Topic
Penicillin
About: Penicillin is a research topic. Over the lifetime, 17916 publications have been published within this topic receiving 368480 citations. The topic is also known as: penicillin antibiotic & PCN.
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TL;DR: This minireview focuses on the specific problems encountered in managing patients with penicillinand cephalosporin-resistant pneumococcal meningitis and discusses some therapeutic alternatives that have recently been explored.
Abstract: Since the isolation of the first penicillin-resistant Streptococcus pneumoniae strain in 1967 (23), there have been many reports of treatment failure in patients with pneumococcal infections caused by strains resistant to penicillin and other antimicrobial agents such as chloramphenicol, macrolides, trimethoprim-sulfamethoxazole, and the cephalosporins. As a result, the selection of antimicrobial agents for the treatment of infections caused by these organisms has become increasingly difficult. In particular, the emergence of pneumococci resistant to broad-spectrum cephalosporins has limited the choices of antibiotics for the treatment of pneumococcal meningitis. This minireview focuses on the specific problems encountered in managing patients with penicillinand cephalosporin-resistant pneumococcal meningitis and discusses some therapeutic alternatives that have recently been explored.
116 citations
TL;DR: In this article, anti-PBP2A beta-lactams with over 10-fold greater penicillin-binding protein 2A affinities and low minimal inhibitory concentrations were developed, primarily in the cephem and carbapenem classes.
116 citations
TL;DR: This study directly proves that penicillin acylates the active site of twoPenicillin-sensitive enzymes, D-alanine carboxypeptidases from Bacillus stearothermophilus and Bacillus subtilis and suggests that these two groups of enzymes are evolutionally related.
Abstract: It has been hypothesized that penicillin acts as a structural analog of the acyl-D-alanyl-D-alanine terminus of nascent bacterial cell wall and that it consequently binds to and acylates the active site of the enzyme(s) that crosslinks the cell wall to form an inactive penicilloyl enzyme [Tipper, D.J. & Strominger, J.L. (1965) Proc. Natl. Acad. Sci. USA 64, 1133-1138]. This study directly proves that penicillin acylates the active site of two penicillin-sensitive enzymes, D-alanine carboxypeptidases from Bacillus stearothermophilus and Bacillus subtilis. Active site peptides were generated by chemical or enzymatic cleavage of these carboxypeptidases after covalently labeling with [14C]penicillin G or after trapping an acyl-enzyme intermediate derived from the depsipeptide substrate. [14C]diacetyl-L-lysyl-D-alanyl-D-lactate. The amino acid sequences of the penicillin- and substrate-labeled peptides were identical. Both penicillin and substrate were covalently bound via an ester linkage to the same active site residue, a serine at position 36 of the B. stearothermophilus carboxypeptidase and the corresponding serine in the B. subtilis carboxypeptidase. The two D-alanine carboxypeptidases showed significant homology around the active site. Moreover, homology between these two enzymes and four beta-lactamases of known sequence suggests that these two groups of enzymes are evolutionally related.
116 citations
TL;DR: Borrelia burgdorferi was most susceptible in vitro to erythromycin, ceftriaxone and cefotaxime, and penicillin G showed poor activity both in vitro and in vivo.
Abstract: The antispirochetal activity in vitro and in vivo of several antibiotics against ten isolates of Borrelia burgdorferi from human spinal fluids and skin biopsies was determined. Borrelia burgdorferi was most susceptible in vitro to erythromycin, ceftriaxone and cefotaxime (MIC90: 0.06, 0.06, 0.12 mcg/ml respectively). Less activity was observed with tetracycline, amoxycillin and lincomycin (MIC90: 0.50 mcg/ml), imipenem and augmentin (MIC90: 0.25 mcg/ml), oxacillin (MIC90: 1 mcg/ml), ciprofloxacin (MIC90: 2 mcg/ml) and ofloxacin (MIC90: 4 mcg/ml). Penicillin G, normally regarded as appropriate treatment for Lyme disease, had an MIC90 of only 4 mcg/ml. With the exception of erythromycin, activity in vitro corresponded to the activity in vivo. Erythromycin, however, was less active in vivo, and penicillin G showed poor activity both in vitro and in vivo.
116 citations
TL;DR: Control of penicillin resistance among strains of Streptococcus pneumoniae will require innovative methods to reduce the selective pressure that results from widespread antibiotic use and to develop effective pneumococcal vaccines that are immunogenic in young infants.
Abstract: Penicillin resistance among strains of Streptococcus pneumoniae has emerged as an important worldwide problem. Beta-lactam-resistant pneumococci also can be resistant to erythromycin, trimethoprim/sulfamethoxazole and tetracycline and are uniformly susceptible to vancomycin and imipenem. Crowded conditions (e.g. daycare centers, hospitals, military barracks and prisons) and prior beta-lactam antibiotic therapy are the principal predisposing factors to colonization and disease. To date the two conditions caused by penicillin- and cephalosporin-resistant pneumococci that have been especially difficult to treat are acute otitis media and meningitis. Concentrations of beta-lactams in cerebrospinal fluid and middle ear fluid are usually inadequate to achieve prompt eradication of some intermediately resistant and most highly resistant pneumococcal strains. Use of unconventional therapeutic agents such as ceftriaxone or clindamycin for acute otitis media and vancomycin or rifampin for meningitis may be necessary. Control of this global problem will require innovative methods to reduce the selective pressure that results from widespread antibiotic use and to develop effective pneumococcal vaccines that are immunogenic in young infants.
116 citations