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

Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Madhu SangaAravind Mittur

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 [(14)C]-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 [(14)C]-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 [(14)C]-nefopam was minimal.

References

Jan 1, 1992·Annual Review of Pharmacology and Toxicology·G J Mulder
Jun 12, 1987·European Journal of Pharmacology·S HunskaarK Hole
Jun 1, 1974·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·A G BoltP Wilson
Apr 1, 1984·British Journal of Clinical Pharmacology·J B Houston, G Taylor
Jun 6, 1981·South African Medical Journal = Suid-Afrikaanse Tydskrif Vir Geneeskunde
Jul 2, 1998·Journal of Pharmaceutical Sciences·C E HopG Kwei
Dec 24, 2004·Anesthesia and Analgesia·Barbara KapferMarcel Chauvin
Jun 6, 2006·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Philippe GirardJean-Marie Gillardin
Sep 18, 2008·British Journal of Anaesthesia·M S EvansM R Tramèr
Jul 21, 2010·Expert Opinion on Pharmacotherapy·Yee-Chi Lee, Phoon-Ping Chen
Oct 26, 2010·Anesthesia and Analgesia·Olivier MimozRené H Levy
Jun 10, 2010·ACS Medicinal Chemistry Letters·Patrik RydbergLars Olsen

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Drug Metabolism and Disposition : the Biological Fate of Chemicals
Felix WaldmeierSujata Vaidyanathan
Drug Metabolism and Disposition : the Biological Fate of Chemicals
S K PaulsonE G Burton
Drug Metabolism and Disposition : the Biological Fate of Chemicals
Kelem KassahunS Aubrey Stoch
© 2022 Meta ULC. All rights reserved