Smoking Cess

Question 1

Bupropion SR: MOA & Clinical Effects

Answer 1

Sustained-release antidepressant used as a non-nicotine aid for smoking cessation

• Noncompetitive antagonist of nicotinic acetylcholine receptors
• Inhibits uptake of NE and DA
  
  • May contribute to antidepressant effect as well as effectiveness in smoking cessation

Clinical effects:

• Decreases cravings for cigarettes
• Decreases symptoms of nicotine withdrawal

Question 2

Bupropion: dosing

(A) Dose titration

(B) Duration of therapy

© Can it be used with NRTs?

(d) By when should the patient start progressing towards abstinence?

Answer 2

(A) Dose titration

• Dose titration
  
  • Start 150 mg PO daily x 3 days
  • Then increase to 150 mg PO BID
    
    • Up-titration reduces risk of seizures

(B) Duration of therapy

• Duration of therapy
  
  • 7 – 12 weeks recommended
  • Can be taken for 12 months if appropriate
• Patient should begin therapy 1 to 2 weeks PRIOR to their quit date to ensure that therapeutic plasma levels of the drug are achieved

c)

• Can be used with or without NRT
• week 7, if not:
  
  • ​​Therapy unlikely to be effective
    
    • Discontinue treatment
    • Reevaluate and restart at a later date
• Dose tapering is not required when stopping

Question 3

Bupropion:

(a) side effects
b) Precautions
c) Contraindications
d) Black box warning

Answer 3

• COMMON SIDE EFFECTS:
  
  • Insomnia
  • Dry mouth
  • Dizziness
  • Anxiety
• LESS COMMON SIDE EFFECTS:
  
  • CNS effects (tremors)
  • Skin rash
• PRECAUTIONS:
  
  • Seizure risk
  • Concurrent medications that lower seizure threshold
  • Uncontrolled hypertension
  • Psychosis
  • Angle-closure glaucoma
  • Severe hepatic cirrhosis
• CONTRAINDICATIONS:
  
  • Seizure disorders
  • Current/prior anorexia or bulimia nervosa
  • Patients undergoing abrupt discontinuation of alcohol or sedatives
  • Patients taking MAOI’s within 14 days (phenelzine)
• BLACK BOX WARNING:
  
  • Suicidal thoughts and behaviors
  • Not recommended in pregnant or breastfeeding

Question 4

Bupropion:

Advantages and disadvantages

Answer 4

• ADVANTAGES:
  
  • Oral formulation
  • Aids with withdrawal symptoms and cravings
  • Added benefit if history of depression
  • No risk of nicotine poisoning
  • Can be used with NRT
• DISADVANTAGES:
  
  • Seizure risk
  • Contraindications and precautions

Question 5

Varenicline (Chantix) :MOA & Clinical effects

Answer 5

MOA:

• Partial agonist selective for alpha 4 beta 2 nicotinic acetylcholine receptor
• Prevents binding of nicotine to receptor

Clinical effects

• Decrease symptoms of nicotine withdrawal
• Blocks effects of nicotine if patient resumes smoking
• Breaks dopamine reward cycle from smoking

Question 6

Varenicline: Dosing

Answer 6

• Patient should begin therapy 1 week PRIOR to their quit date to minimize treatment-related nausea and insomnia
  
  • Day 1 - 3: 0.5mg qd
  • Day 4 - 7: 0.5 mg bid
  • Day 8 to end of treatment: 1 mg bid
• Do NOT use with NRT and take after eating with a full glass of water
• Dosing strategies:
  
  • general quit approach
    
    • Start Chantix and reduce smoking by 50% within first 4 weeks
    • Reduce smoking by an additional 50% in next 4 weeks
    • Continue reducing with the goal of complete abstinence by week 12
    • Continue treatment for additional 12 weeks after abstinence

Question 7

Varenicline: Side effects, precautions, contraindications, black box warning

Answer 7

• SIDE EFFECTS:
  
  • Nausea
  • Sleep disturbances
  • Constipation
  • Flatulence
  • Vomiting
• PRECAUTIONS:
  
  • Alcohol consumption
  • Cardiovascular events
  • Psychiatric illness
  • Renal impairment
• CONTRAINDICATIONS:
  
  • Hypersensitivity to varenicline
• BLACK BOX WARNING
  
  • None
• PREGNANCY
  
  • Limited information, use only if beneficial
    
    • No data on breast milk

Question 8

Varenicline: Advantages & disadvantages

Answer 8

• ADVANTAGES
  
  • Oral formulation
  • Decreases withdrawal symptoms
  • Novel mechanism of action
• DISADVANTAGES
  
  • No generic available
  • High incidence of nausea
  • Cannot take with NRT
  • Possible cardiovascular concerns

Question 9

Clonidine: MOA

Answer 9

• Central acting alpha 2-adrenergic agonist
• Reduces sympathetic outflow from CNS

Question 10

Clonidine: Dosing

Answer 10

• Dosing:
  
  • Oral dosing
    
    • Range: 0.15 to 0.75 mg/day
    • Start: 0.1 mg BID
  • Transdermal dosing
    
    • Range: 0.1 to 0.3 mg/day
    • Start: 0.1 mg patch
  • Titrate by 0.1 mg/day per week as tolerated
  • Duration of therapy has varied across trials
    
    • 3 – 10 weeks

Question 11

Clonidine: Side effects & precautions

Answer 11

• SIDE EFFECTS:
  
  • Dry mouth
  • Drowsiness
  • Dizziness
  • Sedation
  • Constipation
  • Decreased blood pressure
• PRECAUTIONS:
  
  • Rebound hypertension (taper dose)
  • Reduced ventricular function
  • Slow heart rate
  • AV node conduction issues
  • Pregnancy category C

Question 12

Nortriptyline: MOA

Answer 12

Tricyclic antidepressant

Question 13

Nortriptyline: Dosing

Answer 13

• Range: 75 – 100 mg/day
• Start 25 mg QHS
• Duration of therapy:
  
  • 6 – 14 weeks
  • Most trials gradually tapered the dose over an additional 1 – 2 weeks
• Start prior to quit date to achieve steady-state

Question 14

Nortriptyline: side effects & precautions

Answer 14

• SIDE EFFECTS:
  
  • Sedation
  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Lightheadedness
  • Tremor
• PRECAUTIONS:
  
  • Risk of arrhythmias and postural hypotension
  • Pregnancy category D