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

Levofloxacin a
99 ± 10 61-87 24-38 2.52 ± 0.45 1.36 ± 0.21 7 ± 1 1.6 ± 0.8 c 4.5 ± 0.9 μg/mL c
b RD b
a RD b
a
Data from healthy adult male subjects. Gender and age differences related to renal function.
b
CL/F reduced, mild to severe renal impairment (not cleared by hemodialysis). c Following a
single 500-mg oral dose. No significant accumulation with once-daily dosing.
Linezolid
100 35 31 2.1 ± 0.8 0.57-0.71 5.2 ± 1.7 PO: 1.4 ± 0.5 a PO: 16 ± 4 μg/mL a
a Child b Child IV: 15 ± 3 μg/mL b
a
Following a 600-mg oral dose given twice daily to steady state. b Following a 30-minute IV
infusion of a 600-mg dose given twice daily to steady state in patients with gram-positive
infection.
Lisinopril
25 ± 20 88-100 0 4.2 ± 2.2 a 2.4 ± 1.4 a 12 b ~7 c 50 (6.4-343) ng/mL c
b CHF b CHF, RD, Aged i Aged, RD a Aged, RD
i Fem
a
CL/F and V area
/F reported. b Effective t 1/2
to predict steady-state accumulation upon multiple
dosing; a terminal t 1/2
of 30 hours reported. c Following a 2.5- to 40-mg oral dose given daily
to steady state in elderly patients with hypertension and varying degrees of renal function.
EC 90
for ACE inhibition is 27 ± 10 ng/mL.
Lithium
References: Chien SC, et al. Pharmacokinetic profile of levofloxacin following once-daily
500-milligram oral or intravenous doses. Antimicrob Agents Chemother, 1997, 41:2256–2260.
Fish DN, et al. The clinical pharmacokinetics of levofloxacin. Clin Pharmacokinet, 1997,
32:101–119. PDR54, 2000, p. 2157.
References: MacGowan AP. Pharmacokinetic and pharmacodynamic profile of linezolid in
healthy volunteers and patients with Gram-positive infections. J Antimicrob Chemother, 2003,
51(suppl 2):ii17–ii25. Stalker DJ, et al. Clinical pharmacokinetics of linezolid, a novel oxazolidinone
antibacterial. Clin Pharmacokinet, 2003, 42:1129–1140.
100 a 95 ± 15 0 0.35 ± 0.11 b 0.66 ± 0.16 22 ± 8 c IR: 0.5-3 d IR: 1-2 mM d
b RD, Aged b Obes a RD, Aged SR: 2-6 d SR:0.7-1.2 mM d
a Preg
b Obes
i Obes
a
Values as low as 80% reported for some prolonged-release preparations. b Renal CL of Li + parallels
that of Na + . The ratio of Li + and creatinine CL is ~0.2 ± 0.03. c The distribution t 1/2
is 5.6 ± 0.5
hours; this influences drug concentrations for at least 12 hours. d Following a single 0.7-mmol/kg
oral dose of immediate-release (IR) lithium carbonate and sustained-release (SR) tablets.
Reference: Thomson AH, et al. Lisinopril population pharmacokinetics in elderly and renal
disease patients with hypertension. Br J Clin Pharmacol, 1989, 27:57–65.
Reference: Ward ME, et al. Clinical pharmacokinetics of lithium. J Clin Pharmacol, 1994,
34:280–285.
APPENDIX II
DESIGN AND OPTIMIZATION OF DOSAGE REGIMENS: PHARMACOKINETIC DATA
(Continued)
1947