Physiologically-based pharmacokinetic model for Fentanyl in support of the development of Provisional Advisory Levels

Toxicology and Applied Pharmacology

Volumn 273, Issue 3, 2013, Pages 464-476

  Shankaran, Harish ^a   Adeshina, Femi ^b   Teeguarden, Justin G ^a  

^a PACIFIC NORTHWEST NATIONAL LABORATORY   (United States)

^b U S ENVIRONMENTAL PROTECTION AGENCY   (United States)

Author keywords

Anesthetic; Computational modeling; Inhalation; Oral transmucosal; Risk assessment; Route to route extrapolation

Indexed keywords

FENTANYL;

AEROSOL; ARTERIAL CIRCULATION; ARTICLE; CALIBRATION; COMPARTMENT MODEL; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG FORMULATION; HUMAN; NONHUMAN; PAIN; PHARMACOKINETICS; TOXICITY;

ANESTHETIC; COMPUTATIONAL MODELING; INHALATION; ORAL TRANSMUCOSAL; RISK ASSESSMENT; ROUTE-TO-ROUTE EXTRAPOLATION;

ABSORPTION; ADMINISTRATION, INHALATION; ADMINISTRATION, INTRANASAL; ADMINISTRATION, ORAL; ADOLESCENT; ADULT; AGED; AGED, 80 AND OVER; DATABASES, FACTUAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRINKING WATER; DRUG ADMINISTRATION ROUTES; FEMALE; FENTANYL; HUMANS; INHALATION EXPOSURE; MALE; MIDDLE AGED; MODELS, BIOLOGICAL; MONTE CARLO METHOD; RISK ASSESSMENT; SENSITIVITY AND SPECIFICITY; YOUNG ADULT;

EID: 84888882258     PISSN: 0041008X     EISSN: 10960333     Source Type: Journal    
DOI: 10.1016/j.taap.2013.05.024     Document Type: Article

References (73)

