Basic and clinical studies on biapenem in ophthalmology
Keywords:
Biapenem
1994 Volume 42 Issue Supplement4 Pages 650-661
Details
1994 Volume 42 Issue Supplement4 Pages 650-661
We performed basic and clinical studies of biapenem (BIPM), a new parenteral carbapenem antibiotic, in ophthalmology.
BIPM showed a broad antibacterial spectrum against gram-positive, gram-negative and anaerobic bacteria.
The MIC80s against clinical isolates of Staphylococcus aureus (20 strains) and Pseudomonas aeruginosa (20 strains) were 0.19μg/ml and 1.56μg/ml, respectively.
Penetration of BIPM into aqueous humor of the anterior chamber reached a peak of 12.2μg/ml at 30 min after intravenous administration of 50mg/kg to mature white rabbits, and thereafter the level decreased to 0.1μg/ml at 6 hours after administration.
The rate of aqueous humor to blood concentration was 15.1%. Ocular tissue concentrations were 7.7-26.3μg/ml in extraocular tissues and 0.5-2.2μg/g or ml in intraocular tissues at 30min after administration.
Penetration of BIPM into human aqueous humor of the anterior chamber reached 0.24-2.60μg/ml at 35-190min after intravenous drip infusion of 300mg to human volunteers. The penetration into human tear reached a peak of 2.25μg/ml at 15min after initiation of BIPM (300mg) drip infusion for 30min, and the level decreased to 0.31μg/ml 4 hours after administration. The rate of tear to blood concentration was 14.2%.
We treated 21 patients (dacryocystitis 1, lid abscess 1, corneral ulcer 10, endophthalmitis 5 and orbital infection 4) with BIPM drip infusion at a dose of 150, 300, 450 or 600 mg one to three times a day. Three unevaluable cases were deducted, hence 18 cases were evaluated for analysis of the clinical effect. Clinical responses were excellent in 4, good in 11 and fair in 3, therefore the efficacy rate was 83.3%.
The following organisms were isolated from the patients: gram - positive bacteria from 8, gramnegative bacteria from 2 and anaerobic bacteria from 4. The eradication rate was 92.3%.
No side effects were observed in any of the 21 patients. In laboratory data, decrease of white blood cell and increase of BUN were observed in one patient.
