Impact of Biological and Environmental Variabilities on Biological Monitoring An Approach Using Toxicokinetic Models

Similar documents
Application of BEls. rigid lines between safe and dangerous concentrations nor are they an index of toxicity.

Biological Exposure Indices (BEI)

Basic Concepts of TDM

BASIC PHARMACOKINETICS

It the process by which a drug reversibly leaves blood and enter interstitium (extracellular fluid) and/ or cells of tissues.

Naval Medical Research Unit Dayton

Pharmacokinetics I. Dr. M.Mothilal Assistant professor

Unit 2b: EXCRETION OF DRUGS. Ms.M.Gayathri Mpharm (PhD) Department of Pharmaceutics Krishna Teja Pharmacy college Subject code: 15R00603 (BPPK)

Reverse Dosimetry From Human Biomonitoring and In Vitro Concentration- Response Data

General Principles of Pharmacology and Toxicology

EVE 491/591 Toxicology. Toxicant Entry into the Body 2/19/2018. Absorption and Fate of a Toxicant

TOXIC AND ESSENTIAL ELEMENTS

DRUG DISTRIBUTION. Distribution Blood Brain Barrier Protein Binding

Industrial Toxicology

Renal Disease and PK/PD. Anjay Rastogi MD PhD Division of Nephrology

Ecotoxicology. Toxicology Uptake and distribution of xenobiotics

ENVIRONMENTAL TOXICOLOGY

Regulation of fluid and electrolytes balance

SUPPLEMENTARY DATA. Supplementary Table S1. Clinical characteristics of the study subjects.*

A Regional Model of Lung Metabolism for Improving Species Dependent Descriptions of 1,3-Butadiene and its Metabolites

PROBLEM SET 7.1 FLUID VOLUMES, GLOMERULAR FILTRATION AND CLEARANCE

BIO 202 HUMAN ANATOMY AND PHYSIOLOGY II BIO 201 Prefix No. Course Title Prerequisite

IndusChemFate A PBTK-model in MS-Excel applicable for worker and consumer exposure to multiple chemicals User manual

General renal pathophysiology

1. If the MTC is 100 ng/ml and the MEC is 0.12 ng/ml, which of the following dosing regimen(s) are in the therapeutic window?

Principles of Drug Action. Intro to Pharmacology: Principles of Courework Drug Action Intro to Pharmacology

DRUG ELIMINATION II BILIARY EXCRETION MAMMARY, SALIVARY AND PULMONARY EXCRETION

BIOPHARMACEUTICS and CLINICAL PHARMACY

Physiologically Based Toxicokinetic Modeling of Inhaled Ethyl tertiary-butyl Ether in Humans

Principles of Toxicology: The Study of Poisons

Renal Excretion of Drugs

Concurrent Exposure to Ototoxic Chemicals and Noise

PHA Final Exam. Fall On my honor, I have neither given nor received unauthorized aid in doing this assignment.

ISPUB.COM. Review Of Currently Used Inhalation Anesthetics: Part II. O Wenker SIDE EFFECTS OF INHALED ANESTHETICS CARDIOVASCULAR SYSTEM

Update on PBTK model-based derivation of HBM-1 values for ethylene glycol monoethyl ether (acetate)

PHA First Exam Fall 2003

Pharmacokinetics Dr. Iman Lec. 3

TWA [2] (mg/m3) [5] (ppm) [6]

General Principles of Pharmacology and Toxicology

Physiological Modeling of Inhalation Kinetics of Octamethylcyclotetrasiloxane in Humans during Rest and Exercise

Chapter 15 Fluid and Acid-Base Balance

A Speciation Study focused on the Identification of Proximate Toxic Arsenic Metabolites. Kazuo T. Suzuki

Drug elimination and Hepatic clearance Chapter 6

ESSENTIAL TRACE ELEMENTS PREPARED BY B.KIRUTHIGA LECTURER DEPT OF PHARMACEUTICAL CHEMISTRY

A. Incorrect! The alveolus is where gas exchange takes place. B. Correct! Surfactant is the lipid-rich material that permits lung inflation.

