Impact of quinidine on plasma and cerebrospinal fluid concentrations of codeine and morphine after codeine intake

European Journal of Clinical Pharmacology

Volumn 49, Issue 6, 1996, Pages 503-509

  Sindrup, S H ^a   Hofmann, U ^b   Asmussen, J ^c   Mikus, G ^b   Brosen K ^a   Nielsen, F ^a   Ingwersen, S H ^d   Broen Christensen, C ^e  

^a UNIVERSITY OF SOUTHERN DENMARK   (Denmark)

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

^c ODENSE UNIVERSITY HOSPITAL   (Denmark)

^d NOVO NORDISK A S   (Denmark)

^e UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

Cerebrospinal fluid; Codeine; CYP2D6; Morphine; Plasma; Quinidine

Indexed keywords

CODEINE; MORPHINE; QUINIDINE;

ARTICLE; BLOOD BRAIN BARRIER; CLINICAL ARTICLE; DEMETHYLATION; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG METABOLISM; HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL;

EID: 0029981345     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF00195938     Document Type: Article

References (30)

1. Adler TK, Fujimoto JM, Way EL, Baker EM (1955) The metabolic fate of codeine in man. J Pharmacol Exp Ther 114:251-262
2. Agon P, Braeckman R, van Haver D, Denutte H, Goethals P, Donche H, Vermullen F, Deman J, Kaufman J.-M (1988) Drug distribution in dog brain studied by positron emission tomography. Biopharmaceut Drug Disp 9:567-577
3. Alván G, Bechtel P, Iselius L, Gundert-Remy U (1990) Hydroxylation polymorhisms of debrisoquine and mephenytoin in European populations. Eur J Clin Pharmacol 39:533-537
4. Bigger JT, Hoffman BF (1990) Antiarrhytmic drugs. In: Goodman Gilman A, Rall TW, Nies AS, Taylor P (eds) The pharmacological basis of therapeutics. 8th ed. Pergamon Press, New York, pp 840-873
5. Brinn R, Brøsen K, Gram LF, Haghfelt T, Otton SV (1986) Sparteine oxidation is practically abolished in quinidine-treated patients. Br J Clin Pharmacol 22:194-197
6. Brøsen K, Otton SV, Gram LF (1985) Sparteine oxidation polymorphism in Denmark. Pharmacol Toxicol 60:312-314
7. Chen ZR, Somogyi AA, Bochner F (1988) Polymorphic O-demethylation of codeine. Lancet II:914-915
8. Chen ZR, Irvine RJ, Bochner F, Somogui AA (1990) Morphine formation from codeine in rat brain: possible mechanism of codeine analgesia. Life Sci 46:1067-1074
9. Dayer P, Desmeules J, Leemann T, Striberni R (1988) Bioactivation of the narcotic drug codeine in human livers is mediated by the polymorphic monooxygenase catalyzing debrisoquine 4-hydroxylation (cytochrome P450dbl/bufl). Biochem Biophys Res Comm 152:411-416
10. Desmeules J, Gascon M-P, Dayer P, Magistris M (1991) Impact of environmental and genetic factors on codeine analgesia. Eur J Clin Pharmacol 41:23-26
11. Eichelbaum M, Gross AS (1990) The genetic polymorphism of debrisoquine/sparteine metabolism-clinical aspects. Pharmacol Ther 46:377-394
12. Fishman J, Hahn EF, Norton BI (1976) N-demethylation of morphine in rat brain is located in sites with high opiate receptor content. Nature 261:64-65
13. Gaedigk A, Blum M, Gaedigk R, Eichelbaum M, Meyer UA (1991) Deletion of the entire cytochrome P450 CYP2D6 gene as a cause of impaired drug metabolism in poor metabolizers of the debrisoquine/sparteine polymorphism. Am J Hum Genet 48:943-950
14. Hiatt EP, Quinn GP (1945) The distribution of quinine, quinidine, cinchonine and cinchonidine in fluids and tissues of dogs J Pharmacol Exp Ther 83:101-105
15. Hofmann U, Fromm MF, Johnson S, Mikus G (1995) Simultaneous determination of dihydrocodeine and dihydromorphme in serum by gas chromatography/tandem mass spectrometry. J Chromatogr 663:59-65
16. Juan H (1977) Inhibition of algesic effect of bradykinin and acetylcholine by mepacrine. Naunyn-Schmiedeberg's Arch Pharmacology 301:23-27
17. Kagimoto M, Heim M, Kagimoto K, Zeugin T, Meyer UA (1990) Multiple mutations of the human cytochrome P450IID6 gene (CYP2D6) in poor metabolizers of debrisoquine. J Biol Chem 265:17209-17214
18. Mikus G, Bochner F, Eichelbaum M, Horak P, Somogyi AA, Spector S (1994) Endogenous codeine and morphine in poor and extensive metabolisers of the CYP2D6 (debrisoquine/ sparteine) polymorphism. J Pharmacol Exp Ther 268: 546-551
19. Nielsen F, Nielsen KK, Brøsen K (1994) Determination of quinidine, dihydroquinidine, (3s)-3-hydroxyquinidine, and quinidine-N-oxide in plasma and urine by high performance liquid chromatography. J Chromatogr 660:103-110
20. Nielsen MD, Brøsen K, Gram LF (1990) A dose-effect study of the in vivo inhibitory effect of quinidine on sparteine oxidation in man. Br J Clin Pharmacol 29:299-304
21. 3H]GBR-12935 binding proteins. Arch Biochem Biophys 276:424-432
22. Oldendorf WH, Hyman S, Braun L, Oldendorf SZ (1972) Blood brain barrier: penetration of morphine, codeine, heroin, and methadone after carotid injection. Science 128: 984-986
23. Otton SV, Inaba T, Kalow W (1984) Competitive inhibition of sparteine oxidation in human liver by beta-adrenoceptor antagonists and other cardiovascular drugs. Life Sci 34:73-80
24. Pasternak GW, Wood PJ (1986) Multiple mu opiate receptors. Life Sci 38:1889-1898
25. Sindrup SH, Brøsen K, Bjerring P, Arendt-Nielsen L, Angelo HR, Larsen U, Gram LF (1990) Codeine increases pain thresholds to copper vapor laser stimuli in extensive but not in poor metabolizers of sparteine. Clin Pharmacol Ther 48:686-693
26. Sindrup SH, Arendt-Nielsen L, Brøsen K, Bjerring P, Angelo HR, Eriksen B, Gram LF (1992) The effect of quinidine on the analgesic effect of codeine. Eur J Clin Pharmacol 42:587-592
27. Sindrup SH, Poulsen L, Brøsen K, Arendt-Nielsen L, Gram LF (1993) Are poor metabolisers of sparteine/debrisoquine less pain tolerant than extensive metabolisers. Pain 53:335-339
28. Tyndale RF, Sunahara R, Inaba T, Kalow W, Gonzales FJ, Niznik HB (1991) Neuronal cytochrome P450IID1 (debrisoquine/ sparteine-type): potent inhibition of activation by (-)-cocaine and nucleotide sequence identity to human hepatic P450 gene CYP2D6. Mol Pharmacol 40:63-68
29. Yue QY, Svensson J-O, Alm C, Sjöqvist F, Säwe J (1989) Codeine O-demethylation co-segregates with polymorphic debrisoquine hydroxylation. Br J Clin Pharmacol 28:639-645
30. Zanger UM, Vilbois F, Hardwick J, Meyer UA (1988) Absence of hepatic cytochrome P450bufI causes genetically deficient debrisoquine oxidation in man. Biochemistry 27:5447-5454