TABLE 1

Summary of i.v. pharmacokinetic parameters and plasma protein binding values for 670 compounds in humans

Name
VDss
CL
fu
MRT
t1/2
l/kg ml/min/kg h
Abacavir 0.84 13 0.50 1.1 1.0
Abanoquil 6.3 14 N.F. 7.6 5.9
Acarbose 0.32 2.2 N.F. 2.4 2.7
Acebutolol 1.7 10 0.74 2.8 3.5
Acecainide (N-Acetylprocainamide) 1.9 4.0 0.90 7.9 6.4
Acetaminophen (Paracetamol) 1.0 5.0 0.52 3.3 2.5
Acetazolamide 0.37 0.65 0.04 9.5 13
N-Acetylcysteine 0.55 3.1 0.17 3.0 5.5
l-Acetylmethadol 8.3 5.4 0.20 26 18
Acetylsalicylic acid 0.22 12 0.68 0.30 0.26
Acivicin 0.50 0.69 N.F. 12 9.9
Acyclovir 0.71 4.7 0.85 2.5 2.5
Adefovir 0.42 3.7 0.96 1.9 1.6
Adinazolam 0.98 6.2 0.31 2.6 2.1
Albuterol (Salbutamol) 1.9 7.8 0.92 4.1 2.4
Alcuronium 0.32 1.3 N.F. 4.1 3.6
Alfentanil 0.45 3.9 0.086 1.9 1.6
Alfuzosin 1.5 5.9 N.F. 4.2 4.8
Alizapride 1.6 6.6 N.F. 4.0 2.8
Allopurinol 0.58 11 0.97 0.88 0.80
Almotriptan 2.2 8.9 0.60 4.2 3.4
Alosetron 1.1 8.7 0.18 2.1 1.6
Alprazolam 0.80 0.74 0.29 18 12
Alprenolol 3.2 15 0.18 3.6 2.5
Amantadine 6.6 4.8 0.33 23 16
Amdinocillin 0.37 6.3 N.F. 1.0 1.1
Amikacin 0.16 1.1 0.88 2.4 2.4
9-Aminocamptothecin 2.2 6.5 0.003 5.6 7.0
6-Aminohexanoic acid 0.39 2.5 0.92 2.6 4.9
5-Aminosalicylic acid 0.33 9.3 0.39 0.59 0.61
Amiodarone 60 1.9 0.0002 620 820
Amitriptyline 8.7 6.1 0.07 24 17
Amlodipine 17 7.0 0.005 40 34
Amoxicillin 0.25 3.3 0.85 1.3 1.1
Amphetamine 6.1 9.7 0.80 10 7.3
Ampicillin 0.22 2.8 0.85 1.3 1.4
Amrinone 1.3 8.9 0.89 2.4 2.0
Amsacrine 1.6 4.3 0.029 6.2 4.7
Amsalog 0.30 2.6 0.0011 1.9 2.4
Anhydrovinblastine 12 12 N.F. 17 18
Anidulafungin 0.57 0.21 0.16 45 40
Antipyrine 0.77 0.64 0.93 20 12
R-Apomorphine 1.6 40 0.06 0.67 0.68
Aprepitant 0.94 1.0 0.05 16 13
Argatroban 0.17 5.0 N.F. 0.57 0.40
Aripiprazole 4.9 0.83 0.01 98 75
Artesunate 15 1070 0.25 0.32 0.22
Atenolol 0.95 2.5 0.94 6.3 6.1
Atomoxetine 0.85 9.3 0.02 1.5 5.2
Atovaquone 0.60 0.15 0.001 67 63
Atracurium 0.10 5.7 0.52 0.29 0.31
Atropine 3.3 7.6 0.61 7.2 4.1
Azacytidine 0.47 35 N.F. 0.22 0.36
Azapropazone 0.12 0.14 0.004 14 17
Azelastine 15 9.0 0.17 27 22
Azimilide 13 2.4 0.06 100 79
Azithromycin 33 10 0.88 57 69
Azlocillin 0.26 2.5 0.65 1.7 1.2
Aztreonam 0.18 1.5 0.40 2.1 1.5
Bambuterol 1.6 18 N.F. 1.4 2.6
BB 83698 1.1 3.1 N.F. 5.9 9.4
Beclomethasone dipropionate 0.29 36 0.13 0.10 0.50
Benperidol 3.8 8.3 N.F. 7.5 5.8
Betamethasone 1.3 2.8 0.36 7.9 5.6
Betamipron 0.28 9.2 0.17 0.51 0.59
Betaxolol 4.8 3.4 0.40 24 17
Bevantolol 0.67 5.5 0.015 2.0 1.9
Biapenem 0.20 2.5 0.92 1.3 1.1
Bilobalide 2.5 10 N.F. 4.0 3.2
Biperiden 12 12 0.097 17 24
Bisaramil 9.0 17 N.F. 8.8 8.6
Bisoprolol 2.4 3.7 0.66 11 10
BMS-214662 0.84 9.6 N.F. 1.4 1.6
Bortezomib 10 19 0.17 8.8 18
Bosentan 0.29 2.1 0.037 2.3 4.1
Bromazepam 0.85 0.51 0.48 28 21
Bromfenac 0.11 1.3 0.0011 1.5 2.6
Bromopride 3.1 13 0.60 4.0 2.9
Brotizolam 0.75 2.0 0.092 6.0 4.8
Budesonide 3.9 20 0.13 3.2 2.8
