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Diaziquone, 2,5‐diaziridinyl‐3,6‐biscarboethoxyamino‐1,4‐benzoquinone, plasma and cerebrospinal fluid kinetics
Author(s) -
Bachur Nicholas R,
Collins Jerry M,
Kelley James A,
Van Echo David A,
Kaplan Richard S,
Whitacre Margaret
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.1982.90
Subject(s) - cerebrospinal fluid , pharmacokinetics , kinetics , volume of distribution , plasma volume , plasma concentration , distribution (mathematics) , plasma , chemistry , plasma levels , half life , anesthesia , medicine , pharmacology , mathematics , physics , mathematical analysis , quantum mechanics
Plasma and cerebrospinal fluid (CSF) kinetics of diaziquone, 2,5‐diaziridinyl‐3,6‐biscarboethoxyamino‐1,4‐benzoquinone (AZQ), were evaluated after intravenous injection in patients with implanted Ommaya reservoirs. After a 30‐min infusion plasma disappearance was very rapid, with a disposition half‐life of 2 to 6 min and an elimination half‐life of 25 to 35 min. Area under the concentration‐time curve for CSF was 22% to 42% of the corresponding plasma area. Based upon total plasma AZQ concentration, volume of distribution for AZQ was 2.0 to 10.0 l/m 2 . Plasma binding of AZQ was 79% in one normal subject. When the effect of plasma binding is considered, distribution volumes are more plausible and it appears that free plasma AZQ is completely available to the CSF. Clinical Pharmacology and Therapeutics (1982) 31, 650–655; doi: 10.1038/clpt.1982.90