Pharmacokinetic Studies with 3H-Cytisine

Pharmacokinetics of cytisine, an α4β2 nicotinic receptor partial agonist, in healthy smokers following a single dose

“…There is currently limited data on the pharmacokinetics of cytisine in animal studies and none to date reported for humans. The animal data that exist describe pharmacokinetic parameters in rabbits and mice but the doses studied are not clinically relevant in humans …”

“…No metabolites were detected in any plasma or urine sample obtained in this study. The metabolism of cytisine has not been studied extensively, but preclinical studies have found that cytisine undergoes minimal metabolism with 90–95% of the administered dose excreted unchanged in the urine and animal studies in rabbits did not report the presence of metabolic products . Consistent with animal studies, this study found that unchanged cytisine is renally eliminated in humans.…”

Mescal Bean [Sophora secundiflora(Ortega) Lagasca ex DC.]

“…9 The plasma elimination half -life of cytisine in these animal studies is about 3 -4 hours. Based on animal studies, the peak concentration of cytisine occurs about 2 hours after ingestion with bioavailability being about 40%.…”

Cytisine—from Ethomedical use to the Development as a Natural Alternative for Smoking Cessation

“…The pharmacokinetics of cytisine was studied after intravenous or oral administration of tritiated cytisine in dose 2 mg/kg in mice (30). The maximum plasma concentrations are reached 2 hours after oral administration.…”

“…The distribution of [ 3 H] cytisine in different organs and tissues was examined in pharmacokinetic study in rat (30). After oral or intravenous administration, the highest concentrations of cytisine were determined in bile, liver, adrenals and kidney.…”