Successful smoking cessation should involve combining behavioral counseling and drug therapy. The chart below reviews available drug products to assist with smoking cessation, including place in therapy, dosing, possible advantages and disadvantages, as well as patient counseling points.
Abbreviations: ACS = acute coronary syndrome; CV = cardiovascular; NRT = nicotine replacement therapy; MOA = mechanism of action; OTC = over-the-counter.
Nicotine Replacement Therapy (NRT): Combining long-acting WITH short-acting NRT formulations is a first-line option and considered standard of care to help patients stop smoking, even in patients with stable CV disease [Evidence Level A-2]. Some experts also consider combination NRT first-line in stable hospitalized patients with an ACS [Evidence Level C].Per Canadian guidance, oral NRT products may be preferred over the patch in patients who had a recent myocardial infarction or stroke (in the last two weeks) or with poorly controlled CV disease.
Long-acting NRT (patches) provides consistent nicotine levels to help reduce background cravings.2 Short-acting NRT (e.g., gum, lozenge, inhaler) provides as needed relief for breakthrough cravings and a sensory substitute for smoking. Base product selection on patient preferences, as the different NRT dosage forms are generally considered equally effective. NRT can be used for ≥3 months. Short-acting NRT can be continued after the patch has been stopped, if necessary. See product information for suggested NRT tapering regimens.
Products
Dosing
Advantages/Disadvantages
Additional Info/Counseling Points
Patch Available OTC (NicoDerm CQ, NicoDerm[Canada], etc)
Start with the 21 mg patch if patients smoke ≥10 cigarettes/day.
Start with the 14 mg patch if patients smoke <10 cigarettes/day (or if patients weigh <45 kg [Canada]).
Advantages:
Long-acting NRT: provides consistent nicotine levels throughout the day.1,2 Easiest NRT product to use.
Disadvantages:
Possible side effects may include local skin irritation, insomnia (difficulty sleeping), and vivid dreams.1 Insomnia and vivid dreams may lessen after three to four days. Rotate patch sites to minimize skin irritation.
Advise patients to remove the patch at bedtime if they continue to experience difficulty sleeping or vivid dreams after several days.
Tapering is optional after about six weeks on a dose. Tapering does NOT improve smoking cessation rates.
Usually used for about ten to 12 weeks, but can be used for longer than three months.
Lozenge Available OTC (Nicorette, Nicorette Mini Lozenge [Canada], etc)
Available in 2 mg and 4 mg. Use 4 mg for patients who smoke their first cigarette within ≤30 minutes of waking (or who smoke more than 25 cigarettes/day [Canada]).
Max: 20 lozenges/day (max of 15 lozenges/day [Canada]).
Advantages:
Short-acting; allows flexible dosing. Provides an oral substitute for a cigarette.1 May be easier to use than gum, especially for patients with dental work or dentures.
Disadvantages:
Possible side effects may include mouth irritation, hiccups, heartburn, nausea.1 Place lozenge between gum and cheek and allow to melt slowly (takes about 10 minutes to completely dissolve).
No food or drink within 15 minutes before or during use.
Can be used for three months or more.1 Canadian product labeling supports as needed use for up to six months.
Gum Available OTC (Nicorette gum, etc)
Available in 2 mg and 4 mg. Use 4 mg for patients who smoke their first cigarette within ≤30 minutes of waking (or who smoke more than 25 cigarettes/day [Canada]).
Max: 24 pieces/day (20 pieces/day [Canada]).
Advantages:
Short-acting; allows for flexible dosing.1 Provides an oral substitute for a cigarette.
Disadvantages:
Possible side effects may include mouth irritation, jaw soreness, heartburn, hiccups, nausea.1 Proper chewing is required to minimize side effects.2 Chew briefly until tingling sensation begins, then “park” gum inside cheek until tingling fades (usually about 1 minute). Repeat chewing and parking process. Spit gum out after 30 minutes.
No food or drink within 15 minutes before use or during use.
Can be used for three months or more.1 Canadian product labeling supports as needed use for up to six months.
Inhaler Requires a prescription (U.S.); available OTC (Canada).
