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DMD #40758 Sarah Dawson, Simone Stahl, Nikki Paul, Jane Barber and J

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DMD #40758 Sarah Dawson, Simone Stahl, Nikki Paul, Jane Barber and J DMD #40758 Sarah Dawson, Simone Stahl, Nikki Paul, Jane Barber and J Gerald Kenna. In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug induced liver injury in man. Drug Metabolism and Disposition. Supplemental Table 2 Human plasma protein binding, Cmax, Cmax,u and daily dose of test pharmaceuticals DILI Drug Human PPB Maxim Cmax Cmax,u Cmax,u Maxim category plasma referen um referen (g/ml) (M) um protein ce availab ce dose in binding le Cmax man (PPB, in man (mg/ %) (g/ml) day) Cholestatic Acitretin 99.9 Microm 0.418 Xu et al 0.00042 0.001 75 / mixed edex 2008 2.0 Azathioprine 30.0 Microm 2 Regent 1.4 5.05 350 edex hal et al 2.0 1999 Benoxaprofen 99.0 Kratoch 45 Smith 0.45 1.49 600 wil et al et al 2002 1977 Bezafibrate 95.0 Martind 6 Xu et al 0.3 0.829 600 ale 2008 Bosentan 98.0 Martind 4.1 van 0.082 0.149 250 ale Giersbe rgen PL and Dingem anse J 2005 Carbamazepine 80.0 Kratoch 12 Regent 2.4 10.158 1200 wil et al hal et al 2002 1999 Chlorpromazine 97.8 Kratoch 0.3 Xu et al 0.0066 0.021 800 wil et al 2008 2002 Chlorpropamide 96.0 Kratoch 150 Regent 6 21.681 250 wil et al hal et al 2002 1999 Ciprofibrate 95.0 Clarke's 111 Xu et al 5.55 19.194 100 Analysi 2008 s of Drugs and Poisons Clavulanate 22.0 Hardma 2.2 Drug 1.72 8.616 250 n et al label 1995 Cloxacillin 94.6 Hardma 15 Regent 0.81 1.858 1000 n et al hal et al 1995 1999 Clozapine 95.0 Hardma 0.8 Regent 0.04 0.122 900 n et al hal et al 1995 1999 DMD #40758 Cyclosporin A 93.0 Hardma 0.93 Xu et al 0.065 0.054 1050 n et al 2008 1995 Dapsone 73.0 Hardma 2 Regent 0.54 2.175 100, n et al hal et al weekly 1995 1999 Dicloxacillin 95.8 Hardma 18 Martind 0.76 1.607 500 n et al ale 1995 D-Penicillamine 80.0 Martind 5.6 Regent 1.12 7.506 1500 ale hal et al 1999 Erythromycin 95.0 Martind 3.08 Xu et al 0.15 0.210 1000 Estolate ale 2008 Famotidine 17.0 Hardma 0.2 Regent 0.17 0.492 40 n et al hal et al 1995 1999 Fenclozic Acid 98.1 C-lab 126 Chalme 2.41 9.486 400 rs et al 1969 Flucloxacillin 95.0 Martind 30 Regent 1.5 3.305 1000 ale hal et al 1999 Flutamide 90.0 Martind 1.5 Regent 0.15 0.543 750 ale hal et al 1999 Fusidic Acid 94.8 Kratoch 200 Regent 10.4 20.127 480 wil et al hal et al 2002 1999 Glibenclamide 99.0 Olsen 0.2 Regent 0.002 0.004 15 et al hal et al 1995 1999 Ibuprofen 99.0 Kratoch 30 Regent 0.3 1.454 1800 wil et al hal et al 2002 1999 Iproniazid 57.2 C-lab 0.007 Rubin 0.003 0.017 150 et al 1952 Ketoconazole 99.0 Hardma 6 Regent 0.06 0.113 200 n et al hal et al 1995 1999 Methimazole 0.0 Clarke's 2.5 Regent 2.5 21.897 30 Analysi hal et al s of 1999 Drugs and Poisons Nefazodone 99.0 Martind 2 Regent 0.02 0.043 600 ale hal et al 1999 Nifedipine 96.0 Hardma 0.1 Regent 0.004 0.012 30 n et al hal et al 1995 1999 Nitrofurantoin 62.0 Hardma 5 Regent 1.9 7.978 200 n et al hal et al 1995 1999 DMD #40758 Nomifensine 75.0 Clarke's 2 Regent 0.5 2.098 200 Analysi hal et al s of 1999 Drugs and Poisons Pioglitazone 99.0 Martind 1.05 Xu et al 0.011 0.029 45 ale 2008 Ranitidine 15.0 Hardma 1 Regent 0.85 2.703 300 n et al hal et al 1995 1999 Rifampicin 80.0 Martind 10 Regent 2 2.430 600 ale hal et al 1999 Rifamycin SV 80.0 Martind 11 Martind 2.2 3.153 600 ale ale Rosiglitazone 99.8 Martind 0.373 Xu et al 0.00075 0.002 8 ale 2008 Sulindac 93.5 Kratoch 11.4 Xu et al 0.74 2.079 400 wil et al 2008 2002 Sulpiride 40.0 Martind 0.6 Regent 0.36 1.054 800 ale hal et al 1999 Ticlopidine 96.5 Kratoch 2.13 Xu et al 0.075 0.283 500 wil et al 2008 2002 Tolbutamide 96.0 Kratoch 100 Regent 4 14.796 500 wil et al hal et al 2002 1999 Troglitazone 99.0 Clarke's 2.82 Xu et al 0.028 0.064 600 