Aims To compare the pharmacokinetics of eprosartan between young (18-4
5 years) and elderly (65 years) men and between young men and young, p
remenopausal women (18-45 years). Methods Twenty-four subjects (eight
subjects/group) received a single 200mg eprosartan oral dose followed
by serial blood sampling over 24 h. Results Eprosartan was safe and we
ll tolerated. There were no apparent differences in the pharmacokineti
cs of eprosartan between young females and young males or in the plasm
a protein binding of eprosartan (approximate to 98%) for the three gro
ups. On average, AUC (0, infinity) and C-max values were approximate t
o 2-fold higher in elderly men than young men [AUC (0, infinity) 95% C
I: 1.22, 4.34; C-max 95% CI: 0.98, 4.00]. Similarly, unbound AUC (0, i
nfinity) and C-max values were, on average, approximate to 2-fold high
er in elderly men than young men [unbound AUC (0, infinity) 95% CI: 1.
29, 4.44; unbound C-max 95% CI: 1.02, 4.12]. t(max), was delayed in th
e elderly men compared with young men, with a median difference of 2.5
h (95% CI: 1.00, 3.01 h). Conclusions No gender differences were obse
rved in the pharmacokinetics of eprosartan. There were approximate to
two fold higher AUC and C-max,, values for eprosartan observed in elde
rly men as compared with young men, most Likely due to increased bioav
ailability of eprosartan in the elderly. Based on the excellent safety
profile in the elderly in Phase III clinical trials (doses up to 1200
mg eprosartan) eprosartan can be safely administered to elderly hyper
tensive patients without an initial dose adjustment. Subsequently, the
dose of eprosartan, as for other antihypertensive agents, may be indi
vidualized based on tolerability/response.