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Smoking in Cancer Care (PDQ®): Supportive care - Health Professional Information [NCI] - Pharmacological Treatment

Table 4. Nicotine Patches

BrandDoseSide EffectsComments
OTC = over the counter; Rx = prescription.
RxHabitrol7–21 mg/dErythemaUse for 6–12 weeks.
OTCNicoDerm CQ7–21 mg/dPruritusUse for 6–12 weeks.
OTCNicotrol5–15 mg/dBurning at siteUse for 14–20 weeks.
RxProStep11–22 mg/dLocal irritationUse for 6–12 weeks.

Varenicline (Chantix)

Varenicline is a nicotinic acetylcholine receptor partial agonist and the first U.S. Food and Drug Administration (FDA)-approved prescription pharmacologic agent targeted to these nicotinic receptors.[2][Level of evidence: I] Although specific mechanisms of action are unknown, it is thought that the agonist properties result in reduced craving and withdrawal by stimulating release of dopamine, and the antagonist properties prevent inhaled nicotine from binding at the nicotinic receptor sites.[3]

There have been at least 12 published randomized, controlled trials evaluating varenicline versus placebo (or other approved agents for smoking cessation) for its ability to affect abstinence rates related to smoking or the use of smokeless tobacco.[2,4,5,6,7,8,9,10,11,12,13,14] All studies were relatively large (129–607 patients per arm) and involved multiple sites and countries. In all studies, varenicline was statistically better in achieving abstinence rates by self-report and carbon monoxide measures than was placebo, and was often better than the other approved smoking cessation comparator arm. Abstinence rates at 12 weeks can be expected to range from 44% to 49% for varenicline, compared to 11% to 17% for placebo; longer-term rates (52 weeks) range from 14% to 22% for varenicline versus 4% to 8% for placebo.

Most studies evaluated varenicline 1 mg twice a day, using a 1-week titration of 0.5 mg daily for 3 days, 0.5 mg twice a day for 4 days, and then 1 mg twice a day for 11 weeks. However, a few studies evaluated different doses, such as 0.3 mg or 0.5 mg daily or 0.5 mg twice a day, and one study evaluated a flexible dosing schedule during weeks 2 to 12 after all participants were titrated up to 1 mg twice a day in an open-label fashion. From these data, varenicline 0.5 mg twice a day appears to be the minimum dose required to achieve statistically significantly better abstinence rates over placebo.[9,10]

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