Premium
Disposition of cyclosporine after intravenous and multi‐dose oral administration in cats
Author(s) -
Mehl M. L.,
Kyles A. E.,
Craigmill A. L.,
Epstein S.,
Gregory C. R.
Publication year - 2003
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1046/j.1365-2885.2003.00496.x
Subject(s) - cmax , pharmacokinetics , bioavailability , oral administration , cats , pharmacology , disposition , absorption (acoustics) , distribution (mathematics) , medicine , volume of distribution , ciclosporin , chemotherapy , psychology , social psychology , mathematical analysis , physics , mathematics , acoustics
The aim of this study was to evaluate the disposition of cyclosporine after intravenous (i.v.) and oral administration and to evaluate single sampling times for therapeutic monitoring of cyclosporine drug concentrations in cats. Six adult male cats (clinically intact) were used. Two treatments consisting of a single i.v. cyclosporine (1 mg/kg) and multiple oral cyclosporine (3 mg/kg b.i.d p.o. for 2 weeks) doses. Whole blood cyclosporine concentrations were measured at fixed times by high performance liquid chromatography and pharmacokinetic values were calculated. Mean values for the i.v. data included AUC (7413 ng/mL·h), t 1/2 distribution and elimination (0.705 and 9.7 h, respectively), C max (1513 ng/mL), and V d(ss) (1.71 L/kg). Mean values for the oral data included AUC (6243 ng/mL·h), t 1/2 of absorption and elimination (0.227 and 8.19 h, respectively), and C max (480.0 ng/mL). Bioavailability of orally administered cyclosporine was 29 and 25% on days 7 and 14 respectively. Whole blood comment cyclosporine concentration 2 h after administration ( C 2 ) better correlated with AUC on days 7 and 14 than trough plasma concentration ( C 12 ). The rate of oral cyclosporine absorption was less than expected and there was substantial individual variation. Therapeutic drug monitoring strategies for cyclosporine in cats should be re‐evaluated.