Prucalopride and Varenicline (Champix): Case Report of a Possible Drug Interaction at Enteric Serotonin (5-HT) Receptors

Miss Molly Jakeman, Kieran Moriarty and Suzanne Schneider

Bolton NHS Foundation Trust, United Kingdom

^*Correspondance to: Miss Molly Jakeman 

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Abstract:

Background: Prucalopride is a highly selective, high affinity agonist of serotonin (5-HT)₄ receptors on cholinergic motor neurones, and stimulates gastrointestinal motility through enhanced release of acetylcholine. Prucalopride is approved for the treatment of Chronic Constipation (CC) in adult women, for whom standard laxative use has failed to provide adequate relief.Varenicline (Champix), prescribed as a smoking cessation aid, prevents nicotine stimulation of the mesolimbic dopamine system associated with nicotine addiction. Varenicline is a highly selective, high affinity partial agonist at neuronal α4β2 nicotinic receptors. It displays full agonism on a₇/5-HT₃ nicotinic acetylcholine receptors and is a potent agonist of the human 5-HT₃ receptor.Case
Presentation: Prucalopride treatment for an adult white female produced a marked, sustained improvement in her chronic constipation. The benefit disappeared rapidly after commencing varenicline, but was restored equally rapidly, once the varenicline was discontinued.Conclusion: This case suggests a possible drug interaction between prucalopride and varenicline at enteric 5-HT receptors. An interaction between these two medications has not previously been described.

Keywords:

Prucalopride; Varenicline; Serotonin; Receptors; Interaction; Case report

Cite the Article:

Jakeman MM, Moriarty K, Schneider S. Prucalopride and Varenicline (Champix): Case Report of a Possible Drug Interaction at Enteric Serotonin (5-HT) Receptors. Ann Clin Case Rep. 2016; 1: 1175.