Buflomedil 1.3 5.6 0.40 3.9 3.3
Bufuralol 1.7 8.9 0.19 3.2 2.3
Bumetanide 0.16 2.5 0.031 1.1 1.2
Bunazosin 0.72 4.8 0.06 2.5 2.0
Bupivacaine 0.84 4.3 0.056 3.3 3.1
Buprenorphine 4.9 19 0.04 4.9 3.2
Busulphan 0.55 2.4 1.0 3.8 3.4
Butorphanol 12 41 0.17 5.3 4.8
Caffeine 0.63 1.4 0.64 7.5 4.9
Captopril 0.75 12 0.73 1.0 2.0
Carbenicillin 0.17 1.9 0.52 1.5 1.1
Carboplatin 0.26 1.5 1.0 3.0 2.0
Carmustine (N,N′-bis(2-chloroethyl)-N-nitrosourea) 1.2 78 0.23 0.26 0.37
Carumonam 0.18 1.5 0.72 2.0 1.6
Carvedilol 1.3 7.8 0.02 2.8 2.4
Caspofungin 0.13 0.14 0.035 15 27
CB 10-277 0.25 1.3 N.F. 3.0 2.5
Cefadroxil 0.23 2.5 0.39 1.5 1.1
Cefamandole 0.16 3.6 0.25 0.75 0.75
Cefatrizine 0.22 3.3 0.40 1.1 1.2
Cefazolin 0.12 0.89 0.18 2.2 1.7
Cefcanel 0.13 2.6 N.F. 0.83 1.0
Cefepime 0.28 2.2 0.78 2.1 1.9
Cefetamet 0.28 1.9 0.78 2.5 2.1
Cefixime 0.24 1.0 0.31 3.9 3.2
Cefmetazole 0.13 1.5 0.15 1.5 1.5
Cefodizime 0.054 0.61 0.18 1.5 4.2
Cefoperazone 0.17 1.3 0.07 2.2 1.8
Ceforanide 0.17 0.66 0.19 4.3 3.0
Cefotaxime 0.19 2.7 0.60 1.2 1.2
Cefotetan 0.13 0.42 0.15 5.2 4.5
Cefoxitin 0.17 3.6 0.73 0.79 0.81
Cefpirome 0.24 1.9 0.90 2.1 1.7
Cefprozil 0.21 2.9 0.59 1.2 1.2
Ceftazidime 0.31 2.4 0.79 2.2 1.8
Ceftizoxime 0.20 2.1 0.72 1.6 1.5
Ceftobiprole 0.27 1.5 0.62 3.0 3.3
Ceftriaxone 0.085 0.26 0.052 5.4 8.6
Cefuroxime 0.15 2.2 0.12–0.60 1.1 1.1
Cephalexin 0.21 3.9 0.85 0.89 0.57
Cephaloridine 0.46 3.3 0.80 2.3 1.5
Cephalothin 0.070 1.8 0.22 0.65 0.95
Cephapirin 0.13 2.7 0.55 0.80 1.2
Cephradine 0.21 3.3 0.95 1.1 0.85
Cerivastatin 0.33 2.9 0.01 1.8 1.8
Cetrorelix 0.39 1.2 0.14 5.4 12
Chlorambucil 0.26 2.8 0.01 1.5 1.1
Chloramphenicol 0.94 2.4 0.34 6.5 4.6
Clorazepate 0.20 1.1 N.F. 3.0 2.4
Chlordiazepoxide 0.25 0.37 0.056 11 8.3
Chlormethiazole 6.6 33 0.36 3.3 4.5
m-Chlorophenylpiperazine 2.5 6.1 N.F. 7.0 4.7
Chloroquine 140 4.1 0.43 740 570
Chlorpheniramine 3.3 2.5 0.70 22 22
Chlorpromazine 10 16 0.056 10 11
Chlorpropamide 0.19 0.045 0.03 70 46
Chlortetracycline 0.90 2.0 0.52 7.4 7.0
Chlorthalidone 3.9 1.5 0.24 43 36
Cibenzoline 4.1 8.6 0.50 7.8 7.3
Cicaprost 0.08 3.8 N.F. 0.35 1.1
Cidofovir 0.49 2.5 1.0 3.3 2.6
Cilastatin 0.15 2.3 0.60 1.1 0.86
Cilomilast 0.23 0.50 0.006 8.5 7.9
Cimetidine 1.2 8.1 0.78 2.5 2.2
Ciprofloxacin 2.1 8.3 0.70 4.2 3.8
Cisatracurium 0.14 5.4 0.62 0.43 0.42
Citalopram 12 4.3 0.20 47 33
Cladribine 7.7 14 0.79 9.2 16
Clarithromycin 1.5 7.3 0.23 3.4 2.8
Clavulanic acid 0.22 3.1 0.91 1.0 0.90
Clevidipine 0.58 142 0.0038 0.07 0.30
Clinafloxacin 1.9 4.7 0.96 6.7 5.4
Clindamycin 0.79 4.5 0.06 2.9 2.1
Clomipramine 13 8.2 0.029 26 26
Clonazepam 2.9 0.88 0.15 55 38
Clonidine 3.3 4.0 0.56 14 7.6
Clozapine 1.6 2.5 0.055 11 10
Cocaethylene 1.6 13 0.64 2.0 1.5
Cocaine 2.0 32 0.12 1.0 0.76
Codeine 3.5 15 0.70 3.9 4.0
Colchicine 6.1 2.1 0.61 49 58
Conivaptan 0.76 3.0 0.01 4.2 6.7
Cotinine 1.1 0.89 N.F. 21 17
