for Health Care Providers
Table 1: VHA Formulary Choices for Pharmacotherapy of Smoking Cessation
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| * Remove nicotine patch at bedtime. # High dependence: in general, >20 cigarettes per day or use of first cigarette within 30 minutes of awakening. § All NRTs have been shown to double 6- to 12-month abstinence rates compared with placebo. ** Cost based on FSS or BIG4 pricing as listed on PBM website . Note: Two additional prescription products, a nicotine inhaler and nicotine nasal spray, are FDA approved for NRT; however, these products are not available on the VHA National Formulary. For more information on these products, visit the American Lung Association Smoking Cessation Support | |||||
| Bupropion | Nicotine Transdermal Patch | Nicotine Polacrilex Gum | Nicotine Polacrilex Lozenge | Varenicline | |
| Formulations | Bupropion SR 150 mg, 300 mg Bupropion IR 100 mg | (Nicoderm/Habitrol) 21 mg, 14 mg, 7 mg (Nicotrol) 15 mg, 10 mg, 5 mg | 2 mg, 4 mg | 2 mg, 4 mg | 0.5 mg, 1 mg |
| Start instructions | 1-2 weeks before quit date | On quit date | 1 week before quit date | ||
| Recommended regimen | Bupropion SR 150 mg QD for 3 days, then 150 mg BID (8 hours apart) Reduce dosage for patients with cirrhosis: 150 mg QOD Bupropion IR 100 mg QD for 3 days, then 100 mg TID; reduce dosage for patients with cirrhosis: 75 mg QD | High dependence# Low dependence 14 mg for 6-8 weeks, then 7 mg for 2 weeks | High dependence# Low dependence 2 mg Q1-2H for 6 weeks, then Q2-4H for 3 weeks, then Q4-6H for 3 weeks Maximum: 24 pieces/24 hours | High dependence# Low dependence 2 mg Suck 1 lozenge Q1-2H for 6 weeks, then 1 lozenge Q2-4H for 3 weeks, then 1 lozenge Q4-8H for 3 weeks Maximum: 20 lozenges/24 hours or 5 lozenges/6 hours | Initial: 0.5 mg QD on days 1-3, then 0.5 mg BID on days 4-7, then 1 mg BID for total duration of 12 weeks Reduce dosage for CrCl <30: maximum dosage 0.5 mg BID; end-stage renal disease or hemodialysis: 0.5 mg QD |
| Administration comments | Start 1-2 weeks before quitting smoking (to achieve steady-state levels) Continue treatment for 8-12 weeks (if no progress is made by week 8, consider discontinuing therapy) If insomnia, take evening dose in afternoon | Usually worn 16-24 hours; remove overnight Apply between neck and waist Rotate sites Takes 2-3 days for effect after application of first patch | Chew slowly (about 10 chews) until peppery taste is released, then "park" between teeth and gums until flavor dissipates; repeat process on and off for 30 minutes per piece Has been studied in combination with patch | Allow lozenge to dissolve slowly over course of 20-30 minutes, shifting in mouth occasionally Do not chew or swallow (increased risk of GI side effects) Avoid acidic beverages within 15 minutes of use (eg, citrus juices, soft drinks); these decrease absorption | Screen for suicide and violence risk before starting, and monitor before prescribing renewals Start 1 week before quit date Take drug after eating and with 8 oz of water Instruct patient or caregiver to report depression, suicidal ideation, unusual changes in behavior, or worsening of preexisting psychiatric illness An additional 12 weeks of treatment in patients who have successfully stopped smoking may increase likelihood of long-term abstinence |
| 1-year abstinence rates§ | 10-30% (up to 35% when combined with patch) | 16-30% (dose dependent); high-dose patch: 30% | 20-30% | 15-20% | 18.5-23% (12-week course) vs 4-10% with placebo 43.6% (with additional 12-week course) vs 37% with placebo |
| ARV interactions | Metabolized by the cytochrome P450 system; EFV and TPV may ↓ bupropion levels 40-50%; when using with these ARVs, monitor for depression and titrate to clinical effect; RTV may ↑ bupropion levels | None | Does not interact with the cytochrome P450 system; no ARV interactions identified to date | ||
| Time to peak blood concentrations | 3 hours (half life = 21 hours) | 4-10 hours | 15-30 minutes | No data | 3-4 hours |
| Absorption | 20% | 75-90% | 30% | 30% | High; virtually complete absorption |
