Phenadoxone
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Phenadoxone (trade names Heptalgin, Morphidone, and Heptazone) is an
opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
analgesic An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in s ...
of the
open chain In chemistry, an open-chain compound (or 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 having no side ...
class (
methadone Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid used medically to treat chronic pain and opioid use disorder. Prescribed for daily use, the medicine relieves cravings and opioid withdrawal sym ...
and relatives) invented in Germany by Hoechst 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 (1 September 1939 – 2 September 1945) was a World war, global conflict between two coalitions: the Allies of World War II, Allies and the Axis powers. World War II by country, Nearly all of the wo ...
but which were withdrawn from the market for various or no known reason and which now are mostly in Schedule I of the United States' Controlled Substances Act of 1970, or (like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 ...
) in Schedule II but not produced or marketed in the US. Others on this list are
ketobemidone Ketobemidone, sold under the brand name Ketogan (a mixture of ketobemidone and Spasmolytic A29) 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- ...
(Ketogin), dextromoramide (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, sold under the brand names of Pipadone and Diconal is a strong opioid analgesic drug, used for acute pain by mouth ( PO) for adults. It is often used in instances where morphine is indicated but cannot be used due to the patient being ...
(Diconal, Pipadone and Wellconal),
piminodine Piminodine (Alvodine) is an opioid analgesic that is an 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 obstetric analgesia an ...
(Alvodine), propiram (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 meperidin ...
(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 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, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
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. 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 ...
. Phenadoxone is most used at the current time in
Denmark Denmark is a Nordic countries, Nordic country in Northern Europe. It is the metropole and most populous constituent of the Kingdom of Denmark,, . also known as the Danish Realm, a constitutionally unitary state that includes the Autonomous a ...
and various countries in eastern Europe.


References

{{Opioidergics 4-Morpholinyl compounds Ketones Mu-opioid receptor agonists Synthetic opioids Benzhydryl compounds