Phenadoxone
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Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an
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 us ...
analgesic 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 ...
of the
open chain In chemistry, an open-chain compound (also spelled as open chain compound) or acyclic compound (Greek prefix "α", ''without'' and "κύκλος", ''cycle'') is a compound with a linear structure, rather than a cyclic one. An open-chain compound h ...
class (
methadone Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for chronic pain and also for opioid dependence. It is used to treat chronic pain, and it is also used to treat addiction to heroin ...
and relatives) invented in Germany by
Hoechst Hoechst, Hochst, or Höchst may refer to: * Hoechst AG, a former German life-sciences company * Hoechst stain, one of a family of fluorescent DNA-binding compounds * Höchst (Frankfurt am Main), a city district of Frankfurt am Main, Germany ** Fra ...
in 1947. It is one of a handful of useful synthetic analgesics which were used in the United States for various lengths of time in the 20 or so years after the end of the
Second World War World War II or the Second World War, often abbreviated as WWII or WW2, was a world war that lasted from 1939 to 1945. It involved the vast majority of the world's countries—including all of the great powers—forming two opposin ...
but which were withdrawn from the market for various or no known reason and which now are mostly in Schedule I of the United States' Controlled Substances Act of 1970, or (like
phenazocine Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. Effects of phenazocine include analgesia and euphoria, also may include dysphoria and hallucinations at ...
and
bezitramide Bezitramide is an opioid analgesic. Bezitramide itself is a prodrug which is readily hydrolyzed in the gastrointestinal tract to its active metabolite, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica in 1961. It is m ...
) in Schedule II but not produced or marketed in the US. Others on this list are
ketobemidone Ketobemidone, sold under the brand name Ketogan among others, is a powerful synthetic opioid painkiller. Its effectiveness against pain is in the same range as morphine, and it also has some NMDA-antagonist properties imparted, in part, by its m ...
(Ketogin),
dextromoramide Dextromoramide (Palfium, Palphium, Jetrium, Dimorlin) is a powerful opioid analgesic approximately three times more potent than morphine but shorter acting. It is subject to drug prohibition regimes, both internationally through UN treaties and b ...
(Dimorlin, Palfium and others),
phenazocine Phenazocine (brand names Prinadol, Narphen) is an opioid analgesic drug, which is related to pentazocine and has a similar profile of effects. Effects of phenazocine include analgesia and euphoria, also may include dysphoria and hallucinations at ...
(Narphen and Prinadol),
dipipanone Dipipanone (Pipadone) is a strong opioid analgesic drug, used for acute pain by mouth (PO) for adults - initially 10 mg every 6 hours, then increased if necessary up to 30 mg every 6 hours, with the dose to be increased gradually. It is often use ...
(Diconal, Pipadone and Wellconal),
piminodine Piminodine (Alvodine) is an opioid analgesic that is an analog (chemistry), analogue of pethidine (meperidine). It was used in medicine briefly during the 1960s and 70s, but has largely fallen out of clinical use. It was used particularly for ob ...
(Alvodine),
propiram Propiram (Algeril, Dirame, Bay 4503) is a partial mu opioid receptor agonist and weak mu antagonist analgesic from the ampromide family of drugs related to other drugs such as phenampromide and diampromide. It was invented in 1963 in the United ...
(Algeril),
anileridine Anileridine (trade name: Leritine) is a synthetic analgesic drug and is a member of the piperidine class of analgesic agents developed by Merck & Co. in the 1950s. It differs from pethidine (meperidine) in that the ''N''-methyl group of meperidi ...
(Leritine) and
alphaprodine Prodine (trade names Prisilidine and Nisentil) is an opioid analgesic that is an analog of pethidine (meperidine). It was developed in Germany in the late 1940s. There are two isomers of the trans form of prodine, alphaprodine and betaprodine. ...
(Nisentil). Phenadoxone has a US DEA ACSCN of 9637 and recently has had a zero annual manufacturing quota under the Controlled Substances Act 1970. Its withdrawal from US distribution prior to the promulgation of said act is a large part of its Schedule I designation; it is, however, used as a legitimate medication in other countries and consumption is increasing worldwide as indicated below. Phenadoxone is generally considered to be a strong opioid analgesic and is regulated in much the same way as
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 analgesic, pain medication, and is also commonly used recreational drug, recreationally, or to make ...
where it is used. The usual starting dose is 10–20 mg and it has a duration of analgesic effect of 1 to 4 hours. Phenadoxone is not used at this time for purposes other than pain relief. Worldwide consumption of phenadoxone has actually increased slightly in recent years according to a recent report from the
World Health Organization The World Health Organization (WHO) is a specialized agency of the United Nations responsible for international public health. The WHO Constitution states its main objective as "the attainment by all peoples of the highest possible level of h ...
. Like its drug subcategory prototype methadone, phenadoxone can be used as the opioid analgesic in
Brompton cocktail Brompton cocktail, sometimes called Brompton mixture or Brompton's cocktail, was an elixir meant for use as a pain suppressant dosed for prophylaxis. Made from morphine or diacetylmorphine (heroin), cocaine, highly-pure ethyl alcohol (some recipes s ...
. Phenadoxone is most used at the current time in
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and various countries in eastern Europe.


References

{{Opioidergics Morpholines Ketones Mu-opioid receptor agonists Synthetic opioids Benzhydryl compounds