Cyclophosphamide 0.73 1.1 0.87 11 8.0
Cyclosporine 3.3 7.5 0.068 7.3 7.3
Dacarbazine 1.2 2.6 1.0 7.8 6.2
Dalbavancin 0.14 0.010 0.02 230 170
Dalfopristin 0.39 16 0.82 0.41 0.74
Dantrolene 0.37 0.43 N.F. 14 10
Dapsone 0.83 0.48 0.25 29 22
Daptomycin 0.088 0.16 0.083 9.2 8.1
Darifenacin 2.6 12 0.02 3.6 3.6
Decitabine 4.6 130 1.0 0.59 0.58
Delorazepam (Chlordesmethyldiazepam) 2.2 0.17 0.051 220 200
Demethylchlortetracycline 1.3 1.1 0.59 17 12
Denaverine 7.1 5.7 N.F. 21 34
4-Desacetyl-4-methylpaclitaxel carbonate 6.9 8.6 N.F. 13 31
Desipramine 15 11 0.16 23 22
Desmethyldiazepam 0.45 0.12 0.03 63 46
Desmopressin 0.30 1.4 N.F. 3.6 3.0
Dexamethasone 0.94 3.3 0.32 4.7 3.7
Dexfenfluramine 11 11 0.66 18 14
Dexloxiglumide 0.18 3.7 0.024 0.79 1.2
Dexmedetomidine 1.6 11 0.06 2.5 2.2
Dexniguldipine 8.4 9.3 N.F. 15 22
Dexrazoxane 0.55 3.1 1.0 3.0 2.5
DHA paclitaxel 0.068 0.025 0.0038 45 60
Diatrizoic acid (Amidotrizoate) 0.26 1.7 1.0 2.6 1.8
Diazepam 1.0 0.38 0.023 44 42
Diazoxide 0.21 0.060 0.06 58 48
Dibekacin 0.13 0.80 N.F. 2.7 2.4
Dichloroacetic acid 0.19 5.3 N.F. 0.60 0.65
Diclofenac 0.22 3.5 0.005 1.0 1.4
Dicloxacillin 0.11 2.0 0.033 0.92 0.88
Didanosine 0.77 11 0.95 1.2 1.4
Diflunisal 0.097 0.10 0.0016 14 10
Digitoxin 0.44 0.043 0.066 170 180
Digoxin 4.1 1.7 0.70 40 38
Dihydroquinidine 2.8 4.2 0.22 11 5.7
Dilevalol 4.8 29 N.F. 2.8 3.3
Diltiazem 4.1 13 0.18 5.3 5.6
Diphenhydramine 6.5 9.8 0.19 11 9.3
Diprafenone 1.2 11 0.017 1.9 1.5
Diprophylline 0.42 4.8 N.F. 1.5 1.7
Disopyramide 0.52 0.90 0.16 9.6 7.0
Docetaxel 2.1 14 0.04 2.5 11
Dofetilide 3.3 5.2 0.36 11 8.1
Dolasetron 2.0 180 N.F. 0.19 0.13
Domperidone 3.4 9.5 0.082 6.0 7.5
Doxacurium 0.22 2.7 0.53 1.4 1.7
Doxapram 1.2 5.3 N.F. 3.7 4.1
Doxazosin 1.3 1.6 0.017 14 10
Doxepin 12 14 0.20 15 15
Doxifluridine 0.28 11 0.61 0.46 0.35
Doxorubicin 22 15 0.28 24 32
Doxycycline 0.69 0.46 0.12 25 14
DP-b 99 1.1 14 N.F. 1.3 3.5
Drotaverine 1.9 3.5 0.12 9.0 9.3
Edrophonium 1.1 9.6 N.F. 1.9 1.8
Eletriptan 1.6 5.3 0.15 5.0 4.2
Eltanolone 2.0 22 0.010 1.5 4.7
Enalaprilat 0.38 1.6 0.62 4.0 39
Encainide 2.2 13 0.26 2.8 2.6
Endralazine 2.2 13 N.F. 2.7 5.6
Eniporide 1.1 8.2 N.F. 2.3 2.2
Enoxacin 2.0 5.4 0.80 6.2 5.1
Enprofylline 0.63 4.0 0.55 2.6 1.8
Entacapone 0.27 12 0.02 0.38 2.4
Epirubicin 45 20 0.25 38 36
Epristeride 0.54 0.33 0.03 27 27
Eprosartan 0.17 1.9 0.017 1.5 2.1
Eptifibatide 0.17 1.2 0.75 2.4 4.2
Ergotamine 3.6 15 0.02 4.0 2.1
Eritoran 0.048 0.013 N.F. 62 51
Ertapenem 0.12 0.45 0.10 4.4 3.8
Erythromycin 0.95 5.6 0.10 2.8 2.0
Esmolol 1.2 290 0.59 0.070 0.15
Estradiol 1.2 30 0.016 0.7 1.7
Estramustine phosphate 0.12 0.94 N.F. 2.1 2.4
Ethacrynic acid 0.26 8.7 N.F. 0.50 0.50
Ethambutol 1.7 10 0.18 2.7 3.1
Ethinylestradiol 4.3 7.0 0.014 11 9.7
Ethinylestradiol-17-sulfate 0.61 1.3 N.F. 7.8 9.3
Ethinylestradiol-3-sulfate 2.3 4.7 0.011 8.2 8.4
Etilefrine 2.1 14 0.77 2.5 2.2
