Pharmacokinetics of intravenous chloramphenicol sodium succinate in adult patients with normal renal and hepatic function

Burke, James T.; Wargin, William A.; Sherertz, Robert J.; Sanders, Karrie; Blum, Martin; Sarubbi, Felix A.

doi:10.1007/bf01062543

Cited by 33 publications

(5 citation statements)

References 11 publications

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“…when calculated. a References for pharmacokinetic and dosing information were as follows: tobramycin [8], chloramphenicol [9], rifampicin [10], penicillin G [11], vancomycin [12], ciprofloxacin [7], and other quinolones [13]. b The longest dosing interval was calculated by DI ¼ t 1=2 £ log 2 ðC max =MPCÞ, where t 1/2 is the half-life of the plasma drug concentration.…”

Section: Resultsmentioning

confidence: 99%

Restricting the Selection of Antibiotic‐Resistant Mutant Bacteria: Measurement and Potential Use of the Mutant Selection Window

Zhao¹,

Drlica²

2002

J INFECT DIS

197

145

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The selection of antibiotic-resistant mutant bacteria is proposed to occur in a drug concentration range (the mutant selection window) that extends from the minimum inhibitory concentration (MIC) of susceptible cells to the MIC of the least susceptible, single-step bacterial mutants (the mutant prevention concentration [MPC]). MPCs were estimated for tobramycin, chloramphenicol, rifampicin, penicillin, vancomycin, and several fluoroquinolones by use of Escherichia coli and Staphylococcus aureus. Comparisons among reported serum drug levels indicate that new fluoroquinolones are the least likely to enrich populations of resistant mutant bacteria during monotherapy. These data partly explain the selective enrichment of populations of resistant mutant bacteria in medical practice. The mutant selection window range (MPC:MIC) was narrowed for fluoroquinolones by structure modification, pointing to a new direction in antibiotic refinement. The mutant selection window and the MPC were determined for combinations of rifampicin and tobramycin, using S. aureus, as a guide for combination therapy with compounds that alone cannot block enrichment of mutant bacterial populations.

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Section: Resultsmentioning

confidence: 99%

Restricting the Selection of Antibiotic‐Resistant Mutant Bacteria: Measurement and Potential Use of the Mutant Selection Window

Zhao¹,

Drlica²

2002

J INFECT DIS

197

145

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“…Fifteen antimicrobial agents were chosen, based on their recommended use for therapy or prophylaxis of meningococcal infections. PK-PD parameters, protein binding, and the variability of these measurements, were obtained from the published literature for ampicillin, azithromycin, cefotaxime, ceftriaxone, chloramphenicol, ciprofloxacin, doxycycline, levofloxacin, meropenem, minocycline, penicillin G, rifampicin, sulphafurazole, tetracycline and trimethoprim-sulphamethoxazole (Table 1) [8][9][10][11][12][13][14][15][16][17][18][19][20][21]. Data concerning penetration into the cerebrospinal fluid (CSF) were also obtained from the literature [22][23][24].…”

Section: Antimicrobial Agentsmentioning

confidence: 99%

The contribution of pharmacokinetic–pharmacodynamic modelling with Monte Carlo simulation to the development of susceptibility breakpoints for Neisseria meningitidis

