Poor penetration of cefcapene into aqueous humor after oral administration of cefcapene pivoxil to patients undergoing cataract surgery

  • J Infect Chemother. 2020 Feb;26(2):312-315. doi: 10.1016/j.jiac.2019.08.004.
Koh Okamoto  1 Shotaro Asano  2 Takehito Yamamoto  3 Tetsuya Toyono  2 Ryo Yamaguchi  4 Yuta Okada  5 Shu Okugawa  5 Hiroshi Suzuki  4 Kyoji Moriya  5 Makoto Aihara  2
Affiliations
  • 1. Department of Infectious Diseases, Ophthalmology, and Pharmacy, The University of Tokyo Hospital, Tokyo, Japan. Electronic address: [email protected].
  • 2. Department of Ophthalmology, The University of Tokyo Hospital, Tokyo, Japan.
  • 3. Department of Pharmacy, The University of Tokyo Hospital, Tokyo, Japan; The Education Center for Clinical Pharmacy, Graduate School of Pharmaceutical, Sciences, The University of Tokyo, Tokyo, Japan.
  • 4. Department of Pharmacy, The University of Tokyo Hospital, Tokyo, Japan.
  • 5. Department of Infectious Diseases, Ophthalmology, and Pharmacy, The University of Tokyo Hospital, Tokyo, Japan.
Abstract

Objectives: Studies on the penetration of orally administered cephalosporins to the aqueous humor are scarce. Therefore, in this study, we determined the concentration of cefcapene, a third-generation cephalosporin administrated orally as pivalate ester (cefcapene pivoxil), in the aqueous humor of patients undergoing cataract surgery to assess its potential for preventing postoperative endophthalmitis.

Methods: Forty-four patients were administered a single dose of 100 mg cefcapene pivoxil preoperatively. Blood and aqueous humor samples were obtained at the time of surgery, and cefcapene concentrations were measured using ultra-performance liquid chromatography with tandem mass spectrometric detection.

Results: The samples were obtained from 41 eyes of 39 patients (two patients underwent surgery in both eyes). The median cefcapene concentrations in the aqueous humor after 1-2 h, 2-3 h, and later than 3 h were 8.3, 18.4, and 23.7 ng/mL, respectively. The median cefcapene concentrations in serum after 1-2 h, 2-3 h, and later than 3 h were 198.5, 287.2, and 170.3 ng/mL, respectively. Aqueous humor penetration of cefcapene after 1-2 h, 2-3 h, and later than 3 h was 4.1, 7.9, and 13.5% respectively.

Conclusions: Aqueous humor penetration of orally-administered cefcapene pivoxil in patients undergoing cataract surgery was poor. Therefore, cefcapene pivoxil was unlikely to be effective for preventing endophthalmitis after cataract surgery.

Keywords
Aqueous humor; Cefcapene pivoxil; Concentration; Penetration; Postoperative endophthalmitis.
Products