Tigecycline Pharmacokinetics in Subjects With Various Degrees of Renal Function

Korth‐Bradley, Joan M.; Troy, Steven; Matschke, Kyle; Muralidharan, G.; Fruncillo, Richard J.; Speth, John; Raible, Donald G.

doi:10.1177/0091270011416938

Cited by 35 publications

(27 citation statements)

References 16 publications

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“…The primary parameters, V c and Cl were in agreement with those reported previously (Kuti, Dowzicky, & Nicolau, ; Muralidharan et al, ; Rubino et al, ; Van Wart et al, ). The plasma AUC 0–12 in our study (4713 h ng/mL) was also similar to previous reports (Korth‐Bradley et al, ; Muralidharan et al, ). The mean V csf (0.173 L) was similar to the physiological volume of the CSF (about 0.2–0.3 L) and was consistent with a previous study (Li et al, ).…”

Section: Resultssupporting

confidence: 93%

“…Symmetrical peak shape and suitable retention time were obtained by gradient elution conditions. To the best of our knowledge, trifluoroacetic acid was used in the majority of reported studies (Ji et al ., , ; Korth‐Bradley et al, ; Rodvold et al, ). Other researchers have used formic acid (Conte et al ., ; Ozcimen et al ., ) and 90% 10 m m ammonium formate (Chen et al, ).…”

Section: Resultsmentioning

confidence: 99%

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Development and validation of an LC‐MS/MS method for the determination of tigecycline in human plasma and cerebrospinal fluid and its application to a pharmacokinetic study

Mei

Luo

et al. 2016

Biomedical Chromatography

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Tigecycline (TGC) is an important antibiotic in treating various drug-resistant bacteria. The dosage regimen for cerebral intraventricular TGC is still unknown. The aim of the study was to develop and validate liquid chromatography-tandem mass spectrometry (LC-MS/MS) methods for the determination of TGC in human plasma and cerebrospinal fluid (CSF) to obtain an applicable regimen. The ion transitions under ESI positive model were performed at m/z 586.3 > 513.2 and m/z 595.3 > 514.3 for TGC and d9-TGC internal standard (IS). For plasma and CSF samples, the calibration curve of TGC was linear within the ranges 25-2000 and 250-100,000 ng/mL; the IS normalized matrix effect was within the ranges 96.46-101.06% and 101.13-103.58%, respectively, for all. TGC was stable under all tested conditions. The patient received 1 mg intraventricular and 49 mg intravenous administration of TGC. The AUC in plasma and CSF calculated according to our noncompartment model were 4713 and 23,0238 h ng/mL, respectively. Given our findings cerebral intraventricular TGC may be a choice for clinicians to treat drug-resistant Gram-negative bacterial-induced meningitis and the safety and efficacy of this administration route warrants further study.

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Section: Resultssupporting

confidence: 93%

Section: Resultsmentioning

confidence: 99%

Development and validation of an LC‐MS/MS method for the determination of tigecycline in human plasma and cerebrospinal fluid and its application to a pharmacokinetic study

Mei

Luo

et al. 2016

Biomedical Chromatography

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“…Recently published papers suggest that the doses should be increased to improve treatment efficacy in comparison to the currently recommended dose [23][24][25]. A relatively high degree of protein binding (71-78%) and a large volume of distribution (V ss > 900 L) theoretically decreases the elimination of this antibiotic through CRRT [26]. To date there have been no studies on the adsorption of tigecycline on the filter membranes used for CRRT.…”

Section: Discussionmentioning

confidence: 99%

Comparison of adsorption of selected antibiotics on the filters in continuous renal replacement therapy circuits: in vitro studies

et al. 2019

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The aim of this study was to assess the adsorption of selected antibiotics: vancomycin, gentamicin, ciprofloxacine and tigecycline in an experimental continuous veno-venous hemofiltration circuit with the use of both polyethyleneimine-treated polyacrylonitrile (PAN) and the polysulfone (PS) filter membranes. The crystalloid fluid dosed with one of antibiotic was pumped from a reservoir through a hemofiltration circuit (with PAN or PS membrane) and back to reservoir. All ultrafiltrate was also returned to the reservoir. During the procedures samples were collected from the post-hemofilter port at 5, 15, 30, 45, 60, 90, and 120 min. To determine spontaneous degradation of the antimicrobials, an additional bag with each study drug was prepared, which was not attached to the hemofiltration circuit. The samples from these bags were used as controls. In the case of vancomycin, gentamycin and tigecycline there was a statistically significant decrease in the drug concentration in the hemofiltration circuit in comparison to the control for PAN membrane (P < 0.05, P < 0.001, P < 0.001, respectively). In the case of ciprofloxacine adsorption was reversible and the drug concentrations increase to achieve the initial level for both membranes. Our studies indicated that a large portion of the administered dose of antibiotics may be adsorbed on a PAN membrane. In the case of gentamicin and tigecycline this amount is sufficiently big (over 90% of the administered dose) to be of clinical importance. In turn, adsorption on PS membranes is clearly lower (up to 10%) and may be clinically unimportant.

