附录 某些药物代谢动力学数据
| 药 物 | 生物利用度(%) | 尿排泄(%) | 血浆蛋白结合(%) | 清除率(ml·min-1·kg-1) | 分布容积(L/kg) | 半衰期(h) |
| 醋丁洛尔 acebutolol | 37 | 40 | 26 | 6.8 | 1.2 | 2.7 |
| 阿昔洛韦 aciclovir | 15~30 | 75 | 15 | 3.37 | 0.69 | 2.4 |
| 别嘌醇 allopurinol | 80~90 | <10 | <1 | 12.7 | 0.6~1.6 | 1~3 |
| 阿普洛尔 alprenolol | 8.6 | 0.2 | 85 | 15 | 3.3 | 2.5 |
| 金刚烷胺 amantadine | 50~90 | 50~90 | 67 | 4.8 | 6.6 | 16 |
| 两性霉素B amphotericin B | - | 2~5 | >90 | 0.46 | 0.76 | 18 |
| 阿米卡星 amikacin | - | 98 | 4 | 1.3 | 0.27 | 2.3 |
| 胺碘酮 amiodarone | 46 | 0 | 100 | 1.9 | 66 | 25d |
| 阿米替林 amitriptyline | 48 | <2 | 94.8 | 11.5 | 15 | 21.5 |
| 氨苄西林 ampicillin | 62 | 82 | 18 | 1.7 | 0.28 | 1.3 |
| 阿斯匹林 aspirin | 68 | 1.4 | 49 | 9.3 | 0.15 | 0.25 |
| 阿替洛尔 atenolol | 56 | 94 | <5 | 2.4 | 0.95 | 6.1 |
| 阿曲库铵 atracurium | - | <1 | - | 5.5 | 0.16 | 0.33 |
| 阿托品 atropine | 50 | 57 | 14~22 | 5.9 | 1.7 | 4.3 |
| 硫唑嘌呤 azathioprine | 60 | <2 | - | 57 | 0.81 | 0.16 |
| 倍他米松 betamethasone | 72 | 4.8 | 64 | 2.9 | 1.4 | 5.6 |
| 博莱霉素 bleomycin | - | 68 | - | 1.1 | 0.27 | 3.1 |
| 布美他尼 bumetanide | 81 | 62 | 99 | 2.6 | 0.13 | 0.8 |
| 布比卡因 bupivacaine | - | 2 | 95 | 7.1 | 0.9 | 2.4 |
| 咖啡因 caffeine | 100 | 1.1 | 36 | 1.4 | 0.61 | 4.9 |
| 卡托普利 captopril | 65 | 38 | 30 | 12 | 0.81 | 2.2 |
| 卡马西平 carbamazepine | >70 | <1 | 74 | 1.3 | 1.4 | 15 |
| 羧苄西林 carbenicillin | - | 82 | 50 | 0.68 | 0.18 | 1.0 |
| 头孢克洛 cefaclor | - | 52 | 25 | 6.1 | 0.36 | 0.67 |
| 头孢氨苄 cefalexin | 90 | 91 | 14 | 4.3 | 0.26 | 0.9 |
| 头孢孟多 cefamandole | - | 96 | 74 | 2.8 | 0.16 | 0.78 |
| 头孢唑林 cefazolin | - | 80 | 89 | 0.95 | 0.12 | 1.8 |
| 头孢哌酮 cefoperazone | - | 29 | 89~93 | 1.2 | 0.09 | 2.1 |
| 头孢噻肟 cefotaxime | - | 50 | 36 | 3.7 | 0.23 | 1.1 |
| 头孢拉定 cefradine | >90 | 86 | 14 | 5.1 | 0.25 | 0.77 |
| 头孢曲松 ceftriaxone | - | 46 | 90~95 | 0.24 | 0.16 | 7.3 |
| 头孢呋辛 cefuroxime | - | 96 | 33 | 0.94 | 0.19 | 1.7 |
| 苯丁酸氮芥 chlorambucil | 87 | <1 | 99 | 2.6 | 0.29 | 1.3 |
| 氯霉素 chloramphenicol | 75~90 | 25 | 53 | 2.4 | 0.94 | 4.0 |
| 氯喹 chloroquine | 89 | 61 | 61 | 1.8 | 115 | 41 |
| 氯噻嗪 chlorothiazide | 9~56 | 92 | 94.6 | 4.5 | 0.20 | 1.5 |
| 氯丙嗪 chlorpromazine | 32 | 〈1 | 95~98 | 8.6 | 21 | 30 |
| 氯酞酮 chlortalidone | 64 | 65 | 75 | 1.6 | 3.9 | 44 |
| 西米替丁 cimetidine | 62 | 62 | 19 | 8.3 | 1.0 | 2.0 |
| 环丙沙星 ciprofloxacin | 60 | 65 | 40 | 6.0 | 1.8 | 4.1 |
