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Clinical pharmacolinetics of 9, 10-anthracenedicarboxaldehyde-bis [(4,5-dihydro-1H-imidazol-2-yl)hydrazone]dihydrochloride
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Clinical pharmacology of 2,5′-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ)
2,5′-Diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZQ) is an alkylating compound which has exhibited a broad spectrum of antitumor activity against a variety of experimental tumors, particularly those implanted intracranially. We have studied the clinical pharmacology of AZQ in 11 patients with various types of tumors. AZQ was administered at 1–12
mg/
m
2 daily for 5
days by i.v. infusion in 10–30
min.
14
C-labelled AZQ was given on day 1 only. Blood and urine specimens were analyzed radiochemically and chromatographically. The plasma disappearance of unchanged AZQ was essentially biphasic, with an initial plasma
t
1
2
of 1.4 ± 0.4
hr and a terminal
t
1
2
of 45.5 ± 3.1
hr. The apparent volume of distribution was 14.2 ± 3.0
l/kg. The cumulative urinary excretion of unchanged AZQ was 4.3% in 24
hr and 8.6% in 96
hr. The total clearance of the drug was 200
ml/kg/hr. Cerebrospinal fluid AZQ concentration peaked 45–90
min after drug administration, reaching about 70% of that in plasma, and then declined at nearly the same rate