Historique
Article de Périodique
Pharmacokinetics of the combination tablet of buprenorphine and naloxone (2003)
(Pharmacocinétique de l'association buprénorphine et naloxone en comprimés sublinguaux)
Auteur(s) :
C. N. CHIANG ;
R. L. HAWKS
Article en page(s) :
S39-S47
Refs biblio. :
48
Domaine :
Drogues illicites / Illicit drugs
Langue(s) :
Anglais
Thésaurus mots-clés
BUPRENORPHINE
;
NALOXONE
;
OPIACES
;
DEPENDANCE
;
TRAITEMENT DE MAINTENANCE
;
PHARMACOCINETIQUE
Note générale :
Drug and Alcohol Dependence, 2003, 70, (2, Suppl. 1), S39-S47
Note de contenu :
fig. ; tabl.
Résumé :
ENGLISH :
The sublingual combination tablet formulation of buprenorphine and naloxone at a fixed dose ratio of 4:1 has been shown to be as effective as the tablet formulation containing only buprenorphine in treating opiate addiction. The addition of naloxone does not affect the efficacy of buprenorphine for two reasons: (1) naloxone is poorly absorbed sublingually relative to buprenorphine and (2) the half-life for buprenorphine is much longer than for naloxone (32 vs. 1 h for naloxone). The sublingual absorption of buprenorphine is rapid and the peak plasma concentration occurs 1 h after dosing. The plasma levels for naloxone are much lower and decline much more rapidly than those for buprenorphine. Increasing dose results in increasing plasma levels of buprenorphine, although this increase is not directly dose-proportional. There is a large inter-subject variability in plasma buprenorphine levels. Due to the large individual variability in opiate dependence level and the large variability in the pharmacokinetics (PK) of buprenorphine, the effective dose or effective plasma concentration is also quite variable. Doses must be titrated to a clinically effective level for individual patients. (Review's abstract.)
ENGLISH :
The sublingual combination tablet formulation of buprenorphine and naloxone at a fixed dose ratio of 4:1 has been shown to be as effective as the tablet formulation containing only buprenorphine in treating opiate addiction. The addition of naloxone does not affect the efficacy of buprenorphine for two reasons: (1) naloxone is poorly absorbed sublingually relative to buprenorphine and (2) the half-life for buprenorphine is much longer than for naloxone (32 vs. 1 h for naloxone). The sublingual absorption of buprenorphine is rapid and the peak plasma concentration occurs 1 h after dosing. The plasma levels for naloxone are much lower and decline much more rapidly than those for buprenorphine. Increasing dose results in increasing plasma levels of buprenorphine, although this increase is not directly dose-proportional. There is a large inter-subject variability in plasma buprenorphine levels. Due to the large individual variability in opiate dependence level and the large variability in the pharmacokinetics (PK) of buprenorphine, the effective dose or effective plasma concentration is also quite variable. Doses must be titrated to a clinically effective level for individual patients. (Review's abstract.)
Affiliation :
Division Treat. Res. Develop., NIDA, 6001 Executive blvd, MD 20892
Etats-Unis. United States.
Etats-Unis. United States.