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Biomedical subjects

R J Fass

Publications and source records attributed to R J Fass.

At least 55 records · Page 3Linked to original sources

Comparison of oral fluconazole and clotrimazole troches as treatment for oral candidiasis in patients infected with human immunodeficiency virus.

Thirty-nine adult patients with human immunodeficiency virus infection and oral candidiasis were randomly assigned to receive either one fluconazole capsule (100 mg) or five clotrimazole troches (10 mg each) daily for 14 days. Among 36 evaluable patients, clinical resolution rates were 100 and 65%, respectively (P = 0.018). Mycological eradication rates were 75 and 20%, respectively (P = 0.004). Fluconazole-treated patients were more likely to remain disease free during follow-up than those treated with clotrimazole (P = 0.014 at 2 weeks). Prolonged clinical responses correlated with mycological eradication at the end of therapy (P = 0.043).

Acquired Immunodeficiency Syndrome↗

Penicillinase production and in vitro susceptibilities of Staphylococcus lugdunensis.

Of 59 clinical isolates of Staphylococcus lugdunensis, 76% were beta-lactamase negative, with penicillin G MICs of less than or equal to 0.13 microgram/ml, and 24% were beta-lactamase positive, with penicillin MICs of greater than or equal to 0.5 microgram/ml. Bimodal distributions were observed also with ampicillin, ampicillin-sulbactam, and amoxicillin-clavulanate. All strains were susceptible to oxacillin, cephalothin, gentamicin, rifampin, and vancomycin; 98% were erythromycin susceptible.

Anti-Bacterial Agents↗

In vitro activity of BAY v 3522, a new oral cephalosporin.

The in vitro activity of BAY v 3522 was compared with the activities of cephalexin, cefaclor, cefuroxime, cefixime, and amoxicillin-clavulanate. MICs (in micrograms/ml) of BAY v 3522 were as follows: Staphylococcus spp. (except for oxacillin-resistant strains), 0.13 to 1; Streptococcus spp. (except for some viridans group streptococci), less than or equal to 0.015 to 0.25; Enterococcus faecalis, 2 to 8; other enterococci, 0.5 to greater than 32; beta-lactamase-negative Haemophilus influenzae and Branhamella catarrhalis, 0.13 to 1; beta-lactamase-positive H. influenzae and B. catarrhalis, 0.5 to 4; Pasteurella multocida, 0.06 to 0.25; and members of the family Enterobacteriaceae, 0.5 to greater than 32. Among the cephalosporins, BAY v 3522 was the most active against gram-positive cocci and cefixime was the most active against gram-negative bacilli; BAY v 3522 was similar in activity to amoxicillin-clavulanate against most species.

Administration, Oral↗

Intravenous/oral ciprofloxacin versus ceftazidime in the treatment of serious infections.

Seventy-one adult patients with 72 infections were treated, by random selection, with intravenous/oral ciprofloxacin or intravenously administered ceftazidime. Twenty-seven additional patients with 29 infections who were not appropriate for random assignment were treated in an open study with intravenously administered ciprofloxacin only; the latter infections were generally more serious or were caused by ceftazidime-resistant organisms. The most common doses were ciprofloxacin, 200 mg intravenously and 500 mg orally every 12 hours and ceftazidime, 1 to 2 g intravenously every eight to 12 hours. Forty-seven ciprofloxacin-treated infections and 31 ceftazidime-treated infections were evaluable for determination of efficacy. Infections included lower respiratory tract (21 infections), urinary (37 infections), skin/soft tissue (14 infections), bacteremia/endocarditis (four infections), colitis (one infection), and mastoiditis (one infection). Median minimal inhibitory concentrations of ciprofloxacin and ceftazidime were, respectively: for Enterobacteriaceae, Haemophilus influenzae, and Branhamella catarrhalis, no more than 0.06 and no more than 0.25 micrograms/ml; for Pseudomonas aeruginosa, 0.25 and 4 micrograms/ml; for Enterococcus faecalis, 1 and more than 32 micrograms/ml; and for Staphylococcus aureus, 0.25 and 8 micrograms/ml. Ciprofloxacin, 200 mg intravenously, yielded mean serum concentrations 0.5 and eight hours post-intravenous infusion of 2.3 and 0.7 micrograms/ml, respectively. Satisfactory clinical responses were achieved in 17 (81 percent) of 21 patients with intravenous/oral ciprofloxacin, 22 (71 percent) of 31 patients with ceftazidime, and 20 (77 percent) of 26 patients with intravenous ciprofloxacin. The most common treatment failures occurred in complicated skin/soft-tissue infections treated with intravenous/oral ciprofloxacin, complicated urinary tract infections treated with ceftazidime, and necrotizing P. aeruginosa pneumonia treated with intravenous ciprofloxacin; the pneumonia patients all had respiratory failure and had been previously unresponsive to treatment with other appropriate drugs. Serious adverse reactions were observed in three patients, seizures with intravenous ciprofloxacin in two patients, and Clostridium difficile diarrhea with ceftazidime in one patient. We conclude that sequential intravenous/oral ciprofloxacin and ceftazidime were comparable in efficacy and safety; the ability to change from intravenous to oral therapy is a major convenience. Intravenous ciprofloxacin was useful for more serious infections, often caused by ceftazidime-resistant organisms.

