Appendix VIII: Drugs Used for Smoking Cessation

Updated July 2009

What’s New – July 2009 Update

“Disadvantages” column – bupropion and varenicline

Drugs Used for Smoking Cessation

Table 1: Drugs Used for Smoking Cessation

Product	Daily Dose	Duration of Treatment	Common Side Effects	Advantages	Disadvantages
Nicotine-replacement therapy (Low potential for drug-drug interactions with PIs and NNRTIs)
Transdermal patch^a 24 hr (e.g., Nicoderm CQ) 16 hr (e.g., Nicotrol)	7-, 14-, or 21-mg patch worn for 24 hr^b 15-mg patch worn for 16 hr	8 wk 8 wk	Skin irritation, insomnia	Provides steady level of nicotine; easy to use; unobtrusive; available without prescription	User cannot adjust dose if craving occurs; nicotine released more slowly than in other products
Nicotine polacrilex gum (Nicorette)^a 2 mg (<25 cigarettes/d) 4 mg (>25 cigarettes/d)	1 piece/h (<24 pieces/d)	8-12 wk	Mouth irritation, sore jaw, dyspepsia, hiccups	User controls dose; oral substitute for cigarettes; available without prescription	Proper chewing technique needed to avoid side effects and achieve efficacy^c; user cannot eat or drink while chewing the gum; can damage dental work; difficult for denture wearers to use
Nicotine polacrilex lozenge^a 2 mg (<25 cigarettes/d) 4 mg (>25 cigarettes/d)	1 lozenge q1-2h for 6 wk, then q2-4h for 3 wk, then q4-8h for 3 wk, then PRN for 3 mo	3-6 mo	Headache, heartburn, hiccups, nausea, cough	User controls dose; offers rapid delivery of high levels of nicotine	Side effects
Vapor inhaler (Nicotrol Inhaler)^a,/i>	6-16 cartridges/d (delivered dose, 4 mg/ cartridge)	3-6 mo	Mouth and throat irritation, cough	User controls dose; hand-to-mouth substitute for cigarettes	Frequent puffing needed; device visible when used
Nasal spray (Nicotrol NS)^a	1-2 doses/h (1 mg total; 0.5 mg in each nostril; max: 40 mg/d)	3-6 mo	Nasal irritation; sneezing, coughing, teary eyes	User controls dose; offers most rapid delivery of nicotine and the highest nicotine levels of all nicotine- replacement products	Most irritating nicotine replacement product to use^d; device visible when used
Non-nicotine therapy
Sustained-release bupropion (Zyban or Wellbutrin SR)^e	150 mg/d for 3 days, then 150 mg bid	7-12 wk up to 6 mo to maintain abstinence	Insomnia, dry mouth, agitation	Easy to use (pill), no exposure to nicotine	Increases risk of seizure (<0.1%). Efavirenz may decrease bupropion serum concentrations. Titrate to effect. Risk of serious neuropsychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, suicidal thoughts, and attempted suicide. Patients should be counseled to stop taking bupropion and immediately contact their clinician if they experience any of these symptoms.
Varenicline HCl (Chantix)^e	0.5 mg/d for 3 days, then 0.5 mg bid for 3 days, then 1 mg/d for 3 wk, then 1 mg bid	12 wk	Nausea, insomnia, abnormal dreams, headache	Easy to use (pill), no exposure to nicotine, blocks nicotine and therefore pleasure of smoking. Drug interaction unlikely.	Risk of serious neuropsychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, suicidal thoughts, and attempted suicide. Patients should be counseled to stop taking varenicline and immediately contact their clinician if they experience any of these symptoms.
Nortriptyline^f	75-100 mg/d^g	12 wk	Dry mouth, sedation, dizziness	Easy to use (pill), no exposure to nicotine. Serum concentrations may be increased with PI co-administration.	Side effects common; should be used cautiously in patients with coronary heart disease
Clonidine^f	0.1-0.3 mg bid	3-10 wk	Dry mouth, sedation, dizziness	No exposure to nicotine	Side effects limit use

With the exception of varenicline, the information in this appendix is adapted, with permission, from Rigotti NA. Clinical practice. Treatment of tobacco use and dependence. N Engl J Med 2002;346:506-512. Information regarding varenicline is from City Health Information. New York City Department of Health and Mental Hygiene; December 2007/January 2008. Available at: www.nyc.gov/html/doh/downloads/pdf/chi/chi27-1.pdf

^a These products have been approved by the Food and Drug Administration as smoking-cessation aids. The Public Health Service clinical guidelines also recommend them as first-line drugs for smoking cessation.

^b The starting dose is 21 mg/d unless the smoker weighs less than 45.5 kg (100 lb) or smokes fewer than 10 cigarettes per day, in which case the starting dose is 14 mg/d. The starting dose should be maintained for 4 weeks, after which the dose should be decreased every week until it is stopped.

^c The user should chew the gum slowly until he or she experiences a distinct taste, indicating that nicotine is being released. The user should then place the gum between cheek and gum until the taste disappears to allow the nicotine to be absorbed through oral mucosa. The sequence should be repeated for 30 minutes before the gum is discarded. Acidic beverages (such as coffee and soft drinks) reduce the absorption of nicotine and should be avoided for 30 minutes before and during chewing.

^d Tolerance develops to local side effects during the first week of use.

^e Treatment should be started 1 week before the quitting date.

^f This agent has not been approved by the Food and Drug Administration as a smoking-cessation aid. The Public Health Service clinical guidelines recommend it as a second-line drug for smoking cessation.

^g Treatment should be started 10 to 28 days before the quitting date at a dose of 25 mg/d, and the dose should be increased as tolerated.