Drugs online research references









J Pharmacol Exp Ther. 1999 Jan;288(1):88-92.
Noncompetitive functional inhibition at diverse, human nicotinic acetylcholine receptor subtypes by bupropion, phencyclidine, and ibogaine.

Fryer JD, Lukas RJ.

Division of Neurobiology, Barrow Neurological Institute, Phoenix, Arizona, USA.

Nicotinic acetylcholine receptors (nAChR) are diverse members of the neurotransmitter-gated ion channel superfamily and play critical roles in chemical signaling throughout the nervous system. The present study establishes the acute functional effects of bupropion, phencyclidine, and ibogaine on two human nAChR subtypes. Function of muscle-type nAChR (alpha1 beta gamma delta) in TE671/RD cells or of ganglionic nAChR (alpha3 beta4 alpha5+/-beta2) in SH-SY5Y neuroblastoma cells was measured with 86Rb+ efflux assays. Functional blockade of human muscle-type and ganglionic nAChR is produced by each of the drugs in the low to intermediate micromolar range. Functional blockade is insurmountable by increasing agonist concentrations in TE671/RD and SH-SY5Y cells for each of these drugs, suggesting noncompetitive inhibition of nAChR function. Based on these findings, we hypothesize that nAChR are targets of diverse substances of abuse and agents used in antiaddiction/smoking cessation strategies. We also hypothesize that nAChR play heretofore underappreciated roles in depression and as targets for clinically useful antidepressants.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9862757&dopt=Abstract

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uab.edu

The objective of this study was to determine whether the aminoketone antidepressant bupropion has beneficial effects in orgasmic dysfunction. DESIGN: Single-blind, sequential treatment order of three weeks each: placebo, bupropion-SR 150 mg/day, bupropion-SR 300 mg/day. SUBJECTS: Nondepressed women (n = 20) and men (n = 10) having nonphysiologic orgasmic delay or inhibition. MAIN OUTCOME MEASURES: Reported difficulty or delay in achieving orgasm, satisfaction with orgasm and erectile function, and subjective impressions of drug effect. RESULTS: In the women, there were significant improvements relative to baseline (p < .01) on both doses of bupropion-SR in all measured aspects of sexual function, and significant improvements relative to placebo (p < .05) in overall sexual satisfaction on both doses and satisfaction with intensity of orgasm on 150 mg/day (300 mg/day, p = .10). In the men, significant improvements over baseline (p < .01) were observed with both doses in overall sexual satisfaction, ability to achieve an erection, and delay in reaching orgasm/ejaculation; significant improvements relative to placebo (p < .05) were observed in overall sexual satisfaction on both doses, ability to achieve erection on 150 mg/day, and delay in orgasm/ejaculation on 150 mg/day. Seventy percent of subjects reported improvement in libido, arousal, or orgasmic function during bupropion administration. CONCLUSIONS: Bupropion-SR may be a useful agent for treating orgasmic delay and inhibition, and possibly disorders of sexual arousal. The results argue against bupropion's apparent prosexual effect in depressed patients being simply a result of its antidepressant activity.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10929571&dopt=Abstract

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J Clin Psychiatry. 2000 Jul;61(7):466-72.
Treatment of men with major depression: a comparison of sequential cohorts treated with either cognitive-behavioral therapy or newer generation antidepressants.

Thase ME, Friedman ES, Fasiczka AL, Berman SR, Frank E, Nofzinger EA, Reynolds CF 3rd.

Western Psychiatric Institute and Clinic, Department of Psychiatry, University of Pittsburgh School of Medicine, PA 15213, USA.

OBJECTIVE: This report compares response to cognitive-behavioral therapy (CBT) and pharmacotherapy in sequential cohorts of men with DSM-III-R major depression. METHOD: Patients were enrolled in consecutive standardized 16-week treatment protocols conducted in the same research clinic. The first group (N = 52) was treated with Beck's model of CBT, whereas the second group (N = 23) received randomized but open-label treatment with either fluoxetine (N = 10) or bupropion (N = 13). Crossover to the alternate medication was permitted after 8 weeks of treatment for antidepressant nonresponders. The patient groups were well matched prior to treatment. Outcomes included remission and nonresponse rates, as well as both independent clinical evaluations and self-reported measures of depressive symptoms. RESULTS: Despite limited statistical power to detect differences between treatments, depressed men treated with pharmacotherapy had significantly greater improvements on 4 of 6 continuous dependent measures and a significantly lower rate of nonresponse (i.e., 13% vs. 46%). The difference favoring pharmacotherapy was late-emerging and partially explained by crossing over nonresponders to the alternate medication. The advantage of pharmacotherapy over CBT also tended to be larger among the subgroup of patients with chronic depression. CONCLUSION: Results of prior research comparing pharmacotherapy and CBT may have been influenced by the composition of study groups, particularly the gender composition, the choice of antidepressant comparators, or an interaction of these factors. Prospective studies utilizing flexible dosing of modern antidepressants and, if necessary, sequential trials of dissimilar medications are needed to confirm these findings.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10937603&dopt=Abstract

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