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Effects of high‐dose cytarabine
Author(s) -
Hande Kenneth R,
Stein Richard S,
McDonough David A,
Greco F Anthony,
Wolff Steven N
Publication year - 1982
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1982.93
Subject(s) - cytarabine , dosing , cerebrospinal fluid , radioimmunoassay , pharmacokinetics , pharmacology , urine , distribution (mathematics) , chemistry , medicine , chemotherapy , mathematics , mathematical analysis
Plasma, urine, cerebrospinal fluid, and tear concentrations of cytarabine (ara‐C) were measured in 15 patients receiving 3 gm/m 2 IV ara‐C given as a 1 hr infusion every 12 hr for 6 days. The two assay methods used for measuring ara‐C concentrations (high‐pressure liquid chromatography and radioimmunoassay) gave much the same results. Peak plasma ara‐C concentrations (2.0 mM) after high‐dose therapy were 50 times those achieved with more conventional (100 to 300 mg/m 2 ) doses. High doses of ara‐C were not sufficient to saturate cytidine deaminase; plasma ara‐C half‐lifes (t½s) after high‐dose therapy (distribution t½ = 6.2 min; elimination t½ = 154 min) were much the same as those after conventional ara‐C doses. Kinetics of ara‐C were not altered by repeated dosing over a 6‐day period. Cerebrospinal fluid ara‐C concentrations after high‐doses (x̄ = 7.8 μM) were 10 times those after conventional intravenous dosing, but were 0.5% to 1.0% those achieved by intrathecal ara‐C doses. Tear concentrations of 22 and 38 μM were measured in two patients who developed conjunctivitis after high‐dose therapy so that the presence of ara‐C in tears may be a cause of the conjunctivitis seen in some patients. Clinical Pharmacology and Therapeutics (1982) 31, 669–674; doi: 10.1038/clpt.1982.93