The intake of flavanones, the predominant flavonoid in the Citrus genus in human diets is variable but considerable. It is thus unsurprising that they have attracted interest for their claimed positive effects on health. However, to substantiate any purported impact on health and decipher the underlying mechanism(s), knowledge of pharmacokinetics is crucial. The aim of this article is to review currently known aspects of the fate of flavanones in the organism including absorption, metabolism, distribution, and excretion as well as possible kinetic interactions with clinically used drugs. There are three principal keynotes: (1) The level of parent flavanones in plasma is negligible. The major reason for this is that although flavanones are absorbed into enterocytes after oral intake, they are rapidly metabolized, in particular, into conjugates, sulfates and glucuronides, which are the major forms circulating in plasma. (2) A large fraction reaches the colon where it is efficiently metabolized into small absorbable phenolics. (3) The form (aglycone vs. glycoside) and species (e.g. human vs. rat) have important impact. In conclusion, knowledge of the pharmacokinetics of flavanones, in particular of metabolites, their achievable plasma concentration and half-lives, should be borne in mind when their biological effects are investigated.