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Titolo:
Codeine analgesia is due to codeine-6-glucuronide, not morphine
Autore:
Vree, TB; Van Dongen, RTM; Koopman-Kimenai, PM;
Indirizzi:
Acad Hosp St Radboud, Inst Anasthesiol, NL-6525 GA Nijmegen, Netherlands Acad Hosp St Radboud Nijmegen Netherlands NL-6525 GA jmegen, Netherlands Acad Hosp St Radboud, Pain Ctr, NL-6525 GA Nijmegen, Netherlands Acad HospSt Radboud Nijmegen Netherlands NL-6525 GA jmegen, Netherlands
Titolo Testata:
INTERNATIONAL JOURNAL OF CLINICAL PRACTICE
fascicolo: 6, volume: 54, anno: 2000,
pagine: 395 - 398
SICI:
1368-5031(200007/08)54:6<395:CAIDTC>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXTENSIVE METABOLIZERS; PLASMA-CONCENTRATIONS; HEALTHY-VOLUNTEERS; POOR METABOLIZERS; MORPHINE-6-GLUCURONIDE; RECEPTOR; BRAIN; DISPOSITION; SPARTEINE; AGONIST;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Citazioni:
30
Recensione:
Indirizzi per estratti:
Indirizzo: Vree, TB Acad Hosp St Radboud, Inst Anasthesiol, Geert Grooteplein Zuid 10,POB 9101, NL-6525 GA Nijmegen, Netherlands Acad Hosp St Radboud Geert Grooteplein Zuid 10,POB 9101 Nijmegen Netherlands NL-6525 GA
Citazione:
T.B. Vree et al., "Codeine analgesia is due to codeine-6-glucuronide, not morphine", INT J CL PR, 54(6), 2000, pp. 395-398

Abstract

Eighty per cent of codeine is conjugated with glucuronic acid to codeine-6-glucuronide. Only 5% of the dose is O-demethylated to morphine, which in turn is immediately glucuronidated at the 3- and 6- position and excreted renally. Based on the structural requirement of the opiate molecule for interaction with the mu-receptor to result in analgesia, codeine-6-glucuronide in analogy to morphine-6-glucuronide must be the active constituent of codeine. Poor metabolisers of codeine, those who lack the CYP450 2D6 isoenzyme for the O-demethylation to morphine, experience analgesia from codeine-6-glucuronide. Analgesia of codeine does not depend on the formation of morphineand the metaboliser phenotype.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/20 alle ore 16:02:05