Development of a Human PBBK Model for Mixtures: Trio Mixture of Mercury, Lead, and Selenium

Ethylene Oxide

Relative Pesticide and Exposure Route Contribution to Aggregate and Cumulative Dose in Young Farmworker Children

Rational Dose Prediction. Pharmacology. φαρμακον. What does this mean? pharmakon. Medicine Poison Magic Spell

PHA Final Exam Fall 2006

Element B1 / 3 Target Organs and Systems

Relation between airborne arsenic trioxide and

The Case. The Case. The Case. Objectives. What is a solvent?

Bioavailability Adjustments in Human Health Risk Assessment for Metals-Contaminated Sites

BODY FLUID. Outline. Functions of body fluid Water distribution in the body Maintenance of body fluid. Regulation of fluid homeostasis

APPENDIX K - Exposure Limits For Uranium

3. Which of the following would be inconsistent with respiratory alkalosis? A. ph = 7.57 B. PaCO = 30 mm Hg C. ph = 7.63 D.

Concepts in Toxicology Food Toxicology Instructor: Gregory Möller, Ph.D. University of Idaho

Air Toxicology and Epidemiology

ICRP Perspective on Internal Dosimetry OIR and Radiopharmaceuticals

Introduction to. Pharmacokinetics. University of Hawai i Hilo Pre-Nursing Program NURS 203 General Pharmacology Danita Narciso Pharm D

Drug Dosing in Renal Insufficiency. Coralie Therese D. Dimacali, MD College of Medicine University of the Philippines Manila

Basic Biopharmaceutics, Pharmacokinetics, and Pharmacodynamics

MATERIAL SAFETY. St. Paul, Minnesota or (651) (24 hours)

Biology 105 Midterm Exam 4 Review Sheet

Pharmacokinetics of Rifampicin in African Children Evaluation of the new WHO dosing guidelines

Drug dosing in Extremes of Weight

Slide 1. Slide 2. Slide 3. Learning Outcomes. Acid base terminology ARTERIAL BLOOD GAS INTERPRETATION

Appendix E Choose the sign or symptom that best indicates severe respiratory distress.

Chapter-V Drug use in renal and hepatic disorders. BY Prof. C.Ramasamy, Head, Dept of Pharmacy Practice SRM College of Pharmacy, SRM University

PHA Spring First Exam. 8 Aminoglycosides (5 points)

MOLECULAR SIZE, ELECTRICAL CHARGE, AND SHAPE DETERMINE THE FILTERABILITY OF SOLUTES ACROSS THE GLOMERULAR FILTRATION BARRIER

= (6000 ml air / min * 0.04 ml CO 2 / ml air) / 54 ml CO 2 / dl plasma

Indoor emissions. foams) > CH 2 =O; plasticizers, especially dialkyl phthalates. Especially a problem with mobile homes. - Regulations in Sweden

Biopharmaceutics. Tips Worth Tweeting. Contributor: Sandra Earle

UNIVERSITY OF THE WEST INDIES, ST AUGUSTINE

Alabama Department of Postsecondary Education

Analyte Proficiency From All Labs # Analytes: 26 Sample # Statistical Summary # Labs Reporting: 82 Urea Issue Date : 06/30/2016

CASE 27. What is the response of the kidney to metabolic acidosis? What is the response of the kidney to a respiratory alkalosis?

MAJOR FUNCTIONS OF THE KIDNEY

TOXICOLOGY, AND HUMAN HEALTH

WHY... 8/21/2013 LEARNING OUTCOMES PHARMACOKINETICS I. A Absorption. D Distribution DEFINITION ADME AND THERAPEUIC ACTION

The ADME properties of most drugs strongly depends on the ability of the drug to pass through membranes via simple diffusion.

