Bacopa caroliniana (BC) is a perennial creeping herb and popular aquarium plant. This plant is easily cultivated; consequently, it has the potential to be a raw material which is readily available for mass production if it contains useful bioactive substances. The information about the functionality of this plant has been very limited. Therefore, the aims of this research were to analyze the composition of the essential oil (EO) of BC and to study its insecticidal effect on rice weevils. Moreover, the interactive effects of active compounds of the EO on this activity were also investigated. A total of 18 volatile compounds was identified, accounting for ca. 94% of the BC-EO in terms of quantity. Of them, α-terpinolene was the largest compound. The impact of individual volatile compounds on the inhibition of acetylcholine esterase and insecticidal activity were determined. α-Terpinolene exhibited the highest activity on these assays. Both additive and synergistic effects existed in terms of the insecticidal activity. Many compounds found in the BC-EO are widely present in other EOs. Thus, the information obtained from this study is useful for EO-related research, applications in selecting EOs or in seeking the best combination of EOs or individual compounds to achieve efficient insecticidal effects.