PMID: 8592675Nov 1, 1995Paper

Absorption and presystemic metabolism of nefazodone administered at different regions in the gastrointestinal tract of humans

Pharmaceutical Research
P H MaratheR H Barbhaiya

Abstract

The absorption and disposition of nefazodone (NEF) and its metabolites hydroxynefazodone (HO-NEF), m-chlorophenylpiperazine (mCPP) and triazole dione (dione) were assessed in 10 healthy subjects following infusion of NEF solution into the proximal and distal regions of the intestine vs administration of NEF solution orally by mouth. NEF HCl (400 mg) was infused over 5 hours into the proximal or distal intestine through a nasogastric tube, or orally ingested in 10 divided doses over 4.5 hours. The three treatments in the three-period crossover design were separated by one week. The bioavailability of NEF, based on AUC(INF), from proximal and distal regions relative to that from oral administration was 97% and 106%, respectively. NEF was absorbed equally well from all three treatments with median Tmax of 5.0 hours which coincided with the duration of infusion. Mean Cmax of NEF was not different between proximal and oral administrations, however, mean Cmax after distal instillation was 40% lower than that after oral administration. Exposure to HO-NEF, mCPP and dione, following proximal instillation was also comparable to that after oral administration. AUC(INF) of HO-NEF and dione was significantly lower after distal instillation ...Continue Reading

Citations

Sep 19, 2017·Expert Opinion on Drug Discovery·Teruo Murakami
Apr 30, 2002·Clinical Pharmacokinetics·Margaret M Doherty, William N Charman
Jan 20, 1998·Drug and Chemical Toxicology·M M Doherty, K S Pang
Feb 18, 2005·International Journal of Geriatric Psychiatry·Maria Stella T GironBengt Winblad
Jun 27, 2009·Journal of Drug Targeting·Emma L McConnellAbdul W Basit

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