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

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APPENDIX II
DESIGN AND OPTIMIZATION OF DOSAGE REGIMENS: PHARMACOKINETIC DATA
Table AII–1
Pharmacokinetic Data (Continued)
BIOAVAILABILITY URINARY BOUND IN CLEARANCE VOL. DIST. HALF-LIFE PEAK TIME PEAK
(ORAL) (%) EXCRETION (%) PLASMA (%) (mL/min/kg) (L/kg) (hours) (hours) CONCENTRATION
Carboplatin a
— 77 ± 5 0 1.5 ± 0.3 0.24 ± 0.03 2 ± 0.2 0.5 b 39 ± 17 μg/mL b
b RD
a RD
a
Measure of ultrafilterable platinum, which essentially is unchanged carboplatin. b Following a
single 170 to 500-mg/m 2 IV dose (30-minute infusion) given to adult patients with ovarian
cancer.
Carvedilol a
25 <2 95 b 8.7 ± 1.7 1.5 ± 0.3 2.2 ± 0.3 c 1.3 ± 0.3 d 105 ± 12 ng/mL d
S-(–): 15 b LD a Cirr a, i LD
R-(+): 31 i RD, Aged i RD, Aged
a Cirr
a
Racemic mixture: S-(–)-enantiomer responsible for β 1
adrenergic–receptor blockade. R-(+)-
and S-(–)-enantiomers have nearly equivalent α 1
-receptor blocking activity. b R-(+)-enantiomer
is more tightly bound than the S-(–)-antipode. c Longer t 1/2
of ~6 hours has been measured at
lower concentrations. d Following a 12.5-mg oral dose given twice a day for 2 weeks to
healthy young adults.
Cefazolin
>90 80 ± 16 89 ± 2 0.95 ± 0.17 0.19 ± 0.06 a 2.2 ± 0.02 IM: 1.7 ± 0.7 b IV: 237 ± 285 μg/mL b
b RD, LD, b RD, CPBS a RD, Neo a RD, Neo, IM: 42 ± 9.5 μg/mL b
CPBS, Neo,
CPBS
Child
a
V area
reported. b Following a single 1-g IV (model-fitted C max
) or IM dose to healthy adults.
Reference: Gaver RC, et al. The disposition of carboplatin in ovarian cancer patients. Cancer
Chemother Pharmacol, 1988, 22:263–270.
References: Morgan T. Clinical pharmacokinetics and pharmacodynamics of carvedilol. Clin
Pharmacokinet, 1994, 26:335–346. Morgan T, et al. Pharmacokinetics of carvedilol in older
and younger patients. J Hum Hypertens, 1990, 4:709–715.
a Preg i Preg, b Preg, LD
Obes, Child,
LD
i Neo, Obes,
i Obes, Child
Child, LD
Reference: Scheld WM, et al. Moxalactam and cefazolin: Comparative pharmacokinetics in
normal subjects. Antimicrob Agents Chemother, 1981, 79:613–619.