临床上重要的药代动力学膳食咖啡因和药物之间的相互作用。

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Carrillo JA,贝尼特斯J

临床上重要的药代动力学膳食咖啡因和药物之间的相互作用。

Pharmacokinet。2000年8月,39 (2):127 - 53。

PubMed ID

10976659 (在PubMed

]

文摘

咖啡因的食物来源(主要是咖啡、茶和软饮料)是最常见的,在当今世界广泛食用的中枢神经系统兴奋剂。由于其巨大的声望,咖啡因的消费通常被认为是安全的和长期的咖啡因摄入量可能忽视作为一个医学问题。然而,很明显,这种化合物有许多的功能通常与药物滥用有关。此外,医生应该意识到可能的贡献膳食咖啡因的体征和症状的患者。咖啡因的毒性作用是扩展他们的药理作用。最严重的caffeine-related中枢神经系统影响包括癫痫和精神错乱。其他症状影响心血管系统的范围从适度增加心率更严重的心律失常。虽然许多药理作用有抗药性的咖啡因,宽容可能被咖啡因的非线性累积代谢成为饱和。这可能发生与高水平的消费或药代动力学相互作用的结果咖啡因和非处方药或处方药。的多环芳烃hydrocarbon-inducible细胞色素P450 (CYP) 1 a2参与咖啡因的代谢以及一些重要的临床药物。 A number of drugs, including certain selective serotonin reuptake inhibitors (particularly fluvoxamine), antiarrhythmics (mexiletine), antipsychotics (clozapine), psoralens, idrocilamide and phenylpropanolamine, bronchodilators (furafylline and theophylline) and quinolones (enoxacin), have been reported to be potent inhibitors of this isoenzyme. This has important clinical implications, since drugs that are metabolised by, or bind to, the same CYP enzyme have a high potential for pharmacokinetic interactions due to inhibition of drug metabolism. Thus, pharmacokinetic interactions at the CYP1A2 enzyme level may cause toxic effects during concomitant administration of caffeine and certain drugs used for cardiovascular, CNS (an excessive dietary intake of caffeine has also been observed in psychiatric patients), gastrointestinal, infectious, respiratory and skin disorders. Unless a lack of interaction has already been demonstrated for the potentially interacting drug, dietary caffeine intake should be considered when planning, or assessing response to, drug therapy. Some of the reported interactions of caffeine, irrespective of clinical relevance, might inadvertently cause athletes to exceed the urinary caffeine concentration limit set by sports authorities at 12 mg/L. Finally, caffeine is a useful and reliable probe drug for the assessment of CYP1A2 activity, which is of considerable interest for metabolic studies in human populations.

DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
氯氮平	细胞色素P450 1 a2	蛋白质	人类	没有	底物	细节
普萘洛尔	细胞色素P450 1 a2	蛋白质	人类	未知的	底物	细节