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)

Minimal inhibitory concentrations (MICs) of the 4-quinolones ciprofloxacin, enoxacin, norfloxacin, ofloxacin, pefloxacin, difloxacin, A-56620, and CI-934 are consistent world-wide, with allowances for differences in acquired resistance. MICs of these drugs for Enterobacteriaceae correlate with those of nalidixic acid, but resistance to the quinolones is rare if a breakpoint of greater than 2 mg/L is accepted. Most intestinal pathogens are sensitive. Acinetobacter, Pseudomonas aeruginosa, and other Pseudomonas species except Pseudomonas maltophilia are usually sensitive. Ciprofloxacin is generally the most active of the 4-quinolones against these organisms. All of the new agents have antistaphylococcal activity, but that of norfloxacin and ofloxacin is borderline. Against streptococci, including enterococci and pneumococci, the drugs' activity is moderate or poor. Haemophilus influenzae and Branhamella catarrhalis are very sensitive. Gonococci and meningococci are also highly sensitive to the new agents, but activity against Chlamydia trachomatis and the mycoplasmas is borderline. The organisms associated with nonspecific vaginal infection are not very sensitive. Anaerobes except Bacteroides ureolyticus and Clostridium perfringens are mostly resistant.
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PMID:Comparative activity of the 4-quinolones. 327 1

Ciprofloxacin is a new fluoroquinolone that is highly active against many diverse microorganisms. At concentrations of less than 1 microgram/mL it is active against most gram-negative bacteria, including Enterobacteriaceae, Haemophilus, Neisseria, and other Pasteurellaceae, Vibrionaceae, and various species of Pseudomonas and Acinetobacter. Most staphylococci, including strains resistant to methicillin, are also susceptible to ciprofloxacin. Streptococci are not highly susceptible to ciprofloxacin, and obligate anaerobes are generally resistant to this and other quinolones. Ciprofloxacin, like other quinolones, inhibits DNA gyrase, but its bactericidal effects are not completely reversible by inhibitors of protein or RNA synthesis. Thus, unlike many other quinolones, ciprofloxacin may have multiple lethal effects. Resistance is less readily selected in vitro by ciprofloxacin than by nalidixic acid, and single-step mutants usually remain susceptible to clinically achievable concentrations. Resistance mediated by mutations in genes altering DNA gyrase and expression of outer membrane proteins has been described for ciprofloxacin and other quinolones. The antimicrobial spectrum and potency of ciprofloxacin, coupled with its rapid bactericidal effects, make this fluoroquinolone a promising new antimicrobial agent.
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PMID:Ciprofloxacin: in vitro activity, mechanism of action, and resistance. 329 57

The chemistry, mechanism of action, antimicrobial spectrum, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of ciprofloxacin and norfloxacin are reviewed, and mechanisms of antimicrobial resistance and drug and laboratory interactions are described. Norfloxacin is the first antimicrobial in the fluoroquinolone class to be marketed in the United States; ciprofloxacin is under investigation in clinical trials. The fluoroquinolones are structurally related to nalidixic acid. The activity and spectrum are enhanced by the addition of 6-fluoro and 7-piperazino substituents. Quinolone antimicrobials appear to inhibit DNA gyrase, an enzyme specific and essential for all bacteria, as their primary mechanism of action. As a result, DNA synthesis is inhibited. Ciprofloxacin and norfloxacin are active against gram-negative enteric bacteria, Pseudomonas aeruginosa, Haemophilus influenzae, and Neisseria gonorrhoeae. Ciprofloxacin has good activity against Staphylcoccus spp., including methicillin-resistant Staph. aureus. Norfloxacin generally is less potent than ciprofloxacin, particularly against Ps. aeruginosa and Staph. aureus. Peak concentrations occur about one to two hours after an oral administration of either drug. Both drugs are widely distributed in body fluids and tissues and are eliminated by renal excretion, metabolism, and biliary excretion. Dosage reductions are required in severe renal dysfunction. Ciprofloxacin and norfloxacin are effective agents for treating urinary-tract infections, including infections caused by Ps. aeruginosa. The recommended dosage of norfloxacin for urinary-tract infections in adults is 400 mg orally every 12 hours; the drug should be given for 7 to 10 days in uncomplicated infections and for 10 to 21 days in complicated ones. The fluoroquinolones may be useful for treating chronic bacterial prostatitis. Ciprofloxacin is potentially useful for treating sexually transmitted diseases. Ciprofloxacin is active against N. gonorrhoeae, including beta-lactamase-producing strains and strains that are resistant to tetracycline, and Chlamydia spp. Use of ciprofloxacin for treating gastrointestinal infections and for selective decontamination of the gastrointestinal tract is promising. In open studies, ciprofloxacin has been effective against a variety of infections caused by susceptible organisms. Resistance to ciprofloxacin has developed during treatment of infections caused by Ps. aeruginosa, Staph. aureus, and Serratia marcescens. The most frequently reported adverse effects of either drug are gastrointestinal complaints, headache, and dizziness.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Ciprofloxacin and norfloxacin, two fluoroquinolone antimicrobials. 331 72

