Buprenorphine alters desmethylflunitrazepam disposition and flunitrazepam toxicity in rats

Toxicological Sciences

Volumn 106, Issue 1, 2008, Pages 64-73

  Pirnay, Stéphane ^a,b   Megarbane, Bruno ^a,c   Declèves, Xavier ^a   Risède, Patricia ^a   Borron, Stephen W ^d   Bouchonnet, Stéphane ^e   Perrin, Bérangère ^b   Debray, Marcel ^a,f   Milan, Nathalie ^b   Duarte, Tania ^a   Ricordel, Ivan ^b   Baud, Frédéric J ^a,c  

^a INSERM   (France)

^b Centre Universitaire des Saints Pères   (France)

^c HÔPITAL LARIBOISIÈRE   (France)

^d Mays Cancer Center at UT Health San Antonio   (United States)

^e LABORATOIRE HÉTÉROÉLÉMENTS ET COORDINATION   (France)

^f UNIVERSITÉ PARIS DESCARTES   (France)

Author keywords

Buprenorphine; Desmethylflunitrazepam; Flunitrazepam; Interaction; Metabolism; Pharmacokinetics

Indexed keywords

7 AMINOFLUNITRAZEPAM; BUPRENORPHINE; FLUNITRAZEPAM; NORFLUNITRAZEPAM;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTERIAL CARBON DIOXIDE TENSION; ARTICLE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISPOSITION; DRUG HALF LIFE; DRUG MEGADOSE; DRUG POTENTIATION; GAS CHROMATOGRAPHY; LUNG TOXICITY; LUNG VENTILATION; MALE; MASS SPECTROMETRY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PHARMACODYNAMICS; RAT; RESPIRATION DEPRESSION; SPRAGUE DAWLEY RAT;

ANALGESICS, OPIOID; ANIMALS; BIOTRANSFORMATION; BUPRENORPHINE; CARBON DIOXIDE; DRUG INTERACTIONS; FLUNITRAZEPAM; GABA MODULATORS; HYDROGEN-ION CONCENTRATION; INFUSIONS, INTRAVENOUS; MALE; OXYGEN; PULMONARY VENTILATION; RATS; RATS, SPRAGUE-DAWLEY; RESPIRATORY INSUFFICIENCY;

RATTUS;

EID: 54349104507     PISSN: 10966080     EISSN: 10960929     Source Type: Journal    
DOI: 10.1093/toxsci/kfn163     Document Type: Article

References (48)