Excretion of Drugs. Prof. Hanan Hagar Pharmacology Unit Medical College

Lecture 2 Chemical and Biological Agents

The Respiratory System

VOLATILE ORGANIC COMPOUNDS

Applicant Name: GD Sigelei Electroinc Tech Co., Ltd B7 Building, No.1 District, Xicheng Science and Technology Park, Hengli Town, Dongguan, China

ADME Review. Dr. Joe Ritter Associate Professor of Pharmacology

PROVINCE OF BRITISH COLUMBIA ORDER OF THE LIEUTENANT GOVERNOR IN COUNCIL

3/19/2009. The task of the kidney in acid-base balance Excretion of the daily acid load. Buffering of an acid load. A o B - + H + B - A o +OH - C +

Renal Function. 1. Glomerular filtration 2. Active tubular secretion 3. Passive tubular reabsorption 4. Excretion

Blood Gases, ph, Acid- Base Balance

Physiology questions review

Test Report No.T TC Date: JUN 29, 2018 Page 1 of 5

OP01 [Mar96] With regards to pethidine s physical properties: A. It has an octanol coefficient of 10 B. It has a pka of 8.4

Table H3-1 Values Used for Daily Intake/Absorbed Dose Inhalation of Particulates

Terminology. Terminology. Terminology. Molarity number of moles of solute / Liter of solution. a) Terminology b) Body Fluid Compartments

The Islamic University of Gaza- Civil and Environmental Engineering Department Public Health (EENV-5325) Lecture 9: Occupational health and safety

Acid-base balance is one of the most important of the body s homeostatic mechanisms Acid-base balance refers to regulation of hydrogen ion (H + )

Transcription:

ONLINE SUPPLEMENTAL APPENDIX Impact of Biological and Environmental Variabilities on Biological Monitoring An Approach Using Toxicokinetic Models by A. Berthet, A. de Batz, R. Tardif, G. Charest-Tardif, G. Truchon, D. Vernez, and P.O. Droz Table AI presents the data used in the CBTK models for all 14 chemicals. The first line for each chemical indicates the physiological identity of each compartment and chemical species. Then individual parameters are presented. Flow data both at rest and at 50W are indicated. Symbol nomenclature used in Table AI is shown in Table AII. The equations used to calculate each model parameter in Table AI are described by Pierrehumbert et al. (10) in more detail. TABLE AI. Chemical Specific Parameters Used in the Simulations for Each Substance Studied with CBTK Models Chemical/Volumes of Distribution Parameters Symbol At Rest At 50 W Arsenic (As) Central= Total body water (TBW), Metabolite 1 (M1) = TBW Exposure (µg/m 3 ) C exp 10 C Total body volume (TBV) A FV C 0.886 Liver blood flow B BF M1 0.26 (24) 0.16 (24) Total body volume (TBV): blood partition coefficient for inorganic arsenic (-) P TBV:blood 45 (25) TBV: blood partition coefficient for monomethylarsonic acid (MMA) (-) P TBV:blood, M1 8.6 (25) TBV:blood partition coefficient for dimethylarsonic acid (DMA) (-) P TBV:blood, M2 6.7 (25) Liver permeability coefficient for inorganic arsenic (-) P p 0.006 (25) Liver permeability coefficient for MMA (-) P M1 0.02 (25) Maximum metabolism rate of inorganic arsenic (µmol/h/kg 0.75 ) V MM1 0.00463 (25) Michaelis-Menten constant for inorganic arsenic (µmol/l) K MM1 0.15 (25) Maximum metabolism rate of MMA (µmol/h/kg 0.75 ) V MM2 0.00579 (25) Michaelis-Menten constant for MMA (µmol/l) K MM2 0.5 (25) Renal Clearance (l/h per kg -0.3 ) RC C 24 (24) Cadmium (Cd) Central = Total body water, Peripheral = kidneys Exposure (µg/m 3 ) C exp 50 D (14) - Kidneys Kidney volume A FV P 0.004 (25) Kidney blood flow B BF P 0.11 (25) 0.2 (25) TBW: blood affinity coefficient (-) P TBW:blood 60 E Kidney permeability coefficient (-) P P 50 E

