The Experts below are selected from a list of 1020 Experts worldwide ranked by ideXlab platform
Michael N. Dudley - One of the best experts on this subject based on the ideXlab platform.
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in vitro postantibiotic effect following repeated exposure to imipenem Temafloxacin and tobramycin
Antimicrobial Agents and Chemotherapy, 1993Co-Authors: B J Mcgrath, C R Marchbanks, Deborah Gilbert, Michael N. DudleyAbstract:The postantibiotic effect (PAE) following three consecutive 2-h exposures to imipenem, Temafloxacin, and tobramycin was determined in Pseudomonas aeruginosa. A PAE and a bactericidal effect were consistently observed for imipenem following each cycle of drug exposure and regrowth. In contrast, the PAE increased with repeated exposure with Temafloxacin (1.8 to > 5 h), but disappeared with tobramycin by the third exposure (0.9 to 0 h). These data show that the in vitro PAE may change within a strain following multiple cycles of drug exposure and bacterial regrowth.
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in vitro postantibiotic effect following repeated exposure to imipenem Temafloxacin and tobramycin
Antimicrobial Agents and Chemotherapy, 1993Co-Authors: B J Mcgrath, C R Marchbanks, Deborah Gilbert, Michael N. DudleyAbstract:The postantibiotic effect (PAE) following three consecutive 2-h exposures to imipenem, Temafloxacin, and tobramycin was determined in Pseudomonas aeruginosa. A PAE and a bactericidal effect were consistently observed for imipenem following each cycle of drug exposure and regrowth. In contrast, the PAE increased with repeated exposure with Temafloxacin (1.8 to > 5 h), but disappeared with tobramycin by the third exposure (0.9 to 0 h). These data show that the in vitro PAE may change within a strain following multiple cycles of drug exposure and bacterial regrowth.
F Sörgel - One of the best experts on this subject based on the ideXlab platform.
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Hepatobiliary Elimination of Temafloxacin
Clinical Pharmacokinetics, 1992Co-Authors: F Sörgel, G R Granneman, G. Mahr, P. Kujath, W. Fabian, P. NickelAbstract:The biliary excretion of Temafloxacin and Temafloxacin glucuronide was characterised in this study after administration of a single oral Temafloxacin 600mg dose to 8 patients with T-tube drainage of the common bile duct inserted after cholecystectomy or choledochotomy. High performance liquid Chromatographic analyses of plasma, urine and bile samples collected during the 72h after Temafloxacin administration showed that biliary concentrations of unchanged Temafloxacin followed a time-course parallel to plasma concentrations but were 5- to 10-fold higher. Biliary Temafloxacin peak concentrations ranged from 18.74 to 64.35 mg/L and time to peak concentrations from 0.71 to 10.23h. Mean hepatobiliary clearance of Temafloxacin was 3.10 ml/min (0.19 L/h) when calculated for the unchanged drug and 1.43 ml/min (0.09 L/h) when calculated for its biliary excretion as glucuronic acid conjugates. Patients with higher bile production had markedly higher clearance of both Temafloxacin and Temafloxacin glucuronide. The elimination time-course of the conjugate in bile generally paralleled those of Temafloxacin in bile and plasma, although there was a lag in the rate of appearance of the conjugate in bile. Biliary excretion of unchanged Temafloxacin and Temafloxacin glucuronide accounted for approximately 2.2 and 1% of the administered dose, respectively. Thus, it appears that hepatobiliary elimination of Temafloxacin and its glucuronide acid accounts for only a small fraction of total Temafloxacin clearance. Nonetheless, concentrations attained in the bile are far above the minimum inhibitory concentration values of pathogens relevant in biliary tract infections.
