The effect of hydroxy metabolites of clarithromycin to the pharmacokinetic parameters, and determination of hydroxy metabolites ratio of clarithromycin

• Published in: European journal of drug metabolism and pharmacokinetics Vol. 34; no. 1; pp. 27 - 30
• Main Authors: Unal, Durısehvar, Fenercıglu, Aysen, Ozbay, Latıf, Ozkirim, Banu, Erol, Dılek
• Format: Journal Article
• Language: English
• Published: Paris Springer-Verlag 01-01-2009; Médecine & hygiène
• Subjects: Adolescent; Adult; Anti-Bacterial Agents - pharmacokinetics; Anti-Bacterial Agents - pharmacology; Area Under Curve; Biological and medical sciences; Biomedical and Life Sciences; Biomedicine; Biotransformation; Clarithromycin - pharmacokinetics; Clarithromycin - pharmacology; Half-Life; Human Physiology; Humans; Hydroxylation; Male; Medical Biochemistry; Medical sciences; Middle Aged; Pharmaceutical Sciences/Technology; Pharmacology. Drug treatments; Pharmacology/Toxicology; Pharmacy; Stereoisomerism; Young Adult; pharmacokinetic parameters; hydroxy metabolites; Clarithromycin; Antibiotic; Metabolite; Protein synthesis inhibitor; Antibacterial agent; Pharmacokinetics; Macrolide; Quantitative analysis
• ISSN: 0378-7966; 2107-0180
• DOI: 10.1007/BF03191380

Summary
Clarithromycin is a broad-spectrum macrolide antibacterial agent which is effective both in vitro and in vivo against the major pathogens responsible for respiratory tract infections. Clarithromycin’s principal metabolite is 14-(
R
) hydroxyclarithromycin (14-OH-clarithromycin). The other metabolite, namely 14-(
S
) hydroxyclarithromycin is inactive. The purpose of this study was to show the hydroxylation of CLA at the 14 position to form the R and S epimers and to determine the metabolic ratio of 14ROHCLA/CLA and 14SOHCLA/CLA for understanding the metabolization. This study suggest that in healthy adults, the individual variations in therapeutic responses to clarithromycin can be assumed by taking the drug and its metabolites ratios. Clarithromycin and metabolites ratios increase during metabolization.