Dose dependence in human absorption of aminopenicillins. 1979

J Sjövall

The concentration of antibiotic in a focus of infection depends both on the peak serum concentration and on the area under the serum concentration time curve (AUC). A knowledge of the relationship between increased doses and the corresponding response in serum concentration would be relevant as a basis for determining an adequate clinical dosage. Dose-related changes in the two pharmacokinetic variables, peak serum concentration and AUC, after single doses of bacampicillin are compared with data on different aminopenicillins from other studies. With ampicillin there is a nonlinear relationship between both dose-peak and dose-AUC. The results indicate that the poor absorption of oral ampicillin can only be partially compensated for by increasing the oral dose. But with amoxycillin and the ampicillin esters the absorbed amount (AUC) is a linear function of the dose in the dosage range investigated. The increase in peak serum level with high doses of oral ampicillin is far less than proportional, while this tendency was less pronounced for amoxycillin and still less for pivampicillin, talampicillin and bacampicillin.

UI MeSH Term Description Entries
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
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.
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000658 Amoxicillin A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration. Hydroxyampicillin,Actimoxi,Amoxicillin Anhydrous,Amoxicillin Monopotassium Salt,Amoxicillin Monosodium Salt,Amoxicillin Sodium,Amoxicillin Trihydrate,Amoxicillin, (R*)-Isomer,Amoxicilline,Amoxil,Amoxycillin,BRL-2333,Clamoxyl,Clamoxyl G.A.,Clamoxyl Parenteral,Penamox,Polymox,Trimox,Wymox,BRL 2333,BRL2333
D000667 Ampicillin Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic. Penicillin, Aminobenzyl,Amcill,Aminobenzylpenicillin,Ampicillin Sodium,Ampicillin Trihydrate,Antibiotic KS-R1,Omnipen,Pentrexyl,Polycillin,Ukapen,Aminobenzyl Penicillin,Antibiotic KS R1,KS-R1, Antibiotic,Sodium, Ampicillin,Trihydrate, Ampicillin

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