(Nicotrol [U.S.], NicoretteInhaler [Canada])
Puff into mouth or throat until cravings stop. Do not inhale into lungs.
Max: 16 cartridges/day (12 cartridges/day [Canada]). Each cartridge contains about 80 puffs).
Advantages:
Short-acting; allows for flexible dosing.1 Provides a substitute for the hand-to-mouth ritual of smoking.
Disadvantages:
Requires frequent puffing.1 Possible side effects may include mouth and throat irritation. Coughing can also happen if inhaled too deeply.1 Change cartridge when nicotine taste disappears.
Can be used for three months or more.1
Nasal Spray (U.S. only) Requires a prescription (Nicotrol NS)
One spray in each nostril every one to two hours.1
Max: 80 sprays/day.1
Advantages:
Short-acting; allows for flexible dosing.1 Disadvantages:
Associated with the most side effects of the NRT products. Possible side effects may include nasal and throat irritation, runny nose, sneezing, coughing, tearing. Regular use for one week may help patients adjust to side effects.
Patients should not sniff or inhale while spraying and wait two or three minutes after use before blowing their nose.
Can be used for three months or more.
Oral Mist(Canada only) Available OTC (Nicorette QuickMist)
Spray one spray (two sprays if one does not reduce craving) into mouth every 30 minutes, as needed.
Wait a few seconds after spraying before swallowing.
Avoid inhaling the spray.
Max of 64 sprays/day.
Advantages:
Rapid-acting NRT (effects may be seen within 60 seconds) allows for flexible dosing.
Disadvantages:
Possible side effects may include hiccups, throat irritation, heartburn, nausea, strong taste.6 Avoid use for longer than six months, unless instructed to do so by a healthcare professional.
Non-NRT Medications Approved for Smoking Cessation: There are fewer data to support adding these to NRT or combining these medications, but these options can be considered for patients who fail or only partially respond to first-line therapy.
Products
Dosing
Advantages/Disadvantages
Additional Info/Counseling Points
Varenicline Requires a prescription (Chantix [U.S.]; Champix, generics [Canada])
MOA: blocks nicotine binding to alpha-4-beta-2 nicotinic acetylcholine receptors and partially stimulates nicotinic receptors to lessen pleasure from nicotine and reduce cravings, respectively.
Begin one to four weeks BEFORE quit date. However, quit date can range from one week to three months after starting therapy.
Titrate up over several days:
Day 1 to 3: 0.5 mg once a day Day 4 to 7: 0.5 mg twice a day (per Canadian product labeling, patients may continue taking 0.5 mg twice daily instead of titrating up) From day 8 forward: 1 mg twice a day Varenicline can be used for three to six months.
Advantages:
Relieves withdrawal AND blocks reward of smoking. Allows for a flexible quit date.
Disadvantages:
Possible side effects may include constipation, nausea, vomiting, insomnia, vivid dreams, headache, and seizures. Taking varenicline with food and a full glass of water may reduce nausea.1 Monotherapy is considered a first-line option, due to safety and efficacy, even in patients with stable CV disease.
Data are limited and conflicting for use in patients hospitalized with an ACS. Experts recommend using with caution in patients hospitalized with an ACS or to delay starting until discharge (e.g., when patients are more stable) [Evidence Level C].
Similar potential for psychiatric side effects to other smoking cessation meds.
Sustained-Release Bupropion Requires a prescription (Zyban, etc)
MOA: blocks reuptake of dopamine and norepinephrine. Weak nicotinic receptor antagonist.
Begin one to two weeks BEFORE quit date.
Titrate up over a few days:
Day 1 to 3: 150 mg once a day From day 4 forward: 150 mg twice a day Bupropion can be continued for three to six months.
Advantages:
Suppresses weight gain associated with smoking cessation.
Disadvantages:
Possible side effects may include insomnia, agitation, dry mouth, constipation, seizures, and headache.1,13 Can be used safely in patients with CV disease.
Considered second-line after combination NRT or varenicline in patients with stable CV disease or third-line in hospitalized patients with an ACS [Evidence Level C]. Can consider for patients with concomitant depression.
