• DOI:10.3109/00498254.2015.1136989
• Corpus ID: 34603935

Pharmacokinetics, metabolism, and excretion of nefopam, a dual reuptake inhibitor in healthy male volunteers

@article{Sanga2016PharmacokineticsMA,
  title={Pharmacokinetics, metabolism, and excretion of nefopam, a dual reuptake inhibitor in healthy male volunteers},
  author={Madhu Sanga and John A. Banach and Aaron R. Ledvina and Nishit B Modi and Aravind Mittur},
  journal={Xenobiotica},
  year={2016},
  volume={46},
  pages={1001 - 1016}
}

• Madhu Sanga, J. Banach, +2 authors A. Mittur
• Published 21 January 2016
• Medicine
• Xenobiotica

Abstract 1. The disposition of nefopam, a serotonin–norepinephrine reuptake inhibitor, was characterized in eight healthy male volunteers following a single oral dose of 75 mg [14C]-nefopam (100 μCi). Blood, urine, and feces were sampled for 168 h post-dose. 2. Mean (± SD) maximum blood and plasma radioactivity concentrations were 359 ± 34.2 and 638 ± 64.7 ngEq free base/g, respectively, at 2 h post-dose. Recovery of radioactive dose was complete (mean 92.6%); a mean of 79.3% and 13.4% of the dose was recovered in urine and feces, respectively. 3. Three main radioactive peaks were observed in plasma (metabolites M2 A-D, M61, and M63). Intact [14C]-nefopam was less than 5% of the total radioactivity in plasma. In urine, the major metabolites were M63, M2 A-D, and M51 which accounted for 22.9%, 9.8%, and 8.1% of the dose, respectively. An unknown entity, M55, was the major metabolite in feces (4.6% of dose). Excretion of unchanged [14C]-nefopam was minimal.