Varenicline
CHANTIX
What it isPartial agonist at the alpha-4-beta-2 nicotinic receptor; smoking cessation.
Why this oneThe most effective single agent for quitting, because partial agonism both reduces craving and blunts the reward of smoking.
What limits itNausea is common and dose-related. Start one to two weeks before the quit date; renally adjusted.
FDA-approved for
- smoking cessation (2006)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Smoking cessation | Adults | 0.5 mg QD (days 1–3), then 0.5 mg BID (days 4–7) | 1 mg BID for 12 weeks (may add 12 more weeks) | 1 mg BID |
Titration Titrate over the first week before reaching 1 mg BID.
Renal Severe impairment (CrCl <30 mL/min): start 0.5 mg QD, titrate to 0.5 mg BID. ESRD on hemodialysis: max 0.5 mg QD.
Hepatic Undefined
Instructions
- Take after eating with a full glass of water
- Begin dosing 1 week before the quit date (or quit between days 8–35)
- Gradual-quit option: reduce smoking over 12 weeks, continue to 24 weeks total
Cautions
- Serious neuropsychiatric adverse events (mood changes, psychosis, suicidal ideation/behavior)
- Seizures (caution with history or lowered threshold)
- Increased effects of alcohol
- Accidental injury
- Cardiovascular events
- Somnambulism
- Angioedema and hypersensitivity reactions
- Serious (life-threatening) skin reactions
Adverse reactions
- Nausea
- Abnormal/vivid dreams
- Constipation
- Flatulence
- Vomiting
- Insomnia
Pregnancy No suggested increased risk of major birth defects vs. women who smoke; smoking itself carries fetal risk.
Lactation Undefined
NO BOXED WARNINGS
Principal riskNausea; vivid dreams
Cost, est. cash$5–$150/month
Generic entry2021
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityLocal irritation, sensitization or administration-site injury; negligible systemic toxicity at usual use.
Mechanism of action: Varenicline ballicule
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