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BUPROPION SR: SUMMARY Non-nicotine cessation aid Partial nicotinic receptor agonist Oral formulation VARENICLINE VARENICLINE:MECHANISM of ACTION Binds with high affinity and selectivity at 42 neuronal nicotinic acetylcholine receptors - Stimulates low-level agonist activity - Competitively inhibits binding of nicotine Clinical effects - symptoms of nicotine withdrawal - Blocks dopaminergic stimulation responsible for reinforcement & reward associated with smoking VARENICLINE :USE in PREGNANCY and LACTATION Category C drug Use only if potential benefit justifies potential risk Attempt nondrug treatment first Unknown if drug excreted in human breast milk Treatment Day Dose Day 1 to day 3 0.5 mg qd Initial dose titration Day 4 to day 7 0.5 mg bid Day 8 to end of treatment* 1 mg bid * Up to 12 weeks VARENICLINE: DOSING Patients should begin therapy 1 week PRIOR to their quit date

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