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The clinical pharmacokinetics of 2',3'-dideoxycytidine (DDC) were determined after oral and intravenous administration in ten patients with AIDS or AIDS-related complex. A high performance liquid chromatography (HPLC) analysis procedure using cation exchange extraction columns was used to measure DDC levels as low as 0.1 microM (21 ng/mL) in plasma and urine. The kinetics of DDC were linear over the dose range of 0.03 to 0.5 mg/kg. Total body clearance was 227 mL/min/m2 and did not change after 6 to 14 days of dosing. The volume of distribution at steady state was 0.54 L/kg. Plasma half-life was 1.2 hours, and bioavailability was 88%. Most (75%) of the parent drug was found unchanged in the urine. As a result, renal function could play a role in dose adjustment of DDC. Comparison is made between the kinetics of DDC and 3'-azido-2',3'-dideoxythymidine (AZT). Similarities are noted in half-life and bioavailability. However, differences are observed for total body clearance, cerebrospinal fluid penetration, volume of distribution, metabolism, and recovery in urine.
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J M Collins, and
R C Yarchoan, and
R Thomas, and
N McAtee, and
S Broder, and
C E Myers
January 1990,
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R W Klecker, and
J M Collins, and
R C Yarchoan, and
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N McAtee, and
S Broder, and
C E Myers
October 1989,
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R W Klecker, and
J M Collins, and
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N McAtee, and
S Broder, and
C E Myers
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R W Klecker, and
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R W Klecker, and
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R W Klecker, and
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R W Klecker, and
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R W Klecker, and
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R W Klecker, and
J M Collins, and
R C Yarchoan, and
R Thomas, and
N McAtee, and
S Broder, and
C E Myers
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