1. Abduljalil K., Furness P., Johnson T.N., Rostami-Hodjegan A., Soltani H. Anatomical, physiological and metabolic changes with gestational age during normal pregnancy: a database for parameters required in physiologically based pharmacokinetic modelling. Clin. Pharmacokinet. 2012, 51:365-396.
2. Adeshina F., Sonich-Mullin C., Ross R.H., Wood C.S. Health-based provisional advisory levels (PALs) for homeland security. Inhal. Toxicol. 2009, 21(Suppl. 3):12-16.
3. Beavis R.E., Crotty B., Osborne A., Hochmann M. Epidural fentanyl effect on cardiac output and hepatic blood flow. Anaesth. Intensive Care 1991, 19:28-31.
4. Bentley J.B., Borel J.D., Nenad R.E., Gillespie T.J. Age and fentanyl pharmacokinetics. Anesth. Analg. 1982, 61:968-971.
5. Bjorkman S. Reduction and lumping of physiologically based pharmacokinetic models: prediction of the disposition of fentanyl and pethidine in humans by successively simplified models. J. Pharmacokinet. Pharmacodyn. 2003, 30:285-307.
6. Bjorkman S., Stanski D.R., Verotta D., Harashima H. Comparative tissue concentration profiles of fentanyl and alfentanil in humans predicted from tissue/blood partition data obtained in rats. Anesthesiology 1990, 72:865-873.
7. Bjorkman S., Stanski D.R., Harashima H., Dowrie R., Harapat S.R., Wada D.R., Ebling W.F. Tissue distribution of Fentanyl and Alfentanil in the rat cannot be described by a blood-flow limited model. J. Pharmacokinet. Biopharm. 1993, 21:255-279.
8. Bjorkman S., Wada D.R., Stanski D.R., Ebling W.F. Comparative physiological pharmacokinetics of Fentanyl and Alfentanil in rats and humans based on parametric single-tissue models. J. Pharmacokinet. Biopharm. 1994, 22:381-410.
9. Bjorkman S., Wada D.R., Stanski D.R. Application of physiologic models to predict the influence of changes in body composition and blood flows on the pharmacokinetics of fentanyl and alfentanil in patients. Anesthesiology 1998, 88:657-667.
10. Bois F.Y., Jamei M., Clewell H.J. PBPK modelling of inter-individual variability in the pharmacokinetics of environmental chemicals. Toxicology 2010, 278:256-267.
11. Bouzom F., Ball K., Perdaems N., Walther B. Physiologically based pharmacokinetic (PBPK) modelling tools: how to fit with our needs?. Biopharm. Drug Dispos. 2012, 33:55-71.
12. Brown R.P., Delp M.D., Lindstedt S.L., Rhomberg L.R., Beliles R.P. Physiological parameter values for physiologically based pharmacokinetic models. Toxicol. Ind. Health 1997, 13:407-484.
13. Cartwright P., Prys-Roberts C., Gill K., Dye A., Stafford M., Gray A. Ventilatory depression related to plasma fentanyl concentrations during and after anesthesia in humans. Anesth. Analg. 1983, 62:966-974.
14. CDC National Health and Nutrition Examination Survey Data 2007-2008, U.S. Department of Health and Human Services, Centers for Disease Control and Prevention, Hyattsville, MD, (http://wwwn.cdc.gov/nchs/nhanes/search/nhanes07_08.aspx).
15. Christrup L.L., Foster D., Popper L.D., Troen T., Upton R. Pharmacokinetics, efficacy, and tolerability of fentanyl following intranasal versus intravenous administration in adults undergoing third-molar extraction: a randomized, double-blind, double-dummy, two-way, crossover study. Clin. Ther. 2008, 30:469-481.
16. Clewell H.J., Gentry P.R., Covington T.R., Gearhart J.M. Development of a physiologically based pharmacokinetic model of trichloroethylene and its metabolites for use in risk assessment. Environ. Heal. Perspect. 2000, 108(Suppl. 2):283-305.
17. Darwish M., Tempero K., Kirby M., Thompson J. Pharmacokinetics and dose proportionality of fentanyl effervescent buccal tablets in healthy volunteers. Clin. Pharmacokinet. 2005, 44:1279-1286.
