Pharmacology

According to the CDC, use of cessation medications is appropriate for most adult smokers, with the exception of pregnant women, light smokers (i.e., persons who smoke fewer than 5 to 10 cigarettes daily), and persons with specific medical contraindications (e.g., seizure disorders). Nicotine replacement therapy, bupropion (an atypical antidepressant), and varenicline (a selective nicotine receptor partial agonist) are first-line pharmacologic therapies to assist with smoking cessation recommended by the U.S. Department of Health and Human Services.

A 2014 summary of 12 Cochrane reviews found higher abstinence rates with nicotine-replacement therapies (17.6%) and bupropion (19.1%), compared with placebo (10.6%). Varenicline (27.6%) and combination nicotine-replacement therapies (e.g., longer-acting patch plus short-acting inhaler, 31.5%) were most effective for achieving smoking cessation. The analysis found that none of the therapies was associated with an increased rate of serious adverse events.

Pharmacotherapy for the Treatment of Tobacco Dependence

Abbreviations: OTC: over-the-counter; Rx: prescription; SR: sustained-release

 Drug

 Formulation(s)

 Adult Dosage

 Nicotinic Receptor Agonists (Nicotine-Replacement Therapy)

 Transdermal nicotine patches (OTC)

NicoDerm CQ, generics

 Patch delivering 7, 14, or 21 mg per 24 hours

 >10 cigarettes/day:

  • One 21-mg patch/day X 6 weeks
  • One 14-mg patch/day X 2 weeks
  • One 7-mg patch/day X 2 weeks

 <10 cigarettes/day (or <45 kg)

  • One 14-mg patch/day X 6 weeks
  • One 7-mg patch/day X 2 weeks

 Intranasal nicotine spray (Rx)

Nicotrol NS

 10-mL bottles containing 10 mg/mL solution

 Each 50 microliter spray contains 0.5 mg of nicotine. One dose is 1 mg of nicotine (2 sprays, one in each nostril).

  • Start with 1 or 2 doses per hour, which may be increased up to a maximum recommended dose of 40 mg (i.e., 80 sprays, which is somewhat less than 1/2 bottle) per day (maximum duration of therapy 3 months)

Nicotine oral inhaler (Rx)

Nicotrol Inhaler

 10-mg cartridges

  • 6 to 12 cartridges per day X 6–12 weeks
  • Gradual taper (if necessary) over next 6–12 weeks

Nicotine polacrilex gum (OTC)

Nicorette Gum generics

 2 or 4 mg per piece of gum

Smokes within 30 minutes of waking up:

  • 4-mg gum, one piece every 1 to 2 hours X 6 weeks
  • 4-mg gum, one piece every 2 to 4 hours X 3 weeks
  • 4-mg gum, one piece every 4 to 8 hours X 3 weeks

Smokes after 30 minutes of waking up:

  • 2-mg gum, one piece every 1 to 2 hours X 6 weeks
  • 2-mg gum, one piece every 2 to 4 hours X 3 weeks
  • 2-mg gum, one piece every 4 to 8 hours X 3 weeks

Nicotine polacrilex lozenges (OTC)

Nicorette Lozenges,generics
Nicorette Mini Lozenges,generics

 2 or 4 mg per lozenge or mini lozenge

Smokes within 30 minutes of waking up:

  • One 4-mg lozenge/mini lozenge every 1 to 2 hours X 6 weeks
  • One 4-mg lozenge/mini lozenge every 2 to 4 hours X 3 weeks
  • One 4-mg lozenge/mini lozenge every 4 to 8 hours X 3 weeks

Smokes after 30 minutes of waking up:

  • One 2-mg lozenge/mini lozenge every 1 to 2 hours X 6 weeks
  • One 2-mg lozenge/mini lozenge every 2 to 4 hours X 3 weeks
  • One 2-mg lozenge/mini lozenge every 4 to 8 hours X 3 weeks

 Dopaminergic-Noradrenergic Reuptake Inhibitor

Bupropion SR (Rx)

Zyban, generics

 150 mg tablets

Treatment should be initiated before the planned quit day, while the patient is still smoking, because it takes approximately 1 week of treatment to achieve steady-state blood levels of bupropion. The patient should set a “target quit date” within the first 2 weeks of treatment with the drug.

  • Begin dosing with one 150-mg tablet per day for 3 days.
  • Increase dose to 300 mg per day given as one 150-mg tablet twice each day with an interval of at least 8 hours between each dose.
  • Do not exceed 300 mg per day

Nicotinic Receptor Partial Agonist

Varenicline tartrate (Rx)

Chantix

 0.5 or 1 mg tablets

Treatment should be initiated before the planned quit day, while the patient is still smoking. The patient should set a date to stop smoking and begin varenicline dosing one week before this date.

  • Begin dosing with 0.5 mg once daily for 3 days. 
  • Days 4 to 7, increase dose to 0.5 mg twice daily.
  • From day 8 through the end of treatment, dosage is 1 mg twice daily

 Abbreviations: OTC: over-the-counter; Rx: prescription; SR: sustained-release

Learn more about ADA Smoking and Tobacco Cessation.