The effectiveness of the amides piplartine and piperlonguminine isolated from Piper species for controlling L3 and L4 of Aedes aegypti (L.) was assessed through bioassays at concentrations ranging from 1 to 300 µg/ml. Piplartine reduced the mosquito development period and caused larval mortality only at concentrations >100 µg/ml, whereas piperlonguminine resulted in an extended period of mosquito development (10 µg/ml) and caused 100% larval mortality (30 µg/ml) within 24 h. The toxicity and cytotoxic effects of piperlonguminine on epithelial cells of the digestive system of Ae. aegypti were viewed using transmission electron microscopy, which indicated vacuolization of cytoplasm, mitochondrial swelling and leaking of nuclear material. Piperlonguminine was the more effective amide, showing toxic activity with LD₅₀ of ≈12 µg/ml against the larvae of Ae. aegypti.