scholarly journals Network meta-analysis: a comparison of effectiveness and safety of partial agonists of nicotinic acetylcholine receptors varenicline and cytisine for smoking cessation

2018 ◽  
Vol 16 (4) ◽  
pp. 19-32
Author(s):  
Elena V. Radchenko ◽  
Olga A. Sykhovskaya ◽  
Timofey L. Galankin ◽  
Aleksei S. Kolbin ◽  
Maria A. Smirnova
Keyword(s):  
Smoking Cessation ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Meta Analysis ◽  
Efficacy And Safety ◽  
Serious Adverse Events ◽  
Nicotinic Acetylcholine ◽  
Partial Agonists ◽  
Safety Parameters ◽  
Comparison Of Effectiveness

Background. Partial agonists of α4b2 nicotinic acetylcholine receptors are the most effective treatment strategy for tobacco smoking cessation. They are able to alleviate withdrawal symptoms and to reduce smoking satisfaction. The aim of this study was to review the efficacy and safety of nicotinic receptor partial agonists varenicline and cytisine, for smoking cessation. Methods. A search for randomized controlled trials was done using the terms (“cytisine”, “tabex”, “varenicline” or 'partial agonists of nicotinic receptors’) in MEDLINE, EMBASE, eLibrary in May 2018. Types of participants, the doses and duration of the treatments, efficacy and safety parameters, quality of randomization and blinding procedures were evaluated. Bayesian network meta-analysis was performed. Results. Cytisine overcame placebo in the 12, 24 and 52 weeks of therapy with the following odds ratios (ORs) for abstinence: 3.3 (95% CrI 1.8–5.8), 3.9 (2.4–6.7), 3.8 (CrI 1.3–11,9) accordingly. Varenicline in 2 mg/day dose overcame placebo in the 12, 24 and 52 weeks of therapy with the ORs: 4.0 (3.3–4.7), 3.1 (2.5–3.7), 2.9 (2.2–4.1) accor dingly. Varenicline in 1 mg/day dose overcame placebo in 12 and 52 weeks of therapy, the ORs were 3.0 (2.0–4.7) and 2.3 (1.3–4.4) accordingly. Varenicline in 0.5 mg/day dose overcame placebo in 12 weeks of therapy only with the OR 2.4 (1.3–4.4). Cytisine and varenicline 2 mg/day were associated with more gastrointestinal disturbances than placebo with the ORs 6.2 (2.1–22.8) and 2.4 (2.0–2.8) accordingly. Cytisine and varenicline 2 mg/day were associated with more psychiatric problems than placebo with ORs 5.2 (1.9–15.1) and 1.6 (1.3–1.9) accordingly. There was no difference in serious adverse events between the investigated drugs and placebo: OR for cytisine was 2.4 (0.8–6.8), varenicline 0.5 mg/day – 2.0 (0.5–6.6), varenicline 1.0 mg/day – 1.0 (0.3–2.7), varenicline 2 mg/day – 1.0 (0.7–1.4). Conclusion. Cytisine was proved to be as effective and safe aid for smoking cessation as varenicline.

scholarly journals Varenicline for Smoking Cessation: a Review

2016 ◽  
Vol 12 (3) ◽  
pp. 215-220
Author(s):  
G P Rauniar ◽  
A Mishra ◽  
D P Sarraf
Keyword(s):  
Smoking Cessation ◽  
Tobacco Use ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Smoking Prevalence ◽  
Meta Analysis ◽  
Developed Countries ◽  
First Line ◽  
The World ◽  
Quitting Smoking

Tobacco use is the leading cause of preventable death and disability in the world. Although gradually declining in most developed countries, the prevalence of tobacco use has increased among developing countries. Nicotine is an addictive chemical that is inhaled from the tobacco present in the cigarettes. It acts on neuronal nicotinic acetylcholine receptors within the ventral tegmental area of the brain, causing dopamine release in the nucleus accumbens which reinforces nicotine-seeking behavior. Reward through the dopaminergic system is a common thread among many drugs of addiction. According to the National Anti-Tobacco Communication Campaign Strategy for Nepal smoking prevalence in Nepal is higher (38.4%) than the smoking prevalence in the world (29%). Smoking attributable annual deaths in Nepal is estimated at nearly 14,000 (9,000 male deaths and 5,000 female deaths) for population aged 35 and over. First-line pharmacotherapies for smoking cessation are varenicline, sustained-release bupropion and various forms of nicotine replacement therapy (i.e., patch, gum, lozenge, inhaler, nasal spray). These drugs can be used as monotherapy or combination therapy for the treatment of smoking cessation. After studying the outcome of many clinical trials and meta-analysis, it is concluded that cigarette smokers taking varenicline have the most success quitting smoking as compared with those taking other first-line pharmacotherapies for treating smoking cessation.  Health Renaissance 2014;12(3): 215-220

