Very important Drug, asked previously also.
Varenicline:
•MOA: Act on “Nicotinic Ach Receptors” (nAchR).
Main: Partial Agonist of α4β2.
Other: Partial Agonist of α3β4, and α6β2subtypes.
Full Agonist of α7.
•Varenicline (Chantix) is a non-nicotine prescription medicine specifically developed to help adults quit smoking.
•Chantix contains no nicotine, but targets the same receptors that nicotine does.
Chantix is believed to block nicotine from these receptors.
•It both relieves craving and withdrawal and, unlike other medications, reduces the reinforcing effects of nicotine by blocking dopaminergic stimulation responsible for smoking reinforcement/reward.
•The typical quit rate of the use of medication plus physician advice is approximately 20%.
•Regimen: 12 weeks…if smoking cessation achieved,continue for 12 weeks more.
•Avoid in: Preg,Lactation,<18 years old.
•Eliminated by Kidneys. T1/2 is 24 hours.
•No increase in suicide risk (as opposed to previous belief).
•MC S/E: Nausea, Sleep disturbance, Strange dreams.
•Mild chance of some CVS S/E.