Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0034186 (pyelonephritis)
 6,144 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

SQ 14,359 is a new cephamycin-type (7alpha-OCH3) antibiotic belonging to a series containing a 7alpha-ureidoacetyl substituent. The compound is the most potent extended spectrum derivative of this type yet reported, surpassing CS-1170 and cefoxitin by a wide margin. This activity in vitro which extends throughout the Enterobacteriaceae is particularly prominent against Gram-negative organisms that are producers of "cephalosporinase-type" beta-lactamases such as Enterobacter, Serratia, Citrobacter and indole-positive Proteus species. Superior activity also is demonstrated in vitro against streptococci, beta-lactamase-producing staphylococci, Haemophilus influenzae, Neisseria gonorrhoeae, and many Gram-negative pathogens resistant to aminoglycoside antibiotics. Experimental chemotherapeutic studies have confirmed these observations in wound and selected systemic infections in mice as well as acute pyelonephritis and meningitis in rats. The pharmacokinetics for each drug including antibiotic bound to serum was similar in both mice and rats. The pharmacokinetic profile in blood and cerebrospinal fluid favored SQ 14,359.
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PMID:Cephamycin derivatives: comparison of the in vitro and in vivo antibacterial activities of SQ 14,359, CS-1170, and cefoxitin. 71 11

In the early 1980's parenteral third generation cephalosporins changed the hospital use of antibiotics. The MICs of these cephalosporins are several dozen times lower than those of first or second generation cephalosporins for Enterobacteriaceae and they are much more beta-lactamase stable than second generation cephalosporins. After years of research, is has finally been possible to develop orally active compounds possessing the same antibacterial activity as parenteral third generation cephalosporins, either through the use of prodrugs, or by modifying the molecular structure of drugs. Cefixime is an example of the latter. The vinyl group at the 3-position of the cephem nucleus is responsible for the intestinal absorption of the intact molecule, primarily by a carrier-mediated transport mechanism. The aminothiazole ring and the R-oxyimino group on the side-chain at the 7-position are associated with an antibacterial activity similar to that of third generation cephalosporins. Thousands of adults have been treated by cefixime for lower respiratory tract, ear-nose-throat and urinary tract infections, showing that cefixime is a safe and effective antimicrobial agent. The major clinical indications for cefixime in adults are bronchial and pulmonary infections, acute otitis or sinusitis, acute pyelonephritis with no underlying uropathy, and complicated or uncomplicated lower urinary tract infections excluding prostatitis. In all cases, the dosage is 200 mg b.i.d.
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PMID:[Cefixime, the first oral third-generation cephalosporin]. 253 May 27

Sixty pediatric patients (27 males and 33 females) between the ages of 7 months and 11.7 years (mean age = 4.3 yr) were treated with parenteral sulbactam plus ampicillin (1:2 ratio) for lower respiratory tract infections (29 cases), upper respiratory tract infections (4 cases), urinary tract infections (25 cases) or skin/soft tissue infections (2 cases). The infection was mild in 6 cases, moderate in 44 and severe in 10. The infection was acute in 57 patients, recurrent in 1 (cystitis) and was a flare-up of a chronic infection in 2 (pyelonephritis and cystitis). The children received an average dose of 48 mg/kg/d of sulbactam plus 96 mg/kg/d of ampicillin by the i.m. route (43 cases) or by i.v. drip (17 cases) in 3-4 divided doses. The length of treatment ranged between 3 and 10 d (mean duration = 6 d). At the end of therapy, clinical cure was achieved in 53 patients (88.3%), while 6 (10%) had a marked improvement. Only 1 patient, with a lower respiratory tract infection, did not respond to therapy. All 25 patients with urinary tract infection experienced bacteriological cure at the end of treatment. No side effects were reported. Mild and transient changes in laboratory parameters from baseline values were observed in 10 patients (eosinophilia, elevation of SGOT or SGPT) without clinical consequence. Sulbactam plus ampicillin was effective and safe in the treatment of bacterial infections in children and appears to be useful in the treatment of those infections in which beta-lactamase-producing organisms are involved.
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PMID:Clinical evaluation of sulbactam plus ampicillin in the treatment of general pediatric infections. 266 Aug 70

