期刊
XENOBIOTICA
卷 49, 期 11, 页码 1332-1337出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/00498254.2018.1557760
关键词
Cytisine; plant alkaloid; plasma concentration; pharmacokinetics; dose escalation; safety; smoking cessation therapy
资金
- Auckland Medical Research Foundation (AMRF), New Zealand [1 1 15 011]
1. Cytisine, a partial agonist for the alpha(4)beta(2)-nAChR, is used as a smoking cessation medication. Cytisine's current dosing is complex and involves taking 1.5 mg several times a day. The aim of this study was to explore the effect of dose on the pharmacokinetics and safety of cytisine after a single dose in healthy adult smokers. 2. Participants were assigned to one of three groups (n = 6 in each group) to receive a single oral dose of 1.5, 3 or 4.5 mg of cytisine. Blood samples were collected up to 24 h post dose. Pulse, blood pressure and respiratory rate were measured. Adverse effects were recorded. 3. Cytisine reached peak plasma concentration 1-2 h post dose in all participants irrespective of dose, with no dose-dependent changes in the elimination phase. Mean (SD) cytisine exposure (AUC(0-24h)) were 81.9 (15.8), 181.9 (40.8) and 254.5 (48.1) ng.h/mL following 1.5, 3 and 4.5 mg, respectively. 4. Cytisine appears to have predictable pharmacokinetics following a single dose of up to 4.5 mg and may be safe given as a single 4.5 mg dose, which is threefold greater than the recommended dose taken at one time. This study is registered in (ID:NCT02585024).
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