Uncertainty factors for chemical risk assessment: Human variability in the pharmacokinetics of CYP1A2 probe substrates

Food and Chemical Toxicology

Volumn 39, Issue 7, 2001, Pages 681-696

  Dorne, J L C M ^a   Walton, K ^a   Renwick, A G ^a  

^a UNIVERSITY OF SOUTHAMPTON   (United Kingdom)

Author keywords

CYP1A2; Human variability; Pharmacokinetics; Risk assessment; Sensitive subgroups; Uncertainty factors

Indexed keywords

CAFFEINE; CYTOCHROME P450 1A2; PARAXANTHINE; THEOBROMINE; THEOPHYLLINE; WARFARIN;

AGE; AREA UNDER THE CURVE; ARTICLE; DRUG METABOLISM; ETHNIC DIFFERENCE; HUMAN; HUMAN FACTORS RESEARCH; KIDNEY CLEARANCE; KIDNEY DISEASE; LIVER CLEARANCE; LIVER DISEASE; LONG TERM EXPOSURE; MAXIMUM ALLOWABLE CONCENTRATION; METABOLIC CLEARANCE RATE; PARAMETER; PREGNANCY; RISK ASSESSMENT; SMOKING AND SMOKING RELATED PHENOMENA; TECHNIQUE; TOXICOKINETICS;

ADULT; AGED; AREA UNDER CURVE; CAFFEINE; CHILD; CYTOCHROME P-450 CYP1A2; HUMANS; INFANT, NEWBORN; MODELS, BIOLOGICAL; PHARMACOKINETICS; PROBABILITY; REPRODUCIBILITY OF RESULTS; RISK ASSESSMENT; SUBSTRATE SPECIFICITY; THEOBROMINE; THEOPHYLLINE; WARFARIN;

EID: 0034993738     PISSN: 02786915     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0278-6915(01)00005-9     Document Type: Article

References (129)

