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Biomedical subjects

J Guibert

Publications and source records attributed to J Guibert.

At least 55 records · Page 3Linked to original sources
PubMed1986

[Ofloxacin (RU 43280): clinical evaluation in urinary and prostatic infections].

Ofloxacin, a new fluoroquinolone, was given to fifty patients (29 females and 21 males) aged 25 to 86 years with urinary tract infection or prostatitis. Urinary tract infections usually chronic and associated with urologic anomalies, included 17 cases of cystitis and 19 cases of pyelonephritis. 14 patients had prostatitis. Pathogens recovered from the urine were 26 E. coli, 2 Citrobacter, 4 Proteus mirabilis, 2 Klebsiella, 2 Enterobacter, 3 Serratia, 3 Staphylococcus aureus and 11 Pseudomonas. Minimal inhibitory concentrations of ofloxacin ranged from 0.03 to 0.12 microgram/ml (mean MIC: 0.6 microgram/ml) for 27 nalidixic acid-sensitive strains, and from 0.25 to 4 micrograms/ml (mean MIC: 1 microgram/ml) for 26 nalidixic acid-resistant strains. Ofloxacin was given as single drug therapy in all patients, in a daily dosage of 200 mg b.i.d. in 46 patients and 400 mg b.i.d. in 4 patients, for 7 to 97 days (average 40 days). Follow-up after discontinuation of treatment was 3 to 12 months. Therapeutic results were as follows: 17 cures for the 17 cystitis patients, 17 cures and 2 failures by relapse for the 19 cases of pyelonephritis, and 11 cures, 1 failure by persistence of bacteriuria and failure by relapse for the 14 cases of prostatitis. Digestive disorders, i.e. nausea, abdominal pain, constipation, occurred in 6 patients and required withdrawal of the drug in 1; candidiasis of the tongue was recorded in one patient and digestive complaints with neuropsychic disorders in another. Two patients had short-lived, moderate leukopenia with granulopenia and one had transient worsening of preexisting renal failure. Hepatic tolerance was good.

Adult↗
PubMed1985

Pharmacokinetics of cefotiam in humans.

After intravenous bolus injections of 0.5, 1, and 2 g of cefotiam to three healthy volunteers, the mean (+/- standard deviation) total plasma clearances measured for each dose were, respectively, 26.8 +/- 2.7, 22.8 +/- 0.8, and 17.8 +/- 0.9 liters/h; the terminal elimination half-lives were 54.0 +/- 0.1, 68 +/- 15, and 98 +/- 36 min; and the renal clearances were 16.0 +/- 2.9, 13.3 +/- 1.4, and 11.3 +/- 2.6 liters/h. The 24-h urinary recovery was independent of the dose and averaged 53% of the dose. After intramuscular administration of 1 g of cefotiam to three healthy volunteers, a mean (+/- standard deviation) peak concentration of 16.6 +/- 5.1 micrograms/ml was reached at 0.75 to 1 h post dosing. The concurrent intramuscular administration of lidocaine and cefotiam did not modify the kinetics of cefotiam. During a constant-rate infusion, the steady-state plasma clearance decreased slightly when the infusion rate was increased. There was no trend towards accumulation of cefotiam in plasma during chronic treatment with 1 g intravenously every 12 h for 10 days.

Adult↗
PubMed1985

[Clinical evaluation of cefmenoxime in urinary tract and prostatic infections].

Cefmenoxime, a new cephalosporin, was given to fifty patients (28 male and 22 female) aged 15 to 86 years with infection of the urinary tract or prostate. Urinary tract infections, i.e. cystitis in 20 cases and pyelonephritis in 21, were usually chronic and associated with urologic anomalies. Nine patients had infection of the prostate. Pathogens recovered from the urine were 26 E. coli, 8 Klebsiella, 16 Serratia, 5 Proteus mirabilis or indole-positive Proteus, 1 Providencia, and 4 Pseudomonas. Minimal inhibitory concentrations of cefmenoxime ranged from 0.015 to 64 micrograms/ml (mean MIC: 0.12 micrograms/ml). Cefmenoxime was given as single drug therapy in all patients but one, in a daily dosage of 2 g divided into two intramuscular injections, for 3 to 28 days (average 22 days). Follow-up after discontinuation of treatment was four weeks. Therapeutic results were as follows: 13 successes and 7 failures by relapse for the 20 cystitis patients, 13 successes and 7 failures by relapse for the 20 interpretable cases of pyelonephritis, and 4 successes and 5 failures by relapse for the 9 patients with prostate infection. Local tolerance was excellent. Skin rash in 2 patients and diarrhea in 1 required withdrawal of the drug. Three other patients with diarrhea were able to continue treatment. Intolerance to ingestion of alcoholic beverages was reported by 10 patients. Hypereosinophilia was recorded in 2 cases and a transient mononucleosic reaction in one. No renal of hepatic side effects were documented.

