Vol.57 No.S-1 March 2009

Pharmacokinetics and safety of tebipenem pivoxil tablets in healthy volunteers and in patients with reduced renal function

Mitsuyoshi Nakashima¹⁾, Jun Morita²⁾ and Kazumasa Aizawa²⁾

¹⁾Hamamatsu Institute of Clinical Pharmacology & Therapeutics, 40-3 Sukenobu, Naka-ku, Hamamatsu, Shizuoka, Japan
²⁾Clinical Research Department, Meiji Seika Kaisha, LTD.

Abstract

We assessed the pharmacokinetics and safety of tebipenem pivoxil(TBPM-PI), an oral carbapenem antibiotic, and TBPM prodrug, in healthy volunteers and patients with reduced renal function.
Subjects were classified by creatinine clearance (Ccr) into four groups: group I with 6 subjects (Ccr≥80 mL/min), group II with 6 (50≤Ccr<80 mL/min), group III with 2 (30≤Ccr<50 mL/min), and group IV with 3 (Ccr<30 mL/min). TBPM-PI tablets were administered at 250 mg (potency). We observed decreased renal clearance and urinary excretion, increased AUC_0-∞ and C_max, and prolonged t_1/2 together with deteriorated renal function. These changes were particularly marked in group IV. Renal clearance and apparent total clearance of TBPM correlated well with Ccr, and renal function was confirmed to affect TBPM excretion.
We concluded that appropriate use is recommended when TBPM-PI is administered to patients with reduced renal function, given that renal function influences TBPM-PI pharmacokinetics.

Key word

tebipenem pivoxil, renal insufficiency, pharmacokinetics

Received

October 15, 2008

Accepted

December 12, 2008

Jpn. J. Chemother. 57 (S-1): 109-114, 2009