Laboratory and clinical experiments were performed on pivampicillin in ophthalmological field, and the results obtained were as follows.
1. Pivampicillin is rapidly hydrolyzed to ampicillin (ABPC) in the body. ABPC showed a broad antimicrobial spectrum against bacteria causing ocular infection. 2. The ABPC sensitivity was examined on 40 strains of Staphylococcus aureus isolated from the patients of eye infection, and it distributed in the range of ≥0.1->100mcg/ml. The peak of the distribution was seen at 6.3 mcg/ml in 40% of the strains.
3. Blood concentration of pivampicillin following an oral administration of 500mg to healthy adults, reached its peak level (8.9mcg/ml) after 1 hour, and gradually decreased to 6 hours (0.18mcg/ml). A cross over study was performed with ABPC, and the peak blood level of pivampicillin was 1.5 times higher than that with ABPC.
4. Following an oral administration of 50mg/kg rabbit, the aqueous levels were observed from 1 hour to 6 hours, and the peak level was obtained after 1 hour (2.9mcg/ml). Aqueous/serum ratio was 17.9-66.0%. Ocular tissue concentrations at 1 hour after an oral administration of 50mg/kg were high in the eyelid, conjunctiva, cornea, extraocular muscles, retina, chorioid, iris and ciliary body, while low in vitreous body, sclera and crystalline lens.
5. Oral administration of 125-250mg pivampicillin 4 times daily revealed good therapeutic effects in 25 cases out of 27 cases of ocular infections, such as hordeolum, lid abscess, acute dacryocystitis, corneal infiltration, corneal ulcer, tenonitis and orbital phlegmon.
6. As side effects, gastrointestinal disorder and rash were experienced in each case, but no other severe ones were noticed.
