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Titolo:
Use of a propafenone metabolic ratio as a measure of CYP2D6 activity
Autore:
Anzenbacherova, E; Anzenbacher, P; Perlik, F; Kvetina, J;
Indirizzi:
Acad Sci Joint Inst, Inst Expt Biopharmaceut, PRO MED CS Praha as, Hradec Kralove 50002, Czech Republic Acad Sci Joint Inst Hradec Kralove Czech Republic 50002 , Czech Republic Charles Univ, Fac Med, Dept Med 1, Clin Pharmacol Unit, Prague, Czech Republic Charles Univ Prague Czech Republic armacol Unit, Prague, Czech Republic
Titolo Testata:
INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS
fascicolo: 9, volume: 38, anno: 2000,
pagine: 426 - 429
SICI:
0946-1965(200009)38:9<426:UOAPMR>2.0.ZU;2-R
Fonte:
ISI
Lingua:
ENG
Soggetto:
DRUG; PHENOTYPE; EXCRETION; SPARTEINE;
Keywords:
propafenone; CYP2D6 phenotyping; sparteine; pharmacokinetics;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
13
Recensione:
Indirizzi per estratti:
Indirizzo: Anzenbacherova, E Acad Sci Joint Inst, Inst Expt Biopharmaceut, PRO MED CSPraha as, Heyrovskeho 1207, Hradec Kralove 50002, Czech Republic Acad Sci Joint Inst Heyrovskeho 1207 Hradec Kralove Czech Republic 50002
Citazione:
E. Anzenbacherova et al., "Use of a propafenone metabolic ratio as a measure of CYP2D6 activity", INT J CL PH, 38(9), 2000, pp. 426-429

Abstract

Aim: The antiarrythmic drug propafenone is metabolized to its main metabolite by CYP2D6 phenotyping. However, reported ratios obtained from plasma did not reflect the phenotype. The objective of this was to find optimal conditions for plasma sampling based on pharmacokinetic data and to investigatewhether propafenone/metabolite ratios reflect the CYP2D6 phenotype. Patients, materials and methods: The present study was conducted in 14 healthy volunteers phenotyped for CYP2D6 activity by a sparteine test. A single dose of oral propafenone (Profenorm PRO.MED.CS Praha a.s.) was administered, andvenous blood samples were taken up to 24 hours thereafter. Propafenone and24 hours thereafter. Propaferone and hydroxypropaferone were measured by HPLC. Results: The individual data for the respective propafenone/metabolitemetabolic ratio in plasma samples taken at t(max) correlated well with thesparteine metabolic ratio used routinely for CYP2D6 phenotyping. However, when the samples were taken 4 hours after drug intake, the correlation was poor. Conclusion: The results indicate a possibility to use the propafenonemetabolic ratio for determination of the CYP2D6 phenotype in plasma samples taken at single time point (close to the Cmas. i.e. 2 hours after drug intake).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 01:01:32