scholarly journals Diverse strategies targeting α7 homomeric and α6β2* heteromeric nicotinic acetylcholine receptors for smoking cessation

2014 ◽  
pp. n/a-n/a ◽  
Author(s):  
Darlene H. Brunzell ◽  
J. Michael McIntosh ◽  
Roger L. Papke
2018 ◽  
Vol 16 (4) ◽  
pp. 19-32
Author(s):  
Elena V. Radchenko ◽  
Olga A. Sykhovskaya ◽  
Timofey L. Galankin ◽  
Aleksei S. Kolbin ◽  
Maria A. Smirnova

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.


2021 ◽  
Vol 64 (3) ◽  
pp. 216-224
Author(s):  
Hye Sook Choi ◽  
Jae Yeol Kim

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.


2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S586-S586 ◽  
Author(s):  
Kazuo Hashikawa ◽  
Hidefumi Yoshida ◽  
Nobukatsu Sawamoto ◽  
Shigetoshi Takaya ◽  
Chihiro Namiki ◽  
...  

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