18. Darwish M., Kirby M., Robertson P., Hellriegel E., Jiang J.G. Comparison of equivalent doses of fentanyl buccal tablets and arteriovenous differences in fentanyl pharmacokinetics. Clin. Pharmacokinet. 2006, 45:843-850.
19. Darwish M., Kirby M., Robertson P., Hellriegel E., Jiang J.G. Single-dose and steady-state pharmacokinetics of fentanyl buccal tablet in healthy volunteers. J. Clin. Pharmacol. 2007, 47:56-63.
20. Delic J.I., Lilly P.D., MacDonald A.J., Loizou G.D. The utility of PBPK in the safety assessment of chloroform and carbon tetrachloride. Regul. Toxicol. Pharmacol. 2000, 32:144-155.
21. Dumas E.O., Pollack G.M. Opioid tolerance development: a pharmacokinetic/pharmacodynamic perspective. AAPS J. 2008, 10:537-551.
22. Fredheim O.M., Borchgrevink P.C., Klepstad P., Kaasa S., Dale O. Long term methadone for chronic pain: a pilot study of pharmacokinetic aspects. Eur. J. Pain 2007, 11:599-604.
23. Fung D.L., Eisele J.H. Fentanyl pharmacokinetics in awake volunteers. J. Clin. Pharmacol. 1980, 20:652-658.
24. Glass D., McClanahan M., Koller L., Adeshina F. Provisional advisory levels (PALs) for phosgene (CG). Inhal. Toxicol. 2009, 21(Suppl. 3):73-94.
25. Goldhaber S., Dorman D., Gardner D., Adeshina F. Provisional advisory levels (PALs) for acrylonitrile. Inhal. Toxicol. 2009, 21(Suppl. 3):17-55.
26. Goldstein-Dresner M.C., Davis P.J., Kretchman E., Siewers R.D., Certo N., Cook D.R. Double-blind comparison of oral transmucosal fentanyl citrate with oral meperidine, diazepam, and atropine as preanesthetic medication in children with congenital heart disease. Anesthesiology 1991, 74:28-33.
27. Goromaru T., Matsuura H., Yoshimura N., Miyawaki T., Sameshima T., Miyao J., Furuta T., Baba S. Identification and quantitative determination of fentanyl metabolites in patients by gas chromatography-mass spectrometry. Anesthesiology 1984, 61:73-77.
28. Grape S., Schug S.A., Lauer S., Schug B.S. Formulations of fentanyl for the management of pain. Drugs 2010, 70:57-72.
29. Hudson R.J. Variability of fentanyl pharmacokinetics in neonates. Anesthesia and Analgesia 1986, 65:1369-1370.
30. Ibrahim A.E., Feldman J., Karim A., Kharasch E.D. Simultaneous assessment of drug interactions with low- and high-extraction opioids: application to parecoxib effects on the pharmacokinetics and pharmacodynamics of fentanyl and alfentanil. Anesthesiology 2003, 98:853-861.
31. Kharasch E.D., Hoffer C., Whittington D. Influence of age on the pharmacokinetics and pharmacodynamics of oral transmucosal fentanyl citrate. Anesthesiology 2004, 101:738-743.
32. Kharasch E.D., Whittington D., Hoffer C. Influence of hepatic and intestinal cytochrome P4503A activity on the acute disposition and effects of oral transmucosal fentanyl citrate. Anesthesiology 2004, 101:729-737.
33. Labroo R.B., Paine M.F., Thummel K.E., Kharasch E.D. Fentanyl metabolism by human hepatic and intestinal cytochrome P450 3A4: implications for interindividual variability in disposition, efficacy, and drug interactions. Drug Metab. Dispos. 1997, 25:1072-1080.
34. Lee M., Kern S.E., Kisicki J.C., Egan T.D. A pharmacokinetic study to compare two simultaneous 400 microg doses with a single 800 microg dose of oral transmucosal fentanyl citrate. J. Pain Symptom Manage. 2003, 26:743-747.
35. Lennernas B., Hedner T., Holmberg M., Bredenberg S., Nystrom C., Lennernas H. Pharmacokinetics and tolerability of different doses of fentanyl following sublingual administration of a rapidly dissolving tablet to cancer patients: a new approach to treatment of incident pain. Br. J. Clin. Pharmacol. 2005, 59:249-253.
