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

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SECTION VII
CHEMOTHERAPY OF MICROBIAL DISEASES
Table 59–2
Pharmacokinetic Properties of Nucleoside Reverse Transcriptase Inhibitors a
PARAMETER ZIDOVUDINE LAMIVUDINE STAVUDINE b DIDANOSINE c ABACAVIR TENOFOVIR EMTRICITABINE
Oral bioavailability, % 64 86-87 86 42 83 25 93
Effect of meals on AUC b24% (high fat) i i b55% (acidity) i a40% (high fat) i
Plasma t 1/2
, elim, h 1.0 5-7 1.1-1.4 1.5 0.8-1.5 14-17 10
Intracellular t 1/2
, elim 3-4 12-18 3.5 25-40 21 10-50 39
of triphosphate, h
Plasma protein binding, % 20-38 <35 <5 <5 50 <8 <4
Metabolism, % 60-80 (glucu- <36 ND 50 (purine >80 (dehydro- ND 13
ronidation) metabolism) genation and
glucuronidation)
Renal excretion of 14 71 39 18-36 <5 70-80 86
parent drug, %
ABBREVIATIONS: AUC, area under plasma concentration time curve; t 1/2
, elim, half-life of elimination; a, increase; b, decrease; i, no effect; ND, not determined.
a
Reported mean values in adults with normal renal and hepatic function. b Parameters reported for the stavudine capsule formulation. c Parameters reported for the didanosine chewable tablet
formulation.