Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0348321 (Haemophilus)
 15,372 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Sultamicillin at an adult dose of 375-750 mg twice daily or a pediatric dose of 50 mg/kg/d provides effective outpatient/office therapy for community-acquired infections of the upper and lower respiratory tract, urinary tract, and skin/soft tissue structures. Given the incidence of Haemophilus influenzae and Branhamella catarrhalis in otitis media and the frequent occurrence of beta-lactamase-producing strains, it is particularly appropriate for the therapy of otitis media in infants and children. The increasing prevalence of beta-lactamase-producing pathogens in these infections, coupled with the fact that diagnostic bacteriology is often not available or practical in office practice, suggests that the broad use of sultamicillin might be desirable. Several factors support such usage: 1) the superiority of sultamicillin compared with the ampicillin commercial dosage form as a delivery system for ampicillin; 2) the possible occurrence at the infection site of beta-lactamase-producing organisms, not themselves pathogens, which nevertheless impair the activity of the beta-lactam antibiotic against sensitive pathogens; 3) the complementary binding of penicillin-binding proteins by ampicillin and sulbactam in ampicillin-sensitive organisms; 4) the lack of resistance development following repeated exposure of strains sensitive to sulbactam/ampicillin suggested by in vitro studies; and 5) the inability of sulbactam to induce beta-lactamase production. In addition to broad use in community-acquired infections, oral therapy with sultamicillin should also provide convenient outpatient follow-up for initial parenteral sulbactam/ampicillin therapy. Extensive testing of various laboratory parameters has revealed no evidence of systemic toxicity with sultamicillin. The only significant side effect of sultamicillin is diarrhea/loose stools, which, although a frequent complaint in some studies, is of mild to moderate severity and results in a low discontinuation rate.
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PMID:Worldwide clinical experience with sultamicillin. 266 Aug 68

Antimicrobacterial activities of cefteram (CFTM) against clinical isolates collected in 1988 were compared with those of new beta-lactams. 1. Antibacterial activities of CFTM against Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae, Branhamella catarrhalis isolated from acute respiratory tract infections were 8- to 16-fold higher than those of cefaclor (CCL). 2. Activities of cefixime (CFIX) were superior to those of CFTM against B. catarrhalis, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, but were inferior to CFTM against S. pneumoniae, S. pyogenes, Staphylococcus saprophyticus and Staphylococcus aureus. 3. Activities of cefuroxime were superior to those of CCL against each of the 4 tested bacterial species from acute respiratory tract infection and S. aureus by 4-fold, but were inferior to CFTM and CFIX against most of Gram-negative rods. 4. Sultamicillin (SBTPC) is considered to have an activity to inhibit beta-lactamase, but its MICs did not exceed the MICs of ampicillin by itself. SBTPC showed poor antibacterial activities against methicillin-resistant S. aureus (MRSA). Considering these observations, it is apparent that we are faced with a variety of factors in selecting antibiotics for best results.
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PMID:[Antimicrobial activity of cefteram comparison with other oral antibiotics]. 274 61

The pharmacokinetics of sultamicillin and ampicillin suspensions were studied in 20 infants and children 8 months to 69 months of age (mean age, 27 months). Mean peak plasma concentrations of ampicillin and sulbactam occurred at 90 minutes after administration of 42.5 mg of sultamicillin (25 mg of ampicillin/kg and 17.5 mg of sulbactam/kg) per kg to fasting and non-fasting patients. Co-administration of milk usually resulted in higher concentrations of ampicillin and sulbactam, however, the differences in the AUC values between the fasting and fed groups were not statistically significant. Sultamicillin and ampicillin were administered in cross-over fashion to ten children. Plasma concentrations of ampicillin after 42.5 mg of sultamicillin per kg were greater at 20, 40, and 60 min than those after 25 mg of ampicillin per kg alone and the AUC was 39% larger in subjects who received sultamicillin than in those who received ampicillin. Plasma bactericidal activity against a non-beta-lactamase producing Haemophilus influenzae strain was similar for children who were given sultamicillin or ampicillin. Against a beta-lactamase-producing Haemophilus strain the median bactericidal titres were 1:8 at 40, 60 and 90 min after sultamicillin and less than 1:2 at the same intervals after ampicillin.
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PMID:Pharmacokinetics and bactericidal activity of sultamicillin in infants and children. 298 74

Sultamicillin, a dimer of ampicillin and a beta-lactamase-inhibiting agent, sulbactam, was given in oral form to 50 infants and children with acute otitis media. Tympanocentesis was performed on entry into the trial. Beta-lactamase-positive Haemophilus influenzae or Branhamella catarrhalis was isolated from 14 of 73 (19.2%) middle ear effusions in 9 children. Relief of symptoms (fever/otalgia) occurred in all children who completed therapy. However, in 8 children (16%), the antimicrobial agent was discontinued due to presumed adverse side effects (primarily gastrointestinal); vomiting which began prior to entry was noted in another subject who was withdrawn. An additional 14 children completed the course of treatment despite having diarrhea. Of the 41 children who completed drug therapy, 11 (26.8%) were effusion-free after 10 days, and 22 of 33 (66.7%) evaluable children were effusion-free after 6 weeks. Sultamicillin is a novel therapeutic approach to beta-lactamase-producing bacteria. In its oral form, however, diarrhea is a troublesome side effect.
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PMID:Sultamicillin (ampicillin-sulbactam) in the treatment of acute otitis media in children. 300 16