36. Lim C.B., Paech M.J., Sunderland V.B., Roberts M.J., Banks S.L., Rucklidge W.M. Pharmacokinetics of nasal fentanyl. J. Pharm. Pract. Res. 2003, 33:59-63.
37. Lind G.H., Marcus M.A., Mears S.L., Ashburn M.A., Peterson B.J., Bernhisel K.T., Stanley T.H. Oral transmucosal fentanyl citrate for analgesia and sedation in the emergency department. Ann. Emerg. Med. 1991, 20:1117-1120.
38. Marshall T., Dorman D., Gardner D., Adeshina F. Provisional advisory levels (PALs) for hydrogen sulfide (H2S). Inhal. Toxicol. 2009, 21(Suppl. 3):56-72.
39. Mather L.E. Clinical pharmacokinetics of fentanyl and its newer derivatives. Clin. Pharmacokinet. 1983, 8:422-446.
40. Mather L.E., Woodhouse A., Ward M.E., Farr S.J., Rubsamen R.A., Eltherington L.G. Pulmonary administration of aerosolised fentanyl: pharmacokinetic analysis of systemic delivery. Br. J. Clin. Pharmacol. 1998, 46:37-43.
41. McClain D.A., Hug C.C. Intravenous fentanyl kinetics. Clin. Pharmacol. Ther. 1980, 28:106-114.
42. McQuay H.J., Moore R.A., Paterson G.M., Adams A.P. Plasma fentanyl concentrations and clinical observations during and after operation. Br. J. Anaesth. 1979, 51:543-550.
43. Mildh L.H., Scheinin H., Kirvela O.A. The concentration-effect relationship of the respiratory depressant effects of alfentanil and fentanyl. Anesth. Analg. 2001, 93:939-946.
44. Miller F.J., Schlosser P.M., Janszen D.B. Haber's rule: a special case in a family of curves relating concentration and duration of exposure to a fixed level of response for a given endpoint. Toxicology 2000, 149:21-34.
45. Modesti C., Sacco T., Morelli G., Bocci M.G., Ciocchetti P., Vitale F., Perilli V., Sollazzi L. Balanced anestesia versus total intravenous anestesia for kidney transplantation. Minerva Anestesiol. 2006, 72:627-635.
46. Peng P.W., Sandler A.N. A review of the use of fentanyl analgesia in the management of acute pain in adults. Anesthesiology 1999, 90:576-599.
47. Price P.S., Conolly R.B., Chaisson C.F., Gross E.A., Young J.S., Mathis E.T., Tedder D.R. Modeling interindividual variation in physiological factors used in PBPK models of humans. Crit. Rev. Toxicol. 2003, 33:469-503.
48. Riches J.R., Read R.W., Black R.M., Cooper N.J., Timperley C.M. Analysis of clothing and urine from Moscow theatre siege casualties reveals carfentanil and remifentanil use. J. Anal. Toxicol. 2012, 36:647-656.
49. Sawe J., Svensson J.O., Rane A. Morphine metabolism in cancer patients on increasing oral doses-no evidence for autoinduction or dose-dependence. Br. J. Clin. Pharmacol. 1983, 16:85-93.
50. Schiermeier Q. Hostage deaths put gas weapons in spotlight. Nature 2002, 420:7.
51. Scott J.C., Stanski D.R. Decreased fentanyl and alfentanil dose requirements with age. A simultaneous pharmacokinetic and pharmacodynamic evaluation. J. Pharmacol. Exp. Ther. 1987, 240:159-166.
52. Scott J.C., Cooke J.E., Stanski D.R. Electroencephalographic quantitation of opioid effect: comparative pharmacodynamics of fentanyl and sufentanil. Anesthesiology 1991, 74:34-42.
53. Silverstein J.H., Rieders M.F., McMullin M., Schulman S., Zahl K. An analysis of the duration of fentanyl and its metabolites in urine and saliva. Anesth. Analg. 1993, 76:618-621.
54. Singleton M.A., Rosen J.I., Fisher D.M. Pharmacokinetics of fentanyl in the elderly. Br. J. Anaesth. 1988, 60:619-622.
55. Stanley T.H., Hague B., Mock D.L., Streisand J.B., Bubbers S., Dzelzkalns R.R., Bailey P.L., Pace N.L., East K.A., Ashburn M.A. Oral transmucosal fentanyl citrate (lollipop) premedication in human volunteers. Anesth. Analg. 1989, 69:21-27.