A-61827 (A-60969 is the hydrochloric salt of A-61827) is a new aryl-fluoronaphthyridine which is active against aerobic and anaerobic bacteria. The MICs of A-61827 for 90% of strains (MIC90) of staphylococci and streptococci were less than or equal to 1 microgram/ml and were generally 1 to 4 twofold dilutions less than those of ciprofloxacin for these bacteria. The MIC90S of A-61827 for members of the family Enterobacteriaceae and Pseudomonas aeruginosa were also less than or equal to 1 microgram/ml. Ciprofloxacin was 1 to 3 twofold dilutions more active than A-61827 against these gram-negative bacteria. Neisseria gonorrhoeae, Campylobacter jejuni, and Haemophilus influenzae were susceptible to less than 0.06 microgram of A-61827 per ml. The MIC90 of A-61827 for Legionella pneumophila was 0.25 microgram/ml. A-61827 was as potent or 1 to 2 twofold dilutions more potent than ciprofloxacin against these organisms. The MIC90 of A-61827 for all anaerobic bacteria was less than or equal to 4 micrograms/ml compared with less than or equal to 32 micrograms/ml for ciprofloxacin. In mouse protection tests, A-61827 was as active as ciprofloxacin against Escherichia coli, P. aeruginosa, and Salmonella typhimurium and 5 to 10 times more active than ciprofloxacin against Staphylococcus aureus and Streptococcus pyogenes. A-61827 was as active as ciprofloxacin against P. aeruginosa in a mouse pyelonephritis model and more active than ciprofloxacin and metronidazole in a mouse Bacteroides fragilis abscess model. After oral administration of 100 mg/kg to mice, the peak concentrations of A-61827 and ciprofloxacin in serum were 2.3 and 2.4 micrograms/ml and the half-lives in serum were 3.9 and 1.2 h, respectively.
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PMID:A-61827 (A-60969), a new fluoronaphthyridine with activity against both aerobic and anaerobic bacteria. 334 9

Ciprofloxacin is a new quinolone antimicrobial agent with activity against a broad spectrum of gram-negative and gram-positive organisms, including Pseudomonas aeruginosa and methicillin-resistant strains of staphylococci. The efficacy and safety results of 80 clinical studies of the oral form of ciprofloxacin are reported. Drug safety was assessed in 2236 courses in 2203 adult patients treated primarily in the United States. Data from 1676 courses were suitable for analysis of drug efficacy. The unit dose for most patients ranged from 250 mg to 750 mg (median, 500 mg), usually given every 12 hours. The duration of treatment ranged from 3 to 231 days (median, 10 days). Predominant among 1722 infections were those of the urinary tract (43%), skin structures (29%), and respiratory tract (19%); the remainder were bone and joint infections (5%), bacteremias (2%), and intra-abdominal (1%), gastrointestinal (1%), and pelvic infections (less than 1%). Signs and symptoms of infection resolved in 79% of all cases; a further 15% improved, and 5% failed to improve. Pathogens were eradicated in 89% of urinary tract infections and persisted in 5%; 80% of patients still had sterile urine at the 3-to 6-week follow-up. In 81% of nonurinary tract infections, pathogens were eradicated; they persisted in 11%, and superinfection occurred in less than 5%. After treatment, 89% of the 2253 causative organisms were eradicated and 2% were reduced to clinically insignificant counts; 8% persisted. Of 411 isolates of P. aeruginosa, 77% were eradicated, as were 97% of 421 Escherichia coli and 80% of 248 Staphylococcus aureus isolates. Also eradicated were 95% of 166 Klebsiella, 96% of 139 Proteus mirabilis, 100% of 20 other Proteus, 94% of 123 Enterobacter, 100% of 68 Haemophilus influenzae, 96% of 49 Citrobacter, 89% of 45 Serratia, 95% of 41 Streptococcus pneumoniae, 91% of 43 Salmonella, 100% of 38 Morganella morganii, and 100% of 35 Providencia isolates. Adverse reactions were judged probably or possibly drug-related in 14.8% of courses; drug treatment had to be stopped prematurely in 3.5%. The most frequent reactions were gastrointestinal complaints (chiefly nausea, diarrhea, and vomiting), metabolic disorders (elevated SGOT, SGPT, serum creatinine, or blood urea nitrogen), and nervous system effects (dizziness, light-headedness, restlessness, tremor, and headache). Crystalluria, judged to be related to ciprofloxacin, occurred in two patients.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:A survey of clinical experience with ciprofloxacin, a new quinolone antimicrobial. 336 Sep 68

