附录 某些药物代谢动力学数据
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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Bamphotericin 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 |
地尔硫卓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Gpenicillin G | 22 | 70 | 60 | - | 0.2 | 0.6 |
青霉素Vpenicillin 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 The pharmacological basis of therapeuties. 8th ed.Macmillan,1990:1655~1715.
②Melmon K.L.and Morrelli:Clinical pharmacology.3rd ed.Mcgraw-Hill,1992:1029~1072.
③Herfindal E.T.et al:Clinical pharmacy and Therapeutics.3rd ed.1992:364~368.