Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Teicoplanin”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 19 recordsLinked to original sources
PubMed2006

Evaluation and comparison of a methylated teicoplanin aglycone to teicoplanin aglycone and natural teicoplanin chiral stationary phases.

HPLC enantiomeric separations of a wide variety of racemic analytes was evaluated using chiral stationary phases (CSPs) based on the macrocyclic glycopeptides teicoplanin (T), teicoplanin aglycone (TAG), and methylated teicoplanin aglycone (Me-TAG) in two different mobile phase modes, i.e., the RP mode and the polar organic (PO) mode. Comparison of the enantiomeric separations using Chirobiotic T, Chirobiotic TAG, and the methylated form of TAG were conducted in order to gain a better understanding of the roles of the polar functional groups on the CSP. Substantial effects due to the cleavage of saccharides and/or methylation on chiral separations were observed in both separation modes. Improved separation efficiencies for many acidic analytes were obtained by methylating the H-bonding groups of TAG. These groups were believed to be a contributing factor to band broadening on TAG due to their negative effect on mass transfer between the stationary phase and mobile phase. Ionic/dipolar interactions between the carboxylate group of the analytes and the amine groups on T, TAG, or Me-TAG are important for chiral discrimination. Therefore, analytes possessing a carboxyl group are good candidates for successful separations on these CSPs. Hydrophobic interactions are important for enantiomeric separations in the RP mode where the H-bonding interactions between analytes and the chiral selectors are relatively weak. Me-TAG offers higher hydrophobicity, which can accentuate the interactions of analytes with hydrophobic moieties, but these interactions are not necessarily stereoselective. In the PO mobile phase, electrostatic/dipolar interactions between polar functional groups are the dominating interactions in chiral recognition. Another important factor is steric fit, which could be changed with every modification of the T structure. Therefore, substantial changes of enantioseparations were obtained within this studied group of CSPs. The PO mode was shown to be the most powerful mobile phase mode for enantiomeric separations on T-based stationary phases, mainly due to the improved efficiency. Methylation of the TAG proved to be a very useful tool for investigating the chiral recognition mechanism for this group of chiral selectors.

Chromatography, High Pressure Liquid↗
PubMed1994

Randomized comparison trial of teicoplanin i.v., teicoplanin i.m., and cefazolin therapy for skin and soft tissue infections caused by gram-positive bacteria.

Teicoplanin, a glycopeptide antibiotic chemically related to the vancomycin-ristocetin group of antibiotics, has potent activity against aerobic and anaerobic gram-positive bacteria. In this study, we examined the efficacy and safety of teicoplanin for parenteral treatment of skin and soft tissue infections caused by gram-positive bacteria. Ninety-six hospitalized adults with moderate to severe skin and soft tissue infections were randomized to receive either teicoplanin intravenously (i.v.) once a day, teicoplanin intramuscularly (i.m.) once a day, or cefazolin i.v. every 8 hours. We evaluated patients' clinical and microbiologic status and assessed clinical and laboratory adverse events. Of 76 clinically assessable patients, 26 of 26 (100%) given teicoplanin i.v., 21 of 22 (95%) given teicoplanin i.m., and 26 of 28 (93%) given cefazolin showed improvement or cure. Of 60 microbiologically assessable patients, 22 of 22 (100%) given teicoplanin i.v., 16 of 18 (89%) given teicoplanin i.m, and 18 of 20 (90%) given cefazolin were cured. Of 96 patients assessable for adverse events, 7 of 34 (21%) given teicoplanin i.v., 4 of 31 (13%) give teicoplanin i.m., and 1 of 31 (3%) given cefazolin had adverse events. In this study, once daily teicoplanin appeared to be safe and effective therapy for skin and soft tissue infections.

Cefazolin↗
PubMed1998

Efficacy of teicoplanin and autoradiographic diffusion pattern of [14C]teicoplanin in experimental Staphylococcus aureus infection of joint prostheses.

