In vitro activity of teichomycin compared with those of other antibiotics

One hundred clinical isolates of methicillin-resistant (Metr) Staphylococcus aureus from five different geographical origins were tested for their susceptibility to 12 non-li-lactam antibiotics by the broth microdilution technique recommended by the National Committee for Clinical Laboratory Standards.Coumermycin and rifampin showed the highest activity with of MIC90s of 0.032 jig/ml for each compound. No resistance was found to coumermycin, whereas a single Metr S. aureus strain was found to be resistant to rifampin. Ciprofloxacin, vancomycin, and teicoplanin were the next most active compounds with MIC90s of 0.25, 0.5, and 0.5 ,ug/ml, respectively. Norfloxacin was less active, with an MIC90 of 1.0 ,ug/ml. Amikacin was the most active aminoglycoside tested, whereas high levels of resistance were found to tobramycin and gentamicin. Doxycycline and chloramphenicol showed variable results. Geographical variations in results were seen with doxycycline, chloramphenicol, and aminoglycosides. Kill-curve studies showed that coumermycin, ciprofloxacin, teicoplanin, vancomycin, and rifampin were highly bactericidal; more than 90% of the inoculum was killed within 8 h.

“…Chin and Neu (6) also reported effective killing activity of S. aureus by ciprofloxacin at four times the MIC. Similarly, Neu and Labthavikul (16) …”

Section: Discussionmentioning

confidence: 99%

“…Coumermycin, ciprofloxacin, and norfloxacin inhibit DNA gyrase activity within bacterial cells (10,19 (16,17,20).…”

Section: Discussionmentioning

confidence: 99%

Comparison of the activities of coumermycin, ciprofloxacin, teicoplanin, and other non-beta-lactam antibiotics against clinical isolates of methicillin-resistant Staphylococcus aureus from various geographical locations

Aldridge¹,

Janney²,

Sanders³

1985

“…Moreover, new species which are resistant to several antibiotics (i.e., JK corynebacteria) are emerging (10,16,19). Teicoplanin is a glycopeptide antibiotic with an antibacterial spectrum similar to that of vancomycin which is active against multipleantibiotic-resistant, gram-positive bacteria (4,9,13,22). However, it has a longer elimination half-life, which allows once-a-day administration, and appears to be well tolerated (8,14,23).…”

mentioning

confidence: 99%

Teicoplanin in the treatment of gram-positive-bacterial endocarditis

Martino

Venditti

Micozzi

et al. 1989

Intravenous teicoplanin has been used to treat 23 cases of gram-positive-bacterial endocarditis, usually with 3 to 7 mg/kg every 12 h on the first day, followed by 3 to 7 mg/kg every 24 h. For some cases (staphylococcal and enterococcal endocarditis), the dosage was 8 to 14.4 mg/kg per day and/or other antibiotics were given. The mean duration was 48.2 days (range, 23 to 130 days). Of 23 patients, 21 (91.3%) had negative cultures or were cured. A total of 18 patients were treated with teicoplanin alone; of these, 4 had surgery, and all (except 2 who relapsed) were cured. Teicoplanin was combined with one or more antibiotics in five cases; in all cases appropriate cultures were negative, but three patients died during therapy or follow-up. Mild renal impairment was seen in two patients; both were receiving teicoplanin in combination with an aminoglycoside. We conclude that intravenous teicoplanin administered once a day at doses of 7 to 14 mg/kg per day is well tolerated, easy to administer, and may represent an efficacious therapy for gram-positive-bacterial endocarditis.Gram-positive microorganisms still are the most frequent cause of infective endocarditis (6, 24). Moreover, new species which are resistant to several antibiotics (i.e., JK corynebacteria) are emerging (10,16,19). Teicoplanin is a glycopeptide antibiotic with an antibacterial spectrum similar to that of vancomycin which is active against multipleantibiotic-resistant, gram-positive bacteria (4, 9, 13, 22). However, it has a longer elimination half-life, which allows once-a-day administration, and appears to be well tolerated (8,14,23). Although studies with animal models suggested good results with teicoplanin, alone or in combination with other antibiotics, for the treatment of infective endocarditis and other life-threatening infections (3,5,20), the results of recent clinical trials are somewhat conflicting (1,8,11,14,25). Moreover, only a few gram-positive-bacterial endocarditis cases were included in the above studies. The majority of these cases were caused by Staphylococcus species and were treated with a standard dose of 400 mg on the first day followed by 200 mg/day afterwards. Such a schedule of teicoplanin administration proved to be inadequate for the therapy of severe staphylococcal infections in a recent clinical trial (1). We report here our 3 years of experience with 23 cases of gram-positive-bacterial endocarditis, most of which were treated with doses of teicoplanin higher than those previously used. MATERIALS AND METHODSPatients. All subjects were inpatients in various divisions of the Policlinico Umberto I, University of Rome. They were initially considered eligible for the study if they had clinical syndromes consistent with gram-positive-bacterial endocarditis. Only those cases fitting recently recommended strict case definitions were included in the analysis of the results (15, 24). For almost all patients two-dimensional echocardiography was performed, and specific attention was paid not only to the valvular structures but...

