Table 1.

FDA-Approved Medications for Smoking Cessation

	Nicotine Replacement Therapy (NRT) Formulations					Bupropion SR	Varenicline
	Gum	Lozenge	Transdermal Patch	Nasal Spray	Oral Inhaler
Product	Nicorette*, Generic OTC 2 mg, 4 mg	Nicorette Lozenge,* Nicorette Mini Lozenge,* Generic OTC 2 mg, 4 mg	NicoDerm CQ*, Generic OTC (NicoDerm CQ, generic) Rx (generic) 7 mg, 14 mg, 21 mg (24-hour release)	Nicotrol NS† Rx Metered spray 0.5 mg nicotine in 50 mcL aqueous nicotine solution	Nicotrol Inhaler† Rx 10 mg cartridge delivers 4 mg inhaled nicotine vapor	Zyban*, Generic Rx 150 mg sustained-release tablet	Chantix† Rx 0.5 mg, 1 mg tablet
Precautions	Precautions for all NRT formulations Recent (≤ 2 weeks) myocardial infarction Serious underlying arrhythmias Serious or worsening angina pectoris Pregnancy‡ (category D) and breastfeeding Adolescents (<18 years) Precautions specific to certain NRT formulations Gum: Temporomandibular joint disease Nasal spray: Underlying chronic nasal disorders (rhinitis, nasal polyps, sinusitis); Severe reactive airway disease Oral inhaler: Bronchospastic disease					Medications or medical conditions known to lower the seizure threshold Severe hepatic cirrhosis Pregnancy‡ (category C) and breastfeeding Adolescents (<18 years) Warning: Black-boxed warning for neuropsychiatric symptoms§ Contraindications: Seizure disorder Diagnosis of bulimia or anorexia nervosa MAO inhibitor therapy in previous 14 days	Severe renal impairment (dosage adjustment is necessary) Pregnancy‡ (category C) and breastfeeding Adolescents (<18 years) Warning: Black-boxed warning for neuropsychiatric symptoms4
Dosing	1st cigarette ≤30 minutes after waking: 4 mg 1st cigarette >30 minutes after waking: 2 mg Weeks 1–6:  1 piece q 1–2 hours Weeks 7–9:  1 piece q 2–4 hours Weeks 10–12:  1 piece q 4–8 hours Maximum, 24 pieces/day Chew each piece slowly Park between cheek and gum when peppery or tingling sensation appears (~15–30 chews) Resume chewing when tingle fades Repeat chew/park steps until most of the nicotine is gone (generally 30 min) Park in different areas of mouth No food or beverages 15 minutes before or during use Duration: up to 12 weeks	1st cigarette ≤30 minutes after waking: 4 mg 1st cigarette >30 minutes after waking: 2 mg Weeks 1–6:  1 lozenge q 1–2 hours Weeks 7–9:  1 lozenge q 2–4 hours Weeks 10–12:  1 lozenge q 4–8 hours Maximum, 20 lozenges/day Allow to dissolve slowly (20–30 minutes for standard; 10 minutes for mini) Nicotine release may cause a warm, tingling sensation Do not chew or swallow Occasionally rotate to different areas of the mouth No food or beverages 15 minutes before or during use Duration: up to 12 weeks	>10 cigarettes/day: 21 mg/day × 4 weeks (generic)  6 weeks (NicoDerm CQ) 14 mg/day × 2 weeks 7 mg/day × 2 weeks ≤ 10 cigarettes/day: 14 mg/day × 6 weeks 7 mg/day × 2 weeks May wear patch for 16 hours if patient experiences sleep disturbances (remove at bedtime) Duration: 8–10 weeks	1–2 doses/hour (8–40 doses/day) One dose = 2 sprays (one in each nostril); each spray delivers 0.5 mg of nicotine to the nasal mucosa Maximum 5 doses/hour or 40 doses/day For best results, initially use at least 8 doses/day Do not sniff, swallow, or inhale through the nose as the spray is being administered Duration: 3–6 months	6–16 cartridges/day Individualize dosing; initially use 1 cartridge q 1–2 hours Best effects with continuous puffing for 20 minutes Initially use at least 6 cartridges/day Nicotine in cartridge is depleted after 20 minutes of active puffing Inhale into back of throat or puff in short breaths Do NOT inhale into the lungs (like a cigarette) but “puff” as if lighting a pipe Open cartridge retains potency for 24 hours No food or beverages 15 minutes before or during use Duration: 3–6 months	150 mg po q AM × 3 days, then 150 mg po bid Do not exceed 300 mg/day Begin therapy 1–2 weeks prior to quit date Allow at least 8 hours between doses Avoid bedtime dosing to minimize insomnia Dose tapering is not necessary Duration: 7–12 weeks, with maintenance up to 6 months in selected patients	Days 1–3:  0.5 mg po q AM Days 4–7:  0.5 mg po bid Weeks 2–12:  1 mg po bid Begin therapy 1 week prior to quit date; alternatively, the patient can begin therapy and then quit smoking between days 8–35 of treatment Take dose after eating and with a full glass of water Dose tapering is not necessary Dosing adjustment is necessary for patients with severe renal impairment Duration: 12 weeks; an additional 12-week course may be used in selected patients
