Dose-dependent absorption and elimination of cefadroxil in man. 1991

T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
Department of Pharmacology and Pharmaceutics, University of Valencia, Spain.

The pharmacokinetic behaviour of cefadroxil was dose-dependent in healthy male volunteers following the oral administration of single doses of 5, 15, and 30 mg.kg-1. As the dose of cefadroxil increased from 5 to 15 and 30 mg.kg-1, the peak plasma concentrations, normalized to 5 mg.kg-1, decreased significantly from 15.1 to 10.7 and 7.6 mg.l-1, while the corresponding normalized areas under the plasma concentration-time curves from 0 to 2 h decreased significantly from 1258 to 946 and 801 min.mg.l-1. When the same subjects were given 5 mg.kg-1 of cefadroxil together with 45 mg.kg-1 of cephalexin, the absorption of cefadroxil was slowed to a similar or greater extent than with the high dose of cefadroxil. Although the absorption rate decreased as the dose increased, the systemic availability of cefadroxil was essentially complete at all doses, as judged by the 24 h urinary recoveries of the antibiotic. Kinetic analysis of the plasma concentration-time curves gave the best fit with a zero-order followed by a first-order absorption process, consistent with saturable intestinal absorption of cefadroxil. The elimination rate of cefadroxil was directly related to dose and plasma concentrations, and the clearance at the dose of 5 mg.kg-1 was significantly increased by the simultaneous administration of high-dose cephalexin. The renal clearance of cefadroxil ranged from 98 ml.min.l-1 at total plasma cephalosporin (cefadroxil + cephalexin) concentrations less than 2.5 mg.l-1 to 156 mg.l-1 at concentrations greater than 40 mg.l-1.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D008297 Male Males
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D012016 Reference Values The range or frequency distribution of a measurement in a population (of organisms, organs or things) that has not been selected for the presence of disease or abnormality. Normal Range,Normal Values,Reference Ranges,Normal Ranges,Normal Value,Range, Normal,Range, Reference,Ranges, Normal,Ranges, Reference,Reference Range,Reference Value,Value, Normal,Value, Reference,Values, Normal,Values, Reference
D002434 Cefadroxil Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative. 4-Hydroxycephalexin,5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((amino(4-hydroxyphenyl)acetyl)amino)-3-methyl-8-oxo-, (6R-(6alpha,7beta(R*)))-,BL-S 578,BL-S578,Bidocef,Cefadroxil Anhydrous,Cefadroxil Monohydrate,Cephadroxyl,Duricef,S-578,S578,Ultracef,4 Hydroxycephalexin,BL S 578,BL S578,BLS 578,BLS578,S 578
D002506 Cephalexin A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms. 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((aminophenylacetyl)amino)-3-methyl-8-oxo-, (6R-(6alpha,7beta(R*)))-,Cefalexin,Cephalexin Dihydride,Cephalexin Hemihydrate,Cephalexin Hydrochloride,Cephalexin Monohydrate,Cephalexin Monohydrochloride,Cephalexin Monohydrochloride, Monohydrate,Cephalexin, (6R-(6alpha,7alpha(R*)))-Isomer,Cephalexin, (6R-(6alpha,7beta(S*)))-Isomer,Cephalexin, (6R-(6alpha,7beta))-Isomer,Cephalexin, Monosodium Salt,Cephalexin, Monosodium Salt, (6R-(6alpha,7beta))-Isomer,Ceporexine,Palitrex
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
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
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.

Related Publications

T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
March 1952, Pracovni lekarstvi,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
September 1953, Pracovni lekarstvi,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
March 1952, Pracovni lekarstvi,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
January 1993, European journal of clinical pharmacology,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
March 1949, The Journal of industrial hygiene and toxicology,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
July 1950, Archives of industrial hygiene and occupational medicine,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
January 1985, Drugs,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
October 1987, Zhonghua jie he he hu xi za zhi = Zhonghua jiehe he huxi zazhi = Chinese journal of tuberculosis and respiratory diseases,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
November 1963, El Dia medico,
T M Garrigues, and U Martin, and J E Peris-Ribera, and L F Prescott
January 1989, The American journal of clinical nutrition,
Copied contents to your clipboard!