DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table AII–1
Pharmacokinetic Data
Key: Unless otherwise indicated by a specific footnote, the data are presented for the study population as a mean value ± 1 standard deviation, a mean and range (lowest-highest in parentheses) of
values, a range of the lowest-highest values, or a single mean value. ACE, angiotensin-converting enzyme; ADH, alcohol dehydrogenase; Aged, aged; AIDS, acquired immunodeficiency syndrome;
Alb, hypoalbuminemia; Alcohol, chronic consumption of ethanol; Atr Fib, atrial fibrillation; AVH, acute viral hepatitis; Burn, burn patients; C max
, peak concentration; CAD, coronary artery disease;
Celiac, celiac disease; CF, cystic fibrosis; CHF, congestive heart failure; Child, children; COPD, chronic obstructive pulmonary disease; CP, cor pulmonale; CPBS, cardiopulmonary bypass surgery;
CRI, chronic respiratory insufficiency; Crohn, Crohn’s disease; Cush, Cushing’s syndrome; CYP, cytochrome P450; F or Fem, female; Hep, hepatitis; HIV, human immunodeficiency virus; HL,
hyperlipoproteinemia; HTh, hyperthyroid; IM, intramuscular; Inflam, inflammation; IV, intravenous; LD, chronic liver disease; LTh, hypothyroid; M, male; MAO, monoamine oxidase; MI, myocardial
infarction; NAT, N-acetyltransferase; Neo, neonate; NIDDM, non-insulin-dependent diabetes mellitus; NS, nephrotic syndrome; Obes, obese; PDR54, Physicians’ Desk Reference, 54th ed.
Montvale, NJ, Medical Economics Co., 2000; PDR58, Physicians’ Desk Reference, 58th ed. Montvale, NJ, Medical Economics Co., 2004; Pneu, pneumonia; PO, oral administration; Preg, pregnant;
Prem, premature infants; RA, rheumatoid arthritis; Rac, racemic mixture of stereoisomers; RD = renal disease (including uremia); SC, subcutaneous; Smk, smoking; ST, sulfotransferase; T max,
peak time; Tach, ventricular tachycardia; UGT, UDP-glucuronosyl transferase; Ulcer, ulcer patients. Other abbreviations are defined in the text section of this appendix.
BIOAVAILABILITY URINARY BOUND IN CLEARANCE VOL. DIST. HALF-LIFE PEAK TIME PEAK
(ORAL) (%) EXCRETION (%) PLASMA (%) (mL/min/kg) (L/kg) (hours) (hours) CONCENTRATION
Acetaminophen a
88 ± 15 3 ± 1 <20 5.0 ± 1.4 b 0.95 ± 0.12 b 2.0 ± 0.4 0.33–1.4 d 20 μg/mL e
i Child i Neo, Child b Hep c i Aged, Hep c , i RD, Obes,
LTh, HTh, Child Child
i Aged, Child
a Neo, Hep c
a Obes, HTh, Preg
a HTh, Preg
a
Values reported are for doses <2 g; drug exhibits concentration-dependent kinetics above this
dose. b Assuming a 70-kg body weight; reported range, 65-72 kg. c Acetaminophen-induced
hepatic damage or AVH. d Absorption rate, but not extent, depends on gastric emptying; hence,
it is slowed after food as well as in some disease states and co-treatment with drugs that cause
Acetylsalicylic Acid a
gastroparesis. e Mean concentration following a 20-mg/kg oral dose. Hepatic toxicity associated
with levels >300 μg/mL at 4 hours after an overdose.
Reference: Forrest JA, et al. Clinical pharmacokinetics of paracetamol. Clin Pharmacokinet,
1982, 7:93–107.
68 ± 3 1.4 ± 1.2 49 9.3 ± 1.1 0.15 ± 0.03 0.25 ± 0.03 0.39 ± 0.21 b 24 ± 4 μg/mL b
i Aged, LD b RD i Aged, LD i Hep
a
Values given are for unchanged parent drug. Acetylsalicylic acid is converted to salicylic acid
during and after absorption (CL and t 1/2
of salicylate are dose dependent; t 1/2
varies between
2.4 hours after a 300-mg dose to 19 hours when there is intoxication). b Following a single
1.2-g oral dose given to adults.
Reference: Roberts MS, et al. Pharmacokinetics of aspirin and salicylate in elderly subjects
and in patients with alcoholic liver disease. Eur J Clin Pharmacol, 1983, 25:253–261.
(Continued)
APPENDIX II
DESIGN AND OPTIMIZATION OF DOSAGE REGIMENS: PHARMACOKINETIC DATA
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