Administration, Oral↗

Quinolone antibacterial agents for the treatment of genitourinary tract infections.

The fluoroquinolones have expanded the therapeutic options available for the treatment of genitourinary tract infections. Their ease of oral administration, favourable pharmacokinetics, low incidence of adverse reactions, and broad spectrum of in vitro activity against aerobic and facultative organisms make them especially suitable for treating bacteriuria, particularly when pathogens are resistant to other available oral agents. Their efficacy has also been established in the treatment of prostatis, gonorrhea and chancroid. They have lower in vitro activity against chlamydia, ureaplasma and anaerobes, and their role in the treatment of non-gonococcal urethritis, vaginitis and acute pelvic inflammatory disease is less well established.

4-Quinolones↗

Comparative in vitro activities of piperacillin-tazobactam and ticarcillin-clavulanate.

The in vitro activities of ticarcillin, piperacillin, clavulanic acid, tazobactam, ticarcillin-clavulanate, and piperacillin-tazobactam against 819 bacterial isolates were compared. The two beta-lactamase inhibitors, clavulanic acid and tazobactam, had little useful antibacterial activity but enhanced the activities of the penicillins against beta-lactamase-producing strains of Haemophilus influenzae, Branhamella catarrhalis, and methicillin-susceptible Staphylococcus aureus; all strains were susceptible to both combinations. Both enzyme inhibitors also enhanced the activities of the penicillins against most strains of Escherichia coli, Klebsiella spp., Citrobacter diversus, Proteus spp., Providencia spp., and Bacteroides spp. and against occasional strains of Citrobacter freundii, Enterobacter spp., and Serratia marcescens. Clavulanic acid frequently enhanced the activity of ticarcillin against Xanthomonas maltophilia, and tazobactam frequently enhanced the activity of piperacillin against Morganella morganii. Enhancement was observed primarily with strains relatively resistant to the penicillins. In general, clavulanic acid was more effective than tazobactam in enhancing penicillin activity against Klebsiella spp., C. diversus, X. maltophilia, and Bacteroides spp., whereas tazobactam was more effective against Escherichia coli and Proteeae. There was little or no enhancement of activity against Enterococcus faecalis, Aeromonas hydrophila, Pseudomonas aeruginosa, Pseudomonas cepacia, or Acinetobacter anitratus. Clavulanic acid occasionally antagonized the activity of ticarcillin against ticarcillin-susceptible members of the family Enterobacteriaceae, but those strains were still considered susceptible to the combination. Tazobactam never antagonized the activity of piperacillin. In a direct comparison of the activities of ticarcillin-clavulanate and piperacillin-tazobactam, the two were equally active against H. influenzae, B. catarrhalis, and S. aureus; the latter was more active against E. faecalis. For relatively susceptible strains of members of the family Enterobacteriaceae, neither combination was predictably more active than the other, but relatively resistant strains were generally more susceptible to piperacillin-tazobactam. Piperacillin-tazobactam was more active than ticarcillin-clavulanate against A. hydrophila, P. aeruginosa, and P. cepacia, similar in activity against A. anitratus, and less active against X. maltophilia and Bacteroides spp.

