II. Indications
- Tobacco Cessation
- Not considered first-line therapy in teens who use Tobacco
- Decreases Alcohol consumption (consider for Tobacco Cessation in comorbid Alcohol Abuse)
- Decreases intake by 1 drink daily and 20% fewer heavy drinking days
- Mitchell (2012) Psychopharmacology 223(3):299-306 [PubMed]
III. Precautions
- FDA Pregnancy Category C
- Increased cardiovascular events in Tobacco users with history of cardiovascular disease
- May be used in combination with Nicotine Replacement
- Previously, combined Nicotine Replacement AND Chantix was contraindicated
- Combined Verenicline with Nicotine Replacement is more effective than either alone without increased adverse effects
- Avoid combination with Bupropion
- FDA black box warning was removed in 2017 (but still be aware of potential risk)
- Serious neuropsychiatric symptoms
- May cause depressed mood and Suicidality
- May cause behavior change including hostility, Agitation (especially with Alcohol)
IV. Mechanism
- Nicotine binds Nicotinic Acetylcholine Receptor a4b2
- Chantix activity
- Chantix Blocks Nicotine at a4b2 receptors
- Chantix selectively binds a4b2 receptors
V. Dosing
- Start: 0.5 mg once daily on days 1 to 3
- Next: 0.5 mg twice daily on days 4 to 7
- Next: 1 mg twice daily
- Duration
- Set quit date at 1-5 weeks after starting Chantix
- Continue for 12 weeks
- Additional 12 weeks may be used if successful (but mixed data)
- One study: Higher abstinence rates with delaying quit date to 12 weeks and continuing Chantix for 24 weeks
- One study: No benefit to use longer than 12 weeks
- Dosing adjustment: Renal Impairment
- Severe renal Impairment: Max dose 0.5 mg orally twice daily
- End-stage renal disease: Max dose 0.5 mg orally daily
VI. Adverse Effects
- See precautions above
- Nausea (30%)
- Headache (10%)
- Sleep disturbance (Insomnia, or abnormal dreams): 10%
- Constipation
- Flatulence
-
Seizure
- Typically at 2-3 weeks after starting Chantix
-
Suicidal Ideation
- Reported in 1 per 10,000 patients taking Chantix
- Kuehn (2008) JAMA 299(10):1121-2 [PubMed]
VII. Drug Interactions
-
Alcohol
- Increases risk of Intoxication, hostility, aggressive, Amnesia behavior
VIII. Efficacy
- Cessation for >1 year in 20% (10% with Placebo)
- Cessation rates are as good if not better than Zyban
- ATS preferred agent
- Sustained Smoking Cessation at 6 months (NNT 7)
- More effective when combined with Nicotine Replacement
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Related Studies
chantix (on 1/1/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
CHANTIX 1 MG CONT MONTH BOX | Generic | $5.87 each |
CHANTIX 1 MG TABLET | Generic | $5.87 each |
CHANTIX STARTING MONTH BOX | Generic | $6.28 each |
varenicline (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
VARENICLINE 0.5 MG TABLET | Generic | $5.80 each |
VARENICLINE 1 MG CONT MONTH BX | Generic | $4.48 each |
VARENICLINE 1 MG TABLET | Generic | $5.87 each |
VARENICLINE STARTING MONTH BOX | Generic | $6.28 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 |