The in-vitro antibacterial activity of nalidixic acid and the 4-quinolones, ciprofloxacin, norfloxacin, enoxacin, ofloxacin, pefloxacin, A-56619, A-56620 and CI-934 was assessed by determination of MICs. The 4-quinolones were all highly active against most isolates of Enterobacteriaceae, including nalidixic acid-resistant strains. Ciprofloxacin (MICs 0.002-2 mg/l) was the most active and A-56619 (MICs 0.008-32 mg/l) was the least active. A-56619, A-56620, ofloxacin, ciprofloxacin and CI-934 were highly active against Acinetobacter strains, pefloxacin and enoxacin were slightly less active, and a few strains were resistant to norfloxacin. All the compounds, including nalidixic acid, were active against Aeromonas strains (MICs 0.001-0.12 mg/l). Ciprofloxacin (MICs 0.06-1 mg/l) was the most active compound against Pseudomonas aeruginosa; A-56619 and CI-934 (MICs 1-16 mg/l) were the least active against this species. All the compounds were highly active against Haemophilus influenzae, Branhamella catarrhalis and Neisseria gonorrhoeae but the activity of all the compounds was poor against most isolates of Gardnerella vaginalis. All the 4-quinolones were active against staphylococci and CI-934 (MICs 0.03-0.25 mg/l) was the most active. CI-934 (MICs 0.06-2 mg/l) was also the most active compound against all streptococci. Most streptococci were sensitive also to ciprofloxacin (MICs 0.25-4 mg/l) but there were many isolates resistant to the other 4-quinolones. Against the anaerobic bacteria CI-934 was again the most active compound, particularly against the Gram-positive anaerobic cocci. Pefloxacin, enoxacin and norfloxacin had poor activity against most anaerobes. Ofloxacin, ciprofloxacin, A-56619 and A-56620 had good to moderate activity against all species of anaerobes except the Bacteroides fragilis group, against which none of the compounds was very active.
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PMID:The comparative in-vitro activity of eight newer quinolones and nalidixic acid. 346

The in vitro activities of ofloxacin and ciprofloxacin were tested against five selected groups of clinical bacterial isolates. Both were active against: Staphylococcus aureus and Staphylococcus epidermidis, irrespective of their resistance to methicillin or gentamicin; Haemophilus influenzae and Neisseria gonorrhoeae, irrespective of their beta-lactamase production; members of the Enterobacteriaceae family which were resistant to most oral beta-lactams, and most intestinal bacterial pathogens including Campylobacter, Vibrio, Salmonella, Shigella and Yersinia. Ciprofloxacin was found more active than ofloxacin against Pseudomonas with most isolates of Pseudomonas aeruginosa and Pseudomonas fluorescens susceptible, while those of Pseudomonas cepacia were resistant.
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PMID:Comparative in vitro antibacterial activity of ofloxacin and ciprofloxacin against some selected gram-positive and gram-negative isolates. 346 53