| 顺铂 cisplatin | - | 23 | - | 6.3 | 0.28 | 0.53 |
| 氯贝特 clofibrate | 95 | 5.7 | 96.5 | 0.12 | 0.11 | 13 |
| 氯硝西泮 clonazepam | 98 | <1 | 86 | 1.55 | 3.2 | 23 |
| 可乐定 clonidine | 95 | 62 | 20 | 3.1 | 2.1 | 12 |
| 可卡因 cocaine | 57 | <2 | 91 | 32 | 2.0 | 0.8 |
| 可待因 codeine | 50 | 0 | 7 | 11 | 2.6 | 2.9 |
| 环磷酰胺 cyclophosphamide | 74 | 6.5 | 13 | 1.3 | 0.78 | 7.5 |
| 环孢霉素 cyclosporine | 23 | <1 | 93 | 5.9 | 1.2 | 5.6 |
| 氨苯砜 dapsone | 93 | 15 | 73 | 0.6 | 1.0 | 22 |
| 地塞米松 dexamethasone | 78 | 2.6 | 68 | 3.7 | 0.82 | 3.0 |
| 地西泮 diazepam | 100 | <1 | 98.7 | 0.38 | 1.1 | 43 |
| 洋地黄毒甙 digitoxin | >90 | 32 | 97 | 0.055 | 0.54 | 6.7d |
| 地高辛 digoxin | 70 | 60 | 25 | 0.88 | - | 39 |
| 地尔硫
diltiazem | 44 | <4 | 78 | 12 | 3.1 | 3.7 |
| 苯海拉明 diphenhydramine | 72 | 1.9 | 78 | 6.2 | 4.5 | 8.5 |
| 丙吡胺 disopyramide | 83 | 55 | - | 1.2 | 0.59 | 6.0 |
| 多巴酚丁胺 dobutamine | - | - | - | 59 | 0.2 | 2.4 |
| 阿霉素 doxorublicin | 5 | <15 | 79~85 | 17 | 25 | 30 |
| 多西环素 doxycycline | 93 | 41 | 88 | 0.53 | 0.75 | 16 |
| 依那普利 enalapril | 41 | 88 | <50 | 4.9 | 1.7 | 11 |
| 依诺沙星 enoxacin | 79 | 60 | 0 | - | - | 5 |
| 红霉素 erythromycin | 35 | 12 | 84 | 9.1 | 0.78 | 1.6 |
| 艾司洛尔 esmolol | - | <1 | 55 | 170 | 1.9 | 0.13 |
| 乙胺丁醇 ethambutol | 77 | 79 | <5 | 8.6 | 1.6 | 3.1 |
| 乙醇 ethanol | 80 | <3 | - | - | 0.54 | 0.24 |
| 炔雌醇 ethinylestradiol | 40 | - | 98 | 6.3 | 1.5~4.3 | 6~20 |
| 法莫替丁 famotidine | 45 | 67 | 17 | 7.1 | 1.3 | 2.6 |
| 芬太尼 fentanyl | - | 8 | 84 | 13 | 4.0 | 3.7 |
| 氟卡尼 flecainide | 70 | 43 | 61 | 5.6 | 4.9 | 11 |
| 氟氯西林 flucloxacillin | 49 | 41 | 96 | - | 0.11 | 0.8 |
| 氟尿嘧啶 fluorouracil | 28 | <10 | 8~12 | 16 | 0.25 | 11 |
| 氟奋乃静 fluphenazine | - | - | - | - | 20 | 14.7~15.3 |
| 呋噻米 furosemide | 61 | 66 | 98.8 | 2.0 | 0.11 | 92 |
| 庆大霉素 gentamicin | - | >90 | <10 | 0.82 | 0.31 | 2~3 |
| 格列本脲 glibenclamide | 90 | 1 | 99 | 1.5 | 0.12 | 1.6 |
| 胍乙啶 guanethidine | 35 | 43 | 0 | - | 60 | 120 |
| 氟哌啶醇 haloperidol | 61 | 1 | 92 | 11.8 | 18 | 18 |
| 肝素 heparin | - | 0 | - | - | 0.058 | 12 |
| 肼屈嗪 hydralazine | 16~35 | 1~15 | 87 | 56 | 1.5 | 0.96 |
| 氢氯噻嗪 hydrochlorothiazide | 71 | >95 | 58 | 4.9 | 0.83 | 2.5 |
| 氢化可的松 hydrocortisone | - | <1 | 90~95 | - | - | 1~2 |
| 布洛芬 ibuprofen | >80 | <1 | >99 | 0.75 | 0.15 | 2 |
| 米帕明 imipramine | 40 | <2 | 90.1 | 15 | 23 | 18 |
