Pharmacokinetics of mirtazapine and its main metabolites after single intravenous and oral administrations in rats at two dose rates

Rouini, Mohammad-Reza, Lavasani, Hoda, Sheikholeslami, Behjat, Owen, Helen and Giorgi, Mario (2014) Pharmacokinetics of mirtazapine and its main metabolites after single intravenous and oral administrations in rats at two dose rates. DARU Journal of Pharmaceutical Sciences, 22 13: 1-5. doi:10.1186/2008-2231-22-13


Author Rouini, Mohammad-Reza
Lavasani, Hoda
Sheikholeslami, Behjat
Owen, Helen
Giorgi, Mario
Title Pharmacokinetics of mirtazapine and its main metabolites after single intravenous and oral administrations in rats at two dose rates
Journal name DARU Journal of Pharmaceutical Sciences   Check publisher's open access policy
ISSN 1560-8115
2008-2231
Publication date 2014-01-07
Sub-type Article (original research)
DOI 10.1186/2008-2231-22-13
Open Access Status DOI
Volume 22
Issue 13
Start page 1
End page 5
Total pages 5
Place of publication London, United Kingdom
Publisher BioMed Central
Collection year 2015
Language eng
Subject 3002 Drug Discovery
3004 Pharmacology
Formatted abstract
Abstract. Background: Mirtazapine (MRZ) is a human antidepressant drug metabolized to 8-OH mirtazapine (8-OH) and dimethylmirtazapine (DMR) metabolites. Recently, this drug has been proposed as a potential analgesic for use in a multidrug analgesic regime in the context of veterinary medicine. The aim of this study was to assess the pharmacokinetics of MRZ and its metabolites DMR and 8-OH in rats.

Findings. Eighteen fasted, healthy male rats were randomly divided into 3 groups (n = 6). Animals in these groups were respectively administered MRZ at 2 and 10 mg/kg orally and 2 mg/kg intravenously. Plasma MRZ and metabolite concentrations were evaluated by HPLC-FL detection method. After intravenous administration, MRZ was detected in all subjects, while DMR was only detected in three. 8-OH was not detected. After oral administration, MRZ was detected in 3 out of 6 rats treated with 2 mg/kg, it was detected in 6 out of 6 animals in the 10 mg/kg group. DMR was only detectable in the latter group, while 8-OH was not detected in either group. The oral bioavailability was about 7% in both groups.

Conclusions: The plasma concentration of the MRZ metabolite 8-OH was undetectable, and the oral bioavailability of the parental drug was very low.
Keyword Mirtazapine
Metabolites
Rats
Pharmacokinetics
Bioavailability
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2015 Collection
School of Veterinary Science Publications
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 1 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 1 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Tue, 18 Feb 2014, 00:43:46 EST by System User on behalf of School of Veterinary Science