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Pharmacokinetics of Temafloxacin in Patients with Liver Impairment
Clinical Pharmacokinetics, 1992Co-Authors: G R Granneman, G. Mahr, W. Fabian, P. Nickel, C. Locke, W. Kirch, M. Kinzig, K. G. Naber, F SörgelAbstract:A multicentre study was conducted to determine whether liver impairment would alter the pharmacokinetics of Temafloxacin, a new fluoroquinolone antimicrobial agent. 16 patients with cirrhosis and 12 healthy volunteers (the control group) received a single oral 600mg dose of Temafloxacin. Blood and urine were sampled at frequent intervals after drug administration and assayed by high performance liquid chromatography. The mean age of patients with liver impairment was greater than that of the control group; they also had a lower creatinine clearance and urine output. There was no difference between the groups in either the peak plasma Temafloxacin concentration or the time to reach peak concentration. However, the volume of distribution and elimination rate constant of Temafloxacin were significantly lower in the group with liver impairment, as were total Temafloxacin clearance, renal clearance, and the ratio of renal: creatinine clearance. Nonrenal clearance was similar in patients and controls. Creatinine clearance and urine output were found to account for most of the intersubject variability in total clearance as determined by multiple linear regression analysis. Because the altered Temafloxacin pharmacokinetics appear to be primarily due to impaired renal function, this should be the main determinant of Temafloxacin dosage in patients with liver disease.
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Effect of antacid medication on the pharmacokinetics of Temafloxacin.
Clinical pharmacokinetics, 1992Co-Authors: G R Granneman, U Stephan, B Birner, F Sörgel, D MukherjeeAbstract:The effect of an antacid drug (Maalox 70) on the pharmacokinetics of Temafloxacin was studied in 12 healthy young volunteers. The study was designed as a randomised open 2-period crossover trial in which Temafloxacin was administered alone and with Maalox 70. In both treatments, Temafloxacin was administered as a single oral 400mg dose on the morning of day 2. In the antacid regimen, 8 doses of Maalox 70 were administered every 2h on day 1, starting at 8am and ending with the last dose at 10pm; 5 doses were given on day 2, at 2.5 and 1h before administration of Temafloxacin and 1, 3 and 5h after the Temafloxacin dose. With coadministration of Maalox 70, peak plasma Temafloxacin concentrations (Cmax) were reduced to 44.6% (+/- 24.5), and AUC(0-infinity) was reduced to 39.8% (+/- 17.4) of the corresponding values obtained when Temafloxacin was given alone. Urinary excretion of Temafloxacin was reduced to 46.0% (+/- 13.7) of that observed when Temafloxacin was administered alone. Time to peak plasma concentration (tmax = 1.8h) was not affected by antacid administration. Comparable or greater antacid-associated reductions in relative bioavailability have been reported for other quinolones. As with other quinolones, the concurrent administration of Temafloxacin and antacids should be avoided.
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Hepatobiliary Elimination of Temafloxacin
Clinical Pharmacokinectics, 1992Co-Authors: F Sörgel, G R Granneman, G. Mahr, P. Kujath, W. Fabian, P. NickelAbstract:The biliary excretion of Temafloxacin and Temafloxacin glucuronide was characterised in this study after administration of a single oral Temafloxacin 600mg dose to 8 patients with T-tube drainage of the common bile duct inserted after cholecystectomy or choledochotomy.
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Penetration of Temafloxacin into body tissues and fluids.
Clinical Pharmacokinectics, 1992Co-Authors: F SörgelAbstract:The new fluoroquinolone antimicrobial Temafloxacin shows good penetration into a range of body tissues and fluids, after single or repeated oral administration to healthy volunteers and patients undergoing various procedures. Temafloxacin concentrations in respiratory tissues and fluids, nasal secretions, tonsils, prostate, semen, bone and blister fluid were similar to, or greater than, concurrent serum concentrations. Penetration into sinus secretions and cerebrospinal fluid is less marked; nevertheless, Temafloxacin concentrations of approximately 2.4 and 1 mg/L, respectively, were achieved. Concentrations of Temafloxacin observed in these tissues and fluids exceed the minimum concentrations required to eradicate the majority of bacterial pathogens associated with respiratory infections, tonsillitis, sinusitis, prostatitis, bone infections and meningitis. Since elimination of Temafloxacin occurs by the renal route, high concentrations of the drug are also found in the urine. Biliary excretion of Temafloxacin accounts for about 3% and leads to high biliary concentrations of the drug.
G R Granneman - One of the best experts on this subject based on the ideXlab platform.