| 吲哚美辛 indometacin | 98 | 15 | 90 | 2.0 | 0.26 | 2.4 |
| 胰岛素 insulin | - | <2 | 5 | - | 0.08 | 0.1~0.3 |
| 异烟肼 isoniazid | - | 7~29 | 0 | 3.7~7.4 | 0.67 | 1.1~3.1 |
| 硝酸异山梨酯 isosorbide dinitrate | 22~30 | <1 | 28 | 45 | 1.5 | 0.8 |
| 5-单硝酸异山梨酯 isosorbide-5-mononitrate | 93 | <5 | 0 | 1.81 | 0.79 | 4.4 |
| 卡那霉素 kanamycin | - | 90 | 0 | 1.4 | 0.26 | 2.1 |
| 酮康唑 ketoconazole | - | <1 | 99 | 8.4 | 2.4 | 3.3 |
| 拉贝洛尔 labetalol | 18 | <5 | 50 | 25 | 9.4 | 4.9 |
| 左旋多巴 levodopa | - | - | - | 7.7~13 | 0.8~1.1 | 2.2 |
| 利多卡因 lidocaine | 35 | 2 | 70 | 9.2 | 1.1 | 1.8 |
| 林可霉素 lincomycin | 100 | 20 | 72 | - | 0.44 | 5 |
| 锂盐 lithium | 100 | 95 | 0 | 0.35 | 0.79 | 22 |
| 洛伐他汀 lovastatin | 5 | <10 | 95 | 5~21 | - | 1.1~1.7 |
| 巯嘌呤 mercaptopurine | 12 | 22 | 19 | 11 | 0.56 | 0.9 |
| 美沙酮 methadone | 92 | 24 | 89 | 1.4 | 3.8 | 35 |
| 甲氨蝶呤 methotrexate | 70 | 48 | 34 | 2.1 | 0.55 | 7.2 |
| 甲氧氯普胺 metoclopramide | 76 | 20 | 40 | 6.2 | 3.4 | 5.0 |
| 美托洛尔 metoprolol | 38 | 10 | 11 | 15 | 4.2 | 3.2 |
| 甲硝唑 metronidazole | 99 | 10 | 10 | 1.3 | 0.74 | 8.5 |
| 美西律 mexiletine | 87 | 4~15 | 63 | 6.3 | 4.9 | 9.2 |
| 米诺环素 minocycline | 95~100 | 11 | 76 | 1.0 | 1.3 | 16 |
| 米诺地尔 minoxidil | - | 20 | 0 | 24 | 2.7 | 3.1 |
| 吗啡 morphine | 24 | 6~10 | 35 | 24 | 3.3 | 1.9 |
| 纳多洛尔 nadolol | 34 | 73 | 20 | 2.9 | 1.9 | 16 |
| 纳洛酮 naloxone | 2 | 0 | - | 22 | 2.1 | 1.1 |
| 萘普生 naproxen | 99 | <1 | 99.7 | 0.13 | 0.16 | 14 |
| 新斯的明 neostigmine | - | 67 | - | 8.4 | 0.7 | 1.3 |
| 尼卡地平 nicardipine | 19~38 | <1 | 89~99.5 | 13.4 | 1.1 | 1.3 |
| 硝苯地平 nifedipine | 50 | 0 | 96 | 7.0 | 0.78 | 1.8 |
| 硝西泮 nitrazepam | 78 | <1 | 87 | 0.86 | 1.9 | 26 |
| 硝酸甘油 nitroglycerin | <1 | <1 | - | 230 | 3.3 | 2.3min |
| 炔诺酮 norethisterone | 65 | - | 80 | - | 1.5~4.3 | 5~14 |
| 诺氟沙星 norfloxacin | 30~40 | 26~32 | 15~20 | 7.2 | 3.2 | 5 |
| 奥美拉唑 omeprazole | - | <1 | 95 | - | 0.19~0.48 | 1~2.3 |
| 昂丹司琼 ondansetron | 60 | <10 | 70~76 | 10~12 | 2.3 | 3~3.5 |
| 对乙酰氨基酚 paracetamol | 88 | 3 | 0 | 5.0 | 0.95 | 2.0 |
| 培氟沙星 pefloxacin | 1 | <10 | 20~30 | 2.3 | 1.5~1.9 | 7~14 |
| 青霉素G penicillin G | 22 | 70 | 60 | - | 0.2 | 0.6 |
| 青霉素V penicillin V | 60~73 | 26~65 | 75~89 | - | 0.5 | 0.5 |
| 戊巴比妥 pentobarbital | >90 | <1 | 35~45 | 0.8 | 1 | 35~45 |
| 哌替啶 pethidine | 52 | 1~25 | 58 | 17 | 4.4 | 3.2 |
| 苯巴比妥 phenobarbital | 100 | 24 | 51 | 0.062 | 0.54 | 99 |
