Drugs online research references









Chirality. 1993;5(7):495-500.
Synthesis and evaluation of the antidepressant activity of the enantiomers of bupropion.

Musso DL, Mehta NB, Soroko FE, Ferris RM, Hollingsworth EB, Kenney BT.

Division of Organic Chemistry, Burroughs Wellcome Co., Research Triangle Park, North Carolina 27709.

The synthesis of the enantiomers of bupropion, (rac)-2-tert-butylamino-3'-chloropropiophenone 1 (Wellbutrin) is described. The enantiomers were compared with the racemate in both the tetrabenazine-induced sedation model and the inhibition of uptake of biogenic amine assay. No significant differences were found in their potencies to reverse tetrabenazine-induced sedation in mice or in their IC50 values as inhibitors of biogenic amine uptake into nerve endings obtained from mouse brain.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8240925&dopt=Abstract

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Neurobehav Toxicol Teratol. 1985 Mar-Apr;7(2):139-41.
Alcohol interactions with typical and atypical antidepressants.

Tartara A, Formigli L, Crema F, Maurelli M, Perucca E, Marchioni E, Manzo L, Savoldi F.

Selected parameters of central nervous system function have been examined in rabbits and mice given ethyl alcohol (ET) in combination with antidepressant drugs with different pharmacological profiles. A significant prolongation of the ET-induced loss of righting reflex was observed in mice treated with amitriptyline, 3 mg/kg, or trazodone, 8 mg/kg, injected intraperitoneally. The same drugs failed to cause narcosis when given alone to mice at doses up to 40 (amitriptyline) and 100 (trazodone) mg/kg. Rabbits given single 5 mg/kg IV doses of amitriptyline or trazodone exhibited a synchronous EEG pattern with an increase in spectrum total power that became more pronounced after IV injection of a low dose of ET (0.2 g/kg). The increase in the spectrum total power after ET was significantly greater in rabbits given trazodone than in those given amitriptyline. No significant interactive effects were observed in animals receiving combinations of ET with viloxazine, bupropion or fluvoxamine.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3923380&dopt=Abstract

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Albuquerque.VA.GOV

This study was designed to investigate the efficacy of the antidepressant drug bupropion in the treatment of posttraumatic stress disorder (PTSD). Seventeen male combat veterans with chronic PTSD were treated with bupropion in an open-label fashion for 6 weeks. Patients were evaluated with the Clinical Global Impressions Scale for Improvement (CGI-I) at follow-up and rated blindly at baseline and posttreatment with the Clinician Administered PTSD Scale (CAPS), the Hamilton Rating Scale for Depression (HAM-D), and the Hamilton Rating Scale for Anxiety. Three patients discontinued bupropion prematurely because of side effects. Of the remaining 14 patients, 10 were classified as treatment responders by the CGI-I. HAM-D scores decreased significantly from baseline to follow-up. The improvement seen in hyperarousal symptoms was significant but was less significant than the change in depressive symptoms. There was no significant change in Intrusion, Avoidance, or total CAPS scores. It was concluded that bupropion was well tolerated. Patients who had experienced sexual dysfunction with selective serotonin reuptake inhibitors reported no complaints during bupropion treatment. Bupropion decreased depressive symptoms and most patients reported global improvement, although PTSD symptoms remained mostly unchanged. Controlled trials should further clarify the role of bupropion in the treatment of PTSD.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9790155&dopt=Abstract

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