Anti-Bacterial Agents↗

In vitro activity of U-76,252 (CS-807), a new oral cephalosporin.

U-76,252 is the prodrug of U-76,253. MICs of U-76,253 were 0.015 to 0.06 microgram/ml for greater than or equal to 90% of the strains of Streptococcus spp., Haemophilus influenzae, and Proteus mirabilis; 0.25 to 1 microgram/ml for Branhamella catarrhalis, Escherichia coli, Klebsiella spp., and Citrobacter diversus; 1 to 8 micrograms/ml for Staphylococcus spp.; and 2 to greater than 16 micrograms/ml for other members of the family Enterobacteriaceae and Aeromonas hydrophila; for 72% of the latter group, MICs were less than or equal to 4 micrograms/ml. MICs for Pseudomonas aeruginosa and Enterococcus faecalis were greater than 16 micrograms/ml.

Bacteria↗

In vitro activity of cefixime, a new oral cephalosporin.

The in vitro activities of cefixime and seven comparative oral antimicrobials were studied. MIC90S of cefixime were 0.015-1 micrograms/ml for Haemophilus influenzae, Branhamella catarrhalis, Escherichia coli, Klebsiella, Citrobacter diversus, Proteus, Providencia, Aeromonas hydrophila and Streptococcus. MIC90S for other Enterobacteriaceae were greater than or equal to 2 micrograms/ml; 44% of those strains were inhibited by less than or equal 1 microgram/ml. Staphylococcus, Psuedomonas aeruginosa and Enterococcus faecalis were resistant to cefixime.

Administration, Oral↗

Efficacy and safety of oral ciprofloxacin in the treatment of serious respiratory infections.

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.

Administration, Oral↗

In vitro activity of RO 23-6240 (AM-833): a new fluoroquinolone.

The in vitro activities of RO 23-6240 (AM-833) and four comparative fluoroquinolones were studied. Minimal inhibitory concentrations (MICs) of RO 23-6240, which inhibited at least 90% of strains, were less than or equal to 0.03-1 microgram/ml for Staphylococcus aureus, Staphylococcus epidermidis, Enterobacteriaceae, Acinetobacter anitratus Aeromonas hydrophila, Branhamella catarrhalis, and Haemophilus influenzae, 2-8 micrograms/ml for Staphylococcus saprophyticus, streptococci, diphtheroids, and Pseudomonas spp., and 1-32 micrograms/ml for anaerobic species. MICs of ofloxacin, pefloxacin, norfloxacin, and ciprofloxacin paralleled those of RO 23-6240. With all five drugs, MICs were minimally affected by inoculum size and minimal bacterial concentrations (MBCs) were always within two dilution steps (log2) of MICs.

Anti-Bacterial Agents↗

Platelet-mediated bleeding caused by broad-spectrum penicillins.

One hundred fifty-six hospitalized adult patients treated with ticarcillin, piperacillin, mezlocillin, or cefotaxime (control) were prospectively observed for determination of frequencies of platelet dysfunction and bleeding. Increases in bleeding times (greater than or equal to 5 min above pretreatment values) occurred in 73% of patients receiving ticarcillin, 43% receiving piperacillin, 25% receiving mezlocillin, and 17% receiving cefotaxime (P less than .0001); chemotherapy, thrombocytopenia, age of greater than or equal to 60 years, dose of greater than or equal to 12 g per day, and duration of treatment of six or more days were significant covariables. Significant bleeding occurred in 34% of patients treated with ticarcillin, 17% with piperacillin, 2% with mezlocillin, and 5% with cefotaxime (P = .0005); chemotherapy, thrombocytopenia, primary marrow disorders affecting platelet function, prolonged prothrombin time, and azotemia were significant covariables. Bleeding was associated with an elevated pretreatment bleeding time, an increase in bleeding time during treatment, and the maximal observed bleeding time during treatment (P less than .0001).

Adult↗

In vitro antistaphylococcal activity of pefloxacin alone and in combination with other antistaphylococcal drugs.