Etomidate 2.7 13 0.23 2.9 3.5
Etoposide 0.18 0.50 0.12 6.0 5.7
Etoricoxib 1.5 0.79 0.081 32 26
Exatecan (acid) 0.44 0.96 N.F. 7.6 6.7
Famotidine 1.2 6.6 0.84 3.0 2.8
Felodipine 4.4 11 0.0036 6.7 10
Fenoterol 1.2 29 0.53 0.69 0.87
Fenoximone 1.8 29 0.30 1.0 1.0
Fenspiride 3.0 2.6 N.F. 19 14
Fentanyl 0.89 4.7 0.16 3.2 3.0
Finasteride 1.1 2.4 0.095 7.6 6.0
Flavopiridol 1.5 6.1 0.06 4.0 5.2
Flecainide 6.1 4.9 0.52 21 12
Fleroxacin 1.6 2.4 0.73 11 8.6
Flucloxacillin 0.19 2.4 0.043 1.3 1.4
Fluconazole 0.75 0.31 0.89 40 30
Flucytosine 0.68 2.0 1.0 5.7 4.2
Fludarabine 2.2 3.2 0.76 12 11
Flumazenil 0.80 16 0.58 1.0 0.78
Flunitrazepam 1.9 1.4 0.17 23 25
Fluorescein 0.14 1.3 0.11 1.8 1.6
5-Fluorouracil 0.23 26 0.64 0.15 0.12
Flupirtine 1.1 1.6 0.15 11 8.5
Fluticasone propionate 3.6 17 0.10 3.9 6.0
Fluvastatin 0.42 16 0.0079 0.44 0.70
Folinic acid 0.25 5.8 0.087 0.80 1.3
Foscarnet 0.50 2.1 0.85 4.0 4.7
Fosfluconazole 0.15 1.3 0.042 2.0 2.1
Fosfomycin 0.32 2.0 1.0 2.7 1.9
Fosinoprilat 0.13 0.32 0.006 6.8 9.4
Fostriecin 0.086 1.2 N.F. 1.2 1.5
Frovatriptan 3.6 2.5 0.85 22 24
Furosemide 0.12 1.6 0.012 1.3 2.5
Gabapentin 0.71 1.7 0.97 7.0 5.3
Gadoversetamide 0.16 1.2 1.0 2.2 1.7
Galanthamine 2.3 5.6 0.83 6.8 5.3
Ganciclovir 1.0 4.6 0.99 3.7 3.7
Gatifloxacin 1.7 2.8 0.80 11 10
Gefitinib 23 12 0.089 32 34
Gemcitabine 1.5 32 1.0 0.81 1.0
Genaconazole 0.62 0.19 N.F. 54 49
Gentamicin 0.33 1.0 1.0 5.5 4.7
Gestodene 0.46 0.80 0.023 9.6 10
Ginkgolide A 0.62 2.3 N.F. 4.6 3.8
Ginkgolide B 0.91 2.3 N.F. 6.6 5.2
Glimepiride 0.19 0.50 0.005 6.3 10
Glipizide 0.16 0.56 0.02 4.8 3.3
Glyburide 0.080 0.82 0.021 1.6 2.2
Granisetron 3.7 9.1 0.35 6.7 5.2
Guanfacine 5.6 4.5 0.28 22 15
Haloperidol 17 7.8 0.08 36 35
Hexobarbital 1.1 3.4 0.53 5.4 4.9
Hydralazine 1.5 85 0.12 0.29 1.0
Hydrocortisone 0.38 5.7 0.20 1.9 1.6
Hydroflumethiazide 2.2 9.7 N.F. 3.8 5.2
Hydromorphone 4.3 28 0.86 2.6 2.3
Hydroxychloroquine 700 11 0.57 1300 850
3′-Hydroxycotinine 0.85 1.8 N.F. 7.9 5.9
3(S)-Hydroxydihydroquinidine 6.8 12 0.47 9.4 6.7
2-Hydroxyimipramine 6.6 9.2 0.36 12 10
7-Hydroxystaurosporine 0.15 0.0037 0.0022 680 790
Hydroxyurea 0.52 1.5 1.0 4.8 3.4
Hypericin 0.25 0.13 N.F. 32 42
Ibandronic acid (Ibandronate) 0.55 1.8 0.15 5.1 14
Ibuprofen 0.15 0.82 0.006 3.0 1.6
Ibutilide 12 26 0.60 7.7 7.0
Idarubicin 38 24 0.076 26 16
Idazoxan 3.3 10 N.F. 5.5 4.2
Ifetroban 4.4 6.4 N.F. 11 22
Ifosfamide 0.62 1.1 1.0 9.4 6.6
Iloprost 0.37 16 0.40 0.39 0.57
Imatinib 3.9 3.3 0.05 20 22
Imipenem 0.24 3.0 0.86 1.3 0.95
Imipramine 12 13 0.075 15 16
Imipramine N-oxide 1.9 12 N.F. 2.6 1.8
Indinavir 0.82 18 0.36 0.76 1.0
Indocyanine green 0.035 6.8 0.05 0.086 0.065
Indomethacin 0.096 1.3 0.01 1.2 1.4
Indoramin 4.9 20 0.15 4.1 4.3
Intoplicine 11 18 N.F. 11 19
Iohexol 0.16 2.0 1.0 1.3 1.5
Iopamidol 0.28 1.9 1.0 2.5 2.1
Iopromide 0.22 1.4 0.99 2.6 2.6
Iothalamic acid (Iothalamate) 0.17 2.4 0.98 1.2 1.3
