Cymbopogon citratus is a widely distributed perennial herb belonging to the Poaceae family and has been extensively consumed for its medicinal,cosmetic,and nutritional effects for centuries.A large number of reports have been published describing the pharmacological,biological,and therapeutic actions of this herb.In this review,we summarized the literatures on related studies(up to January,2014) that highlighted the pharmacologic and biological effects of the major phytochemicals isolated from C.citratus extracts and its essential oil.The components of the essential oils found in C.citratus have a similar pharmacokinetic properties,including absorption,distribution,metabolism,and excretion.They are quickly absorbed following oral,pulmonary,and dermal administration.Based on the published reports,it can also be inferred that,after absorption from the small intestine,some phytochemicals in C.citratus can undergo oxidation,glucuronidation,sulfation,and/or O-methylation.Excretion is through urine,feces and/or expired volatiles.The biotransformation reactions of C.citratus bioactive constituents are essential for its relatively safe consumption and therapeutic applications.The data available so far warrant further studies evaluating C.citratus pharmacokinetics.Reliable pharmacokinetic data in humans would be critical for a better understanding of the the systemic handling of C.citratus. Cymbopogon citratus is a widely distributed perennial herb belonging to the Poaceae family and has been extensively consumed for its medicinal, cosmetic, and nutritional effects for centuries. A large number of reports have been published describing the pharmacological, biological, and therapeutic actions of this herb . This this review, we summarized the literatures on related studies (up to January, 2014) that highlighted the pharmacologic and biological effects of the major phytochemicals isolated from C. citratus extracts and its essential oils. The components of the essential oils found in C .citratus have a similar pharmacokinetic properties, including absorption, distribution, metabolism, and excretion. They are quickly administered following oral, pulmonary, and dermal administration. Based on the published reports, it can also be inferred that, after absorption from the small intestine , some phytochemicals in C. citratus can undergo oxidation, glucuronidation, sulfation, and / or O-methylation. Excretion is throug h urine, feces and / or expired volatiles. The biotransformation reactions of C. citratus bioactive constituents are essential for its relatively safe consumption and therapeutic applications. The data available so far warrant further studies evaluating C. citratus pharmacokinetics. Reliable pharmacokinetic data in human would be critical for a better understanding of the systemic handling of C. citratus.