Beach C A, Mays D C, Guiler R C, Jacober C H, Gerber N
Clin Pharmacol Ther. 1986 Mar;39(3):265-70. doi: 10.1038/clpt.1986.37.
The kinetics of caffeine elimination were investigated in 10 normal male subjects and in 11 recovering alcoholics before and during disulfiram dosing. In normal subjects the total body clearance of caffeine declined 30% (142 to 99 ml/min) at the maintenance dose of disulfiram, 250 mg/day, and 29% (161 to 114 ml/min) at the loading dose of 500 mg/day. In recovering alcoholics, the total body clearance decreased from 333 to 253 ml/min, a 24% change. The mean caffeine t1/2 increased 39% and 34% in normal subjects after 250 and 500 mg disulfiram, respectively, and 29% in recovering alcoholics. The inhibition of caffeine elimination was moderate in most subjects. However, the clearance of caffeine decreased by greater than or equal to 50% after disulfiram in three of the 11 recovering alcoholics. These patients may have an increased risk of cardiovascular and cerebral excitation associated with higher concentrations of caffeine, which could complicate withdrawal from alcohol.
在10名正常男性受试者和11名正在康复的酗酒者中,研究了在服用双硫仑之前及期间咖啡因的消除动力学。在正常受试者中,当双硫仑维持剂量为250毫克/天时,咖啡因的全身清除率下降了30%(从142毫升/分钟降至99毫升/分钟);当负荷剂量为500毫克/天时,清除率下降了29%(从161毫升/分钟降至114毫升/分钟)。在正在康复的酗酒者中,全身清除率从333毫升/分钟降至253毫升/分钟,变化了24%。在正常受试者中,服用250毫克和500毫克双硫仑后,咖啡因的平均半衰期分别增加了39%和34%,在正在康复的酗酒者中增加了29%。在大多数受试者中,咖啡因消除的抑制作用为中等程度。然而,在11名正在康复的酗酒者中,有3人在服用双硫仑后咖啡因清除率下降了50%或更多。这些患者因咖啡因浓度升高而出现心血管和脑兴奋的风险可能增加,这可能会使戒酒过程变得复杂。