Ipecac was used as an insect repellant and amoebicide by South American Indians. It was introduced in Europe in the late 16th century and became well known in medicine. Ipecac is used as an expectorant and emetic and in the treatment of amoebic dysentery. Both emetine and synthetic drug 2,3-dehydro emetine are anti-amoebic and act primarily on the intestinal wall and the liver. Emetine hydrochloride has been used extensively as an anti-protozoan in the treatment of amoebiasis, pyorrhea alveolaris and other amoebic diseases. The emetic action of the alkaloids is valuable and the crude drug extract in the form of ipecac emetic mixture is an important preparation used for drug overdose or poisoning. The emetic mixture is often a standard component in poison antidote kits. Ipecac extracts are still components of a number of compound expectorant preparations.

Emetine has more expectorant and less emetic action than cephaeline which is why the Brazilian root is preferred for such mixtures. Emetine may also be prepared by the methylation of cephaeline. Both emetine and cephaeline are potent inhibitors of protein synthesis, inhibiting at the translocation stage. They display anti-tumour, anti-viral and anti-amoebic activity but are too toxic for therapeutic use. In recent studies, o-methyl psychotrine has shown the ability to inhibit viral replication through inhibition of HIV-reverse transcriptase. This gives it a potential in the treatment of AIDS.