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PubMed1972

7-(Alpha-(1-methyl-4-pyridinothio)-acetamido) cephalosporanic acid.

7-[alpha-(1-Methyl-4-pyridiniothio)-acetamido] cephalosporanic acid, referred to herein as BL-S 217, is a new broad-spectrum semisynthetic cephalosporin that offers several advantages over cephalothin. A comparison of the activity in vitro of these antibiotics indicates that BL-S 217 is about eightfold more effective against Streptococcus pyogenes and Diplococcus pneumoniae. Against gram-negative bacteria, BL-S 217 possesses a broader antibacterial spectrum than cephalothin, particularly against members of the Enterobacteriaceae family; e.g., BL-S 217 inhibited over 20% more strains of both Escherichia coli and Klebsiella than cephalothin and also showed some advantage in tests against Salmonella and Enterobacter. Overall, of 208 strains of Enterobacteriaceae tested, 172 were susceptible to BL-S 217 compared to 149 for cephalothin. BL-S 217 was less bound to human serum proteins than cephalothin and gave higher peak blood levels in mice after intramuscular administration. The LD(50) of BL-S 217 in mice after subcutaneous administration was in excess of 4,000 mg/kg. When administered by the same route to mice experimentally infected with cephalothin-sensitive bacterial strains, this new cephalosporin was 20 times more effective than cephalothin in S. pyogenes and D. pneumoniae infections and 3 to 4 times more efficacious in an E. coli infection. Its therapeutic efficacy was comparable to that of cephalothin in infections produced by strains of Staphylococcus aureus, Klebsiella pneumoniae, and Proteus mirabilis.

Acetamides↗
PubMed1977

Antibiotic prophylaxis for open-heart surgery.

A randomized, prospective study of the relative effectiveness of broad-spectrum versus specific antistaphylococal antibiotic prophylaxis in patients having open-heart surgery was performed between May, 1972, and June, 1973. All patients undergoing open-heart surgery was assigned randomly (by hospital number) to receive either methicillin or cephalothin beginning the night before operation. There were 132 patients in the cephalothin group and 129 in the methicillin group. There was no statistically significant differences in age or duration of hospitalization, cardiopulmonary bypass, urinary tract drainage, or postoperative fever. There was a significant difference in the ratio of male to total patients (cephalothin group, 0.67; methicillin group, 0.52; p less than 0.02) and duration of operation (cephalothin group, 4.27 hours; methicillin group, 3.87 hours; p less than 0.05). The methicillin group had a statistically significant higher rate of urinary tract infection (cephalothin group, 3 cases; emthicillin group, 22 cases, p less than 0.05), pneumonia (cephalothin group, no cases; methicillin group, 9 cases; p less than 0.01), and episodes of sepsis and prosthetic valve endocarditis (cephalothin group, no cases; methicillin group, 11 cases, p less than 0.001). The incidence of wound infections and positive blood cultures from blood obtained immediately after termination of cardiopulmonary bypass was not significantly different between the two groups. Cephalothin has replaced methicillin as the routine prophylaxis for open-heart surgery at our institution.

Bacterial Infections↗