A physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) model for the organophosphate insecticide chlorpyrifos in rats and humans

Toxicological Sciences

Volumn 66, Issue 1, 2002, Pages 34-53

  Timchalk, C ^a   Nolan, R J ^b   Mendrala, A L ^c   Dittenber, D A ^c   Brzak, K A ^c   Mattsson, J L ^b  

^a PACIFIC NORTHWEST NATIONAL LABORATORY   (United States)

^b DOW AGROSCIENCES LLC   (United States)

^c DOW CHEMICAL COMPANY   (United States)

Author keywords

Chlorpyrifos; Esterase inhibition; Organophosphate insecticide; Physiologically based pharmacokinetics

Indexed keywords

ACETYLCHOLINESTERASE; CHLORPYRIFOS; CHOLINESTERASE; ESTERASE INHIBITOR; ORGANOPHOSPHATE INSECTICIDE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD LEVEL; BRAIN LEVEL; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DOSIMETRY; ENZYME INHIBITION; ERYTHROCYTE LEVEL; FEMALE; HUMAN; HUMAN EXPERIMENT; MALE; METABOLISM; METABOLITE; MODEL; MOLECULAR DYNAMICS; NONHUMAN; QUANTITATIVE ANALYSIS; RAT; RISK ASSESSMENT; TARGET ORGAN; TOXICOKINETICS;

ACETYLCHOLINESTERASE; ADMINISTRATION, CUTANEOUS; ADMINISTRATION, ORAL; ALGORITHMS; ANIMALS; AREA UNDER CURVE; BRAIN; CHLORPYRIFOS; CHOLINESTERASE INHIBITORS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; ERYTHROCYTES; FEMALE; HUMANS; INSECTICIDES; MALE; MODELS, BIOLOGICAL; RATS; RATS, INBRED F344; TIME FACTORS;

ANIMALIA;

EID: 0036191658     PISSN: 10966080     EISSN: None     Source Type: Journal    
DOI: 10.1093/toxsci/66.1.34     Document Type: Article

References (77)

