Practice Exams: Section 1 : Adinazolam - Section 1

14.5 Adinazolam - Section 1

Fleishaker [Pharm Res 8 (2): 162-7(1991),Pharm Res 6 (5): 379-86(1989),Psychopharm 99:34-9(1989),Psychopharm 105:1815(1991)];Kroboth [J Clin Pharmacol 31:580-6(1991)]; Wagner [Biopharm Drug Dis 8:405-25(1987)].

14.5.1

ADINAZOLAM DATA

Adinazolam (AD) is a triazolobenzodiazepine prodrug which has been shown to have antidepressant activity through its metabolite, N-desmethyladinazolam (NDMAD). Both AD and NDMAD are excreted into the urine. The following data regarding AD and NDMAD was collected from the works cited. AD appears to interfere with mental ability. One of the tests was the ability to Substitute Digits for Symbols (DSST) and the interference of that process was the response measured below:
PROBLEM TABLE 11 - 1.

Pharmacological Response
Time (hrs)
2 4 6 8 12

% Pharm Response
59.7 45.3 29.5 15.5 0

% Pharm Response
33 48 59 68 74

NDMADC Conc (ng/,L)

200 300 400 500 600

From the above information find the pharmacokinetic parameters:

PROBLEM TABLE 11 - 1.

Five mg IV bolus dose of AD yieled: (intercept of extrapolated metabolite line is 150 ng/mL)
Urine Data Time (mid) t
0.5 15.4 23.5 27.3 1 2 4 6

Plasma Data Time (hr)

0.5 1 2 3 4 5 6 8 10 12 15 18 20 22 24 7.5 14.7

Cp (AD) (ng/mL)
47 40 28

Cpm(NDMAD) (ng/mL)

AD Ecretion Rate (mg/hr)

0.56 0.48 0.34 0.18 0.09

28 27 24.9 20 15 11 7.5 4.2 2.8 1.9 1.2

Basic Pharmacokinetics
Copyright 1996 Michael C. Makoid All Rights Reserved

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