Penetration of Antimicrobial Agents into the Prostate

Abstract

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.

Antibiotic Resistance in Uropathogenic E. Coli Strains Isolated from Non-Hospitalized Patients in Pakistan

“…Furthermore, we found that up to 76.3% of the isolates showed resistance towards co-amoxiclav and that 42% isolates showed resistance to fluoroquinolones [12][13][14]. Fluoroquinolones are considered as first choice for the treatment of UTIs in men, mainly because it has advantages over co-amoxiclav, which are related to its pharmacokinetic properties [15,16]. However, observed higher percentages of resistances against both drugs indicated that they could render their efficacies as therapeutic agents, particularly in Indian sub-continent.…”

“…As an alternative choice, nitrofurantoin could be considered as a drug of choice, given the low level of resistance found against this antibiotic [17]. However, there is no data on the effectiveness of this drug in the treatment of male patients and pharmacokinetic properties of this antibiotic are not better than those of fluoroquinolones [16]. Prevalence of MDR strains of UPEC was investigated in this study and it appeared that 77.5% of all the screened isolates were resistant to three or more than three of the tested antibiotics.…”

Susceptibility to Alternative Oral Antimicrobial Agents in Relation to Sequence Type ST131 Status and Coresistance Phenotype among Recent Escherichia coli Isolates from U.S. Veterans

“…For organisms known to be ST131, the only conventional drugs with less than 25% resistance prevalence are ceftriaxone, imipenem, and nitrofurantoin (10), making oral doxycycline and minocycline potentially attractive alternative options. Furthermore, both doxycycline and minocycline are known to have excellent prostatic penetration, with concentrations as high as 40 to 100% and 60% of serum levels, respectively (16).…”

Fosfomycin for the Treatment of Prostate Infection

“…Major factors determining the penetration of antimicrobial agents into the prostatic tissue have been reported to include a high level of lipid solubility, low degree of ionization, high dissociation constant, low protein binding and small molecular size (2,6). FQs satisfy these conditions, and their use is recommended as optimal agents for the treatment of prostate infections (2).…”