Irbesartan 0.94 2.3 0.10 6.8 14
Irinotecan 3.5 7.0 0.51 8.3 9.0
Irofulven 3.1 140 N.F. 0.40 0.30
Isepamicin 0.32 1.3 0.95 4.1 24
Isoniazid 0.82 7.4 1.0 1.8 1.0
Isoproterenol 1.5 56 0.71 0.43 0.41
Isosorbide dinitrate 1.9 31 0.72 1.0 1.7
Isosorbide-2-mononitrate 0.86 6.2 N.F. 2.3 1.9
Isosorbide-5-mononitrate 0.70 2.0 1.0 5.8 4.1
Isoxicam 0.19 0.07 0.035 44 33
Isradipine 1.5 26 0.04 1.0 3.3
Itraconazole 7.4 5.1 0.002 24 25
IVL745 0.25 11 N.F. 0.38 1.6
Ixabepilone 11 10 N.F. 18 17
Kanamycin 0.26 1.4 0.99 3.1 2.1
Ketamine 2.9 19 0.47 2.5 2.8
Ketanserin 3.9 6.7 0.055 9.7 12
Ketobemidone 0.48 9.2 N.F. 0.87 2.3
Ketoprofen 0.13 1.6 0.008 1.4 2.1
Ketorolac 0.11 0.35 0.0068 5.2 5.1
KRN-5500 0.17 2.7 N.F. 1.1 1.3
KW-2170 12 18 N.F. 11 32
Labetalol 4.8 23 0.50 3.5 4.4
Lamifiban 0.29 1.9 0.94 2.5 2.1
Lamivudine 1.3 4.8 0.94 4.4 9.1
Lansoprazole 0.28 4.4 0.021 1.1 1.0
Letrozole 1.9 0.57 0.41 59 45
Leuprolide 0.38 2.0 0.54 3.1 2.9
Levodopa 1.7 23 0.76 1.2 1.3
Levofloxacin 1.2 1.9 0.75 11 8.8
Levomepromazine 12 9.9 N.F. 21 30
Levonorgestrel 1.5 1.8 0.025 14 9.4
Levosimendan 0.24 3.8 0.02 1.1 1.1
Lidocaine 1.8 16 0.33 1.9 1.6
Lincomycin 1.0 2.1 0.14–0.72 7.5 5.6
Linezolid 0.58 1.8 0.69 5.4 4.5
Lisinopril 0.89 1.2 1.0 12 42
Lithium carbonate 0.62 1.3 1.0 7.9 7.8
Lorazepam 1.3 1.0 0.09 22 17
Lorcainide 6.6 16 0.15 6.9 6.5
Lormetazepam 1.6 4.0 0.12 6.7 4.9
Losartan 0.37 8.2 0.01 0.75 1.8
Lovastatin (acid) 0.87 7.2 0.043 1.3 1.4
Loxiglumide 0.24 1.0 N.F. 4.0 5.2
Maprotiline 45 14 0.11 54 51
Maxipost 10 15 0.0038 11 37
Mebendazole 1.2 15 0.086 1.3 1.1
Medroxalol 7.9 16 N.F. 8.2 11
Melagatran 0.23 1.9 0.93 2.0 1.6
Meloxicam 0.15 0.12 0.003 21 18
Melperone 14 46 N.F. 5.0 3.9
Melphalan 0.48 7.0 0.14 1.1 1.0
MEN-10755 2.4 2.5 N.F. 17 21
Meperidine 2.3 4.9 0.42 6.4 7.9
Mepivacaine 0.95 6.8 0.30 2.5 2.0
Meprobamate 0.70 0.60 1.0 19 14
Meptazinol 3.3 28 0.73 2.0 1.7
6-Mercaptopurine 1.0 15 0.85 1.1 1.0
Meropenem 0.30 3.9 0.87 1.3 1.0
Metformin 0.64 7.4 1.0 1.4 1.7
Methadone 4.4 1.7 0.21 43 31
Methamphetamine 4.3 4.4 0.85 16 12
Methicillin 0.32 6.6 0.43 0.80 0.64
Methimazole 0.86 3.7 N.F. 3.8 2.4
Methohexital 1.1 12 0.27 1.5 1.6
Methotrexate 0.43 2.1 0.37 3.4 3.9
Methyldopa 0.69 3.5 0.85 3.3 5.9
Methylnaltrexone 2.6 22 N.F. 2.0 2.5
7α-Methyl-19-nortestosterone 0.80 20 N.F. 0.67 0.65
Methylphenidate 2.2 0.55 0.85 4.5 4.8
Methylprednisolone 1.2 6.1 0.23 3.5 2.3
7-Methylthiomethylpaclitaxel 11 6.4 N.F. 29 32
Metoclopramide 3.2 5.7 0.60 9.4 7.2
Metocurine 0.40 1.2 0.65 5.6 5.1
Metolazone 1.6 1.4 0.05 19 20
Metoprolol 3.1 13 0.88 4.0 3.6
Metrizoate 0.17 2.7 1.0 1.0 1.3
Metronidazole 0.40 0.85 0.96 7.8 7.1
Mexiletine 5.9 8.3 0.36 12 9.9
Mezlocillin 0.09 2.1 0.70 0.71 1.2
Mibefradil 3.1 4.0 0.005 13 13
Micafungin 0.21 0.17 0.0023 21 16
Midazolam 1.1 5.3 0.017 3.5 3.1
Miglitol 0.28 1.7 1.0 2.7 2.3
Milrinone 0.25 6.2 0.035 0.67 0.80
