Prostatic tissue and fluid concentrations of trimethoprim and sulfamethoxazole experimental and clinical studies

Madsen, Paul O.; Kjær, Torben; Baumueller, Axel

doi:10.1016/0090-4295(76)90339-3

Cited by 45 publications

(14 citation statements)

References 6 publications

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“…This could not be explained easily by the differences in their dissociation constants and their pH of the isoelectric points. Several reasons must be considered, including an active secretion mechanism [67]. In general, the concentrations in urine are much higher and the concentrations in prostatic fluid are well below the corresponding plasma concentrations.…”

Section: Discussionmentioning

confidence: 99%

“…Thus, a weak base, such as trimethoprim (with a pKa of 7.4), will be concentrated in an acid prostatic fluid as found in dogs [14], but not in an alkaline milieu (eg, seminal fluid). The pH of prostatic fluid in patients with chronic bacterial prostatitis often is alkaline, thus concentrations in prostatic secretion may be inadequate [15,16]. The FQs in clinical use, amphoteric or zwitterionic drugs, are neither pure acids nor bases, but have characteristics of both [17,18].…”

Section: Theoretical Considerationsmentioning

confidence: 99%

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Fluoroquinolone antimicrobial agents in the treatment of prostatitis and recurrent urinary tract infections in men

Wagenlehner

Naber

2005

Curr Infect Dis Rep

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Chronic bacterial prostatitis is the most frequent cause for recurrent urinary tract infection in young and middle-aged men. The selection of an appropriate antimicrobial agent that has optimal pharmacokinetics for urine and prostatic secretion and tissue is important in both entities. Fluoroquinolones possess several pharmacologic characteristics that favor them for treatment of urinary tract infection and prostatitis. The pharmacokinetics of fluoroquinolones and the theoretical background of drug penetration into the prostate are outlined. Analyzing the concentrations of various fluoroquinolones in urine, prostatic and seminal fluid, and in prostatic tissue, it becomes obvious that the fluoroquinolones differ in plasma concentrations and in their concentrations at these sites. Nevertheless, overall, the concentrations at the site of infection of most of the fluoroquinolones should be sufficient for the treatment of chronic bacterial prostatitis and vesiculitis and recurrent urinary tract infection in men caused by susceptible pathogens.

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Section: Discussionmentioning

confidence: 99%

Section: Theoretical Considerationsmentioning

confidence: 99%

Fluoroquinolone antimicrobial agents in the treatment of prostatitis and recurrent urinary tract infections in men

Wagenlehner

Naber

2005

Curr Infect Dis Rep

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“…In one study, the secretion ratio of trimethoprim to sulfamethoxazole was 7:1, while in another, the ratio was 2.5:1 [76,77]. Although Dabhoiwala et al [72] believe that sulfamethoxazole achieves sufficient concentrations in prostatic tissue to be synergistic with trimethoprim, it is not clear that this is true for prostatic secretion [74,75].…”

Section: Trimethoprim-sulfamethoxazolementioning

confidence: 99%

Penetration of Antimicrobial Agents into the Prostate

et al. 2003

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In the present review article, the penetration of antimicrobial agents into prostatic fluid and tissue was examined. Three major factors determining the diffusion and concentration of antimicrobial agents in prostatic fluid and tissue are the lipid solubility, dissociation constant (pKa) and protein binding. The normal pH of human prostatic fluid is 6.5–6.7, and it increases in chronic prostatitis, ranging from 7.0 to 8.3. A greater concentration of antimicrobial agents in the prostatic fluid occurs in the presence of a pH gradient across the membrane separating plasma from prostatic fluid. Of the available antimicrobial agents, β-lactam drugs have a low pKa and poor lipid solubility, and thus penetrate poorly into prostatic fluid, expect for some cephalosporins, which achieve greater than or equal to the inhibitory concentration. Good to excellent penetration into prostatic fluid and tissue has been demonstrated with many antimicrobial agents, including tobramycin, netilmicin, tetracyclines, macrolides, quinolones, sulfonamides and nitrofurantoin.

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“…This cannot easily be explained by the differences in their dissociation constants and the pH of their isoelectric points. Several reasons must be considered, including an active secretion mechanism [56]. In general, the concentrations in prostatic fluid are well below the corresponding plasma concentrations.…”

Section: Discussionmentioning

confidence: 99%

“…The pH of prostatic fluid in patients with CBP is also often alkaline, thus concentrations in prostatic secretion may be inadequate [12,13]. The fluoroquinolones in clinical use are neither pure acids nor bases, but have characteristics of both, i.e.…”

Section: Mycoplasma Hominismentioning

confidence: 99%