MICs of pefloxacin and nine antistaphylococcal drugs were determined for 200 isolates of Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, and Staphylococcus saprophyticus. All the strains were susceptible to pefloxacin, vancomycin, and rifampin. Oxacillin-resistant strains were uniformly resistant to cephalothin and were more likely to be resistant to gentamicin, erythromycin, clindamycin, doxycycline, and trimethoprim-sulfamethoxazole than were oxacillin-susceptible strains. Time-kill studies with 23 strains of S. aureus, S. epidermidis, and S. haemolyticus indicated that the relative order of bactericidal activities was gentamicin greater than or equal to pefloxacin greater than oxacillin greater than vancomycin greater than rifampin. Pefloxacin combined with oxacillin or vancomycin killed staphylococci more rapidly than oxacillin or vancomycin alone but less rapidly than pefloxacin alone. Gentamicin combined with oxacillin, vancomycin, or pefloxacin resulted in the most rapid killing of gentamicin-susceptible strains. Rifampin combined with oxacillin, vancomycin, or pefloxacin reduced the bactericidal activities of those drugs, but rifampin resistance was not observed as it was with rifampin alone. Pefloxacin is a potentially useful antistaphylococcal agent.

Anti-Bacterial Agents↗

Efficacy and safety of oral ciprofloxacin for treatment of serious urinary tract infections.

Eighty-three patients with serious urinary tract infections were treated with oral ciprofloxacin. Of these patients, 79 were hospitalized, and 41 had known structural or neurologic abnormalities of the urinary tract. The most common pathogens were members of the family Enterobacteriaceae (MICs, less than or equal to 0.06 microgram/ml), Pseudomonas aeruginosa (MICs, 0.13 to 2 micrograms/ml), and Enterococcus faecalis (MICs, 0.5 to 2 micrograms/ml). Sixty-eight patients were able to be evaluated for determining efficacy; all responded symptomatically, and all urinary pathogens were eradicated on days 3 to 5 of treatment. Five patients, who were treated for a relatively short duration (2 to 10 days), relapsed 5 to 9 days posttreatment. Six patients became colonized with yeasts during treatment, and seven patients developed bacterial reinfections 5 to 9 days posttreatment. All patients whose infections relapsed or who developed infections with new organisms had neurogenic bladders, structural abnormalities of the genitourinary tract, or urinary catheters. There was no instance of bacteria developing resistance during treatment. Ciprofloxacin probably caused nausea with or without vomiting in 7 of the 83 patients, headache in 3 patients, and mild elevation of hepatic enzymes in 2 patients; other adverse reactions were observed but were probably not drug related. Oral ciprofloxacin was effective and safe for the treatment of serious urinary tract infections caused by a variety of bacterial pathogens.

Administration, Oral↗

In vitro activity of cefpiramide (SM-1652) against gram-negative bacilli.

The susceptibilities of 317 gram-negative bacilli to cefpiramide, cefotaxime, and piperacillin were determined by standardized microdilution and disk diffusion tests. Cefpiramide and piperacillin were more consistently active against nonfermenters than against Enterobacteriaceae, whereas cefotaxime was more active against Enterobacteriaceae. Inhibitory zone diameters of approximately 75-micrograms cefpiramide disks correlated well with minimal inhibitory concentrations (r = 0.85); breakpoints for defining susceptibility and resistance were recommended.

Cefotaxime↗

Treatment of skin and soft tissue infections with oral ciprofloxacin.

Thirty adult patients with severe skin and soft tissue infections (four with contiguous osteomyelitis) caused by a variety of bacterial pathogens were treated with oral ciprofloxacin. Favourable clinical responses were observed in 23 (92%) of the 25 evaluable cases. All Enterobacteriaceae and anaerobic bacteria were eradicated during treatment. Enterococci, Staphylococcus aureus, and Pseudomonas aeruginosa were usually eradicated but occasional strains persisted during treatment. Strains that persisted during treatment were associated with therapeutic failure in two cases, one with contiguous osteomyelitis and one with vascular gangrene. The only significant adverse reaction observed was nausea and/or vomiting in five of the 30 patients.