Adolescent↗
PubMed1985

Single- and multiple-dose pharmacokinetics of lenampicillin (KBT-1585) in healthy human subjects: comparative studies with amoxicillin.

Lenampicillin (LAPC) is a novel prodrug of ampicillin (ABPC) which is under development by KANEBO Ltd. and TORII Pharmaceutical Co. The single- and multiple-dose pharmacokinetic studies were performed on six healthy male volunteers. Amoxicillin (AMPC) was used as control drug. The oral single-dose studies of LAPC (equivalent to 250 mg ANPC) and of AMPC (500 mg) demonstrated that the mean peak serum concentrations of ABPC and AMPC were 11.4 +/- 0.8 micrograms/ml at 40 min and 8.5 +/- 0.7 micrograms/ml at 50-90 min, respectively. The half-lives and the areas under the concentration-time curves were the same for both antibiotics on an equimolar basis. The oral multiple-dose studies of LAPC and AMPC (twice a day for 8 days with the same single dose as above) showed that no measurable accumulation and no remarkable variations between the single- and multiple-dose pharmacokinetics were observed. No adverse effects were recorded for any subject. LAPC proved to have unique pharmacokinetic properties as compared with AMPC and high safety, and its further development to clinical trials appears warranted.

Administration, Oral↗
PubMed1984

Pharmacokinetics and dosage adjustment of cefotiam in renal impaired patients.

The pharmacokinetics of cefotiam were investigated after intravenous administration of 1 g to 2 healthy volunteers with normal renal function and to 16 patients whose creatinine clearance ranged from 4.7 to 0.1 l/h (78 to 1.66 ml/min). The elimination half-life varied from 1.1 h in normal subjects to 13 h in patients and the total plasma clearance from 21 to 0.6 l/h (350 to 10 ml/min). The urinary recovery decreased from 62% of the dose in normal subjects to 1.1% in patients, and the renal clearance from 15 to 0.01 l/h (250 to 0.5 ml/min). Plasma and renal clearances of cefotiam correlated well with the creatinine clearance. The dosage schedule for cefotiam in patients with normal renal function can be used in the presence of renal failure when the creatinine clearance is equal to or greater than 1 l/h (16.6 ml/min). For patients whose creatinine clearance is less than 1 l/h, the dose must be decreased to 75% of that for a patient with normal renal function only when it is given every 6 or 8 h.

Adult↗
PubMed1984

Pharmacokinetics of cefotiam and cefsulodin after simultaneous administration to patients with impaired renal function.

The possible influence of the concomitant administration of cefotiam and cefsulodin on their respective pharmacokinetics was studied in 15 patients with renal insufficiency and 10 anuric patients. Linear relations were found between the clearance of creatinine and the total clearance, as well as the renal clearance, of each drug. These relations for each cephalosporin were not significantly different from previous results obtained after separate administration. In hemodialyzed patients, the two cephalosporins were readily eliminated from the blood after simultaneous administration: ca. 35% of the dose of cefotiam and 30% of the dose of cefsulodin was recovered in the dialysate over 5 h. These results suggest that the pharmacokinetics of the two drugs are not modified by their simultaneous administration and that the dosing schedule previously proposed for administration of the two cephalosporins alone in the presence of renal insufficiency can be applied without modification when they are given together. Patients on hemodialysis should receive a loading dose after each dialysis period, and then reduced doses according to recommendations for anuric patients.

