Pharmacotherapy
Note: Combining behavioral therapy with pharmacotherapy is significantly more effective than either alone.
- First-Line Agents:
- Varenicline:
- MOA: α4β2 nicotinic acetylcholine receptor partial agonist; reduces craving and withdrawal while blocking nicotine binding.
- Efficacy: Most effective monotherapy for smoking cessation.
- Adverse Effects: Nausea, insomnia, vivid/abnormal dreams.
- Clinical Pearl: Black box warning for neuropsychiatric events removed by FDA; safe in stable psychiatric pts, but monitor for mood changes/suicidality.
- Bupropion SR:
- MOA: Norepinephrine-dopamine reuptake inhibitor (NDRI).
- Key Benefits: Minimizes post-cessation weight gain; excellent for pts with co-morbid major depressive disorder (MDD).
- Contraindications:
- Seizure disorders (lowers seizure threshold).
- Current or prior diagnosis of bulimia or anorexia nervosa.
- Abrupt withdrawal from alcohol, benzodiazepines, or barbiturates.
- Use of MAO inhibitors within 14 days.
- Adverse Effects: Insomnia, dry mouth, headache, agitation.
- Nicotine Replacement Therapy (NRT):
- Options: Transdermal patch (long-acting); gum, lozenge, nasal spray, inhaler (short-acting).
- Combination NRT (e.g., patch + gum/lozenge) is superior to monotherapy NRT and roughly equal in efficacy to varenicline.
- Precautions: Caution in acute coronary syndrome (<2 weeks post-MI), serious arrhythmias, or severe angina.
- Varenicline:
- Second-Line Agents (used if first-line fails, contraindicated, or unavailable):
- Nortriptyline (TCA).
- Clonidine (α2-adrenergic agonist).