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Marianna Bruno, Marcia Wright, Christine L Baker, Birol Emir, Eric Carda, Michelle Clausen, Catherine Sigler, Aanal Patel
BACKGROUND: Cigarette smoking is the leading preventable cause of death and is responsible for more than 480,000 deaths per year in the United States. Smoking cessation is challenging for many patients. Regardless of available treatment options, most quit attempts are unaided, and it takes multiple attempts before a patient is successful. With the ever-increasing use of smartphones, mobile apps hold promise in supporting cessation efforts. This study evaluates the ease of use and user satisfaction with the Pfizer Meds app to support smoking cessation among patients prescribed varenicline (Chantix)...
April 17, 2018: JMIR MHealth and UHealth
Kandace L Amend, Muhammad Younus, Kenneth R Petronis, Jingping Mo, John D Seeger, Robert Gately, Xiangmei Gu, Cheryl Enger
PURPOSE: To evaluate the Risk Evaluation and Mitigation Strategies (REMS) for varenicline by assessing patients' understanding of the varenicline medication guide (MG) at pre-specified time points: 18 months, 3 years, and 7 years after the REMS approval. METHODS: Self-administered surveys were mailed to people who received varenicline based on a pharmacy dispensing. Survey questions assessed understanding of potential risks outlined in the MG: neuropsychiatric symptoms, skin reactions, allergic reactions, and cardiovascular risks...
February 6, 2018: Pharmacoepidemiology and Drug Safety
Tim Markovic, Benjamin N Rocke, David C Blakemore, Vincent Mascitti, Michael C Willis
Pyridine rings are ubiquitous in drug molecules; however, the pre-eminent reaction used to form carbon-carbon bonds in the pharmaceutical industry, the Suzuki-Miyaura cross-coupling reaction, often fails when applied to these structures. This phenomenon is most pronounced in 2-substituted pyridines, and results from the difficulty in preparing, the poor stability of, and low efficiency in reactions of pyridine-2-boronates. We demonstrate that by replacing these boronates with pyridine-2-sulfinates, a cross-coupling process of unrivalled scope and utility is realized...
June 1, 2017: Chemical Science
Anitha P Govind, Yolanda F Vallejo, Jacob R Stolz, Jing-Zhi Yan, Geoffrey T Swanson, William N Green
To better understand smoking cessation, we examined the actions of varenicline (Chantix) during long-term nicotine exposure. Varenicline reduced nicotine upregulation of α4β2-type nicotinic receptors (α4β2Rs) in live cells and neurons, but not for membrane preparations. Effects on upregulation depended on intracellular pH homeostasis and were not observed if acidic pH in intracellular compartments was neutralized. Varenicline was trapped as a weak base in acidic compartments and slowly released, blocking (125)I-epibatidine binding and desensitizing α4β2Rs...
July 18, 2017: ELife
John A Rosecrans, Richard Young
S(-)-Nicotine is the major pharmacologically active substance in tobacco and can function as an effective discriminative stimulus in both experimental animals and humans. In this model, subjects must detect and communicate the nicotine drug state versus the non-drug state. This review describes the usefulness of the procedure to study nicotine, presents a general overview of the model, and provides some relevant methodological details for the establishment of this drug as a stimulus. Once established, the (-)-nicotine stimulus can be characterized for dose response and time course effects...
April 9, 2017: Current Topics in Behavioral Neurosciences
Sun Hwa Lee, Seong Jong Yun, Seokyong Ryu, Seung Won Choi, Hye Jin Kim, Tae Kyug Kang, Sung Chan Oh, Suk Jin Cho
Varenicline (Champix®, Chantix®) is a partial agonist of the α4β2 nicotinic acetylcholine receptor (nAChR) and a full agonist of the α7 nAChR. It has been used for smoking cessation since 2006. Varenicline has been associated with adverse cardiovascular (CV) events, including myocardial infarction, which may be caused by activation of the α7 nAChR receptor that in turn stimulates parasympathetic output from the brainstem to the heart, release of catecholamines, and has a prothrombotic effect. However, among the adverse CV events, the issue related to the varenicline-induced pulmonary thromboembolism (PTE) has not being addressed...
