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NERVOUS SYSTEM › OTHER NERVOUS SYSTEM DRUGS › DRUGS USED IN ADDICTIVE DISORDERS › Drugs used in nicotine dependence
varenicline
N07BA03
Forms & Strengths
- Oral tablet: 0.5 mg
- Oral tablet: 1 mg
- Oral titration pack: 0.5 mg (11 tabs) and 1 mg (42 tabs)
Adult Dosing
- Days 1-3: 0.5 mg orally once daily
- Days 4-7: 0.5 mg orally twice daily
- Day 8 to end of treatment (12 weeks): 1 mg orally twice daily
- Consider additional 12 weeks of treatment for successful quitters to maintain abstinence
Pediatric Dosing
- Safety and efficacy not established in pediatric patients <18 years
Indications
- Smoking cessation aid in adults
Mechanism of Action
- Selective alpha-4 beta-2 nicotinic acetylcholine receptor partial agonist
- Reduces symptoms of nicotine withdrawal by stimulating the receptor (agonist effect)
- Reduces the rewarding effects of nicotine by competitively binding to the receptor (antagonist effect)
Contraindications
- Hypersensitivity to varenicline or any component of the formulation
- History of serious hypersensitivity reactions or skin reactions (e.g., Stevens-Johnson syndrome)
Adverse Reactions
- Nausea (most common)
- Insomnia
- Abnormal dreams
- Headache
- Nasopharyngitis
- Serious neuropsychiatric events (depression, suicidal ideation)
Drug Interactions
- Nicotine replacement therapy: Increased risk of adverse events such as nausea and dizziness
- Alcohol: May increase intoxication effects or exacerbate neuropsychiatric adverse events
- Cimetidine: May increase systemic exposure of varenicline via renal clearance inhibition
Curated Content: Needs Vetting Before Put to Clinical Use