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Tissue-directed pharmacokinetics.
Am J Med. 1991 Sep 12; 91(3A):5S-11S.AJ

Abstract

Azalide antibiotics demonstrate pharmacokinetics distinct from all antibacterial agents in common use. Following oral absorption, conventional oral antibiotics diffuse through serum and interstitial compartments and are eliminated rapidly. A minimal to moderate degree of intracellular penetration may be observed. The pharmacokinetics of azithromycin, the first azalide, are characterized by a rapid and extensive movement of the drug from the serum into intracellular compartments. A dynamic equilibrium exists between the intracellular, interstitial, and serum compartments, with predominant flux into tissue sites. Azithromycin is concentrated to a high degree within phagocytes and transported by chemotactic mechanisms to the site of infection. High concentrations of azithromycin are found in pulmonary, genital, and lymphatic tissues. Azithromycin's serum levels decline in a polyphasic manner with a terminal half-life of approximately 60 hours. These kinetics allow azithromycin to be administered once daily. It is predicted that after drug administration for 5 days, therapeutic levels of azithromycin will be maintained at the tissue sites of infection for an additional 4-7 days. Consideration of the extravascular pharmacodynamics of azithromycin is necessary when making predictions regarding its therapeutic application.

Authors+Show Affiliations

State University of New York, Buffalo 14209.No affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

1656743

Citation

Schentag, J J., and C H. Ballow. "Tissue-directed Pharmacokinetics." The American Journal of Medicine, vol. 91, no. 3A, 1991, 5S-11S.
Schentag JJ, Ballow CH. Tissue-directed pharmacokinetics. Am J Med. 1991;91(3A):5S-11S.
Schentag, J. J., & Ballow, C. H. (1991). Tissue-directed pharmacokinetics. The American Journal of Medicine, 91(3A), 5S-11S.
Schentag JJ, Ballow CH. Tissue-directed Pharmacokinetics. Am J Med. 1991 Sep 12;91(3A):5S-11S. PubMed PMID: 1656743.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Tissue-directed pharmacokinetics. AU - Schentag,J J, AU - Ballow,C H, PY - 1991/9/12/pubmed PY - 1991/9/12/medline PY - 1991/9/12/entrez SP - 5S EP - 11S JF - The American journal of medicine JO - Am J Med VL - 91 IS - 3A N2 - Azalide antibiotics demonstrate pharmacokinetics distinct from all antibacterial agents in common use. Following oral absorption, conventional oral antibiotics diffuse through serum and interstitial compartments and are eliminated rapidly. A minimal to moderate degree of intracellular penetration may be observed. The pharmacokinetics of azithromycin, the first azalide, are characterized by a rapid and extensive movement of the drug from the serum into intracellular compartments. A dynamic equilibrium exists between the intracellular, interstitial, and serum compartments, with predominant flux into tissue sites. Azithromycin is concentrated to a high degree within phagocytes and transported by chemotactic mechanisms to the site of infection. High concentrations of azithromycin are found in pulmonary, genital, and lymphatic tissues. Azithromycin's serum levels decline in a polyphasic manner with a terminal half-life of approximately 60 hours. These kinetics allow azithromycin to be administered once daily. It is predicted that after drug administration for 5 days, therapeutic levels of azithromycin will be maintained at the tissue sites of infection for an additional 4-7 days. Consideration of the extravascular pharmacodynamics of azithromycin is necessary when making predictions regarding its therapeutic application. SN - 0002-9343 UR - https://www.unboundmedicine.com/medline/citation/1656743/Tissue_directed_pharmacokinetics_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0002-9343(91)90394-D DB - PRIME DP - Unbound Medicine ER -