Prosthesis infections are difficult to cure. Infection with methicillin-resistant staphylococci is becoming more common in patients with orthopedic implants. Using a recently developed model of methicillin-resistant Staphylococcus aureus (MRSA) infection of a knee prosthesis, we compared the efficacies of teicoplanin and vancomycin. [14C]teicoplanin diffusion in this model was also studied by autoradiography. A partial knee replacement was performed with a silicone implant fitting into the intramedullary canal of the tibia, and 10(7) CFU of MRSA was injected into the knee. Treatment with teicoplanin or vancomycin (20 or 60 mg/kg of body weight, respectively, given intramuscularly twice daily) was started 7 days after inoculation and was continued for 7 days. The teicoplanin and vancomycin MICs for MRSA were 1 microg/ml. Mean peak and trough levels in serum were 39.1 and 23.5 microg/ml, respectively, for teicoplanin and 34.4 and 18.5 microg/ml, respectively, for vancomycin. Fifteen days after the end of therapy, the animals were killed and their tibias were removed, pulverized, and quantitatively cultured. Teicoplanin and vancomycin significantly reduced (P < 0. 05) the bacterial density (2.7 +/- 1.3 and 3.3 +/- 1.6 log10 CFU/g of bone, respectively) compared to those for the controls (5.04 +/- 1.4 log10 CFU/g of bone). The bacterial covents of teicoplanin- and vancomycin-treated rabbits were comparable. The [14C]teicoplanin autoradiographic diffusion patterns in rabbits with prostheses, two of which were uninfected and two of which were infected, were studied 15 days after inoculation. Sixty minutes after the end of an infusion of 250 microCi of [14C]teicoplanin, autoradiography showed that in the infected animals, the highest levels of radioactivity were located around the prosthesis and in the periosteum, bone marrow, and trabecular bone. Radioactivity was less intense in epiphyseal disk cartilage, femoral cartilage, articular ligaments, and muscles and was weak in compact bone. A similar distribution pattern was seen in uninfected rabbits. Thus, teicoplanin may represent an effective alternative therapy for the treatment of these infections.

Animals↗
PubMedDate not supplied

Comparative in vitro activity of teicoplanin and vancomycin against United States teicoplanin clinical trial isolates of gram-positive cocci.

In this study, the in vitro activity of teicoplanin and vancomycin was directly compared against 503 Gram-positive cocci isolated during the U.S. teicoplanin clinical trials. Both antibiotics were equally active against oxacillin-sensitive Staphylococcus aureus, oxacillin-sensitive and oxacillin-resistant Staphylococcus epidermidis, and other coagulase-negative staphylococci, except Staphylococcus haemolyticus. Teicoplanin was fourfold more active than vancomycin against oxacillin-resistant S. aureus (MIC90, 0.5 vs. 2.0 micrograms/ml), whereas vancomycin was more active than teicoplanin (MIC90, 2.0 vs. 8.0 micrograms/ml) against oxacillin-resistant S. haemolyticus. Teicoplanin was two- to eightfold more active than vancomycin against the streptococci and enterococci tested.

Anti-Bacterial Agents↗
PubMed2004

Enantioseparation of dipeptides and tripeptides by micro-HPLC comparing teicoplanin and teicoplanin aglycone as chiral selectors.

Chiral separation of glycyl- and diastereomeric dipeptides and tripeptides was performed by micro-HPLC using macrocyclic antibiotics as chiral selectors. Teicoplanin was compared with teicoplanin aglycone (TAG) regarding selectivity, efficiency and separation time. The stationary phases are based on teicoplanin and TAG chemically bonded to 3.5 mum silica gel. The material was packed into 10 cm x 1 mm stainless steel microcolumns. Different mobile phases were checked using the reversed phase mode. Both teicoplanin and TAG were found to show good chiral separation ability for dipeptides. Glycyl-dipeptides were baseline resolved and most of the diastereomeric dipeptides and tripeptides were separated into their four isomers. In this study, teicoplanin was found to be advantageous compared to TAG regarding separation time, although TAG showed the higher resolution power. Baseline resolution for some glycyl-dipeptides was obtained within 3 min, diastereomeric dipeptides were resolved in 7 min. This method was also shown to be applicable for enantiomer purity control.

Chromatography, High Pressure Liquid↗
PubMed1991

In-vitro effects of teicoplanin, teicoplanin derivative MDL 62211 and vancomycin on human polymorphonuclear cell function.

