Roxithromycin Pharmacokinetics in Hospitalized Geriatric Patients: Oral Administration of Whole Versus Crushed Tablets.

BACKGROUND: Drug administration as tablets to debilitated elderly patients in crushed form can modify the pharmacokinetic characteristics of the active components. Only scarce information is available on the pharmacokinetics when administered in such form. The aim of this study was to evaluate the pharmacokinetics of roxithromycin administered in crushed form and to compare it with the pharmacokinetics of a group of geriatric patients receiving it in the conventional tablet form. METHODS: Twenty patients from the acute ward of the Shmuel Harofeh Geriatric Medical Center in stable, clinical, and hemodynamic condition were studied. Patients in group 1 (n = 10) received medications orally in tablet form. Group 2 (n = 10) included age- and disease-matched patients from the same department, who received oral roxithromycin in crushed tablet form. The mean daily dose was the same in both groups: 300 mg (150 mg twice daily). The patients received the drug for 3 days before the initiation of the study. Blood samples for determination of the roxithromycin concentration were taken at the baseline, 1 hour before the drug administration, and at 1, 3, 4, 6, 8, and 10 hours after drug administration. Roxithromycin concentration was measured by a liquid chromatography-tandem mass spectrometry method. RESULTS: Pharmacokinetic parameters of roxithromycin were significantly different between the 2 groups: the Cmin and Cmax were significantly higher, the tmax significantly longer, AUC0-10 larger, and CL/F smaller in group 2. CONCLUSIONS: Roxithromycin pharmacokinetic parameters were significantly different between the 2 patient groups resulting in higher drug serum concentrations in the crushed tablets group. The impact of the increased drug exposure is unclear.