Amobarbital—a probe of hepatic drug oxidation in man

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Abstract
Some aspects of the fate of amobarbital were investigated since this drug is being used as a probe to gauge drug oxidation in man. The mean ratio of' orally available over intravenously injected amobarbital was established as 0.99 ± 0.11 (SD), by comparing integrated concentration-time curves, indicating complete absorption and absence of a first-pass eff'ect. One subject ingested 200 mg of amobarbital sodium, and amobarbital concentrations in serum were monitored for 5 days thereafter. Elimination of amobarbital under these conditions followed first-order kinetics. One subject ingested amobarbital 7 times over a period of 3 yr; plasma clearances (32.1 ± 1.8 [SD] ml/min) exhibited remarkable constancy, while biologic half/lives (26.5 ± 3.1 hr) and distribution volumes (73.6 ± 8.0 L) showed some fluctuation. The distribution of parameters of amobarbital elimination was investigated in 36 unrelated subjects. Amobarbital half-lives (23.8 ± 6.7 hr) appeared to be normally distributed, while the clearances (36.7 ± 10.0 ml/min) might not follow a normal distribution.

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