Pharmacokinetic and clinical studies on sulbactam/ampicillin (SBT/ABPC) were carried out in the field of pediatrics. 1. Absorption and excretion Serum levels and urinary excretion of SBT/ABPC were studied in 4 children with ages 6 to 8 years. The mean serum concentration of SBT at 15 minutes following a single intravenous injection of 30 mg/kg of SBT/ABPC was 27.4 +/- 2.2 micrograms/ml and that of ABPC was 42.8 +/- 3.9 micrograms/ml, and their concentrations declined with mean half-lives of 1.06 +/- 0.15 hours and 0.84 +/- 0.05 hour, respectively, and at 6 hours were 0.3 +/- 0.2 microgram/ml and 0.2 +/- 0.1 microgram/ml on the average, respectively. The urinary recovery rates of SBT and ABPC at 6 hours after the injection were 59.0 +/- 22.4% and 58.4 +/- 25.3% on the average, respectively. 2. Clinical study SBT/ABPC was used for the treatment of a total of 36 pediatric patients with ages ranging 2 months to 11 years and it's clinical effectiveness, bacteriological efficacy and adverse effects were evaluated. Clinical efficacies in 5 patients with acute purulent tonsillitis, 26 with acute pneumonia and 1 with acute pyelonephritis were judged to be excellent in 27 cases and good in 5 cases with an overall efficacy ratio of 100.0%. Clinical efficacies in 6 patients whose infections were caused by beta-lactamase producing strains were judged to be excellent in all cases. Bacteriological efficacies of SBT/ABPC were assessed on 1 strain of Staphylococcus aureus (beta-lactamase producing strain), 2 strains of Streptococcus pneumoniae, 16 strains of Haemophilus influenzae (5 beta-lactamase producing strains and 11 non-beta-lactamase producing strains), 1 non-beta-lactamase strain of Haemophilus parainfluenzae and 2 strains of Escherichia coli (non-beta-lactamase producing strains). All strains except 1 strain of H. influenzae (beta-lactamase producing strain) which decreased in number were eradicated with a bacteriological eradication rate of 95.5%. Only 1 patient complained of diarrhea which was suspected to be related to the drug. No other side effect was reported. Elevations of GOT and GPT were observed in only 1 patient. The above results suggested that SBT/ABPC was a useful drug with preferable safety profile in the treatment for pediatric patients with infectious disease caused by beta-lactamase producing strains as well as those by non-beta-lactamase producing strains.
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PMID:[Studies on sulbactam/ampicillin in the field of pediatrics]. 266 50

Sulbactam/Ampicillin (SBT/ABPC), a combination at a fixed ratio of ABPC and SBT which is an irreversible inhibitor of beta-lactamase in a 2:1 ratio, was clinically evaluated for its efficacy and safety in 24 patients with ages from 5 month-old to 12 years old with bacterial infection. The results obtained are summarized as follows. 1. A pharmacokinetic study following 30 mg/kg SBT/ABPC administration by 30 minutes drip infusion or intravenous bolus injection showed that mean half-lives of SBT and ABPC were 48.9 minutes and 40.2 minutes, respectively, and mean urinary excretion rates of SBT and ABPC in the first 6 hours were 67.1% and 48.3%, respectively. 2. SBT/ABPC was administered to 14 patients with bronchopneumonia, 4 patients with tonsillitis, a patient each with acute upper respiratory infection, with submandibular lymphadenitis, with phlegmon, with enterocolitis, with pyelonephritis and with cystitis at a daily dosage of 88.2-133.3 mg/kg, divided into 3 or 4, by intravenous bolus injection or by 30 minutes drip infusion. Clinical responses of the 24 patients were as follows: excellent: 17 patients, good: 7 patients. The efficacy rate was 100%. 3. Neither clinical adverse reactions nor abnormal laboratory test values, except slight eosinophilia in a patient and an elevation of GOT, GPT in another were observed. 4. MICs of SBT/ABPC against 7 strong beta-lactamase producing strains isolated from some of the patients were as follows. MIC against a strain of Staphylococcus aureus was 3.13 micrograms/ml, MICs against 2 out of 5 strains of Branhamella catarrhalis were 0.10 microgram/ml and those of the remaining 3 strains were 0.20 microgram/ml. MIC against a strain of Haemophilus parainfluenzae was 3.13 micrograms/ml. 5. These data described above show that SBT/ABPC has excellent bactericidal capacity against beta-lactamase producing bacteria as well as beta-lactamase non-producing Gram-positive and negative bacteria and suggest that SBT/ABPC is a very useful antibiotic for pediatric patients.
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PMID:[Clinical evaluation of sulbactam/ampicillin in children]. 266 51

The therapeutic effects produced by ticarcillin plus clavulanic acid were compared with those of ticarcillin and clavulanic acid separately against infections in the mouse caused by beta-lactamase-producing bacteria. The infections studied included a pneumonia model, a local tissue infection and pyelonephritis. The distribution of ticarcillin and clavulanic acid in infected animals was evaluated by measurement of the concentrations of the substances present at sites of infection. The results showed that both ticarcillin and clavulanic acid were well-distributed in the mouse and at the doses employed were present at the sites of infection at concentrations of the same order as those obtained in man after administration of ticarcillin/clavulanic acid formulations (Timentin). The protection of ticarcillin by clavulanic acid from inactivation by the beta-lactamases produced in vivo by Bacteroides fragilis, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa was demonstrated by the pronounced bactericidal effects produced by the ticarcillin/clavulanic acid combination against the ticarcillin-refractory infections studied.
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PMID:Antibacterial effects of ticarcillin/clavulanic acid in animal models of infection. 308 34