The in-vitro effects on human neutrophil (PMN) functions of three structurally related glycopeptide antibiotics, vancomycin, teicoplanin and the teicoplanin derivative MDL 62211 were investigated. Teicoplanin and MDL 62211 significantly inhibited adherence, chemotaxis, phagocytosis and killing of Candida albicans by PMN's at a concentration of 500 mg/l, whereas PMN viability was only affected at drug concentrations of 2000 mg/l. Vancomycin interfered with PMN adherence and phagocytosis only at a concentration of 2000 mg/l without affecting PMN viability. Chemotaxis and killing of C. albicans were also not affected by this concentration. Teicoplanin and the teicoplanin-derivative MDL 62211 was found to have adverse effects on selected indices of PMN function in vitro only at concentrations higher than those employed in therapy, while vancomycin interfered only at very high concentrations.

Anti-Bacterial Agents↗
PubMed2006

In vivo survival of teicoplanin-resistant Staphylococcus aureus and fitness cost of teicoplanin resistance.

Glycopeptide resistance, in a set of in vitro step-selected teicoplanin-resistant mutants derived from susceptible Staphylococcus aureus SA113, was associated with slower growth, thickening of the bacterial cell wall, increased N-acetylglucosamine incorporation, and decreased hemolysis. Differential transcriptome analysis showed that as resistance increased, some virulence-associated genes became downregulated. In a mouse tissue cage infection model, an inoculum of 10(4) CFU of strain SA113 rapidly produced a high-bacterial-load infection, which triggered MIP-2 release, leukocyte infiltration, and reduced leukocyte viability. In contrast, with the same inoculum of the isogenic glycopeptide-resistant derivative NM67, CFU initially decreased, resulting in the elimination of the mutant in three out of seven cages. In the four cages in which NM67 survived, it partially regained wild-type characteristics, including thinning of the cell wall, reduced N-acetylglucosamine uptake, and increased hemolysis; however, the survivors also became teicoplanin hypersusceptible. The elimination of the teicoplanin-resistant mutants and selection of teicoplanin-hypersusceptible survivors in the tissue cages indicated that glycopeptide resistance imposes a fitness burden on S. aureus and is selected against in vivo, with restoration of fitness incurring the price of resistance loss.

Animals↗
PubMed1991

Activities of two new teicoplanin amide derivatives (MDL 62211 and MDL 62873) compared with activities of teicoplanin and vancomycin against 800 recent staphylococcal isolates from France and the United States.

MDL 62211 is the amide derivative of the teicoplanin complex and MDL 62873 is a more focused amide derivative of the teicoplanin A2-2 peak. Each investigational compound had nearly identical activity and was 2- to 16-fold more active than teicoplanin or vancomycin. The MDL 62873 MICs for 90% of the strains tested were as follows: Staphylococcus aureus, oxacillin susceptible, 0.12 micrograms/ml; S. aureus, oxacillin resistant, 0.25 micrograms/ml; coagulase-negative staphylococci (CNS), oxacillin susceptible, 0.25 micrograms/ml; and CNS, oxacillin resistant, 2 micrograms/ml. CNS isolates from France were generally more susceptible than those tested in the United States. Teicoplanin-resistant U.S. isolates were usually Staphylococcus haemolyticus (1.8% of all tested strains), for which MICs ranged from 32 to greater than 128 micrograms/ml. MDL 62873 was not active against the Bacteroides fragilis group but was generally effective against gram-positive anaerobic strains.

Anti-Bacterial Agents↗
PubMed1994

Teicoplanin plus pefloxacine versus teicoplanin plus netilmicin in empiric therapy of febrile patients with cancer and neutropenia. A randomized study of two once daily regimens in patients with previously inserted catheters.