“…It is active against aerobic and anaerobic gram-positive bacteria (4,8,12,15). Its effect on susceptible bacteria is bactericidal, and like vancomycin, it interferes with cell wall synthesis (18).…”

mentioning

confidence: 99%

Pharmacokinetics of teicoplanin upon multiple-dose intravenous administration of 3, 12, and 30 milligrams per kilogram of body weight to healthy male volunteers

Smithers¹,

Kulmala²,

Thompson³

et al. 1992

Teicoplanin pharmacokinetics were evaluated after multiple-dose intravenous administration to healthy male volunteers by using a randomized, double-blind, parallel design. Doses of 3, 12, or 30 mg of teicoplanin per kg of body weight were administered every 24 h for 14 days as 60-min constant-rate intravenous infusions. Blood and urine samples were collected over 21 days and analyzed by a microbiological assay. Twenty-three subjects were included in the pharmacokinetic analysis. The median pharmacokinetic parameters upon multiple-dose intravenous administration of 3, 12, and 30 mg/kg included steady-state volumes of distribution of 0.94, 0.77, and 0.68 liter/kg; total clearances of 11.9, 12.0, and 13.2 ml/h/kg; and terminal disposition half-lives of 143, 166, and 96 h, respectively. Renal clearance accounted for approximately 95% of total clearance. No dose-related differences existed for teicoplanin total or renal clearance. The steady-state volume of distribution decreased significantly with increasing doses. As a result of the decrease in the volume of distribution, the terminal disposition half-life at 30 mg/kg was significantly decreased. However, the decreases in the volume of distribution and terminal disposition half-life are of limited clinical importance, since steady-state trough concentrations in serum increase in proportion to dose. Combined results of all multiple-dose studies with similar durations of sample collection indicate no dose-related differences for any pharmacokinetic parameters from 3 to 12 mg/kg. As observed in the present study, no dose-related differences exist for teicoplanin total and renal clearances from 3 to 30 mg/kg. However, at 30 mg/kg, a significant decrease in the steady-state volume of distribution is observed. As a consequence of the reduction in the volume of distribution at 30 mg/kg with no change in clearance, the terminal disposition half-life is decreased.Teicoplanin is a new glycopeptide antibiotic, chemically related to vancomycin and ristocetin. It is active against aerobic and anaerobic gram-positive bacteria (4,8,12,15). Its effect on susceptible bacteria is bactericidal, and like vancomycin, it interferes with cell wall synthesis (18).In earlier studies, the pharmacokinetics of teicoplanin were determined on the basis of plasma concentration-time profiles obtained over 3 to 4 days (22, 24). A review of these studies has recently been published (16). In more recent studies, the duration of sample collection has been extended up to 3 weeks, resulting in a more complete characterization of the serum concentration-time profile (1,11,14,21). As a result of the increase in the duration of sample collection, teicoplanin total clearance was found to be slightly less and the volumes of distribution and terminal disposition half-life were found to be greater than previously reported. Results from these more recent studies indicate that the pharmacokinetics of teicoplanin upon multiple-dose intravenous administration are linear over the range of 3 to 12 mg/kg of body wei...