Haemophilus influenzae is a frequent cause of recurrent or chronic lower respiratory tract infections in patients suffering from cystic fibrosis (CF) and other chronic obstructive pulmonary disease (COPD). Ampicillin and its derivatives are routinely used in treatment, but resistant strains producing beta-lactamase frequently necessitate the use of other antibiotics. Sultamicillin is a compound agent for oral use in which ampicillin and the beta-lactamase inhibitor sulbactam are linked as a double ester. This combination is active in vitro against many beta-lactamase producing bacteria including ampicillin-resistant H. influenzae. Eight CF children and ten children with other COPD suffering from chronic or recurrent H. influenzae infection of the lower respiratory tract were treated with sultamicillin orally, 25 mg/kg, 12-hourly, for two weeks. Nine infections were caused by ampicillin-resistant strains. At the end of the treatment 65% of the patients were free of H. influenzae. The only adverse reaction was diarrhoea which occurred in 14 patients, and necessitated withdrawal of one patient from the study.
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PMID:Sultamicillin--a new antibiotic in the treatment of persistent lower respiratory tract infections caused by Haemophilus influenzae. 301 25

Sultamicillin fine granules were used orally in 18 pediatric patients with infections in doses ranging 7.3-10.0 mg/kg t.i.d. or q.i.d. The following is a summary of the results: 1. Clinical efficacies in 16 cases with tonsillitis were excellent in 13 cases, good in 2 cases and fair in 1 case. Efficacy in 1 case of bronchitis and 1 case of pneumonia were good. The overall efficacy rate in the 18 cases was 94.4%. 2. Four out of 5 strains of Staphylococcus aureus were eradicated but 1 strain persisted. Three out of 7 strains of Haemophilus influenzae were rated as eradicated, 1 strain as decreased and 3 strains as persisted. Two strains of Streptococcus pyogenes and 3 strains of Haemophilus parainfluenzae were eradicated. The bacteriological efficacy rate for the 17 strains was 70.6%. Four strains out of the 17 were found to produce beta-lactamase and 3 strains were suspected, to produce the enzyme, but of these 7 strains, 5 strains were eradicated. 3. Diarrhea and loose stool were observed as side effects in each of 2 cases. It appeared that diarrhea was related to this drug. A slight elevation of GOT was observed in 1 case in laboratory tests. 4. This drug appears to be easy for children to take in terms of taste and smell.
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PMID:[Clinical experience with sultamicillin fine granules in pediatric field]. 324 67

Sultamicillin (SBTPC) is a mutual prodrug in which ampicillin (ABPC) and a potent beta-lactamase inhibitor sulbactam (SBT) are ester-bound in an equimolar ratio. SBTPC is hydrolyzed during absorption after oral administration to provide ABPC and SBT for systemic circulation. In the present study, the antimicrobial activities of SBTPC against 50 isolates each of 6 species (Staphylococcus aureus, Klebsiella pneumoniae subsp. pneumoniae, Branhamella catarrhalis, Haemophilus influenzae, Streptococcus pneumoniae and Streptococcus pyogenes) of bacteria freshly obtained from upper respiratory tract infections were examined in relation to their bacterial beta-lactamase producing abilities. beta-Lactamase producing strains were identified using the acidometry disc method with benzylpenicillin (PCG) of cefazolin (CEZ) as a substrate, and their frequencies of appearance were calculated as follows: S. aureus 86%; K. pneumoniae subsp. pneumoniae 100%; B. catarrhalis 68%; H. influenzae 24%. Fourteen per cent of S. aureus strains examined were beta-lactamase positive using both PCG and CEZ acidometry discs. SBTPC, however, demonstrated excellent antimicrobial activities even against these beta-lactamase producing strains. Good activities were observed especially against those bacterial strains producing penicillinase (PCase). Average MIC80 values of SBTPC were 3.13 micrograms/ml for S. aureus and K. pneumoniae subsp. pneumoniae, 0.39 micrograms/ml for B. catarrhalis and H. influenzae, 0.05 micrograms/ml for S. pneumoniae and 0.025 micrograms/ml for S. pyogenes. As SBTPC was shown to possess excellent antimicrobial activities against PCase producing strains, the enhancement in activities of SBTPC compared to ABPC alone can be attributed to the inhibition of beta-lactamase by SBT which, as noted above, is a component of SBTPC in an equimolar ratio to ABPC.
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PMID:[Antimicrobial activities of sultamicillin against clinical isolates from upper respiratory tract infections]. 326 8