title: Clinical pharmacokinetics of etintidine.
abstract: The pharmacokinetics of etintidine (E), a potent H2 blocker, were studied in 12 normal, fasted subjects. The subjects received five ascending doses of E HCl in capsules at 72-h intervals. Blood and urine samples were collected and the plasma and urine levels of E were determined by HPLC. Following oral administration, plasma E levels showed double peaks in half of the subjects. Mean Cmax (0.42, 2.11, 3.82, 4.50, and 7.15 micrograms ml-1), AUC0-infinity (0.96, 4.94, 11.3, 17.5, and 24.5 h micrograms ml-1), and the amount of E excreted unchanged in 72 h (20, 54.8, 170, 320, and 371 mg) were determined. These parameters indicate the amount of E absorbed increased linearly with dose for each individual. Renal clearance was independent of the dose and the mean value (16.6 lh-1) was about twice that of the creatinine clearance (which did not significantly change as a result of E treatment), indicating that E is actively secreted into the renal tubules. As E was eliminated rapidly from the body (t1/2 less than 2 h), no substantial accumulation of E is expected after multiple dose treatment.
authors.affiliation: Research Laboratories, Ortho Pharmaceutical Corporation, Raritan, NJ 08869-0602.
authors.forename: S M
authors.initials: SM
authors.lastname: Huang
authors.forename: T B
authors.initials: TB
authors.lastname: Marriott
authors.forename: H S
authors.initials: HS
authors.lastname: Weintraub
authors.forename: J D
authors.initials: JD
authors.lastname: Arnold
authors.forename: J
authors.initials: J
authors.lastname: Boccagno
authors.forename: R
authors.initials: R
authors.lastname: Abels
authors.forename: W
authors.initials: W
authors.lastname: Harris
mesh_terms: D000284:Administration, Oral; D000328:Adult; D002851:Chromatography, High Pressure Liquid; D003404:Creatinine / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006634:Histamine H1 Antagonists / Q000493:pharmacokinetics*; D006801:Humans; D007093:Imidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male
chemical_list: D006634:Histamine H1 Antagonists; D007093:Imidazoles; C036616:etintidine; D003404:Creatinine