It is a derivative of the better-known opioid etorphine, a very potent veterinary painkiller and anesthetic medication used primarily for the sedation of large animals such as elephants, giraffes, and rhinos.

[3] It is several thousand times stronger than morphine (between 1000× and 12000× more potent depending what method is used for comparison),[1] although it is poorly absorbed when taken orally.

Sublingual forms of dihydroetorphine are used in China at doses ranging from 20 to 40 μg repeated every 3–4 hours, and are reported to cause strong analgesia and relatively mild side effects compared to other opioids, although all the usual opioid side effects such as dizziness, sedation, nausea, constipation, and respiratory depression can occur.

[6][7] It is presumably controlled as an "ester, ether, [or] salt" of etorphine in the United States under the Controlled Substances Act 1970, and/or its pieces of the morphine carbon skeleton put it under the "morphine rule" thereof and/or the 1986 analogues act; it does not have its own ACSCN.

[citation needed] Dihydroetorphine is illegal in Italy, as are its parent compounds etorphine and acetorphine.