The New Macrolide Antibiotics: Azithromycin, Clarithromycin, Dirithromycin, and Roxithromycin

Bahal, Neeta; Nahata, Milap C.

doi:10.1177/106002809202600112

Cited by 145 publications

(74 citation statements)

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“…On the basis of data for adults, azithromycin has a greater distribution in tissues, a longer elimination half-life, and a lower incidence of adverse effects than erythromycin (1,3,6,9). These pharmacokinetic features allow once-daily dosing and a shorter duration of therapy.…”

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confidence: 99%

“…It is active in vitro against a variety of microorganisms, including Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae, Neisseria gonorrhoeae, Legionella pneumophila, Escherichia coli, Klebsiella pneumoniae, and Borrelia burgdorferi (1,4,8,10). Azithromycin has recently been approved by the U.S. Food and Drug Administration for use in adult patients but has not yet been approved for children.…”

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confidence: 99%

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Pharmacokinetics of azithromycin in pediatric patients with acute otitis media

Nahata

Korányi

Luke

et al. 1995

Antimicrob Agents Chemother

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The objective of our study was to characterize the pharmacokinetics of azithromycin after the oral administration of multiple doses in suspension to children with acute otitis media. Thirteen children (ranging in age from 7.5 months to 5 years) received a single oral dose of 10 mg of azithromycin per kg of body weight on day 1 followed by single daily doses of 5 mg/kg on days 2 to 5. Each child fasted overnight before receiving the final dose on day 5. Multiple blood samples were collected after the last dose. Concentrations of azithromycin in serum were measured by a specific high-performance liquid chromatography-mass spectrometry method. The means and standard deviations for the maximum concentration of azithromycin in serum, the time to maximum concentration of azithromycin in serum, the area under the concentration-time curve (from 0 to 24 h), and the elimination half-life were 224 ؎ 120 ng/ml, 1.8 ؎ 0.4 h, 1,841 ؎ 651 ng ⅐ h/ml, and 31.6 ؎ 6.6 h, respectively. Concentrations in serum (means ؎ standard deviations) at 0 h (predose) and at 24, 48, and 72 h after the final dose were 51 ؎ 26, 47 ؎ 21, 27 ؎ 17, and 17 ؎ 13 ng/ml, respectively. Thus, the once-daily administration of azithromycin resulted in sustained systemic exposure to the drug. The drug dosage regimen used in this study should lead to tissue drug concentrations exceeding the MICs for common pathogens.

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Pharmacokinetics of azithromycin in pediatric patients with acute otitis media

Nahata

Korányi

Luke

et al. 1995

Antimicrob Agents Chemother

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“…Specifically, the impact on Gardnerella vaginalis is predictably due to metronidazole [12] while that on Gram negative rods (predominantly aerobic) is attributable to azithromycin [13][14]. It is paradoxical that these changes did not translate to improved birth outcomes [11].…”

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Impact of interconception antibiotics on the endometrial microbial flora

Tita

Cliver

Goepfert

et al. 2007

American Journal of Obstetrics and Gynecology

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Objective-To evaluate the impact of an interconceptional antibiotic regimen on the endometrial microbial flora and histology.Study Design-Secondary analysis of a double-blind randomized placebo-controlled trial of prophylactic metronidazole + azithromycin given to 241 women (118 on antibiotics and 123 on placebo) with a prior preterm delivery to prevent recurrent preterm delivery. Endometrial cultures and histology were obtained at randomization and 2 weeks after treatment. The prevalence of either the new acquisition or the resolution of individual microbes, categories of microbes and plasma cell endometritis were compared using Chi square or Fisher exact tests.Results-Overall, antibiotics were associated with lower acquisition and higher resolution of microbes. Of women without Gardnerella vaginalis at baseline, 14% on antibiotics vs. 34% on placebo had positive endometrial culture for the organism after treatment (p<0.05), while of those with Gardnerella at baseline, 57% vs. 33% (p<0.05) had a negative follow-up culture. Other Gramnegative rods, especially aerobes in general also manifested similar patterns. The impact on anaerobes and plasma cell endometritis was not definitive but there was a trend toward the increased resolution of the former (77% vs. 55%) and reduced acquisition of the latter (28% vs. 50%). Conclusion-The antibiotic regimen prevented acquisition and promoted resolution, but not eradication, of Gram-negative rods such as Gardnerella vaginalis and the aerobic sub-category.