scholarly journals Update on pharmacotherapy for smoking cessation

2021 ◽  
Vol 64 (3) ◽  
pp. 216-224
Author(s):  
Hye Sook Choi ◽  
Jae Yeol Kim
Keyword(s):  
Smoking Cessation ◽  
Cigarette Smoking ◽  
Adverse Events ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
First Line ◽  
Effective Agent ◽  
Nicotinic Acetylcholine ◽  
Increased Risk

Cigarette smoking is the leading preventable cause of death, and smoking cessation is the only way to reduce the risk of developing and dying from smoking-related diseases. The binding of nicotine to <i>α</i>4<i>β</i>2 nicotinic acetylcholine receptors in the ventral tegmental area causes transmission of signals to nuclear accumbens, where neurotransmitters, such as dopamine, are released. Euphoric feelings and satisfaction acquired due to the released neurotransmitters make smokers reach for a cigarette once again after a short while, thereby completing a repeating cycle of addiction. Medications for smoking cessation, such as nicotine replacement therapy (NRT), bupropion, and varenicline, are designed to cope with nicotine addiction. NRT provides nicotine to ameliorate withdrawal symptoms, and all forms of NRT are equally effective in smoking cessation than placebo. Bupropion, originally developed as an antidepressant, decreases craving, leading to smoking cessation, which makes it one of the first-line drugs for smoking cessation. Many studies have shown that varenicline is the most effective agent for smoking cessation. No significant long-term adverse events have been reported for NRT, bupropion, or varenicline. However, bupropion should not be used in patients with an increased risk for seizure.

scholarly journals Countering Opioid-induced Respiratory Depression in Male Rats with Nicotinic Acetylcholine Receptor Partial Agonists Varenicline and ABT 594

2020 ◽  
Vol 132 (5) ◽  
pp. 1197-1211
Author(s):  
Jun Ren ◽  
Xiuqing Ding ◽  
John J. Greer
Keyword(s):  
Respiratory Depression ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Male Rats ◽  
Whole Body ◽  
Vehicle Group ◽  
Opioid Overdose ◽  
Sprague Dawley ◽  
Nicotinic Acetylcholine ◽  
Partial Agonists

Abstract Background Opioids can induce significant respiratory depression when administered as analgesics for the treatment of acute, postoperative, and chronic pain. There are currently no pharmacologic means of reversing opioid-induced respiratory depression without interfering with analgesia. Further, there is a growing epidemic of opioid overdose that could benefit from therapeutic advancements. The aim of this study was to test the ability of two partial agonists of α4β2 nicotinic acetylcholine receptors, varenicline (used clinically for smoking cessation) and ABT 594 (tebanicline, developed as an analgesic), to reduce respiratory depression induced by fentanyl, remifentanil, morphine, and a combination of fentanyl and diazepam. Methods Whole body plethysmographic recordings, nociception testing, and righting reflex testing were used to examine ventilation, analgesia, and sedation in adult male Sprague–Dawley rats. Results Pre-, co-, or postadministration of varenicline or ABT 594 did not alter baseline breathing but markedly reduced opioid-induced respiratory depression. Varenicline had no effect on fentanyl-induced analgesia and ABT 594 potentiated fentanyl-induced analgesia. Specifically, 10-min administration of fentanyl induced a decrease in respiratory rate to 43 ± 32% of control in vehicle group, which was alleviated by preadministration of varenicline (85 ± 14% of control, n = 8, P &lt; 0.001) or ABT 594 (81 ± 36% of control, n = 8, P = 0.001). ABT 594 or varenicline with a low dose of naloxone (1 µg/kg), but not varenicline alone, partially reversed fentanyl-induced lethal apnea, but neither compound provided the very rapid and complete reversal of apnea achieved with high doses of naloxone (0.03 to 1 mg/kg). Administration of varenicline (n = 4, P = 0.034) or ABT 594 (n = 4, P = 0.034) prevented lethal apneas induced by the combination of fentanyl and diazepam. Conclusions Activation of α4β2 nicotinic acetylcholine receptors by varenicline and ABT 594 counters opioid-induced respiratory depression without interfering with analgesia. Editor’s Perspective What We Already Know about This Topic What This Article Tells Us That Is New

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