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CHAPTER 3  Pharmacokinetics & Pharmacodynamics: Rational Dosing & the Time Course of Drug Action          43


                    TABLE 3–1   Pharmacokinetic and pharmacodynamic parameters for selected drugs in adults. (See Holford et al,
                                 2013, for parameters in neonates and children.)
                                    Oral       Urinary   Bound in           Volume of
                                    Availability   Excretion   Plasma   Clearance   Distribution   Target      Toxic
                     Drug           (F) (%)    (%) 1    (%)      (L/h/70 kg) 2  (L/70 kg)  Half-Life (h)  Concentration  Concentration
                     Acetaminophen      88        3        0     21             67      2         15 mg/L      >300 mg/L
                     Acyclovir          23        75       15    19.8           48      2.4       …            …
                                                                                                        3
                     Amikacin           …         98       4     5.46           19      2.3       10 mg/L …    …
                     Amoxicillin        93        86       18    10.8           15      1.7       …            …
                     Amphotericin       …         4        90    1.92           53      18        …            …
                     Ampicillin         62        82       18    16.2           20      1.3       …            …
                     Aspirin            68        1        49    39             11      0.25      …            …
                     Atenolol           56        94       5     10.2           67      6.1       1 mg/L       …
                     Atropine           50        57       18    24.6           120     4.3       …            …
                     Captopril          65        38       30    50.4           57      2.2       50 ng/mL     …
                     Carbamazepine      70        1        74    5.34           98      15        6 mg/L       >9 mg/L
                     Cephalexin         90        91       14    18             18      0.9       …            …
                     Cephalothin        …         52       71    28.2           18      0.57      …            …
                     Chloramphenicol    80        25       53    10.2           66      2.7       …            …
                     Chlordiazepoxide  100        1        97    2.28           21      10        1 mg/L       …
                     Chloroquine        89        61       61    45            13,000   214       20 ng/mL     250 ng/mL
                     Chlorpropamide     90        20       96    0.126          6.8     33        …            …
                     Cimetidine         62        62       19    32.4           70      1.9       0.8 mg/L     …
                     Ciprofloxacin      60        65       40    25.2           130     4.1       …            …
                     Clonidine          95        62       20    12.6           150     12        1 ng/mL      …
                     Cyclosporine       30        1        98    23.9           244     15        200 ng/mL    >400 ng/mL
                     Diazepam          100        1        99    1.62           77      43        300 ng/mL    …
                     Digoxin            70        67       25    9              500     39        1 ng/mL      >2 ng/mL
                     Diltiazem          44        4        78    50.4           220     3.7       …            …
                     Disopyramide       83        55       2     5.04           41      6         3 mg/mL      >8 mg/mL
                     Enalapril          95        90       55    9              40      3         > 0.5 ng/mL  …
                     Erythromycin       35        12       84    38.4           55      1.6       …            …
                     Ethambutol         77        79       5     36             110     3.1       …            >10 mg/L
                     Fluoxetine         60        3        94    40.2          2500     53        …            …
                     Furosemide         61        66       99    8.4            7.7     1.5       …            >25 mg/L
                     Gentamicin         …         76       10    4.7            20      3         3 mg/L 3     …
                     Hydralazine        40        10       87    234            105     1         100 ng/mL    …
                     Imipramine         40        2        90    63            1600     18        200 ng/mL    >1 mg/L
                     Indomethacin       98        15       90    8.4            18      2.4       1 mg/L       >5 mg/L
                     Labetalol          18        5        50    105            660     4.9       0.1 mg/L     …
                     Lidocaine          35        2        70    38.4           77      1.8       3 mg/L       >6 mg/L
                     Lithium           100        95       0     1.5            55      22        0.7 mEq/L    >2 mEq/L
                     Meperidine         52        12       58    72             310     3.2       0.5 mg/L     …
                                                                                                                   (continued)
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