration dose-dependently up-regulated DA transporters in caudate putamen and nucleus accumbens. In contrast, nomifensine self-administration did not alter DA transporter levels. These data provide evidence for heterogeneity among DA reuptake inhibitors, with some of these drugs being able to up-regulate DA transporters after their self-administration, whereas others lack this neuroadaptive response.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9103538&dopt=Abstract
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Clin Pharmacol Ther. 1997 Apr;61(4):476-87.
Comparative sexual side effects of bupropion, fluoxetine, paroxetine, and sertraline.
Modell JG, Katholi CR, Modell JD, DePalma RL.
Department of Psychiatry, University of Alabama at Birmingham School of Medicine 35294-0018, USA.
OBJECTIVE: To investigate patient reported prosexual side effects of the aminoketone antidepressant bupropion (INN, amfebutamone) and to compare directly the sexual side effects of bupropion and the selective serotonin reuptake inhibitor (SSRI) antidepressants fluoxetine, paroxetine, and sertraline. METHODS: One hundred seven psychiatric outpatient respondents receiving current treatment with one of the above antidepressants anonymously completed questionnaires that allowed reporting of both decreases and increases in sexual function. The main outcome measures were antidepressant-associated changes in libido, arousal, duration of time from arousal to orgasm, intensity of orgasm, and duration of orgasm relative to that experienced before the onset of the patients' psychiatric illnesses. RESULTS: Bupropion-treated patients reported significant increases in libido, level of arousal, intensity of orgasm, and duration of orgasm beyond levels experienced premorbidly. The three SSRIs to an equal degree significantly decreased libido, arousal, duration of orgasm, and intensity of orgasm below levels experienced premorbidly. Overall, 27% of the SSRI-treated patients had no adverse sexual side effects; in contrast, 86% of patients treated with bupropion had no adverse sexual effects, and 77% of bupropion-treated patients reported at least one aspect of heightened sexual functioning. CONCLUSIONS: SSRI-induced adverse sexual effects appear to be the rule rather than the exception and may be substantially underreported unless patients are specifically asked about the effects of these medications on various aspects of sexual function. In contrast, prosexual effects were reported by the majority of patients treated with bupropion. The findings are reviewed in light of the neurochemistry of these agents and the sexual response.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9129565&dopt=Abstract
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Biomed Chromatogr. 1997 May-Jun;11(3):174-9.
Enantiomeric determination of the phenylmorpholinol metabolite of bupropion in human plasma using coupled achiral-chiral liquid chromatography.
Suckow RF, Zhang MF, Cooper TB.
Analytical Psychopharmacology Division, New York State Psychiatric Institute, New York 10032, USA.
A coupled achiral-chiral stationary phase liquid chromatographic technique was developed to separate and quantitate the enantiomers of the phenylmorpholinol metabolite (2) of the antidepressant bupropion (1) in human plasma. At the retention time of 2, a switching valve loaded a portion of the eluting compound onto a protein-bonded chiral stationary phase which resolved 2 into the (+) and (-) stereoisomers using an aqueous mobile phase of potassium phosphate (pH = 6.25) and 5% 2-propanol. All eluting compounds were monitored using UV detection at 214 nm, and no plasma endogenous material or other commonly used psychotropic drugs were found to interfere. Within-day and between-day variation were less than 6% over the expected concentration range, and a limit of quantitation of about 125 ng/mL of 2 was observed. Steady-state plasma samples from 17 patients receiving 1 were found to contain the (-) enantiomer to the extent of about 96% of total 2. The potential clinical implications of these results are not known since all previous pharmacological studies were carried out with the racemic 2.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9192113&dopt=Abstract
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