Kidney: blood affinity coefficient (-) P kidney:blood 60,000,000,000 F Renal Clearance (l/h per kg -0.3 ) RC C 200 F Carbon monoxide (CO) Central=Whole blood Exposure (ppm) C exp 35 (14) Deposit rate (%) 100 G Blood volume A FV P 0.07 (25) Blood: air affinity coefficient (-) P blood:air 500 H Hemoglobin concentration (g Hb/l) 150 (1) Link rate (%) 85 (1) Affinity (ml CO/g Hb) 1.49 (1) Chromium (Cr) Central=Total body water, Peripheral=richly perfused tissues (RP) (i.e., heart, liver, brain) Exposure (µg/m 3 ) C exp 50 I (14) - RP RP volume A FV P 0.076 (10) RP blood flow B BF P 0.70 (10) 0.43 (10) TBW: blood affinity coefficient (-) P TBW:blood 17 J RP permeability coefficient (-) P P 4 K RP: blood affinity coefficient (-) P RP:blood 400,000 L Renal Clearance (l/h per kg -0.3 ) RC C 52.02 (25) Cobalt (Co) Central=TBW, Peripheral=richly perfused tissues (RP) Exposure (µg/m 3 ) C exp 50 M (14) - RP RP volume A FV P 0.076 (10) RP blood flow B BF P 0.70 (10) 0.43 (10) TBW: blood affinity coefficient (-) P TBW:blood 2 N RP permeability coefficient (-) P P 65 N RP: blood affinity coefficient (-) P RP:blood 2 10 6 O Urinary excretion constant (h -1 /kg -0.3 ) k u,c 0.03444 P Ethylbenzene Central=Richly (RP) and slowly perfused tissues (SP), Peripheral=Fat Exposure (ppm) C exp 100 (14) Deposit rate (%) 60 (14) RP and SP volume 1 FV C 0.886 - Fat Fat volume A FV P 0.19 (24) Fat blood flow B BF P 0.05 (24) 0.06 (24) Liver blood flow B BF M1 0.26 (24) 0.16 (24) RP and SP: air partition coefficient (-) P RP and SP:air 26.02 (24) Blood: air partition coefficient (-) P blood:air 28.02 (24) Fat: air partition coefficient (-) P fat:air 1566.0 (24) Maximum metabolism rate (µmol/h/kg 0.75 ) V MM1 68.76 (24) Michaelis-Menten constant (µmol/l) K MM1 13.09 (24) Ethylbenzene fraction metabolized to mandelic acid / Ethylbenzene fraction metabolized to phenylglyoxilic acid F 2 /F 1 2 (24) Mandelic acid excretion rate (h -1 /kg -0.3 ) k u,m2 0.49 (24)

