The seeds of the plant contain numerous lysergic acid amides, including ergine, ergonovine and isoergine, a chemical group from which derives the well known psychedelic, LSD. Psychedelic effects experienced after consumption of the seeds are usually attributed to ergine (also known as d-Lysergic acid amide, or Lyserg Sauer Amide), although the validity of this claim is disputed. For more information, refer to ergine.

While ergine is listed as a DEA Schedule III substance in the United States, Hawaiian baby woodrose is not controlled. Thus, while possession of any part of the plant is legal, an ergine extraction is prosecutable by US law, however no such prosecutions have occurred. The plant is not monitored as a major controlled substance precursor, since a synthesis of LSD from ergine, while possible, is impractical.

The seeds also contain glycosides. These compounds may cause some of the reported side-effects from eating the crushed seeds. Many people believe the fuzzy coating of the seed causes the nausea, but this "fur" is inert; the nauseating factor is contained in the seed itself.