1. Becherucci, C., Palmi, M., and Segre, G. (1985). Pharmacokinetics of flunitrazepam in rats studied by a radioreceptor assay. Pharmacol. Res. Commun. 17, 733-747.
2. Berthault, F., Kintz, P., and Mangin, P. (1996). Simultaneous high-performance liquid chromatographic analysis of flunitrazepam and four metabolites in serum. J. Chromatogr. B Biomed. Appl. 685 383-387.
3. Borron, S. W., Monier, C., Risede, P., and Baud, F. J. (2002). Flunitrazepam variably alters morphine, buprenorphine, and methadone lethality in the rat. Hum. Exp. Toxicol. 21, 599-605.
4. Buckley, N. A., and McManus, P. R. (2004). Changes in fatalities due to overdose of anxiolytic and sedative drugs in the UK (1983-1999). Drug Saf. 27, 135-141.
5. Coller, J. K., Somogyi, A. A., and Bochner, F. (1998). Quantification of flunitrazepam's oxidative metabolites, 3-hydroxyflunitrazepam and desmethylflunitrazepam, in hepatic microsomal incubations by high-performance liquid chromatography. J. Chromatogr. B Biomed. Sci. Appl. 719, 87-92.
6. Cowan, A. (1995). Update on the general pharmacology of buprenorphine. In Buprenorphine: Combating Drug Abuse With a Unique Opioid (A. Cowan and J. W. Lewis, Eds.), pp. 31-47. Wiley-Liss, New York.
7. Cowan, A. (2003). Buprenorphine: New pharmacological aspects. Int. J. Clin. Pract. Suppl. 3-8.
8. Cowan, A., Doxey, J., and Harry, E. (1977). The animal pharmacology of buprenorphine, an oripavine analgesic agent. Br. J. Pharmacol. 60, 547-554.
9. Dahan, A., Yassen, A., Bijl, H., Romberg, R., Sarton, E., Teppema, L., Olofsen, E., and Danhof, M. (2005). Comparison of the respiratory effects of intravenous buprenorphine and fentanyl in humans and rats. Br. J. Anaesth 94, 825-834.
10. Dahan, A., Yassen, A., Romberg, R., Sarton, E., Teppema, L., Olofsen, E., and Danhof, M. (2006). Buprenorphine induces ceiling in respiratory depression but not in analgesia. Br. J. Anaesth. 96, 627-632.
11. Drouet-Coassolo, C., Iliadis, A., Coassolo, P., Antoni, M., and Cano, J. P. (1990). Pharmacokinetics of flunitrazepam following single dose oral administration in liver disease patients compared with healthy volunteers. Fundam. Clin. Pharmacol. 4, 643-651.
12. Druid, H., Holmgren, P., and Ahlner, J. (2001). Flunitrazepam: An evaluation of use, abuse and toxicity. Forensic Sci. Int. 122 136-141.
13. Drummer, O. H., Syrjanen, M. L., and Cordner, S. M. (1993). Deaths involving the benzodiazepine flunitrazepam. Am. J. Forensic Med. Pathol. 14, 238-243.
14. Emmanuelli, J., and Desenclos, J. C. (2005). Harm reduction interventions, behaviors and associated health outcomes in France, 1996-2003. Addiction 100, 1690-1700.
15. Garretty, D. J., Wolff, K., Hay, A. W., and Raistrick, D. (1997). Benzodiazepine misuse by drug addicts. Ann. Clin. Biochem. 34 68-73.
16. Gueye, P. N., Borron, S. W., Risede, P., Monier, C., Buneaux, F., Debray, M., and Baud, F. J. (2002a). Buprenorphine and midazolam act in combination to depress respiration in rats. Toxicol. Sci. 65 107-114.
17. Gueye, P. N., Borron, S. W., Risede, P., Monier, C., Buneaux, F., Debray, M., and Baud, F. J. (2001). Lack of effect of single high doses of buprenorphine on arterial blood gases in the rat. Toxicol. Sci. 62, 148-154.
18. Gueye, P. N., Megarbane, B., Borron, S. W., Adnet, F., Galliot-Guilley, M., Ricordel, I., Tourneau, J., Goldgran-Toledano, D., and Baud, F. J. (2002b). Trends in opiate and opioid poisonings in addicts in north-east Paris and suburbs, 1995-99. Addiction 97, 1295-1304.
19. Heel, R. C., Brogden, R. N., Speight, T. M., and Avery, G. S. (1979). Buprenorphine: A review of its pharmacological properties and therapeutic efficacy. Drugs 17, 81-110.
20. Henry, J. (1999). Fatal opioid toxicity - A clinical perspective. Addiction 94, 974-975.
21. Hesse, L. M., Venkatakrishnan, K., von Moltke, L. L., Shader, R. I., and Greenblatt, D. J. (2001). CYP3A4 is the major CYP isoform mediating the in vitro hydroxylation and demethylation of flunitrazepam. Drug Metab. Dispos. 29, 133-140.
22. Hojer, J., Baehrendtz, S., and Gustafsson, L. (1989). Benzodiazepine poisoning: Experience of 702 admissions to an intensive care unit during a 14-year period. J. Intern. Med. 226, 117-122.
23. Ibrahim, R. B., Wilson, J. G., Thorsby, M. E., and Edwards, D. J. (2000). Effect of buprenorphine on CYP3A activity in rat and human liver microsomes. Life Sci. 66, 1293-1298.
24. Kilicarslan, T., Haining, R. L., Rettie, A. E., Busto, U., Tyndale, R. F., and Sellers, E. M. (2001). Flunitrazepam metabolism by cytochrorne P450S 2C19 and 3A4. Drug Metab. Dispos. 29, 460-465.
25. Kilicarslan, T., and Sellers, E. M. (2000). Lack of interaction of buprenorphine with flunitrazepam metabolism. Am. J. Psychiatry 157, 1164-1166.
26. Kintz, P. (2001). Deaths involving buprenorphine: A compendium of French cases. Forensic Sci. Int. 121, 65-69.