It is estimated that more than 110 million dollars' worth of oral antibiotics will have been sold in Canada in 1987. In the next few years several new oral antimicrobial agents will reach the market, including beta-lactamase inhibitors, cephalosporins, monobactams, erythromycins and quinolones. Most of these new agents have a broader spectrum of antibacterial activity than the presently available oral antibiotics. A few have a longer half-life and can be administered once a day. The new oral drugs, especially the quinolones and possibly beta-lactams, will now be used to treat infections that in the past could be treated only parenterally. Exacerbations of pulmonary infections due to Pseudomonas aeruginosa in cystic fibrosis can now be successfully treated at home with the new quinolones. Osteomyelitis, arthritis, pneumonia and pyelonephritis will most likely be treated at home in the future. In severe infections patients will be admitted to hospital for short courses of parenteral therapy, followed by oral treatment. If used appropriately the new oral agents may lead to new approaches to the treatment of infectious diseases.
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PMID:The future of new oral antibiotics including the quinolones. 327 79

The comparative efficacies of ticarcillin and ticarcillin plus clavulanic acid have been determined in the mouse against experimental infections caused by ticarcillin-resistant bacteria. The infections studied comprised an intraperitoneal infection, local tissue infections, pyelonephritis, and pneumonia. Both ticarcillin and clavulanic acid penetrated readily to the sites of infection studied and at the doses employed were present at concentrations of the same order as those obtained in humans after the administration of ticarcillin-clavulanic acid formulations (Timentin; Beecham). At these concentrations, the ticarcillin-clavulanic acid combination caused significant bactericidal effects at the sites of infection against the ticarcillin-resistant strains of Bacteroides fragilis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus investigated. The efficacy of ticarcillin plus clavulanic acid against the infections resistant to therapy with ticarcillin demonstrated the beta-lactamase-inhibitory activity of clavulanic acid in vivo.
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PMID:Bactericidal effects of ticarcillin-clavulanic acid against beta-lactamase-producing bacteria in vivo. 352 31

Tigemonam, a new monobactam with excellent activity against gram-negative bacteria, was evaluated for in vivo efficacy and absorption after oral administration to laboratory animals. Tigemonam is absorbed when administered orally to mice and dogs. In a variety of gram-negative systemic infections in mice, orally administered tigemonam was efficacious in all infections studied. Comparison drugs such as amoxicillin, cephalexin, and cefaclor were less efficacious, especially in infections caused by beta-lactamase-producing organisms. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin. Tigemonam was well absorbed in laboratory animals and with its excellent gram-negative spectrum of activity should prove of value in oral antibiotic therapy in humans.
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PMID:In vivo evaluation of tigemonam, a novel oral monobactam. 355 30

Temocillin is a beta-lactamase-stable penicillin with a selective. Gram-negative spectrum of activity and a long half-life. Previous studies in adult patients have demonstrated its efficacy and safety in the treatment of Gram-negative infections. The aim of the study was to evaluate the clinical and bacteriological efficacy and safety of temocillin in children with complicated urinary tract infections. Twenty-two children, aged 3 months to 13 years (mean 5.8 years) were treated with temocillin i.v. at a dose of 25 mg/kg 12 hourly for a mean period of 5.9 days (range 3-12 days). Acute pyelonephritis was diagnosed in 21 patients (one case associated with septicaemia); one patient presented recurrent bacteriuria due to a multiresistant pathogen. Some 20/22 children presented an underlying condition complicating the urinary tract infection (UTl). The causative pathogens, isolated from the urine, were: E. coli (17), Proteus mirabilis (3), Enterobacter cloacae (1), enterococcus (1). The enterococcus and one Proteus mirabilis were found to be resistant to temocillin. Clinical improvement was obtained after 24-36 h in all children with temocillin-sensitive organisms. Bacteriological cure was obtained in all patients with temocillin-sensitive organisms. The two patients with temocillin-resistant pathogens were treated with another antibiotic. Follow-up treatment was given per os during +/- 2 weeks. No adverse reactions or abnormal laboratory values were noted. In the authors' limited experience temocillin proved to be effective and safe in the treatment of pyelonephritis often due to ampicillin-resistant strains in children.
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PMID:Temocillin in the treatment of pyelonephritis in children. 362 46


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