Minocycline 1.6 1.2 N.F. 22 17
Mirtazapine 4.2 8.0 0.15 8.8 15
Mitoxantrone 12 7.9 0.25 25 53
Mivacurium (cis/cis) 0.27 5.2 0.70 0.87 0.83
Moclobemide 1.1 10 0.77 1.8 1.5
Montelukast 0.15 0.68 0.002 3.8 5.0
Morphine 2.3 26 0.65 1.5 2.0
Morphine-6-glucuronide 0.12 2.2 N.F. 0.91 1.4
Moxalactam 0.17 0.72 0.39 3.9 2.9
Moxifloxacin 1.4 2.4 0.60 9.7 8.2
Moxonidine 1.8 11 0.93 2.7 2.2
Nadolol 1.9 2.9 0.14 11 9.2
Nafcillin 0.22 3.3 0.13 1.1 0.70
Nalbuphine 4.6 22 0.50 3.5 3.7
Nalmefene 8.2 15 0.65 9.1 8.8
Naloxone 1.7 23 0.54 1.2 1.1
Naltrexone 7.6 57 0.79 2.2 1.9
Napsagatran 0.36 6.4 N.F. 0.94 1.9
Naratriptan 2.4 6.6 0.70 6.1 6.6
Nateglinide 0.15 1.8 0.029 1.4 1.5
Nebivolol 11 14 N.F. 13 10
Nefazodone 0.51 7.5 0.01 1.1 1.2
Nefopam 5.6 12 N.F. 8.1 5.0
Nelarabine 4.9 81 0.80 1.0 0.50
Neostigmine 0.74 9.2 N.F. 1.3 1.3
Netilmicin 0.073 0.55 1.0 2.2 3.2
Nevirapine 1.3 0.30 0.32 81 53
Nicardipine 1.0 11 0.01 1.5 4.1
Nicotine 2.6 18 0.95 2.4 2.0
Nifedipine 0.79 7.3 0.044 1.8 1.9
Nimodipine 1.1 15 0.016 1.2 1.3
Nisoldipine 5.5 15 0.003 6.5 11
Nitrazepam 1.7 0.86 0.13 33 26
Nitrendipine 6.1 25 0.02 4.1 8.2
Nitrofurantoin 0.57 9.7 0.17 0.98 0.97
Nizatidine 1.0 9.8 0.65 1.7 1.5
NK 611 0.30 0.40 0.013 17 14
Nomifensine 6.0 22 0.40 4.5 6.5
Nortilidine 2.5 9.9 N.F. 4.2 4.4
Nortriptyline 22 10 0.12 37 30
Ofloxacin 1.6 2.5 0.75 11 8.9
Olcegepant 0.31 2.6 N.F. 1.9 2.5
Olsalazine 0.070 1.2 N.F. 0.97 0.90
Omeprazole 0.24 8.4 0.05 0.48 0.58
Ondansetron 1.8 5.8 0.27 5.2 3.4
Oseltamivir acid 0.37 4.8 0.97 1.3 1.8
Oxacillin 0.19 6.3 0.07 0.50 0.70
Oxazepam 0.59 1.1 0.04 8.9 6.7
Oxiracetam 0.55 1.8 N.F. 4.9 7.5
Oxybutynin 0.85 5.1 0.0034 2.7 7.2
Oxycodone 2.5 6.1 0.55 6.8 5.5
Oxytetracycline 1.7 2.0 0.90 12 10
Paclitaxel 3.0 6.4 0.12 7.8 11
Palonosetron 6.3 2.6 0.38 40 39
Pamidronic acid (Pamidronate) 1.8 2.5 N.F. 12 32
Pancuronium 0.20 1.5 0.090 2.2 1.9
Panipenem 0.19 2.6 N.F. 1.2 0.96
Pantoprazole 0.17 2.2 0.02 1.9 1.9
Papaverine 1.0 11 0.073 1.4 1.8
Paricalcitol 0.41 0.89 0.0016 7.7 5.3
Paroxetine 18 18 0.06 17 13
Pefloxacin 1.5 2.0 0.75 13 11
Penciclovir 1.1 8.4 0.84 2.4 2.1
Penicillin G 0.24 6.9 0.40 0.58 0.70
Pentamidine 53 74 N.F. 12 25
Pentazocine 3.4 23 0.39 2.5 2.5
Pentobarbital 0.91 0.47 0.39 32 22
Pentoxifylline 1.8 39 N.F. 0.77 1.2
Perindoprilat 0.76 1.7 0.16 7.6 29
Perphenazine 18 27 0.07 11 9.4
Phenacetin 1.4 21 0.47 1.1 0.92
Phencyclidine 6.9 5.1 0.35 23 16
Phenethicillin 0.30 4.2 0.25 1.2 0.91
Phenobarbital 0.54 0.063 0.49 140 99
Phenoxymethylpenicillin 0.41 6.8 0.45 1.0 0.84
Pimobendan 2.0 14 0.024 2.2 1.8
Pindolol 1.2 7.7 0.58 2.6 2.2
Piperacillin 0.27 4.0 0.50 1.1 0.96
Pipecuronium 0.35 3.0 0.98 1.9 1.9
Piretanide 0.17 3.1 0.058 0.91 1.3
Piritramide 4.7 7.8 0.061 10 8.0
Pirmenol 1.4 1.8 0.13 13 8.4
PNU-145156E 0.27 0.0047 N.F. 960 730
Pravastatin (acid) 0.46 14 0.50 0.59 0.78
Prazosin 0.73 4.7 0.060 2.6 2.0