Burgess

Frei

Lewis

et al. 2007

Clinical Microbiology and Infection

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This study used pharmacokinetic-pharmacodynamic (PK-PD) modelling and MICs of 15 antimicrobial agents, derived from testing a large international culture collection, to assist in the development of interpretative criteria, i.e., breakpoints, for Neisseria meningitidis. PK parameters, protein binding, percentage penetration into cerebrospinal fluid (CSF), and the variability of these values, were extracted from the published literature for the 15 agents. PK-PD parameters have not been developed specifically for N. meningitidis in animal or human studies. Thus, it was necessary to invoke PK-PD targets from other organisms that cause infections at similar sites. The PK-PD targets utilised were: time above the MIC for at least 50% of the dosing interval for all beta-lactams, chloramphenicol, sulphafurazole and trimethoprim-sulphamethoxazole; an AUC/MIC ratio of >or=25 for the tetracyclines and macrolides; and an AUC/MIC ratio of >or=125 for the fluoroquinolones. A 10 000-subject Monte Carlo simulation was designed with the usual dosing regimens of each antimicrobial agent at MIC values of 0.03-64 mg/L in both serum and CSF. The PK-PD breakpoint was defined as the MIC at which the calculated target attainment was >or=95%. Using these assumptions, the proposed PK-PD breakpoints were: azithromycin, 0.125 mg/L; doxycycline, 0.25 mg/L; cefotaxime, ciprofloxacin and levofloxacin, 0.5 mg/L; penicillin G, meropenem, rifampicin, tetracycline and minocycline, 1 mg/L; chloramphenicol and sulphafurazole, 2 mg/L; and ampicillin, ceftriaxone and trimethoprim-sulphamethoxazole, 4 mg/L. Proposed PK-PD breakpoints applicable to CSF were: penicillin and cefotaxime, 0.06 mg/L; rifampicin, 0.125 mg/L; ceftriaxone, meropenem and trimethoprim-sulphamethoxazole, 0.25 mg/L; ampicillin, 0.5 mg/L; and chloramphenicol, 1 mg/L.

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“…The bioavailability of chloramphenicol following i.v. chloramphenicol SS administration is approximately 0.7 in humans (Glazko et al ., ; Burke et al ., ), 10–12 week old calves (Reiche et al ., ) and adolescent pigtail macaques (Koup et al ., ) as approximately 30% of the succinate ester is excreted unhydrolyzed in the urine. This limitation may have led to an overestimation of chloramphenicol clearance and volume of distribution in the current study, which could only be estimated as apparent values (CL/ F and V ss / F , respectively).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of chloramphenicol following administration of intravenous and subcutaneous chloramphenicol sodium succinate, and subcutaneous chloramphenicol, to koalas (Phascolarctos cinereus)

Black

McLachlan

Griffith

et al. 2012

Vet Pharm & Therapeutics

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Clinically normal koalas (n = 19) received a single dose of intravenous (i.v.) chloramphenicol sodium succinate (SS) (25 mg/kg; n = 6), subcutaneous (s.c.) chloramphenicol SS (60 mg/kg; n = 7) or s.c. chloramphenicol base (60 mg/kg; n = 6). Serial plasma samples were collected over 24-48 h, and chloramphenicol concentrations were determined using a validated high-performance liquid chromatography assay. The median (range) apparent clearance (CL/F) and elimination half-life (t(1/2)) of chloramphenicol after i.v. chloramphenicol SS administration were 0.52 (0.35-0.99) L/h/kg and 1.13 (0.76-1.40) h, respectively. Although the area under the concentration-time curve was comparable for the two s.c. formulations, the absorption rate-limited disposition of chloramphenicol base resulted in a lower median C(max) (2.52; range 0.75-6.80 μg/mL) and longer median tmax (8.00; range 4.00-12.00 h) than chloramphenicol SS (C(max) 20.37, range 13.88-25.15 μg/mL; t(max) 1.25, range 1.00-2.00 h). When these results were compared with susceptibility data for human Chlamydia isolates, the expected efficacy of the current chloramphenicol dosing regimen used in koalas to treat chlamydiosis remains uncertain and at odds with clinical observations.

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Pharmacokinetics of intravenous chloramphenicol sodium succinate in adult patients with normal renal and hepatic function

Cited by 33 publications

References 11 publications

Restricting the Selection of Antibiotic‐Resistant Mutant Bacteria: Measurement and Potential Use of the Mutant Selection Window

Restricting the Selection of Antibiotic‐Resistant Mutant Bacteria: Measurement and Potential Use of the Mutant Selection Window

The contribution of pharmacokinetic–pharmacodynamic modelling with Monte Carlo simulation to the development of susceptibility breakpoints for Neisseria meningitidis

Pharmacokinetics of chloramphenicol following administration of intravenous and subcutaneous chloramphenicol sodium succinate, and subcutaneous chloramphenicol, to koalas (Phascolarctos cinereus)

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