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“…We have previously reported on the activities of AZI and CILA in the beige mouse test system (5, 17) and have compared the in vivo activities of these two agents against eight MAC isolates (6). Comparative trials of AZI and CIA in combination with other agents in patients with disseminated MAC infections will be necessary to determine any clinically significant differences in their efficacies and tolerances in this patient population.One pharmacokinetic advantage of AZI and CLA in the treatment of disseminated MAC infection is the high concentration of drug achieved in tissues (2,14,21). AZI also has a long half-life in serum and tissues, making it potentially useful for intermittent administration (9, 10).…”

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“…One pharmacokinetic advantage of AZI and CLA in the treatment of disseminated MAC infection is the high concentration of drug achieved in tissues (2,14,21). AZI also has a long half-life in serum and tissues, making it potentially useful for intermittent administration (9, 10).…”

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Intermittent azithromycin for treatment of Mycobacterium avium infection in beige mice

Klemens

Cynamon

1994

Antimicrob Agents Chemother

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The activity of azithromycin (AZI) was evaluated in the beige mouse model of disseminated Mycobacterium avium infection. Mice were infected intravenously with approximately 107 viable M. avium ATCC 49601. AZI at 50, 100, or 200 mg/kg of body weight or clarithromycin (CLA) at 200 mg/kg was given by gavage 5 days per week for 4 weeks. Groups of treated mice were compared with untreated control animals. A dose-related reduction in cell counts in organs was observed with AZI treatment. AZI at 200 mg/kg was more active than CLA at 200 mg/kg against organisms in spleens. The activities of these two agents at 200 mg/kg were comparable against organisms' in lungs. In a second study, AZI at 200 mg/kg was given daily for 5 days; this was followed by intermittent AZI treatment for the next 3 weeks. The activities of AZI given on a three-times-and five-times-per-week basis in the continuation phase were comparable. AZI given on a once-weekly basis was less active. The regimen of AZI given in combination with rifapentine on a once-weekly basis for 8 weeks showed promising activity. Clinical evaluation of AZI and rifapentine will help to define the roles of these agents in the treatment of disseminated M. avium complex infection.Azithromycin (AZI) and clarithromycin (CLA) are promising new agents for the treatment of disseminated Mycobacterium avium complex (MAC) infection in individuals with AIDS (7,19,23). We have previously reported on the activities of AZI and CILA in the beige mouse test system (5, 17) and have compared the in vivo activities of these two agents against eight MAC isolates (6). Comparative trials of AZI and CIA in combination with other agents in patients with disseminated MAC infections will be necessary to determine any clinically significant differences in their efficacies and tolerances in this patient population.One pharmacokinetic advantage of AZI and CLA in the treatment of disseminated MAC infection is the high concentration of drug achieved in tissues (2,14,21). AZI also has a long half-life in serum and tissues, making it potentially useful for intermittent administration (9, 10).The purpose of the present study was to compare the activities of AZI and CIA over a longer treatment period than we used in our previous studies and to explore the activity of AZI admi'nistered on an intermittent basis against MAC in the beige mouse test system. The activity of AZI alone and in combination with rifapentine (RPT) against MAC was assessed. (5,6,17). The MICs of AZI and CLA were determined in modified Mueller-Hinton broth (pH 7.4) supplemented with 5% Middlebrook oleic acid-albumin-dextrosecatalase (OADC) enrichment (Difco Laboratories, Detroit, Mich.) (11,20). The MIC of RPT was determined in modified 7H10 broth (7H10 agar formulation with agar and malachite green omitted; pH 6.6) supplemented with 5% OADC enrichment (4). The MICs of AZI, CLA, and RPT (in micrograms per milliliter) for M. avium ATCC 49601 are 8, 4, and 0.125, respectively. A cell suspension with a predominantly (>95%) transparent coloni...

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The New Macrolide Antibiotics: Azithromycin, Clarithromycin, Dirithromycin, and Roxithromycin

Abstract: The new macrolide antibiotics appear to offer an improvement over erythromycin. Definitive conclusions about the role of these drugs should await completion of ongoing clinical studies.

Cited by 145 publications

References 46 publications

Pharmacokinetics of azithromycin in pediatric patients with acute otitis media

Pharmacokinetics of azithromycin in pediatric patients with acute otitis media

Impact of interconception antibiotics on the endometrial microbial flora

Intermittent azithromycin for treatment of Mycobacterium avium infection in beige mice

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