Literature DB >> 8913468

Safety, toleration, and pharmacokinetics of intravenous azithromycin.

D R Luke1, G Foulds, S F Cohen, B Levy.   

Abstract

To date, the clinical pharmacology of large intravenous doses of azithromycin has not been described. In the present study, single 2-h intravenous infusions of 1, 2, and 4 g of azithromycin were administered to three parallel groups (in each group, six received active drug and two received placebo) of healthy male subjects. Toleration (assessed by scores of subject-administered visual analog scale tests spanning 0 [good] to 10 [poor]), safety, pharmacokinetics, and serum motilin levels were monitored for up to 240 h after the start of each intravenous infusion. Mean nausea scores of 0.0, 0.0, 1.0, and 0.5 and abdominal cramping scores of 0.0, 0.0, 0.4, and 0.4 for 12-h periods after doses of 0, 1, 2, and 4 g of azithromycin, respectively, suggested that azithromycin was well tolerated. Because of the standardized 1-mg/ml infusates, all subjects in the 4-g dosing group complained of an urgent need to urinate. There were no consistent trends in endogenous motilin levels throughout the study. The maximum concentration of azithromycin in serum (10 micrograms/ml after a 4-g dose) and the area under the concentration-time curve (82 micrograms.h/ml after a 4-g dose) were dose related. The mean pharmacokinetic parameters were an elimination half-life of 69 h, total systemic clearance of 10 ml/min/kg, and a volume of distribution at steady state of 33.3 liters/kg. The pharmacokinetic results suggest that the long half-life of azithromycin is due to extensive uptake and slow release of the drug from tissues rather than an inability to clear the drug. Single intravenous doses of up to 4 g of azithromycin in healthy subjects are generally well tolerated, and quantifiable concentrations may persist in serum for 10 days or more.

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Year:  1996        PMID: 8913468      PMCID: PMC163579     

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  17 in total

1.  An open study to compare the pharmacokinetics, safety and tolerability of a multiple-dose regimen of azithromycin in young and elderly volunteers.

Authors:  P Coates; R Daniel; A C Houston; J H Antrobus; T Taylor
Journal:  Eur J Clin Microbiol Infect Dis       Date:  1991-10       Impact factor: 3.267

2.  High-performance liquid chromatographic assay with electrochemical detection for azithromycin in serum and tissues.

Authors:  R M Shepard; G S Duthu; R A Ferraina; M A Mullins
Journal:  J Chromatogr       Date:  1991-04-19

3.  Erythromycin is a motilin receptor agonist.

Authors:  T Peeters; G Matthijs; I Depoortere; T Cachet; J Hoogmartens; G Vantrappen
Journal:  Am J Physiol       Date:  1989-09

4.  Fasting plasma motilin levels are related to the interdigestive motility complex.

Authors:  T L Peeters; G Vantrappen; J Janssens
Journal:  Gastroenterology       Date:  1980-10       Impact factor: 22.682

5.  The pharmacokinetics of azithromycin in human serum and tissues.

Authors:  G Foulds; R M Shepard; R B Johnson
Journal:  J Antimicrob Chemother       Date:  1990-01       Impact factor: 5.790

6.  In vitro activities of azithromycin (CP 62,993), clarithromycin (A-56268; TE-031), erythromycin, roxithromycin, and clindamycin.

Authors:  A L Barry; R N Jones; C Thornsberry
Journal:  Antimicrob Agents Chemother       Date:  1988-05       Impact factor: 5.191

7.  Erythromycin induces migrating motor complex in human gastrointestinal tract.

Authors:  T Tomomasa; T Kuroume; H Arai; K Wakabayashi; Z Itoh
Journal:  Dig Dis Sci       Date:  1986-02       Impact factor: 3.199

8.  Erythromycin mimics exogenous motilin in gastrointestinal contractile activity in the dog.

Authors:  Z Itoh; M Nakaya; T Suzuki; H Arai; K Wakabayashi
Journal:  Am J Physiol       Date:  1984-12

9.  Interpretative criteria for the agar diffusion susceptibility test with azithromycin.

Authors:  A L Barry; R N Jones
Journal:  J Antimicrob Chemother       Date:  1988-11       Impact factor: 5.790

10.  Release of motilin in man.

Authors:  P Mitznegg; S R Bloom; N Christofides; H Besterman; W Domschke; S Domschke; E Wünsch; L Demling
Journal:  Scand J Gastroenterol Suppl       Date:  1976
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  14 in total

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Authors:  Diana Amantea; Michelangelo Certo; Francesco Petrelli; Giacinto Bagetta
Journal:  Assay Drug Dev Technol       Date:  2016-07-08       Impact factor: 1.738

2.  Interspecies scaling for the prediction of drug clearance in children: application of maximum lifespan potential and an empirical correction factor.

Authors:  Iftekhar Mahmood
Journal:  Clin Pharmacokinet       Date:  2010-07       Impact factor: 6.447

3.  A randomized controlled comparison of azithromycin and ofloxacin for treatment of multidrug-resistant or nalidixic acid-resistant enteric fever.

Authors:  N T Chinh; C M Parry; N T Ly; H D Ha; M X Thong; T S Diep; J Wain; N J White; J J Farrar
Journal:  Antimicrob Agents Chemother       Date:  2000-07       Impact factor: 5.191

4.  Susceptibilities of neonatal respiratory isolates of Ureaplasma urealyticum to antimicrobial agents.

Authors:  A Matlow; C Th'ng; D Kovach; P Quinn; M Dunn; E Wang
Journal:  Antimicrob Agents Chemother       Date:  1998-05       Impact factor: 5.191

5.  Mechanistic study of the azithromycin dosage-form-dependent food effect.

Authors:  William Curatolo; George Foulds; Robert Labadie
Journal:  Pharm Res       Date:  2010-04-06       Impact factor: 4.200

Review 6.  Interdisciplinary science and the design of a single-dose antibiotic therapy.

Authors:  William Curatolo
Journal:  Pharm Res       Date:  2011-02-11       Impact factor: 4.200

7.  Effects of food on a gastrically degraded drug: azithromycin fast-dissolving gelatin capsules and HPMC capsules.

Authors:  William Curatolo; Ping Liu; Barbara A Johnson; Angela Hausberger; Ernest Quan; Thomas Vendola; Neha Vatsaraj; George Foulds; John Vincent; Richa Chandra
Journal:  Pharm Res       Date:  2011-02-18       Impact factor: 4.200

8.  Suppressive effect of azithromycin on Plasmodium berghei mosquito stage development and apicoplast replication.

Authors:  Shoichi Shimizu; Yoshio Osada; Tamotsu Kanazawa; Yoshiya Tanaka; Meiji Arai
Journal:  Malar J       Date:  2010-03-10       Impact factor: 2.979

9.  Steady-state plasma and bronchopulmonary concentrations of intravenous levofloxacin and azithromycin in healthy adults.

Authors:  Keith A Rodvold; Larry H Danziger; Mark H Gotfried
Journal:  Antimicrob Agents Chemother       Date:  2003-08       Impact factor: 5.191

10.  Azithromycin Dose To Maximize Efficacy and Suppress Acquired Drug Resistance in Pulmonary Mycobacterium avium Disease.

Authors:  Devyani Deshpande; Jotam G Pasipanodya; Tawanda Gumbo
Journal:  Antimicrob Agents Chemother       Date:  2016-03-25       Impact factor: 5.191

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