27. Korttila, K., and Linnoila, M. (1976). Amnesic action of and skills related to driving after intravenous flunitrazepam. Acta Anaesthesiol. Scand. 20, 160-168.
28. Lai, S. H., Yao, Y. J., and Lo, D. S. (2006). A survey of buprenorphine related deaths in Singapore. Forensic Sci. Int. 162, 80-86.
29. Libong, D., Pirnay, S., Bruneau, C., Rogalewicz, F., Ricordel, I., and Bouchonnet, S. (2003). Adsorption-desorption effects in ion trap mass spectrometry using in situ ionization. J. Chromatogr. A 1010 123-128.
30. Mandema, J. W., Sansom, L. N., Dios-Vièitez, M. C., Hollander-Jansen, M., and Danhof, M. (1991). Pharmacokinetic-pharmacodynaniic modeling of the electroencephalographic effects of benzodiazepines. Correlation with receptor binding and anticonvulsant activity. J. Pharmacol. Exp. Ther. 257, 472-478.
31. Maruyama, T., Furuie, M. A., Hibino, S., and Otagiri, M. (1992). Comparative study of interaction mode of diazepines with human serum albumin and alpha 1-acid glycoprotein. J. Pharm. Sci. 81, 16-20.
32. McCormick, G. Y., White, W. J., Zagon, I. S., and Lang, C. M. (1984). Effects of diazepam on arterial blood gas concentrations and pH of adult rats acutely and chronically exposed to methadone. J. Pharmacol. Exp. Ther. 230, 353-359.
33. Mégarbane, B., Lesguillons, N., Galliot-Guilley, M., Borron, S. W., Trout, H., Declèves, X., Risède, P., Monier, C., Boschi, G., and Baud, F. J. (2005b). Cerebral and plasma kinetics of a high dose of midazolam and correlations with its respiratory effects in rats. Toxicol. Lett. 159, 22-31.
34. Mégarbane, B., Pirnay, S., Borron, S. W., Trout, H., Monier, C., Risède, P., Boschi, G., and Baud, F. J. (2005a). Flunitrazepam does not alter cerebral distribution of buprenorphine in the rat. Toxicol. Lett. 157, 211-219.
35. Nielsen, S., and Taylor, D. A. (2005). The effect of buprenorphine and benzodiazepines on respiration in the rat. Drug Alcohol Depend 79, 95-101.
36. Ohtani, M., Kotaki, H., Nishitateno, K., Sawada, Y., and Iga, T. (1997). Kinetics of respiratory depression in rats induced by buprenorphine and its metabolite, norbuprenorphine. J. Pharmacol. Exp. Ther. 281 428-433.
37. Pirnay, S., Borron, S., Giudicelli, C., Tourneau, J., Baud, F. J., and Ricordel, I. (2004a). A critical review of the causes of death among post-mortem toxicological investigations: Analysis of 34 buprenorphine-associated and 35 methadone-associated deaths. Addiction 99, 978-988.
38. Pirnay, S., Bouchonnet, S., Herve, F., Libong, D., Milan, N., D'Athis, P., Baud, F. J., and Ricordel, I. (2004b). Development and validation of a gas chromatography-mass spectrometry method for the simultaneous determination of buprenorphine, flunitrazepam and their metabolites in rat plasma: Application to the pharmacokinetic study. J. Chromatogr. B Anal. Technol. Biomed Life Sci. 807, 335-342.
39. Pirnay, S., Ricordel, I., Libong, D., and Bouchonnet, S. (2002). Sensitive method for the detection of 22 benzodiazepines by gas chromatography-ion trap tandem mass spectrometry. J. Chromatogr. A 954, 235-245.
40. Randall, L. O., and Kappell, B. (1973). Pharmacological activity of some benzodiazepines and their metabolites. In The Benzodiazepines (S. Garattini, L. O. Randall, and E. Mussini, Eds.), pp. 27-51. Raven Press, New York.
41. Reynaud, M., Tracqui, A., Petit, G., Potard, D., and Courty, P. (1998). Six deaths linked to misuse of buprenorphine-benzodiazepine combinations. Am. J. Psychiatry 155, 448-449.
42. Shah, V. P., Midlia, K. K., Findlay, J. W., Hill, H. M., Hulse, J. D., McGilveray, I. J., McKay, G., Miller, K. J., Patnaik, R. N., Powell, M. L., et al. (2000). Bioanalytical method validation - A revisit with a decade of progress. Pharm. Res. 17, 1551-1557.
43. Tracqui, A., Kintz, P., and Ludes, B. (1999). Buprenorphine-related deaths among drug addicts in France: A report on 20 fatalities. J. Anal. Toxicol. 22, 430-434.
44. Umehara, K., Shimokawa, Y., and Miyamoto, G. (2002). Inhibition of human drug metabolizing cytochrome P450 by buprenorphine. Biol. Pharm. Bull. 25, 682-685.
45. Verborgh, C., De Coster, R., D'Haese, J., Camu, F., and Meert, T. F. (1998). Effects of chlordiazepoxide on opioid-induced antinociception and respiratory depression depression in restrained rats. Pain 37, 103-110.
46. Verwey, B., Eling, P., Wientjes, H., and Zitman, F. G. (2000). Memory impairment in those who attempted suicide by benzodiazepine overdose. J. Clin. Psychiatry 61, 456-459.
47. Walsh, S., Preston, K., Stitzer, M., Cone, E., and Bigelow, G. (1994). Clinical pharmacology of buprenorphine: Ceiling effect at high doses. Clin. Pharmacol. Ther. 65, 569-590.
48. Zbinden, G., and Randall, L. O. (1967). Pharmacology of benzodiazepines: Laboratory and clinical correlations. In Advances in Pharmacology (S. Garattini and P. A. Shore, Eds.), pp. 213-291. Academic Press, New York.