What are the oral medications and dosages for smoking cessation?

Oral Medications for Smoking Cessation

The two primary oral medications for smoking cessation are varenicline and bupropion, with varenicline being the most effective single pharmacotherapy option, increasing quit rates almost 3-fold compared to placebo. 1, 2

First-Line Oral Pharmacotherapy Options

Varenicline (Preferred)

Varenicline is recommended as the preferred oral medication due to superior efficacy compared to bupropion and single forms of nicotine replacement therapy. 2

Standard Dosing Regimen:

• Start 1-2 weeks before quit date 1, 3
• Days 1-3: 0.5 mg once daily 1, 3
• Days 4-7: 0.5 mg twice daily 1, 3
• Week 2-12: 1 mg twice daily (if tolerated) 1, 3
• Take after eating with a full glass of water 3

Treatment Duration:

• Standard course: 12 weeks 1, 2
• For successful quitters: Consider additional 12 weeks to increase long-term abstinence 1, 2, 3

Key Warnings and Contraindications:

• Nausea occurs in 30-40% of patients but is typically mild-to-moderate and diminishes over time 2
• Monitor for neuropsychiatric symptoms including depression and suicidal ideation, though recent large trials show no increased risk compared to placebo 1
• Contraindicated in patients with brain metastases due to seizure risk 1
• Dose adjustment for severe renal impairment: 0.5 mg once daily, titrate to maximum 0.5 mg twice daily 3

Bupropion (Alternative)

Bupropion is an effective alternative when varenicline is contraindicated or not tolerated, though less effective than varenicline. 1

Standard Dosing Regimen:

• Start 1-2 weeks before quit date 1
• Days 1-3: 150 mg once daily 1
• Day 4 through week 12: 150 mg twice daily (if tolerated) 1
• Maximum dose: 300 mg per day 1

Treatment Duration:

• Standard course: 7-12 weeks 1
• May extend to 6 months-1 year for continued cessation 1

Critical Contraindications:

• Seizure disorders or conditions increasing seizure risk (stroke, brain metastases) 1
• Concurrent MAO inhibitor use (increased hypertensive reaction risk) 1
• Concurrent tamoxifen use 1
• Closed-angle glaucoma 1
• Monitor for neuropsychiatric symptoms including depression and suicidal ideation 1

Clinical Implementation Algorithm

Initial Assessment:

1. Screen for contraindications to varenicline (brain metastases, severe renal impairment) 1, 3
2. Screen for contraindications to bupropion (seizure risk, MAO inhibitors, tamoxifen, glaucoma) 1
3. Assess psychiatric history for both medications 1

Treatment Selection:

• First choice: Varenicline unless contraindicated 2
• Second choice: Bupropion if varenicline contraindicated or not tolerated 1
• Consider combining bupropion with nicotine replacement therapy for enhanced efficacy 1

Follow-Up Schedule:

• First visit: Within 2-3 weeks of starting medication to assess side effects and smoking status 1, 2
• Subsequent visits: At minimum 12-week intervals during therapy 1
• Post-treatment follow-up recommended 1

Management of Treatment Failure:

• If patient continues smoking or relapses: Consider switching to the alternative oral medication or intensifying behavioral therapy 1, 2
• If reduction efforts stall: Switch to different pharmacotherapy 1
• Encourage continued therapy through brief slips as withdrawal symptoms peak within 1-2 weeks then subside 1

Critical Clinical Pearls

Behavioral counseling is essential and significantly improves outcomes when combined with pharmacotherapy. 2 Provide 4 or more counseling sessions during the 12-week treatment course, with sessions lasting 10-30+ minutes. 2

The neuropsychiatric safety concerns with both varenicline and bupropion have been largely refuted by a large multicenter RCT (n=8,058) showing no increased rates of neuropsychiatric adverse events compared to nicotine patches or placebo in patients with or without psychiatric disorders. 1

Side effects from these medications are minimal and acceptable compared to the risks of continued smoking. 1 Serious side effects are extremely rare. 1

For patients unable to quit abruptly, consider a gradual reduction approach with varenicline: reduce smoking by 50% within first 4 weeks, another 50% in next 4 weeks, with complete abstinence by 12 weeks, followed by additional 12 weeks of treatment (24 weeks total). 3