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药物的光学异构体在药理作用强度上存在差异,这是众所周知的普遍现象。例如拟肾上腺素类药肾上腺素、去甲肾上腺素、苯肾上腺素、麻黄碱、阿拉明以及左旋多巴、左旋眯唑、氯霉素等都是以左旋体供临床应用。此外,药物的光学异构体在药物动力学中也存在差异。本文对此作一综述。吸收和首过代谢有报道表明,仅主动吸收的药物才具立体选择性。如L-多巴的吸收较D-多巴快,D-甲氨喋呤的吸收率仅为L-甲氨喋呤的2.5%(10mg)。某些药物口服给药时,肝脏对其首过代谢具有立体选择性。Vogelgesang等应用稳定同位素技术在5名健康受
It is a well-known phenomenon that the optical isomers of drugs differ in the intensity of pharmacological effects. For example, the adrenergic drugs epinephrine, norepinephrine, phenylephrine, ephedrine, Alamin and levodopa, levamisole, chloramphenicol and so on are for L-type body for clinical use. In addition, optical isomers of drugs also differ in pharmacokinetics. This article gives a summary of this. Absorption and first-pass metabolism There are reports that only the active absorption of the drug stereospecific. If L-dopa is absorbed more rapidly than D-dopa, the absorption rate of D-methotrexate is only 2.5% (10 mg) of L-methotrexate. When administered orally to certain drugs, the liver is stereoselective for its first-pass metabolism. Vogelgesang et al. Applied stable isotope techniques in 5 healthy subjects