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Hepatobiliary Elimination of Temafloxacin
Clinical Pharmacokinetics, 1992Co-Authors: F Sörgel, G R Granneman, G. Mahr, P. Kujath, W. Fabian, P. NickelAbstract:The biliary excretion of Temafloxacin and Temafloxacin glucuronide was characterised in this study after administration of a single oral Temafloxacin 600mg dose to 8 patients with T-tube drainage of the common bile duct inserted after cholecystectomy or choledochotomy. High performance liquid Chromatographic analyses of plasma, urine and bile samples collected during the 72h after Temafloxacin administration showed that biliary concentrations of unchanged Temafloxacin followed a time-course parallel to plasma concentrations but were 5- to 10-fold higher. Biliary Temafloxacin peak concentrations ranged from 18.74 to 64.35 mg/L and time to peak concentrations from 0.71 to 10.23h. Mean hepatobiliary clearance of Temafloxacin was 3.10 ml/min (0.19 L/h) when calculated for the unchanged drug and 1.43 ml/min (0.09 L/h) when calculated for its biliary excretion as glucuronic acid conjugates. Patients with higher bile production had markedly higher clearance of both Temafloxacin and Temafloxacin glucuronide. The elimination time-course of the conjugate in bile generally paralleled those of Temafloxacin in bile and plasma, although there was a lag in the rate of appearance of the conjugate in bile. Biliary excretion of unchanged Temafloxacin and Temafloxacin glucuronide accounted for approximately 2.2 and 1% of the administered dose, respectively. Thus, it appears that hepatobiliary elimination of Temafloxacin and its glucuronide acid accounts for only a small fraction of total Temafloxacin clearance. Nonetheless, concentrations attained in the bile are far above the minimum inhibitory concentration values of pathogens relevant in biliary tract infections.
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Pharmacokinetics of Temafloxacin in Patients with Liver Impairment
Clinical Pharmacokinetics, 1992Co-Authors: G R Granneman, G. Mahr, W. Fabian, P. Nickel, C. Locke, W. Kirch, M. Kinzig, K. G. Naber, F SörgelAbstract:A multicentre study was conducted to determine whether liver impairment would alter the pharmacokinetics of Temafloxacin, a new fluoroquinolone antimicrobial agent. 16 patients with cirrhosis and 12 healthy volunteers (the control group) received a single oral 600mg dose of Temafloxacin. Blood and urine were sampled at frequent intervals after drug administration and assayed by high performance liquid chromatography. The mean age of patients with liver impairment was greater than that of the control group; they also had a lower creatinine clearance and urine output. There was no difference between the groups in either the peak plasma Temafloxacin concentration or the time to reach peak concentration. However, the volume of distribution and elimination rate constant of Temafloxacin were significantly lower in the group with liver impairment, as were total Temafloxacin clearance, renal clearance, and the ratio of renal: creatinine clearance. Nonrenal clearance was similar in patients and controls. Creatinine clearance and urine output were found to account for most of the intersubject variability in total clearance as determined by multiple linear regression analysis. Because the altered Temafloxacin pharmacokinetics appear to be primarily due to impaired renal function, this should be the main determinant of Temafloxacin dosage in patients with liver disease.
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Pharmacokinetics of Temafloxacin in humans after multiple oral doses.
Antimicrobial Agents and Chemotherapy, 1992Co-Authors: G R Granneman, P Carpentier, P J Morrison, A G PernetAbstract:The multiple-dose pharmacokinetics and tolerance of Temafloxacin, a new fluoroquinolone antibacterial agent, were evaluated in healthy volunteers. Temafloxacin was found to be well tolerated when administered orally every 12 h for 7 days at doses of 100, 200, 300, 400, 600, and 800 mg. Steady-state maximum and minimum concentrations in plasma were proportional to dose, averaging slightly over 1.0 and 0.5 microgram/ml/100 mg administered. Analyses of variance found no significant differences among the dosage groups in total apparent clearances (CLT/F), renal clearances (CLR), or nonrenal clearances, which averaged 197, 119, and 78 ml/min, respectively. The half-life increased slightly with dose, averaging 8.4 h overall. The extent of absorption of Temafloxacin was quite reproducible, with day-to-day intrasubject variability in minima averaging under 10%. Renal glomerular filtration of unbound drug was the dominant elimination process; however, tubular secretion and reabsorption also appear to occur. Secretion was estimated to account for about 12% of CLT/F during a regimen of 600 mg every 12 h. CLR was relatively constant for urine flow rates above 1 ml/min, but reabsorption appeared to occur under low-flow conditions, resulting in day-versus-night differences in CLR. Intersubject variability in CLT/F over the eightfold range in dosage was only 20%, and 60% of this variance was accounted for by differences in body surface area (or lean body mass), concentration in plasma, and urine flow rate. Overall, it appears that the pharmacokinetics of Temafloxacin are essentially linear, reproducible within a subject, and predictable among subjects.
