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Page: Pharmacokinetics
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Bupropion is metabolized in the liver. It has several active metabolites: R,R-hydroxybupropion, S,S-hydroxybupropion, threo-hydrobupropion and erythro-hydrobupropion. These active metabolites are further metabolized to inactive metabolites and eliminated through excretion into the urine. Pharmacological data on bupropion and its metabolites combined from several sources are presented in the Table below. In addition, bupropion is known to inhibit weakly ?1 adrenaline receptor (with 14% potency of its dopamine uptake inhibition) and histamine H1 receptor (with 9% potency of dopamine uptake inhibition).
Thus, the biological activity of bupropion can be attributed to a great degree to its active metabolites, in particular to S,S-hydroxybupropion. GSK is developing this metabolite as a separate drug radafaxine. Significant interspecies differences in metabolism of bupropion exist, with guinea pigs' metabolism of the drug being closest to the human metabolism. Particular caution is needed when extrapolating the results of the experiments on rats to humans since hydroxybupropion, the main metabolite of bupropion in humans, is absent in rats.
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