July 2017: American Journal of Emergency Medicine
Julia N Soulakova, Lisa J Crockett
Introduction: The study estimated the prevalence of unassisted quitting (ie, quitting without pharmacological aids or other interventions) among former smokers and identified the most common smoking cessation methods used by U.S. adult smokers who quit smoking between 2007 and 2011. Among long-term quitters, smoking-related behaviors and factors associated with using pharmacological methods and quitting unassisted were examined. Methods: The analytic sample consisted solely of former smokers, including 3,583 "long-term quitters" (those who quit 1 to 3 years prior to the survey) and 2,205 "recent quitters" (those who quit within a year prior to the survey), who responded to the 2010-2011 Tobacco Use Supplement to the Current Population Survey...
December 13, 2017: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
Tuo-Yen Tseng, Paul Krebs, Antoinette Schoenthaler, Selena Wong, Scott Sherman, Mirelis Gonzalez, Antonio Urbina, Charles M Cleland, Donna Shelley
Smoking represents an important health risk for people living with HIV (PLHIV). Low adherence to smoking cessation pharmacotherapy may limit treatment effectiveness. In this study, 158 participants recruited from three HIV care centers in New York City were randomized to receive 12-weeks of varenicline (Chantix) either alone as standard care (SC) or in combination with text message (TM) support or TM plus cell phone-delivered adherence-focused motivational and behavioral therapy (ABT). Generalized linear mixed-effect models found a significant decline in varenicline adherence from week 1-12 across treatment groups...
July 2017: AIDS and Behavior
Janice C Froehlich, Stephen M Fischer, Julian E Dilley, Emily R Nicholson, Teal N Smith, Nick J Filosa, Logan C Rademacher
BACKGROUND: This study examined whether varenicline (VAR), or naltrexone (NTX), alone or in combination, reduces alcohol drinking in alcohol-preferring (P) rats with a genetic predisposition toward high voluntary alcohol intake. METHODS: Alcohol-experienced P rats that had been drinking alcohol (15% v/v) for 2 h/d for 4 weeks were fed either vehicle (VEH), VAR alone (0.5, 1.0, or 2.0 mg/kg body weight [BW]), NTX alone (10.0, 15.0, or 20.0 mg/kg BW), or VAR + NTX in 1 of 4 dose combinations (0...
September 2016: Alcoholism, Clinical and Experimental Research
Mojdeh Mostafavi, Paul Hardy, L Eugene Arnold
OBJECTIVE: To explore the potential benefits of varenicline (CHANTIX® ), a highly specific partial agonist of neuronal α4β2 nicotinic acetylcholine receptors (nAChR), for autistic symptoms, and present resulting biochemical changes in light of dopamine-related genotype. METHODS: The clinical and biochemical changes exhibited by a 19-year-old severely autistic man following the use of low-dose varenicline in an ABA experiment of nature, and his genotype, were extracted from chart review...
November 2016: Journal of Child and Adolescent Psychopharmacology
Andrew M Busch, Eleanor L Leavens, Theodore L Wagener, Maria L Buckley, Erin M Tooley
PURPOSE: The use of electronic cigarettes (e-cigarettes) has risen dramatically in recent years. However, there are currently no published data on the use of e-cigarettes among cardiac patients. The current study reports on the prevalence, reasons for use, and perceived risks of e-cigarettes among patients with post-acute coronary syndrome (ACS). The relationship between e-cigarette use and post-ACS tobacco smoking cessation is also explored. METHODS: Participants were drawn from a randomized trial of smoking cessation treatments following hospitalization for ACS...
September 2016: Journal of Cardiopulmonary Rehabilitation and Prevention
James S Yeh, Ameet Sarpatwari, Aaron S Kesselheim
Boxed warnings-also known as "black box" warnings-can be a powerful tool in communicating drug risks to physicians and patients. The overall number of boxed warnings has grown in recent years as the US Food and Drug Administration (FDA) has approved more drugs on the basis of limited pre-marketing information and as new safety issues for marketed drugs have been identified. Two recent manufacturers' petitions to remove boxed warnings on the drugs rosiglitazone (Avandia) and varenicline (Chantix) have led to divergent FDA decisions and revealed different considerations involved in boxed warning imposition and removal...
August 2016: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
Steven T Pittenger, Scott T Barrett, Shinnyi Chou, Rick A Bevins
While research has revealed heightened vulnerability to meth addiction in women, preclinical models rarely use female subjects when investigating meth seeking and relapse. The goal of the present study was to examine the effects of varenicline (Chantix(®)), a partial α4β2 and full α7 nicotinic acetylcholine receptor agonist, on meth self-administration and reinstatement in female rats. Sprague-Dawley rats were surgically implanted with an indwelling jugular catheter. Half of the rats were then trained to self-administer meth (0...