Other Medications Used for Smoking Cessation
Products
Dosing
Advantages/Disadvantages
Additional Info/Counseling Points
Clonidine Requires a prescription. Not FDA- or Health Canada-approved for smoking cessation.
Oral tablets (Catapres, generics)
Transdermal patch (U.S. only; Catapres TTS, generics)
MOA: stimulates alpha-2-adrenoceptors, reducing sympathetic outflow to reduce cravings, restlessness, and anxiety associated with smoking cessation.
Begin ≤3 days BEFORE quit date.
Oral tablets: Start with 0.1 mg twice daily, titrate up to a max total daily dose of about 0.7 to 0.8 mg/day.
Transdermal patch: Start with 0.1 mg patch applied once weekly, titrate up to a max of 0.3 mcg patch applied once weekly.
Treatment durations in studies for smoking cessation ranged from four to 11 weeks.
Advantages:
Available in multiple dosage forms, including oral tablets and once-weekly transdermal patch.
Disadvantages:
Possible side effects may include constipation, dizziness, drowsiness, dry mouth, postural hypotension (low blood pressure upon standing), sedation, and weakness.13 Can be considered for patients unable to take, or who are unsuccessful with, approved smoking cessation therapies (e.g., NRT, varenicline).
May enhance smoking cessation, but efficacy data are conflicting, and it is rarely used.
Do not stop abruptly, especially with higher doses or longer durations of therapy. Taper over two to four days to avoid discontinuation symptoms (e.g., agitation, confusion, rapid rise in blood pressure).
Nortriptyline Requires a prescription. Not FDA- or Health Canada-approved for smoking cessation.
(Pamelor[U.S.], Aventyl[Canada], generics)
MOA: noradrenergic effects may replace those of nicotine.
Begin nortriptyline about 10 to 28 days BEFORE quit date.
Start with 25 mg once daily.15Slowly titrate to a max total daily dose of 75 to 100 mg.
Usually taken for 12 weeks, but some continue therapy for up to six months.
Advantages:
May have similar efficacy compared to bupropion.15 Disadvantages:
Possible side effects may include rapid heart rate, blurry vision, dry mouth, constipation, trouble urinating, postural hypotension (low blood pressure upon standing), and QT prolongation.
Can be considered for patients unable to take or who are unsuccessful with approved smoking cessation therapies (e.g., NRT, varenicline).
Rarely used. May enhance smoking cessation, but efficacy data are conflicting.
Potential for QT prolongation should be considered, especially in patients with CV disease.
Do not stop abruptly.13-15Taper slowly to avoid flu-like symptoms, insomnia, etc.
Other Options Being Evaluated for Smoking Cessation
Cytisine (not available in the U.S.; available as a licensed natural health product [Cravv] in Canada)
Proposed MOA: a partial-agonist with a high affinity for the alpha-4-beta-2 nicotinic acetylcholine receptor, similar to varenicline.
Used for years in Europe, where it is available OTC.
Preliminary evidence shows promising abstinence rates when compared to placebo or NRT.
Naltrexone
Proposed MOA: opioid antagonist may reduce nicotine craving by reducing the activation of the mesolimbic dopamine.
To date, data show naltrexone does NOT improve smoking cessation rates compared to placebo.
Topiramate
Proposed MOA: not completely understood, but may involve weight loss effects, and effects on dopamine and serotonin.12 Preliminary evidence shows promising abstinence rates when compared to placebo.
E-cigarettes
Encourage use of other therapies with proven efficacy and safety over use of e-cigarettes for smoking cessation.1 The long-term safety of e-cigarettes is still unknown.1 E-cigarettes may expose patients to fewer and lower levels of toxic compounds compared to smoking cigarettes.1 If patients choose to use e-cigarettes as a method of smoking cessation, advise patients to switch completely and then wean off of e-cigarettes.1 Smoking even one cigarette a day may increase the risk of stroke and CV disease.21 For more information on the use of e-cigarettes, see our chart, E-cigarette and Vaping FAQs