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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)