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Titre du document / Document title

Drug acetylation in liver disease

Auteur(s) / Author(s)

LEVY M. (1) ; CARACO Y. (1) ; GEISSLINGER G. (2) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Clinical Pharmacology Unit, Division of Medicine, Hadassah University Hospital, Jerusalem, ISRAEL
(2) Department of Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nürnberg, Erlangen, ALLEMAGNE

Résumé / Abstract

N-Acetylation is a phase II conjugation reaction mediated in humans by the polymorphic N-acetyltransferase 2 (NAT2) and N-acetyltransferase I (NAT1). Acetylation of some drugs may be modestly decreased in patients with chronic liver disease, whereas acute liver injury has no effect on drug acetylation. For NAT2 substrates, the impairment in acetylation capacity seems to be phenotype-specific, with a more prominent effect heing exerted in rapid than slow acetylators. Thus, in the presence of significant hepatic dysfunction. the activity of NAT2 may not exhibit its usual bimodal distribution, and hence phenotypic assignment may not be reliable. Furthermore, it remains to be evaluated whether the precautions advised for slow acetylators when treated with drugs metabolised by NAT2 apply to all patients (regardless of phenotype) with liver cirrhosis.

Revue / Journal Title

Clinical pharmacokinetics    ISSN  0312-5963   CODEN CPKNDH 

Source / Source

1998, vol. 34, no3, pp. 219-226 (42 ref.)

Langue / Language

Anglais

Editeur / Publisher

Adis International, Auckland, NOUVELLE-ZELANDE  (1976) (Revue)

Mots-clés anglais / English Keywords

Acetylation

;

Drug

;

Metabolism

;

Cirrhosis

;

Viral hepatitis B

;

Asymptomatic

;

Acute

;

Chronic

;

Acetylator phenotype

;

Enzymatic activity

;

Pharmacogenetics

;

Human

;

Review

;

Arylamine N-acetyltransferase

;

Viral disease

;

Infection

;

Digestive diseases

;

Hepatic disease

;

Acyltransferases

;

Transferases

;

Enzyme

;

Mots-clés français / French Keywords

Acétylation

;

Médicament

;

Métabolisme

;

Cirrhose

;

Hépatite virale B

;

Asymptomatique

;

Aigu

;

Chronique

;

Phénotype acétylateur

;

Activité enzymatique

;

Pharmacogénétique

;

Homme

;

Article synthèse

;

Arylamine N-acetyltransferase

;

N-Acétyltransférase

;

Virose

;

Infection

;

Appareil digestif pathologie

;

Foie pathologie

;

Acyltransferases

;

Transferases

;

Enzyme

;

Mots-clés espagnols / Spanish Keywords

Acetilación

;

Medicamento

;

Metabolismo

;

Cirrosis

;

Hepatitis vírica B

;

Asintomático

;

Agudo

;

Crónico

;

Fenotipo acetilador

;

Actividad enzimática

;

Farmacogenética

;

Hombre

;

Artículo síntesis

;

Arylamine N-acetyltransferase

;

Virosis

;

Infección

;

Aparato digestivo patología

;

Hígado patología

;

Acyltransferases

;

Transferases

;

Enzima

;

Localisation / Location

INIST-CNRS, Cote INIST : 15599, 35400007906481.0040

Nº notice refdoc (ud4) : 2178708



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