1. Studies on the use of uncertainty factors in deriving RfDs
2. Selective inhibition of warfarin metabolism by diltiazem in humans
3. The disposition of caffeine during and after pregnancy
4. Effect of venlaflaxine on CYP-1A2-dependent pharmacokinetics and metabolism of caffeine
5. Theophylline pharmacokinetics and liver function indexes in chronic liver disease
6. Pharmacokinetic profile of caffeine in the premature newborn infant with apnea
7. Pharmacokinetics of diuretics and methylxanthines in the neonate
8. A comparison of the pharmacokinetics of theophylline in asthmatic children in the acute episode and in remission
9. Theophylline kinetics in chronic obstructive airway disease in the elderly
10. The effect of acute and chronic renal failure on theophylline clearance
11. Inhibition of elimination of caffeine by disulfiram in normal subjects and recovering alcoholics
12. Theophylline in childhood asthma. Pharmacokinetic and clinical study
13. Comparison of theophylline and theobromine metabolism in man
14. The absolute bioavailability of caffeine in man
15. Comparative pharmacokinetics of caffeine in young and elderly men
16. Pharmacokinetics of theophylline in young and elderly subjects
17. Pharmacokinetics of caffeine during and after pregnancy
18. Addressing human variability in risk assessment - The robustness of the intraspecies uncertainty factor
19. Human cytochrome P-450(PA) (P-450IA2), the phenacetin O-deethylase, is primarily responsible for the hepatic 3-demethylation of caffeine and N-oxidation of carcinogenic arylamines
20. Uncertainty factors and interindividual variation
21. Biotransformation of caffeine, paraxanthine, theophylline, and theobromine by polycyclic aromatic hydrocarbon-inducible cytochrome(s) P-450 in human liver microsomes
22. A urinary metabolite ratio that reflects systemic caffeine clearance
23. Biotransformation of caffeine in human liver microsomes from foetuses, neonates, infants and adults
24. Kinetics of intravenous theophylline
25. Oxidation of caffeine to theobromine and theophylline is catalyzed primarily by flavin-containing monooxygenase in liver microsomes
26. Disposition of a flow-limited drug (lidocaine) and a metabolic capacity-limited drug (theophylline) in liver cirrhosis
27. Onset of xenobiotic metabolism in children: Toxicological implications
28. Theophylline kinetics in relation to age: The importance of smoking
29. Famotidine and theophylline pharmacokinetics. An unexpected cimetidine-like interaction in patients with chronic obstructive pulmonary disease
30. Dose-dependency of caffeine metabolism with repeated dosing
31. The effect of liver disease on urine caffeine metabolite ratios
32. Impaired elimination of caffeine in cirrhosis
33. Evolution of science-based uncertainty factors in noncancer risk assessment
34. Regulatory history and experimental support of uncertainty (safety) factors
35. Hepatic drug metabolism and aging
36. Role of cytochrome P4501A2 in chemical carcinogenesis: Implications for human variability in expression and enzyme activity
37. Disposition of intravenous theophylline in asthmatic children: Bayesian approach vs direct pharmacokinetic calculations
38. Pharmacokinetics of theophylline in children with asthma
39. Farmacocinetica de cafeina en pacientes enestado critico
40. Caffeine based measures of CYP IA2 activity correlate with oral clearance of tacrine in patients with Alzheimer's disease
41. Theophylline kinetics in a geriatric group
42. Theophylline pharmacokinetics in pregnancy
43. Biotransformation of caffeine and theophylline in mammalian cell lines genetically engineered for expression of single cytochrome P450 isoforms
44. Theophylline disposition in obesity
45. Effects of tobacco smoking and oral contraceptive use on theophylline disposition
46. Cytochrome P450 isoform selectivity in human hepatic theobromine metabolism
47. Theophylline pharmacokinetics in premature infants with apnea
48. Effect of formula feeding on oral absorption of caffeine in premature infants
49. Factors influencing theophylline disposition in 179 newborns
50. Caffeine pharmacokinetics in the neonate
51. Pharmacokinetic aspects of caffeine in premature infants with apnoea
52. Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1
53. Risk evaluation: Criteria arising from legal traditions and experience with quantitative risk assessment in the United States
54. Human variability in susceptibility to toxic chemicals - A preliminary analysis of pharmacokinetic data from normal individuals
55. The mechanism of the interaction between amiodarone and warfarin in humans
56. Factors affecting theophylline pharmacokinetics in premature infants with apnea
57. Bioavailability and pharmacokinetics of theophylline following plain uncoated and sustained-release dosage forms in relation to smoking habit. II. Multiple dose study
58. Theophylline pharmacokinetics in black Zimbabwean males
59. Gender differences in hepatic induction and inhibition of theophylline pharmacokinetics and metabolism
60. Influence of smoking on caffeine elimination in healthy volunteers and in patients with alcoholic liver cirrhosis
61. Influence of race or ethnicity on pharmacokinetics of drugs
62. Predictability of the effects of race or ethnicity on pharmacokinetics of drugs
63. Chronopharmacokinetics of theophylline after sustained release and intravenous administration to adults
64. Effects of altitude (4300 M) on the pharmacokinetics of caffeine and cardio-green in humans
65. Human P450 metabolism of warfarin, 1997
66. Dose-dependent pharmacokinetics and psychomotor effects of caffeine in humans
