Owen J A, Nakatsu S L, Fenemore J, Condra M, Surridge D H, Morales A
Department of Pharmacology and Toxicology, Queen's University, Kingston, Ontario, Canada.
Eur J Clin Pharmacol. 1987;32(6):577-82. doi: 10.1007/BF02455991.
The kinetic disposition of yohimbine was examined in eight young male subjects following a single oral dose of 10 mg yohimbine hydrochloride. The drug was rapidly absorbed (absorption half-time 0.17 +/- 0.11 h) and rapidly eliminated from the plasma (elimination half-life 0.60 +/- 0.26 h). This clearance of yohimbine from plasma was constant over approximately 10 elimination half-lives, suggesting that distribution into a second pharmacokinetically distinct compartment was not responsible for the rapid decline in plasma yohimbine levels. Urinary excretion and the partitioning of the drug into red blood cells (RBC) was investigated. In the 24 h following oral administration of the drug, virtually no yohimbine was eliminated in the urine (0.35 +/- 0.50% of the administered dose). Furthermore, only 20% of blood-borne yohimbine was located in RBC. These results suggest that yohimbine is eliminated primarily through metabolism since the rapid plasma clearance of yohimbine was not the result of renal elimination or sequestration by RBC.
在8名年轻男性受试者单次口服10毫克盐酸育亨宾后，对育亨宾的动力学处置进行了研究。该药物吸收迅速（吸收半衰期为0.17±0.11小时），并从血浆中迅速消除（消除半衰期为0.60±0.26小时）。育亨宾从血浆中的清除在大约10个消除半衰期内保持恒定，这表明分布到第二个药代动力学不同的隔室并非血浆育亨宾水平迅速下降的原因。对尿液排泄以及药物在红细胞（RBC）中的分配情况进行了研究。在口服该药物后的24小时内，尿液中几乎没有育亨宾被消除（占给药剂量的0.35±0.50%）。此外，血源性育亨宾仅有20%存在于红细胞中。这些结果表明，育亨宾主要通过代谢消除，因为育亨宾在血浆中的快速清除并非肾脏消除或被红细胞隔离的结果。