Fluorides Central=Total body water, Peripheral=bones Exposure (mg/m 3 ) C exp 2.5 Q (14) Skeleton volume A FV P 0.132 (26) Skeleton blood flow B BF P 0.0093 (26) TBW: blood affinity coefficient (-) P TBW:blood 3 R Bones permeability coefficient (-) P P 0.455 R Bones: blood affinity coefficient (-) P bones:blood 662 S Renal Clearance (l/h per kg -0.3 ) RC C 25.755 T Ethyleneglycol monomethylether (EGEE) Central=Total body water, Metabolite1 (M1)=Total body water Exposure (ppm) C exp 5 (14) Deposit rate (%) 80 (27) Liver blood flow B BF P 0.26 (10,24) 0.16 (10,24) Water: air partition coefficient EGEE (-) P water:air 23 069 (27) Blood: air partition coefficient EGEE (-) P blood:air 22 093 (27) Water: blood partition coefficient of 2-ethoxyacetic acid (EAA) (-) P water:blood 1.00 (28) Maximum metabolism rate (µmol/h/kg 0.75 ) V MM1 1460.44 (29) Michaelis-Menten constant (µmol/l) K MM1 1200 (29) EGEE fraction metabolized to EAA / fraction metabolized to ethylene glycol (EG) (-) F 2 /F 1 2.00 (29) EAA renal Clearance (l/h per kg -0.3 ) k u,m2 1.4308 D Inorganic mercury (IHg) Central Total body water, Peripheral=kidneys Exposure (µg/m 3 ) C exp 25 (14) - Kidney Kidney volume A FV P 0.004 (26) Kidney blood flow B BF P 0.11 (26) Kidney: blood partition coefficient (-) P kidney:blood 473,396,562 U Kidney permeability coefficient (-) P P 307.40 U Renal excretion constant (h 1 per kg 0.3 ) k u,c 0.001715 U Biliary excretion constant (h 1 per kg 0.3 ) k f,p 0.055216 U Methyl isobutyl ketone (MIBK) Central=Total body water, Peripheral=Fat Exposure (ppm) C exp 50 (14) Deposit rate (%) 80 (30) Fat volume A FV P 0.19 (10) Fat blood flow B BF P 0.05 (10) 0.06 (10) Water: air partition coefficient (-) P water:air 79 (14) Blood: air partition coefficient (-) P blood:air 90 (14) Fat: air partition coefficient (-) P fat:air 926 (14) Urinary excretion constant (h -1 /kg -0.3 ) k u,p 0.0138 V Metabolism constant (h -1 /kg -0.3 ) K MM1 12.423 V Pentachlorophenol Central=Total body water, Metabolite=undefined

Exposure (µg/m 3 ) C exp 500 (14) Deposit rate (%) 80 W Central: air affinity coefficient (-) P central:air 125,000 X Blood: air affinity coefficient (-) P blood:air 250,000 X Urinary excretion constant (h -1 /kg -0.3 ) for free PCP k u,p 0.00074 X Metabolism constant (h -1 /kg -0.3 ) K MM1 0.00457 X Urinary excretion constant (h -1 /kg -0.3 ) for combined PCP k u,p 0.00074 X Phenol (Ph) Central=TB Exposure (ppm) C exp 5 (14) Total body water (TBW) A FV C 0.886 Renal Clearance (l/h per kg -0.3 ) RC C 43.936 Y Lead (Pb) Central=Total body water minus peripheral compartment, Peripheral=skeleton Exposure (µg/m 3 ) C exp 150 (14) Total body volume (TBV) A FV C 0.886 - Skeleton Skeleton volume A FV P 0.132 (26) Skeleton blood flow B BF P 0.0093 (26) TBV: blood partition coefficient (-) P TBV:blood 207.93 Z Bones: blood partition coefficient (-) P bones:blood 31,881,434 Z Renal Clearance (l/h per kg -0.3 ) RC C 17.7558 (31) Toluene (TOL) Central=Richly (RP) and slowly perfused tissues (SP), Peripheral=Fat, Metabolite=undefined Exposure (ppm) C exp 50 (14) RP and SP volume A FV C 0.886 Fat Liver Fat volume A FV P 0.19 (10) Liver volume (metabolism) A FV M1 0.026 (10) Fat blood flow B BF P 0.05 (24) 0.06 (24) Liver blood flow B BF M1 0.26 (24) 0.16 (24) Blood: air partition coefficient (-) P blood:air 15.6 (32) SP: air partition coefficient (-) P SP:air 27.7 (33) Fat: air partition coefficient (-) P fat:air 1021.0 (33) Michaelis-Menten maximum rate (µmol/h/kg 0.75 ) V MM1 52.09 (10) Michaelis-Menten constant (µmol/l) K MM1 5.97 (10) Fraction of TOL metabolized to hippuric acid (HA)/Fraction of TOL metabolised to o-cresol (-) F 2 /F 1 1281 (10) o-cresol excretion rate constant (l/h per kg -0.3 ) k u,m2 0.715 (34) A Expressed in fraction of body weight. B Expressed in fraction of cardiac output. C ACGIH TLV-TWA. (14) D Simulation of an exposure to 50 µg/m 3, but only 45% of dust is considered to reach the pulmonary alveoli. (26) E Determined according to the following considerations: (1) cadmium half-life in blood is 100 days (25) ; (2) cadmium blood concentration at steady state is about 50 nmol/l. (25) F Determined according to the following considerations: (1) urinary cadmium half-life is 20 years; (25) (2) cadmium half-life in body is 10 years (25).

