II. Indications

  1. Tobacco Cessation
  2. Not considered first-line therapy in teens who use Tobacco
  3. Decreases Alcohol consumption (consider for Tobacco Cessation in comorbid Alcohol Abuse)
    1. Decreases intake by 1 drink daily and 20% fewer heavy drinking days
    2. Mitchell (2012) Psychopharmacology 223(3):299-306 [PubMed]

III. Precautions

  1. FDA Pregnancy Category C
  2. Increased cardiovascular events in Tobacco users with history of cardiovascular disease
    1. http://www.fda.gov/Drugs/DrugSafety/ucm259161.htm
  3. Avoid combination with other Tobacco Cessation medications
    1. Do not use with Nicotine Replacement
    2. Safety in combination with Bupropion is unknown
      1. However, both agents increase risk of Seizures
  4. FDA black box warning was removed in 2017 (but still be aware of potential risk)
    1. Serious neuropsychiatric symptoms
    2. May cause depressed mood and Suicidality
    3. May cause behavior change including hostility, agitation (especially with Alcohol)

IV. Mechanism

  1. Nicotine binds nicotinic acetylcholine receptor a4b2
    1. Binding stimulates CNS mesolimbic Dopamine system
    2. Reinforces nicotine exposure
  2. Chantix activity
    1. Chantix Blocks nicotine at a4b2 receptors
    2. Chantix selectively binds a4b2 receptors

V. Dosing

  1. Start: 0.5 mg once daily on days 1 to 3
  2. Next: 0.5 mg twice daily on days 4 to 7
  3. Next: 1 mg twice daily
  4. Duration
    1. Set quit date at 1-5 weeks after starting Chantix (consider quitting at 12 weeks)
    2. Continue for 12 weeks
    3. Additional 12 weeks may be used if successful
      1. Higher abstinence rates with delaying quit date to 12 weeks and continuing Chantix for 24 weeks
      2. Ebbert (2015) JAMA 313(7):687-94 +PMID:25688780 [PubMed]
  5. Dosing adjustment: Renal Impairment
    1. Severe renal Impairment: Max dose 0.5 mg PO bid
    2. End-stage renal disease: Max dose 0.5 mg PO daily

VI. Adverse Effects

  1. See precautions above
  2. Nausea (30%)
  3. Headache (10%)
  4. Sleep disturbance (Insomnia, or abnormal dreams): 10%
  5. Constipation
  6. Flatulence
  7. Seizure
    1. Typically at 2-3 weeks after starting Chantix
  8. Suicidal Ideation
    1. Reported in 1 per 10,000 patients taking Chantix
    2. Kuehn (2008) JAMA 299(10):1121-2 [PubMed]

VII. Drug Interactions

  1. Alcohol
    1. Increases risk of Intoxication, hostility, aggressive, amnesia behavior

VIII. Cost

  1. Monthly: $120

IX. Efficacy

  1. Cessation for >1 year in 20% (10% with Placebo)
  2. Cessation rates are as good if not better than Zyban
  3. Number Needed to Treat (for longterm cessation): 9
  4. More effective when combined with Nicotine Replacement
    1. Koegelenberg (2014) JAMA 312(2): 155-61 [PubMed]

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Cost: Medications

chantix (on 6/1/2016 at Medicaid.Gov Survey of pharmacy drug pricing)
CHANTIX 0.5 MG TABLET $5.45 each
CHANTIX 1 MG CONT MONTH BOX $5.33 each
CHANTIX 1 MG TABLET $5.33 each
CHANTIX STARTING MONTH BOX $5.74 each

Ontology: varenicline (C1569608)

Definition (NCI_NCI-GLOSS) A drug used to help people stop smoking by acting the same way nicotine acts in the brain. It is a type of nicotine receptor partial agonist.
Definition (NCI) A partial agonist of the nicotinic acetylcholine receptor (nAChR) subtype alpha4beta2. Nicotine stimulation of central alpha4beta2 nAChRs located at presynaptic terminals in the nucleus accumbens causes the release of the neurotransmitter dopamine, which may be associated with the experience of pleasure; nicotine addiction constitutes a physiologic dependence related to this dopaminergic reward system. As an AChR partial agonist, varenicline attenuates the craving and withdrawal symptoms that occur with abstinence from nicotine but is not habit-forming itself.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C500838
SnomedCT 420507002, 421772003
English Varenicline, Varenicline (product), Varenicline (substance), 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine (2R,3R)-2,3-dihydroxybutqanedioate, varenicline [Chemical/Ingredient], cns stimulants varenicline, varenicline (medication), VARENICLINE, varenicline, 6,7,8,9-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)benzazepine
Spanish vareniclina (sustancia), vareniclina, vareniclina (producto)

Ontology: Chantix (C1712042)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C500838
English Chantix