Bezitramide
Encyclopedia
Bezitramide is a narcotic analgesic
. Bezitramide itself is a prodrug
which is readily hydrolyzed
in the gastrointestinal tract
to its main metabolite
, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica
in 1961. It is most commonly marketed under the trade name Burgodin.
The drug was pulled from the shelves in the Netherlands in 2004 after fatal overdose cases, including one where a five year old child took one tablet from his mother's purse, ate it, and promptly died.
Bezitramide is regulated much the same as morphine
in all known jurisdictions and is a Schedule II
substance under the United States' Controlled Substances Act of 1970. However, it has to this point never been marketed in the United States.
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
. Bezitramide itself is a prodrug
Prodrug
A prodrug is a pharmacological substance administered in an inactive form. Once administered, the prodrug is metabolised in vivo into an active metabolite, a process termed bioactivation. The rationale behind the use of a prodrug is generally for absorption, distribution, metabolism, and...
which is readily hydrolyzed
Hydrolysis
Hydrolysis is a chemical reaction during which molecules of water are split into hydrogen cations and hydroxide anions in the process of a chemical mechanism. It is the type of reaction that is used to break down certain polymers, especially those made by condensation polymerization...
in the gastrointestinal tract
Gastrointestinal tract
The human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
to its main metabolite
Metabolite
Metabolites are the intermediates and products of metabolism. The term metabolite is usually restricted to small molecules. A primary metabolite is directly involved in normal growth, development, and reproduction. Alcohol is an example of a primary metabolite produced in large-scale by industrial...
, despropionyl-bezitramide. Bezitramide was discovered at Janssen Pharmaceutica
Janssen Pharmaceutica
Janssen Pharmaceutica is pharmaceutical company, established in Belgium in 1953 by Paul Janssen. Its headquarters are located in Beerse, in the Campine region of the province of Antwerp, Belgium. It was created not as a subsidiary of a chemical factory but solely with the aim of conducting...
in 1961. It is most commonly marketed under the trade name Burgodin.
The drug was pulled from the shelves in the Netherlands in 2004 after fatal overdose cases, including one where a five year old child took one tablet from his mother's purse, ate it, and promptly died.
Bezitramide is regulated much the same as morphine
Morphine
Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was first isolated in 1804 by Friedrich Sertürner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists' shop. It was more...
in all known jurisdictions and is a Schedule II
Controlled Substances Act
The Controlled Substances Act was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970. The CSA is the federal U.S. drug policy under which the manufacture, importation, possession, use and distribution of certain...
substance under the United States' Controlled Substances Act of 1970. However, it has to this point never been marketed in the United States.