ArticlePharmaceutical research2008
Telithromycin pharmacokinetics in rat model of diabetes mellitus induced by alloxan or streptozotocin.
Article in Pharmaceutical research, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Pharmacokinetic assessment of cefpodoxime proxetil in diabetic rats.Journal of diabetes and metabolic disorders · 2023Article
- Metabolic Profiling and Investigation of the Modulatory Effect ofAntioxidants (Basel, Switzerland) · 2023Article
- Strategies for preclinical pharmacokinetic investigation in streptozotocin-induced diabetes mellitus (DMIS) and alloxan-induced diabetes mellitus (DMIA) rat models: case studies and perspectives.European journal of drug metabolism and pharmacokinetics · 2015Review
- Pharmacokinetics of itraconazole in diabetic rats.Antimicrobial agents and chemotherapy · 2010Article
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Authors and funding
2 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeIt has been reported that telithromycin is primarily metabolized via hepatic CYP3A1/2 in rats, the expression and/or mRNA level of hepatic CYP3A1/2 increase in rat model of diabetes mellitus induced by alloxan (DMIA) or streptozotocin (DMIS), and intestinal CYP3A1/2 enzyme activity decreases in rat model of DMIS. Thus, the pharmacokinetic changes of telithromycin in both models of diabetes mellitus compared with those in the control rats were evaluated.
methodsTelithromycin was administered (50 mg/kg) intravenously or orally to both rat models of diabetes and their respective control rats.
resultsAfter intravenous administration of telithromycin to both models of diabetes, the non-renal clearance (CLNR) was significantly faster (32.3 and 53.1% increase for rat models of DMIA and DMIS, respectively) and the AUC was significantly smaller (25.0 and 33.8% decrease, respectively) than those in their respective controls. However, after oral administration of telithromycin, the AUC was comparable to that in their respective controls.
conclusionsThe faster CLNR after intravenous administration was due to increased hepatic CYP3A1/2 in both models of diabetes. The comparable AUC after oral administration was mainly due to decreased intestinal CYP3A1/2 activity. Alloxan and streptozotocin appear to influence some pharmacokinetics of telithromycin in a different fashion.
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