67. The pharmacokinetics of theophylline and enprofylline in patients with liver cirrhosis and in patients with chronic renal disease
68. Effect of hemodialysis on the pharmacokinetics of theophylline in chronic renal failure
69. Alterations in theophylline metabolism during the first year of life
70. Tacrine is not an ideal probe drug for measuring CYP1A2 activity in vivo
71. The aging liver. Drug clearance and an oxygen diffusion barrier hypothesis
72. 100-fold margin of safety
73. Quantitative assessment of caffeine partial clearances in man
74. Comparative pharmacokinetics of caffeine and its primary demethylated metabolites paraxanthine, theobromine and theophylline in man
75. Paraxanthine metabolism in humans: Determination of metabolic partial clearances and effects of allopurinol and cimetidine
76. Pharmacokinetic changes during pregnancy and their clinical relevance
77. Individual and combined effects of cimetidine and ciprofloxacin on theophylline metabolism in male nonsmokers
78. Aging and drug interactions. III. Individual and combined effects of cimetidine and ciprofloxacin on theophylline metabolism in healthy male and female nonsmokers
79. Pharmacokinetic analysis of the disposition of intravenous theophylline in young children
80. Pharmacokinetics of theophylline in hepatic disease
81. Effect of cimetidine on caffeine disposition in smokers and nonsmokers
82. Uncertainty and variability in human exposures to soil contaminants through home-grown food: A Monte Carlo assessment
83. Theobromine metabolism in man
84. Influence of cimetidine, sulfinpyrazone, and cigarette smoking on theobromine metabolism in man
85. The effect of smoking on caffeine elimination: Implications for its use as a semiquantitative test of liver function
86. Phenotyping of CYP1A2 in Japanese population by analysis of caffeine urinary metabolites: Absence of mutation prescribing the phenotype in the CYP1A2 gene
87. Scientific basis for uncertainty factors used to establish occupational exposure limits for pharmaceutical active ingredients
88. Use of toxicokinetic and toxicodynamic data to reduce uncertainties when setting occupational exposure limits for pharmaceuticals
89. Plasma and salivary pharmacokinetics of caffeine in man
90. Phenotypic polymorphism and gender-related differences of CYP1A2 activity in a Chinese population
91. Drug metabolism in pregnancy, infancy and childhood
92. Pharmacokinetic and clinical study of controlled release theophylline: Administration to 20 infants from 6 to 38 months old
93. Theophylline disposition in patients with hepatic cirrhosis
94. 2 breath test
95. Safety factors and establishment of acceptable daily intakes
96. Data-derived safety factors for the evaluation of food additives and environmental contaminants
97. Inter-ethnic differences in xenobiotic metabolism
98. Human variability and noncancer risk assessment - An analysis of the default uncertainty factor
99. Toxicokinetics in infants and children in relation to the ADI and TDI
100. An analysis of the need for an additional uncertainty factor for infants and children
101. Theophylline pharmacokinetics after intramuscular administration
102. Elimination of theobromine metabolites in healthy adults, 1996
103. Pharmacokinetics of intravenous theophylline in pregnant patients at term
104. Theophylline pharmacokinetics in the young infant
105. Functional significance of a C- > A polymorphism in intron 1 of the cytochrome P450 CYP1A2 gene tested with caffeine
106. Pharmacokinetics of intravenous caffeine in critically ill patients
107. Caffeine clearance and biotransformation in patients with chronic liver disease
108. Theophylline pharmacokinetics in normal elderly subjects
109. High levels of methylxanthines in chocolate do not alter theobromine disposition
110. Establishing data-derived uncertainty factors from published pharmaceutical clinical trial data
111. Delayed ontogenesis of CYP1A2 in the human liver
112. Determination of human hepatic cytochrome P4501A2 activity in vitro use of tacrine as an isoenzyme-specific probe
113. Pharmacokinetics and metabolism of theophylline in patients with liver diseases
114. Pharmacokinetics of theophylline in premature infants on the first day of life
115. The pharmacokinetics of theophylline in pregnancy
116. Disposition of caffeine and its metabolites in man
117. Caffeine as a probe for CYP1A2 activity: Potential influence of renal factors on urinary phenotypic trait measurements
118. Estimation of cytochrome P-450 CYP1A2 activity in 863 healthy Caucasians using a saliva-based caffeine test
119. Theobromine kinetics and metabolic disposition
120. The effect of vitamin C on the pharmacokinetics of caffeine in elderly men
121. The concept of the acceptable daily intake: An historical review
122. Uncertainty factors for chemical risk assessment: Interspecies differences in the in vivo pharmacokinetics and metabolism of CYP1A2 substrates
123. Principles for the safety assessment of food additives and contaminants in food
124. International programme on chemical safety: Assessing human health risks of chemicals: Derivation of guidance values for health-based exposure limits
125. Principles for the assessment of risks to human health from exposure to chemicals
126. Caffeine clearance by two point analysis: A measure of liver function in chronic liver disease
127. Evaluation of theophylline clearance in children with bronchial asthma
128. Characterization of human cytochromes P450 involved in theophylline 8-hydroxylation
129. Relationship between caffeine concentrations in plasma and saliva