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

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Furosemide a

71 ± 35 71 ± 10 98.6 ± 0.4 1.66 ± 0.58 0.13 ± 0.06 1.3 ± 0.8 1.4 ± 0.8 c 1.7 ± 0.9 μg/mL c

(43-73) (50-80) (96-99) (1.5-3.0) (0.09-0.17) (0.5-2.0)

i CHF, LD, b CF b RD, NS, b Aged, RD, b a NS, Neo, a Aged, RD, b

CRI LD, Alb, CHF, Neo, Prem Prem, LD CHF, Prem,

Aged

Neo, LD

i Aged i CHF, Smk i LD i RD, CHF, i NS

a CF

Aged, Smk

a

Data from healthy adult male subjects. No significant gender differences described. Range of

mean values from multiple studies shown in parentheses. b CL/F reduced, mild renal impairment.

Aged: CL/F reduced with declining renal function. c Following a single 40-mg oral dose

(tablet). Ototoxicity occurs at concentrations >25 μg/mL.

Gabapentin

60 a 64-68 <3 1.6 ± 0.3 0.80 ± 0.09 6.5 ± 1.0 2-3 b 4 μg/mL b

b Aged, RD

a RD

a

Decreases with increasing dose. Value for 300- to 600-mg dose reported. b Following an

800-mg oral dose given three times daily to steady state in healthy adults. Efficacious at

concentrations >2 μg/mL.

Galantamine a

100 (91-110) 20 (18-22) 18 5.7 (5.0-6.3) b 2.6 (2.4-2.9) 5.7 (5.2-6.3) 2.6 ± 1.0 d 96 ± 29 ng/mL d

b RD, c LD c

a

Primarily metabolized by CYP2D6, CYP3A4, and glucuronidation. b CYP2D6 poor metabolizers

show a lower CL, but dose adjustment is not required. c ln patients with mild to moderate

hepatic or renal insufficiency. d Following a 12-mg oral dose given twice daily for 7 days in

healthy, elderly adults.

Ganciclovir

References: Andreasen F, et al. The pharmacokinetics of frusemide are influenced by age. Br J

Clin Pharmacol, 1983, 16:391–397. Ponto LL, et al. Furosemide (frusemide). A pharmacokinetic/pharmacodynamic

review (part I). Clin Pharmacokinet, 1990, 18:381–408. Waller ES,

et al. Disposition and absolute bioavailability of furosemide in healthy males. J Pharm Sci,

1982, 71:1105–1108.

References: Bialer M. Comparative pharmacokinetics of the newer antiepileptic drugs. Clin

Pharmacokinet, 1993, 24:441–452. McLean MJ. Gabapentin. In: Wyllie E, ed. The Treatment of

Epilepsy: Principles and Practice, 2nd ed. Baltimore, Williams & Wilkins, 1997, pp. 884–898.

References: Bickel U, et al. Pharmacokinetics of galanthamine in humans and corresponding

cholinesterase inhibition. Clin Pharmacol Ther, 1991, 50:420–428. Huang F, et al.

Pharmacokinetic and safety assessments of galantamine and risperidone after the two drugs

are administered alone and together. J Clin Pharmacol, 2002, 42:1341–1351. Scott LJ, et al.

Galantamine: A review of its use in Alzheimer’s disease. Drugs, 2000, 60:1095–1122.

3-5 91 ± 5 1-2 3.4 ± 0.5 1.1 ± 0.2 3.7 ± 0.6 PO: 3.0 ± 0.6 a IV: 6.6 ± 1.8 μg/mL a

a Food b RD a RD PO: 1.2 ± 0.4 μg/mL a

a Food

APPENDIX II

DESIGN AND OPTIMIZATION OF DOSAGE REGIMENS: PHARMACOKINETIC DATA

a

Following a single 6-mg/kg IV dose (1-hour infusion) or a 1000-mg oral dose given with

food three times a day to steady state.

References: Aweeka FT, et al. Foscarnet and ganciclovir pharmacokinetics during concomitant

or alternating maintenance therapy for AIDS-related cytomegalovirus retinitis. Clin

Pharmacol Ther, 1995, 57:403–412. PDR54, 2000, p. 2624.

(Continued)

1935

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