The antibacterial activity of four new fluoroquinolone carboxylic acids, pefloxacin, ofloxacin, enoxacin and ciprofloxacin, against 256 clinical isolates was investigated by means of an agar dilution method. Generally, all quinolones tested had a high activity against Gram-negative bacteria. More than 90% of Enterobacteriaceae strains were inhibited by a quinolone concentration of 0.4 microgram/ml. Also strains usually resistant to conventional beta-lactam antibiotics, and sometimes to third-generation cephalosporins, like Enterobacter spp., Serratia spp, and Yersinia spp. were susceptible to the tested quinolones. Ciprofloxacin was 5 to 25-fold more potent on a weight basis against Enterobacteriaceae than the other quinolones. Neisseria meningitidis, Neisseria gonorrhoeae, and Haemophilus influenzae were extremely susceptible to the new quinolones. Ciprofloxacin was about 10 times more potent against Pseudomonas aeruginosa than the other quinolones, and was the only quinolone that was sufficiently active against all tested P. aeruginosa strains (MIC less than or equal to 0.4 microgram/ml). The activity against Gram-positive bacteria was considerably lower. All the quinolones investigated had an acceptable activity against many of the methicillin-sensitive and methicillin-resistant Staphylococcus aureus and coagulase-negative staphylococci. The majority of the Streptococcus spp. tested was quinolone-resistant, and was Listeria monocytogenes. Generally, it was evident that ciprofloxacin was more potent on a weight basis than the other quinolones, but this difference was counterbalanced by a higher achievable serum concentration for ofloxacin. Some of the investigated fluoroquinolones might constitute valid therapeutical alternatives to beta-lactam antibodies and aminoglycosides in the treatment of serious bacterial infections.
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PMID:Comparative in vitro activities of pefloxacin, ofloxacin, enoxacin and ciprofloxacin against 256 clinical isolates. 347 10

The clinical efficacy, safety, and optimal dosage of oral ciprofloxacin for the treatment of respiratory infections were studied in a multicenter, open trial in Japan. Five hundred seventy-one patients with respiratory infections received orally administered ciprofloxacin (the majority received 600 mg daily). Clinical efficacy was evaluated in 542 of these patients, and safety was analyzed in 568 patients. Clinical efficacy was excellent or good in 80.9 percent of patients with pneumonia, and in 71.3 percent of patients with chronic airway infections. The overall bacteriologic eradication rate was 68.5 percent. In infections caused by Hemophilus influenzae, the rate was 90.8 percent. Side effects were observed in 4.6 percent of patients, and abnormal laboratory findings were noted in 6.9 percent; however, there were no severe reactions. Ciprofloxacin may be a very useful agent for the treatment of respiratory infections.
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PMID:Clinical efficacy of ciprofloxacin in the treatment of patients with respiratory tract infections in Japan. 355 31

Fifty-two patients with serious respiratory infections were treated with orally administered ciprofloxacin; 42 patients were evaluable for the efficacy analysis and all were evaluable for determining adverse reactions. Cures were achieved in 24 patients with infections (14 with bronchitis, 10 with pneumonia) caused by Hemophilus influenzae, Streptococcus pneumoniae, or Branhamella catarrhalis, and pathogens were rapidly eradicated from respiratory secretions. Seventeen patients had infections (seven bronchitis, 10 pneumonia) caused by Enterobacteriaceae or Pseudomonas aeruginosa; many of these patients were critically ill and were enrolled in the study because their pathogens were resistant to multiple drugs or because their infections had not responded to alternate antimicrobial therapy. All patients had favorable clinical responses, and members of the Enterobacteriaceae were rapidly eradicated from respiratory secretions. However, five of 12 strains of P. aeruginosa persisted during treatment; minimal inhibitory concentrations for these strains increased 4- to 16-fold as infections continued to resolve. One patient with Staphylococcus aureus infection also showed a response. Ciprofloxacin probably caused nausea, vomiting, or both in three of the 52 patients and possibly contributed to similar symptoms in another three patients (6 to 12 percent). Other possible adverse reactions, including central nervous system symptoms, were also observed but were not clearly drug-related.
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PMID:Efficacy and safety of oral ciprofloxacin in the treatment of serious respiratory infections. 355 37


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