Pharmacokinetics of cytisine, an α<sub>4</sub>β<sub>2</sub> nicotinic receptor partial agonist, in healthy smokers following a single dose

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  • Soo Hee Jeong
    University of Auckland Pharmacology & Clinical Pharmacology Auckland New Zealand
  • David Newcombe
    University of Auckland School of Population Health Auckland New Zealand
  • Janie Sheridan
    University of Auckland School of Pharmacy Auckland New Zealand
  • Malcolm Tingle
    University of Auckland Pharmacology & Clinical Pharmacology Auckland New Zealand

Abstract

<jats:p>Cytisine, an α<jats:sub>4</jats:sub>β<jats:sub>2</jats:sub> nicotinic receptor partial agonist, is a plant alkaloid that is commercially extracted for use as a smoking cessation medication. Despite its long history of use, there is very little understanding of the pharmacokinetics of cytisine. To date, no previous studies have reported cytisine concentrations in humans following its use as a smoking cessation agent. A high performance liquid chromatography‐ultraviolet (HPLC‐UV) method was developed and validated for analysis of Tabex® and nicotine‐free oral strips, two commercial products containing cytisine. A sensitive liquid chromatography‐mass spectrometry (LC‐MS) method was developed and validated for the quantification of cytisine in human plasma and for the detection of cytisine in urine. Single‐dose pharmacokinetics of cytisine was studied in healthy smokers. Subjects received a single 3 mg oral dose administration of cytisine. Cytisine was detected in all plasma samples collected after administration, including 15 min post‐dose and at 24 h. Cytisine was renally excreted and detected as an unchanged drug. No metabolites were detected in plasma or urine collected in the study. No adverse reactions were reported. Copyright © 2014 John Wiley & Sons, Ltd.</jats:p>

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