Cigarette smoking is a difficult problem

Cigarette smoking is a difficult problem that pharmacists and other healthcare professionals can play an important role in. Varenicline is one of the main medications that can be used to help curb this addiction. In this post, I will lay out my most important varenicline clinical pearls that I have learned from my practice as a pharmacist.

Let’s start with how the drug works. Unlike nicotine replacement therapy, varenicline is not a true agonist at nicotine receptors. Varenicline is a partial agonist. Because of this mechanism of action, varenicline can bind and partially stimulate nicotine receptors, all the while blocking full agonists (i.e. nicotine) from binding. By preventing activation of the nicotine receptor, it can reduce the reward sensation of using cigarettes.

The most problematic adverse effects that I have had patients report are in relation to sleep. Insomnia and very vivid dreams are two of the most common complaints I have heard from patients. If the patient encounters adverse effects relating to sleep, one might consider taking the evening dose a little earlier in the day and/or possibly reducing the dose.

Nausea is also a potential adverse effect and one of the major reasons why the dose is started low and titrated upward over time. It is also recommended to be administered after eating and with a full glass of water.

Nausea, insomnia, and abnormal dreams are the most common varenicline clinical pearls you should know are it relates to adverse effects.

Psychiatric changes had been reported in the past and I definitely remember learning this in school. In fact, there used to be a boxed warning on this medication for these issues. However, more data has come out that has been favorable. The boxed warning of the risk of neuropsychiatric events has now been removed, but there is still the verbiage in the package insert.

Can I take varenicline while I am still smoking? The historic recommendation on this question was that patients should stop smoking 1 week after starting varenicline. The idea behind this is that it gives the drug time to reach a steady-state. It is now an acceptable option to consider using varenicline in combination with smoking for a longer period of time to allow patients to taper down on smoking if they desire.