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Effect of antacid medication on the pharmacokinetics of Temafloxacin.
Clinical pharmacokinetics, 1992Co-Authors: G R Granneman, U Stephan, B Birner, F Sörgel, D MukherjeeAbstract:The effect of an antacid drug (Maalox 70) on the pharmacokinetics of Temafloxacin was studied in 12 healthy young volunteers. The study was designed as a randomised open 2-period crossover trial in which Temafloxacin was administered alone and with Maalox 70. In both treatments, Temafloxacin was administered as a single oral 400mg dose on the morning of day 2. In the antacid regimen, 8 doses of Maalox 70 were administered every 2h on day 1, starting at 8am and ending with the last dose at 10pm; 5 doses were given on day 2, at 2.5 and 1h before administration of Temafloxacin and 1, 3 and 5h after the Temafloxacin dose. With coadministration of Maalox 70, peak plasma Temafloxacin concentrations (Cmax) were reduced to 44.6% (+/- 24.5), and AUC(0-infinity) was reduced to 39.8% (+/- 17.4) of the corresponding values obtained when Temafloxacin was given alone. Urinary excretion of Temafloxacin was reduced to 46.0% (+/- 13.7) of that observed when Temafloxacin was administered alone. Time to peak plasma concentration (tmax = 1.8h) was not affected by antacid administration. Comparable or greater antacid-associated reductions in relative bioavailability have been reported for other quinolones. As with other quinolones, the concurrent administration of Temafloxacin and antacids should be avoided.
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The effect of food on the bioavailability of Temafloxacin. A review of 3 studies.
Clinical pharmacokinetics, 1992Co-Authors: G R Granneman, D MukherjeeAbstract:Temafloxacin is a new fluoroquinolone antibacterial agent. Previous pharmacokinetic studies have shown that the extent of absorption of Temafloxacin is independent of dose and that the dispositional pharmacokinetics are linear. The pharmacokinetics of 3 tablet formulations of Temafloxacin were investigated in phase I studies in healthy adult volunteers, to determine whether the bioavailability is altered by the presence of food. Results of these studies indicate that the absorption of Temafloxacin is slightly enhanced by concomitant administration of food. Thus, special coordination of Temafloxacin administration and meals appears to be unnecessary.
B J Mcgrath - One of the best experts on this subject based on the ideXlab platform.
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in vitro postantibiotic effect following repeated exposure to imipenem Temafloxacin and tobramycin
Antimicrobial Agents and Chemotherapy, 1993Co-Authors: B J Mcgrath, C R Marchbanks, Deborah Gilbert, Michael N. DudleyAbstract:The postantibiotic effect (PAE) following three consecutive 2-h exposures to imipenem, Temafloxacin, and tobramycin was determined in Pseudomonas aeruginosa. A PAE and a bactericidal effect were consistently observed for imipenem following each cycle of drug exposure and regrowth. In contrast, the PAE increased with repeated exposure with Temafloxacin (1.8 to > 5 h), but disappeared with tobramycin by the third exposure (0.9 to 0 h). These data show that the in vitro PAE may change within a strain following multiple cycles of drug exposure and bacterial regrowth.
