Varenicline: mode of action, efficacy, safety and accumulated experience salient for clinical populations
Open Access
- 14 March 2020
- journal article
- review article
- Published by Taylor & Francis Ltd in Current Medical Research and Opinion
- Vol. 36 (5), 713-730
- https://doi.org/10.1080/03007995.2020.1729708
Abstract
Objective: Varenicline, a selective partial agonist of the α4β2 nicotinic acetylcholine receptor, is a smoking cessation pharmacotherapy that more than doubles the chance of quitting smoking at 6 months compared with placebo. This article reviews salient knowledge of the discovery, pharmacological characteristics, and the efficacy and safety of varenicline in general and in specific populations of smokers and provides recommendations to support use in clinical practice. Methods: Literature searches for varenicline were conducted using PubMed, with date limitations of 2000–2018 inclusive, using search terms covering the discovery, mechanism of action, pharmacokinetics, efficacy and safety in different populations of smokers, alternative quit approaches and combination therapy. Selection of safety and efficacy data was limited to clinical trials, meta-analyses and observational studies. Results: Standard administration of varenicline is efficacious in helping smokers to quit, including smokers with cardiovascular disease and chronic obstructive pulmonary disease. Furthermore, varenicline efficacy may be improved with pre-loading, a gradual quitting approach for smokers unwilling or unable to quit abruptly, and extended treatment in smokers who have recently quit to help maintain abstinence. Initial concerns regarding the association of varenicline with increased risk of neuropsychiatric and cardiovascular adverse events have been disproven after extensive clinical evaluations, and the benefit-risk profile of varenicline is considered favorable. Conclusions: Varenicline is efficacious and safe for all adult smokers with a range of clinical characteristics. Evidence suggests that approaches offering greater flexibility in timing and duration of treatment may further extend treatment efficacy and clinical reach.Keywords
This publication has 103 references indexed in Scilit:
- Is a combination of varenicline and nicotine patch more effective in helping smokers quit than varenicline alone? A randomised controlled trialBMC Medicine, 2013
- Effects of 21 days of varenicline versus placebo on smoking behaviors and urges among non-treatment seeking smokersJournal of Psychopharmacology, 2012
- Results of an initial clinical trial of varenicline for the treatment of cocaine dependenceDrug and Alcohol Dependence, 2012
- The Effects of Extended Pre-Quit Varenicline Treatment on Smoking Behavior and Short-Term Abstinence: A Randomized Clinical TrialClinical Pharmacology & Therapeutics, 2011
- A Randomized Placebo-Controlled Trial of Varenicline for Smoking Cessation Allowing Flexible Quit DatesNicotine & Tobacco Research, 2011
- Risk of serious adverse cardiovascular events associated with varenicline: a systematic review and meta-analysisCMAJ : Canadian Medical Association Journal, 2011
- Varenicline for smoking cessation in people with schizophrenia: a double blind randomized pilot studySchizophrenia Research, 2011
- Nicotine receptor partial agonists for smoking cessationPublished by Wiley ,2011
- A Clinical Practice Guideline for Treating Tobacco Use and Dependence: 2008 Update: A U.S. Public Health Service ReportAmerican Journal of Preventive Medicine, 2008
- Prediction of Creatinine Clearance from Serum CreatinineNephron, 1976