Flavonoids as GABAA receptor ligands: the whole story?

S Roberts, Dmitri Bezinover, Piotr Janicki, Piotr Janicki
Journal of Experimental Pharmacology   unpublished
Chemotherapy-induced nausea and vomiting and postoperative nausea and vomiting are one of the most frequent but also very concerning consequences for patients undergoing chemotherapy or surgical procedures under general anesthesia. There are a variety of mechanisms involved in the activation of nausea and vomiting. Serotonin, a ubiquitous central and peripheral neurotransmitter, is thought to be the predominant mediator of the perception of nausea and triggering of the vomiting response in both
more » ... the brain and the periphery via the 5-hydroxytryptamine type 3 (5-HT 3) receptor pathways. 5-HT 3 receptor antagonists disrupt this pathway, largely at the level of the vagal afferent pathways, to decrease nausea and vomiting. This review will focus on dolasetron, an older but sill commonly used 5-HT 3 receptor antagonist and its multimodal mechanism of action, safety and tolerability, patient considerations, and a review of the current literature on its use to combat both chemotherapy-induced and postoperative nausea and vomiting in these two important patient populations.