Magnussen I, Oxlund H R, Alsbirk K E, Arnold E
Acta Pharmacol Toxicol (Copenh). 1979 Aug;45(2):87-90. doi: 10.1111/j.1600-0773.1979.tb02365.x.
Serum concentrations of diazepam and N-desmethyldiazepam were measured in six adult patients following administration of 10 mg diazepam in solution by the rectal, intravenous, and intramuscular routes. Maximum serum concentrations of 121--200 ng/ml were recorded from 10 to 20 min. after the rectal instillation, whereas following intramuscular injection the levels rose slowly and irregularly, reaching a maximum (62--186 ng/ml) in 1 to 24 hours. The bioavailability of diazepam given by rectal instillation was found to be 50 +/- 17 per cent (mean +/- S. D.) as compared with the intravenous administration. The possible reasons for the low bioavailability are discussed. It is concluded that administration by rectal tube provides a useful alternative to the tablets (and intramuscular injections) when a rapid onset of effect of the drug is wanted, and when intravenous administration is not applicable or practical.
对6名成年患者经直肠、静脉和肌肉注射途径给予10mg地西泮溶液后，测定了血清中地西泮和N-去甲基地西泮的浓度。直肠滴注后10至20分钟记录到最大血清浓度为121 - 200ng/ml，而肌肉注射后血药浓度上升缓慢且不规则，1至24小时达到最大值（62 - 186ng/ml）。与静脉给药相比，经直肠滴注给予地西泮的生物利用度为50±17%（平均值±标准差）。讨论了生物利用度低的可能原因。得出结论，当需要药物快速起效且静脉给药不适用或不可行时，经直肠给药是片剂（和肌肉注射）的一种有用替代方法。
