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Varenicline displays full agonism on α 7 nicotinic acetylcholine receptors and is a partial agonist on the α 4 β 2, α 3 β 4, and α 6 β 2 subtypes. [37] [38] [39] Varenicline's partial agonism on the α 4 β 2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's.
ABC also quotes an MD who regularly prescribes varenicline, so he is an expert: "Richard Honaker prescribes Chantix to patients and while he urges caution with the drug, he believes the possible risks may still be worth the benefit."More patients by far are able to quit smoking with this drug than anything else we have," Honaker said."
However, more recent studies indicate less serious neuropsychiatric side effects. For example, a 2016 study involving 8,144 patients treated at 140 centers in 16 countries "did not show a significant increase in neuropsychiatric adverse events attributable to varenicline or bupropion relative to nicotine patch or placebo". [45]
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Varenicline tartrate: Champix, Chantix 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine [27] Film coated tablet Partial agonist of the nicotinic acetylcholine receptor, subtype α 4 β 2 [28] Treatment of tobacco dependence [28] Galantamine hydrobromide: Reminyl, Nivalin, Razadyne and Razadyn ER
In 2011, a randomized controlled trial with 740 patients found cytisine improved 12-month abstinence from nicotine from 2.4% with placebo to 8.4% with cytisine. [12] A 2013 meta-analysis of eight studies demonstrated that cytisine has similar effectiveness to varenicline but with substantially lower side effects. [13]
It is not necessarily true that a physician and patient will have a conversation about a drug's boxed warning after it is issued. [4] For instance, an FDA-mandated boxed warning decreased rosiglitazone use by 70%, but that still meant 3.8 million people were given the drug.
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