TABLE B-1 Evaluation of Comparability, Pharmacokinetics, and Pharmacodynamic Interactions of Halcion

Source

Type

Population

Number of Subjects

Drug and Dose

Duration

Outcome/Comments

Greenblatt et al. (1989)

Placebo-control

Healthy

16

Placebo

Single dose

Time to peak: flurazepam, 1-1.2 ha; temazepam, 1.5 h; Halcion, 0.95 h. Time to elimination: flurazepam, >24 hb; temazepam, 8.7 h; Halcion, 2.0 h.

12

flurazepam 15 mg

13

Temazepam 15 mg

12

Halcion 0.25 mg

Mouret et al. (1990)

?

?

?

Zopliclone

Single dose

Time to peak: 75 min; time to elimination: 5-6.5 h

Mauri et al. (1993)

?

?

?

Quazepam

Desalkylflurazepam

Oxoquazepam

OH-Triazolam

Single dose, Very low concn.

Time to elimination: quazepam, 30-40 h; Desalkylflurazepam Oxoquazepam, 40-70 h; OH-Triazolam, 30-40 h.

Monti et al. (1994)

?

?

?

Zolpidem

Single dose

Time to peak: 0.33-0.67 h. Time to elimination: 2-3 h

Adam and Oswald (1988)

?

?

?

Lormetazepam

Single dose

Time to elimination: 10-20 h. Humpel et al. (1980)

Eberts et al. (1981)

NA

Bedtime

6

71.1 mCi of

Halcion

Free alpha-OH triazolam

Free 4-OH triazolam

Single dose

Time to peak: Halcion, 1.3 h; Alpha-OH triazolam gluconate, 1.3 h; 4-HTT-gluconate, 2.5 h; others, levels low for kinetics. Time to elimination: Halcion, 2.3 h; Alpha-OH triazolam gluconate, 3.9 h; 4-HTT-gluconate, 3.8 h.

 

 

 

 

Alpha-OH triazolam gluconate

4-HTT-gluconate

 

Free alpha-OH triazolam 69% of urine14C (free + conjugated); Free 4-OH triazolam 11% of urine14C (free + conjugated)



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