Varenicline (CHAMPIX) – Mechanism of Action | Psychopharmacology | Clinical Application

Posted on:January 21, 2023
Last Updated: January 21, 2023
Time to read: 8 minutes

Varenicline (CHANTIX /CHAMPIX) is a nicotinic acetylcholine receptor (nAChR) partial agonist indicated as a smoking cessation drug. [Cahill et al. 2013]

Varenicline has been shown to be superior to placebo and nicotine-replacement therapies. It is often used alongside behavioural support, which may include face-to-face counselling or group therapies to help people who smoke quit as soon as possible. [Ranney et al. 2006]

However, safety concerns about varenicline have been raised, especially for patients with psychiatric disorders. [Tobin and Tobin 2015]

The initial trials performed by Pfizer excluded patients with psychiatric disorders. Since its approval in 2006, the FDA has published additional warnings (in 2007, 2009, and 2011) about the risk of serious neuropsychiatric side effects. [CHAMPIX® (varenicline) Tablets Prescribing Information]