Uncertainty factors for chemical risk assessment: Interspecies differences in the in vivo pharmacokinetics and metabolism of human CYP1A2 substrates

Food and Chemical Toxicology

Volumn 39, Issue 7, 2001, Pages 667-680

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

^a UNIVERSITY OF SOUTHAMPTON   (United Kingdom)

Author keywords

CYP1A2; Interspecies; Metabolism; Toxicokinetics; Uncertainty factors

Indexed keywords

BIOCHEMICAL MARKER; CAFFEINE; CYTOCHROME P450 1A2; N DEMETHYLASE; PARAXANTHINE; THEOBROMINE; THEOPHYLLINE;

ABSORPTION; AREA UNDER THE CURVE; ARTICLE; BIOAVAILABILITY; BIOTRANSFORMATION; BODY WEIGHT; DRUG METABOLISM; EXCRETION; HUMAN; IN VIVO STUDY; LIVER BLOOD FLOW; LIVER WEIGHT; MAXIMUM ALLOWABLE CONCENTRATION; METABOLIC CLEARANCE RATE; NONHUMAN; RISK ASSESSMENT; SPECIES DIFFERENCE; TOXICOKINETICS;

ANIMALS; CAFFEINE; CYTOCHROME P-450 CYP1A2; DOGS; HUMANS; MICE; MODELS, BIOLOGICAL; PHARMACOKINETICS; PROBABILITY; RABBITS; RATS; REPRODUCIBILITY OF RESULTS; RISK ASSESSMENT; SPECIES SPECIFICITY; SUBSTRATE SPECIFICITY; THEOBROMINE; THEOPHYLLINE;

ANIMALIA; CANIS FAMILIARIS; ORYCTOLAGUS CUNICULUS;

EID: 0034988335     PISSN: 02786915     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0278-6915(01)00006-0     Document Type: Article

References (120)