| 保泰松 phenybutazone | 80~100 | 1 | 96.1 | 0.023 | 0.097 | 56 |
| 苯妥英 phenytoin | 90 | 2 | 89 | - | 0.64 | 6~24 |
| 吲哚洛尔 pindolol | 75 | 54 | 51 | 8.3 | 2.3 | 3.6 |
| 哌拉西林 piperacillin | - | 71 | 16~48 | 2.6 | 0.18 | 0.93 |
| 吡罗昔康 piroxicam | - | <5 | 99.3 | 0.036 | 0.15 | 48 |
| 哌唑嗪 prazosin | 68 | <1 | 95 | 3.0 | 0.6 | 2.9 |
| 泼尼松龙 prednisolone | 82 | 26 | 90~95 | 8.7 | 1.5 | 2.2 |
| 泼尼松 prednisone | 80 | 3 | 75 | 3.6 | 0.97 | 3.6 |
| 普鲁卡因胺 procainamide | 83 | 67 | 16 | 2.7 | 1.9 | 3.0 |
| 异丙嗪 promethazine | - | - | 70~80 | 18 | 13 | 12 |
| 普罗帕酮 propafenone | 3~40 | <1 | 97 | - | - | 9~25(PM) 3~8(EM) |
| 普萘洛尔 propafenone | 26 | <0.5 | 87 | 16 | 4.3 | 3.9 |
| 乙胺嘧啶 pyrimethamine | - | 65 | 87 | 0.41 | 2.9 | 83 |
| 奎尼丁 quinidine | 80 | 18 | 87 | 4.7 | 2.7 | 6.2 |
| 雷尼替丁 ranitidine | 52 | 69 | 15 | 10.4 | 1.3 | 2.1 |
| 利福平 rifampin | - | 7 | 89 | 3.5 | 0.97 | 3.5 |
| 东莨菪碱 scopolamine | 27 | 6 | - | 16 | 1.4 | 2.9 |
| 索他洛尔 sotalol | 60 | 60 | 54 | - | 0.7 | 9 |
| 链激酶 streptokinase | - | 0 | - | 0.15 | 0.016 | 1.4 |
| 链霉素 streptomycin | - | 50~60 | 48 | 1.2 | 0.25 | 2.6 |
| 磺胺嘧啶 sulfadiazine | 100 | 57 | 54 | 0.55 | 0.29 | 9.9 |
| 磺胺异恶唑 sulfafurazole | 96 | 49 | 91.4 | 0.33 | 0.15 | 6.6 |
| 磺胺甲恶唑 sulfamethoxazol | 100 | 14 | 62 | 0.32 | 0.21 | 10.1 |
| 舒林酸 sulindac | - | 0 | 99.4 | 1.5 | 2 | 15 |
| 特布他林 terbutaline | 14 | 56 | 20 | 3.4 | 1.8 | 14 |
| 硫喷妥 thiopental | - | <1 | 85 | 3.9 | 2.3 | 9.0 |
| 替卡西林 ticarcillin | - | 92 | 65 | 2.0 | 0.21 | 1.3 |
| 噻马洛尔 timolol | 50 | 15 | 60 | 7.3 | 2.1 | 4.1 |
| 妥布霉素 tobramycin | - | 90 | <10 | 0.98 | 0.33 | 2.2 |
| 甲苯磺丁脲 tolbutamide | 93 | 0 | 96 | 0.24 | 0.10 | 5.9 |
| 氨苯蝶啶 triamterene | 54 | 52 | 61 | 63 | 13.4 | 4.2 |
| 筒箭毒碱 tubocurarine | - | 63 | 50 | 1.9 | 0.39 | 2.0 |
| 万古霉素 vancomycin | - | 79 | 30 | 1.4 | 0.39 | 5.6 |
| 维库溴铵 vecuronium bromide | - | 18 | 30 | 3.0 | 2.1 | 1.5 |
| 维拉帕米 verapamil | 22 | <3 | 90 | 15 | 5 | 4.0 |
| 华法林 warfarin | 93 | <2 | 99 | 0.045 | 0.14 | 37 |
本表资简化自①A.G.Gilman et al(ed):Goodman and Gilman’s Thepharmacological basis of therapeuties. 8th ed.Macmillan,1990:1655~1715.
②Melmon K.L.andMorrelli:Clinical pharmacology.3rd ed.Mcgraw-Hill,1992:1029~1072.
③Herfindal E.T.etal:Clinical pharmacy and Therapeutics.3rd ed.1992:364~368.
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