Adult↗
PubMed1984

[Clinical evaluation of azthreonam in severe urinary tract infections].

Azthreonam, the first monobactam, was given to 40 patients with urinary tract infection. Patients included 27 females, aged 17 to 77 years. UTI was complicated cystitis in 10 patients, pyelonephritis in 11, and prostatitis in 19. The following bacteria were recovered from urine: 12 E. coli, 1 Levinea , 3 Proteus mirabilis, 7 Klebsiella, 14 Serratia and 14 Pseudomonas. MICs of azthreonam ranged from 0.0035 to 16 micrograms/ml (mean 0.12 microgram/ml). Azthreonam was given intramuscularly, as monotherapy, in a daily dosage of 2 g, in two divided doses, for 10 to 29 days (mean: 28 days). Follow-up was at least 4 weeks after completion of treatment. Therapeutic results were as follows: 8 cures and 2 failures by relapse in 10 cystitis , 6 cures and 5 failures by relapse in 11 pyelonephritis , and 12 cures and 7 failures by relapse in 19 prostatitis . General and local tolerance were excellent. There were no hematologic or renal side effects. Transaminases SGOT and especially SGPT increased transiently in 7 patients and returned to normal after treatment was discontinued; premature withdrawal was needed in only one case.

Adolescent↗
PubMed1983

Pharmacokinetics of single intravenous and intramuscular doses of cefotetan in normal human volunteers.

The pharmacokinetic parameters of cefotetan were determined in six healthy adults after intramuscular (im) and intravenous (iv) administration of a single dose. After an iv bolus injection of 1 g cefotetan the mean peak serum level was 179.6 mg/l (S.E.M. +/- 14.2 mg/l) at 2 min. The apparent volume of distribution was 10.29 l (S.E.M. +/- 0.66 l). After im injections of 500 mg and 1 g of cefotetan the mean peak levels were 35 mg/l (S.E.M. +/- 1.6 mg/l) and 74 mg/l (S.E.M. +/- 3.6 mg/l) at 82 and 97 min respectively; the level at 12 h was 4.5 mg/l after 500 mg and 10.4 mg/l after 1 g. Cefotetan was slowly eliminated. The serum half-life was about 3.1 h after 1 g iv injection and varied from 3.4 to 3.7 h after the 500 mg and 1 g im injections. About 75% of the dose was excreted in the urine during the first 24 h after 1 g iv bolus injection; after 500 mg and 1 g im injection 60 to 65% of the dose was recovered in the urine during the same time period.

Adult↗
PubMed1982

Pharmacokinetics of cefroxadin (CGP 9000) in man.

The pharmacokinetics of cefroxadin have been studied after the administration of single oral and intravenous doses to healthy volunteers. Cefroxadin was assayed by HPLC. The kinetics in plasma following i.v. administration were described by using a three-compartment model. An additional disposition phase was observed following oral administration that could not be detected after the low i.v. dose. The terminal half-life was 1.03 h. The apparent volume of distribution at the steady state was consistent with a diffusion of the antibiotic in all extracellular fluids. The AUC after oral administration was linearly related to the dose. The urinary excretion amounted to 95% of the dose with virtually complete absorption of orally administered drug.

Administration, Oral↗
PubMed1982

[Clinical evaluation of cefotiam in adults urinary tract infections (author's transl)].

Cefotiam, a new broad-spectrum cephalosporin was used for the treatment of 30 cases of urinary-tract infections (UTI). Patients, 20 females, 10 males were between 23 and 76 years old. UTI were 17 cystitis, 9 pyelonephritis and 4 prostatitis. Bacteria isolated from urine were : 24 E. Coli, 3 Proteus mirabilis, 1 Providencia, 3 Klebsiella, 3 Enterobacter, 2 Serratia, 1 Staphylococcus coagulase--, DNAse--. MIC's of cefotiam ranged from 0.003 to 32 micrograms/ml (median MIC : 0.06 microgram/ml). Cefotiam was given intramuscularly in monotherapy, at the daily dosage of 1 and 2 g in two injections during 7 to 28 days. Followup of patients were at least 4 weeks after the end of treatment. Therapeutic results were : 15 cures and 2 failures by relapse in 17 cystitis, 6 cures and 3 failures by relapse in 9 pyelonephritis, 4 cures in 4 prostatitis. General tolerance was excellent in all cases. Intramusculary injections were well tolerated with a 2 p. cent lidocain solution. Biological tolerance and particularly renal tolerance was good in all patients.