Adolescent↗

In vitro activities of Ro 19-5247 and Ro 15-8074, new oral cephalosporins.

The in vitro activities of two new oral cephalosporins, Ro 19-5247 and Ro 15-8074, were compared with the in vitro activities of cefuroxime, cefaclor, amoxicillin-clavulanate, trimethoprim-sulfamethoxazole (TMP-SMZ), and doxycycline against a variety of bacterial species. MIC50s (MICs required to inhibit 50% of strains) of Ro 19-5247 were less than or equal to 0.13 micrograms/ml for streptococci (except Streptococcus faecalis) and Haemophilus influenzae; 0.25 to 2 micrograms/ml for most strains of Enterobacteriaceae, Aeromonas hydrophila, Branhamella catarrhalis, and gram-positive anaerobic bacteria; and 1 to 8 micrograms/ml for methicillin-susceptible staphylococci. MIC50s of Ro 15-8074 were similar to those of Ro 19-5247, except that gram-positive aerobes and anaerobes were less susceptible. Both Ro 19-5247 and Ro 15-8074 had greater in vitro activity against strains of Enterobacteriaceae than did comparative beta-lactams and doxycycline; TMP-SMZ had the broadest spectrum of activity against these organisms. None of the cephalosporins were active against methicillin-resistant staphylococci, S. faecalis, most nonfermenters, or Bacteroides sp. Inoculum size variations affected MICs in a species-dependent manner for beta-lactams and unpredictably for TMP-SMZ but had little effect for doxycycline. Bactericidal activity was consistent with beta-lactams, inconsistent with TMP-SMZ, and uncommon with doxycycline.

Anti-Bacterial Agents↗

In vitro susceptibilities of four species of coagulase-negative staphylococci.

The in vitro susceptibilities of 260 strains of coagulase-negative staphylococci to penicillin G, oxacillin, nafcillin, methicillin, cephalothin, and seven non-beta-lactam antimicrobial agents were determined and compared with the susceptibilities of 54 strains of Staphylococcus aureus with known patterns of susceptibility. Penicillin G susceptibility for S. aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, and Staphylococcus hominis was readily determined by using beta-lactamase tests with induced cells and with a standardized microdilution test. MIC criteria for susceptibility used for S. aureus were applicable to the coagulase-negative species. Percentages of organisms susceptible were as follows: S. epidermidis, 7%; S. haemolyticus, 5%; and S. hominis, 47%. Oxacillin susceptibility for these four species was readily determined by using a modification of the microdilution test. MIC criteria for susceptibility used for S. aureus were applicable to S. haemolyticus and S. hominis, but alternate criteria were necessary for S. epidermidis. Percentages of organisms susceptible were as follows: S. epidermidis, 29%; S. haemolyticus, 36%; and S. hominis, 97%. Staphylococcus saprophyticus differed from the other staphylococcal species; all strains were beta-lactamase negative and were penicillin susceptible but had higher penicillin G MICs than did susceptible strains of the other species. There was total cross resistance among the penicillinase-resistant penicillins and cephalothin for the coagulase-negative staphylococci as well as for S. aureus; oxacillin MICs were more reliable than MICs of the other drugs or a standardized disk diffusion test for distinguishing resistant from susceptible strains. Vancomycin, rifampin, and ciprofloxacin were consistently active against all staphylococci. Erythromycin, clindamycin, gentamicin, and trimethoprim-sulfamethoxazole were more active against oxacillin-susceptible staphylococci than against oxacillin-resistant staphylococci.

Anti-Bacterial Agents↗

In vitro activity of LY146032 against staphylococci, streptococci, and enterococci.

The in vitro activities of LY146032 and seven comparative antimicrobial agents against 14 species of staphylococci, streptococci, and enterococci were studied. MICs of LY146032 were less than or equal to 0.5 microgram/ml for all staphylococci, including oxacillin-resistant strains; less than or equal to 0.25 microgram/ml for all streptococci (except viridans group streptococci); and less than or equal to 4 micrograms/ml for all viridans group streptococci and enterococci. MICs were minimally affected by variations in inoculum size, and LY146032 was bactericidal against all species tested.

Anti-Bacterial Agents↗