Analysi 2008 s of Drugs and Poisons Valproate 93.0 Kratoch 100 Regent 7 48.540 4200 wil et al hal et al 2002 1999 Hepato- Acetaminophen 0.0 Hardma 25 Regent 25 165.388 4000 cellular n et al hal et al 1995 1999 Acyclovir 15.0 Hardma 5 Regent 4.25 18.871 4000 n et al hal et al 1995 1999 Alpidem 99.1 Clarke's 0.27 Clarke's 0.0024 0.006 150 Analysi Analysi s of s of Drugs Drugs and and Poisons Poisons Carmustine 77.0 Clarke's 0.0078 Clarke's 0.0018 0.008 346 Analysi Analysi (200/m2 s of s of ) Drugs Drugs and and Poisons Poisons Cinchophen 95.0 Axelrod 90 Axelrod 4.5 18.053 300 and and DMD #40758 Chenki Chenki n 1954 n 1954 Dihydralazine 75.5 C-lab 0.5 Regent 0.12 0.645 300 hal et al 1999 Felbamate 25.0 Hardma 0.095 Regent 0.071 0.299 3600 n et al hal et al 1995 1999 Fialuridine 64.3 C-lab 0.238 Bowshe 0.085 0.228 17.5 r et al 1994 Furosemide 98.8 Hardma 6 Regent 0.072 0.218 600 n et al hal et al 1995 1999 Glafenine 96.7 C-lab 0.7 Xu et al 0.023 0.062 1200 2008 Gliclazide 95.0 Clarke's 4.6 Xu et al 0.23 0.711 320 Analysi 2008 s of Drugs and Poisons Isoniazid 0.0 Hardma 10.5 Xu et al 10.5 76.564 300 n et al 2008 1995 Leflunomide 99.4 Clarke's 63 Regent 0.38 1.399 20 Analysi hal et al s of 1999 Drugs and Poisons Levofloxacin 40.0 Martind 5.7 Xu et al 3.42 9.464 500 ale 2008 Methotrexate 53.0 Kratoch 2.27 Regent 1.07 2.348 25, wil et al hal et al weekly 2002 1999 Methyldopa 16.0 Hardma 5 Regent 4.2 19.884 3000 n et al hal et al 1995 1999 Probenecid 95.0 Goodm 200 Regent 10 35.043 500 an hal et al Gilman 1999 1985 Propranolol 87.0 Hardma 0.3 Regent 0.039 0.150 120 n et al hal et al 1995 1999 Salicylic Acid 80.0 Hardma 250 Regent 50 362.004 topical n et al hal et al use 1995 1999 Tacrine 55.0 Hardma 0.0158 Xu et al 0.0071 0.036 160 n et al 2008 1995 Tolcapone 99.0 Martind 13 Regent 0.13 0.476 200 ale hal et al 1999 Zileuton 93.0 Martind 3.1 Xu et al 0.22 0.918 2400 ale 2008 DMD #40758 None Amoxicillin 18.0 Hardma 15 Regent 12.3 33.661 1500 n et al hal et al 1995 1999 Aricept 95.0 Martind 0.0116 Rogers 0.00058 0.002 10 ale et al 1998 Betaine 50.7 C-lab 118.9 Schwab 58.7 496.490 20000 et al 2006 Buspirone 95.0 Martind 0.004 Regent 0.0002 0.001 60 ale hal et al 1999 Clobetasol 97.5 C-lab 0.016 Hehir et 0.00039 0.001 Topical Propionate al 1983 (25mg/ wk) Cromolyn 70.0 Clarke's 0.3 Moss et 0.09 0.192 Inhalati Analysi al 1971 on s of (6.4mg) Drugs and Poisons Cycloserine 20.0 Clarke's 34 Clarke's 27.2 266.432 1000 Analysi Analysi s of s of Drugs Drugs and and Poisons Poisons Dexamethasone 68.0 Hardma 0.088 Xu et al 0.028 0.072 9 n et al 2008 1995 Dopamine 48.7 C-lab 0.023 Onasch 0.012 0.077 Intraven et al ous 2000 (20g/k g/min) Flumazenil 50.0 Hardma 0.34 Xu et al 0.17 0.561 5 n et al 2008 1995 Isoproterenol 68.0 Clarke's 0.0003 Clarke's 0.00009 0.0005 Injectio Analysi Analysi 6 n or s of s of inhalati Drugs Drugs on and and (1mg) Poisons Poisons Ketotifen 91.7 C-lab 0.0006 Clarke's 0.00005 0.0002 3 Analysi 0 s of Drugs and Poisons Methapyrilene 68.9 C-lab 0.05 Clarke's 0.016 0.060 20 Analysi s of Drugs and Poisons Pargyline 83.9 C-lab 0.16 Campb 0.026 0.162 300 ell et al 1992 Physostigmine 65.9 C-lab 0.005 Regent 0.0017 0.006 Injectio hal et al n (2mg) DMD #40758 1999 Picotamide 76.0 C-lab 2.02 Fossati 0.48 1.288 1200 et al 1992 Pinacidil 40.0 Clarke's 0.075 Xu et al 0.045 0.183 75 Analysi 2008 s of Drugs and Poisons Practolol 30.0 Kratoch 5 Regent 3.5 13.141 1200 wil et al hal et al 2002 1999 Praziquantel 91.6 C-lab 0.64 Xu et al 0.054 0.172 4200 2008 (one day adminis tration, 4 doses) Pyridoxine 0.0 Clarke's 0.02056 Xu et al 0.021 0.122 600 Analysi 4 2008 s of Drugs and Poisons Streptomycin 48.0 Hardma 37.5 Xu et al 19.5 33.529 Intramu n et al 2008 scular 1995 (2000 mg) References Axelrod J and Chenkin T.
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