Drugs online research references
J Vet Pharmacol Ther. 2002 Apr;25(2):99-104.
Pharmacokinetics of azithromycin in foals after i.v. and oral dose and disposition into phagocytes.
Davis JL, Gardner SY, Jones SL, Schwabenton BA, Papich MG.
Department of Clinical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, North Carolina 27606, USA.
The properties of azithromycin suggest that it may be an alternative to erythromycin for treatment of Rhodococcus equi pneumonia in foals. To investigate this possibility, the disposition of azithromycin in plasma, polymorphonuclear leukocytes (PMN), and alveolar cells was examined after a single administration in foals. Azithromycin suspension was administered orally (p.o.) at a dose of 10 mg/kg to five healthy 2-3-month-old foals. Two weeks later, azithromycin for injection was administered by intravenous (i.v.) infusion at a dose of 5 mg/kg to the same foals. Plasma samples were collected after p.o. and i.v. administration. Peripheral blood PMN and bronchoalveolar lavage fluid and alveolar cells were collected after p.o. administration. Azithromycin concentrations were determined by reverse-phase high-performance liquid chromatography (HPLC) with coulometric electrochemical detection. Azithromycin p.o. absorption was variable with a mean systemic availability of 39% (+/-20%). The plasma half-life was 16 and 18.3 h after i.v. and p.o. administration, respectively. Azithromycin had a very large volume of distribution (V(d)) of 11.6 L/kg [V(d(ss))] and 12.4 L/kg [V(d(area))]. The large V(d) can be attributed to high tissue and intracellular concentrations, exhibited by the high concentration of azithromycin in PMN and alveolar cells. The PMN half-life was 49.2 h. Dosage of 10 mg/kg of azithromycin p.o. once daily for foals with R. equi pneumonia is recommended for further study.
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etsu.esu
Azithromycin is an important antibiotic for the treatment of several different Gram-positive and Gram-negative bacterial infections. Erythromycin and clarithromycin are less useful antibiotics against Gram-negative infections. This difference in inhibitory activity was explored by comparing the effects of azithromycin and erythromycin on cellular functions in Haemophilus influenzae cells. Effects of both antibiotics on translation, cell viability, and growth rates have been measured. An IC(50) of 0.4 microg/ml was found for the effects of azithromycin on each of these processes. For erythromycin, an IC(50) of 1.5 microg/ml was observed, indicating a fourfold lower sensitivity of the organisms to this compound. The features of a second target for macrolide antibiotic inhibition in H. influenzae cells have also been examined. Inhibition of the synthesis of the large 50S ribosomal subunit was measured. Subunit formation was prevented in a concentration dependent fashion, with azithromycin showing a ninefold greater effect on this process compared with erythromycin. Synthesis of the 30S ribosomal subunit was not effected. Pulse and chase labeling kinetics confirmed the slower synthesis rate of the 50S particle in the presence of each antibiotic. The results are discussed in terms of the stronger effect of azithromycin on ribosome biosynthesis in this organism.
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virginia.edu
Polymorphonuclear leukocytes (PMNL) concentrate, transport, and release certain antimicrobial agents as they move in a chemotactic gradient. Antipyretic agents are frequently used in febrile patients receiving antimicrobial agents. Thus, the influence of ibuprofen, acetaminophen, and acetylsalicylic acid on uptake, transport, and release of azithromycin and moxifloxacin was studied. Uptake of the antimicrobial agents by human PMNL and the effect of the antipyretics were quantitated by bioassay of released antimicrobial agent. Transport and release were determined in chemotactic plates overlaid with sentinel bacteria that could detect transported and released antimicrobial agent. None of the antipyretics altered PMNL directed or non-directed movement. Uptake of azithromycin was significantly inhibited by acetylsalicylic acid but not by the other antipyretics. All of the antipyretic agents studied at therapeutic levels inhibited transport and release of both azithromycin and moxifloxacin. Administration of any of these antipyretic agents with antimicrobial agents that are transported and released by PMNL could compromise the efficacy of therapy.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12001049&dopt=Abstract
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