56. Stoeckel H., Schuttler J., Magnussen H., Hengstmann J.H. Plasma fentanyl concentrations and the occurrence of respiratory depression in volunteers. Br. J. Anaesth. 1982, 54:1087-1095.
57. Striebel H.W., Kramer J., Luhmann I., Rohierse-Hohler I., Rieger A. Pharmacokinetics of intranasal Fentanyl. Schmerz 1993, 7:122-125.
58. Streisand J.B., Stanley T.H., Hague B., van Vreeswijk H., Ho G.H., Pace N.L. Oral transmucosal fentanyl citrate premedication in children. Anesth. Analg. 1989, 69:28-34.
59. Streisand J.B., Varvel J.R., Stanski D.R., Le Maire L., Ashburn M.A., Hague B.I., Tarver S.D., Stanley T.H. Absorption and bioavailability of oral transmucosal fentanyl citrate. Anesthesiology 1991, 75:223-229.
60. Streisand J.B., Busch M.A., Egan T.D., Smith B.G., Gay M., Pace N.L. Dose proportionality and pharmacokinetics of oral transmucosal fentanyl citrate. Anesthesiology 1998, 88:305-309.
61. Sweeney B.P., Bromilow J. Liver enzyme induction and inhibition: implications for anaesthesia. Anaesthesia 2006, 61:159-177.
62. Tan Y.M., Liao K.H., Conolly R.B., Blount B.C., Mason A.M., Clewell H.J. Use of a physiologically based pharmacokinetic model to identify exposures consistent with human biomonitoring data for chloroform. J. Toxicol. Environ. Health A 2006, 69:1727-1756.
63. Tan Y.M., Liao K.H., Clewell H.J. Reverse dosimetry: interpreting trihalomethanes biomonitoring data using physiologically based pharmacokinetic modeling. J. Expo. Sci. Environ. Epidemiol. 2007, 17:591-603.
64. Tanaka E. Clinically important pharmacokinetic drug-drug interactions: role of cytochrome P450 enzymes. J. Clin. Pharm. Ther. 1998, 23:403-416.
65. ten Berge W.F., Zwart A., Appelman L.M. Concentration-time mortality response relationship of irritant and systemically acting vapours and gases. J. Hazard Mater. 1986, 13:301-309.
66. Thompson C.M., Johns D.O., Sonawane B., Barton H.A., Hattis D., Tardif R., Krishnan K. Database for physiologically based pharmacokinetic (PBPK) modeling: physiological data for healthy and health-impaired elderly. J. Toxicol. Environ. Health B Crit. Rev. 2009, 12:1-24.
67. Upton R.N., Foster D.J., Christrup L.L., Dale O., Moksnes K., Popper L. A physiologically-based recirculatory meta-model for nasal fentanyl in man. J. Pharmacokinet. Pharmacodyn. 2012, 39:561-576.
68. Waara-Wolleat K.L., Hildebrand K.R., Stewart G.R. A review of intrathecal fentanyl and sufentanil for the treatment of chronic pain. Pain Med. 2006, 7:251-259.
69. Wheeler M., Birmingham P.K., Dsida R.M., Wang Z., Cote C.J., Avram M.J. Uptake pharmacokinetics of the Fentanyl Oralet in children scheduled for central venous access removal: implications for the timing of initiating painful procedures. Paediatr. Anaesth. 2002, 12:594-599.
70. Wheeler M., Birmingham P.K., Lugo R.A., Heffner C.L., Cote C.J. The pharmacokinetics of the intravenous formulation of fentanyl citrate administered orally in children undergoing general anesthesia. Anesth. Analg. 2004, 99:1347-1351. (table of contents).
71. Yassen A., Kan J.M., Olofsen E., Suidgeest E., Dahan A., Danhof M. Mechanism-based pharmacokinetic-pharmacodynamic modeling of the respiratory-depressant effect of buprenorphine and fentanyl in rats. J. Pharmacol. Exp. Ther. 2006, 319:682-692.
72. Yokley K., Tran H.T., Pekari K., Rappaport S., Riihimaki V., Rothman N., Waidyanatha S., Schlosser P.M. Physiologically-based pharmacokinetic modeling of benzene in humans: a Bayesian approach. Risk Anal. 2006, 26:925-943.
73. Young R.A., Bast C.B., Wood C.S., Adeshina F. Overview of the standing operating procedure (SOP) for the development of provisional advisory levels (PALs). Inhal. Toxicol. 2009, 21(Suppl. 3):1-11.