Pharmacokinetics of the anti‐inflammatory drug ximoprofen in healthy young and elderly subjects: comparison with elderly rheumatic patients.

Abstract

The pharmacokinetics of ximoprofen were studied in young and elderly subjects after single and repeated doses up to 30 mg. In healthy elderly subjects (30 mg dose), a mean peak plasma drug concentration of 1.78 micrograms ml‐1 +/‐ 0.83 s.d. occurred at a mean time of 1.95 h +/‐ 1.40 s.d. and, thereafter, concentrations declined monoexponentially with a mean half‐life of 3.8 h +/‐ 1.4 s.d. Comparison of these data with those from younger healthy subjects showed that peak drug concentrations, areas under the curve and half‐lives were about two‐ fold greater in the elderly, these differences probably reflecting a lower systemic drug clearance. Similar results were obtained on comparing data from young healthy subjects and elderly rheumatic patients receiving single and repeated doses of ximoprofen (15 mg twice daily). In patients, the half‐life of ximoprofen was 2.5 h +/‐ 0.7 s.d. Within either group, pharmacokinetic parameters after single or repeated doses were similar: ximoprofen did not accumulate in the plasma of the young or elderly.

Pain in Chronic Kidney Disease: A Scoping Review

“…All alterations in pharmacokinetics have been suggested to be related to decreased protein binding and subsequent changes in the volume of distribution and in some cases changes in metabolism of the medication .…”

“…Studies of other acetic acid derivatives, etodolac, bromfenac and indomethacin, in CKD and ESRD patients, do not suggest that any dose adjustment is necessary (167)(168)(169). Propionic acid derivatives (the -profens): 11 studies identified CKD Studies evaluating ketoprofen, ximoprofen and benoxaprofen have shown increased half-life in CKD (170)(171)(172)(173).…”

“…In mild CKD: 80% reduction in urinary prostaglandins, 28% reduction in CrCl and a 40% increase in serum creatinine after 1 week of treatment with ibuprofen (161). All alterations in pharmacokinetics have been suggested to be related to decreased protein binding and subsequent changes in the volume of distribution and in some cases changes in metabolism of the medication (170,(173)(174)(175).…”

The influence of renal function on the enantioselective pharmacokinetics and pharmacodynamics of ketoprofen in patients with rheumatoid arthritis.

“…These data are presented as sigmoidal Emax model parameter estimates. The data from one subject (13) were not included since they were not amenable to modelling. No …”

“…A low percentage of the dose of such drugs is cleared renally in unchanged form yet, paradoxically, a number of them have diminished clearance in patients with renal dysfunction, or in elderly patients in whom renal function is reduced [8][9][10][11][12][13][14]. Moreover, coadministration of probenecid has caused a decrease in the plasma clearance of these NSAIDs [15][16][17][18][19].…”