Goniewicz Maciej Lukasz, Koszowski Bartosz, Czogała Jan, Sobczak Andrzej
Zakład Chemii Ogólnej i Nieorganicznej, Katedry Chemii Ogólnej i Analitycznej, Slaskiego Uniwersytetu Medycznego w Katowicach.
Przegl Lek. 2007;64(10):899-902.
Cigarette smokers believe that quitting smoking is the hardest thing in their life. Modern pharmacology offers a wide range of various drugs and therapies that might support smoking cessation. One of the most effective drug is varenicline. Varenicline has been introduced this year to Polish pharmaceutical market by Pfizer company under the trade name Champix. The aim of the study was to critically review all new information about Champix pharmacology and pharmacokinetics but also evaluate safety and economical aspects of using this new drug. From the presented data it might be concluded that nowadays varenicline is the most effective drug used in smoking cessation (about 40%). The unique properties of varenicline, which is a partial agonist and antagonist to alpha4beta2 nicotinic receptor, are the reasons of dual mechanism of the drug action. The agonist effect is caused by binding to nicotinic receptors and stimulating receptor-mediated activity. The antagonist effect occurs when varenicline blocks the ability of nicotine to activate nicotinic receptors. The most frequently adverse effects of varenicline are: nausea, headache, insomnia, and abnormal dreams. Although the price of complete therapy with Champix seems to be quite high, but potential benefits (in case of therapy finished successfully) are much higher than these costs. Pharmacological properties of varenicline described in the article, along with its high relative effectiveness and safeness, make the drug very attractive and promising for the smokers who want to quit.
吸烟者认为戒烟是他们生活中最困难的事情。现代药理学提供了各种各样的药物和疗法来辅助戒烟。最有效的药物之一是伐尼克兰。今年，辉瑞公司以畅沛（Champix）为商品名将伐尼克兰引入波兰药品市场。本研究的目的是严格审查关于畅沛药理学和药代动力学的所有新信息，同时评估使用这种新药的安全性和经济性。从所呈现的数据可以得出结论，如今伐尼克兰是用于戒烟最有效的药物（成功率约为40%）。伐尼克兰作为α4β2烟碱受体的部分激动剂和拮抗剂所具有的独特性质，是其双重作用机制的原因。激动剂效应是通过与烟碱受体结合并刺激受体介导的活性而产生的。当伐尼克兰阻断尼古丁激活烟碱受体的能力时，就会产生拮抗剂效应。伐尼克兰最常见的不良反应有：恶心、头痛、失眠和异常梦境。虽然使用畅沛进行完整治疗的价格似乎相当高，但潜在益处（如果治疗成功完成）远高于这些成本。本文中描述的伐尼克兰的药理学特性，以及其较高的相对有效性和安全性，使得该药物对想要戒烟的吸烟者非常有吸引力且前景广阔。