1. The effects of phenobarbital and beta-naphthoflavone on the elimination kinetics and metabolite pattern of caffeine in the beagle dog
2. Stimulation of caffeine metabolism in the rat by 3-methylcholanthrene
3. Relationship between the clearance of caffeine and its 7-N-demethylation in developing beagle puppies
4. Caffeine metabolism in the new-born
5. Effects of chronic left ventricular failure on hepatic oxygenation and theophylline elimination in the rat
6. Accelerated clearance of intravenously administered theophylline and phenobarbital by oral doses of activated charcoal in rats
7. Identification, kinetic and quantitative study of [2-14C] and [1-Me-14C]caffeine metabolites in rat's urine by chromatographic separations
8. 14C]caffeine in rats, mice, and Chinese hamsters
9. Metabolic pathway of theobromine in the rat and identification of two new metabolites in human urine
10. Theophylline kinetics: Dose dependency and single sample prediction of clearance
11. In vivo, ex vivo and in vitro effects of L-NAME and L-arginine on the metabolism of theophylline in the rabbit
12. Disposition of caffeine in the rabbit
13. Interspecies variations in caffeine metabolism related to cytochrome P4501A enzymes
14. Biodisposition of theophylline I. Genetic variation in inbred mice
15. Biodisposition of theophylline II. Effect of aromatic hydrocarbon treatment in mice
16. Caffeine metabolism in liver slices during postnatal development in rats
17. Comparison of theophylline and theobromine metabolism in man
18. Comparative pharmacokinetics of caffeine in young and elderly men
19. Caffeine disposition after oral doses
20. Kinetics and metabolism of theobromine in male rats
21. Interspecies comparison of in vivo caffeine pharmacokinetics in man, monkey, rabbit, rat, and mouse
22. Interspecies comparison of caffeine disposition
23. Antipyrine and caffeine dispositions in clinically normal dogs and dogs with progressive liver disease
24. Pharmacokinetics of paraxanthine, one of the primary metabolites of caffeine, in the rat
25. Theophylline pharmacokinetics and metabolism in rabbits following single and repeated administration of Capsicum
26. Interspecies variation in liver weight, hepatic blood flow, and antipyrine intrinsic clearance: Extrapolation of data to benzodiazepines and phenytoin
27. Pharmacokinetics of theophylline before and after nephrectomy in dogs
28. Theophylline elimination in the pregnant and fetal rabbit
29. Urinary excretion of caffeine and its metabolites in the mouse
30. Pharmacokinetic interaction between theophylline and chloramphenicol in rats
31. Role of CYP1A2 in caffeine pharmacokinetics and metabolism: Studies using mice deficient in CYP1A2
32. Does the animal-to-human uncertainty factor incorporate interspecies differences in surface area?
33. Biotransformation of caffeine, paraxanthine, theophylline, and theobromine by polycyclic aromatic hydrocarbon-inducible cytochrome(s) P-450 in human liver microsomes
34. Biotransformation of caffeine in human liver microsomes from foetuses, neonates, infants and adults
35. Pharmacokinetics of theophylline and its metabolites in the rabbit
36. Involvement of CYP3A1, 2B1, and 2E1 in C-8 hydroxylation and CYP 1A2 and flavin-containing monooxygenase in N-demethylation of caffeine: Identified by using inducer treated rat liver microsomes that are characterized with testosterone metabolic patterns
37. Respiratory acidemia and theophylline pharmacokinetics in the awake dog
38. Uncertainty factors for chemical risk assessment: Human variability in the in vivo pharmacokinetics of CYP1A2 substrates
39. Caffeine and paraxanthine pharmacokinetics in the rabbit: Concentration and product inhibition effects
40. Regulatory history and experimental support of uncertainty (safety) factors
41. Evolution of science-based factors in noncancer risk assessment
42. Quantitation of cytochrome P450 enzymes (CYP1A1/2, 2B11, 2C21 and 3A12) in dog liver microsomes by enzyme-linked immunosorbent assay
43. Metabolism of caffeine by mouse liver microsomes: GSH or cytosol causes a shift in products from 1,3,7-trimethylurate to a substituted diaminouracil
44. Biotransformation of caffeine and theophylline in mammalian cell lines genetically engineered for expression of single cytochrome P450 isoforms
45. Interspecies metabolism and pharmacokinetic scaling of theophylline disposition
46. Cytochrome P450 isoform selectivity in human hepatic theobromine metabolism
47. Caffeine pharmacokinetics in the neonate: Human and animal studies
48. The influence of dietary restriction on the metabolism of theophylline and antipyrine in the ageing female BN/BiRij rat
49. Biotransformation of caffeine, paraxanthine, theobromine and theophylline by cDNA-expressed human CYP1A2 and CYP2E1
50. Mammalian Cytochromes P-450
51. Biotransformation of caffeine by cDNA-expressed human cytochromes P-450
52. Absolute bioavailability of oral theophylline
53. Studies on methyl-xanthines in intact and hypophysectomised rats: Differences in pharmacokinetics and adrenocorticol response
54. Relationship of urinary metabolites of theophylline to serum theophylline levels
55. Kinetic and dynamic data of analgesics and NSAIDS drugs reduce 10X uncertainty factors
56. The CYP1 family
57. Metabolic rate of female rats as a function of age and body size
