As an aid to smoking cessation treatment
#仿單變更2021
藥理
Varenicline binds with high affinity and selectivity at α4β2 neuronal nicotinic acetylcholine receptors. This binding produces agonist activity at a sub-type of the nicotinic receptor, but at a significantly lower level than nicotine. Varenicline also prevents nicotine binding to α4β2 receptors, which prevents stimulation of the central nervous mesolimbic dopamine system.
藥動學
High bioavailability; protein binding: <20%; Varenicline undergoes minimal metabolism with 92% excreted unchanged in the urine. Elimination half-life:~24 hour
禁忌症
Hypersensitivity to the active substance or to any excipients.
initial, 0.5 mg ORALLY once daily for days 1 through 3, then 0.5 mg twice daily for days 4 through 7, then 1 mg twice daily; duration of treatment is 12 weeks. Varenicline should be taken after eating, with a full glass of water.
小兒調整劑量
Use is not recommended, efficacy has not been established in patients <18 years of age <20210316>