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Azithromycin--spectrum of activity, pharmacokinetics, and clinical applications.
Pharmacotherapy. 1992; 12(3):161-73.P

Abstract

Azithromycin is an azalide antimicrobial agent. Structurally related to the macrolide antibiotic erythromycin, its mechanism of activity (similar to erythromycin) is interference with bacterial protein synthesis by binding to the 50S component of the 70S ribosomal subunit. Although slightly less potent than erythromycin against gram-positive organisms, azithromycin demonstrates superior activity in vitro against a wide variety of gram-negative bacilli, including Haemophilus influenzae. Absorption is approximately 37% after a 500-mg oral dose. The large volume of distribution (23 L/kg) and low peak serum level (0.4 micrograms/ml) are consistent with data demonstrating extensive tissue distribution and intracellular accumulation. Metabolism is predominantly hepatic (to inactive metabolites), with biliary excretion a major pathway of elimination. Drug elimination is biphasic, with a terminal half-life of up to 5 days. Published trials have examined the efficacy and safety of azithromycin in the treatment of adults with upper and lower respiratory tract infections, skin and skin structure infections, streptococcal pharyngitis, and sexually transmitted diseases. Many used a 5-day course of 250 mg once daily, supplemented with a 250-mg dose on the first day of therapy. Selected trials in sexually transmitted diseases examined single 1-g doses. Promising results also were obtained with oral daily doses of 500 mg in patients with human immunoviral infection who also had Mycobacterium avium complex infection and in animals with toxoplasmosis. Adverse reactions are primarily gastrointestinal (nausea, diarrhea, abdominal pain), with minimal laboratory abnormalities reported. Gastrointestinal tolerance is better than that of erythromycin. Drug interactions have not been observed to date, although coadministration of azithromycin with a large meal may reduce absorption by up to 50%.

Authors+Show Affiliations

Division of Infectious Diseases, Duke University Medical Center, Durham, North Carolina 27710.No affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Review

Language

eng

PubMed ID

1319048

Citation

Drew, R H., and H A. Gallis. "Azithromycin--spectrum of Activity, Pharmacokinetics, and Clinical Applications." Pharmacotherapy, vol. 12, no. 3, 1992, pp. 161-73.
Drew RH, Gallis HA. Azithromycin--spectrum of activity, pharmacokinetics, and clinical applications. Pharmacotherapy. 1992;12(3):161-73.
Drew, R. H., & Gallis, H. A. (1992). Azithromycin--spectrum of activity, pharmacokinetics, and clinical applications. Pharmacotherapy, 12(3), 161-73.
Drew RH, Gallis HA. Azithromycin--spectrum of Activity, Pharmacokinetics, and Clinical Applications. Pharmacotherapy. 1992;12(3):161-73. PubMed PMID: 1319048.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Azithromycin--spectrum of activity, pharmacokinetics, and clinical applications. AU - Drew,R H, AU - Gallis,H A, PY - 1992/1/1/pubmed PY - 1992/1/1/medline PY - 1992/1/1/entrez SP - 161 EP - 73 JF - Pharmacotherapy JO - Pharmacotherapy VL - 12 IS - 3 N2 - Azithromycin is an azalide antimicrobial agent. Structurally related to the macrolide antibiotic erythromycin, its mechanism of activity (similar to erythromycin) is interference with bacterial protein synthesis by binding to the 50S component of the 70S ribosomal subunit. Although slightly less potent than erythromycin against gram-positive organisms, azithromycin demonstrates superior activity in vitro against a wide variety of gram-negative bacilli, including Haemophilus influenzae. Absorption is approximately 37% after a 500-mg oral dose. The large volume of distribution (23 L/kg) and low peak serum level (0.4 micrograms/ml) are consistent with data demonstrating extensive tissue distribution and intracellular accumulation. Metabolism is predominantly hepatic (to inactive metabolites), with biliary excretion a major pathway of elimination. Drug elimination is biphasic, with a terminal half-life of up to 5 days. Published trials have examined the efficacy and safety of azithromycin in the treatment of adults with upper and lower respiratory tract infections, skin and skin structure infections, streptococcal pharyngitis, and sexually transmitted diseases. Many used a 5-day course of 250 mg once daily, supplemented with a 250-mg dose on the first day of therapy. Selected trials in sexually transmitted diseases examined single 1-g doses. Promising results also were obtained with oral daily doses of 500 mg in patients with human immunoviral infection who also had Mycobacterium avium complex infection and in animals with toxoplasmosis. Adverse reactions are primarily gastrointestinal (nausea, diarrhea, abdominal pain), with minimal laboratory abnormalities reported. Gastrointestinal tolerance is better than that of erythromycin. Drug interactions have not been observed to date, although coadministration of azithromycin with a large meal may reduce absorption by up to 50%. SN - 0277-0008 UR - https://www.unboundmedicine.com/medline/citation/1319048/Azithromycin__spectrum_of_activity_pharmacokinetics_and_clinical_applications_ L2 - https://onlinelibrary.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0277-0008&date=1992&volume=12&issue=3&spage=161 DB - PRIME DP - Unbound Medicine ER -