Pharmacokinetics of active metabolites of ethyl loflazepate in the aged.
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The pharmacokinetics of benzodiazepines in three aged patients who took maintenance doses of ethyl loflazepate (Lof) and developed disturbance of consciousness following asphyxia (cases 1 and 3), and congestive heart failure (case 2) were examined. After admission, we measured serum concentrations of active metabolites of benzodiazepines by using two methods of gas chromatography and benzodiazepine receptor assay, and assessed the changes in pharmacokinetic values. On admission serum concentrations of Lof were 256ng/ml, 363ng/ml and 425ng/ml. Serum benzodiazepine-receptor binding activities, expressed as diazepam equivalent concentrations were 1, 800ng/ml, 1, 400ng/ml and 2, 200ng/ml in cases 1, 2 and 3, respectively. All of these values in three cases revealed toxic levels of benzodiazepines. Serum concentrations of Lof and serum benzodiazepine-receptor binding activities decreased to 115ng/ml and 480ng/ml on the 7th hospital day in case 1, 41ng/ml and 300ng/ml on the 29th hospital day in case 2, and 322ng/ml and 1, 500ng/ml on the third hospital day in case 3, respectively. The elimination half-times (T1/2) of Lof were 124 hours and 121 hours in case 1 and 3, respectively, and was significantly prolonged to 212 hours in case 2. The T1/2 of benzodiazepine-receptor binding activity was also significantly prolonged to 313 hours in case 2. In the administration of benzodiazepines to the aged, one should consider; 1) that subclinical dysfunction of liver and kidney may lower total drug clearance (CL), or body weight loss may decrease distribution volume (Vd) and increase plasma level of Lof, 2) decreased CL or elevated Vd due to increased amount of fatty tissue may prolong T1/2, and 3) hypoalbuminemia from malnutrition or co-administration of other benzodiazepines may increase plasma concentrations of free-benzodiazepines. We concluded that when administering benzodiazepines to the aged, symptoms should be observed in detail and plasma levels of drug carefully monitored.
- 一般社団法人 日本救急医学会の論文
一般社団法人 日本救急医学会 | 論文
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