Steady-state serum and intrapulmonary pharmacokinetics and pharmacodynamics of tigecycline

Conte, John E.; Golden, Jeffrey A.; Kelly, Mary Grace; Zurlinden, Elisabeth

doi:10.1016/j.ijantimicag.2005.02.013

Cited by 157 publications

(138 citation statements)

References 26 publications

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“…In contrast, ICU-physicians have the daily challenge of treating patients with VAP due to MDR-bacteria. The high intrapulmonary concentration of tigecycline [5] as well as the prevalence in our study of VAP due to MDRAcinetobacter spp. (61%), ESBL-producing EB (12%), and MRSA (11%) -all of them susceptible to tigecycline (at least in vitro)-seem to explain the reasons why physicians choose the drug to treat these patients.…”

Section: Discussionmentioning

confidence: 52%

Indications of a new antibiotic in clinical practice: results of the tigecycline initial use registry

et al. 2008

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Tigecycline is the first of a new class of antibiotics named glycylcyclines and it was approved for the treatment of complicated intra-abdominal infections and complicated skin and skin structure infections. Notwithstanding this, tigecycline's pharmacological and microbiological profile which includes multidrug-resistant pathogens encourages physicians' use of the drug in other infections. We analyzed, during the first months after its launch, the tigecycline prescriptions for 113 patients in 12 institutions. Twenty-five patients (22%) received tigecycline for approved indications, and 88 (78%) for "off label" indications (56% with scientific support and 22% with limited or without any scientific support). The most frequent "off label" use was ventilator associated pneumonia (VAP) (63 patients). The etiology of infections was established in 105 patients (93%). MDR-Acinetobacter spp. was the microorganism most frequently isolated (50% of the cases). Overall, attending physicians reported clinical success in 86 of the 113 patients (76%). Our study shows that the "off label" use of tigecycline is frequent, especially in VAP. due to MDRAcinetobacter spp., where the therapeutic options are limited (eg: colistin). Physicians must evaluate the benefits/ risks of using this antibiotic for indications that lack rigorous scientific support.

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Section: Discussionmentioning

confidence: 52%

Indications of a new antibiotic in clinical practice: results of the tigecycline initial use registry

et al. 2008

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“…This makes the MPC approach likely to apply to many classes of antibiotics, including tigecycline. Pharmacokinetic measurements with tigecycline indicate that the maximum concentrations in serum and lung epithelial lining fluid of healthy subjects (N¼30) were 0.72 and 0.37 mg ml -1 , respectively, when tigecycline was administered as a 100 mg first dose followed by six 50 mg doses given every 12 h. 15 Sun et al 16 reported that the maximum concentrations of tigecycline in serum and skin blister fluid of healthy subjects (N¼10) were 0.82 and 0.27 mg ml -1 , respectively. Although MIC for tigecycline with A. baumannii is below the susceptibility breakpoint (p2 mg ml -1 ), the MPC is above the attainable surum, lung tissue and skin tissue levels.…”

mentioning

confidence: 99%

Mutant prevention concentration of tigecycline for carbapenem-susceptible and -resistant Acinetobacter baumannii