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in vitro postantibiotic effect following repeated exposure to imipenem Temafloxacin and tobramycin
Antimicrobial Agents and Chemotherapy, 1993Co-Authors: B J Mcgrath, C R Marchbanks, Deborah Gilbert, Michael N. DudleyAbstract:The postantibiotic effect (PAE) following three consecutive 2-h exposures to imipenem, Temafloxacin, and tobramycin was determined in Pseudomonas aeruginosa. A PAE and a bactericidal effect were consistently observed for imipenem following each cycle of drug exposure and regrowth. In contrast, the PAE increased with repeated exposure with Temafloxacin (1.8 to > 5 h), but disappeared with tobramycin by the third exposure (0.9 to 0 h). These data show that the in vitro PAE may change within a strain following multiple cycles of drug exposure and bacterial regrowth.
William J. Mogabgab - One of the best experts on this subject based on the ideXlab platform.
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Single-dose oral Temafloxacin versus parenteral ceftriaxone in the treatment of gonococcal urethritis/cervicitis.
The American journal of medicine, 1991Co-Authors: William J. MogabgabAbstract:Temafloxacin is an oral fluoroquinolone with potent in vitro activity against Neisseria gonorrhoeae. The efficacy and safety of a single dose of Temafloxacin were compared with ceftriaxone, the current treatment of choice for gonorrhea, in a randomized, multicenter study. A total of 421 patients with uncomplicated gonococcal urethritis or cervicitis were randomly assigned to receive a single oral dose of Temafloxacin 200 mg (n = 63) or 400 mg (n = 175), or a single intramuscular injection of ceftriaxone 250 mg (n = 183). In evaluable patients, bacteriologic cure rates were greater than 99% for both Temafloxacin and ceftriaxone recipients. Corresponding clinical cure rates were 93.6% and 94.6%, respectively. Both regimens were well tolerated. A single oral dose of Temafloxacin appears to be as safe and effective as injectable ceftriaxone in the treatment of uncomplicated gonococcal urethritis or cervicitis.
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single dose oral Temafloxacin versus parenteral ceftriaxone in the treatment of gonococcal urethritis cervicitis
The American Journal of Medicine, 1991Co-Authors: William J. MogabgabAbstract:Abstract Temafloxacin is an oral fluoroquinolone with potent in vitro activity against Neisseria gonorrhoeae . The efficacy and safety of a single dose of Temafloxacin were compared with ceftriaxone, the current treatment of choice for gonorrhea, in a randomized, multicenter study. A total of 421 patients with uncomplicated gonococcal urethritis or cervicitis were randomly assigned to receive a single oral dose of Temafloxacin 200 mg (n = 63) or 400 mg (n = 175), or a single intramuscular injection of ceftriaxone 250 mg (n = 183). In evaluable patients, bacteriologic cure rates were >99% for both Temafloxacin and ceftriaxone recipients. Corresponding clinical cure rates were 93.6% and 94.6%, respectively. Both regimens were well tolerated. A single oral dose of Temafloxacin appears to be as safe and effective as injectable ceftriaxone in the treatment of uncomplicated gonococcal urethritis or cervicitis.
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Single-dose oral Temafloxacin versus parenteral ceftriaxone in the treatment of gonococcal urethritis/cervicitis.
The American Journal of Medicine, 1991Co-Authors: William J. MogabgabAbstract:Abstract Temafloxacin is an oral fluoroquinolone with potent in vitro activity against Neisseria gonorrhoeae . The efficacy and safety of a single dose of Temafloxacin were compared with ceftriaxone, the current treatment of choice for gonorrhea, in a randomized, multicenter study. A total of 421 patients with uncomplicated gonococcal urethritis or cervicitis were randomly assigned to receive a single oral dose of Temafloxacin 200 mg (n = 63) or 400 mg (n = 175), or a single intramuscular injection of ceftriaxone 250 mg (n = 183). In evaluable patients, bacteriologic cure rates were >99% for both Temafloxacin and ceftriaxone recipients. Corresponding clinical cure rates were 93.6% and 94.6%, respectively. Both regimens were well tolerated. A single oral dose of Temafloxacin appears to be as safe and effective as injectable ceftriaxone in the treatment of uncomplicated gonococcal urethritis or cervicitis.
