title: Pharmacokinetics and absolute rectal bioavailability of hydrocortisone acetate in distal colitis.
abstract: The hydrocortisone pharmacokinetic profiles of hydrocortisone acetate foam (Proctocort) administered rectally was assessed in healthy volunteers and patients with ulcerative colitis or X-irradiation colitis. Endogenous production of hydrocortisone was suppressed by dexamethasone. Comparison of these data with those obtained after intravenous administration enabled assessment of absolute bioavailability, which was 30.0 +/- 15.1% in healthy volunteers vs. 16.4 +/- 14.8% in patients (P = 0.09). Maximal concentrations of hydrocortisone were also decreased in patients, 277 +/- 215 nmol/L vs. 610 +/- 334 nmol/L (P = 0.03). There was a nonsignificant tendency to faster absorption of hydrocortisone in patients vs. healthy volunteers, as the times to peak concentration were, respectively, 2.5 +/- 1.2 h vs. 2.8 +/- 0.8 h (P = 0.64), and the mean absorption times were 1.96 +/- 1.45 h vs. 2.54 +/- 1.62 h (P = 0.46). Thus, rectal inflammation resulted in a lower absorption of hydrocortisone. In addition systemic plasma levels remained in the physiological range, so that only minor side effects are to be expected.
authors.affiliation: Département de Pharmacotoxicologie, Hôpital Avicenne, Bobigny, France.
authors.forename: O
authors.initials: O
authors.lastname: Petitjean
authors.forename: J L
authors.initials: JL
authors.lastname: Wendling
authors.forename: M
authors.initials: M
authors.lastname: Tod
authors.forename: K
authors.initials: K
authors.lastname: Louchahi
authors.forename: P
authors.initials: P
authors.lastname: Nicolas
authors.forename: G
authors.initials: G
authors.lastname: Perret
authors.forename: A
authors.initials: A
authors.lastname: Astier
mesh_terms: D000285:Administration, Rectal; D000328:Adult; D000368:Aged; D001682:Biological Availability; D003092:Colitis / Q000097:blood* / Q000188:drug therapy; D005260:Female; D006801:Humans; D006854:Hydrocortisone / Q000031:analogs & derivatives* / Q000097:blood* / Q000493:pharmacokinetics / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged
chemical_list: C021650:hydrocortisone acetate; D006854:Hydrocortisone