From the Guidelines
Varenicline is the most effective single pharmacotherapy option for smoking cessation, increasing the odds of quitting by almost 3-fold compared to placebo. When considering smoking cessation, it is essential to prioritize the most effective treatment options to reduce morbidity, mortality, and improve quality of life. According to a Cochrane network meta-analysis 1, varenicline has been shown to be more efficacious than bupropion and single forms of nicotine replacement therapy (NRT), with an odds ratio (OR) of 2.88 (95% CI, 2.40–3.47) compared to placebo. Some key points to consider when prescribing varenicline include:
- The standard treatment regimen, which typically begins with a one-week titration and continues for 12 weeks total
- Common side effects, such as nausea, sleep disturbances, headache, and vivid dreams
- The need for cautious use in patients with psychiatric conditions, as it may worsen mood disorders or cause behavioral changes in some individuals
- The potential for increased alcohol effects, and the recommendation to reduce alcohol consumption while taking varenicline
- The importance of monitoring patients for neuropsychiatric symptoms. Overall, varenicline is a highly effective treatment option for smoking cessation, and its use should be considered for patients who are motivated to quit smoking, as it can significantly improve their chances of success and reduce the risks associated with smoking 1.
From the FDA Drug Label
Varenicline tablets are indicated for use as an aid to smoking cessation treatment. The answer to the question about Varenicline is that it is indicated for use as an aid to smoking cessation treatment 2, 2, 2.
- Key points:
- Nicotinic receptor partial agonist
- Aid to smoking cessation treatment The dosage and administration instructions are provided in the label, but the question does not ask for this information.
From the Research
Varenicline Overview
- Varenicline is an orally administered small molecule with partial agonist activity at the alpha4beta2 nicotinic acetylcholine receptor 3.
- It was approved by the US FDA and the European Medicines Agency in 2006 as an aid to smoking cessation 3.
- Varenicline has been shown to be effective in smoking cessation, with higher abstinence rates compared to placebo and other treatments such as bupropion and nicotine replacement therapy 3, 4, 5, 6.
Pharmacokinetics and Pharmacodynamics
- Varenicline exhibits linear pharmacokinetics following single- and multiple-dose administration 4.
- It is almost entirely absorbed following oral administration, and absorption is unaffected by food, smoking, or the time of day 3.
- Varenicline undergoes minimal metabolism and is primarily excreted unchanged in the urine 3, 4.
- The elimination half-life of varenicline is approximately 24 hours, and steady-state conditions are reached within 4 days of repeat dosing 4.
Efficacy and Safety
- Varenicline has been shown to be effective in smoking cessation, with higher abstinence rates compared to placebo and other treatments 3, 4, 5, 6.
- The most common adverse events associated with varenicline are nausea, insomnia, and headache 5.
- Varenicline has been shown to be generally well-tolerated, with few treatment discontinuations due to adverse events 5.
- A study comparing 0.5 mg and 1 mg varenicline found no difference in smoking cessation effectiveness, adherence, or side effects between the two doses 7.
Dosage and Administration
- The usual oral dosage of varenicline is 1 mg twice daily for 12 weeks, with an initial titration week 4.
- Varenicline treatment should begin 7 days before the proposed smoking quit date, and dose titration is recommended to minimize dose-related nausea 5.
- A dose reduction to 1 mg/day is indicated for subjects with severe renal insufficiency 4.