Prostatic tissual distribution of alfuzosin in patients with benign prostatic hyperplasia following repeated oral administration.
OBJECTIVE
The blood and prostatic concentrations of alfuzosin were determined in patients with benign prostatic hyperplasia (BPH).


METHODS
12 patients scheduled for BPH surgery were treated with alfuzosin 5 mg twice daily prior to surgery in an open trial. Seven doses were given over a 4-day period. Blood samples were drawn before the first and the last intake (day 3). On day 4 (surgery day), a blood and prostate tissue sample were taken simultaneously 12 hours after the last drug intake.


RESULTS
Mean trough blood levels were 6.0+/-4.6 ng/ml and 5.8+/-3.7 ng/ml on day 3 and day 4, respectively, indicating a stable alfuzosin concentration. The mean prostate concentration on day 4 was 12.3+/-5.6 ng/g. Alfuzosin prostate and blood concentrations at 12 hours post dosing on day 4 were significantly correlated (r=0.804, p=0.0016); the prostate-blood ratio was 2.4+/-0.7.


CONCLUSIONS
Oral administration of alfuzosin leads to a high diffusion of the drug into the prostate of BPH patients.
Mottet
Nicolas
N
Urology Department, Central Hospital Gaston Doumergue, 5 Rue Hoche, 30029 Nimes Cedex 9, France.
Bressolle
Françoise
F
Delmas
Vincent
V
Robert
Michèle
M
Costa
Pierre
P
D000284:Administration, Oral; D000317:Adrenergic alpha-Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000368:Aged; D001682:Biological Availability; D001707:Biopsy, Needle; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005500:Follow-Up Studies; D006801:Humans; D008297:Male; D008875:Middle Aged; D011300:Preoperative Care; D011336:Probability; D011470:Prostatic Hyperplasia / Q000188:drug therapy* / Q000473:pathology / Q000601:surgery; D011799:Quinazolines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012720:Severity of Illness Index; D020728:Transurethral Resection of Prostate / Q000379:methods; D016896:Treatment Outcome
D000317:Adrenergic alpha-Antagonists; D011799:Quinazolines; C047638:alfuzosin