[Relationship between protein binding and antimicrobial activities of antibiotics against Streptococcus pneumoniae
1Department of Pediatrics, Asahikawa Kosei Hospital.
Insights
Tebipenem and panipenem showed high activity against Streptococcus pneumoniae, while cefditoren and meropenem were most effective against Haemophilus influenzae. Albumin-containing broth increased MIC90 values for tested antibiotics.
Area of Science:
- Microbiology
- Infectious Diseases
- Pharmacology
Background:
- Pediatric bloodstream infections pose significant health risks.
- Streptococcus pneumoniae and Haemophilus influenzae are common bacterial pathogens in children.
- Antimicrobial resistance necessitates ongoing surveillance and evaluation of drug efficacy.
Purpose of the Study:
- To evaluate the in vitro antimicrobial activity of various antibiotics against clinical isolates of Streptococcus pneumoniae and Haemophilus influenzae.
- To compare antibiotic susceptibility testing using standard broth versus albumin-containing broth.
- To identify effective oral and intravenous antibiotic options for treating pediatric infections caused by these pathogens.
Main Methods:
- Microbroth dilution method was employed for susceptibility testing.
- Fifty S. pneumoniae and 42 H. influenzae isolates were tested.
- Testing was performed in both standard broth and broth supplemented with 4.5% albumin.
Main Results:
- Tebipenem exhibited the highest oral activity against S. pneumoniae (MIC90 ≤ 0.06 µg/mL).
- Panipenem demonstrated the highest intravenous activity against S. pneumoniae (MIC90 ≤ 0.12 µg/mL).
- Cefditoren showed the highest oral activity against H. influenzae (MIC90 ≤ 0.06 µg/mL).
- Meropenem displayed the highest intravenous activity against H. influenzae (MIC90 ≤ 0.06 µg/mL).
- Albumin-containing broth resulted in higher MIC90 values compared to standard broth, particularly for highly protein-bound antibiotics.
Conclusions:
- Tebipenem, panipenem, cefditoren, and meropenem are potent agents against the studied S. pneumoniae and H. influenzae isolates.
- The presence of albumin in testing media significantly impacts antibiotic MIC90 values, reflecting in vivo conditions.
- These findings aid in optimizing antibiotic selection for pediatric infections caused by these common pathogens.
Abstract:
Fifty isolates of Streptococcus pneumoniae and 42 isolates of Haemophilus influenzae were isolated from the blood of children admitted to pediatric wards of hospitals in subprefucture between January 1998 and December 2005. The susceptibilities were measured by a microbroth dilution method using a standard broth and a broth containing 4.5% albumin. Against S. pneumoniae, penicillin G, ampicillin, cefotaxime, ceftriaxone, panipenem, meropenem, vancomycin, cefditoren, cefcapene, cefteram, faropenem and tebipenem were used and against H. influenzae, ampicillin, piperacillin, cefotaxime, ceftriaxone, panipenem, meropenem, clavulanic acid/ amoxicillin, cefditoren, cefcapene, cefteram, faropenem and tebipenem were used. Against S. pneumoniae, tebipenem was the highest antimicrobial activity in oral antibiotics (MIC90; < or = 0.06 microg/ml) and panipenem showed the highest activity for intravenous antibiotics (MIC90; < or = 0.12 microg/ml). Against H. influenzae, cefditoren was the highest activity for oral antibiotics (MIC90; < or = 0.06 microg/ml) and meropenem showed the highest activity for intravenous antibiotics (MIC90; < or = 50.06 microg/ml). The MIC90s measured by albumin containing broth were higher than those measured by standard broth. Protein binding rates of ceftriaxone, cefditoren, and faropenem were greater than 90%, and the MIC90 of these antibiotics measured by albumin addition methods were over 4-fold higher than those measured by standard methods.
Related Concept Videos
Factors Affecting Protein-Drug Binding: Drug-Related Factors
One crucial factor in drug-protein binding is the drug's lipophilicity or its affinity for fat. More lipophilic drugs tend to have higher binding extents. For example, highly lipophilic drugs like cloxacillin exhibit substantial protein binding, with as much as 95% of the drug binding to proteins. In contrast,...
Antimicrobial Proteins
Interferons
Interferons (IFNs) are proteins produced by lymphocytes, macrophages, and fibroblasts infected with viruses. While IFNs cannot prevent viruses from entering and...
Factors Affecting Protein-Drug Binding: Protein-Related Factors
The physicochemical properties of a drug play a significant role in its ability to bind to proteins. Lipophilic drugs, which dissolve in fats, oils, and lipids, can be bound by...
Mechanism of Antibiotic Resistance in MRSA
Factors Affecting Protein-Drug Binding: Drug Interactions
Displacement interactions can have varying outcomes, ranging from toxicity to virtually...
Protein-Drug Binding: Mechanism and Kinetics
Various forces drive these interactions, including hydrogen bonds, hydrophobic interactions, ionic bonds, electrostatic interactions, and van der Waals forces. These bonds enable drugs to bind to specific sites on proteins,...