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“…Two studies (17)(18) found no significant change in the tigecycline pharmacokinetics in patients with impaired renal function, and tigecycline was not cleared by dialysis. There is no need to adjust the dose in patients with impaired renal function or in patients undergoing hemodialysis treatment (11).…”

Section: Figmentioning

confidence: 99%

Tigecycline Treatment Causes a Decrease in Fibrinogen Levels

Zhang

Zhou

2015

Antimicrob Agents Chemother

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The objective of this study was to assess the impact of tigecycline treatment on coagulation parameters, specifically fibrinogen, in patients with severe infections. We examined 20 cases of tigecycline-treated patients with severe infections, including hospitalacquired pneumonia, complicated intra-abdominal infections, complicated skin and soft tissue infections, and bloodstream infections. We monitored the relative markers of coagulation and renal and liver function before, during, and after treatment. Fibrinogen (FIB) levels decreased significantly after the use of tigecycline and normalized after the cessation of treatment. FIB levels significantly decreased in the patients treated with the recommended dose or a higher treatment dose. The FIB levels decreased more in the higher-treatment-dose group. There was no difference in the decrease in FIB levels or the FIB level recovery by age. Prothrombin time (PT), activated partial thromboplastin time (APTT), and thrombin time (TT) were prolonged after tigecycline use. The TT decreased after the cessation of treatment, and the PT and APTT also decreased but not to a significant level. There was no change in platelet, alanine aminotransferase (ALT), or creatinine (Cr) levels associated with treatment. The use of tigecycline was associated with decreased FIB levels, which returned to normal after the cessation of treatment. A highdose treatment group showed greater decreases in FIB levels than did patients treated with the recommended dose. The decline in FIB was not related to patient age. The use of tigecycline was associated with prolonged PT, APTT, and TT.T igecycline is a novel broad-spectrum intravenous antibiotic that inhibits bacterial protein synthesis. Tigecycline functions by binding to the 30S ribosomal subunit and preventing aminoacylated tRNA molecules from entering the ribosomal A site. Tigecycline contains a glycylamino group substituted for the 9-minocycline group, a substitution rarely seen in any natural or semisynthetic tetracycline compound, which gives tigecycline unique microbiological properties. Tigecycline is not affected by the two major bacterial tetracycline resistance mechanisms, efflux and ribosomal protection mechanisms (1). Tigecycline has a very broad spectrum of antibacterial activity, with Grampositive cocci (including methicillin-resistant Staphylococcus aureus, [MRSA] and vancomycin-resistant enterococci [VRE]) (2), Gram-negative bacilli (including Acinetobacter spp. and Stenotrophomonas maltophilia) (3), and anaerobic bacteria (4) having relatively high sensitivities. Kadoyama et al. (5) summarized a total of 248 tigecycline-related adverse reactions, the most common being nausea, vomiting, elevated levels of alanine aminotransferase, bilirubin, alkaline phosphatase, and aspartate aminotransferase, and hepatic dysfunction. In a number of studies, patients showed good tolerance of tigecycline, indicating that it is safe (6-7). However, there were two case reports that tigecycline can induce decreases in fibrinogen (FIB) levels (...

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Tigecycline Pharmacokinetics in Subjects With Various Degrees of Renal Function

Cited by 35 publications

References 16 publications

Development and validation of an LC‐MS/MS method for the determination of tigecycline in human plasma and cerebrospinal fluid and its application to a pharmacokinetic study

Development and validation of an LC‐MS/MS method for the determination of tigecycline in human plasma and cerebrospinal fluid and its application to a pharmacokinetic study

Comparison of adsorption of selected antibiotics on the filters in continuous renal replacement therapy circuits: in vitro studies

Tigecycline Treatment Causes a Decrease in Fibrinogen Levels

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