Ketobemidone structure

Ketobemidone is a powerful opioid analgesic. Its potency is equal to morphine, and it also has some NMDA-antagonist properties. This makes it useful for some types of pain that don't respond well to other opioids. Image File history File links Ketobemidone. ... Image File history File links Ketobemidone. ... An opioid is any agent that binds to opioid receptors, found principally in the central nervous system and gastrointestinal tract. ... An analgesic (colloquially known as a painkiller) is any member of the diverse group of drugs used to relieve pain and to achieve analgesia. ... Morphine (INN) (IPA: ) is an extremely powerful opiate analgesic drug and is the principal active agent in opium. ... NMDA (N-methyl-D-aspartic acid) is an amino acid derivative acting as a specific agonist at the NMDA receptor, and therefore mimics the action of the neurotransmitter glutamate on that receptor. ...

It is used for all types of severe pain, such as postoperative, cancer, kidney stones and fractures. Cancer is a class of diseases or disorders characterized by uncontrolled division of cells and the ability of these cells to invade other tissues, either by direct growth into adjacent tissue through invasion or by implantation into distant sites by metastasis. ... Bladder stone redirects here. ... A bone fracture is a medical condition in which a bone becomes cracked, splintered, or bisected as a result of physical trauma. ...

History

It was first synthesized in 1942 by Eisleb. The first study of it in man was published in 1946, and it was introduced in clinical medicine shortly after.

Chemistry

Ketobemidone is 1-methyl-4-(3-hydroxyphenyl)-4-propionylpiperidine. It is usually available as the hydrochloride, which is a white powder. It is synthesized by alkylating (3-methoxyphenyl)acetonitrile with bis(2-chloroethyl)methylamine, followed by reaction with ethylmagnesiumbromide, and finally hydrolysis with hydrobromic acid. In chemistry, hydrochlorides are salts resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (mostly amines). ... Mechlorethamine also known as chlormethine, mustine, nitrogen mustard and HN2 and sold under the brand name Mustargen, is the prototype anticancer chemotherapeutic drug. ... It has been suggested that this article or section be merged into hydrogen bromide. ...

Pharmacology

Experiments on former addicts indicated it was more addictive than other opioids, so in 1954 the Economic and Social Council took a resolution urging goverments to stop manufacture and use of ketobemidone^[1] . As a result ketobemidone is mostly used in the scandinavian countries, with Denmark topping the statistics^[2] . This result was not in agreement with clinical observations, and another study in 1958 didn't find it more addictive than morphine^[3]. That study noticed that while for morphine the dose for euphoria is the same as that for analgesia, for ketobemidone the analgesic dose was well below the euphoric dose. Scandinavia is a region in Northern Europe. ... Look up euphoria in Wiktionary, the free dictionary. ...

Analgesia after 5-10 mg orally or 5-7.5 mg intravenously lasts 3-5 hours. The bioavailability for oral doses is 34%. Ketobemidone is also availible in preparations with a spasmolytic, which can improve the analgesia. The milligram (symbol mg) is an SI unit of mass. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ...

Ketobemidone is mainly metabolised by conjugation of the phenolic hydroxyl group, and by N-desmethylation. Only about 16% is excreted unchanged. Conjugation may refer to: Grammatical conjugation, the modification of runnign a verb from its basic form Latin conjugation, Spanish conjugation and The English verb, each with complex conjugation forms Marriage, relationship between two individuals In mathematics: Complex conjugation, the operation which multiplies the imaginary part of a complex number by...

Pfizer manufactures ketobemidone under the tradename Ketogan. Ketogan is availible as tablets, suppositories and injection fluid. Pfizer, Incorporated (NYSE: PFE), is the worlds largest pharmaceutical company based in New York City. ... Common disk-shaped tablets A pharmacological tablet is a medicinal or other active substance mixed with binder powders and pressed into a tablet form. ... A suppository is a medicine that is inserted either into the rectum (rectal suppository) or into the vagina (vaginal suppository) where it melts. ...

References

1. ^ UNODC. Development of Synthetic Narcotic Drugs. Retrieved on 2006-09-07.
2. ^ INCB. Statistical information on narcotic drugs. Retrieved on 2006-09-07.
3. ^ Bondesson, Ulf (1982). "Biological fate of ketobemidone in man". Abstracts of Uppsala dissertations from the Faculty of Pharmacy 68.

United Nations Office on Drugs and Crime (UNODC) is a United Nations agency which was founded in 1997 as the Office for Drug Control and Crime Prevention with the intent to fight drugs and crime on an international level. ... 2006 (MMVI) is a common year starting on Sunday of the Gregorian calendar. ... September 7 is the 250th day of the year (251st in leap years). ... Mr. ... 2006 (MMVI) is a common year starting on Sunday of the Gregorian calendar. ... September 7 is the 250th day of the year (251st in leap years). ...