Dihydroetorphine was developed by K. W. Bentley at McFarlan-Smith in the 1960s and is a potent

opioid Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use ...

analgesic used mainly in China. It is a

derivative In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. ...

of the better-known opioid

etorphine Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the r ...

, a very potent veterinary painkiller and

anesthetic An anesthetic (American English) or anaesthetic (British English; see spelling differences) is a drug used to induce anesthesia ⁠— ⁠in other words, to result in a temporary loss of sensation or awareness. They may be divided into two ...

medication used primarily for the sedation of large animals such as elephants, giraffes, and rhinos. Dihydroetorphine is a semi- synthetic

used mainly as a strong

painkiller An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It i ...

for humans. It is several thousand times stronger than

morphine Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies (''Papaver somniferum''). It is mainly used as a pain medication, and is also commonly used recreationally, or to make other illicit opioids. T ...

(between 1000x and 12000x more potent depending what method is used for comparison), 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 Dizziness is an imprecise term that can refer to a sense of disorientation in space, vertigo, or lightheadedness. It can also refer to disequilibrium or a non-specific feeling, such as giddiness or foolishness. Dizziness is a common medical c ...

, sedation,

nausea Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the ...

constipation Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the bowel movement ...

, and respiratory depression can occur.

Transdermal Transdermal is a route of administration wherein active ingredients are delivered across the skin for systemic distribution. Examples include transdermal patches used for medicine delivery. The drug is administered in the form of a patch or ointme ...

patches of dihydroetorphine have also been developed. Dihydroetorphine is considered to be somewhat less addictive than many other opioids, and it is also sometimes used in China as a substitute maintenance drug for opioid addicts, in a similar fashion to how the related drug

buprenorphine Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal ...

is used in western nations. It is presumably controlled as an "ester, ether, salt ..." of

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 Administrative Controlled Substances Code Number (ACSCN) is a number assigned to drugs listed on the schedules created by the US Controlled Substances Act (CSA). The ACSCN is defined in 21 CFR § 1308.03(a). Each chemical/drug on one of the schedu ...

. Regulation elsewhere may vary but would likely be similar to that for other strong opioid agonists. Dihydroetorphine is illegal in Italy, as are its parent compounds

and

acetorphine Acetorphine is a potent opioid analgesic, up to 8700 times stronger than morphine by weight. It is a derivative of the more well-known opioid etorphine, which is used as a very potent veterinary painkiller and anesthetic medication, primarily f ...

(April 2022 data).

References

External links

* 4,5-Epoxymorphinans Semisynthetic opioids Mu-opioid receptor agonists Phenols Tertiary alcohols Ethers {{analgesic-stub

See also

References

External links