Back to Browse Journals » Drug, Healthcare and Patient Safety » Volume 2

Preclinical pharmacology, efficacy, and safety of varenicline in smoking cessation and clinical utility in high risk patients

Authors Zheng-Xiong Xi

Published 14 April 2010 Volume 2010:2 Pages 39—48

DOI https://doi.org/10.2147/DHPS.S6299

Review by Single-blind

Peer reviewer comments 5

Zheng-Xiong Xi

National Institute on Drug Abuse, Intramural Research Program, Baltimore, MD, USA

Abstract: Smoking is still the most prominent cause of preventable premature death in the United States and an increasing cause of morbidity and mortality throughout the world. Although the current treatments such as nicotine replacement therapy (NRT) and bupropion are effective, long-term abstinence rates are low. Mechanism studies suggest that the pleasurable effects of smoking are mediated predominantly by nicotine, which activates the brain reward system by activation of brain α4β2 nicotinic acetylcholine receptors (nAChRs). Varenicline is a novel α4β2 nAChR partial agonist and has been found to be even more effective than NRT or bupropion in attenuating smoking satisfaction and in relieving craving and withdrawal symptoms after abstinence. Thus, varenicline has been recently approved to be a first-line medication for smoking cessation in the United States and European countries. Varenicline is generally well tolerated in healthy adult smokers, with the most commonly reported adverse effects being nausea, insomnia, and headache. However, growing postmarketing data has linked varenicline to an increase in neuropsychiatric symptoms such as seizures, suicidal attempts, depression, and psychosis as well as serious injuries potentially relating to unconsciousness, dizziness, visual disturbances, or movement disorders. Therefore, new safety warnings are issued to certain high risk populations, such as patients with mental illness and operators of commercial vehicles and heavy machinery. In particular, pilots, air traffic controllers, truck and bus drivers have been banned from taking varenicline.

Keywords: nicotine, varenicline, α4β2 nicotinic acetylcholine receptor, nAChRs, partial agonist, smoking cessation

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Readers of this article also read:

Angiotensin receptor blocker telmisartan suppresses renal gluconeogenesis during starvation

Tojo A, Hatakeyama S, Kinugasa S, Nangaku M

Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy 2015, 8:103-113

Published Date: 13 February 2015

Diabetes and sexual dysfunction: current perspectives

Maiorino MI, Bellastella G, Esposito K

Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy 2014, 7:95-105

Published Date: 6 March 2014

The effects of diet- and diet plus exercise-induced weight loss on basal metabolic rate and acylated ghrelin in grade 1 obese subjects

Lopes AL, Fayh AP, Campos LG, Teixeira BC, Carteri RBK, Ribeiro JL, Friedman R, Reischak-Oliveira A

Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy 2013, 6:469-475

Published Date: 29 November 2013

New developments in the treatment of optic neuritis

Thomas M Jenkins, Ahmed T Toosy

Eye and Brain 2010, 2:83-94

Published Date: 18 June 2010