Prednisolone 0.86 2.9 0.25 4.8 3.4
Prednisone 0.57 2.5 0.27 3.8 2.9
Prilocaine 3.7 29 0.72 2.2 1.8
Primaquine 4.0 5.8 N.F. 11 7.1
Probenecid 0.13 0.25 0.13 8.7 5.9
Procainamide 2.2 10 0.84 3.7 3.1
Prochlorperazine 22 16 N.F. 23 9.0
Procyclidine 0.74 0.86 N.F. 14 12
Promazine 8.1 14 0.11 9.6 7.9
Promethazine 14 14 0.09 17 14
Propafenone 2.2 16 0.038 2.2 2.1
Propofol 4.7 36 0.016 2.2 3.2
Propoxyphene 12 15 0.24 13 18
Propranolol 3.1 12 0.13 4.3 3.4
Propylthiouracil 0.34 3.1 0.18 1.8 1.3
Pseudohypericin 0.56 0.62 N.F. 15 20
Pyridostigmine 1.1 9.6 1.0 1.8 1.5
Pyrimethamine 0.43 0.052 0.095 140 140
Quercetin 0.12 11 0.009 0.20 0.60
Quinacrine 45 5.1 0.13 150 120
Quinaprilat 0.13 0.93 0.32 2.3 2.3
Quinidine 2.9 4.0 0.26 12 6.6
Quinine 1.8 1.9 0.30 16 11
Quinupristin 0.67 16 0.34 0.70 0.87
Rabeprazole 0.22 4.0 0.037 0.92 1.0
Ranitidine 1.2 9.6 0.95 2.1 2.1
Reboxetine 0.65 0.82 0.019 13 10
Recainam 1.4 4.5 0.86 5.2 5.0
Remifentanil 0.40 37 0.30 0.18 0.80
Remoxipride 0.65 1.7 0.16 6.4 5.5
Repaglinide 0.35 7.8 0.015 0.75 0.87
Repinotan 0.21 2.2 N.F. 1.6 1.2
Ribavirin 14 5.2 1.0 45 45
Ribostamycin 0.25 1.5 N.F. 2.8 2.5
Rifabutin 9.3 2.4 0.29 65 37
Rifampin 0.97 3.5 0.20 4.6 3.8
Risedronic acid (Risedronate) 6.3 1.5 0.76 70 200
Risperidone 1.1 5.4 0.10 3.4 3.2
Ritodrine 4.4 31 0.64 2.4 2.6
Rivastigmine 1.3 12 0.60 1.9 1.4
Rizatriptan 1.9 16 0.86 2.0 2.2
Rocuronium 0.21 3.7 0.54 0.95 1.6
Rolitetracycline 0.54 0.97 0.50 9.3 8.8
Romidepsin 1.2 7.4 N.F. 2.6 11
Ropivacaine 0.75 5.5 0.06 2.3 2.2
Roquinimex 0.21 0.082 N.F. 43 31
Rosiglitazone 0.20 0.65 0.002 5.1 3.9
Rosuvastatin 1.7 11 0.12 2.6 2.0
RPR 109881A 12 14 N.F. 14 20
Saquinavir 3.6 13 0.028 4.6 13
SarCNU 0.76 9.0 N.F. 1.4 1.0
Sch34343 0.30 7.5 0.35 0.67 0.80
Scopolamine 3.1 16 N.F. 3.2 4.5
Selegiline 1.9 20 0.13 1.6 1.3
Sematilide 0.82 3.7 0.96 3.7 3.8
Sildenafil 1.4 9.1 0.04 2.6 3.9
Sisomicin 0.19 1.0 0.15 3.2 2.4
Sitafloxacin 1.5 3.7 0.51 6.7 6.6
Sitagliptin 2.8 6.0 0.62 7.8 12
Solifenacin 8.2 2.1 0.02 65 52
Sotalol 1.3 2.0 0.62 11 6.3
Sparfloxacin 3.9 2.7 0.55 24 20
Spectinomycin 0.13 0.99 N.F. 2.2 1.8
Squalamine 0.23 1.2 N.F. 3.2 9.5
Stavudine 0.67 8.2 1.0 1.4 1.4
Streptomycin 0.34 0.78 0.65 7.3 4.3
Sufentanil 9.4 15 0.075 10 14
Sulbactam 0.32 5.1 0.62 1.0 1.1
Sulbenicillin 0.15 1.6 0.50 1.6 1.2
Sulfadiazine 0.29 0.55 0.44 8.8 7.0
Sulfamethoxazole 0.30 0.36 0.23 14 9.8
Sulfinpyrazone 0.12 0.34 0.017 5.9 6.2
Sulfisoxazole 0.17 0.30 0.079 9.4 7.4
Sumatriptan 1.7 19 0.83 1.5 1.7
Suprofen 0.040 0.76 0.006 0.88 2.1
Suramin 0.54 0.0057 0.003 1400 1200
Tacrine 11 56 0.25 3.3 3.3
Tacrolimus 1.2 0.70 0.01 27 26
Talinolol 3.3 4.9 0.39 11 11
Tamsulosin 0.21 0.62 0.01 5.6 6.8
Tegaserod 5.3 18 0.02 4.9 11
Teicoplanin A2-1 1.5 0.20 0.11 140 150
Telavancin 0.11 0.20 0.07 9.2 6.7
Telithromycin 3.0 14 0.41 3.6 12
Telmisartan 5.3 8.4 0.004 11 20
Temozolomide 0.50 3.6 N.F. 2.3 1.5