G Deposit rate is supposed equal to 100% because of its small molecular weight H Determined according to the following consideration: the carboxyhemoglobin half-life is 5 hours. (25) I Simulation of an exposure to 50 µg/m 3, but only 15% of smoke is considered to reach the pulmonary alveoli; (26) of this 15%, 60% is considered soluble and distributed in the central compartment directly, and the other 40% was taken to be insoluble and distributed with a half-life of 120 days, (35) which means an approximate constant flow of 0.15 µmol/hour. J Determined according to the following considerations, (1) kidney clearance is calculated from glomerular filtration; (2) the half-life of urinary elimination is 7 hours. (25) K Determined according to the following consideration: the slow half-life of central compartment is 30 hours. (25) L Determined according to the following consideration: the half-life of the peripheral compartment is 3 years. (25) M Workers are exposed to 50 µg/m 3, but only 30% of mixed dust and smoke lay down on pulmonary alveoli. (26) N Determined according to the following considerations: (1) the half-life of transfer between the central compartment and the peripheral compartment is 12 hours; (25) (2) cobalt blood concentration at steady state is about 40 nmol/l. (25) O Determined according to the following consideration: the cobalt half-life in richly perfused tissues is 2 years. (25) P Determined according to the following considerations: the urinary and blood cobalt half-life in RP tissue is 3 days. (25) Q Simulation of an exposure to 2.5 mg/m 3, but only 45% of dust is considered to reach the pulmonary alveoli. (26) R Determined according to the following considerations: (1) kidney clearance is equal to the glomerular filtration; (14) (2) fluorides half-life in TBW is 6 hours; (25) (3) 50% of fluorides are quickly eliminated and the other 50% accumulate in bones. (25) S Determined according to the following consideration: the fluorides half-life in bones is 18 days. (25) T Fluorides clearance is equal to the glomerular filtration. (31) U Determined according to following considerations: (1) at steady state, 90% of the total body burden is found in the kidney; (36) (2) the half-life of Hg in blood is 3 days; (31) (3) the half-life of Hg in kidney is 60 days; (31) (4) at steady state, 58% is excreted in urine. (36) V Determined according to following considerations: (1) elimination by exhalation represents about 10% of the absorbed dose; (2) urinary elimination represents 0.04% of the absorbed dose; (3) elimination by metabolism represents the rest of the absorbed dose. (30) W Value chosen by default in this study for solvents. X Determined according to the following considerations: (1) elimination percentages of free and combined PCP in urine are 12 and 74 % respectively; (37) (2) the rest is eliminated in the expired air; (3) free PCP clearance is 0.075 l/hour; (37) and (4) plasmatic concentration at the end of shiftwork is next to 19 µmol/l. (25) Y Determined according to the half-life of Ph in the whole body - 3.5 hours. (14) Z Determined according to the half-life of Pb in blood, 37.5 days, and in the skeleton, 20 years. (31)

TABLE AII. Symbol Nomenclature Used in Table AI Symbol Definition Units BF i Fraction of cardiac output in the compartment i C exp Exposure dose µg/m 3 or ppm F 2 /F 1 Fraction differentiation between metabolite 1 and 2 FV i Volume of compartment i expressed as fraction of body weight k f,i Feces excretion rate constant for compartment i l/h per kg -0.3 K Mi Michaelis-Menten constant for metabolite i µmol/l or l/h per kg -0.3 k u,i Urine excretion rate constant for compartment i l/h per kg -0.3 P i:j Affinity or partition coefficient between media i and media j P Mi Permeability of metabolite compartment P p Permeability of peripheral compartment RC i Renal clearance from compartment i l/h per kg -0.3 V Mi Michaelis-Menten maximum rate for metabolite i µmol/h per kg 0.75