In a comparative randomized trial, teicoplanin 5 mg/kg plus either netilmicin 5 mg/kg or pefloxacine 10 mg/kg was administered in a once daily empiric therapy to 40 cancer patients with fever and neutropenia after cytotoxic chemotherapy. Both regimens were analyzed with respect to the localisation of the underlying disease, catheter presence and agents isolated from blood culture. The cure and improvement rate were 80% (teicoplanin plus netilmicin) and 85% (teicoplanin plus pefloxacin), with no statistically significant difference between the groups. Teicoplanin with either an aminoglycoside or a quinolone administered once daily seems to be a suitable approach in empiric therapy for fever in neutropenia and may prevent catheter insertion in cancer patients.

Adult↗
PubMed1992

Teicoplanin in the treatment of bone and joint infections. Teicoplanin Bone and Joint Cooperative Study Group, USA.

Teicoplanin is a new glycopeptide antibiotic with activity against Gram-positive bacteria, including methicillin-resistant organisms. Teicoplanin is administered once daily, either intravenously or intramuscularly. Teicoplanin was given once daily, intravenously or intramuscularly, in the treatment of hospitalized or ambulatory patients with Gram-positive bone or joint infections. A total of 90/98 patients were evaluated for efficacy; 41 had acute osteomyelitis, 41 had chronic osteomyelitis, and 8 had septic arthritis. At the end of therapy, 37 acute osteomyelitis patients were cured/improved with a 90% cure rate at 6-month follow-up; 2 relapsed and 1 failed. At the end of therapy 30 chronic osteomyelitis patients were cured/improved with an 88% cure rate at 6-month follow-up; 2 relapsed and 1 failed. 100% of the septic arthritis patients were cured at the end of therapy and at 1-month follow-up. The most common bacterial isolates cultured from bone were S. aureus (39 isolates), S. epidermidis (11 isolates), other coagulase-negative staphylococci (20 isolates), enterococci (6 isolates), and other streptococcal species (20 isolates). The most common bacterial isolates cultured from joint fluid were S. aureus (6 isolates) and S. epidermidis (2 isolates). All patients tolerated the intramuscular or intravenous routes of administration well. Adverse reactions were mild and most cases did not require discontinuation of therapy. The majority of therapy was administered on an outpatient basis. Teicoplanin was safe, effective, convenient and relatively well tolerated in patients with acute or chronic osteomyelitis or septic arthritis.

Acute Disease↗
PubMed2005

Thermodynamic origin of the chiral recognition of tryptophan on teicoplanin and teicoplanin aglycone stationary phases.

The D-, L-tryptophan binding and the chiral recognition properties of the teicoplanin and teicoplanin aglycone (TAG) chiral stationary phase (CSPs) were compared at various column temperatures. The solute adsorption isotherms (bi-Langmuir model) were determined for both the two CSPs using the perturbation method. It was demonstrated that the sugar units were involved in the reduction of the apparent enantioselectivity through two phenomena: (i) the inhibition of some enantioselective contacts with low-affinity binding regions of the aglycone and (ii) a decrease in the stereoselective properties of the aglycone high-affinity binding pocket. The phenomenon (ii) was governed by both a decrease in the ratio of the enantiomer adsorption constant and a strong reduction of the site accessibility for D- and L-tryptophan. In addition, a temperature effect study was performed to investigate the chiral recognition mechanism at the aglycone high-affinity pocket. An enthalpy-entropy compensation analysis derived from the Grunwald model as well as the comparison with the literature data demonstrated that the enantioselective binding mode was dependent on an interface dehydration process. The change in the enantioselective process observed between the TAG and teicoplanin CSP was characterized by a difference of ca. 2-3 ordered water molecules released from the species interface.

Absorption↗
PubMedDate not supplied

A randomized clinical trial of ceftriaxone and teicoplanin versus ceftazidime and teicoplanin as antibiotic therapy in febrile neutropenic cancer patients and bone marrow transplant recipients.

