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. 2022 Jun 1;50(Suppl):77–138.

Table 4.

Dosage guidelines, safety aspects and other clinical considerations for Varenicline and Bupropion

Varenicline Bupropion
Formats 1st week of treatment: 0.5 mg tablet
Rest of treatment period: 1 mg tablet
Follow-up: 1 mg 150 mg extended-release tablets
150 mg sustained release tablets
Dosage Days 1–3: 0.5 mg /24 h
Days 4–7: 0.5 mg /12 h
Stop smoking between days 7 and 10
Day 8–12 weeks: 1 mg/12 h
Start: 1 week before stopping
Take with water after eating
Dose adjustment in patients with renal insufficiency
Duration: 12 weeks, with possible extension of 12 weeks
Possible start 1 month before D-day with a weekly reduction regimen
Days 1-6: 150 mg/24 h
Day 7 and following: 150 mg twice a day with at least 8 hours between doses and not close to bedtime
Stop smoking during the 2nd week of treatment
Duration:7-9 weeks
Precautions Adjust dose for kidney failure (clearance
< 30 mL/min consider half the dose)
Contraindicated in end-stage renal failure, pregnancy and lactation
Drugs that lower the proconvulsive threshold
Liver disease
Adolescents
Pregnancy and lactation
Contraindications History of seizures
Eating disorders
Sudden interruption of alcohol or benzodiazepine consumption (risk of seizure)
Use of MAOIs in the previous 2 weeks.
Side effects (most common) Nausea, headache, insomnia, nasopharyngitis, gastrointestinal disorders Nausea, headache, insomnia, dry mouth, anxiety, gastrointestinal disorder s and seizures
Advantages Most effective drug in monotherapy
Two daily doses and good adherence
Different mechanism of action in second treatments
Absence of hepatic metabolism.
Lower risk of interactions
Good adherence
Less weight gain
Useful in patients with depression
Possible combination with NRT
Disadvantages Seizure risk