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Pharmacokinetic comparison of two models of endocarditis prophylaxis with amoxycillin

Paulsen, Otto; Höglund, P LU and Schalén, C LU (1989) In Scandinavian Journal of Infectious Diseases 21(6). p.73-669
Abstract

From studies on prophylaxis against experimental streptococcal endocarditis using amoxycillin in a single dose, it has been deduced that serum concentrations above 0.12 mg/l should be maintained for at least 10 h after antibiotic administration. Since concentrations above this level are reported to occur following an oral dose of 3 g of amoxycillin, this doses for prophylaxis has become widely accepted in USA and the UK, and presently also in Sweden. Nevertheless, in individuals who cannot tolerate a high single dose of amoxycillin, there is need for an alternative dosage regimen. In the present study, we have compared the pharmacokinetics in 12 healthy volunteers, of a single dose of 3 g of amoxycillin with those of 1 g as single dose... (More)

From studies on prophylaxis against experimental streptococcal endocarditis using amoxycillin in a single dose, it has been deduced that serum concentrations above 0.12 mg/l should be maintained for at least 10 h after antibiotic administration. Since concentrations above this level are reported to occur following an oral dose of 3 g of amoxycillin, this doses for prophylaxis has become widely accepted in USA and the UK, and presently also in Sweden. Nevertheless, in individuals who cannot tolerate a high single dose of amoxycillin, there is need for an alternative dosage regimen. In the present study, we have compared the pharmacokinetics in 12 healthy volunteers, of a single dose of 3 g of amoxycillin with those of 1 g as single dose or combined with 1 g of probenecid. The combination resulted in an AUC twice as large as that achieved after 1 g of amoxycillin, and was slightly, but not significantly, larger than that after 3 g. However, amoxycillin concentrations above 0.12 mg/l were sustained for almost 14 h with the combination as compared to 10.4 hours following 3 g of amoxycillin only (p less than 0.001). Thus, the combination should be a convenient alternative in patients unable to tolerate a higher oral dose of amoxycillin, and in situations when an antibacterial effect of longer duration is desired.

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published
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keywords
Adult, Amoxicillin, Dose-Response Relationship, Drug, Drug Combinations, Endocarditis, Bacterial, Female, Humans, Male, Middle Aged, Models, Biological, Probenecid, Streptococcal Infections, Clinical Trial, Comparative Study, Journal Article, Randomized Controlled Trial
in
Scandinavian Journal of Infectious Diseases
volume
21
issue
6
pages
73 - 669
publisher
Informa Healthcare
external identifiers
  • scopus:0024829919
ISSN
0036-5548
language
English
LU publication?
yes
id
7bb55898-a1d3-4631-9fd5-8f3e49fc4e48
date added to LUP
2017-09-14 23:55:10
date last changed
2017-09-18 16:28:27
@article{7bb55898-a1d3-4631-9fd5-8f3e49fc4e48,
  abstract     = {<p>From studies on prophylaxis against experimental streptococcal endocarditis using amoxycillin in a single dose, it has been deduced that serum concentrations above 0.12 mg/l should be maintained for at least 10 h after antibiotic administration. Since concentrations above this level are reported to occur following an oral dose of 3 g of amoxycillin, this doses for prophylaxis has become widely accepted in USA and the UK, and presently also in Sweden. Nevertheless, in individuals who cannot tolerate a high single dose of amoxycillin, there is need for an alternative dosage regimen. In the present study, we have compared the pharmacokinetics in 12 healthy volunteers, of a single dose of 3 g of amoxycillin with those of 1 g as single dose or combined with 1 g of probenecid. The combination resulted in an AUC twice as large as that achieved after 1 g of amoxycillin, and was slightly, but not significantly, larger than that after 3 g. However, amoxycillin concentrations above 0.12 mg/l were sustained for almost 14 h with the combination as compared to 10.4 hours following 3 g of amoxycillin only (p less than 0.001). Thus, the combination should be a convenient alternative in patients unable to tolerate a higher oral dose of amoxycillin, and in situations when an antibacterial effect of longer duration is desired.</p>},
  author       = {Paulsen, Otto and Höglund, P and Schalén, C},
  issn         = {0036-5548},
  keyword      = {Adult,Amoxicillin,Dose-Response Relationship, Drug,Drug Combinations,Endocarditis, Bacterial,Female,Humans,Male,Middle Aged,Models, Biological,Probenecid,Streptococcal Infections,Clinical Trial,Comparative Study,Journal Article,Randomized Controlled Trial},
  language     = {eng},
  number       = {6},
  pages        = {73--669},
  publisher    = {Informa Healthcare},
  series       = {Scandinavian Journal of Infectious Diseases},
  title        = {Pharmacokinetic comparison of two models of endocarditis prophylaxis with amoxycillin},
  volume       = {21},
  year         = {1989},
}