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Year : 2012  |  Volume : 44  |  Issue : 1  |  Page : 20--25

Pharmacokinetics of venlafaxine and its major metabolite o-desmethylvenlafaxine in freely moving mice using automated dosing/sampling system

Bijay Aryal1, Dipendra Aryal1, Eun-Joo Kim2, Hyung-Gun Kim1 
1 Department of Pharmacology, College of Medicine, Dankook University, San#29, Anseo-dong, Dongnam-gu Cheonan, Choongnam, Republic of Korea
2 Department of Pharmacology, Korea Institute of Toxicology, 100 Jangdong, Yuseong Ku, Daejeon, Republic of Korea

Correspondence Address:
Hyung-Gun Kim
Department of Pharmacology, College of Medicine, Dankook University, San#29, Anseo-dong, Dongnam-gu Cheonan, Choongnam
Republic of Korea

Objective: To assess the pharmacokinetics of venlafaxine (VEN) and its major metabolite o-desmethylvenlafaxine (ODV) in freely moving mice using automated dosing/infusion (ADI) and automated blood sampling (ABS) systems. In addition, concentration of VEN and its metabolite ODV were also measured in brain by microdialysis. Materials and Methods: Venlafaxine was administered directly via jugular vein or gastric catheterization and blood samples were collected through carotid artery. A series of samples with 10 μl of blood was collected from the mouse using ADI/ABS and analyzed with a validated LC-MS/MS system. Extracellular concentrations of VEN and ODV in brain were investigated by using microdialysis procedure. Results: The bioavailability of VEN was 11.6%. The percent AUC ratios of ODV to VEN were 18% and 39% following intravenous and intragastric administration, respectively. The terminal half-life of venlafaxine was about two hours. Extracellular concentration of VEN contributed 3.4% of the blood amount, while ODV was not detected in dialysate. Conclusion: This study suggests that besides rapid absorption of VEN, the first-pass metabolism is likely to contribute for its lower bioavailability in the mouse. The proposed automated technique can be used easily to conduct pharmacokinetic studies and is applicable to high-throughput manner in mouse model.


How to cite this article:
Aryal B, Aryal D, Kim EJ, Kim HG. Pharmacokinetics of venlafaxine and its major metabolite o-desmethylvenlafaxine in freely moving mice using automated dosing/sampling system.Indian J Pharmacol 2012;44:20-25


How to cite this URL:
Aryal B, Aryal D, Kim EJ, Kim HG. Pharmacokinetics of venlafaxine and its major metabolite o-desmethylvenlafaxine in freely moving mice using automated dosing/sampling system. Indian J Pharmacol [serial online] 2012 [cited 2021 Apr 18 ];44:20-25
Available from: https://www.ijp-online.com/article.asp?issn=0253-7613;year=2012;volume=44;issue=1;spage=20;epage=25;aulast=Aryal;type=0