Adverse Effects	Mouth/jaw soreness Hiccups Dyspepsia Hypersalivation Effects associated with incorrect chewing technique: Lightheadedness Nausea/vomiting Throat and mouth irritation	Nausea Hiccups Cough Heartburn Headache Flatulence Insomnia	Local skin reactions (erythema, pruritus, burning) Headache Sleep disturbances (insomnia, abnormal/vivid dreams); associated with nocturnal nicotine absorption	Nasal and/or throat irritation (hot, peppery, or burning sensation) Rhinitis Tearing Sneezing Cough Headache	Mouth and/or throat irritation Cough Headache Rhinitis Dyspepsia Hiccups	Insomnia Dry mouth Nervousness/difficulty concentrating Rash Constipation Seizures (risk is 0.1%) Neuropsychiatric symptoms (rare; see Precautions)	Nausea Sleep disturbances (insomnia, abnormal/vivid dreams) Constipation Flatulence Vomiting Neuropsychiatric symptoms (rare; see Precautions)
Advantages	Might satisfy oral cravings Might delay weight gain Patients can titrate therapy to manage withdrawal symptoms Variety of flavors are available	Might satisfy oral cravings Might delay weight gain Easy to use and conceal Patients can titrate therapy to manage withdrawal symptoms Variety of flavors are available	Provides consistent nicotine levels over 24 hours Easy to use and conceal Once daily dosing associated with fewer compliance problems FDA-approved for use in combination with bupropion SR	Patients can titrate therapy to rapidly manage withdrawal symptoms	Patients can titrate therapy to manage withdrawal symptoms Mimics hand-to-mouth ritual of smoking (could also be perceived as a disadvantage)	Easy to use; oral formulation might be associated with fewer compliance problems Might delay weight gain Can be used safely with NRT; FDA-approved for use in combination with nicotine transdermal patch Might be beneficial in patients with depression	Easy to use; oral formulation might be associated with fewer compliance problems Offers a new mechanism of action for patients who have failed other agents
Disadvantages	Need for frequent dosing can compromise compliance Might be problematic for patients with significant dental work Patients must use proper chewing technique to minimize adverse effects Gum chewing may not be socially acceptable	Need for frequent dosing can compromise compliance Gastrointestinal side effects (nausea, hiccups, heartburn) might be bothersome	Patients cannot titrate the dose to acutely manage withdrawal symptoms Allergic reactions to adhesive might occur Patients with dermatologic conditions should not use the patch	Need for frequent dosing can compromise compliance Nasal/throat irritation may be bothersome Patients must wait 5 minutes before driving or operating heavy machinery Patients with chronic nasal disorders or severe reactive airway disease should not use the spray	Need for frequent dosing can compromise compliance Initial throat or mouth irritation can be bothersome Cartridges should not be stored in very warm conditions or used in very cold conditions Patients with underlying bronchospastic disease must use with caution	Seizure risk is increased Several contraindications and precautions preclude use in some patients (see Precautions) Patients should be monitored for potential neuropsychiatric symptoms§ (see Precautions)	May induce nausea in up to one third of patients Patients should be monitored for potential neuropsychiatric symptoms4 (see Precautions)
Cost/day||	2 mg or 4 mg: $1.90–$5.48 (9 pieces)	2 mg or 4 mg: $3.05–$4.10 (9 pieces)	$1.52–$3.40 (1 patch)	$4.32 (8 doses)	$7.74 (6 cartridges)	$2.54–$6.22 (2 tablets)	$6.54 (2 tablets)

Abbreviations: MAO, monoamine oxidase; NRT, nicotine replacement therapy; OTC, over-the-counter (non-prescription product); Rx, prescription product.

^*Marketed by GlaxoSmithKline.

^†Marketed by Pfizer.

^‡The USPHS Clinical Practice Guideline (37) states that pregnant smokers should be encouraged to quit without medication based on insufficient evidence of effectiveness and theoretical concerns with safety. Pregnant smokers should be offered behavioral counseling interventions that exceed minimal advice to quit.

^§In July 2009, the FDA mandated that the prescribing information for all bupropion- and varenicline-containing products include a black-boxed warning highlighting the risk of serious neuropsychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, suicidal thoughts and behavior, and attempted suicide. Clinicians should advise patients to stop taking varenicline or bupropion SR and contact a healthcare provider immediately if they experience agitation, depressed mood, and any changes in behavior that are not typical of nicotine withdrawal, or if they experience suicidal thoughts or behavior. If treatment is stopped due to neuropsychiatric symptoms, patients should be monitored until the symptoms resolve.

^||Wholesale acquisition cost from Red Book Online. Thomson Reuters, July 2013. This Table was adapted with permission from The Regents of the University of California, RxforChange (http://rxforchange.ucsf.edu/)