NDA 20-358 |
16a |
Table 1: The Effects
of Bupropion and Three of its Major Metabolites in the
Antitertrabenazine
(Anti-TBZ) and Lethal Effects (LD50) in the Mouse
After Intraperitoneal
Administration
Compound |
Anti-TBZ ED50 mg/kg |
LD50 mg/kg |
Bupropion |
12.5 |
230 |
306U73 |
22 |
95 |
494U73 |
60 |
135 |
17U67 |
60 |
150 |
Amitriptyline |
4 |
75 |
handwritten: (I.P. dosing)
Plasma and urinary metabolites include
biotransformation products formed via reduction of the carbonyl group and/or
hydroxylation of the tert-butyl group of bupropion. Four basic metabolites have been
identified. They are the erythro-
and threo-amino alcohols of bupropion (17U67 and 494U73, respectively),
the erythro-amino diol of bupropion (287U73), and a morpholinol
metabolite (306U73)
TPZZ/93/0012/00 4
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