Authors: Ramón SotomayorZárate Katia Gysling Usoa E Busto Bruce K Cassels Lutske Tampier María Elena Quintanilla
Publish Date: 2013/01/24
Volume: 227, Issue: 2, Pages: 287-298
Abstract
Neuronal nicotinic acetylcholine receptors nAChRs are pharmacological targets that have recently been implicated in the reinforcing effects of many drugs of abuse including ethanol Varenicline and cytisine are nAChR partial agonists in clinical use as smoking cessation aids However their efficacies to reduce alcohol consumption have not been fully studiedRepeated dosing 05 or 10 mg/kg/day ip of varenicline or cytisine for three consecutive days to male UChB rats preexposed to 10 v/v ethanol and water 24 h/day for 4 weeks significantly reduced alcohol intake and preference of ethanol over water during 1 and 24h ethanol access periods This effect was specific for ethanol intake and was not observed for 02 saccharin or water consumption Varenicline appears to be more effective than cytisine probably due to its more favorable pharmacokinetic and pharmacodynamic properties Longterm use of both nAChRs ligands for more than 8–10 days induced tolerance to their effects on ethanol consumptionThis preclinical study in UChB rats demonstrated that both varenicline and cytisine reduce alcohol intake with varenicline producing a greater and longerlasting reduction than cytisine However dose adjustment will have to be considered as a possible way to counter tolerance arising after continued use
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