Indicated as an aid to smoking cessation treatment in adults.
Partial agonist activity at the alpha4beta2 nicotinic acetylcholine receptor that competitively blocks the receptor and only partially activates it.
The receptor mediates nicotine dependence and releases dopamine: varenicline reduces nicotine withdrawal symptoms and blocks nicotine inhaled in cigarette smoke from binding to the receptor reducing the rewarding effects of cigarettes smoked.
Penetrates the CNS.
It reduces nicotine withdrawal symptoms and blocks nicotine inhaled in cigarette smoke from binding to the receptor, reducing the rewarding effects of cigarettes smoked.
Binds to the receptor and leads to partial stimulation of the receptor mediated release of dopamine in the reward center and competitively inhibits binding of the receptor by cigarette nicotine and suppresses the symptoms of nicotine withdrawal.
Reduces cigarette smoke pharmacological reward.
May be associated with behavior changes including depression, hostility, aggression, suicidal ideology, and suicide.
May increase the risk of serious neuropsychiatric or cardiovascular events.
Used in dosage increasing from 0.5-1 mg/day for one week before the target quit date to generate sufficient systemic levels and to habituate users to the possible occurrence of nausea and therefore in doses of 2 mg/day for up to six months.
Effective at 2mg/d for 12 weeks.
Meta-analyses show that pooled risk ratio for continuous abstinence at six months or longer for varenicline at 2 mg/d vs placebo is 2.7.
At 3 mg/d of varenicline there is limited adverse events and high success rates in patients that failed 2mg/d.(Jimenez-Ruiz CA et al).
Alleviates smoking withdrawal discomfort and urges to smoke after smoking sensation.
For tobacco dependent adults for whom treatment is initiated, varenicline is recommended over nicotine patches, bupropion, and E-cigarettes.
Foes not have excess neuropsychiatric events and compared with bupropion and NRT, or placebo.