Kg. Naber et al., PENETRATION OF CIPROFLOXACIN INTO PROSTATIC FLUID, EJACULATE AND SEMINAL FLUID IN VOLUNTEERS AFTER AN ORAL DOSE OF 750 MG, The Journal of urology, 150(5), 1993, pp. 1718-1721
To evaluate an effective dose for the treatment of bacterial prostatit
is the concentrations of ciprofloxacin were measured in prostatic flui
d, ejaculate and the cell-free seminal fluid of 15 healthy volunteers
who received an oral dose of 750 mg. ciprofloxacin while in a fasting
state. Venous blood samples were taken in all subjects at 1, 2, 3 and
4 hours. In 6 subjects blood samples were also taken after 8 and 12 ho
urs. Urine was collected in all subjects during 0 to 4 hours and in th
e 6 subjects also during 4 to 8 hours and 8 to 12 hours. Prostatic flu
id could be obtained in 10 subjects by prostatic massage 4 hours after
drug intake. So as not to contaminate the urethra with ciprofloxacin
the subjects were not allowed to void until 4 hours after drug intake.
Iopamidol (3.162 gm.), a renal contrast agent, was administered intra
venously concomitantly with oral ciprofloxacin intake. After 8 hours i
ohexol (3.235 gm.) was administered intravenously. These agents were m
easured in prostatic fluid, ejaculate and seminal fluid to assess the
contamination of those fluids by urine. All drug measurements were don
e by high pressure liquid chromatography. The median plasma concentrat
ions of ciprofloxacin were 2.1 mg./l. at 1 hour (maximum concentration
), 0.9 mg./l. at 4 hours and 0.2 mg./l. at 12 hours. The median concen
tration in prostatic fluid was 0.23 mg./l. with a fluid-to-plasma conc
entration ratio of 0.23. The median concentration in the ejaculate (se
minal fluid) after 4 hours was 7.4 mg./l. (6.6 mg./l.) and after 12 ho
urs it was 2.0 mg./l. (1.9 mg./l.) with corresponding ejaculate (semin
al fluid)-to-plasma concentration ratios of 8.4 (7.7) and 8.0 (6.6), r
espectively. Thus, ciprofloxacin is concentrated several-fold in ejacu
late and seminal fluid but not in prostatic fluid. According to the re
sults the concentrations of ciprofloxacin in prostatic fluid exceed th
e minimal inhibitory concentration-90% for Enterobacteriaceae but not
for Pseudomonas, enterococci and staphylococci, whereas the concentrat
ions in ejaculate and seminal fluid are sufficiently elevated to inclu
de the total spectrum of sensitive strains causing bacterial prostatis
.