Pharmacokinetic comparison of two models of endocarditis prophylaxis with amoxycillin
(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.
(Less)
- author
- Paulsen, Otto ; Höglund, P LU and Schalén, C LU
- organization
- publishing date
- 1989
- type
- Contribution to journal
- publication status
- published
- subject
- 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
-
- pmid:2617209
- 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
- 2024-01-14 05:12:06
@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}}, 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}}, 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}}, }