Escobar-Chávez José Juan, Domínguez-Delgado Clara Luisa, Rodríguez-Cruz Isabel Marlen
Unidad de Investigación Multidisciplinaria, Facultad de Estudios Superiores Cuautitlán-Universidad Nacional Autónoma de México, Cuautitlán Izcalli, Estado de México, México.
Drug Des Devel Ther. 2011;5:211-24. doi: 10.2147/DDDT.S10033. Epub 2011 Apr 18.
Cigarette smoking is the primary cause of lung cancer, cardiovascular diseases, reproductive disorders, and delayed wound healing all over the world. The goals of smoking cessation are both to reduce health risks and to improve quality of life. The development of novel and more effective medications for smoking cessation is crucial in the treatment of nicotine dependence. Currently, first-line smoking cessation therapies include nicotine replacement products and bupropion. The partial nicotinic receptor agonist, varenicline, has recently been approved by the US Food and Drug Administration (FDA) for smoking cessation. Clonidine and nortriptyline have demonstrated some efficacy, but side effects may limit their use to second-line treatment products. Other therapeutic drugs that are under development include rimonabant, mecamylamine, monoamine oxidase inhibitors, and dopamine D3 receptor antagonists. Nicotine vaccines are among newer products seeking approval from the FDA. Antidrug vaccines are irreversible, provide protection over years and need booster injections far beyond the critical phase of acute withdrawal symptoms. Interacting with the drug in the blood rather than with a receptor in the brain, the vaccines are free of side effects due to central interaction. For drugs like nicotine, which interacts with different types of receptors in many organs, this is a further advantage. Three anti-nicotine vaccines are today in an advanced stage of clinical evaluation. Results show that the efficiency of the vaccines is directly related to the antibody levels, a fact which will help to optimize the vaccine effect. The vaccines are expected to appear on the market between 2011 and 2012.
在全球范围内，吸烟是导致肺癌、心血管疾病、生殖系统紊乱以及伤口愈合延迟的主要原因。戒烟的目标既是降低健康风险，也是提高生活质量。研发新型且更有效的戒烟药物对于治疗尼古丁依赖至关重要。目前，一线戒烟疗法包括尼古丁替代产品和安非他酮。部分烟碱受体激动剂伐尼克兰最近已获美国食品药品监督管理局（FDA）批准用于戒烟。可乐定和去甲替林已显示出一定疗效，但副作用可能限制它们仅用于二线治疗产品。其他正在研发的治疗药物包括利莫那班、美加明、单胺氧化酶抑制剂以及多巴胺D3受体拮抗剂。尼古丁疫苗是正在寻求FDA批准的较新产品之一。抗药疫苗是不可逆的，能提供数年的保护，并且在急性戒断症状的关键阶段之后还需要多次加强注射。疫苗在血液中与药物相互作用，而非与大脑中的受体相互作用，因此不会因中枢相互作用而产生副作用。对于像尼古丁这样在许多器官中与不同类型受体相互作用的药物来说，这是一个额外的优势。如今有三种抗尼古丁疫苗正处于临床评估的后期阶段。结果表明，疫苗的有效性与抗体水平直接相关，这一事实将有助于优化疫苗效果。这些疫苗预计在2011年至2012年之间上市。