March 1, 2016: Behavioural Brain Research
Thomas J Tobin, Mary L Tobin
Smoking cessation remains a positive therapeutic goal and should be encouraged for the millions of individuals who continue to smoke and struggle to quit. While psychiatric nurses should encourage patients to start or continue smoking cessation therapies, they must be aware of the additional safety concerns relating to the use of varenicline (Chantix). Research published subsequent to the last clinical update in this journal (Tobin, 2007 ) has prompted additional warnings from the Food and Drug Administration concerning varenicline for smoking cessation therapy...
2015: Issues in Mental Health Nursing
Kelly E Dunn, Taylor F Marcus, Cynthia Kim, Jennifer R Schroeder, Ryan Vandrey, Annie Umbricht
INTRODUCTION: Varenicline (Chantix) is a first-line treatment for smoking cessation but does not produce cessation in many individuals. It may be possible to improve abstinence by co-administering varenicline with other medications. Zonisamide (Zonegran) has a similar pharmacologic profile to topiramate, which has been shown to reduce smoking, but is better tolerated. This study evaluated whether combined zonisamide and varenicline reduced tobacco withdrawal and increased abstinence among smokers trying to quit, relative to varenicline and placebo...
May 2016: Nicotine & Tobacco Research: Official Journal of the Society for Research on Nicotine and Tobacco
Brittany A Toffey, Marcie Rabin, Roger Kurlan
Varenicline (Chantix[R]) is a nicotinic acetylcholine receptor partial agonist used to aid smoking cessation. Adverse psychiatric and behavioral effects of the drug are recognized and national drug monitoring has included reports of tardive dyskinesia, but no cases have been described in the literature. We now report the first two cases of varenicline-related withdrawal emergent dyskinesias.
2015: Open Neurology Journal
Daniel E Falk, I-Jen P Castle, Megan Ryan, Joanne Fertig, Raye Z Litten
OBJECTIVES: To explore whether varenicline (Chantix) showed more efficacy in treating certain subgroups of patients. In a recent multisite trial, varenicline was shown to be effective in reducing drinking in alcohol-dependent patients, both smokers and nonsmokers. Given the heterogeneity among alcohol-dependent patients, secondary analyses were conducted to determine whether certain subgroups responded more favorably than others to treatment with varenicline. METHODS: Data were drawn from a phase 2 randomized, double-blind, placebo-controlled multisite 13-week trial of varenicline in alcohol-dependent patients (Litten et al...
July 2015: Journal of Addiction Medicine
Karin A Kasza, K Michael Cummings, Matthew J Carpenter, Monica E Cornelius, Andrew J Hyland, Geoffrey T Fong
AIMS: To evaluate trends in use of stop-smoking medications (SSMs) before and after varenicline (Chantix™) was introduced to the market-place in the United States, and to determine whether varenicline reached segments of the population unlikely to use other SSMs. DESIGN: Cohort survey. SETTING: United States. PARTICIPANTS: A nationally representative sample of adult smokers in the United States interviewed as part of the International Tobacco Control Four Country Survey between 2004 and 2011...
February 2015: Addiction
Nicole L Yohn, Jill R Turner, Julie A Blendy
Although nicotine mediates its effects through several nicotinic acetylcholine receptor (nAChR) subtypes, it remains to be determined which nAChR subtypes directly mediate heightened anxiety during withdrawal. Relative success in abstinence has been found with the nAChR partial agonist varenicline (Chantix; Pfizer, Groton, CT); however, treatment with this drug fails to alleviate anxiety in individuals during nicotine withdrawal. Therefore, it is hypothesized that success can be found by the repurposing of other nAChR partial agonists for cessation therapies that target anxiety...
May 2014: Journal of Pharmacology and Experimental Therapeutics
Rishi Sharma, Pradeep Sahota, Mahesh M Thakkar
BACKGROUND: Alcohol and nicotine are the most commonly abused drugs. The frequent co-morbidity of alcohol and nicotine addiction has led to the hypothesis that they may act via a common substrate: the nicotinic acetylcholine receptors (nAChRs) especially α4β2 and α7 subtypes, the most prevalent nAChRs in the brain. Compelling evidence suggests that alcohol enhances the function of α4β2 subtype. The FDA approved smoking cessation drug, varenicline ("Chantix"), a partial agonist of α4β2 nAChR subtype, reduces alcohol self-administration and alcohol craving in humans and rodents...
May 2014: Alcoholism, Clinical and Experimental Research
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