伐尼克兰 (Champix, Chantix, Tyrvaya)

概览

Varenicline is a partial agonist at nicotinic acetylcholine receptors used as an aid in smoking cessation.

作用机制

Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectivity for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.

适应症

For use as an aid in smoking cessation. Varenicline as a nasal spray is indicated for the symptomatic treatment of dry eye disease.

• Dry Eye Syndrome (DES)