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The N Dealkylated Tolterodine

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the N-dealkylated tolterodine. The remainder of population is referred to as the “extensive metabolizers.” Pharmacokinetic studies revealed tolterodine is metabolized at the slower rate in poor metabolizers when compared to extensive metabolizers; these results in higher serum concentrations of the tolterodine and negligible concentrations of 5-HMT.
Excretion:
Following administration of 5 mg oral dose of tolterodine solution to healthy volunteers, in urine 77% of radioactivity was recovered and in feces 17% was recovered in 7 days. As intact tolterodine less than 1% (< 2.5% in poor metabolizers) of the dose was recovered, and 5% to 14% (< 1% in poor metabolizers) was recovered as 5-HMT.
A summary of the mean (± standard deviation) pharmacokinetic parameters, tolterodine extended release and the 5HMT in poor (PM) and extensive (EM) metabolizers is provided. These data was obtained following multiple and single doses of tolterodine extended release were administered daily to the 17 healthy male volunteers (4 PM, 13 EM).
2.5 Drug Interactions:(7)
Potent CYP2D6 inhibitors:
Fluoxetine is selective serotonin reuptake inhibitor and potent inhibitor of CYP2D6 activity. It was observed that the fluoxetine significantly inhibits metabolism of the tolterodine immediate release in an extensive metabolizers, resulting in the increase in tolterodine AUC. There was 52% decrease in Cmax and 20% decrease in the AUC of 5-hydroxymethyl tolterodine. The sum of unbound serum concentrations
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