Pharmacokinetics of dihydrocodeine and its active metabolite after single and multiple oral dosing

British Journal of Clinical Pharmacology

Volumn 48, Issue 3, 1999, Pages 317-322

  Ammon, Susanne ^a   Hofmann, Ute ^a   Griese, Ernst Ulrich ^a   Gugeler, Nadja ^a   Mikus, Gerd ^a  

^a DR MARGARETE FISCHER BOSCH INSTITUTE OF CLINICAL PHARMACOLOGY   (Germany)

Author keywords

Dihydrocodeine; Dihydromorphine; Multiple dose; Pharmacokinetics; Single dose

Indexed keywords

DIHYDROCODEINE; DIHYDROMORPHINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CLINICAL TRIAL; CONSTIPATION; DEMETHYLATION; DRUG BLOOD LEVEL; EUPHORIA; HEADACHE; HUMAN; HUMAN EXPERIMENT; MALE; NAUSEA; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; STEADY STATE; STOMACH PAIN; URINALYSIS; URINE RETENTION; VERTIGO; VOMITING; XEROSTOMIA;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; ANALGESICS, OPIOID; CODEINE; HUMANS; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; THERAPEUTIC EQUIVALENCY;

EID: 0032840025     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2125.1999.00042.x     Document Type: Article

References (20)

1. Rowell FJ, Seymour RA, Rawlins MD. Pharmacokinetics of intravenous and oral dihydrocodeine and its acid metabolites. Eur J Clin Pharmacol 1983; 25: 419-424.
2. Davies KN, Castleden CM, McBurney A, Jagger C. The effect of ageing an the pharmacokinetics of dihydrocodeine. Eur J Clin Pharmacol 1989; 37: 375-379.
3. Fromm MF, Hofman U, Griese E-U, Mikus G. Dihydrocodeine: a new opioid substrate for the polymorphic CYP2D6 in humans. Clin Pharmacol Ther 1995; 58: 374-382.
4. Wotherspoon HA, Kenny GNC, McArdle CS. Analgesic efficacy of controlled release dihydrocodeine. Anaesthesia 1991: 46: 915-917.
5. Chen ZR, Somogyi AA, Bochner F. Polymorphic O-demethylation of codeine. Lancet 1988; ii: 914-915.
6. Dayer P, Desmeules J, Leeman T, Striberni R. Bioactivation of the narcotic drug codeine in humans is medicated by the polymorphic monooxygenase catalysing debrisoquin 4-hydroxylation. Biochem Biophys Res Commun 1988; 152: 411-416.
7. Yue QJ, Svennson JO, Alm C, Sjöquist F, Säwe J. Codeine O-demethylation co-seggregates with polymorphic debrisoquine hydroxylation. Br J Clin Pharmacol 1989; 28: 639-645.
8. Mikus G, Trausch B, Rodewald C, et al. Effects of codeine on gastrointestinal motility in relation to CYP2D6 phenotype. Clin Pharmacol Ther 1997; 61: 459-465.
9. Kirkwood LC, Nation RL, Somogyi AA. Characterisation of the human cytochrome P450 enzymes involved in the metabolism of dihydrocodeine. Br J Clin Pharmacol 1997; 44: 549-555.
10. Eckhardt K, Li S, Ammon S, Schänzle G, Mikus G, Eichelbaum M. Same incidence of adverse drug events after codeine administration irrespective of the genetically determined differences in morphine formation. Pain 1998; 76: 27-33.
11. Poulsen L, Brosen K, Arendt-Nielsen L, Gram LF, Elback K, Sindrup SH. Codeine and morphine in extensive and poor metabolizers of sparteine: pharmacokinetics, analgesic effect and side effects. Eur J Clin Pharmacol 1996; 51: 289-295.
12. Wilder-Smith CH, Hufschmid E, Thormann W. The visceral and somatic antinociceptive effects of dihydrocodeine and ist metabolite, dihydromorphine. A cross-over study with extensive and quinidine-induced poor metabolizers. Br J Clin Pharmacol 1998; 45: 575-581.
13. Eichelbaum M, Bertilsson L, Säwe J, Zekorn C. Polymorphic oxidation of sparteine and debrisoquine: related pharmacogenetic entities. Clin Pharmacol Ther 1982; 31: 184-186.
14. Stüven T, Griese E-U, Kroemer HK, Eichelbaum M, Zanger U. Rapid detection of CYP2D6 null alleles by long distance - and multiplex - polymerase chain reaction. Pharmacogenetics 1996; 6: 417-421.
15. Griese EU, Zanger UM, Brudermanns U, et al. Assessment of the predictive power of genotypes for the in-vivo catalytic function of CYP2D6 in a German population. Pharmacogenetics 1998; 8: 15-26.
16. Hofmann U, Fromm MF, Johnson S, Mikus G. Simultaneous determination of dihydrocodeine and dihydromorphine in serum by gas chromatography-tandem mass spectrometry. J Chromatogr B Biomed Appl 1995; 663: 59-65.
17. Kirkwood L, Nation R.I., Somogyi AA. Glucuronidation of dihydrocodeine by human liver microsomes and the effect of inhibitors. Clin Exp Pharmacol Physiol 1998; 25: 266-270.
18. Mikus G, Ulmer A, Mörike K, Hofmann U. Heroin substitution therapy: Pharmacokinetics of dihydrocodeine. Naunyn-Schmiedeberg's Arch Pharmacol 1998; 358(Suppl 2): P 47.28.
19. Chen ZR, Somogyi AA, Reynolds G, Bochner F. Disposition and metabolism of codeine after single and chronic doses in one poor and seven extensive metabolizers. Br J Clin Pharmacol 1991; 31: 381-390.
20. Yuc QY, Hasselström J, Svensson JO, Säwe J. Pharmacokinetics of codeine and ist metabolites in Caucasian healthy volunteers: comparisons between extensive and poor hydroxilators of debrisoquine. Br J Clin Pharmacol 1991; 31: 635-642.