Comparative pharmacokinetics of macrolides. 1987

O G Nilsen
Department of Pharmacology and Toxicology, Faculty of Medicine, University of Trondheim, Norway.

The search for erythromycin derivatives with improved antibacterial and/or pharmacokinetic properties, has led to the synthesis of several new agents. Roxithromycin, an ether oxime derivative of erythromycin, is one of the more promising. The main differences between erythromycin and roxithromycin are their kinetics, roxithromycin giving higher serum concentrations than erythromycin at equimolar oral doses. Its elimination half-life is also longer, about 12 h compared to 2-3 h for erythromycin. As their tissue distributions and antibiotic profiles are similar, roxithromycin can be administered in lower daily doses and at less frequent intervals. A suitable dosage regimen for roxithromycin seems to be 150 mg every 12 h. From a pharmacokinetic point of view, daily dosing with roxithromycin would be equivalent to the administration of erythromycin every 6 h.

UI MeSH Term Description Entries
D007933 Leucomycins An antibiotic complex produced by Streptomyces kitasatoensis. The complex consists of a mixture of at least eight biologically active components, A1 and A3 to A9. Leucomycins have both antibacterial and antimycoplasmal activities.
D008108 Liver Diseases, Alcoholic Liver diseases associated with ALCOHOLISM. It usually refers to the coexistence of two or more subentities, i.e., ALCOHOLIC FATTY LIVER; ALCOHOLIC HEPATITIS; and ALCOHOLIC CIRRHOSIS. Alcoholic Liver Diseases,Alcoholic Liver Disease,Liver Disease, Alcoholic
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004917 Erythromycin A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins. Erycette,Erymax,Erythromycin A,Erythromycin C,Erythromycin Lactate,Erythromycin Phosphate,Ilotycin,T-Stat,Lactate, Erythromycin,Phosphate, Erythromycin,T Stat,TStat
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000042 Absorption The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D000375 Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. Senescence,Aging, Biological,Biological Aging
D014018 Tissue Distribution Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios. Distribution, Tissue,Distributions, Tissue,Tissue Distributions

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