58. Multiplicity of cytochrome P-450 species involved in theophylline metabolism in mouse hepatic microsomes
59. A study on bioavailability of theophylline in rabbits as influenced by fatty diet
60. The effect of amiodarone on theophylline pharmacokinetics in the rat
61. Caffeine disposition and effects in young and one-year-old rats
62. Urinary excretion of an uracilic metabolite from caffeine by rat, monkey and man
63. Kinetics and metabolism of theobromine in male and female non-pregnant and pregnant rabbits. II
64. 100-fold margin of safety
65. Quantitative assessment of caffeine partial clearances in man
66. Comparative pharmacokinetics of caffeine and its primary demethylated metabolites paraxanthine, theobromine and theophylline in man
67. Theophylline metabolism by the rat liver microsomal system
68. Safety assessment of chemicals with threshold effects
69. Acceptable daily intake: Inception, evolution, and application
70. Theophylline metabolism by human, rabbit and rat liver microsomes and by purified forms of cytochrome P450
71. Pharmacokinetics of caffeine and its demethylated metabolites in lactating adult rabbits and neonatal offspring
72. Elimination kinetics and protein binding of theophylline in the rabbit
73. Comparative theobromine metabolism in five mammalian species
74. Theobromine metabolism in man
75. Bioavailability study of a theophylline oral controlled release capsule containing film coated mini-tablets in beagle dogs
76. Effect of hypoalbuminemia on the disposition of theophylline
77. P450 in the rat and man: Methods of investigation, substrate specificities and relevance to cancer
78. The P-450 superfamily: Update on new sequences, gene mapping, and recommended nomenclature
79. Comparative pharmacokinetics of theophylline and dyphylline following intravenous injection in rabbits
80. Pharmacokinetics of theophylline in beagle dogs and asthmatic patients after multiple oral doses of sustained-release theophylline tablet formulation
81. Effect of tamoxifen on the pharmacokinetics of theophylline in rats
82. Circadian rhythms in theophylline disposition: Simulation and observations in the dog
83. Identification of two new metabolites of caffeine in the rat urine
84. Fluvoxamine is a potent inhibitor of the metabolism of caffeine in vitro
85. Safety factors and establishment of acceptable daily intakes
86. Data-derived safety factors for the evaluation of food additives and environmental contaminants
87. Human variability and noncancer risk assessment - An analysis of the default uncertainty factor
88. Elimination of theobromine metabolites in healthy adults
89. Pharmacokinetics of theophylline: A dose-range study
90. In vitro metabolism of theophylline by rat and human liver tissue
91. A new cytochrome P450 form belonging to the CYP2D in dog liver microsomes: Purification, cDNA cloning, and enzyme characterization
92. Theophylline disposition during acute and chronic hypoxia in the conscious dog
93. Interindividual variations in human liver cytochrome P-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: Studies with liver microsomes of 30 Japanese and 30 Caucasians
94. Isolation and characterisation of four cytochrome P450 isozymes from untreated and phenobarbital-treated dogs
95. Theobromine metabolism and pharmacokinetics in pregnant and nonpregnant Sprague-Dawley rats
96. High levels of methylxanthines in chocolate do not alter theobromine disposition
97. Diet-induced alterations in theobromine disposition and toxicity in the rat
98. In vivo and in vitro biotransformation of theobromine by phenobarbital- and 3-methylcholanthrene-inducible cytochrome P-450 monooxygenases in rat liver. Role of thiol compounds
99. Temporal variation in the disposition of theophylline and its metabolites
100. Assessing human health risks of chemicals and drugs: An overview
101. In vivo and in vitro trimethadione oxidation activity of the liver from various animal species including mouse, hamster, rat, rabbit, dog, monkey and human
102. Changes in caffeine, lidocaine and trimethadione metabolism in carbon tetrachloride-intoxicated rats as assessed by "cocktail" study
103. Changes in the enzymatic activities of beagle liver during maturation as assessed both in vitro and in vivo
104. Disposition of caffeine and its metabolites in man
105. Theobromine kinetics and metabolic disposition
106. Caffeine metabolism by human hepatic cytochromes P450: Contributions of 1A2, 2E1 and 3A isoforms
107. Dose-dependent elimination of theophylline in rats
108. Pharmacokinetics of theobromine and its metabolites in rabbits
109. The concept of the acceptable daily intake: An historical review
110. Effect of caffeine on circulating theophylline levels in beagle dogs
111. Extrapolation of animal toxicity to humans: Interspecies comparisons in drug development
112. Urinary metabolites of caffeine in young dogs
113. Effect of Aroclor 1254, phenobarbital and polycyclic aromatic hydrocarbons on the plasma clearance of caffeine in the rat
114. Effects of phenobarbital and 3-methylcholanthrene pretreatment on the plasma half-life and urinary excretion profile of theophylline and its metabolites in rats
115. Comparative pharmacokinetics of theophylline in rabbits and in humans with hyperlipidemia
116. Pharmacokinetic interactions between isoniazid and theophylline in rats
117. Characterization of human cytochromes P450 involved in theophylline 8-hydroxylation