2009

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Acinetobacter baumannii has become a serious nosocomial pathogen, particularly with cases of ventilator-associated pneumonia and bacteraemia. 1 In recent years, many outbreaks of nosocomial infections caused by carbapenem-resistant A. baumannii have been reported. 2,3 These carbapenem-resistant isolates are often resistant to multiple agents, such as cephalosporins, fluoroquinolones, aminoglycosides, tetracyclines and sulbactam. 2,3 Carbapenems once had a crucial role in the management of serious nosocomial A. baumannii infections. Unfortunately, the prevalence of carbapenem-resistant isolates appears to be increasing. In China, the rate of carbapenem-resistance in A. baumannii isolates was 40-60% in 2005. 4 These features make A. baumannii infections very difficult to treat as options are limited. A new broad-spectrum glycylcycline, tigecycline, shows good in vitro activity against A. baumannii 5,6 and is now considered a good treatment option for multidrug-resistant A. baumannii infections. 7,8 However, tigecycline-resistant A. baumannii has been observed after tigecycline treatment of A. baumannii infections. 7-9 Whether tigecycline is particularly prone to emergence of resistance with A. baumannii is unknown.Mutant prevention concentration (MPC) and the mutant selection window theory has been proposed as new measures for propensity of an antimicrobial to develop resistance. 10 To assess the propensity for A. baumannii to develop resistance, we measured the MPC of tigecycline. Eighty A. baumannii sputum isolates were collected from three hospitals in Beijing. Fifty were carbapenem-resistant isolates (MICX16 mg ml -1 to either meropenem or imipenem); they were also resistant to broad-spectrum beta-lactams, aminoglycosides and fluoroquinolones. Thirty isolates were susceptible to meropenem, imipenem, aminoglycosides and fluoroquinolones. Staphylococcus aureus ATCC 29213 and Escherichia coli ATCC 25922 served as quality-control strains. Bacterial cultures were grown in MullerHinton broth or on Muller-Hinton agar at 37 1C. Stock solutions of tigecycline (5.12 mg ml -1 ) were prepared from i.v. injection powder (Wyeth Pharmaceutical, Philadelphia, PA, USA) in sterile water. MIC was determined according to Clinical and Laboratory Standards Institute using Muller-Hinton agar. As no interpretive criterion for tigecycline with A. baumannii has been established, Clinical and Laboratory Standards Institute interpretive criteria for Enterobacteriaceae were used for A. baumannii, as had been reported in previous literature (susceptible MIC p2 mg ml -1 ; intermediate MIC, 42 but o8 mg ml -1 ; resistant MIC, X8 mg ml -1 ). 7,8 For determination of the MPC, high-density cultures were prepared from overnight cultures grown in liquid medium followed by a 10-fold dilution and 4 h of incubation with shaking at 37 1C. Then, the suspension was centrifuged (4000 g for 10 min) and re-suspended in fresh Mueller-Hinton broth to yield a concentration of about 10 10 c.f.u. ml -1 . A series of agar plates containing known antibiotic...

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“…The available literature contains a description of TIG extraction with SPE method for both human (Conte et al 2005) and rat plasma (Munyeza et al 2016). However, in contrast to LLE extraction, SPE method is time-and labour-consuming, because it includes numerous steps needed to perform the entire extraction process.…”

Section: Discussionmentioning

confidence: 99%

“…There are only a few reports on determination of TIG; the validated LC-MS/MS assay was developed for determination of TIG in human plasma (Conte et al 2005, Rodvold et al 2006, Hoffmann et al 2007, Pai 2014, Xie et al 2014, bone (Ji et al 2007, Ji et al 2008, Bhattacharya et al 2014) and skin blister (Sun et al 2005). Most of the methods for determination of TIG in a biological matrix mentioned above lack sufficient information about the settings of a detector, therefore any attempt to their adaptation to animal experiments may cause difficulties and often require optimization followed by repeated validation.…”

Section: Introductionmentioning

confidence: 99%

Determination of tigecycline in turkey plasma by LC-MS/MS: validation and application in a pharmacokinetic study

Jasiecka-Mikołajczyk

Jaroszewski

2017

Polish Journal of Veterinary Sciences

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Tigecycline (TIG), a novel glycylcycline antibiotic, plays an important role in the management of complicated skin and intra-abdominal infections. The available data lack any description of a method for determination of TIG in avian plasma. In our study, a selective, accurate and reversed-phase high performance liquid chromatography-tandem mass spectrometry method was developed for the determination of TIG in turkey plasma. Sample preparation was based on protein precipitation and liquid-liquid extraction using 1,2-dichloroethane. Chromatographic separation of TIG and minocycline (internal standard, IS) was achieved on an Atlantis T3 column (150 mm x 3.0 mm, 3.0 μm) using gradient elution. The selected reaction monitoring transitions were performed at 293.60 m/z → 257.10 m/z for TIG and 458.00 m/z → 441.20 m/z for IS. The developed method was validated in terms of specificity, selectivity, linearity, lowest limit of quantification, limit of detection, precision, accuracy, matrix effect, carry-over effect, extraction recovery and stability. All parameters of the method submitted to validation met the acceptance criteria. The assay was linear over the concentration range of 0.01-100 μg/ml. This validated method was successfully applied to a TIG pharmacokinetic study in turkey after intravenous and oral administration at a dose of 10 mg/kg at various time-points.

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Steady-state serum and intrapulmonary pharmacokinetics and pharmacodynamics of tigecycline

Cited by 157 publications

References 26 publications

Indications of a new antibiotic in clinical practice: results of the tigecycline initial use registry

Indications of a new antibiotic in clinical practice: results of the tigecycline initial use registry

Mutant prevention concentration of tigecycline for carbapenem-susceptible and -resistant Acinetobacter baumannii

Determination of tigecycline in turkey plasma by LC-MS/MS: validation and application in a pharmacokinetic study

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