Temsirolimus 3.0 7.7 N.F. 10 18
Teniposide 0.41 0.19 0.0044 37 16
Tenofovir 0.83 3.1 0.93 3.8 5.8
Tenoxicam 0.19 0.03 0.0085 92 67
Terazosin 0.98 1.1 0.08 15 9.0
Terbutaline 1.5 3.4 0.75 7.4 15
Terodiline 5.1 1.1 0.08 81 56
Tesaglitazar 0.13 0.039 0.0011 56 45
Tetracycline 1.2 1.5 0.78 12 9.4
Δ9-Tetrahydrocannabinol 8.9 3.2 0.05 46 33
Tezosentan 0.28 8.1 0.0085 0.58 3.8
Thalidomide 0.95 3.4 0.40 4.3 4.7
Theophylline 0.51 0.86 0.61 9.9 7.2
Thionylan (Methapyrilene) 3.3 28 N.F. 2.0 1.6
Thiopental 1.2 8.2 0.14 2.4 2.0
Thiotepa 1.6 6.7 0.90 4.0 2.7
Tiagabine 1.1 1.6 0.04 12 10
Tiazofurin 1.1 2.4 N.F. 7.6 5.9
Ticarcillin 0.16 1.8 0.55 1.5 1.0
Tigecycline 12 3.8 0.20 53 48
Tilidine 4.0 16 0.21 4.2 5.0
Timolol 1.5 8.5 0.90 3.0 2.2
Tinidazole 0.59 0.60 0.80 16 13
Tirapazamine 0.56 8.9 0.81 1.0 0.78
Tirofiban 0.99 4.3 0.36 1.8 1.6
Tizanidine 2.4 11 0.70 3.6 2.4
Tobramycin 0.23 1.6 1.0 2.4 2.0
Tocainide 1.8 2.2 0.87 14 12
Tolamolol 4.0 14 0.089 4.8 2.5
Tolbutamide 0.12 0.21 0.05 9.5 7.0
Tolcapone 0.12 1.9 0.0012 1.1 1.1
Toloxatone 1.5 11 0.49 2.3 1.6
Tolterodine 1.5 8.4 0.037 3.0 2.4
Tomopenem 0.23 1.9 0.91 2.0 1.7
Topixantrone 57 27 N.F. 39 45
Topotecan 1.8 13 0.65 2.3 2.3
Torsemide 0.21 0.53 0.01 6.6 5.1
Trabectedin 25 12 N.F. 35 44
Tramadol 2.8 6.5 0.80 7.2 5.8
Tranexamic acid 0.38 2.4 N.F. 2.6 2.3
Traxoprodil 4.4 27 0.63 2.6 3.7
Trazodone 0.52 1.4 N.F. 6.2 7.3
Triamcinolone acetonide 1.4 9.4 0.20 2.5 2.4
Triamterene 13 63 0.42 3.4 4.3
Triazolam 0.58 3.0 0.10 3.2 2.7
Trimazosin 0.18 0.96 N.F. 3.1 3.1
Trimethoprim 1.5 2.1 0.50 12 9.6
Trimetrexate 0.77 0.77 0.05 17 17
Trimipramine 16 16 0.051 17 23
Tropisetron 9.7 26 N.F. 6.3 5.6
Trospectomycin 0.70 1.7 N.F. 6.9 11
Trovafloxacin 1.3 1.4 0.24 15 11
Troxacitabine 1.0 2.4 N.F. 6.9 82
Tubocurarine 0.45 3.4 0.58 2.2 2.0
UK-240,455 0.80 6.0 0.13 2.2 1.4
Urapidil 0.75 3.1 N.F. 4.0 3.5
Valproic acid 0.14 0.16 0.08 15 12
Valsartan 0.22 0.49 0.04 7.5 9.5
Valspodar 1.8 2.6 0.022 12 10
Vancomycin 0.54 1.3 0.70 6.9 6.5
Vardenafil 3.0 13 0.05 3.8 4.5
Vecuronium bromide 0.30 4.5 0.25 1.1 1.4
Venlafaxine 4.4 14 0.73 5.2 5.0
Verapamil 3.7 18 0.093 3.4 2.8
Verlukast 0.11 0.68 0.0004 2.7 2.3
Viloxazine 0.73 2.1 N.F. 5.8 4.1
Vinblastine 28 3.1 0.14 150 67
Vincristine 2.4 2.0 0.40 20 23
Vindesine 5.0 2.2 N.F. 38 35
Vinorelbine 23 20 0.87 18 26
Voriconazole 2.2 8.3 0.42 4.4 5.6
Vorinostat 0.50 28 0.29 0.30 0.76
Warfarin 0.13 0.055 0.015 39 29
Xamoterol 0.64 3.0 0.97 3.6 7.7
Zalcitabine 0.54 5.6 N.F. 1.6 1.2
Zaleplon 1.3 16 0.40 1.4 1.1
Zanamivir 0.23 1.6 0.86 2.4 1.7
Zidovudine 1.8 25 0.80 1.2 1.3
Ziprasidone 1.0 5.1 0.0012 3.3 3.1
Zoledronic acid 0.60 2.2 0.78 4.5 11
Zolmitriptan 1.8 6.7 0.75 4.6 3.6
Zolpidem 0.54 4.3 0.08 2.1 1.7
Zonampanel 0.19 5.3 N.F. 0.60 0.78
Zopiclone 1.3 3.3 0.20 6.6 5.2
Zotarolimus
1.3
0.67
N.F.
33
35

  • N.F., data not found; SarCNU, sarmustine