Page 58 - Basic _ Clinical Pharmacology ( PDFDrive )

44 SECTION I Basic Principles

TABLE 3–1 Pharmacokinetic and pharmacodynamic parameters for selected drugs in adults. (See Holford et al,
2013, for parameters in neonates and children.) (Continued)
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
Methotrexate 70 48 34 9 39 7.2 750 μM-h 4,5 >950 μM-h
Metoprolol 38 10 11 63 290 3.2 25 ng/mL …
Metronidazole 99 10 10 5.4 52 8.5 4 mg/L …
Midazolam 44 56 95 27.6 77 1.9 … …
Morphine 24 8 35 60 230 1.9 15 ng/mL …
Nifedipine 50 0 96 29.4 55 1.8 50 ng/mL …
Nortriptyline 51 2 92 30 1300 31 100 ng/mL >500 ng/mL
Phenobarbital 100 24 51 0.258 38 98 15 mg/L >30 mg/L
Phenytoin 90 2 89 Conc 45 Conc 10 mg/L >20 mg/L
dependent 5 dependent 6
Prazosin 68 1 95 12.6 42 2.9 … …
Procainamide 83 67 16 36 130 3 5 mg/L >14 mg/L
Propranolol 26 1 87 50.4 270 3.9 20 ng/mL …
Pyridostigmine 14 85 … 36 77 1.9 75 ng/mL …
Quinidine 80 18 87 19.8 190 6.2 3 mg/L >8 mg/L
Ranitidine 52 69 15 43.8 91 2.1 100 ng/mL …
Rifampin ? 7 89 14.4 68 3.5 … …
Salicylic acid 100 15 85 0.84 12 13 200 mg/L >200 mg/L
Sulfamethoxazole 100 14 62 1.32 15 10 … …
Tacrolimus 20 … 98 7 3 8 133 8 28 10 mcg/L …
Terbutaline 14 56 20 14.4 125 14 2 ng/mL …
Tetracycline 77 58 65 7.2 105 11 … …
Theophylline 96 18 56 2.8 35 8.1 10 mg/L >20 mg/L
Tobramycin … 90 10 4.62 18 2.2 … …
Tocainide 89 38 10 10.8 210 14 10 mg/L …
Tolbutamide 93 0 96 1.02 7 5.9 100 mg/L …
Trimethoprim 100 69 44 9 130 11 … …
Tubocurarine … 63 50 8.1 27 2 0.6 mg/L …
Valproic acid 100 2 93 0.462 9.1 14 75 mg/L >150 mg/L
Vancomycin … 79 30 5.88 27 5.6 20 mg/L 3 …
Verapamil 22 3 90 63 350 4 … …
Warfarin 93 3 99 0.192 9.8 37 … …
Zidovudine 63 18 25 61.8 98 1.1 … …
1
Assuming creatinine clearance 100 mL/min/70 kg.
2 Convert to mL/min by multiplying the number given by 16.6.
3
Average steady-state concentration.
4 Target area under the concentration-time curve after a single dose.
5
Can be estimated from measured C using CL = V max /(K m + C); V max = 415 mg/d, K m = 5 mg/L. See text.
6 Varies because of concentration-dependent clearance.
7
Bound in whole blood (%).
8 Based on whole blood standardized to hematocrit 45%.