| Advantages (+) Disadvantages (-) | (+) Good adherence; ease of use; can be combined with patch; consistent rate of exposure; helps with withdrawal symptoms (-) Many drug interactions resulting from metabolism by CYP 2B6; CNS side effects; must be adjusted for hepatic insufficiency; increased risk of seizures | (+) Best adherence; easy to use; consistent rate of exposure; unobtrusive (-) Less effective than gum for cravings; difficult to control titration; absorption increased at elevated temperatures; should abstain from smoking while using NRT | (+) Helps prevent sudden urges; can titrate to adjust for cravings; oral substitute for cigarettes; slow release of nicotine reduces addiction potential (-) Difficult for those with poor dentition or dentures; must learn proper chewing technique; should abstain from smoking while using NRT; must abstain from drinking/eating during gum use; swallowing nicotine causes GI side effects (hiccups, diarrhea or constipation, flatulence, belching) | (+) Easy to use; discreet; higher immediate levels; can titrate to adjust for cravings; reduces self-reported withdrawal symptoms (-) Must abstain from drinking/eating during lozenge use; should abstain from smoking while using NRT | (+) Good adherence; ease of use; consistent rate of exposure; higher rate of abstinence compared with bupropion and placebo (-) Potential for serious neuropsychiatric side effects, particularly in patients with underlying psychiatric disease or violence risk; dosage adjust for renal insufficiency (CrCl <30); high incidence of nausea; not studied in patients with underlying mental illness |
| Adverse effects | Anxiety Disturbed concentration Dizziness Insomnia Constipation Dry mouth Nausea Seizures (risk: 1:1,000) | Sleep disturbances Local skin irritation Bone pain Headache Nausea | Local mouth irritation Jaw pain Hiccups Dyspepsia Rhinitis Nausea | Local mouth irritation/tingling Heartburn, indigestion, nausea (if chewed) Headache Nausea, diarrhea Flatulence | Dream disorders Headache Insomnia Abnormal behavior Agitation Depressed mood Suicidal thoughts Constipation Flatulence Nausea, vomiting Consider dosage reduction for patients sensitive to adverse effects (eg, nausea, headache, insomnia) |
| VHA National Formulary restrictions | None | None | None | Restricted to patients who cannot tolerate gum (eg, dentures, missing teeth, TMJ, previous head or neck surgery) | Must meet criteria for use Restricted to patients without active mental health disorders or with clinically stable mental health disorders who have had >1 relapse on NRT or bupropion |
| VHA cost** and average cost per day based on above regimens | SR: $0.48/tablet $0.96/day IR: $0.28/tablet $0.84/day | 14 mg patches: $2.50/patch $2.50/day | 2 mg gum: $12.62/50 pieces $20.12/110 pieces $0.18-$0.25/piece $2.20-$6/day 4 mg gum: $13.70/50 pieces $25.69/110 pieces $0.23-$0.27/piece $2-$6.50/day | 2 mg or 4 mg lozenge: $29.45/72 lozenges $0.41/lozenge $5-8/day | 0.5 mg and 1mg tablets: $1.17/tablet $2.34/day |
| Contraindications and relative contraindications | Contraindications: History of seizures Predisposition to seizures (eg, severe head trauma, CNS tumor, cirrhosis) Abrupt withdrawal from heavy, daily alcohol or other sedative MAO inhibitor within 14 days Bulimia, anorexia nervosa Relative contraindications: Hypersensitivity Pregnancy category B | Relative contraindications: Hypersensitivity Pregnancy category D Use within 14 days post MI, or in patients with serious or worsening angina Patients should be advised not to smoke while on NRT | Relative contraindications: Serious neuropsychiatric disorders (including suicidal and homicidal ideation) History of suicidal, homicidal, or assaultive behavior in the past 12 weeks Untreated or unstable mental disorder such as psychotic disorder, bipolar disorder, major depressive disorder, and PTSD Severe renal impairment Pregnancy category C | ||
| Comments | Use with caution in patients with liver, kidney failure Avoid in patients on MAO inhibitors | In combination with behavioral program, patch doubles the quit rate Durability of cessation is better with 21 mg patches than with 14 or 7 mg patches Using the 21 mg patch yields roughly 40-50% the plasma nicotine levels of smoking 1.5 packs per day | In combination with an intensive behavioral program, nicotine gum can double the quit rate Using 2 mg ad lib yields roughly 40% plasma nicotine levels of smoking 1 pack per day | In combination with an intensive behavioral program, nicotine lozenges can increase the quit rate | Not first-line therapy for smoking cessation Ask patients about any psychiatric history before prescribing varenicline,as above Monitor for signs/symptoms of psychiatric illness during use Monitor serum creatinine levels; as renal function decreases (as seen in elderly patients), dosage reductions may be necessary |
.From Smoking Cessation
Primary Care of Veterans with HIV
Office of Clinical Public Health Programs
Veterans Health Administration, 2009
