[Review: New antimicrobial agent series XXII: Aspoxicillin].

The results of clinical and laboratory studies on aspoxicillin (ASPC) are summarized in this paper. 1. ASPC possesses a broad antibacterial spectrum in vitro against Gram-positive and Gram-negative bacteria. ASPC shows more potent activity in vivo and stronger bactericidal action than expected from in vitro activity. 2. Peak blood levels of ASPC after intravenous injection or intravenous drip infusion are dose dependent and half-lives of ASPC in these cases are about 1.6 hours. ASPC is excreted in active form mostly into urine via kidney. ASPC is satisfactorily transferred into various tissues and body fluids, such as bile, sputum. The binding rate of ASPC to serum protein is much lower than penicillin derivatives like piperacillin (PIPC), sulbenicillin (SBPC) and ampicillin (ABPC). 3. In an open clinical trial of ASPC, 1,845 cases were evaluated. Clinical effects were excellent in 543 cases (29.4%) and good in 822 cases (44.6%), and the efficacy rate for cases judged as excellent and good comprised 74.0%. 4. Comparative studies in which the efficacy of ASPC was compared to efficacies of PIPC and SBPC were performed in patients with respiratory tract infections, postoperative wound infections and suppurative otitis media. ASPC showed satisfactory clinical effects in all trials. 5. In the above open and comparative clinical studies of ASPC, incidence of adverse side reaction was only 1.95% (45/2,304), and main side effects were skin rash and diarrhea.