Pharmacokinetics of cytisine, an α4 β2 nicotinic receptor partial agonist, in healthy smokers following a single dose

Drug Test Anal. 2015 Jun;7(6):475-82. doi: 10.1002/dta.1707. Epub 2014 Sep 17.


Cytisine, an α4 β2 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.

Keywords: LC-MS; cytisine; human plasma; pharmacokinetics; α4β2 nicotinic partial agonist.

Publication types

  • Validation Study

MeSH terms

  • Adult
  • Alkaloids / blood
  • Alkaloids / pharmacokinetics*
  • Alkaloids / urine
  • Azocines / blood
  • Azocines / pharmacokinetics
  • Azocines / urine
  • Chromatography, High Pressure Liquid
  • Drug Partial Agonism*
  • Humans
  • Male
  • Nicotinic Antagonists / blood
  • Nicotinic Antagonists / pharmacokinetics
  • Nicotinic Antagonists / urine
  • Quinolizines / blood
  • Quinolizines / pharmacokinetics
  • Quinolizines / urine
  • Receptors, Nicotinic / metabolism*
  • Young Adult


  • Alkaloids
  • Azocines
  • Nicotinic Antagonists
  • Quinolizines
  • Receptors, Nicotinic
  • nicotinic receptor beta2
  • cytisine