Adult↗
PubMed1981

[Kinetics of cefotaxime in healthy subjects (author's transl)].

Serum and urinary levels of cefotaxime after either intramuscular (i.m.) or intravenous (i.v.) administration were determined in 6 normal human subjects. By the i.m. route the serum half-life was 80 minutes. The peak serum concentration, at 30 minutes, reached 12 and 24 mcg/ml after injection of 500 mg and 1 g. Concentrations in the urine were 500 mcg/ml within 6 hours after an injection of 500 mg; they reached 1000 mcg/ml after an injection of 1 g. Urinary elimination amounted to 50% during the first 6 hours; it reached 60% during 24 hours. By the i.v. route, the serum half-life was 40 minutes. The concentration in the serum was more than 100 mcg/ml at the fifth minute after an injection of 1 g. Concentrations in the urine were 1300 mcg/ml within 4 hours after injection of cefotaxime. The urinary elimination amounted to 60--64% during 12 hours. Intravenous infusion of 1 g during 4 hours gave a serum level, from the second hour, approaching 15 mcg/ml. The concentration in the urine was 600 mcg/ml within 4 hours. The urinary elimination amounted to 50% in 12 hours. Protein binding of cefotaxime ranged from 36 to 38%.

Adult↗
PubMed1981

[Clinical evaluation of cefotaxime at various dosage levels in urinary tract infections (author's transl)].

In this study, 63 patients with various urinary tract infections were treated with cefotaxime in different dosages. They were aged from 10 to 82 years (mean: 59). The cases included 33 cystitis, 25 pyelonephritis, 4 chronic prostatitis and 1 orchiepididymitis. 85 strains of enterobacteria were identified: 20 E. coli, 2 Citrobacter freundi, 5 Proteus mirabilis, 12 indole positive Proteus, 1 Providentia, 11 Klebsiella, 3 Enterobacter cloacae and 31 Serratia marescens and liquefaciens. 80 of these strains had MIC less than or equal to 1 mcg/ml (median: 0,12 mcg/ml). More than 2/3 of the patients were treated with a daily dose of 1.50 to 2 g, and 52 (median: 0.12 mcg/ml). More than 2/3 of the patients results showed 43 cures (9 of these with reinfection) and 20 relapses. Isolated enterobacteria strains were sensitive to cefotaxime in patients with recurrence. Relapses were due to underlying urological pathology. Among reinfection organisms, only one, an Enterobacter cloacae, was resistant to cefotaxime. The clinical, local, systemic and biological tolerance was good. Cefotaxime has been very effective in the treatment of severe urinary tract infections, especially in chronic pyelonephritis and cystitis, at an average daily dose of 2 g.

Adolescent↗
PubMed1979

Synergistic activity of co-trimazine and co-trimoxazole in the urine.

Co-trimazine (sulphadiazine, 410 mg + trimethoprim, 90 mg) is a new drug combination developed especially for use in the treatment of urinary tract infections. In cross-over experiments in volunteers receiving daily doses of co-trimazine (2 X 500 mg and 1 X 1000 mg), co-trimoxazole (2X960 mg), or nitrofurantoin (3X50 mg), the degree of antibacterial activity of co-trimazine in the urine was at least as high as that of co-trimoxazole and much higher and more consistent than that of nitrofurantoin. In further cross-over experiments in volunteers receiving co-trimazine 2X1000 mg or co-trimoxazole 2X960 mg for four days no or only slight activity was found in the urine against a sulphonamide-resistant Group D streptococcus, but distinct synergistic activity between the components was found against four Escherichia coli strains sensitive to trimethoprim and sensitive or resistant to sulphonamides. Against three of the latter strains the degree of activity in the urine was higher after co-trimazine than after cotrimoxazole. The synergistic action of trimethoprim and sulphonamide in the urine appeared greater with the former than with the latter combination.

Drug Combinations↗