A prospective, randomized clinical trial comparing combination therapy with ceftriaxone and teicoplanin versus ceftazidime and teicoplanin in the treatment of febrile episodes in neutropenic cancer patients and bone marrow transplant recipients was performed. One hundred and two patients were randomized, but two patients were considered unevaluable for efficacy, and three patients were withdrawn due to incorrect randomization. Of the remaining 97 patients, infection resolved without modification of therapy in 31/49 (63%) patients treated with ceftriaxone/teicoplanin versus 27/48 (56%) patients treated with ceftazidime/teicoplanin (P = 0.48). Of all 97 patients treated therapy was modified in 18/49 (36%) with ceftriaxone/teicoplanin and 21/48 (43%) with ceftazidime/teicoplanin. Nineteen patients treated with ceftriaxone/teicoplanin received netilmicin and 21 patients treated with ceftazidime/teicoplanin also received netilmicin according to the study design (escalation therapy). When netilmicin was added infection resolved in 78% of patients treated with ceftriaxone/teicoplanin versus 84% of those treated with ceftazidime/teicoplanin. It was concluded that combination therapy with ceftriaxone/teicoplanin is an alternative to combination therapy with ceftazidime/teicoplanin, and has the advantage of once daily administration.

Adolescent↗
PubMed2006

The discriminatory power of MALDI-TOF mass spectrometry to differentiate between isogenic teicoplanin-susceptible and teicoplanin-resistant strains of methicillin-resistant Staphylococcus aureus.

To explore the discriminatory power of matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS) for detecting subtle differences in isogenic isolates, we tested isogenic strains of Staphylococcus aureus differing in their expression of resistance to methicillin or teicoplanin. More important changes in MALDI-TOF MS spectra were found with strains differing in methicillin than in teicoplanin resistance. In comparison, very minor or no changes were recorded in pulsed-field gel electrophoresis profiles or peptidoglycan muropeptide digest patterns of these strains, respectively. MALDI-TOF MS might be useful to detect subtle strain-specific differences in ionizable components released from bacterial surfaces and not from their peptidoglycan network.

Anti-Bacterial Agents↗
PubMed1986

Teicoplanin, antibiotics from Actinoplanes teichomyceticus nov. sp. VII. Preparation and NMR characteristics of the aglycone of teicoplanin.

Several hydrolytic reactions that transform teicoplanin or its pseudo-aglycones into the aglycone with good yields are described. The most interesting approach is hydrolytic removal of the sugars in benzyl alcohol with the formation of the aglycone benzyl ester which is then submitted to hydrogenolysis. A detailed description of the 1H and 13C NMR spectra of the teicoplanin aglycone hydrochloride is presented. All the signals were attributed to the hydrogen and carbon atoms using homo and heteronuclear COSY. The relevant interactions through space between the hydrogen atoms were obtained by NOE. The structural aspects are discussed in terms of the well-known mechanism of action of the glycopeptide antibiotics.

Anti-Bacterial Agents↗
PubMed1987

Teicoplanin, antibiotics from Actinoplanes teichomyceticus nov. sp. VIII. Opening of the polypeptide chain of teicoplanin aglycone under hydrolytic conditions.

Hydrolysis of teicoplanin (a complex of five closely related factors plus one, more polar component) under selected conditions (acids in a biphasic hydroalcoholic medium) gives the single aglycone with good yields. When the reaction is carried out in homogeneous hydroalcoholic phase the removal of the sugars yields two new compounds. On the basis of fast atom bombardment mass spectra (FAB-MS), acid-base titration, IR, UV and 1H NMR analyses it has been demonstrated that these compounds are two diastereoisomers; they differ from the teicoplanin aglycone in having additional carboxyl and amino groups derived from the hydrolysis of an amide bond. Although the molecular shape of the new aglycones is greatly modified, they still maintain some antibacterial activity which might be correlated with residual binding ability towards the terminal D-alanyl-D-alanine residue of the cell-wall mucopeptides.

Actinomycetales↗
PubMed1989

Synthesis and biological activity of N63-carboxypeptides of teicoplanin and teicoplanin aglycone.

A series of peptide derivatives of teicoplanin A2 (CTA) and deglucoteicoplanin (TD) was prepared by condensation of the 63-carboxyl function with the alpha-amino group of selected amino acids and their derivatives. The modification of the ionic character of CTA and TD influenced their in vitro and in vivo antimicrobial properties to a different extent, depending on the structure of the amino acidic moiety at C-63. A certain effect on binding strength to Ac2-L-Lys-D-Ala-D-Ala, a synthetic model of the antibiotic's target peptide, was also observed.

Animals↗