1. A physiologically based pharmacokinetic and pharmacodynamic model for paraoxon in rainbow trout
2. Inhibition of acetylcholinesterase and butyrylcholinesterase by chlorpyrifos-oxon
3. Development of physiologically based pharmacokinetic and physiologically based pharmacodynamic models for applications in toxicology and risk assessment
4. Physiologically based pharmacokinetics and the risk assessment process for methylene chloride
5. Biological monitoring of exposure to organophosphorus insecticides by assay of urinary alkylphosphates: Influence of protective measures during manual operations with treated plants
6. Rat urinary metabolites from O,O-diethyl-O-(3,5,6-trichloro-2-pyridyl)phosphorothioate
7. Physiological parameter values for physiologically based pharmacokinetic models
8. Determination of chlorpyrifos, chlorpyrifos oxon, and 3,5,6-trichloro-2-pyridinol in rat and human blood
9. Biotransformation of parathion in human liver: Participation of CYP3A4 and its inactivation during microsomal parathion oxidation
10. Comparative metabolism: The principal causes of differential susceptibility to toxic and carcinogenic agents
11. Kinetic analysis of the in vitro inhibition, aging and reactivation of brain acetylcholinesterase from rat and channel catfish by paraoxon and chlorpyrifos-oxon
12. Oxidative desulfuration of chlorpyrifos, chlorpyrifos-methyl, and leptophos by rat brain and liver
13. Blood cholinesterase levels in a group of Malaysian blood donors
14. Tissue-specific effects of chlorpyrifos on carboxylesterase and cholinesterase activity in adult rats: An in vitro and in vivo comparison
15. Role of aliesterase in organophosphate poisoning
16. Physiologically based pharmacokinetics of 2-butoxyethanol and its major metabolite, 2-butoxyacetic acid, in rats and humans
17. Chlorpyrifos metabolites in serum and urine of poisoned persons
18. Pseudocholinesterases of mammalian plasma: Physiocochemical properties and organophosphate inhibition in eleven species
19. A new and rapid colorimetric determination of acetylcholinesterase activity
20. Identification of the cytochrome P450 isoenzymes involved in the metabolism of diazinon in the rat liver
21. Acute toxicity of pesticides
22. Physiologically based pharmacokinetic and pharmacodynamic model for the inhibition of acetylcholinesterase by diisopropylfluorophosphate
23. How to determine if an additional 10X safety factor is needed for chemicals: A case study with chlorpyrifos
24. Oral and dermal absorption of chlorpyrifos: A human volunteer study
25. Separation and purification of multiple forms of microsomal cytochrome P-450. Activities of different forms of cytochrome P-450 towards several compounds of environmental interest
26. Molecular and physical mechanisms of first-pass extraction
27. Pesticide residues in urine of adults living in the United States: Reference range concentrations
28. Assessment of drug exposure in rat dietary studies
29. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals
30. Chlorpyrifos oxon interacts with the mammalian multidrug-resistance protein, P-glycoprotein
31. Biological monitoring of organophosphorus pesticide exposure among children of agricultural workers in central Washington state
32. Inhibition of lymphocytic neuropathy target esterase predicts the development of organophosphate-induced delayed polyneuropathy
33. Kinetic parameters of desulfuration and dearylation of parathion and chlorpyrifos by rat liver microsomes
34. A kinetic analysis of hepatic microsomal activation of parathion and chlorpyrifos in control and phenobarbital-treated rats
35. The effect of blood flow and detoxification on in vivo cholinesterase inhibition by soman in rats
36. A pharmacodynamic model for soman in the rats
37. Studies on the acute and long-term oral toxicity of chlorpyrifos (o,o-diethyl-o-(3,5,6-trichloro-2-pyridyl) phosphorothioate)
38. A physiological pharmacokinetic model for dermal absorption of vapors in the rat
39. 50 values represent?
40. Maturational differences in chlorpyrifos-oxonase activity may contribute to age-related sensitivity to chlorpyrifos
41. Toxic effects of pesticides
42. Microsomal metabolism of thiono-sulfur compounds, mechanisms, and toxicological significance
43. Chlorpyrifos: Pharmacokinetics in human volunteers
44. The relationship of oral chlorpyrifos: Effects on behavior, cholinesterase inhibition, and muscarinic- receptor density in rat
45. Metabolic characterization of the major human small intestinal cytochrome P450s
46. Appendix G: Inhibition of cholinesterases and an evaluation of the methods used to measure cholinesterase activity
47. Cytochrome P-450 1A1 expression in human small bowel: Interindividual variation and inhibition by ketoconazole
48. Assessing dermal absorption
49. Assessment of the percutaneous absorption of trichloroethylene in rats and humans using MS/MS real-time breath analysis and physiologically based pharmacokinetic modeling
50. Organophosphate detoxification potential of various rat tissues via A-esterase and aliesterase activity
51. An algorithm for predicting tissue: Blood partition coefficients of organic chemicals from n-octonol: Water partition coefficient data
52. Use of Screening Questionnaires to Identify Exposed and Sensitive Population Groups in the Region V NHEXAS Children's Pesticide Study
53. A physiologically based description of the inhalation pharmacokinetics of styrene in rats and humans
54. Toxicokinetics-pharmacokinetics in toxicology
55. Illness and excretion of organophosphate metabolites four months after household pest extermination
56. Evidence for the activation of organophosphate pesticides by cytochromes P450 3A4 and 2D6 in human liver microsomes
57. Cultured adult rat jejunal explants as a model for studying regulation of CYP3A
58. Aggregate exposures under the Food Quality Protection Act: An approach using chlorpyrifos
59. Gastrointestinal absorption of xenobiotics in physiologically based pharmacokinetic models. A two-compartment description
60. A physiologically based pharmacokinetic model of parathion based on chemical-specific parameters determined in vitro
61. Mammalian toxicology of organophosphorus pesticides
62. Kinetic analyses of the microsomal biotransformation of the phosphorothioate insecticides chlorpyrifos and parathion
63. The role of hepatic biotransformation in mediating the acute toxicity of the phosphorothionate insecticide chlorpyrifos
64. Health effects of pesticides
65. Toxicokinetic and toxicodynamic aspects of organophosphate (OP) insecticide poisoning
66. Urinary excretion of diethylphosphorus metabolites in persons poisoned by quinalphos or chlorpyrifos
67. Species variation in the specificity of cholinesterases in human and rat blood samples
68. Drug metabolism by cytochromes P450 in the liver and small bowel
69. Malathion percutaneous absorption after repeated administration to man
70. In vivo and in vitro percutaneous absorption and skin evaporation of isofenphos in man
71. Percutaneous absorption of diazinon in humans
72. Effect of vehicle on the pharmacokinetics and uptake of four halogenated hydrocarbons from the gastrointestinal tract of the rat
73. Lack of carcinogenicity of chlorpyrifos insecticide in a high-dose, 2-year dietary toxicity study in Fischer 344 rats
74. Characterization of human small intestinal cytochromes P-450
75. Comparative cholinergic neurotoxicity of chlorpyrifos exposures in pre-weanling and adult rats